AU2014315113B2 - 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
AU2014315113B2
AU2014315113B2 AU2014315113A AU2014315113A AU2014315113B2 AU 2014315113 B2 AU2014315113 B2 AU 2014315113B2 AU 2014315113 A AU2014315113 A AU 2014315113A AU 2014315113 A AU2014315113 A AU 2014315113A AU 2014315113 B2 AU2014315113 B2 AU 2014315113B2
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ric
hydrocarbyl
halo
cyano
optionally substituted
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AU2014315113A1 (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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    • 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)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (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)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
AU2014315113A 2013-09-06 2014-09-05 Pyrazolo[1,5-a]pyrimidine-based compounds, compositions comprising them, and methods of their use Active AU2014315113B2 (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
AU2014315113A1 AU2014315113A1 (en) 2016-03-10
AU2014315113B2 true AU2014315113B2 (en) 2018-10-04

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AU2014315113A Active AU2014315113B2 (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)

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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)

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US9737542B2 (en) 2013-10-11 2017-08-22 Bristol-Myers Squibb Company Pyrrolotriazine kinase inhibitors
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
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
EP3215509B1 (en) 2014-11-06 2020-02-26 Lysosomal Therapeutics Inc. Substituted pyrrolo[1,2-a]pyrimidines and their use in the treatment of medical disorders
BR112018070586A8 (pt) 2016-04-06 2023-03-14 Lysosomal Therapeutics Inc Compostos de pirazol[1,5-a]pirimidinil carboxamida e seu uso no tratamento de distúrbios médicos
WO2017176962A1 (en) 2016-04-06 2017-10-12 Lysosomal Therapeutics, Inc. Pyrrolo[1,2-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders
JP7046827B2 (ja) 2016-04-06 2022-04-04 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 イミダゾ［１，５－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
CN109311902B (zh) 2016-05-05 2022-07-15 Bial研发投资股份有限公司 取代的咪唑并[1,2-b]哒嗪、咪唑并[1,5-b]哒嗪、相关化合物及其用途
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

Citations (6)

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WO2003091256A1 (en) * 2002-04-23 2003-11-06 Shionogi & Co., Ltd. PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVE AND NAD(P)H OXIDASE INHIBITOR CONTAINING THE SAME
WO2007039439A1 (en) * 2005-09-27 2007-04-12 F.Hoffmann-La Roche Ag Oxadiazolyl pyrazolo-pyrimidines as mglur2 antagonists
WO2008138889A2 (en) * 2007-05-11 2008-11-20 Novartis Ag 3, 6-disubstituted-imidazo [1, 2-b] pyridazines and 3, 5-disubstituted pyrazolo[1, 5-a] pyrimidines as phosphatidylinositol-3-kinase inhibitors
WO2012156756A2 (en) * 2011-05-19 2012-11-22 Centro Nacional De Investigaciones Oncológicas (Cnio) New compounds
WO2013134336A2 (en) * 2012-03-09 2013-09-12 Lexicon Pharmaceuticals, Inc. Inhibition of adaptor associated kinase 1 for the treatment of pain
WO2013147711A1 (en) * 2012-03-30 2013-10-03 Agency For Science, Technology And Research Bicyclic heterocyclic derivatives as mnk1 and mnk2 modulators and uses thereof

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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
US7329662B2 (en) 2003-10-03 2008-02-12 Hoffmann-La Roche Inc. Pyrazolo-pyridine
PT1863818E (pt) 2005-03-23 2010-04-09 Hoffmann La Roche Derivados de acetilenil-pirazolo-pirimidina 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
RU2009120389A (ru) * 2006-10-30 2010-12-10 Новартис АГ (CH) Гетероциклические соединения в качестве противовоспалительных агентов
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
EP2350071B1 (en) * 2008-10-22 2014-01-08 Array Biopharma, Inc. SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS TRK KINASE INHIBITORS
MX2011012369A (es) * 2009-05-20 2012-03-16 Cylene Pharmaceuticals Inc Pirazolopirimidinas y heterociclos relacionados como inhibidores de cinasa.
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
US8946237B2 (en) * 2010-01-14 2015-02-03 Merck Sharp & Dohme Corp. Pyrazolo[1,5-A]pyrimidines as mark inhibitors
WO2013134228A1 (en) * 2012-03-09 2013-09-12 Lexicon Pharmaceuticals, Inc. PYRAZOLO[1,5-a]PYRIMIDINE-BASED COMPOUNDS, COMPOSITIONS COMPRISING THEM, AND METHODS OF THEIR USE

Patent Citations (6)

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Publication number Priority date Publication date Assignee Title
WO2003091256A1 (en) * 2002-04-23 2003-11-06 Shionogi & Co., Ltd. PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVE AND NAD(P)H OXIDASE INHIBITOR CONTAINING THE SAME
WO2007039439A1 (en) * 2005-09-27 2007-04-12 F.Hoffmann-La Roche Ag Oxadiazolyl pyrazolo-pyrimidines as mglur2 antagonists
WO2008138889A2 (en) * 2007-05-11 2008-11-20 Novartis Ag 3, 6-disubstituted-imidazo [1, 2-b] pyridazines and 3, 5-disubstituted pyrazolo[1, 5-a] pyrimidines as phosphatidylinositol-3-kinase inhibitors
WO2012156756A2 (en) * 2011-05-19 2012-11-22 Centro Nacional De Investigaciones Oncológicas (Cnio) New compounds
WO2013134336A2 (en) * 2012-03-09 2013-09-12 Lexicon Pharmaceuticals, Inc. Inhibition of adaptor associated kinase 1 for the treatment of pain
WO2013147711A1 (en) * 2012-03-30 2013-10-03 Agency For Science, Technology And Research Bicyclic heterocyclic derivatives as mnk1 and mnk2 modulators and uses thereof

Also Published As

Publication number Publication date
CN105517553A (zh) 2016-04-20
US9862724B2 (en) 2018-01-09
DK3041475T3 (da) 2024-12-02
PT3041475T (pt) 2025-01-07
EP3041475A1 (en) 2016-07-13
CN105517553B (zh) 2020-03-27
JP6472450B2 (ja) 2019-02-20
US20150175610A1 (en) 2015-06-25
CA2923317C (en) 2023-04-04
HK1217658A1 (zh) 2017-01-20
WO2015035117A1 (en) 2015-03-12
EP3041475B1 (en) 2024-10-09
AR097545A1 (es) 2016-03-23
US20170081330A1 (en) 2017-03-23
JP2016529315A (ja) 2016-09-23
TW201542550A (zh) 2015-11-16
ES3009382T3 (en) 2025-03-26
AU2014315113A1 (en) 2016-03-10
CA2923317A1 (en) 2015-03-12

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DA3 Amendments made section 104

Free format text: THE NATURE OF THE AMENDMENT IS: AMEND THE NAME OF THE INVENTOR TO READ BI, YINGZHI; GARDYAN, MICHAEL WALTER; GREEN, MICHAEL ALAN; KUMI, GODWIN AND ZHANG, YULIAN

FGA Letters patent sealed or granted (standard patent)