MX2023006715A - Proceso para la preparacion de (9s)-n-[3-(6-metilpirimidin-4-il)-3 -azabiciclo[3.2.1]octan-8-il]-9-(2,3,4-trifluorofenil)-6,7,8,9-te trahidro-5h-[1,2,4]triazolo[1,5-a]azepin-2-amina y su forma solida. - Google Patents

Proceso para la preparacion de (9s)-n-[3-(6-metilpirimidin-4-il)-3 -azabiciclo[3.2.1]octan-8-il]-9-(2,3,4-trifluorofenil)-6,7,8,9-te trahidro-5h-[1,2,4]triazolo[1,5-a]azepin-2-amina y su forma solida.

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Publication number
MX2023006715A
MX2023006715A MX2023006715A MX2023006715A MX2023006715A MX 2023006715 A MX2023006715 A MX 2023006715A MX 2023006715 A MX2023006715 A MX 2023006715A MX 2023006715 A MX2023006715 A MX 2023006715A MX 2023006715 A MX2023006715 A MX 2023006715A
Authority
MX
Mexico
Prior art keywords
preparation
solid form
azepin
methylpyrimidin
octan
Prior art date
Application number
MX2023006715A
Other languages
English (en)
Inventor
Guocai Zhang
Weichun Chen
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of MX2023006715A publication Critical patent/MX2023006715A/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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

Abstract

La presente invención se refiere al proceso para la preparación de un compuesto (I), y su forma sólida, que es un modulador de ?-secretasa y puede ser útil para la profilaxis y el tratamiento de una enfermedad asociada al depósito de ß-amiloide en el cerebro, en particular la enfermedad de Alzheimer, y otras enfermedades, tales como angiopatía amiloide cerebral, hemorragia cerebral hereditaria con amiloidosis, tipo holandés (HCHWA-D), demencia multiinfarto, demencia pugilística y síndrome de Down.
MX2023006715A 2020-12-11 2021-12-09 Proceso para la preparacion de (9s)-n-[3-(6-metilpirimidin-4-il)-3 -azabiciclo[3.2.1]octan-8-il]-9-(2,3,4-trifluorofenil)-6,7,8,9-te trahidro-5h-[1,2,4]triazolo[1,5-a]azepin-2-amina y su forma solida. MX2023006715A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN2020135740 2020-12-11
PCT/EP2021/084887 WO2022122864A1 (en) 2020-12-11 2021-12-09 Process for the preparation of (9s)-n-[3-(6-methylpyrimidin-4-yl)-3-azabicyclo[3.2.1]octan-8-yl]-9-(2,3,4-trifluorophenyl)-6,7,8,9-tetrahydro-5h-[1,2,4]triazolo[1,5-a]azepin-2-amine and its solid form

Publications (1)

Publication Number Publication Date
MX2023006715A true MX2023006715A (es) 2023-06-23

Family

ID=79092930

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2023006715A MX2023006715A (es) 2020-12-11 2021-12-09 Proceso para la preparacion de (9s)-n-[3-(6-metilpirimidin-4-il)-3 -azabiciclo[3.2.1]octan-8-il]-9-(2,3,4-trifluorofenil)-6,7,8,9-te trahidro-5h-[1,2,4]triazolo[1,5-a]azepin-2-amina y su forma solida.

Country Status (12)

Country Link
US (1) US20240018143A1 (es)
EP (1) EP4259630A1 (es)
JP (1) JP2023553051A (es)
KR (1) KR20230118102A (es)
CN (1) CN116685589A (es)
AR (1) AR124194A1 (es)
AU (1) AU2021393968A1 (es)
CA (1) CA3199042A1 (es)
IL (1) IL303507A (es)
MX (1) MX2023006715A (es)
TW (1) TW202235076A (es)
WO (1) WO2022122864A1 (es)

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2512840T3 (es) 2010-01-15 2014-10-24 Janssen Pharmaceuticals, Inc. Derivados de triazol bicíclicos sustituidos novedosos como moduladores de gamma-secretasa
JP6980751B2 (ja) * 2016-07-14 2021-12-15 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft 縮合ピリミジン誘導体
AR109829A1 (es) 2016-09-29 2019-01-30 Hoffmann La Roche Derivados de piperidina puenteados
AR110001A1 (es) 2016-11-01 2019-02-13 Hoffmann La Roche Derivados heteroarilo bicíclicos
JP7335248B2 (ja) 2018-01-22 2023-08-29 エフ. ホフマン-ラ ロシュ アーゲー トリアゾロ-アゼピン誘導体
IL283994B2 (en) 2018-12-27 2024-05-01 Hoffmann La Roche Process for preparing exo-tert-butyl N-(3-azabicyclo[3.2.1]octane-8-YL)carbamate
JP2023503509A (ja) * 2019-11-29 2023-01-30 エフ.ホフマン-ラ ロシュ アーゲー (9S)-2-ブロモ-9-(2,3,4-トリフルオロフェニル)-6,7,8,9-テトラヒドロ-5H-[1,2,4]トリアゾロ[1,5-a]アゼピンの製造方法

Also Published As

Publication number Publication date
KR20230118102A (ko) 2023-08-10
CA3199042A1 (en) 2022-06-16
US20240018143A1 (en) 2024-01-18
EP4259630A1 (en) 2023-10-18
WO2022122864A1 (en) 2022-06-16
TW202235076A (zh) 2022-09-16
JP2023553051A (ja) 2023-12-20
CN116685589A (zh) 2023-09-01
AR124194A1 (es) 2023-02-22
IL303507A (en) 2023-08-01
AU2021393968A1 (en) 2023-05-11

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