CN112424197B - 作为gaba受体调节剂的二氟甲基-苯基三唑类 - Google Patents

作为gaba受体调节剂的二氟甲基-苯基三唑类 Download PDF

Info

Publication number
CN112424197B
CN112424197B CN201980047952.XA CN201980047952A CN112424197B CN 112424197 B CN112424197 B CN 112424197B CN 201980047952 A CN201980047952 A CN 201980047952A CN 112424197 B CN112424197 B CN 112424197B
Authority
CN
China
Prior art keywords
alkyl
pain
disorder
group
halogen
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
CN201980047952.XA
Other languages
English (en)
Chinese (zh)
Other versions
CN112424197A (zh
Inventor
J·S·拉森
F·宾德尔
Y·崔
O·胡克
R·利平斯基
F·蒙特尔
M·奥斯特迈尔
A·佩雷拉
S·彼得斯
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Boehringer Ingelheim International GmbH
Original Assignee
Boehringer Ingelheim International GmbH
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 Boehringer Ingelheim International GmbH filed Critical Boehringer Ingelheim International GmbH
Publication of CN112424197A publication Critical patent/CN112424197A/zh
Application granted granted Critical
Publication of CN112424197B publication Critical patent/CN112424197B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201980047952.XA 2018-07-20 2019-07-19 作为gaba受体调节剂的二氟甲基-苯基三唑类 Active CN112424197B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP18184716.1 2018-07-20
EP18184716 2018-07-20
PCT/EP2019/069593 WO2020016443A1 (en) 2018-07-20 2019-07-19 Difluoromethyl-phenyl triazoles as gaba receptor modulators

Publications (2)

Publication Number Publication Date
CN112424197A CN112424197A (zh) 2021-02-26
CN112424197B true CN112424197B (zh) 2025-04-22

Family

ID=63014393

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201980047952.XA Active CN112424197B (zh) 2018-07-20 2019-07-19 作为gaba受体调节剂的二氟甲基-苯基三唑类

Country Status (8)

Country Link
US (2) US10941137B2 (https=)
EP (1) EP3823967B1 (https=)
JP (1) JP7311583B2 (https=)
CN (1) CN112424197B (https=)
AR (1) AR117615A1 (https=)
BR (1) BR102019014802A2 (https=)
TW (1) TW202019915A (https=)
WO (1) WO2020016443A1 (https=)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI901650B (zh) * 2020-03-26 2025-10-21 匈牙利商羅特格登公司 啶及吡啶并〔３，４－ｃ〕嗒衍生物
EP4149933B1 (en) * 2020-05-13 2024-06-12 F. Hoffmann-La Roche AG New triazolyl derivatives as gaba a alpha5 pam
EP3950683A1 (en) * 2020-08-05 2022-02-09 Boehringer Ingelheim International GmbH Difluoromethyl-pyridin-2-yl triazoles
ES3061465T3 (en) * 2020-08-05 2026-04-06 Saniona As Difluoromethyl-pyridin-2-yl triazoles
EP3971179A1 (en) * 2020-09-22 2022-03-23 Boehringer Ingelheim International GmbH Difluoromethyl-pyridin-2-yl triazoles
EP3992188A1 (en) * 2020-10-29 2022-05-04 Boehringer Ingelheim International GmbH Difluoromethyl-pyridin-2-yl triazoles
AU2022327398A1 (en) * 2021-08-12 2024-03-21 Shanghai SIMR Biotechnology Co., Ltd Substituted triazole derivative, preparation method therefor, pharmaceutical composition thereof, and use thereof
HU231691B1 (hu) 2021-09-29 2025-10-28 Richter Gedeon Nyrt GABAA ALFA5 receptor modulátor hatású biciklusos aminszármazékok
CN116462664B (zh) * 2022-03-08 2025-07-01 上海赛默罗生物科技有限公司 吡唑环类化合物、其制备方法、组合物及应用
CN116854680A (zh) * 2022-03-28 2023-10-10 上海赛默罗生物科技有限公司 异噁唑-杂环类衍生物、药物组合物和用途
CN119080754A (zh) * 2023-06-05 2024-12-06 武汉人福创新药物研发中心有限公司 作为α5-GABAA受体调节剂的杂环化合物及其用途

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101868458A (zh) * 2007-12-04 2010-10-20 弗·哈夫曼-拉罗切有限公司 异*唑并-哒嗪衍生物
WO2014001278A1 (en) * 2012-06-26 2014-01-03 Aniona Aps A phenyl triazole derivative and its use for modulating the gabaa receptor complex

Family Cites Families (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101263139A (zh) 2005-09-19 2008-09-10 弗·哈夫曼-拉罗切有限公司 作为GABA Aα5逆激动剂的异唑衍生物
AU2006301376A1 (en) 2005-10-11 2007-04-19 F. Hoffmann-La Roche Ag Isoxazole derivatives
ES2341131T3 (es) 2005-11-09 2010-06-15 F.Hoffmann-La Roche Ag Derivados de 3-aril-isoxazol-4-carbonil-benzofurano.
JP5015172B2 (ja) 2005-12-23 2012-08-29 エフ．ホフマン−ラ ロシュ アーゲー アリール−イソオキサゾロ−４−イル−オキサジアゾール誘導体
WO2007074089A1 (en) 2005-12-27 2007-07-05 F. Hoffmann-La Roche Ag Aryl-isoxazol-4-yl-imidazo[1, 5-a]pyridine derivatives
ATE527255T1 (de) 2005-12-27 2011-10-15 Hoffmann La Roche Aryl-isoxazol-4-yl-imidazol-derivate
TW200812982A (en) 2006-05-24 2008-03-16 Lilly Co Eli Compounds and methods for modulating FXR
AU2007267183B2 (en) 2006-05-31 2011-10-20 F. Hoffmann-La Roche Ag Aryl-4-ethynyl-isoxazole derivatives
EP1894924A1 (en) 2006-08-29 2008-03-05 Phenex Pharmaceuticals AG Heterocyclic FXR binding compounds
EP1894928A1 (en) 2006-08-29 2008-03-05 PheneX Pharmaceuticals AG Heterocyclic fxr binding compounds
MX2009014001A (es) 2007-06-22 2010-01-28 Hoffmann La Roche Derivados de isoxazol-imidazol.
KR101175859B1 (ko) 2007-12-04 2012-08-24 에프. 호프만-라 로슈 아게 이속사졸로-피라진 유도체
KR101237576B1 (ko) 2007-12-04 2013-03-04 에프. 호프만-라 로슈 아게 아이속사졸로-피리딘 유도체
EP2128158A1 (en) 2008-05-26 2009-12-02 Phenex Pharmaceuticals AG Heterocyclic cyclopropyl-substituted FXR binding compounds
US8389550B2 (en) 2009-02-25 2013-03-05 Hoffmann-La Roche Inc. Isoxazoles / O-pyridines with ethyl and ethenyl linker
US8222246B2 (en) 2009-04-02 2012-07-17 Hoffmann-La Roche Inc. Substituted isoxazoles
US20100280019A1 (en) 2009-04-30 2010-11-04 Roland Jakob-Roetne Isoxazoles
KR101367012B1 (ko) 2009-05-05 2014-03-14 에프. 호프만-라 로슈 아게 이속사졸-피리딘 유도체
CA2760597C (en) 2009-05-05 2017-08-22 F. Hoffmann-La Roche Ag Isoxazole-pyridazine derivatives
CA2759598C (en) 2009-05-05 2017-09-12 F. Hoffmann-La Roche Ag Isoxazole-thiazole derivatives as gaba a receptor inverse agonists for use in the treatment of cognitive disorders
JP5460858B2 (ja) 2009-05-05 2014-04-02 エフ．ホフマン−ラ ロシュ アーゲー イソオキサゾール−ピラゾール誘導体
BRPI1013766A2 (pt) 2009-05-07 2016-04-05 Hoffmann La Roche "derivados de isoxazol-piridina como moduladores de gaba"
EP2289883A1 (en) 2009-08-19 2011-03-02 Phenex Pharmaceuticals AG Novel FXR (NR1H4) binding and activity modulating compounds
MX341471B (es) 2010-11-05 2016-08-22 Hoffmann La Roche Uso de compuestos farmaceuticos activos para el tratamiento de estados patologicos del sistema nervioso central.
KR20130100348A (ko) * 2010-11-09 2013-09-10 에프. 호프만-라 로슈 아게 Gaba 수용체에 대한 리간드로서의 트라이아졸 유도체
US8742097B2 (en) * 2010-11-09 2014-06-03 Hoffmann-La Roche Inc. Triazole compounds I
JP2014122161A (ja) 2011-03-31 2014-07-03 Astellas Pharma Inc ピラゾール化合物
CA2876780A1 (en) * 2012-06-26 2014-01-03 Saniona Aps A phenyl triazole derivative and its use for modulating the gabaa receptor complex
WO2014001281A1 (en) 2012-06-26 2014-01-03 Aniona Aps A phenyl triazole derivative and its use for modulating the gabaa receptor complex
WO2014001280A1 (en) * 2012-06-26 2014-01-03 Aniona Aps A phenyl triazole derivative and its use for modulating the gabaa receptor complex
BR112019006571A2 (pt) 2016-12-08 2019-07-02 F. Hoffmann-La Roche Ag derivados de éter de isoxazolila como gaba a alfa5 pam

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101868458A (zh) * 2007-12-04 2010-10-20 弗·哈夫曼-拉罗切有限公司 异*唑并-哒嗪衍生物
WO2014001278A1 (en) * 2012-06-26 2014-01-03 Aniona Aps A phenyl triazole derivative and its use for modulating the gabaa receptor complex

Also Published As

Publication number Publication date
US10941137B2 (en) 2021-03-09
JP7311583B2 (ja) 2023-07-19
US20200024261A1 (en) 2020-01-23
EP3823967B1 (en) 2022-08-31
WO2020016443A1 (en) 2020-01-23
AR117615A1 (es) 2021-08-18
TW202019915A (zh) 2020-06-01
EP3823967A1 (en) 2021-05-26
CN112424197A (zh) 2021-02-26
US20210147393A1 (en) 2021-05-20
JP2021531291A (ja) 2021-11-18
BR102019014802A2 (pt) 2020-02-04

Similar Documents

Publication Publication Date Title
CN112424197B (zh) 作为gaba受体调节剂的二氟甲基-苯基三唑类
CN116888115B (zh) 二氟甲基-吡啶-2-基三唑
MX2013011107A (es) Derivados de pirazolidin-3-ona.
EP1960391A1 (en) Piperazine derivatives and their use in therapy
US10421750B2 (en) Substituted morpholine derivatives having activity against pain
US10689398B2 (en) OXA-Diazaspiro compounds having activity against pain
TWI915398B (zh) 二氟甲基-吡啶-2-基三唑
CN105612154A (zh) 作为詹纳斯激酶的抑制剂的n-氰基甲基酰胺
HK40129488A (en) Difluoromethyl-pyridin-2-yl triazoles
US20190315726A1 (en) Multi-substituted pyrimidine derivatives with excellent kinase inhibitory activities
EP3971179A1 (en) Difluoromethyl-pyridin-2-yl triazoles
EP3992188A1 (en) Difluoromethyl-pyridin-2-yl triazoles
EP3950683A1 (en) Difluoromethyl-pyridin-2-yl triazoles
US20160060275A1 (en) Tricyclic triazolic compounds

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant
TG01 Patent term adjustment
TG01 Patent term adjustment