CN104302649B - 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 - Google Patents

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 Download PDF

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CN104302649B
CN104302649B CN201380012483.0A CN201380012483A CN104302649B CN 104302649 B CN104302649 B CN 104302649B CN 201380012483 A CN201380012483 A CN 201380012483A CN 104302649 B CN104302649 B CN 104302649B
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pyrimidin
mmol
pyrazolo
compound
piperazine
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CN104302649A (zh
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毕映枝
肯尼斯·戈登·卡森
吉奥范尼·钱凯塔
迈克尔·爱伦·格林
戈德温·库米
爱伦·梅恩
张玉莲
格伦·格雷戈里·齐普
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Lexicon Pharmaceuticals Inc
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Lexicon Genetics Inc
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    • 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
    • A61P25/28Drugs 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002Heterocyclic compounds

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201380012483.0A 2012-03-09 2013-03-05 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 Active CN104302649B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261608765P 2012-03-09 2012-03-09
US61/608,765 2012-03-09
PCT/US2013/029056 WO2013134228A1 (en) 2012-03-09 2013-03-05 PYRAZOLO[1,5-a]PYRIMIDINE-BASED COMPOUNDS, COMPOSITIONS COMPRISING THEM, AND METHODS OF THEIR USE

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CN104302649A CN104302649A (zh) 2015-01-21
CN104302649B true CN104302649B (zh) 2017-06-23

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IL (1) IL234486A (enExample)
IN (1) IN2014DN07384A (enExample)
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NZ (1) NZ630721A (enExample)
PL (1) PL2834243T3 (enExample)
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RU (1) RU2014140735A (enExample)
SG (1) SG11201405561RA (enExample)
TR (1) TR201808280T4 (enExample)
TW (1) TW201341386A (enExample)
UY (1) UY34668A (enExample)
WO (1) WO2013134228A1 (enExample)
ZA (1) ZA201406149B (enExample)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX381849B (es) 2012-03-09 2025-03-13 Lexicon Pharmaceuticals Inc Compuestos a base de pirazol[1,5-a]pirimidina, composiciones que los comprenden, y métodos para su uso.
EP2822559B1 (en) 2012-03-09 2018-05-02 Lexicon Pharmaceuticals, Inc. Imidazo[1,2-b]pyridazine-based compounds, compositions comprising them, and uses thereof
US8901305B2 (en) 2012-07-31 2014-12-02 Bristol-Myers Squibb Company Aryl lactam kinase inhibitors
US9708337B2 (en) 2013-02-22 2017-07-18 Bristol-Myers Squibb Company Aryl amide-based kinase inhibitors
TW201542550A (zh) * 2013-09-06 2015-11-16 Lexicon Pharmaceuticals Inc 吡唑并[1,5-a]嘧啶基化合物、包含彼之組合物以及使用彼之方法
EP3054955B1 (en) 2013-10-11 2018-05-30 Bristol-Myers Squibb Company Pyrrolotriazine kinase inhibitors
WO2015112806A2 (en) 2014-01-24 2015-07-30 Tp Therapeutics, Inc. Diaryl macrocycles as modulators of protein kinases
EA201691397A1 (ru) * 2014-01-31 2016-11-30 Бристол-Майерс Сквибб Компани Хинолиновые ингибиторы киназы
TW201620911A (zh) * 2014-03-17 2016-06-16 雷西肯製藥股份有限公司 銜接子關聯激酶1之抑制劑、包含其之組成物、及其使用方法
US20170239249A1 (en) * 2014-09-30 2017-08-24 Bristol-Myers Squibb Company Quinazoline-based kinase inhibitors
PL3233863T3 (pl) * 2014-12-15 2024-11-12 Cmg Pharmaceutical Co., Ltd. Związki heteroarylowe ze skondensowanymi pierścieniami i ich zastosowanie jako inhibitorów trk
US10174044B2 (en) 2015-04-10 2019-01-08 Bristol-Myers Squibb Company Fused pyridines as kinase inhibitors
ES2864839T3 (es) 2015-07-02 2021-10-14 Turning Point Therapeutics Inc Macrociclos de diarilo quirales como moduladores de proteína quinasas
ES2979111T3 (es) 2015-07-06 2024-09-24 Turning Point Therapeutics Inc Polimorfo de macrociclo de diarilo
MX383823B (es) 2015-07-21 2025-03-14 Turning Point Therapeutics Inc Macrociclos de diarilo quirales y usos de los mismo.
HK1256751A1 (zh) 2015-11-02 2019-10-04 Janssen Pharmaceutica Nv [1,2,4]三唑并[1,5-a]嘧啶-7-基化合物
CN109715165A (zh) 2016-07-28 2019-05-03 Tp生物医药公司 巨环激酶抑制剂
ES2912264T3 (es) 2016-11-02 2022-05-25 Janssen Pharmaceutica Nv Compuestos de [1,2,4]triazolo[1,5-a]pirimidina como inhibidores de PDE2
EA039102B1 (ru) 2016-11-02 2021-12-03 Янссен Фармацевтика Нв Соединения [1,2,4]триазоло[1,5-a]пиримидина в качестве ингибиторов pde2
TWI764950B (zh) * 2016-11-02 2022-05-21 比利時商健生藥品公司 Pde2抑制劑
TWI808958B (zh) 2017-01-25 2023-07-21 美商特普醫葯公司 涉及二芳基巨環化合物之組合療法
US11046698B2 (en) 2017-07-28 2021-06-29 Nimbus Lakshmi, Inc. TYK2 inhibitors and uses thereof
MY201925A (en) 2017-07-28 2024-03-23 Turning Point Therapeutics Inc Macrocyclic compounds and uses thereof
AU2018383571B2 (en) * 2017-12-15 2023-09-21 Pyramid Biosciences, Inc. 5-(2-(2,5-difluorophenyl)pyrrolidin-1 -yl)-3-(1H-pyrazol-1-yl)pyrazolo(1,5-a)pyrimidine derivatives and related compounds as Trk kinase inhibitors for treating cancer
JP7194188B2 (ja) 2017-12-19 2022-12-21 ターニング・ポイント・セラピューティクス・インコーポレイテッド 疾患を治療するための大環状化合物
WO2019120194A1 (zh) * 2017-12-22 2019-06-27 深圳市塔吉瑞生物医药有限公司 一种取代的吡唑并[1,5-a]嘧啶化合物及其药物组合物及用途
CN109575025B (zh) 2018-01-23 2020-09-11 深圳市塔吉瑞生物医药有限公司 取代的吡唑并[1,5-a]嘧啶类的大环化合物
WO2020063751A1 (en) * 2018-09-27 2020-04-02 Fochon Pharmaceuticals, Ltd. Substituted imidazo [1, 2-a] pyridine and [1, 2, 4] triazolo [1, 5-a] pyridine compounds as ret kinase inhibitors
US11414431B2 (en) * 2018-10-15 2022-08-16 Nimbus Lakshmi, Inc. Substituted pyrazolo[1,5-a]pyrimidines as TYK2 inhibitors
EP4138844A1 (en) 2020-04-21 2023-03-01 Lexicon Pharmaceuticals, Inc. 4-(3-(pyridin-3-yl)pyrazolo[1,5-a]pyrimidin-5-yl)piperazine for use in the the treatment of cov-229e or cov-oc43 coronaviruses infections
EP4138829A1 (en) 2020-04-21 2023-03-01 Lexicon Pharmaceuticals, Inc. Aak1 inhibitors for use in treating viral infections
US11478733B2 (en) 2020-11-24 2022-10-25 Caterpillar Inc. Filter interlock with tabs mating with a pedestal or a housing
TW202525819A (zh) * 2023-09-08 2025-07-01 加拿大商薩泰洛斯生物科學公司 Ap2相關激酶1抑制劑及其用途

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1236780A (zh) * 1998-03-11 1999-12-01 弗·哈夫曼-拉罗切有限公司 吡唑并嘧啶和吡唑并三嗪
WO2011087999A1 (en) * 2010-01-14 2011-07-21 Merck Sharp & Dohme Corp. Pyrazolo[1,5-a]pyrimidines as mark inhibitors

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
KR20090073121A (ko) 2006-09-29 2009-07-02 노파르티스 아게 Pi3k 지질 키나제 억제제로서의 피라졸로피리미딘
US20120058997A1 (en) * 2006-11-06 2012-03-08 Supergen, Inc. Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors
BRPI0912668A2 (pt) * 2008-05-13 2016-01-26 Irm Llc composto e composições como inibidores de quinase
KR101853026B1 (ko) * 2008-10-22 2018-04-27 어레이 바이오파마 인크. TRK 키나아제 억제제로서 치환된 피라졸로[1,5­a] 피리미딘 화합물
AR077468A1 (es) * 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
TW201113286A (en) 2009-09-03 2011-04-16 Array Biopharma Inc Substituted pyrazolo[1,5-a]pyrimidine compounds as mTOR inhibitors
EP3409278B8 (en) * 2011-07-21 2020-11-04 Sumitomo Dainippon Pharma Oncology, Inc. Heterocyclic protein kinase inhibitors
MX381849B (es) 2012-03-09 2025-03-13 Lexicon Pharmaceuticals Inc Compuestos a base de pirazol[1,5-a]pirimidina, composiciones que los comprenden, y métodos para su uso.
HK1199814A1 (en) * 2012-03-09 2015-07-24 Lexicon Pharmaceuticals, Inc. Inhibition of adaptor associated kinase 1 for the treatment of pain
EP2822559B1 (en) 2012-03-09 2018-05-02 Lexicon Pharmaceuticals, Inc. Imidazo[1,2-b]pyridazine-based compounds, compositions comprising them, and uses thereof
TW201620911A (zh) * 2014-03-17 2016-06-16 雷西肯製藥股份有限公司 銜接子關聯激酶1之抑制劑、包含其之組成物、及其使用方法

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1236780A (zh) * 1998-03-11 1999-12-01 弗·哈夫曼-拉罗切有限公司 吡唑并嘧啶和吡唑并三嗪
WO2011087999A1 (en) * 2010-01-14 2011-07-21 Merck Sharp & Dohme Corp. Pyrazolo[1,5-a]pyrimidines as mark inhibitors

Also Published As

Publication number Publication date
US20150183792A1 (en) 2015-07-02
TR201808280T4 (tr) 2018-07-23
TW201341386A (zh) 2013-10-16
KR101965025B1 (ko) 2019-04-02
HUE038786T2 (hu) 2018-11-28
JP2015509535A (ja) 2015-03-30
MX345830B (es) 2017-02-17
MX381849B (es) 2025-03-13
US9403832B2 (en) 2016-08-02
IN2014DN07384A (enExample) 2015-04-24
MX2014010589A (es) 2014-09-18
KR20140138864A (ko) 2014-12-04
DK2834243T3 (en) 2018-07-23
PL2834243T3 (pl) 2018-09-28
EP2834243B1 (en) 2018-04-25
ES2676224T3 (es) 2018-07-17
AU2013230128A1 (en) 2014-09-25
NZ630721A (en) 2016-12-23
ZA201406149B (en) 2016-06-29
AU2013230128B2 (en) 2017-08-17
CA2866143C (en) 2020-08-04
UY34668A (es) 2013-10-31
US20130253194A1 (en) 2013-09-26
US8946415B2 (en) 2015-02-03
PT2834243T (pt) 2018-08-01
CA2866143A1 (en) 2013-09-12
HK1201257A1 (en) 2015-08-28
BR112014022000A2 (pt) 2017-06-20
EP2834243A1 (en) 2015-02-11
SG11201405561RA (en) 2014-10-30
RU2014140735A (ru) 2016-04-27
US20170129896A1 (en) 2017-05-11
AR090292A1 (es) 2014-11-05
CN104302649A (zh) 2015-01-21
JP6418950B2 (ja) 2018-11-07
IL234486A (en) 2016-10-31
BR112014022000A8 (pt) 2021-06-15
WO2013134228A1 (en) 2013-09-12

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