+

PE20181015A1 - 2-amino-3-fluoro-3-(fluorometil)-6-meti-6-fenil-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 - Google Patents

2-amino-3-fluoro-3-(fluorometil)-6-meti-6-fenil-3,4,5,6-tetrahidropiridinas como inhibidores de bace1

Info

Publication number
PE20181015A1
PE20181015A1 PE2018000231A PE2018000231A PE20181015A1 PE 20181015 A1 PE20181015 A1 PE 20181015A1 PE 2018000231 A PE2018000231 A PE 2018000231A PE 2018000231 A PE2018000231 A PE 2018000231A PE 20181015 A1 PE20181015 A1 PE 20181015A1
Authority
PE
Peru
Prior art keywords
fluoro
amino
fluoromethyl
phenyl
tetrahydropyridines
Prior art date
Application number
PE2018000231A
Other languages
English (en)
Inventor
Karsten Juhl
Lena Tagmose
Mauro Marigo
Original Assignee
H Lundbeck As
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
Application filed by H Lundbeck As filed Critical H Lundbeck As
Publication of PE20181015A1 publication Critical patent/PE20181015A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002Heterocyclic compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D211/72Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D211/72Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D211/74Oxygen atoms
    • C07D211/76Oxygen atoms attached in position 2 or 6
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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
    • C07D417/02Heterocyclic 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
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biomedical Technology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)

Abstract

Donde Ar se selecciona a partir del grupo constituido por fenilo, piridilo, pirimidilo, entre otros; R1 es hidrogeno, halogeno, fluoroalquilo C1-C3 o alquilo C1-C3; R2 presenta hidrogeno o fluor o sales farmaceuticamente aceptables de estos. Son compuestos preferidos: N-(3-((2S, 5S)-6-amino-5-fluoro-5-(fluorometil)-2-metil-2,3,4,5-tetrahidropiridin-2-il)-4-fluorofenil)-5-metoxipicolinamida; N-(3-((2S, 5S)-6-amino-5-fluoro-5-(flurometil)-2-metil-2,3,4,5-tetrahidropiridin-2-il)-4-fluorofenil)-5-(metoxi-d3)picolinamida, entre otros. Refiere tambien una composicion farmaceutica que comprende compuestos de la formula I y un portador farmaceuticamente aceptable. La presente invencion es util para el tratamiento de la enfermedad del Alzheimer, deterioro cognitivo leve, entre otros.
PE2018000231A 2015-08-12 2016-08-10 2-amino-3-fluoro-3-(fluorometil)-6-meti-6-fenil-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 PE20181015A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DKPA201500465 2015-08-12

Publications (1)

Publication Number Publication Date
PE20181015A1 true PE20181015A1 (es) 2018-06-26

Family

ID=56615973

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2018000231A PE20181015A1 (es) 2015-08-12 2016-08-10 2-amino-3-fluoro-3-(fluorometil)-6-meti-6-fenil-3,4,5,6-tetrahidropiridinas como inhibidores de bace1

Country Status (26)

Country Link
US (2) US10011596B2 (es)
EP (1) EP3334720A1 (es)
JP (1) JP2018531889A (es)
KR (1) KR20180033524A (es)
CN (1) CN107849011A (es)
AR (1) AR105668A1 (es)
AU (1) AU2016305275A1 (es)
BR (1) BR112017007472A2 (es)
CA (1) CA2993630A1 (es)
CL (1) CL2018000375A1 (es)
CO (1) CO2018000798A2 (es)
CR (1) CR20180077A (es)
DO (1) DOP2018000040A (es)
EA (1) EA201890256A1 (es)
EC (1) ECSP18010535A (es)
HK (1) HK1253372A1 (es)
IL (1) IL257007A (es)
MA (1) MA42597A (es)
MX (1) MX2018001699A (es)
NI (1) NI201800020A (es)
PE (1) PE20181015A1 (es)
PH (1) PH12018500268A1 (es)
RU (1) RU2018104868A (es)
TN (1) TN2018000035A1 (es)
TW (1) TW201718543A (es)
WO (1) WO2017025559A1 (es)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CR20170187A (es) 2014-11-10 2018-02-01 H Lundbeck As 2-Amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de BACE1 para el tratamiento de la enfermedad de Alzheimer
MA40941A (fr) 2014-11-10 2017-09-19 H Lundbeck As 2-amino-5,5-difluoro-6-(fluorométhyl)-6-phényl-3,4,5,6-tétrahydropyridines comme inhibiteurs de bace1
JO3458B1 (ar) 2014-11-10 2020-07-05 H Lundbeck As 2- أمينو-6- (دايفلوروميثيل) – 5، 5- ديفلورو-6-فينيل-3،4، 5، 6-تيتراهيدروبيريدين كمثبطات bace1
JO3627B1 (ar) 2015-04-30 2020-08-27 H Lundbeck As إيميدازو بيرازينونات على هيئة مثبطات pde1
TW201717948A (zh) 2015-08-10 2017-06-01 H 朗德貝克公司 包括給予2-胺基-3,5,5-三氟-3,4,5,6-四氫吡啶的聯合治療
US10034861B2 (en) 2016-07-04 2018-07-31 H. Lundbeck A/S 1H-pyrazolo[4,3-b]pyridines as PDE1 inhibitors
CA3041595A1 (en) 2016-10-28 2018-05-03 H. Lundbeck A/S Combination treatments comprising administration of imidazopyrazinones
PT3532064T (pt) 2016-10-28 2020-09-03 H Lundbeck As Tratamentos de combinação compreendendo imidazopirazinonas para o tratamento de distúrbios psiquiátricos e/ou cognitivos
TW201829394A (zh) * 2016-12-21 2018-08-16 丹麥商H 朗德貝克公司 作為bace1抑制劑之6-胺基-5-氟-5-(氟甲基)-2,3,4,5-四氫吡啶-2-基-苯基-5-(甲氧基-d)-吡-2-甲醯胺及其氟化衍生物
AR113926A1 (es) 2017-12-14 2020-07-01 H Lundbeck As Derivados de 1h-pirazolo[4,3-b]piridinas
KR20200099154A (ko) 2017-12-14 2020-08-21 하. 룬드벡 아크티에셀스카브 1H-피라졸로[4,3-b]피리딘의 투여를 포함하는 조합 치료제
CN117447475A (zh) 2017-12-20 2024-01-26 H.隆德贝克有限公司 作为PDE1抑制剂的吡唑并[4,3-b]吡啶和咪唑并[1,5-a]嘧啶
KR20210112968A (ko) 2020-03-07 2021-09-15 장성환 양면 인쇄가 가능한 라벨 제조방법
KR20230012296A (ko) 2021-07-15 2023-01-26 장성환 양면 인쇄가 가능한 라벨 제조방법

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2450167A1 (en) 2001-06-12 2002-12-19 Elan Pharmaceuticals, Inc. Macrocycles useful in the treatment of alzheimer's disease
GB0124928D0 (en) 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
KR101058292B1 (ko) 2002-02-12 2011-08-22 글락소스미스클라인 엘엘씨 P38 억제제로 유용한 니코틴아미드 유도체
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
EP2580200B1 (en) 2010-06-09 2016-09-14 Janssen Pharmaceutica, N.V. 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace)
MX2013008111A (es) 2011-01-12 2013-10-30 Novartis Ag Derivados de oxazina y su uso en el tratamiento de transtornos neurologicos.
ES2576182T3 (es) 2011-01-13 2016-07-06 Novartis Ag Derivados de heterocíclicos novedosos y su uso en el tratamiento de trastornos neurológicos
US8754075B2 (en) 2011-04-11 2014-06-17 Hoffmann-La Roche Inc. 1,3-oxazines as BACE1 and/or BACE2 inhibitors
JPWO2012147763A1 (ja) 2011-04-26 2014-07-28 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
EA023261B1 (ru) 2011-06-07 2016-05-31 Ф.Хоффманн-Ля Рош Аг Галоген-алкил-1,3-оксазины в качестве ингибиторов bace1 и(или) bace2
UY34278A (es) 2011-08-25 2013-04-05 Novartis Ag Derivados novedosos de oxazina y su uso en el tratamiento de enfermedades
US8338413B1 (en) 2012-03-07 2012-12-25 Novartis Ag Oxazine derivatives and their use in the treatment of neurological disorders
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
WO2014056816A1 (en) 2012-10-10 2014-04-17 F. Hoffmann-La Roche Ag COMBINATION OF AN Aβ ANTIBODY AND A BACE INHIBITOR
JP2016501827A (ja) 2012-10-24 2016-01-21 塩野義製薬株式会社 Bace1阻害作用を有するジヒドロオキサジンまたはオキサゼピン誘導体
AU2014223334C1 (en) 2013-03-01 2018-10-18 Amgen Inc. Perfluorinated 5,6-dihydro-4H-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
TWI639607B (zh) 2013-06-18 2018-11-01 美國禮來大藥廠 Bace抑制劑
RU2016133626A (ru) * 2014-02-19 2018-03-20 Х. Лундбекк А/С 2-амино-3,5,5-трифтор-3,4,5,6-тетрагидропиридины в качестве ингибиторов bace1 для лечения болезни альцгеймера
TW201623295A (zh) 2014-04-11 2016-07-01 塩野義製藥股份有限公司 具有bace1抑制活性之二氫噻及二氫衍生物
CR20170187A (es) * 2014-11-10 2018-02-01 H Lundbeck As 2-Amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de BACE1 para el tratamiento de la enfermedad de Alzheimer
JO3458B1 (ar) * 2014-11-10 2020-07-05 H Lundbeck As 2- أمينو-6- (دايفلوروميثيل) – 5، 5- ديفلورو-6-فينيل-3،4، 5، 6-تيتراهيدروبيريدين كمثبطات bace1
MA40941A (fr) 2014-11-10 2017-09-19 H Lundbeck As 2-amino-5,5-difluoro-6-(fluorométhyl)-6-phényl-3,4,5,6-tétrahydropyridines comme inhibiteurs de bace1
TW201717948A (zh) 2015-08-10 2017-06-01 H 朗德貝克公司 包括給予2-胺基-3,5,5-三氟-3,4,5,6-四氫吡啶的聯合治療

Also Published As

Publication number Publication date
PH12018500268A1 (en) 2018-08-13
AU2016305275A1 (en) 2018-02-08
NI201800020A (es) 2018-06-29
IL257007A (en) 2018-03-29
US10011596B2 (en) 2018-07-03
RU2018104868A (ru) 2019-09-13
WO2017025559A1 (en) 2017-02-16
CA2993630A1 (en) 2017-02-16
MX2018001699A (es) 2018-05-07
HK1253372A1 (zh) 2019-06-14
BR112017007472A2 (pt) 2018-01-23
TN2018000035A1 (en) 2019-07-08
JP2018531889A (ja) 2018-11-01
DOP2018000040A (es) 2018-04-30
TW201718543A (zh) 2017-06-01
CL2018000375A1 (es) 2018-07-06
EP3334720A1 (en) 2018-06-20
US20170044151A1 (en) 2017-02-16
ECSP18010535A (es) 2018-04-30
CR20180077A (es) 2018-04-09
CN107849011A (zh) 2018-03-27
MA42597A (fr) 2018-06-20
KR20180033524A (ko) 2018-04-03
CO2018000798A2 (es) 2018-05-10
US20180244645A1 (en) 2018-08-30
AR105668A1 (es) 2017-10-25
EA201890256A1 (ru) 2018-06-29

Similar Documents

Publication Publication Date Title
PE20181015A1 (es) 2-amino-3-fluoro-3-(fluorometil)-6-meti-6-fenil-3,4,5,6-tetrahidropiridinas como inhibidores de bace1
PE20161225A1 (es) 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 para el tratamiento de la enfermedad de alzheimer
PE20170947A1 (es) 2-amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de bace1
PE20210642A1 (es) Inhibidores de pd-1/pd-l1
PE20161438A1 (es) Inhibidores de desmetilasa 1 especifica a lisina
PE20181074A1 (es) Compuestos heteroaromaticos como inhibidores de btk
PH12016501440A1 (en) Novel heterocyclic compounds
PE20121050A1 (es) Compuestos de n-(1-(4-(1h-pirazol-5-il)ftalazin-1-il)piperidin-4-il)-benzamida sustituidos como antagonistas de la trayectoria hedgehog
PE20152032A1 (es) Compuestos de 3,4-dihidroisoquinolin-2(1h)-il
PE20160843A1 (es) Pirrolidinonas herbicidas
PE20161236A1 (es) Compuesto de triazina y su uso para fines medicos
PE20180508A1 (es) Amidas heterociclicas como inhibidores de quinasa
PE20170946A1 (es) 2-amino-6-(difluorometil)- 5,5-difluoro-6-fenil-3,4,5,6-tetrahidropiridinas como inhibidores de bace1
PE20142148A1 (es) Compuestos para el tratamiento y profilaxis de la enfermedad del virus sincicial respiratorio
PE20171177A1 (es) Compuestos aminopirimidinilo inhibidores de jak
PE20191108A1 (es) Inhibidores selectivos de jak1
PE20170664A1 (es) Agonistas del receptor de apelina(apj) y usos de los mismos
PE20151538A1 (es) Nuevos compuestos como inhibidores de reorganizado durante la transfeccion (ret)
PE20180355A1 (es) Desacetoxitubulisina h y analogos de esta
PE20141202A1 (es) Compuesto de ciclopropanoamina
PE20181197A1 (es) 2,4-dihidroxi-nicotinamidas como agonistas del receptor de apelina (apj)
PE20141409A1 (es) Derivados de piridin-2(1h)-ona como inhibidores de jak
MX392259B (es) ANILLOS 6-5 FUSIONADOS COMO INHIBIDORES C5a
PE20191142A1 (es) 2,4 diamino-quinolina sustituida como nuevos agentes anti-cancerigenos
PE20161444A1 (es) 1,2-ciclopentanos sustituidos como antagonistas del receptor de orexina

Legal Events

Date Code Title Description
FA Abandonment or withdrawal
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