CA2923317C - Pyrazolo[1,5-a]pyrimidine-based compounds, compositions comprising them, and methods of their use - Google Patents

Pyrazolo[1,5-a]pyrimidine-based compounds, compositions comprising them, and methods of their use Download PDF

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Publication number
CA2923317C
CA2923317C CA2923317A CA2923317A CA2923317C CA 2923317 C CA2923317 C CA 2923317C CA 2923317 A CA2923317 A CA 2923317A CA 2923317 A CA2923317 A CA 2923317A CA 2923317 C CA2923317 C CA 2923317C
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Prior art keywords
compound
hydrocarbyl
disease
pyrazolo
ric
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CA2923317A
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English (en)
French (fr)
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CA2923317A1 (en
Inventor
Yingzhi Bi
Michael Walter Gardyan
Michael Alan Green
Godwin KUMI
Yulian Zhang
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Lexicon Pharmaceuticals Inc
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Lexicon Pharmaceuticals Inc
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Publication of CA2923317A1 publication Critical patent/CA2923317A1/en
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    • 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
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic 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
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/24—Antidepressants
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CA2923317A 2013-09-06 2014-09-05 Pyrazolo[1,5-a]pyrimidine-based compounds, compositions comprising them, and methods of their use Active CA2923317C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361874395P 2013-09-06 2013-09-06
US61/874,395 2013-09-06
PCT/US2014/054209 WO2015035117A1 (en) 2013-09-06 2014-09-05 PYRAZOLO[1,5-a]PYRIMIDINE-BASED COMPOUNDS, COMPOSITIONS COMPRISING THEM, AND METHODS OF THEIR USE

Publications (2)

Publication Number Publication Date
CA2923317A1 CA2923317A1 (en) 2015-03-12
CA2923317C true CA2923317C (en) 2023-04-04

Family

ID=51542502

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2923317A Active CA2923317C (en) 2013-09-06 2014-09-05 Pyrazolo[1,5-a]pyrimidine-based compounds, compositions comprising them, and methods of their use

Country Status (12)

Country Link
US (2) US20150175610A1 (https=)
EP (1) EP3041475B1 (https=)
JP (1) JP6472450B2 (https=)
CN (1) CN105517553B (https=)
AR (1) AR097545A1 (https=)
AU (1) AU2014315113B2 (https=)
CA (1) CA2923317C (https=)
DK (1) DK3041475T3 (https=)
ES (1) ES3009382T3 (https=)
PT (1) PT3041475T (https=)
TW (1) TW201542550A (https=)
WO (1) WO2015035117A1 (https=)

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EP3054955B1 (en) 2013-10-11 2018-05-30 Bristol-Myers Squibb Company Pyrrolotriazine kinase inhibitors
US20180185368A1 (en) 2014-11-06 2018-07-05 Lysosomal Therapeutics Inc. Substituted pyrrolo[1,2-a]pyrimidines and their use in the treatment of medical disorders
EP4406616A3 (en) 2014-11-06 2024-11-06 Bial-R&D Investments, S.A. Substituted pyrazolo(1,5-a)pyrimidines and their use in the treatment of medical disorders
US20170333435A1 (en) 2014-11-06 2017-11-23 Lysosomal Therapeutics Inc. Substituted imidazo[1,5-a]pyrimidines and their use in the treatment of medical disorders
AU2017246455B2 (en) 2016-04-06 2021-09-30 Bial - R&D Investments, S.A. Pyrazolo[1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders
EP3440081A4 (en) 2016-04-06 2019-09-18 Lysosomal Therapeutics Inc. PYRROLO [1,2-A] PYRIMIDINYL-CARBOXAMIDE COMPOUNDS AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDER
CA3020305A1 (en) 2016-04-06 2017-10-12 Lysosomal Therapeutics Inc. Imidazo [1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders
KR102530515B1 (ko) 2016-05-05 2023-05-09 비알 - 알&디 인베스트먼츠, 에스.에이. 치환된 이미다조[1,2-b]피리다진, 치환된 이미다조[1,5-b]피리다진, 관련 화합물, 및 의학적 장애의 치료에서의 그의 용도
WO2017192931A1 (en) 2016-05-05 2017-11-09 Lysosomal Therapeutics Inc. SUBSTITUTED IMDAZO[1,2-α]PYRIDINES, SUBSTITUTED IMIDAZO[1,2-α]PYRAZINES, RELATED COMPOUNDS, AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS
CN113271940A (zh) * 2018-10-15 2021-08-17 林伯士拉克许米公司 Tyk2抑制剂和其用途

Family Cites Families (22)

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US5464764A (en) 1989-08-22 1995-11-07 University Of Utah Research Foundation Positive-negative selection methods and vectors
WO1993004169A1 (en) 1991-08-20 1993-03-04 Genpharm International, Inc. Gene targeting in animal cells using isogenic dna constructs
US6194410B1 (en) * 1998-03-11 2001-02-27 Hoffman-La Roche Inc. Pyrazolopyrimidine and pyrazolines and process for preparation thereof
US7662826B2 (en) * 2002-04-23 2010-02-16 Shionogi & Co., Ltd. Pyrazolo [1,5-a] pyrimidine derivative and nad (p) h oxidase inhibitor containing the same
US7329662B2 (en) 2003-10-03 2008-02-12 Hoffmann-La Roche Inc. Pyrazolo-pyridine
WO2006099972A1 (en) 2005-03-23 2006-09-28 F. Hoffmann-La Roche Ag Acetylenyl-pyrazolo-pvrimidine derivatives as mglur2 antagonists
JP5048675B2 (ja) 2005-09-27 2012-10-17 エフ．ホフマン−ラ ロシュ アーゲー ｍＧｌｕＲ２アンタゴニストとしてのオキサジアゾリルピラゾロ−ピリミジン類
JP4847275B2 (ja) * 2005-10-21 2011-12-28 田辺三菱製薬株式会社 ピラゾロ［１，５−ａ］ピリミジン化合物
WO2008045664A2 (en) * 2006-10-06 2008-04-17 Kalypsys, Inc. Heterocyclic pde4 inhibitors as antiinflammatory agents
JP2010508315A (ja) * 2006-10-30 2010-03-18 ノバルティス アーゲー 抗炎症剤としてのヘテロ環式化合物
AR067326A1 (es) * 2007-05-11 2009-10-07 Novartis Ag Imidazopiridinas y pirrolo -pirimidinas sustituidas como inhibidores de cinasa de lipido
KR101324804B1 (ko) * 2008-05-13 2013-11-01 아이알엠 엘엘씨 키나제 억제제로서의 질소 함유 융합 헤테로사이클 및 그의 조성물
TWI491610B (zh) * 2008-10-09 2015-07-11 必治妥美雅史谷比公司 作為激酶抑制劑之咪唑并嗒腈
MY169791A (en) * 2008-10-22 2019-05-15 Array Biopharma Inc Substituted pyrazolo [1,5-a] pyrimidine compounds as trk kinase inhibitors
WO2010135581A1 (en) 2009-05-20 2010-11-25 Cylene Pharmaceuticals, Inc. Pyrazolopyrimidines and related heterocycles as kinase inhibitors
AR077468A1 (es) * 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
WO2011073316A1 (en) * 2009-12-18 2011-06-23 Novartis Ag 4-aryl-butane-1,3-diamides
WO2011087999A1 (en) * 2010-01-14 2011-07-21 Merck Sharp & Dohme Corp. Pyrazolo[1,5-a]pyrimidines as mark inhibitors
PL2710018T3 (pl) * 2011-05-19 2022-04-04 Fundación Del Sector Público Estatal Centro Nacional De Investigaciones Oncológicas Carlos III (F.S.P. CNIO) Związki makrocykliczne jako inhibitory kinaz białkowych
CN104302649B (zh) * 2012-03-09 2017-06-23 莱西肯医药有限公司 基于吡唑并[1,5‑a]嘧啶的化合物、包含它们的组合物及其使用方法
DK2822555T3 (en) 2012-03-09 2018-02-05 Lexicon Pharmaceuticals Inc Inhibition of adapter-associated kinase 1 for the treatment of pain
GB201205669D0 (en) * 2012-03-30 2012-05-16 Agency Science Tech & Res Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof

Also Published As

Publication number Publication date
PT3041475T (pt) 2025-01-07
CN105517553B (zh) 2020-03-27
US20150175610A1 (en) 2015-06-25
TW201542550A (zh) 2015-11-16
US20170081330A1 (en) 2017-03-23
AU2014315113A1 (en) 2016-03-10
AR097545A1 (es) 2016-03-23
EP3041475B1 (en) 2024-10-09
CN105517553A (zh) 2016-04-20
HK1217658A1 (zh) 2017-01-20
ES3009382T3 (en) 2025-03-26
JP2016529315A (ja) 2016-09-23
CA2923317A1 (en) 2015-03-12
AU2014315113B2 (en) 2018-10-04
DK3041475T3 (da) 2024-12-02
JP6472450B2 (ja) 2019-02-20
EP3041475A1 (en) 2016-07-13
US9862724B2 (en) 2018-01-09
WO2015035117A1 (en) 2015-03-12

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