+

WO2008133274A1 - 環式基で置換されたアミノジヒドロチアジン誘導体 - Google Patents

環式基で置換されたアミノジヒドロチアジン誘導体 Download PDF

Info

Publication number
WO2008133274A1
WO2008133274A1 PCT/JP2008/057847 JP2008057847W WO2008133274A1 WO 2008133274 A1 WO2008133274 A1 WO 2008133274A1 JP 2008057847 W JP2008057847 W JP 2008057847W WO 2008133274 A1 WO2008133274 A1 WO 2008133274A1
Authority
WO
WIPO (PCT)
Prior art keywords
optionally substituted
substituted lower
lower alkyl
cyclic groups
derivatives substituted
Prior art date
Application number
PCT/JP2008/057847
Other languages
English (en)
French (fr)
Inventor
Yuusuke Tamura
Shinji Suzuki
Yukio Tada
Shuji Yonezawa
Chiaki Fujikoshi
Sae Matsumoto
Yuuji Kooriyama
Tatsuhiko Ueno
Original Assignee
Shionogi & Co., Ltd.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority to US12/596,796 priority Critical patent/US8168630B2/en
Priority to BRPI0811034-4A2A priority patent/BRPI0811034A2/pt
Priority to ES08751985.6T priority patent/ES2476605T3/es
Priority to MX2009011498A priority patent/MX2009011498A/es
Priority to CN200880021335.4A priority patent/CN101687827B/zh
Priority to AU2008245082A priority patent/AU2008245082B8/en
Priority to RU2009143333/04A priority patent/RU2476430C2/ru
Priority to JP2009511888A priority patent/JP5383484B2/ja
Priority to CA002683887A priority patent/CA2683887A1/en
Priority to EP08751985.6A priority patent/EP2147914B1/en
Application filed by Shionogi & Co., Ltd. filed Critical Shionogi & Co., Ltd.
Publication of WO2008133274A1 publication Critical patent/WO2008133274A1/ja
Priority to US13/417,786 priority patent/US8541408B2/en
Priority to US13/887,745 priority patent/US8884062B2/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/02Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C215/04Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated
    • C07C215/20Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated the carbon skeleton being saturated and containing rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1617Organic compounds, e.g. phospholipids, fats
    • A61K9/1623Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D279/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/041,3-Thiazines; Hydrogenated 1,3-thiazines
    • C07D279/061,3-Thiazines; Hydrogenated 1,3-thiazines not condensed with other rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pyridine Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

アミロイドβタンパク質の産生、分泌または沈着により誘発される疾患の治療剤として有用な式(I)に示される化合物を提供する。 式(I): (式中、環Aは置換基を有していてもよい炭素環式基または置換基を有していてもよい複素環式基であり、 R1は置換基を有していてもよい低級アルキル、置換基を有していてもよい低級アルケニルまたは置換基を有していてもよい低級アルキニルであり、 R2aおよびR2bは各々独立して水素、置換基を有していてもよい低級アルキルまたは置換基を有していてもよいアシルであり、 R3a、R3b、R3cおよびR3dは各々独立して水素、ハロゲン、ヒドロキシ、置換基を有していてもよい低級アルキル等である) で示される化合物もしくはその製薬上許容される塩またはそれらの溶媒和物。
PCT/JP2008/057847 2007-04-24 2008-04-23 環式基で置換されたアミノジヒドロチアジン誘導体 WO2008133274A1 (ja)

Priority Applications (12)

Application Number Priority Date Filing Date Title
CA002683887A CA2683887A1 (en) 2007-04-24 2008-04-23 Aminodihydrothiazine derivatives substituted with a cyclic group having inhibitory activity against production of amyloid beta protein
ES08751985.6T ES2476605T3 (es) 2007-04-24 2008-04-23 Derivados de aminohidrotiazina sustituidos con grupos cíclicos
MX2009011498A MX2009011498A (es) 2007-04-24 2008-04-23 Derivados de aminodihidrotiazina sustituida con un grupo ciclico.
CN200880021335.4A CN101687827B (zh) 2007-04-24 2008-04-23 环状基团取代的氨基二氢噻嗪衍生物
AU2008245082A AU2008245082B8 (en) 2007-04-24 2008-04-23 Aminodihydrothiazine derivatives substituted with a cyclic group
US12/596,796 US8168630B2 (en) 2007-04-24 2008-04-23 Aminodihydrothiazine derivatives substituted with a cyclic group
JP2009511888A JP5383484B2 (ja) 2007-04-24 2008-04-23 環式基で置換されたアミノジヒドロチアジン誘導体
RU2009143333/04A RU2476430C2 (ru) 2007-04-24 2008-04-23 Производные аминодигидротиазина, замещенные циклической группой
EP08751985.6A EP2147914B1 (en) 2007-04-24 2008-04-23 Aminodihydrothiazine derivatives substituted with cyclic groups
BRPI0811034-4A2A BRPI0811034A2 (pt) 2007-04-24 2008-04-23 Derivados de aminodi-hidrotiazina substituídos com um grupo cíclico e seus usos e composições farmacêuticas
US13/417,786 US8541408B2 (en) 2007-04-24 2012-03-12 Aminodihydrothiazine derivatives substituted with a cyclic group
US13/887,745 US8884062B2 (en) 2007-04-24 2013-05-06 Aminodihydrothiazine derivatives substituted with a cyclic group

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
JP2007-114288 2007-04-24
JP2007114288 2007-04-24
JP2007-290589 2007-11-08
JP2007290589 2007-11-08

Related Child Applications (2)

Application Number Title Priority Date Filing Date
US12/596,796 A-371-Of-International US8168630B2 (en) 2007-04-24 2008-04-23 Aminodihydrothiazine derivatives substituted with a cyclic group
US13/417,786 Division US8541408B2 (en) 2007-04-24 2012-03-12 Aminodihydrothiazine derivatives substituted with a cyclic group

Publications (1)

Publication Number Publication Date
WO2008133274A1 true WO2008133274A1 (ja) 2008-11-06

Family

ID=39925723

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2008/057847 WO2008133274A1 (ja) 2007-04-24 2008-04-23 環式基で置換されたアミノジヒドロチアジン誘導体

Country Status (13)

Country Link
US (3) US8168630B2 (ja)
EP (2) EP2147914B1 (ja)
JP (2) JP5383484B2 (ja)
KR (1) KR20100017255A (ja)
CN (1) CN101687827B (ja)
AU (1) AU2008245082B8 (ja)
BR (1) BRPI0811034A2 (ja)
CA (1) CA2683887A1 (ja)
ES (1) ES2476605T3 (ja)
MX (1) MX2009011498A (ja)
RU (1) RU2476430C2 (ja)
TW (1) TW200902526A (ja)
WO (1) WO2008133274A1 (ja)

Cited By (106)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009091016A1 (ja) * 2008-01-18 2009-07-23 Eisai R & D Management Co., Ltd. 縮合アミノジヒドロチアジン誘導体
WO2009151098A1 (ja) * 2008-06-13 2009-12-17 塩野義製薬株式会社 βセクレターゼ阻害作用を有する含硫黄複素環誘導体
US7648983B2 (en) 2008-05-02 2010-01-19 Eli Lilly And Company BACE inhibitors
WO2010038686A1 (ja) 2008-09-30 2010-04-08 エーザイ・アール・アンド・ディー・マネジメント株式会社 新規な縮合アミノジヒドロチアジン誘導体
WO2010047372A1 (ja) * 2008-10-22 2010-04-29 塩野義製薬株式会社 Bace1阻害活性を有する2-アミノピリミジン-4-オンおよび2-アミノピリジン誘導体
US20100168094A1 (en) * 2008-12-30 2010-07-01 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
WO2010113848A1 (ja) 2009-03-31 2010-10-07 塩野義製薬株式会社 Bace1阻害作用を有するイソチオウレア誘導体またはイソウレア誘導体
US7868000B2 (en) 2005-06-14 2011-01-11 Schering Corporation Aspartyl protease inhibitors
WO2011005738A1 (en) 2009-07-09 2011-01-13 Eli Lilly And Company Bace inhibitors
WO2011029803A1 (en) * 2009-09-11 2011-03-17 F. Hoffmann-La Roche Ag 2 -aminodihydro [1, 3] thiazines as bace 2 inhibitors for the treatment of diabetes
WO2011048525A1 (en) * 2009-10-20 2011-04-28 Pfizer Inc. Novel heteroaryl imidazoles and heteroaryl triazoles as gamma-secretase modulators
WO2011058763A1 (ja) 2009-11-13 2011-05-19 塩野義製薬株式会社 アミノリンカーを有するアミノチアジンまたはアミノオキサジン誘導体
WO2011071109A1 (ja) 2009-12-11 2011-06-16 塩野義製薬株式会社 アミノ基を有する縮合ヘテロ環化合物
WO2011070781A1 (ja) 2009-12-09 2011-06-16 塩野義製薬株式会社 置換アミノチアジン誘導体
WO2011069934A1 (en) 2009-12-11 2011-06-16 F. Hoffmann-La Roche Ag 2-amino-5, 5-difluoro-5, 6-dihydro-4h-oxazines as bace 1 and/or bace 2 inhibitors
WO2011071135A1 (ja) 2009-12-11 2011-06-16 塩野義製薬株式会社 オキサジン誘導体
WO2011071057A1 (ja) * 2009-12-09 2011-06-16 塩野義製薬株式会社 含硫黄複素環誘導体を含有するアルツハイマー症の治療用または予防用医薬組成物
WO2011077726A1 (ja) 2009-12-24 2011-06-30 塩野義製薬株式会社 4-アミノ-1,3-チアジンまたはオキサジン誘導体
US7973067B2 (en) 2003-12-15 2011-07-05 Schering Corporation Heterocyclic aspartyl protease inhibitors
WO2011115928A1 (en) 2010-03-15 2011-09-22 Amgen Inc. Amino -dihydrooxazine and amino - dihydrothiazine spiro compounds as beta - secretase modulators and their medical use
WO2011115938A1 (en) 2010-03-15 2011-09-22 Amgen Inc. Spiro-tetracyclic ring compounds as beta - secretase modulators
EP2411001A1 (en) * 2009-03-23 2012-02-01 Merck Sharp & Dohme Corp. P2x3, receptor antagonists for treatment of pain
WO2012019056A1 (en) 2010-08-05 2012-02-09 Amgen Inc. Amino-iso-indole, amino-aza-iso-indole, amino-dihydroisoquinoline and amino-benzoxazine compounds as beta-secretase modulators and methods of use
US8168630B2 (en) 2007-04-24 2012-05-01 Shionogi & Co., Ltd. Aminodihydrothiazine derivatives substituted with a cyclic group
US8168641B2 (en) 2006-06-12 2012-05-01 Schering Corporation Aspartyl protease inhibitors
WO2012057247A1 (ja) 2010-10-29 2012-05-03 塩野義製薬株式会社 縮合アミノジヒドロピリミジン誘導体
WO2012057248A1 (ja) 2010-10-29 2012-05-03 塩野義製薬株式会社 ナフチリジン誘導体
US8173642B2 (en) 2005-10-25 2012-05-08 Shionogi & Co., Ltd. Aminodihydrothiazine derivatives
US8183252B2 (en) 2003-12-15 2012-05-22 Schering Corporation Heterocyclic aspartyl protease inhibitors
WO2012071279A1 (en) 2010-11-23 2012-05-31 Amgen Inc. Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use
US8207164B2 (en) 2009-07-24 2012-06-26 Novartis Ag Oxazine derivatives and their use in the treatment of neurological disorders
WO2012093148A1 (en) 2011-01-06 2012-07-12 Eisai R&D Management Co., Ltd Fused aminodihydrothiazine derivatives
WO2012109165A1 (en) 2011-02-07 2012-08-16 Amgen Inc. 5-amino-oxazepine and 5-amino-thiazepane compounds as beta-secretase antagonists and methods of use
WO2012112462A1 (en) 2011-02-15 2012-08-23 Amgen Inc. Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators and methods of use
CN102652129A (zh) * 2009-12-10 2012-08-29 霍夫曼-拉罗奇有限公司 氨基噁嗪衍生物
WO2012147763A1 (ja) 2011-04-26 2012-11-01 塩野義製薬株式会社 オキサジン誘導体およびそれを含有するbace1阻害剤
WO2012147762A1 (ja) 2011-04-26 2012-11-01 塩野義製薬株式会社 ピリジン誘導体およびそれを含有するbace1阻害剤
US8338407B2 (en) 2011-01-21 2012-12-25 Eisai R&D Management Co., Ltd. Fused aminodihydrothiazine derivatives
WO2013044092A1 (en) 2011-09-21 2013-03-28 Amgen Inc. Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
US8426584B2 (en) 2011-01-21 2013-04-23 Eisai R&D Management Co., Ltd. Methods and compounds useful in the synthesis of fused aminodihydrothiazine derivatives
US8450331B2 (en) 2008-04-22 2013-05-28 Merck Sharp & Dohme Corp. Thiophenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use
US8450308B2 (en) 2008-08-19 2013-05-28 Vitae Pharmaceuticals, Inc. Inhibitors of beta-secretase
US8461160B2 (en) 2009-05-08 2013-06-11 Hoffmann-La Roche, Inc. Dihydropyrimidinones
US8501733B2 (en) 2008-07-28 2013-08-06 Eisai R&D Management Co., Ltd. Spiroaminodihydrothiazine derivatives
US8552197B2 (en) 2009-11-12 2013-10-08 Ranbaxy Laboratories Limited Sorafenib ethylsulfonate salt, process for preparation and use
US8557826B2 (en) 2009-10-08 2013-10-15 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions, and their use
US8563543B2 (en) 2009-10-08 2013-10-22 Merck Sharp & Dohme Corp. Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
US8569310B2 (en) 2009-10-08 2013-10-29 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions and their use
JP2014500293A (ja) * 2010-12-22 2014-01-09 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ ベータ−セクレターゼ(BACE)の阻害剤として有用な5,6−ジヒドロ−イミダゾ[1,2−a]ピラジン−8−イルアミン誘導体
US8633212B2 (en) 2009-03-13 2014-01-21 Vitae Pharmaceuticals, Inc. Inhibitors of beta-secretase
US8637508B2 (en) 2011-01-13 2014-01-28 Novartis Ag Heterocyclic derivatives and their use in the treatment of neurological disorders
US8653067B2 (en) 2007-04-24 2014-02-18 Shionogi & Co., Ltd. Pharmaceutical composition for treating Alzheimer's disease
CN103608344A (zh) * 2011-06-07 2014-02-26 霍夫曼-拉罗奇有限公司 [1,3]噁嗪类
CN103717592A (zh) * 2011-06-07 2014-04-09 霍夫曼-拉罗奇有限公司 作为bace1和/或bace2抑制剂的卤代-烷基-1,3噁嗪类
WO2014059185A1 (en) 2012-10-12 2014-04-17 Amgen Inc. Amino - dihydrothiazine and amino - dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use
JP2014510769A (ja) * 2011-04-11 2014-05-01 エフ.ホフマン−ラ ロシュ アーゲー Bace1及び/又はbace2阻害剤としての1,3−オキサジン
US8722708B2 (en) 2005-06-14 2014-05-13 Merck Sharp & Dohme Inc. Substituted isoindolines as aspartyl protease inhibitors
US8729071B2 (en) 2009-10-08 2014-05-20 Merck Sharp & Dohme Corp. Iminothiadiazine dioxide compounds as BACE inhibitors, compositions and their use
WO2014078314A1 (en) 2012-11-15 2014-05-22 Amgen Inc. Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
JP2014515001A (ja) * 2011-04-20 2014-06-26 塩野義製薬株式会社 Trpv4阻害活性を有する芳香族複素環誘導体
JP2014527074A (ja) * 2011-09-12 2014-10-09 エフ.ホフマン−ラ ロシュ アーゲー N−(5−シクロアルキル−又は5−ヘテロシクリル)−ピリジン−3−イルカルボキサミド
US8889703B2 (en) 2010-02-24 2014-11-18 Vitae Pharmaceuticals, Inc. Inhibitors of beta-secretase
US8981112B2 (en) 2012-03-05 2015-03-17 Vitae Pharmaceuticals, Inc. Inhibitors of β-secretase
US9018391B2 (en) 2012-08-27 2015-04-28 Boehringer Ingelheim International Gmbh Inhibitors of beta-secretase
JP2015514073A (ja) * 2012-03-20 2015-05-18 エラン ファーマシューティカルズ, リミテッド・ライアビリティ・カンパニー スピロ環式ジヒドロ−チアジンおよびジヒドロ−オキサジンbace阻害剤、ならびにその組成物および使用
JP2015517981A (ja) * 2012-02-29 2015-06-25 バルーク エス.ブルームバーグ インスティテュート B型肝炎ウイルス共有結合閉環状dna形成の阻害剤およびそれらの使用方法
US9079914B2 (en) 2009-07-22 2015-07-14 Eisai R&D Management Co., Ltd. Fused aminodihydro-oxazine derivatives
US9139594B2 (en) 2009-07-22 2015-09-22 Eisai R&D Management Co., Ltd. Fused aminodihydropyrimidone derivatives
US9145426B2 (en) 2011-04-07 2015-09-29 Merck Sharp & Dohme Corp. Pyrrolidine-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
WO2015156421A1 (en) 2014-04-11 2015-10-15 Shionogi & Co., Ltd. Dihydrothiazine and dihydrooxazine derivatives having bace1 inhibitory activity
US9175013B2 (en) 2011-01-21 2015-11-03 Eisai R&D Management Co., Ltd. Fused aminodihydrothiazine derivatives
US9181236B2 (en) 2011-08-22 2015-11-10 Merck Sharp & Dohme Corp. 2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use
US9221839B2 (en) 2011-04-07 2015-12-29 Merck Sharp & Dohme Corp. C5-C6 oxacyclic-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
US9290477B2 (en) 2012-09-28 2016-03-22 Vitae Pharmaceuticals, Inc. Inhibitors of β-secretase
US9416129B2 (en) 2012-10-17 2016-08-16 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds as BACE inhibitors, compositions and their use
US9422277B2 (en) 2012-10-17 2016-08-23 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds as BACE inhibitors, compositions and their use
US9447085B2 (en) 2012-12-14 2016-09-20 Merck Sharp & Dohme Corp. Iminothiadiazine dioxides containing a thioamide, amidine, or amide oxime group as BACE inhibitors, compositions, and their use
US9499502B2 (en) 2011-04-13 2016-11-22 Merck Sharp & Dohme Corp. 5-substituted iminothiazines and their mono- and dioxides as BACE inhibitors, compositions, and their use
US9540359B2 (en) 2012-10-24 2017-01-10 Shionogi & Co., Ltd. Dihydrooxazine or oxazepine derivatives having BACE1 inhibitory activity
WO2017061534A1 (en) 2015-10-08 2017-04-13 Shionogi & Co., Ltd. Dihydrothiazine derivatives
WO2017111042A1 (en) 2015-12-25 2017-06-29 Shionogi & Co., Ltd. Process and intermediates for preparation of thiazine derivatives
JP2017521453A (ja) * 2014-07-25 2017-08-03 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft ピリジル−トリアザビシクル
JP2017523223A (ja) * 2014-08-08 2017-08-17 アムジエン・インコーポレーテツド β−セクレターゼ阻害剤としてのシクロプロピル縮合チアジン−2−アミン化合物及び使用方法
JP2018513191A (ja) * 2015-04-21 2018-05-24 オールジェネシス バイオセラピューティクス インコーポレイテッド Bace1阻害剤としての化合物およびそれらの使用
JP2020503292A (ja) * 2016-12-15 2020-01-30 アムジエン・インコーポレーテツド β−セクレターゼ阻害剤としてのチアジン誘導体および使用方法
JP2020504739A (ja) * 2016-12-22 2020-02-13 インサイト・コーポレイションIncyte Corporation Pd−l1内在化誘導物質としてのテトラヒドロイミダゾ[4,5−c]ピリジン誘導体
US11407749B2 (en) 2015-10-19 2022-08-09 Incyte Corporation Heterocyclic compounds as immunomodulators
US11414433B2 (en) 2018-05-11 2022-08-16 Incyte Corporation Heterocyclic compounds as immunomodulators
US11465981B2 (en) 2016-12-22 2022-10-11 Incyte Corporation Heterocyclic compounds as immunomodulators
US11535615B2 (en) 2015-12-22 2022-12-27 Incyte Corporation Heterocyclic compounds as immunomodulators
US11566026B2 (en) 2016-12-22 2023-01-31 Incyte Corporation Heterocyclic compounds as immunomodulators
US11572366B2 (en) 2015-11-19 2023-02-07 Incyte Corporation Heterocyclic compounds as immunomodulators
US11608337B2 (en) 2016-05-06 2023-03-21 Incyte Corporation Heterocyclic compounds as immunomodulators
US11613536B2 (en) 2016-08-29 2023-03-28 Incyte Corporation Heterocyclic compounds as immunomodulators
US11629154B2 (en) 2018-04-27 2023-04-18 Shionogi & Co., Ltd. Tetrahydropyranooxazine derivatives having selective BACE1 inhibitory activity
US11673883B2 (en) 2016-05-26 2023-06-13 Incyte Corporation Heterocyclic compounds as immunomodulators
US11718605B2 (en) 2016-07-14 2023-08-08 Incyte Corporation Heterocyclic compounds as immunomodulators
US11753406B2 (en) 2019-08-09 2023-09-12 Incyte Corporation Salts of a PD-1/PD-L1 inhibitor
US11760756B2 (en) 2020-11-06 2023-09-19 Incyte Corporation Crystalline form of a PD-1/PD-L1 inhibitor
US11780836B2 (en) 2020-11-06 2023-10-10 Incyte Corporation Process of preparing a PD-1/PD-L1 inhibitor
US11787793B2 (en) 2016-12-22 2023-10-17 Incyte Corporation Heterocyclic compounds as immunomodulators
US11866451B2 (en) 2019-11-11 2024-01-09 Incyte Corporation Salts and crystalline forms of a PD-1/PD-L1 inhibitor
US11866434B2 (en) 2020-11-06 2024-01-09 Incyte Corporation Process for making a PD-1/PD-L1 inhibitor and salts and crystalline forms thereof
US11873309B2 (en) 2016-06-20 2024-01-16 Incyte Corporation Heterocyclic compounds as immunomodulators
US12247026B2 (en) 2018-03-30 2025-03-11 Incyte Corporation Heterocyclic compounds as immunomodulators
US12247038B2 (en) 2019-09-30 2025-03-11 Incyte Corporation Pyrido[3,2-d]pyrimidine compounds as immunomodulators

Families Citing this family (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2009291602B2 (en) * 2008-09-11 2013-02-14 Amgen Inc. Spiro-tetracyclic ring compounds as betasecretase modulators and methods of use
US8673894B2 (en) * 2010-05-07 2014-03-18 Hoffmann-La Roche Inc. 2,5,6,7-tetrahydro-[1,4]oxazepin-3-ylamine or 2,3,6,7-tetrahydro-[1,4]oxazepin-5-ylamine compounds
NZ604018A (en) 2010-06-07 2015-02-27 Novomedix Llc Furanyl compounds and the use thereof
EA201291366A1 (ru) * 2010-06-09 2013-04-30 Янссен Фармацевтика Нв Производные 5-амино-3,6-дигидро-1h-пиразин-2-она в качестве ингибиторов бета-секретазы (bace)
JP5711813B2 (ja) 2010-06-09 2015-05-07 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプJanssen Pharmaceutica Naamloze Vennootschap βセクレターゼ(BACE)の阻害剤として有用な5,6−ジヒドロ−2H−[1,4]オキサジン−3−イル−アミン誘導体
DK2483255T3 (da) * 2010-07-13 2014-01-20 Novartis Ag Oxazinderivater samt deres anvendelse ved behandling af neurologiske lidelser
US8524897B2 (en) 2011-01-12 2013-09-03 Novartis Ag Crystalline oxazine derivative
US8404680B2 (en) * 2011-02-08 2013-03-26 Hoffmann-La Roche Inc. N-[3-(5-amino-3,3a,7,7a-tetrahydro-1H-2,4-dioxa-6-aza-inden-7-yl)-phenyl]-amides as BACE1 and/or BACE2 inhibitors
UA109800C2 (xx) 2011-03-01 2015-10-12 ПОХІДНІ 6,7-ДИГІДРОПІРАЗОЛО$1,5-a]ПІРАЗИН-4-ІЛАМІНУ, КОРИСНІ ЯК ІНГІБІТОРИ БЕТА-СЕКРЕТАЗИ (BACE)
MX340031B (es) 2011-03-09 2016-06-21 Janssen Pharmaceutica Nv Derivados de 3,4-dihidropirrolo[1,2-a]pirazin-1-ilamina utiles como inhibidores de beta-secretasa (bace).
UY34278A (es) * 2011-08-25 2013-04-05 Novartis Ag Derivados novedosos de oxazina y su uso en el tratamiento de enfermedades
EA024716B1 (ru) * 2011-12-06 2016-10-31 Янссен Фармацевтика Нв Производные 5-(3-аминофенил)-5-алкил-5,6-дигидро-2h-[1,4]оксазин-3-амина
MX354173B (es) * 2012-01-26 2018-02-16 Hoffmann La Roche Fluorometil-5,6-dihidro-4h-[1,3]oxazinas.
US8338413B1 (en) 2012-03-07 2012-12-25 Novartis Ag Oxazine derivatives and their use in the treatment of neurological disorders
WO2013182638A1 (en) * 2012-06-08 2013-12-12 H. Lundbeck A/S 2 -aminothiazinylheteroaryls as bace1 inhibitors for the treatment alzheimer's disease
US9489013B2 (en) 2012-12-20 2016-11-08 Merck Sharp & Dohme Corp. C6-azaspiro iminothiadiazine dioxides as bace inhibitors, compositions, and their use
JP2016504998A (ja) 2012-12-20 2016-02-18 メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. Bace阻害剤としてのc5,c6オキサ環縮合イミノチアジンジオキシド化合物、組成物およびそれらの使用
WO2014120658A1 (en) 2013-01-29 2014-08-07 Amgen Inc. Fused multicyclic 3-amino-5,6-dihydro-2h-1,4-thiazine derivatives and their use as beta-secretase inhibitors
TW201446758A (zh) 2013-03-01 2014-12-16 Amgen Inc 作爲β-分泌酶抑制劑的全氟化5,6-二氫-4H-1,3-□-2-胺化合物及其用途
AU2014225604B2 (en) 2013-03-08 2018-05-17 Amgen Inc. Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
CN104211639A (zh) * 2013-06-05 2014-12-17 中国科学院上海药物研究所 一类炔基杂环类化合物及其应用
EP3008067B1 (en) 2013-06-12 2017-03-29 Janssen Pharmaceutica N.V. 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazin-3(2h)-one derivatives as inhibitors of beta-secretase (bace)
ES2697684T3 (es) 2013-06-12 2019-01-25 Janssen Pharmaceutica Nv Derivados de 4-amino-6-fenil-5,6-dihidroimidazo[1,5 a]pirazina como inhibidores de beta-secretasa (BACE)
US9751886B2 (en) 2013-06-12 2017-09-05 Janssen Pharmaceutica Nv 4-amino-6-phenyl-6,7-dihydro[1,2,3]triazolo[1,5-A]pyrazine derivatives as inhibitors of beta-secretase (BACE)
JO3318B1 (ar) 2013-06-18 2019-03-13 Lilly Co Eli مثبطات bace
US9096615B2 (en) 2013-07-30 2015-08-04 Amgen Inc. Bridged bicyclic amino thiazine dioxide compounds as inhibitors of beta-secretase and methods of use thereof
WO2015094930A1 (en) 2013-12-18 2015-06-25 Merck Sharp & Dohme Corp. C-6 spirocarbocyclic iminothiadiazine dioxides as bace inhibitors, compositions, and their use
WO2015197187A1 (en) * 2014-06-24 2015-12-30 Grünenthal GmbH Pyrazolyl-based carboxamides v
WO2016096979A1 (en) 2014-12-18 2016-06-23 Janssen Pharmaceutica Nv 2,3,4,5-tetrahydropyridin-6-amine and 3,4-dihydro-2h-pyrrol-5-amine compound inhibitors of beta-secretase
WO2016207345A1 (en) * 2015-06-24 2016-12-29 Pierre Fabre Medicament 3-amino-pyrazin-2-yl carboxamide and 2-amino-pyridin-3-yl carboxamide derivatives as polo-like kinase 1 (plk-1) inhibitors for the treatment of cancer
US10246429B2 (en) 2015-08-06 2019-04-02 Amgen Inc. Vinyl fluoride cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
JP2017071603A (ja) * 2015-10-09 2017-04-13 塩野義製薬株式会社 ジヒドロチアジンまたはジヒドロオキサジン誘導体を含有する医薬組成物
AU2017378316B2 (en) 2016-12-15 2021-04-01 Amgen Inc. Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use
JP7177773B2 (ja) 2016-12-15 2022-11-24 アムジエン・インコーポレーテツド β-セクレターゼ阻害剤としてのオキサジン誘導体および使用方法
EP3555106B1 (en) 2016-12-15 2022-03-09 Amgen Inc. Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use
MX387729B (es) 2016-12-15 2025-03-18 Amgen Inc Derivados de dióxido de 1,4-tiazina y dióxido 1,2,4-tiadiazina como inhibidores de beta-secretasa y métodos de uso.
WO2018165501A1 (en) * 2017-03-10 2018-09-13 Lycera Corporation INDOLINYL SULFONAMIDE AND RELATED COMPOUNDS FOR USE AS AGONISTS OF RORγ AND THE TREATMENT OF DISEASE
WO2018172852A1 (en) * 2017-03-21 2018-09-27 Arbutus Biopharma Corporation Substituted dihydroindene-4-carboxamides and analogs thereof, and methods using same
KR20220024012A (ko) * 2019-06-28 2022-03-03 바텔리 메모리얼 인스티튜트 산화 공정을 통한 pfas의 파괴 및 오염된 장소로의 운송에 적합한 장치
US11806346B2 (en) * 2020-05-13 2023-11-07 Chdi Foundation, Inc. HTT modulators for treating Huntington's disease
US12281116B2 (en) 2021-11-17 2025-04-22 Chdi Foundation, Inc. HTT modulators for treating Huntington's disease
TW202430152A (zh) * 2022-11-30 2024-08-01 美商纜圖藥品公司 野生型kit抑制劑

Citations (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3227713A (en) 1966-01-04 Azine derivatives
US3235551A (en) 1966-02-15 Novel derivatives of
WO1996014842A1 (en) 1994-11-15 1996-05-23 Merck & Co., Inc. Substituted heterocycles as inhibitors of nitric oxide synthase
WO2002096897A1 (en) 2001-05-30 2002-12-05 Neurologic, Inc. PHOSPHINYLMETHYL AND PHOSPHORYLMETHYL SUCCINIC AND GLUTARIC ACID ANALOGS AS β-SECRETASE INHIBITORS
WO2004043916A1 (en) 2002-11-12 2004-05-27 Merck & Co., Inc. Phenylcarboxamide beta-secretase inhibitors for the treatment of alzheimer's disease
WO2005058311A1 (en) 2003-12-15 2005-06-30 Schering Corporation Heterocyclic aspartyl protease inhibitors
WO2005097767A1 (en) 2004-03-30 2005-10-20 Merck & Co., Inc. 2-aminothiazole compounds useful as aspartyl protease inhibitors
WO2005111031A2 (en) 2004-04-30 2005-11-24 Schering Corporation Neuropeptide receptor modulators
WO2006041405A1 (en) 2004-10-15 2006-04-20 Astrazeneca Ab Substituted amino-pyrimidones and uses thereof
WO2006041404A1 (en) 2004-10-15 2006-04-20 Astrazeneca Ab Substituted amino-compounds and uses thereof
US20070004786A1 (en) 2005-06-30 2007-01-04 Wyeth Amino-5-(5-membered)hetero-arylimidazolone compounds and the use thereof for beta-secretase modulation
US20070004730A1 (en) 2005-06-30 2007-01-04 Wyeth Amino-5-(6-membered)heteroarylimidazolone compounds and the use thereof for beta-secretase modulation
US20070027199A1 (en) 2005-07-29 2007-02-01 Wyeth Cycloalkyl amino-hydantoin compounds and use thereof for beta-secretase modulation
WO2007049532A1 (ja) 2005-10-25 2007-05-03 Shionogi & Co., Ltd. アミノジヒドロチアジン誘導体

Family Cites Families (179)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2899426A (en) 1959-08-11 Synthesis of l
GB140144A (en) 1918-12-30 1920-03-25 Henry Holden Illingworth Improvements in and relating to stop-motions for gill-boxes
WO1995009619A2 (en) 1993-10-04 1995-04-13 The Wellcome Foundation Limited Substituted urea and isothiourea derivatives as no synthase inhibitors
SU110580A1 (ru) * 1957-04-15 1957-11-30 Герингклее Вальтер Способ получени производных дигидро-мета-тиазина-Д-3,4, замещенных у циклических атомов углерода
US3115494A (en) 1961-10-13 1963-12-24 Mcneilab Inc 2-amino-5, 6-dihydro-4ii-1, 3-oxazines and a process for their preparation
BE637923A (ja) 1962-09-29
US3636116A (en) 1968-09-03 1972-01-18 Dow Chemical Co 1 2-substituted indene compounds
SU465792A3 (ru) 1968-11-06 1975-03-30 Хиноин Гиогисцер-Ес Вегиесцети Термекек Гиара Рт (Фирма) Способ получени гетероциклических соединений
US3577428A (en) 1969-04-14 1971-05-04 Colgate Palmolive Co 2-amino-4-aryloxyalkyl-4-alkyl-2-oxazolines
US3719674A (en) 1971-02-08 1973-03-06 Dow Chemical Co 1,2-substituted indene compounds
DE2426653C3 (de) 1974-06-01 1982-05-06 Bayer Ag, 5090 Leverkusen Derivate des 2-Amino-1,3-thiazins
DD140144A1 (de) 1978-11-08 1980-02-13 Horst Hartmann Verfahren zur herstellung von p-aminophenylsubstituierten 2-amino-1,3-thiaziniumsalzen
US4311840A (en) 1980-11-13 1982-01-19 E. R. Squibb & Sons, Inc. 2,3,6,7-Tetrahydro-2-thioxo-4H-oxazolo[3,2-a]-1,3,5 triazin-4-ones
JPS62120374A (ja) 1985-11-20 1987-06-01 Yoshitomi Pharmaceut Ind Ltd 1,3−チアジンまたは1,3−オキサジン誘導体
FI95572C (fi) 1987-06-22 1996-02-26 Eisai Co Ltd Menetelmä lääkeaineena käyttökelpoisen piperidiinijohdannaisten tai sen farmaseuttisen suolan valmistamiseksi
CA1332151C (en) 1988-01-28 1994-09-27 Roman Amrein Use of a benzamide to treat cognitive disorder
US5236942A (en) 1990-04-19 1993-08-17 Merrell Dow Pharmaceuticals Inc. 5-aryl-4-alkyl-3H-1,2,4-triazole-3-thiones useful in the treatment of Altzheimer's dementia
US5328915A (en) 1992-09-17 1994-07-12 E. I. Du Pont De Nemours And Company Arthropodicidal amidrazone ureas
CN1095710A (zh) 1992-11-27 1994-11-30 惠尔康基金会集团公司 酶抑制剂
GB9418912D0 (en) 1994-09-20 1994-11-09 Fisons Corp Pharmaceutically active compounds
DE4442116A1 (de) * 1994-11-25 1996-05-30 Cassella Ag 2-Amino-1,3-thiazine als Hemmstoffe der Stickstoffmonoxid-Synthase
AU2629795A (en) 1994-12-12 1996-07-03 Chugai Seiyaku Kabushiki Kaisha Aniline derivative having the effect of inhibiting nitrogen monoxide synthase
JPH08333258A (ja) 1994-12-14 1996-12-17 Japan Tobacco Inc チアジン又はチアゼピン誘導体及びそれら化合物を含有してなる一酸化窒素合成酵素阻害剤
DE4444930A1 (de) 1994-12-16 1996-06-27 Cassella Ag 2-Amino-1,3-thiazepine und deren Verwendung als Hemmstoffe der Stickstoffmonoxid-Synthase
DE69620191T2 (de) 1995-08-11 2002-07-18 Pfizer Inc., New York (1s,2s)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidin-1-yl)-1-propanol-methansulfonat trihydrat
JPH0967355A (ja) 1995-08-31 1997-03-11 Tokyo Tanabe Co Ltd チアジン誘導体、チアゾール誘導体及びそれらの製造方法
HUP9602538A3 (en) 1995-09-18 1997-08-28 Sankyo Co New urea and amide derivatives having acat inhibitory activity, their preparation and their use
SK45898A3 (en) 1995-10-17 1999-01-11 Astra Pharma Prod Pharmaceutically active quinazoline compounds
JP2000509028A (ja) 1996-04-13 2000-07-18 アストラ・フアーマシユウテイカルズ・リミテツド アミノイソキノリンおよびアミノチエノピリジン誘導体ならびに抗炎症剤としてのそれらの使用
US6096753A (en) 1996-12-05 2000-08-01 Amgen Inc. Substituted pyrimidinone and pyridone compounds and methods of use
US5952374A (en) 1997-09-29 1999-09-14 Protein Technologies International, Inc. Method for inhibiting the development of Alzheimer's disease and related dementias- and for preserving cognitive function
SE9703693D0 (sv) 1997-10-10 1997-10-10 Astra Pharma Prod Novel combination
TW460460B (en) 1997-11-04 2001-10-21 Chugai Pharmaceutical Co Ltd Heterocyclic compounds having NOS inhibitory activities
US6294695B1 (en) 1998-03-26 2001-09-25 Mount Sinai School Of Medicine Of The City University Of New York Aminobenzoic acid derivatives having anti-tumorigenic activity methods of making and using the same
AUPP285898A0 (en) 1998-04-07 1998-04-30 Fujisawa Pharmaceutical Co., Ltd. Amido derivatives
SE9802333D0 (sv) 1998-06-29 1998-06-29 Astra Pharma Prod Novel combination
US7375125B2 (en) 1999-08-04 2008-05-20 Ore Pharmaceuticals, Inc. Melanocortin-4 receptor binding compounds and methods of use thereof
AU780787B2 (en) 1999-09-17 2005-04-14 Millennium Pharmaceuticals, Inc. Benzamides and related inhibitors of factor Xa
US20030060487A1 (en) 2000-04-12 2003-03-27 Bamdad R. Shoshana Treatment of neurodegenerative disease
US20040110743A1 (en) 2000-05-19 2004-06-10 Masaomi Miyamato -Secretase inhibitors
US6420566B2 (en) 2000-06-09 2002-07-16 Aventis Pharma S.A. Pharmaceutical compositions containing a 4, 5-dihydro-1, 3-thiazol-2-ylamine derivative, novel derivatives and preparation thereof
US6713276B2 (en) 2000-06-28 2004-03-30 Scios, Inc. Modulation of Aβ levels by β-secretase BACE2
WO2002062766A2 (en) 2001-02-07 2002-08-15 Millennium Pharmaceuticals, Inc. Melanocortin-4 receptor binding compounds and methods of use thereof
WO2002088101A2 (en) 2001-04-27 2002-11-07 Vertex Pharmaceuticals Incorporated Inhibitors of bace
EP1453789A2 (en) 2001-11-08 2004-09-08 Elan Pharmaceuticals, Inc. N,n'-substituted-1,3-diamino-2-hydroxypropane derivatives
AU2002358874B2 (en) 2001-11-09 2007-09-06 Aventis Pharma S.A. 2-amino-4-heteroarylethyl thiazoline derivatives and their use an inhibitors of inducible no-synthase
CA2465877C (fr) 2001-11-09 2009-12-29 Aventis Pharma S.A. Utilisation de derives de 2-amino-4-pyridylmethyl-thiazoline comme inhibiteurs de non-synthase inductible
CA2669810A1 (fr) 2001-11-09 2003-05-15 Aventis Pharma S.A. Composes intermediaires pour la preparation de derives de 2-amino-thiazoline
WO2003082191A2 (en) 2002-03-28 2003-10-09 Merck & Co., Inc. Substituted 2,3-diphenyl pyridines
WO2004000312A2 (de) 2002-06-19 2003-12-31 Solvay Pharmaceuticals Gmbh Arzneimittel zur behandlung von eine inhibition oder aktivitätsverminderung von ph-wert-regulierenden bikarbonat-transporter-proteinen erfordernden erkrangungen
AU2003249983A1 (en) 2002-07-18 2004-02-09 Actelion Pharmaceuticals Ltd Piperidines useful for the treatment of central nervous system disorders
WO2004014843A1 (ja) 2002-08-09 2004-02-19 Takeda Chemical Industries, Ltd. 置換アミノ化合物およびその用途
TW200502221A (en) 2002-10-03 2005-01-16 Astrazeneca Ab Novel lactams and uses thereof
JP2004149429A (ja) 2002-10-29 2004-05-27 Takeda Chem Ind Ltd インドール化合物およびその用途
JP2006096665A (ja) 2002-10-29 2006-04-13 Ono Pharmaceut Co Ltd 脊柱管狭窄症治療剤
RU2252936C2 (ru) 2002-12-05 2005-05-27 Институт физиологически активных веществ РАН S-замещенные n-1-[(гетеро)арил]алкил-n`-[(гетеро)арил]алкилизотиомочевины, способ их получения, фармацевтическая композиция, способ изучения глутаматэргической системы, способы лечения (варианты)
EP1631560A2 (en) 2003-04-25 2006-03-08 3-Dimensional Pharmaceuticals, Inc. C-fms kinase inhibitors
GB0324498D0 (en) 2003-07-21 2003-11-26 Aventis Pharma Inc Heterocyclic compounds as P2X7 ion channel blockers
WO2005032493A2 (en) 2003-10-07 2005-04-14 Renovis, Inc. Amide compounds as ion channel ligands and uses thereof
US7592348B2 (en) 2003-12-15 2009-09-22 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
PE20060299A1 (es) 2004-06-16 2006-05-18 Wyeth Corp DIFENILIMIDAZOPIRIMIDINA E -IMIDAZOL AMINAS COMO INHIBIDORES DE ß-SECRETASA
CN101005877A (zh) 2004-08-23 2007-07-25 默克公司 作为用于治疗或预防糖尿病的二肽基肽酶-ⅳ抑制剂的稠合三唑衍生物
EP1791818A1 (en) 2004-09-14 2007-06-06 The Genetics Company, Inc. Hydrazone derivatives and their use as beta secretase inhibitors
WO2006043405A1 (ja) 2004-10-18 2006-04-27 Mitsubishi Chemical Corporation 糖鎖構造解析方法
WO2006065204A1 (en) 2004-12-14 2006-06-22 Astrazeneca Ab Substituted aminopyridines and uses thereof
JP5184891B2 (ja) 2005-01-07 2013-04-17 シンタ ファーマシューティカルズ コーポレーション 炎症及び免疫に関連する用途に用いる化合物
WO2006076284A2 (en) 2005-01-14 2006-07-20 Wyeth AMINO-IMIDAZOLONES FOR THE INHIBITION OF ß-SECRETASE
EP1848692A1 (en) 2005-02-14 2007-10-31 Wyeth AZOLYLACYLGUANIDINES AS ß-SECRETASE INHIBITORS
WO2006088694A1 (en) 2005-02-14 2006-08-24 Wyeth SUBSTITUTED THIENYL AND FURYL ACYLGUANIDINES AS β-SECRETASE MODULATORS
WO2006088705A1 (en) 2005-02-14 2006-08-24 Wyeth Terphenyl guanidines as [beta symbol] -secretase inhibitors
CA2600570C (en) 2005-03-14 2011-12-06 Transtech Pharma, Inc. Benzazole derivatives, compositions, and methods of use as .beta.-secretase inhibitors
EP1891021B1 (en) 2005-06-14 2019-01-23 Merck Sharp & Dohme Corp. Aspartyl protease inhibitors
EP2345411B1 (en) 2005-06-14 2013-10-02 Merck Sharp & Dohme Corp. Heterocyclic aspartyl protease inhibitors, preparation and use thereof
CA2612227C (en) 2005-06-14 2014-04-22 Taigen Biotechnology Co., Ltd. Pyrimidine compounds
EP1896477B1 (en) 2005-06-14 2010-09-22 Schering Corporation Aspartyl protease inhibitors
WO2007002220A2 (en) 2005-06-21 2007-01-04 Bristol-Myers Squibb Company Aminoacetamide acyl guanidines as beta-secretase inhibitors
WO2007038271A1 (en) 2005-09-26 2007-04-05 Wyeth Amino-5- [4- (difluoromethoxy) phenyl] -5-phenylimidazolone compounds as inhibitors of the beta-secretase (bace)
EP1951682A4 (en) 2005-11-15 2011-06-15 Astrazeneca Ab NEW 2-AMINOPYRIMIDONE OR 2-AMINOPYRIDINONE DERIVATIVES AND THEIR USE
EP1951680A4 (en) 2005-11-15 2011-08-10 Astrazeneca Ab NOVEL 2-AMINOPYRIMIDINONE DERIVATIVES AND THEIR USE
TW200804290A (en) 2005-11-15 2008-01-16 Astrazeneca Ab Compounds and uses thereof
JP2009520686A (ja) 2005-11-21 2009-05-28 アストラゼネカ・アクチエボラーグ 新規な2−アミノ−イミダゾール−4−オン化合物並びに認知障害、アルツハイマー病、神経変性及び認知症の治療に使用する医薬の製造におけるその使用
TW200734311A (en) 2005-11-21 2007-09-16 Astrazeneca Ab New compounds
AR058381A1 (es) 2005-12-19 2008-01-30 Astrazeneca Ab Compuestos derivados de 2-aminopiridin-4-onas y una composicion farmaceutica
JP2009520027A (ja) 2005-12-19 2009-05-21 ワイス 2−アミノ−5−ピペリジニルイミダゾロン化合物およびβ−セクレターゼ調節におけるその使用
PE20071025A1 (es) 2006-01-31 2007-10-17 Mitsubishi Tanabe Pharma Corp Compuesto amina trisustituido
WO2007092854A2 (en) 2006-02-06 2007-08-16 Janssen Pharmaceutica N.V. 2-AMINO-QUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF β-SECRETASE (BACE)
US7776882B2 (en) 2006-02-06 2010-08-17 Baxter Ellen W 2-amino-3,4-dihydro-quinoline derivatives useful as inhibitors of β-secretase (BACE)
EP2004630A4 (en) 2006-04-05 2010-05-19 Astrazeneca Ab 2-AMINOPYRIMIDIN-4-ONES AND THEIR USE FOR THE TREATMENT OR PREVENTION OF PATHOLOGIES RELATED TO PROTEIN A
TW200808751A (en) 2006-04-13 2008-02-16 Astrazeneca Ab New compounds
CA2649736C (en) 2006-04-20 2013-11-26 Janssen Pharmaceutica N.V. Heterocyclic compounds as inhibitors of c-fms kinase
EP2644600B1 (en) 2006-06-12 2017-01-11 Merck Sharp & Dohme Corp. Heterocyclic aspartyl protease inhibitors
BRPI0713187A2 (pt) 2006-07-20 2012-10-16 Mehmet Kahraman método de inibir rho-quinase, método de tratamento de doença mediada por rho-quinase, composto e composição farmacêutica
TW200817406A (en) 2006-08-17 2008-04-16 Wyeth Corp Imidazole amines as inhibitors of β-secretase
MX2009006227A (es) 2006-12-12 2009-06-22 Schering Corp Inhibidores de aspartil proteasa que contienen un sistema de anillo triciclico.
US8093254B2 (en) 2006-12-12 2012-01-10 Schering Corporation Aspartyl protease inhibitors
TW200831080A (en) 2006-12-15 2008-08-01 Irm Llc Compounds and compositions as inhibitors of cannabinoid receptor 1 activity
KR101222412B1 (ko) 2007-02-15 2013-01-15 에프. 호프만-라 로슈 아게 Taar1 리간드로서의 2-아미노옥사졸린
WO2008133273A1 (ja) 2007-04-24 2008-11-06 Shionogi & Co., Ltd. アルツハイマー症治療用医薬組成物
KR20100017255A (ko) 2007-04-24 2010-02-16 시오노기 앤드 컴파니, 리미티드 환식기로 치환된 아미노다이하이드로싸이아진 유도체
GB0713686D0 (en) 2007-07-13 2007-08-22 Addex Pharmaceuticals Sa New compounds 2
JP4846769B2 (ja) 2007-07-30 2011-12-28 田辺三菱製薬株式会社 医薬組成物
WO2009064418A1 (en) 2007-11-14 2009-05-22 Amgen Inc. Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use
CN101910143B (zh) 2008-01-18 2013-08-21 卫材R&D管理有限公司 稠合的氨基二氢噻嗪衍生物
EP2238111B1 (en) 2008-01-28 2013-01-16 Janssen Pharmaceutica NV 6-substituted-thio-2-amino-quinoline derivatives useful as inhibitors of -secretase (bace)
NZ586830A (en) 2008-01-29 2012-02-24 Janssen Pharmaceutica Nv 2-amino-quinoline derivatives useful as inhibitors of beta-secretase (bace)
ES2475206T3 (es) 2008-02-01 2014-07-10 Takeda Pharmaceutical Company Limited Derivados de oxima como inhibidores de HSP90
WO2009103626A1 (en) 2008-02-18 2009-08-27 F. Hoffmann-La Roche Ag 4, 5-dihydro-oxazol-2-yl amine derivatives
PE20091834A1 (es) 2008-04-22 2009-12-19 Schering Corp Compuestos de 2-imino-3-metilpirrolopirimidinona tiofenilo-sustituida como inhibidores de bace-1 y composiciones que los contienen
TWI431004B (zh) 2008-05-02 2014-03-21 Lilly Co Eli Bace抑制劑
PH12013500242A1 (en) 2008-06-13 2013-04-08 Shionogi & Co Sulfur-containing heterocyclic derivative having b-secretase-inhibiting activity
KR20110048491A (ko) 2008-07-28 2011-05-11 에자이 알앤드디 매니지먼트 가부시키가이샤 스피로아미노디하이드로티아진 유도체들
WO2010013302A1 (ja) 2008-07-28 2010-02-04 エーザイ・アール・アンド・ディー・マネジメント株式会社 スピロアミノジヒドロチアジン誘導体
US20110251172A1 (en) 2008-08-13 2011-10-13 Rivkin Alexey A Purine derivatives for treatment of alzheimer's disease
EP2312946A4 (en) 2008-08-13 2012-10-24 Merck Sharp & Dohme PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF ALZHEIMER'S DISEASE
CN102171221B (zh) 2008-09-30 2013-11-06 卫材R&D管理有限公司 新的稠合的氨基二氢噻嗪衍生物
CN102186841A (zh) 2008-10-22 2011-09-14 盐野义制药株式会社 具有bace1抑制活性的2-氨基嘧啶-4-酮及2-氨基吡啶衍生物
WO2010056195A1 (en) 2008-11-14 2010-05-20 Astrazeneca Ab New compounds 575
TW201020244A (en) 2008-11-14 2010-06-01 Astrazeneca Ab New compounds
US20100125081A1 (en) 2008-11-14 2010-05-20 Astrazeneca Ab New compounds 574
JPWO2010113848A1 (ja) 2009-03-31 2012-10-11 塩野義製薬株式会社 Bace1阻害作用を有するイソチオウレア誘導体またはイソウレア誘導体
KR101123178B1 (ko) 2009-04-09 2012-06-13 (주)에스메디 2-아릴벤조싸이오펜 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 퇴행성 뇌질환의 진단 또는 치료용 약학적 조성물
US9174999B2 (en) 2009-05-07 2015-11-03 The Board Of Trustees Of The Leland Stanford Junior University Methods and compositions for studying, imaging, and treating pain
US8461160B2 (en) 2009-05-08 2013-06-11 Hoffmann-La Roche, Inc. Dihydropyrimidinones
AR077277A1 (es) 2009-07-09 2011-08-17 Lilly Co Eli Compuestos de biciclo (1,3)tiazin-2-amina formulacion farmaceutica que lo comprende y su uso para la manufactura de un medicamento util para el tratamiento de la enfermedad de alzheimer
GB0912777D0 (en) 2009-07-22 2009-08-26 Eisai London Res Lab Ltd Fused aminodihydropyrimidone derivatives
GB0912778D0 (en) 2009-07-22 2009-08-26 Eisai London Res Lab Ltd Fused aminodihydro-oxazine derivatives
AR077328A1 (es) 2009-07-24 2011-08-17 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos
US8188079B2 (en) 2009-08-19 2012-05-29 Hoffman-La Roche Inc. 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines
US20110065695A1 (en) 2009-09-11 2011-03-17 Jeremy Beauchamp Use of aminodihydrothiazines for the treatment or prevention of diabetes
WO2011044184A1 (en) 2009-10-08 2011-04-14 Schering Corporation Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
US8569310B2 (en) 2009-10-08 2013-10-29 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions and their use
US8563543B2 (en) 2009-10-08 2013-10-22 Merck Sharp & Dohme Corp. Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
EP2500344A4 (en) 2009-11-13 2013-05-01 Shionogi & Co AMINOTHIAZIN OR AMINOOXAZINE DERIVATIVES WITH AN AMINO TERMINATION
US8435994B2 (en) 2009-11-16 2013-05-07 Merck Sharp & Dohme Corp. Substituted [1,2,4]triazolo[4,3-alpha]quinoxalines as adenosine A2a receptor antagonists
JP5554346B2 (ja) 2009-12-09 2014-07-23 塩野義製薬株式会社 含硫黄複素環誘導体を含有するアルツハイマー症の治療用または予防用医薬組成物
WO2011070781A1 (ja) 2009-12-09 2011-06-16 塩野義製薬株式会社 置換アミノチアジン誘導体
US7964594B1 (en) 2009-12-10 2011-06-21 Hoffmann-La Roche Inc. Amino oxazine derivatives
EP2511269A4 (en) 2009-12-11 2013-04-24 Shionogi & Co FUSED HETEROCYCLIC COMPOUND HAVING AN AMINO GROUP
PH12012501081A1 (en) 2009-12-11 2012-10-29 Shionogi & Co Oxazine derivatives
UA103272C2 (uk) 2009-12-11 2013-09-25 Ф. Хоффманн-Ля Рош Аг 2-аміно-5,5-дифтор-5,6-дигідро-4h-оксазини як інгібітори bace1 і/або bace2
US20120258961A1 (en) 2009-12-24 2012-10-11 Shionogi & Co., Ltd. 4-amino-1,3-thiazine or oxazine derivative
NZ600136A (en) 2009-12-31 2013-09-27 Novartis Ag Pyrazine derivatives and their use in the treatment of neurological disorders
US8673894B2 (en) 2010-05-07 2014-03-18 Hoffmann-La Roche Inc. 2,5,6,7-tetrahydro-[1,4]oxazepin-3-ylamine or 2,3,6,7-tetrahydro-[1,4]oxazepin-5-ylamine compounds
EA201291366A1 (ru) 2010-06-09 2013-04-30 Янссен Фармацевтика Нв Производные 5-амино-3,6-дигидро-1h-пиразин-2-она в качестве ингибиторов бета-секретазы (bace)
JP5711813B2 (ja) 2010-06-09 2015-05-07 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプJanssen Pharmaceutica Naamloze Vennootschap βセクレターゼ(BACE)の阻害剤として有用な5,6−ジヒドロ−2H−[1,4]オキサジン−3−イル−アミン誘導体
KR20130089231A (ko) 2010-06-28 2013-08-09 얀센 파마슈티카 엔.브이. 알츠하이머병 및 다른 형태의 치매 치료용으로 유용한 3-아미노-5,6-디하이드로-1h-피라진-2-온 유도체
DK2483255T3 (da) 2010-07-13 2014-01-20 Novartis Ag Oxazinderivater samt deres anvendelse ved behandling af neurologiske lidelser
US8815881B2 (en) 2010-08-09 2014-08-26 Hoffmann-La Roche Inc. 1,4,5,6-tetrahydro-pyrimidin-2-ylamine compounds
CN103097389B (zh) 2010-09-22 2015-10-14 詹森药业有限公司 用作β-分泌酶(BACE)抑制剂的4,7-二氢-吡唑并[1,5-a]吡嗪-6-基胺衍生物
EP2634186A4 (en) 2010-10-29 2014-03-26 Shionogi & Co naphthyridine
WO2012057247A1 (ja) 2010-10-29 2012-05-03 塩野義製薬株式会社 縮合アミノジヒドロピリミジン誘導体
JP5834091B2 (ja) 2010-12-22 2015-12-16 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプJanssen Pharmaceutica Naamloze Vennootschap ベータ−セクレターゼ(BACE)の阻害剤として有用な5,6−ジヒドロ−イミダゾ[1,2−a]ピラジン−8−イルアミン誘導体
GB201100181D0 (en) 2011-01-06 2011-02-23 Eisai Ltd Fused aminodihydrothiazine derivatives
KR101569260B1 (ko) 2011-01-13 2015-11-13 노파르티스 아게 신규 헤테로시클릭 유도체 및 신경계 장애의 치료에서의 그의 용도
US20140128385A1 (en) 2011-01-13 2014-05-08 Novartis Ag Bace-2 inhibitors for the treatment of metabolic disorders
US9242943B2 (en) 2011-01-18 2016-01-26 Siena Biotech S.P.A. 1,4 oxazines as BACE1 and/or BACE2 inhibitors
GB201101140D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
GB201101139D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
US8399459B2 (en) 2011-02-02 2013-03-19 Hoffmann-La Roche Inc. 1,4 oxazines as BACE1 and/or BACE2 inhibitors
US8404680B2 (en) 2011-02-08 2013-03-26 Hoffmann-La Roche Inc. N-[3-(5-amino-3,3a,7,7a-tetrahydro-1H-2,4-dioxa-6-aza-inden-7-yl)-phenyl]-amides as BACE1 and/or BACE2 inhibitors
US20130040971A1 (en) 2011-02-14 2013-02-14 Boehringer Ingelheim International Gmbh 6-cycloalkyl-pyrazolopyrimidinones for the treatment of cns disorders
US8809345B2 (en) 2011-02-15 2014-08-19 Boehringer Ingelheim International Gmbh 6-cycloalkyl-pyrazolopyrimidinones for the treatment of CNS disorders
US8815841B2 (en) 2011-02-18 2014-08-26 Hoffmann-La Roche Inc. 1,4-Oxazepines as BACE1 and/or BACE2 inhibitors
UA109800C2 (xx) 2011-03-01 2015-10-12 ПОХІДНІ 6,7-ДИГІДРОПІРАЗОЛО$1,5-a]ПІРАЗИН-4-ІЛАМІНУ, КОРИСНІ ЯК ІНГІБІТОРИ БЕТА-СЕКРЕТАЗИ (BACE)
US9067924B2 (en) 2011-03-04 2015-06-30 Hoffmann-La Roche Inc. 1,4 thiazepines/sulfones as BACE1 and/or BACE2 inhibitors
MX340031B (es) 2011-03-09 2016-06-21 Janssen Pharmaceutica Nv Derivados de 3,4-dihidropirrolo[1,2-a]pirazin-1-ilamina utiles como inhibidores de beta-secretasa (bace).
US8748418B2 (en) 2011-03-18 2014-06-10 Hoffmann-La Roche Inc. 1,4-oxazepines as BACE1 and/or BACE2 inhibitors
US8877744B2 (en) 2011-04-04 2014-11-04 Hoffmann-La Roche Inc. 1,4-Oxazepines as BACE1 and/or BACE2 inhibitors
US8754075B2 (en) 2011-04-11 2014-06-17 Hoffmann-La Roche Inc. 1,3-oxazines as BACE1 and/or BACE2 inhibitors
US20140235626A1 (en) 2011-04-26 2014-08-21 Shionogi & Co., Ltd. Pyridine derivatives and a pharmaceutical composition for inhibiting bace1 containing them
EP2703399A4 (en) 2011-04-26 2014-10-15 Shionogi & Co OXAZINE DERIVATIVE AND BACE-1 HEMMER THEREOF
US8785436B2 (en) 2011-05-16 2014-07-22 Hoffmann-La Roche Inc. 1,3-oxazines as BACE 1 and/or BACE2 inhibitors
US8604024B2 (en) 2011-05-24 2013-12-10 Bristol-Myers Squibb Company Compounds for the reduction of beta-amyloid production
AR086539A1 (es) 2011-05-24 2014-01-08 Bristol Myers Squibb Co COMPUESTOS PARA LA REDUCCION DE LA PRODUCCION DE b-AMILOIDE
US9079919B2 (en) 2011-05-27 2015-07-14 Hoffmann-La Roche Inc. Spiro-[1,3]-oxazines and spiro-[1,4]-oxazepines as BACE1 and/or BACE2 inhibitors
MX2013014007A (es) 2011-06-07 2014-03-12 Hoffmann La Roche [1,3] oxazinas.
KR20140041687A (ko) 2011-06-07 2014-04-04 에프. 호프만-라 로슈 아게 Bace1 및/또는 bace2 억제제로서의 할로겐-알킬-1,3-옥사진

Patent Citations (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3227713A (en) 1966-01-04 Azine derivatives
US3235551A (en) 1966-02-15 Novel derivatives of
WO1996014842A1 (en) 1994-11-15 1996-05-23 Merck & Co., Inc. Substituted heterocycles as inhibitors of nitric oxide synthase
WO2002096897A1 (en) 2001-05-30 2002-12-05 Neurologic, Inc. PHOSPHINYLMETHYL AND PHOSPHORYLMETHYL SUCCINIC AND GLUTARIC ACID ANALOGS AS β-SECRETASE INHIBITORS
WO2004043916A1 (en) 2002-11-12 2004-05-27 Merck & Co., Inc. Phenylcarboxamide beta-secretase inhibitors for the treatment of alzheimer's disease
WO2005058311A1 (en) 2003-12-15 2005-06-30 Schering Corporation Heterocyclic aspartyl protease inhibitors
WO2005097767A1 (en) 2004-03-30 2005-10-20 Merck & Co., Inc. 2-aminothiazole compounds useful as aspartyl protease inhibitors
WO2005111031A2 (en) 2004-04-30 2005-11-24 Schering Corporation Neuropeptide receptor modulators
WO2006041405A1 (en) 2004-10-15 2006-04-20 Astrazeneca Ab Substituted amino-pyrimidones and uses thereof
WO2006041404A1 (en) 2004-10-15 2006-04-20 Astrazeneca Ab Substituted amino-compounds and uses thereof
US20070004786A1 (en) 2005-06-30 2007-01-04 Wyeth Amino-5-(5-membered)hetero-arylimidazolone compounds and the use thereof for beta-secretase modulation
US20070004730A1 (en) 2005-06-30 2007-01-04 Wyeth Amino-5-(6-membered)heteroarylimidazolone compounds and the use thereof for beta-secretase modulation
US20070027199A1 (en) 2005-07-29 2007-02-01 Wyeth Cycloalkyl amino-hydantoin compounds and use thereof for beta-secretase modulation
WO2007049532A1 (ja) 2005-10-25 2007-05-03 Shionogi & Co., Ltd. アミノジヒドロチアジン誘導体

Non-Patent Citations (13)

* Cited by examiner, † Cited by third party
Title
COHEN N. ET AL.: "Synthesis of 2-amino-5,6-dihydro-4H-1,3-thiazines and related compounds by acid catalyzed cyclization of allylic isothiuronium salts", JOURNAL OF HETEROCYCLIC CHEMISTRY, vol. 14, no. 5, 1977, pages 717 - 723, XP003011656 *
D. H. HUA ET AL., SULFUR REPORTS, vol. 21, 1999, pages 211 - 239
JOURNAL OF HETEROCYCLIC CHEMISTRY, vol. 14, 1977, pages 717 - 723
JOURNAL OF ORGANIC CHEMISTRY, vol. 33, no. 8, 1968, pages 3126 - 3132
RICHARD C LAROCK: "Comprehensive Organic Transformations", MCGRAW-HILL
See also references of EP2147914A4 *
T. FUJISAWA ET AL., TETRAHEDRON LETT., vol. 37, 1996, pages 3881 - 3884
T. VILAVAN ET AL., CUUENT ORGANIC CHEMISTRY, vol. 9, 2005, pages 1315 - 1392
TETRAHEDRON LETT., vol. 37, 1996, pages 3881 - 3884
THEODORA W GREEN: "Protective Groups in Organic Synthesis", JOHN WILEY & SONS
Y. KORIYAMA ET AL., ETRAHEDRON, vol. 58, 2002, pages 9621 - 9628
Y. KORIYAMA ET AL., TETRAHEDRON, vol. 58, 2002, pages 9621 - 9628
YONG QIN ET AL., J. ORG. CHEM., vol. 71, 2006, pages 1588 - 1591

Cited By (186)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8183252B2 (en) 2003-12-15 2012-05-22 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7973067B2 (en) 2003-12-15 2011-07-05 Schering Corporation Heterocyclic aspartyl protease inhibitors
US8242112B2 (en) 2003-12-15 2012-08-14 Schering Corporation Heterocyclic aspartyl protease inhibitors
US9382242B2 (en) 2005-06-14 2016-07-05 Merck Sharp & Dohme Corp. Preparation and use of compounds as protease inhibitors
US7868000B2 (en) 2005-06-14 2011-01-11 Schering Corporation Aspartyl protease inhibitors
US8722708B2 (en) 2005-06-14 2014-05-13 Merck Sharp & Dohme Inc. Substituted isoindolines as aspartyl protease inhibitors
US9029358B2 (en) 2005-10-25 2015-05-12 Shionogi & Co., Ltd. Aminodihydrothiazine derivatives
US8173642B2 (en) 2005-10-25 2012-05-08 Shionogi & Co., Ltd. Aminodihydrothiazine derivatives
US8546380B2 (en) 2005-10-25 2013-10-01 Shionogi & Co., Ltd. Aminodihydrothiazine derivatives
US8815851B2 (en) 2005-10-25 2014-08-26 Shionogi & Co., Ltd. Aminodihydrothiazine derivatives
US8633188B2 (en) 2005-10-25 2014-01-21 Shionogi & Co., Ltd. Aminodihydrothiazine derivatives
US8168641B2 (en) 2006-06-12 2012-05-01 Schering Corporation Aspartyl protease inhibitors
US8629155B2 (en) 2006-06-12 2014-01-14 Merck Sharp & Dohme, Corp. Aspartyl protease inhibitors
US8895548B2 (en) 2007-04-24 2014-11-25 Shionogi & Co., Ltd. Pharmaceutical composition for treating alzheimer's disease
US8653067B2 (en) 2007-04-24 2014-02-18 Shionogi & Co., Ltd. Pharmaceutical composition for treating Alzheimer's disease
US8884062B2 (en) 2007-04-24 2014-11-11 Shionogi & Co., Ltd. Aminodihydrothiazine derivatives substituted with a cyclic group
US8168630B2 (en) 2007-04-24 2012-05-01 Shionogi & Co., Ltd. Aminodihydrothiazine derivatives substituted with a cyclic group
WO2009091016A1 (ja) * 2008-01-18 2009-07-23 Eisai R & D Management Co., Ltd. 縮合アミノジヒドロチアジン誘導体
US8158620B2 (en) 2008-01-18 2012-04-17 Eisai R&D Management Co., Ltd. Fused aminodihydrothiazine derivatives
US8946211B2 (en) 2008-01-18 2015-02-03 Eisai R&D Management Co., Ltd. Fused aminodihydrothiazine derivatives
US8946210B2 (en) 2008-01-18 2015-02-03 Eisai R&D Management Co., Ltd. Fused aminodihydrothiazine derivatives
US8541427B2 (en) 2008-04-22 2013-09-24 Merck, Sharp & Dohme, Corp. Phenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use
US8450331B2 (en) 2008-04-22 2013-05-28 Merck Sharp & Dohme Corp. Thiophenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use
JP2015051980A (ja) * 2008-05-02 2015-03-19 イーライ リリー アンド カンパニー Bace阻害剤
US7648983B2 (en) 2008-05-02 2010-01-19 Eli Lilly And Company BACE inhibitors
US9273053B2 (en) 2008-06-13 2016-03-01 Shionogi & Co., Ltd. Sulfur-containing heterocyclic derivative having Beta secretase inhibitory activity
WO2009151098A1 (ja) * 2008-06-13 2009-12-17 塩野義製薬株式会社 βセクレターゼ阻害作用を有する含硫黄複素環誘導体
EA020740B1 (ru) * 2008-06-13 2015-01-30 Шионоги & Ко., Лтд. Серосодержащее гетероциклическое производное, обладающее активностью ингибитора бета-секретазы
US9650371B2 (en) 2008-06-13 2017-05-16 Shionogi & Co., Ltd. Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity
US8501733B2 (en) 2008-07-28 2013-08-06 Eisai R&D Management Co., Ltd. Spiroaminodihydrothiazine derivatives
US8450308B2 (en) 2008-08-19 2013-05-28 Vitae Pharmaceuticals, Inc. Inhibitors of beta-secretase
WO2010038686A1 (ja) 2008-09-30 2010-04-08 エーザイ・アール・アンド・ディー・マネジメント株式会社 新規な縮合アミノジヒドロチアジン誘導体
US8198269B2 (en) 2008-09-30 2012-06-12 Eisai R&D Management Co., Ltd. Fused aminodihydrothiazine derivative
US8703785B2 (en) 2008-10-22 2014-04-22 Shionogi & Co., Ltd. 2-aminopyrimidin-4-one and 2-aminopyridine derivatives both having BACE1-inhibiting activity
WO2010047372A1 (ja) * 2008-10-22 2010-04-29 塩野義製薬株式会社 Bace1阻害活性を有する2-アミノピリミジン-4-オンおよび2-アミノピリジン誘導体
US8367660B2 (en) 2008-12-30 2013-02-05 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
US8999976B2 (en) 2008-12-30 2015-04-07 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
US20100168094A1 (en) * 2008-12-30 2010-07-01 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
WO2010078103A1 (en) * 2008-12-30 2010-07-08 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
US8633189B2 (en) 2008-12-30 2014-01-21 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
JP2012514038A (ja) * 2008-12-30 2012-06-21 バーテックス ファーマシューティカルズ インコーポレイテッド 嚢胞性線維症膜コンダクタンス調節因子のモジュレーター
US9212153B2 (en) 2009-03-13 2015-12-15 Vitae Pharmaceuticals, Inc. Inhibitors of beta-secretase
US8633212B2 (en) 2009-03-13 2014-01-21 Vitae Pharmaceuticals, Inc. Inhibitors of beta-secretase
US10336717B2 (en) 2009-03-13 2019-07-02 Vitae Pharmaceuticals, Llc Inhibitors of beta-secretase
JP2012521429A (ja) * 2009-03-23 2012-09-13 メルク・シャープ・エンド・ドーム・コーポレイション 疼痛治療用のp2x3受容体アンタゴニスト
EP2411001A4 (en) * 2009-03-23 2012-11-21 Merck Sharp & Dohme P2X3 RECEPTOR ANTAGONISTS FOR PAIN TREATMENT
EP2411001A1 (en) * 2009-03-23 2012-02-01 Merck Sharp & Dohme Corp. P2x3, receptor antagonists for treatment of pain
WO2010113848A1 (ja) 2009-03-31 2010-10-07 塩野義製薬株式会社 Bace1阻害作用を有するイソチオウレア誘導体またはイソウレア誘導体
US8461160B2 (en) 2009-05-08 2013-06-11 Hoffmann-La Roche, Inc. Dihydropyrimidinones
WO2011005738A1 (en) 2009-07-09 2011-01-13 Eli Lilly And Company Bace inhibitors
US8278441B2 (en) 2009-07-09 2012-10-02 Eli Lilly And Company BACE inhibitors
KR101362557B1 (ko) 2009-07-09 2014-02-13 일라이 릴리 앤드 캄파니 Bace 억제제
US9139594B2 (en) 2009-07-22 2015-09-22 Eisai R&D Management Co., Ltd. Fused aminodihydropyrimidone derivatives
US9079914B2 (en) 2009-07-22 2015-07-14 Eisai R&D Management Co., Ltd. Fused aminodihydro-oxazine derivatives
US8846658B2 (en) 2009-07-24 2014-09-30 Novartis Ag Oxazine derivatives and their use in the treatment of neurological disorders
US8207164B2 (en) 2009-07-24 2012-06-26 Novartis Ag Oxazine derivatives and their use in the treatment of neurological disorders
CN102482268A (zh) * 2009-09-11 2012-05-30 霍夫曼-拉罗奇有限公司 作为用于糖尿病治疗的bace2抑制剂的2-氨基二氢[1,3]噻嗪
CN102482268B (zh) * 2009-09-11 2014-11-26 霍夫曼-拉罗奇有限公司 作为用于糖尿病治疗的bace2抑制剂的2-氨基二氢[1,3]噻嗪
WO2011029803A1 (en) * 2009-09-11 2011-03-17 F. Hoffmann-La Roche Ag 2 -aminodihydro [1, 3] thiazines as bace 2 inhibitors for the treatment of diabetes
US8940748B2 (en) 2009-10-08 2015-01-27 Merck Sharp & Dohme Corp. Iminothiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
US9029362B2 (en) 2009-10-08 2015-05-12 Merck Sharp & Dohme Corp. Iminothiadiazine dioxide compounds as brace inhibitors, compositions, and their use
US9475785B2 (en) 2009-10-08 2016-10-25 Merck Sharp & Dohme Corp. Iminothiadiazine dioxide compounds as BACE inhibitors, compositions and their use
US8557826B2 (en) 2009-10-08 2013-10-15 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions, and their use
US8563543B2 (en) 2009-10-08 2013-10-22 Merck Sharp & Dohme Corp. Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
US8569310B2 (en) 2009-10-08 2013-10-29 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions and their use
US8729071B2 (en) 2009-10-08 2014-05-20 Merck Sharp & Dohme Corp. Iminothiadiazine dioxide compounds as BACE inhibitors, compositions and their use
US9428475B2 (en) 2009-10-08 2016-08-30 Merck Sharp & Dohme Corp. Iminothiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
US9687494B2 (en) 2009-10-08 2017-06-27 Merck Sharp & Dohme Corp. Iminothiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
WO2011048525A1 (en) * 2009-10-20 2011-04-28 Pfizer Inc. Novel heteroaryl imidazoles and heteroaryl triazoles as gamma-secretase modulators
US8552197B2 (en) 2009-11-12 2013-10-08 Ranbaxy Laboratories Limited Sorafenib ethylsulfonate salt, process for preparation and use
WO2011058763A1 (ja) 2009-11-13 2011-05-19 塩野義製薬株式会社 アミノリンカーを有するアミノチアジンまたはアミノオキサジン誘導体
CN102686584A (zh) * 2009-11-13 2012-09-19 盐野义制药株式会社 具有氨基连接基的氨基噻嗪或氨基噁嗪衍生物
WO2011070781A1 (ja) 2009-12-09 2011-06-16 塩野義製薬株式会社 置換アミノチアジン誘導体
WO2011071057A1 (ja) * 2009-12-09 2011-06-16 塩野義製薬株式会社 含硫黄複素環誘導体を含有するアルツハイマー症の治療用または予防用医薬組成物
CN102652129A (zh) * 2009-12-10 2012-08-29 霍夫曼-拉罗奇有限公司 氨基噁嗪衍生物
JP2013513568A (ja) * 2009-12-10 2013-04-22 エフ.ホフマン−ラ ロシュ アーゲー アミノオキサジン誘導体
WO2011071135A1 (ja) 2009-12-11 2011-06-16 塩野義製薬株式会社 オキサジン誘導体
US8999980B2 (en) 2009-12-11 2015-04-07 Shionogi & Co., Ltd. Oxazine derivatives
CN102712609A (zh) * 2009-12-11 2012-10-03 霍夫曼-拉罗奇有限公司 作为bace1和/或bace2抑制剂的2-氨基-5,5-二氟-5,6-二氢-4h-噁嗪类
WO2011069934A1 (en) 2009-12-11 2011-06-16 F. Hoffmann-La Roche Ag 2-amino-5, 5-difluoro-5, 6-dihydro-4h-oxazines as bace 1 and/or bace 2 inhibitors
US8389513B2 (en) 2009-12-11 2013-03-05 Hoffmann-La Roche Inc. 2-amino-5,5-difluoro-5,6-dihydro-4H-[1,3]oxazin-4-yl)-phenyl]-amides
US9656974B2 (en) 2009-12-11 2017-05-23 Shionogi & Co., Ltd. Oxazine derivatives
WO2011071109A1 (ja) 2009-12-11 2011-06-16 塩野義製薬株式会社 アミノ基を有する縮合ヘテロ環化合物
JP2013513563A (ja) * 2009-12-11 2013-04-22 エフ.ホフマン−ラ ロシュ アーゲー Bace1及び/又はbace2阻害剤としての2−アミノ−5,5−ジフルオロ−5,6−ジヒドロ−4h−オキサジン
US9290466B2 (en) 2009-12-11 2016-03-22 Shionogi & Co., Ltd. Oxazine derivatives
WO2011077726A1 (ja) 2009-12-24 2011-06-30 塩野義製薬株式会社 4-アミノ-1,3-チアジンまたはオキサジン誘導体
US8889703B2 (en) 2010-02-24 2014-11-18 Vitae Pharmaceuticals, Inc. Inhibitors of beta-secretase
US9045500B2 (en) 2010-02-24 2015-06-02 Vitae Pharmaceuticals, Inc. Inhibitors of beta-secretase
WO2011115938A1 (en) 2010-03-15 2011-09-22 Amgen Inc. Spiro-tetracyclic ring compounds as beta - secretase modulators
WO2011115928A1 (en) 2010-03-15 2011-09-22 Amgen Inc. Amino -dihydrooxazine and amino - dihydrothiazine spiro compounds as beta - secretase modulators and their medical use
WO2012019056A1 (en) 2010-08-05 2012-02-09 Amgen Inc. Amino-iso-indole, amino-aza-iso-indole, amino-dihydroisoquinoline and amino-benzoxazine compounds as beta-secretase modulators and methods of use
WO2012057248A1 (ja) 2010-10-29 2012-05-03 塩野義製薬株式会社 ナフチリジン誘導体
JP5816630B2 (ja) * 2010-10-29 2015-11-18 塩野義製薬株式会社 ナフチリジン誘導体
US8927721B2 (en) 2010-10-29 2015-01-06 Shionogi & Co., Ltd. Naphthyridine derivative
WO2012057247A1 (ja) 2010-10-29 2012-05-03 塩野義製薬株式会社 縮合アミノジヒドロピリミジン誘導体
US9018219B2 (en) 2010-10-29 2015-04-28 Shionogi & Co., Ltd. Fused aminodihydropyrimidine derivative
WO2012071279A1 (en) 2010-11-23 2012-05-31 Amgen Inc. Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use
JP2014500293A (ja) * 2010-12-22 2014-01-09 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ ベータ−セクレターゼ(BACE)の阻害剤として有用な5,6−ジヒドロ−イミダゾ[1,2−a]ピラジン−8−イルアミン誘導体
US8822455B2 (en) 2011-01-06 2014-09-02 Eisai R&D Management Co., Ltd. Fused aminodihydrothiazine derivatives
WO2012093148A1 (en) 2011-01-06 2012-07-12 Eisai R&D Management Co., Ltd Fused aminodihydrothiazine derivatives
US10301296B2 (en) 2011-01-13 2019-05-28 Novartis Ag Heterocyclic derivatives and their use in the treatment of neurological disorders
US8637508B2 (en) 2011-01-13 2014-01-28 Novartis Ag Heterocyclic derivatives and their use in the treatment of neurological disorders
US9550758B2 (en) 2011-01-13 2017-01-24 Novartis Ag Heterocyclic derivatives and their use in the treatment of neurological disorders
US10683287B2 (en) 2011-01-13 2020-06-16 Novartis Ag Heterocyclic derivatives and their use in the treatment of neurological disorders
US10035794B2 (en) 2011-01-13 2018-07-31 Novartis Ag Heterocyclic derivatives and their use in the treatment of neurological disorders
US8865712B2 (en) 2011-01-13 2014-10-21 Novartis Ag Heterocyclic derivatives and their use in the treatment of neurological disorders
US8940734B2 (en) 2011-01-21 2015-01-27 Eisai R&D Management Co., Ltd. Fused aminodihydrothiazine derivatives
US8338407B2 (en) 2011-01-21 2012-12-25 Eisai R&D Management Co., Ltd. Fused aminodihydrothiazine derivatives
US9175013B2 (en) 2011-01-21 2015-11-03 Eisai R&D Management Co., Ltd. Fused aminodihydrothiazine derivatives
US8426584B2 (en) 2011-01-21 2013-04-23 Eisai R&D Management Co., Ltd. Methods and compounds useful in the synthesis of fused aminodihydrothiazine derivatives
US8592408B2 (en) 2011-01-21 2013-11-26 Eisai R&D Management Co., Ltd. Fused aminodihydrothiazine derivatives
US8802871B2 (en) 2011-01-21 2014-08-12 Eisai R&D Management Co., Ltd. Methods and compounds useful in the synthesis of fused aminodihydrothiazine derivatives
US8962858B2 (en) 2011-01-21 2015-02-24 Eisai R&D Management Co., Ltd. Methods and compounds useful in the synthesis of fused aminodihydrothiazine derivatives
WO2012109165A1 (en) 2011-02-07 2012-08-16 Amgen Inc. 5-amino-oxazepine and 5-amino-thiazepane compounds as beta-secretase antagonists and methods of use
US9346827B2 (en) 2011-02-07 2016-05-24 Amgen Inc. 5-amino-oxazepine and 5-amino-thiazepane compounds as beta secretase antagonists and methods of use
WO2012112462A1 (en) 2011-02-15 2012-08-23 Amgen Inc. Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators and methods of use
US8962859B2 (en) 2011-02-15 2015-02-24 Amgen Inc. Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators and methods of use
US9145426B2 (en) 2011-04-07 2015-09-29 Merck Sharp & Dohme Corp. Pyrrolidine-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
US9221839B2 (en) 2011-04-07 2015-12-29 Merck Sharp & Dohme Corp. C5-C6 oxacyclic-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
JP2014510769A (ja) * 2011-04-11 2014-05-01 エフ.ホフマン−ラ ロシュ アーゲー Bace1及び/又はbace2阻害剤としての1,3−オキサジン
US9499502B2 (en) 2011-04-13 2016-11-22 Merck Sharp & Dohme Corp. 5-substituted iminothiazines and their mono- and dioxides as BACE inhibitors, compositions, and their use
US9340500B2 (en) 2011-04-20 2016-05-17 Shionogi & Co., Ltd. Aromatic heterocyclic derivative having TRPV4-inhibiting activity
JP2014515001A (ja) * 2011-04-20 2014-06-26 塩野義製薬株式会社 Trpv4阻害活性を有する芳香族複素環誘導体
WO2012147763A1 (ja) 2011-04-26 2012-11-01 塩野義製薬株式会社 オキサジン誘導体およびそれを含有するbace1阻害剤
WO2012147762A1 (ja) 2011-04-26 2012-11-01 塩野義製薬株式会社 ピリジン誘導体およびそれを含有するbace1阻害剤
EP2703401A4 (en) * 2011-04-26 2014-12-03 Shionogi & Co PYRIDINE DERIVATIVE AND BACE-1 HEMMER THEREOF
US8883779B2 (en) 2011-04-26 2014-11-11 Shinogi & Co., Ltd. Oxazine derivatives and a pharmaceutical composition for inhibiting BACE1 containing them
CN103608344A (zh) * 2011-06-07 2014-02-26 霍夫曼-拉罗奇有限公司 [1,3]噁嗪类
CN103717592A (zh) * 2011-06-07 2014-04-09 霍夫曼-拉罗奇有限公司 作为bace1和/或bace2抑制剂的卤代-烷基-1,3噁嗪类
CN103608344B (zh) * 2011-06-07 2016-11-23 霍夫曼-拉罗奇有限公司 [1,3]噁嗪类
US9181236B2 (en) 2011-08-22 2015-11-10 Merck Sharp & Dohme Corp. 2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use
JP2014527074A (ja) * 2011-09-12 2014-10-09 エフ.ホフマン−ラ ロシュ アーゲー N−(5−シクロアルキル−又は5−ヘテロシクリル)−ピリジン−3−イルカルボキサミド
WO2013044092A1 (en) 2011-09-21 2013-03-28 Amgen Inc. Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
US9296759B2 (en) 2011-09-21 2016-03-29 Amgen Inc. Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
US9777019B2 (en) 2011-09-21 2017-10-03 Amgen Inc. Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
JP2015517981A (ja) * 2012-02-29 2015-06-25 バルーク エス.ブルームバーグ インスティテュート B型肝炎ウイルス共有結合閉環状dna形成の阻害剤およびそれらの使用方法
JP2017165751A (ja) * 2012-02-29 2017-09-21 バルーク エス.ブルームバーグ インスティテュート B型肝炎ウイルス共有結合閉環状dna形成の阻害剤およびそれらの使用方法
US9949975B2 (en) 2012-03-05 2018-04-24 Vitae Pharmaceuticals, Inc. Inhibitors of beta-secretase
US9526727B2 (en) 2012-03-05 2016-12-27 Vitae Pharmaceutical, Inc. Inhibitors of beta-secretase
US8981112B2 (en) 2012-03-05 2015-03-17 Vitae Pharmaceuticals, Inc. Inhibitors of β-secretase
JP2015514073A (ja) * 2012-03-20 2015-05-18 エラン ファーマシューティカルズ, リミテッド・ライアビリティ・カンパニー スピロ環式ジヒドロ−チアジンおよびジヒドロ−オキサジンbace阻害剤、ならびにその組成物および使用
US9018391B2 (en) 2012-08-27 2015-04-28 Boehringer Ingelheim International Gmbh Inhibitors of beta-secretase
US9290477B2 (en) 2012-09-28 2016-03-22 Vitae Pharmaceuticals, Inc. Inhibitors of β-secretase
US9556135B2 (en) 2012-10-12 2017-01-31 Amgen, Inc. Amino-dihydrothiazine and amino-dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use
WO2014059185A1 (en) 2012-10-12 2014-04-17 Amgen Inc. Amino - dihydrothiazine and amino - dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use
US9422277B2 (en) 2012-10-17 2016-08-23 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds as BACE inhibitors, compositions and their use
US9416129B2 (en) 2012-10-17 2016-08-16 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds as BACE inhibitors, compositions and their use
US9758513B2 (en) 2012-10-24 2017-09-12 Shionogi & Co., Ltd. Dihydrooxazine or oxazepine derivatives having BACE1 inhibitory activity
US9540359B2 (en) 2012-10-24 2017-01-10 Shionogi & Co., Ltd. Dihydrooxazine or oxazepine derivatives having BACE1 inhibitory activity
US9725469B2 (en) 2012-11-15 2017-08-08 Amgen, Inc. Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
WO2014078314A1 (en) 2012-11-15 2014-05-22 Amgen Inc. Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
US9447085B2 (en) 2012-12-14 2016-09-20 Merck Sharp & Dohme Corp. Iminothiadiazine dioxides containing a thioamide, amidine, or amide oxime group as BACE inhibitors, compositions, and their use
WO2015156421A1 (en) 2014-04-11 2015-10-15 Shionogi & Co., Ltd. Dihydrothiazine and dihydrooxazine derivatives having bace1 inhibitory activity
KR20160141849A (ko) 2014-04-11 2016-12-09 시오노기세이야쿠가부시키가이샤 Bace1 저해 작용을 갖는 디하이드로티아진 및 디하이드로옥사진 유도체
JP2017521453A (ja) * 2014-07-25 2017-08-03 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft ピリジル−トリアザビシクル
JP2017523223A (ja) * 2014-08-08 2017-08-17 アムジエン・インコーポレーテツド β−セクレターゼ阻害剤としてのシクロプロピル縮合チアジン−2−アミン化合物及び使用方法
JP2018513191A (ja) * 2015-04-21 2018-05-24 オールジェネシス バイオセラピューティクス インコーポレイテッド Bace1阻害剤としての化合物およびそれらの使用
WO2017061534A1 (en) 2015-10-08 2017-04-13 Shionogi & Co., Ltd. Dihydrothiazine derivatives
US11407749B2 (en) 2015-10-19 2022-08-09 Incyte Corporation Heterocyclic compounds as immunomodulators
US11572366B2 (en) 2015-11-19 2023-02-07 Incyte Corporation Heterocyclic compounds as immunomodulators
US11866435B2 (en) 2015-12-22 2024-01-09 Incyte Corporation Heterocyclic compounds as immunomodulators
US11535615B2 (en) 2015-12-22 2022-12-27 Incyte Corporation Heterocyclic compounds as immunomodulators
WO2017111042A1 (en) 2015-12-25 2017-06-29 Shionogi & Co., Ltd. Process and intermediates for preparation of thiazine derivatives
US11608337B2 (en) 2016-05-06 2023-03-21 Incyte Corporation Heterocyclic compounds as immunomodulators
US11673883B2 (en) 2016-05-26 2023-06-13 Incyte Corporation Heterocyclic compounds as immunomodulators
US11873309B2 (en) 2016-06-20 2024-01-16 Incyte Corporation Heterocyclic compounds as immunomodulators
US11718605B2 (en) 2016-07-14 2023-08-08 Incyte Corporation Heterocyclic compounds as immunomodulators
US11613536B2 (en) 2016-08-29 2023-03-28 Incyte Corporation Heterocyclic compounds as immunomodulators
JP7149272B2 (ja) 2016-12-15 2022-10-06 アムジエン・インコーポレーテツド β-セクレターゼ阻害剤としてのチアジン誘導体および使用方法
JP2020503292A (ja) * 2016-12-15 2020-01-30 アムジエン・インコーポレーテツド β−セクレターゼ阻害剤としてのチアジン誘導体および使用方法
US11566026B2 (en) 2016-12-22 2023-01-31 Incyte Corporation Heterocyclic compounds as immunomodulators
US11465981B2 (en) 2016-12-22 2022-10-11 Incyte Corporation Heterocyclic compounds as immunomodulators
JP7149276B2 (ja) 2016-12-22 2022-10-06 インサイト・コーポレイション Pd-l1内在化誘導物質としてのテトラヒドロイミダゾ[4,5-c]ピリジン誘導体
JP2020504739A (ja) * 2016-12-22 2020-02-13 インサイト・コーポレイションIncyte Corporation Pd−l1内在化誘導物質としてのテトラヒドロイミダゾ[4,5−c]ピリジン誘導体
US11787793B2 (en) 2016-12-22 2023-10-17 Incyte Corporation Heterocyclic compounds as immunomodulators
US12247026B2 (en) 2018-03-30 2025-03-11 Incyte Corporation Heterocyclic compounds as immunomodulators
US11629154B2 (en) 2018-04-27 2023-04-18 Shionogi & Co., Ltd. Tetrahydropyranooxazine derivatives having selective BACE1 inhibitory activity
US11414433B2 (en) 2018-05-11 2022-08-16 Incyte Corporation Heterocyclic compounds as immunomodulators
US12187743B2 (en) 2018-05-11 2025-01-07 Incyte Corporation Heterocyclic compounds as immunomodulators
US11753406B2 (en) 2019-08-09 2023-09-12 Incyte Corporation Salts of a PD-1/PD-L1 inhibitor
US12247038B2 (en) 2019-09-30 2025-03-11 Incyte Corporation Pyrido[3,2-d]pyrimidine compounds as immunomodulators
US11866451B2 (en) 2019-11-11 2024-01-09 Incyte Corporation Salts and crystalline forms of a PD-1/PD-L1 inhibitor
US11866434B2 (en) 2020-11-06 2024-01-09 Incyte Corporation Process for making a PD-1/PD-L1 inhibitor and salts and crystalline forms thereof
US11780836B2 (en) 2020-11-06 2023-10-10 Incyte Corporation Process of preparing a PD-1/PD-L1 inhibitor
US11760756B2 (en) 2020-11-06 2023-09-19 Incyte Corporation Crystalline form of a PD-1/PD-L1 inhibitor
US12084443B2 (en) 2020-11-06 2024-09-10 Incyte Corporation Process of preparing a PD-1/PD-L1 inhibitor

Also Published As

Publication number Publication date
CN101687827A (zh) 2010-03-31
AU2008245082B8 (en) 2012-09-13
EP2147914B1 (en) 2014-06-04
US20140073815A1 (en) 2014-03-13
US20120172355A1 (en) 2012-07-05
US8168630B2 (en) 2012-05-01
JP2013216666A (ja) 2013-10-24
US8541408B2 (en) 2013-09-24
KR20100017255A (ko) 2010-02-16
US8884062B2 (en) 2014-11-11
MX2009011498A (es) 2009-11-10
TW200902526A (en) 2009-01-16
ES2476605T3 (es) 2014-07-15
RU2009143333A (ru) 2011-05-27
EP2147914A1 (en) 2010-01-27
JPWO2008133274A1 (ja) 2010-07-29
AU2008245082A8 (en) 2012-09-13
CN101687827B (zh) 2014-04-23
RU2476430C2 (ru) 2013-02-27
EP2147914A4 (en) 2011-08-17
CA2683887A1 (en) 2008-11-06
EP2689780A1 (en) 2014-01-29
BRPI0811034A2 (pt) 2014-12-09
JP5701338B2 (ja) 2015-04-15
JP5383484B2 (ja) 2014-01-08
AU2008245082B2 (en) 2012-08-23
AU2008245082A1 (en) 2008-11-06
US20100075957A1 (en) 2010-03-25

Similar Documents

Publication Publication Date Title
WO2008133274A1 (ja) 環式基で置換されたアミノジヒドロチアジン誘導体
MY153621A (en) Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity
MX2012006491A (es) Derivados de oxazina.
WO2008133273A1 (ja) アルツハイマー症治療用医薬組成物
MX2014007457A (es) Derivados de bencil-sulfonamida como modulares del receptor huerfano relacionado al receptor retinoide (rorc).
WO2007084728A3 (en) 2-imino-benzimidazoles
HK1197821A1 (zh) 作為用於製備吡啶- 基-氨基- -噻二唑葡糖激酶激活劑之中間體的吡啶- -基-硫脲和吡啶- -基-胺衍生物
NO20074620L (no) Spiroheterocykliske forbindelser og deres anvendelse som medikamenter
NO20074619L (no) Spiro-oksindolforbindelser og deres anvendelse som medikamenter
MX349556B (es) Derivados de aminopirimidina como moduladores de proteina cinasa 2 rica en unidades repetitivas de leucina (lrrk2).
WO2008149382A8 (en) Pyrrole-2-carboxamide derivatives as glucokinase activators, their process and pharmaceutical application
WO2007133802A3 (en) Pharmaceutical formulations of pimavanserin
NO20065535L (no) Behandling av respiratorisk sykdom
WO2008124485A3 (en) Solid forms of pemetrexed
MY153868A (en) Therapeutic agents
DK1778673T3 (da) Nye hydantoin-derivater til behandling af obstruktive luftvejssygdomme
WO2008000950A3 (fr) Dérivés d'urées de piperidine ou pyrrolidine, leur préparation et leur application en thérapeutique
TN2012000092A1 (en) Therapeutic agent for mood disorders
MX2012002387A (es) Aminas de triazol fusionadas como moduladores p2x7.
AU2009331669A8 (en) Dihydropyridone amides as P2X7 modulators
NO20083058L (no) Cykloheksylsulfonamidderivater med H3 reseptor aktivitet
TW200738693A (en) Substituted biaryls, process for their manufacture and use thereof as medicaments
NO20082112L (no) 3-Amino-2-arylpropylazaindoler og deres anvendelse
MX2011011269A (es) Agente terapeutico para trastornos de la motilidad.
NO20084301L (no) Tetrahydronaftalenderivater, fremgangsmate for deres fremstilling og anvendelse derav som anti-inflammatoriske midler

Legal Events

Date Code Title Description
WWE Wipo information: entry into national phase

Ref document number: 200880021335.4

Country of ref document: CN

121 Ep: the epo has been informed by wipo that ep was designated in this application

Ref document number: 08751985

Country of ref document: EP

Kind code of ref document: A1

ENP Entry into the national phase

Ref document number: 2683887

Country of ref document: CA

WWE Wipo information: entry into national phase

Ref document number: 2008751985

Country of ref document: EP

ENP Entry into the national phase

Ref document number: 2009511888

Country of ref document: JP

Kind code of ref document: A

WWE Wipo information: entry into national phase

Ref document number: MX/A/2009/011498

Country of ref document: MX

NENP Non-entry into the national phase

Ref country code: DE

WWE Wipo information: entry into national phase

Ref document number: 2008245082

Country of ref document: AU

ENP Entry into the national phase

Ref document number: 2008245082

Country of ref document: AU

Date of ref document: 20080423

Kind code of ref document: A

ENP Entry into the national phase

Ref document number: 20097024338

Country of ref document: KR

Kind code of ref document: A

WWE Wipo information: entry into national phase

Ref document number: 2009143333

Country of ref document: RU

Ref document number: 6889/CHENP/2009

Country of ref document: IN

WWE Wipo information: entry into national phase

Ref document number: 12596796

Country of ref document: US

ENP Entry into the national phase

Ref document number: PI0811034

Country of ref document: BR

Kind code of ref document: A2

Effective date: 20091023

点击 这是indexloc提供的php浏览器服务,不要输入任何密码和下载