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 PDFInfo
- 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
Links
- VNTNANCAPVJRJP-UHFFFAOYSA-N 3,4-dihydrothiazin-2-amine Chemical group NN1CCC=CS1 VNTNANCAPVJRJP-UHFFFAOYSA-N 0.000 title 1
- 125000004122 cyclic group Chemical group 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 102000013455 Amyloid beta-Peptides Human genes 0.000 abstract 1
- 108010090849 Amyloid beta-Peptides Proteins 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 125000002837 carbocyclic group Chemical group 0.000 abstract 1
- 230000008021 deposition Effects 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 230000028327 secretion Effects 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
- C07C215/02—Compounds 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
- C07C215/04—Compounds 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
- C07C215/20—Compounds 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
- A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
- C07D279/04—1,3-Thiazines; Hydrogenated 1,3-thiazines
- C07D279/06—1,3-Thiazines; Hydrogenated 1,3-thiazines not condensed with other rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic 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
- C07D417/02—Heterocyclic 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
- C07D417/12—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic 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
- C07D417/14—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic 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
- C07D471/02—Heterocyclic 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
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic 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
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic 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
- C07D495/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic 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
- C07D513/02—Heterocyclic 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
- C07D513/04—Ortho-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
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)
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)
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)
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)
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 |
-
2008
- 2008-04-23 KR KR1020097024338A patent/KR20100017255A/ko not_active Ceased
- 2008-04-23 CA CA002683887A patent/CA2683887A1/en not_active Abandoned
- 2008-04-23 BR BRPI0811034-4A2A patent/BRPI0811034A2/pt not_active IP Right Cessation
- 2008-04-23 JP JP2009511888A patent/JP5383484B2/ja not_active Expired - Fee Related
- 2008-04-23 TW TW097114828A patent/TW200902526A/zh unknown
- 2008-04-23 CN CN200880021335.4A patent/CN101687827B/zh not_active Expired - Fee Related
- 2008-04-23 EP EP08751985.6A patent/EP2147914B1/en not_active Not-in-force
- 2008-04-23 ES ES08751985.6T patent/ES2476605T3/es active Active
- 2008-04-23 EP EP20130174492 patent/EP2689780A1/en not_active Withdrawn
- 2008-04-23 AU AU2008245082A patent/AU2008245082B8/en not_active Ceased
- 2008-04-23 MX MX2009011498A patent/MX2009011498A/es active IP Right Grant
- 2008-04-23 US US12/596,796 patent/US8168630B2/en not_active Expired - Fee Related
- 2008-04-23 RU RU2009143333/04A patent/RU2476430C2/ru not_active IP Right Cessation
- 2008-04-23 WO PCT/JP2008/057847 patent/WO2008133274A1/ja active Application Filing
-
2012
- 2012-03-12 US US13/417,786 patent/US8541408B2/en not_active Expired - Fee Related
-
2013
- 2013-05-06 US US13/887,745 patent/US8884062B2/en not_active Expired - Fee Related
- 2013-06-07 JP JP2013121172A patent/JP5701338B2/ja not_active Expired - Fee Related
Patent Citations (14)
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)
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 |
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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 |
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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 |
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