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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    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (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 (enExample)
EP (1) EP3041475B1 (enExample)
JP (1) JP6472450B2 (enExample)
CN (1) CN105517553B (enExample)
AR (1) AR097545A1 (enExample)
AU (1) AU2014315113B2 (enExample)
CA (1) CA2923317C (enExample)
DK (1) DK3041475T3 (enExample)
ES (1) ES3009382T3 (enExample)
PT (1) PT3041475T (enExample)
TW (1) TW201542550A (enExample)
WO (1) WO2015035117A1 (enExample)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
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ES2678877T3 (es) 2013-10-11 2018-08-20 Bristol-Myers Squibb Company Inhibidores de pirrolotriazina quinasa
KR102662215B1 (ko) 2014-11-06 2024-05-02 비알 - 알&디 인베스트먼츠, 에스.에이. 치환된 피라졸로(1,5-a)피리미딘 및 의학적 장애의 치료에서의 그의 용도
WO2016073891A1 (en) 2014-11-06 2016-05-12 Lysosomal Therapeutics Inc. Substituted pyrrolo[1,2-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
US11192892B2 (en) 2016-04-06 2021-12-07 Bial—R&D Investments, S.A. Substituted pyrazolo[1,5-a]pyrimidines for the treatment of medical disorders
JP7034935B2 (ja) 2016-04-06 2022-03-14 リソソーマル・セラピューティクス・インコーポレイテッド ピロロ[1,2-a]ピリミジニルカルボキサミド化合物および医学的障害の処置におけるその使用
WO2017176961A1 (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
WO2017192930A1 (en) 2016-05-05 2017-11-09 Lysosomal Therapeutics Inc. SUBSTITUTED IMIDAZO[1,2-b]PYRIDAZINES, SUBSTITUTED IMIDAZO[1,5-b]PYRIDAZINES, RELATED COMPOUNDS, AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS
US11345698B2 (en) 2016-05-05 2022-05-31 Bial—R&D Investments, S.A. Substituted imidazo[1,2-a]pyridines, substituted imidazo[1,2-a]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
AU2515992A (en) 1991-08-20 1993-03-16 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
CN100343255C (zh) * 2002-04-23 2007-10-17 盐野义制药株式会社 吡唑并[1,5-a]嘧啶衍生物和含有该衍生物的NAD(P)H氧化酶抑制剂
US7329662B2 (en) * 2003-10-03 2008-02-12 Hoffmann-La Roche Inc. Pyrazolo-pyridine
EP1863818B1 (en) 2005-03-23 2010-03-10 F.Hoffmann-La Roche Ag Acetylenyl-pyrazolo-pvrimidine derivatives as mglur2 antagonists
ES2340321T3 (es) 2005-09-27 2010-06-01 F.Hoffmann-La Roche Ag Oxadiazolilpirazolo-pirimidinas, como antagonistas de mglur2.
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
US20090275586A1 (en) 2006-10-06 2009-11-05 Kalypsys, Inc. Heterocyclic inhibitors of pde4
CA2667962A1 (en) * 2006-10-30 2008-05-08 Novartis Ag Heterocyclic compounds as antiinflammatory agents
AR067326A1 (es) * 2007-05-11 2009-10-07 Novartis Ag Imidazopiridinas y pirrolo -pirimidinas sustituidas como inhibidores de cinasa de lipido
WO2009140128A2 (en) * 2008-05-13 2009-11-19 Irm Llc Compounds and compositions as kinase inhibitors
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
SG196855A1 (en) * 2008-10-22 2014-02-13 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
EP2523552B1 (en) * 2010-01-14 2015-05-13 Merck Sharp & Dohme Corp. Pyrazolo[1,5-a]pyrimidines as mark inhibitors
US9284334B2 (en) * 2011-05-19 2016-03-15 Fundación Centro Nacional De Investigaciones Oncologicas Carlos Iii Macrocyclic compounds as protein kinase inhibitors
HUE036040T2 (hu) 2012-03-09 2018-06-28 Lexicon Pharmaceuticals Inc Adaptor-asszociált kináz 1 gátlása fájdalom kezelésére
RU2014140735A (ru) 2012-03-09 2016-04-27 Лексикон Фармасьютикалз, Инк. ПРОИЗВОДНЫЕ ПИРАЗОЛО[1, 5-a]ПИРИМИДИНА, КОМПОЗИЦИИ, СОДЕРЖАЩИЕ УКАЗАННЫЕ СОЕДИНЕНИЯ, И СПОСОБЫ ИХ ПРИМЕНЕНИЯ
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
JP2016529315A (ja) 2016-09-23
CN105517553A (zh) 2016-04-20
CN105517553B (zh) 2020-03-27
TW201542550A (zh) 2015-11-16
WO2015035117A1 (en) 2015-03-12
EP3041475B1 (en) 2024-10-09
AU2014315113B2 (en) 2018-10-04
PT3041475T (pt) 2025-01-07
CA2923317A1 (en) 2015-03-12
US20150175610A1 (en) 2015-06-25
HK1217658A1 (zh) 2017-01-20
DK3041475T3 (da) 2024-12-02
US9862724B2 (en) 2018-01-09
EP3041475A1 (en) 2016-07-13
ES3009382T3 (en) 2025-03-26
AU2014315113A1 (en) 2016-03-10
JP6472450B2 (ja) 2019-02-20
US20170081330A1 (en) 2017-03-23
AR097545A1 (es) 2016-03-23

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