CN1909908A - 用于治疗蛋白激酶依赖性疾病的吡唑并[1,5－a]嘧啶－7－基－胺衍生物 - Google Patents

用于治疗蛋白激酶依赖性疾病的吡唑并[1,5－a]嘧啶－7－基－胺衍生物 Download PDF

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Publication number
CN1909908A
CN1909908A CNA2005800030379A CN200580003037A CN1909908A CN 1909908 A CN1909908 A CN 1909908A CN A2005800030379 A CNA2005800030379 A CN A2005800030379A CN 200580003037 A CN200580003037 A CN 200580003037A CN 1909908 A CN1909908 A CN 1909908A
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phenyl
methyl
pyrazolo
pyrimidin
ylamine
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Chinese (zh)
Inventor
G·博尔德
A·弗勒尔斯海默
P·菲雷
P·因巴赫
升谷敬一
J·舍普费尔
G·马蒂尼-巴伦
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Novartis AG
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Novartis AG
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Application filed by Novartis AG filed Critical Novartis AG
Publication of CN1909908A publication Critical patent/CN1909908A/zh
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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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Transplantation (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CNA2005800030379A 2004-01-22 2005-01-21 用于治疗蛋白激酶依赖性疾病的吡唑并[1,5－a]嘧啶－7－基－胺衍生物 Pending CN1909908A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US53822004P 2004-01-22 2004-01-22
US60/538,220 2004-01-22

Publications (1)

Publication Number Publication Date
CN1909908A true CN1909908A (zh) 2007-02-07

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ID=34807167

Family Applications (1)

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CNA2005800030379A Pending CN1909908A (zh) 2004-01-22 2005-01-21 用于治疗蛋白激酶依赖性疾病的吡唑并[1,5－a]嘧啶－7－基－胺衍生物

Country Status (17)

Country Link
EP (1) EP1708710A1 (fr)
JP (1) JP2007519662A (fr)
KR (1) KR20070009546A (fr)
CN (1) CN1909908A (fr)
AR (1) AR049769A1 (fr)
AU (1) AU2005205915B2 (fr)
BR (1) BRPI0507071A (fr)
CA (1) CA2552885A1 (fr)
EC (1) ECSP066718A (fr)
IL (1) IL176737A0 (fr)
MA (1) MA28400B1 (fr)
NO (1) NO20063758L (fr)
PE (1) PE20051089A1 (fr)
RU (1) RU2006130003A (fr)
TN (1) TNSN06226A1 (fr)
TW (1) TW200528103A (fr)
WO (1) WO2005070431A1 (fr)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102918043A (zh) * 2010-02-19 2013-02-06 诺瓦提斯公司 作为cdk4/6抑制剂的吡咯并嘧啶化合物
CN103097380A (zh) * 2010-08-09 2013-05-08 株式会社创药分子设计 酪蛋白激酶1δ 及酪蛋白激酶1ε 抑制剂
CN105906630A (zh) * 2015-04-06 2016-08-31 四川百利药业有限责任公司 用作fgfr抑制剂的n-(1h-吡唑-5-基)嘧啶并吡唑-4,6-二取代胺类化合物
CN106588893A (zh) * 2016-12-01 2017-04-26 北京万全德众医药生物技术有限公司 维拉佐酮双氧化物的制备
CN109836428A (zh) * 2019-02-27 2019-06-04 华东师范大学 具有免疫抑制活性的吡唑[4,3-d]嘧啶衍生物及用途
CN114751910A (zh) * 2022-05-17 2022-07-15 重庆文理学院 一种可诱导细胞巨泡式死亡的化合物及其制备方法和应用
CN117843642A (zh) * 2022-10-09 2024-04-09 麦科萨药业(苏州)有限公司 一种双官能化合物及其用途

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US7563798B2 (en) * 2002-09-04 2009-07-21 Schering Corporation Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
US7605155B2 (en) * 2002-09-04 2009-10-20 Schering Corporation Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
GB0515026D0 (en) * 2005-07-21 2005-08-31 Novartis Ag Organic compounds
EP1931676B1 (fr) 2005-10-06 2011-11-16 Schering Corporation Pyrazolopyrimidines en tant qu'inhibiteurs de protéines kinases
BRPI0616985B1 (pt) * 2005-10-06 2021-10-26 Merck Sharp & Dohme Corp. Composto de pirazolo[1,5-a]pirimidina, e, uso de um composto
ES2403206T3 (es) 2005-12-23 2013-05-16 Ariad Pharmaceuticals, Inc. Compuestos bicíclicos de heteroarilo
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WO2007109183A2 (fr) * 2006-03-20 2007-09-27 Novartis Ag Mutations et polymorphismes de la tyrosine kinase 1 liée au fms
GB0606805D0 (en) * 2006-04-04 2006-05-17 Novartis Ag Organic compounds
GB0606804D0 (en) * 2006-04-04 2006-05-17 Novartis Ag Organic Compounds
CN101516888A (zh) * 2006-09-28 2009-08-26 诺瓦提斯公司 吡唑并[1,5-a]嘧啶衍生物及其治疗用途
BRPI0717564A2 (pt) 2006-09-29 2013-10-22 Novartis Ag Pirazolopirimidinas como inibidores de pi3k lipídeo cinase
EP1918291A1 (fr) * 2006-10-30 2008-05-07 Novartis AG Dérives de pyrazole fusionnes substitués de 3-aminocarbonyle comme modulateurs de protéine kinase
JP5198562B2 (ja) * 2007-06-07 2013-05-15 メルク・シャープ・アンド・ドーム・コーポレーション 置換−３−アミノピラゾールの合成
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EP2615916B1 (fr) 2010-09-16 2017-01-04 Merck Sharp & Dohme Corp. Dérivés condensés de pyrazole utilisés comme nouveaux inhibiteurs erk
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EP3322706B1 (fr) 2015-07-16 2020-11-11 Array Biopharma, Inc. Composés substitués de pyrazolo[1,5-a]pyridines comme inhibiteurs de la kinase ret
TWI704148B (zh) 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
JOP20190077A1 (ar) 2016-10-10 2019-04-09 Array Biopharma Inc مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret
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CN110267960B (zh) 2017-01-18 2022-04-26 阿雷生物药品公司 作为RET激酶抑制剂的取代的吡唑并[1,5-a]吡嗪化合物
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
TWI876442B (zh) 2017-10-10 2025-03-11 美商絡速藥業公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物
TWI791053B (zh) 2017-10-10 2023-02-01 美商亞雷生物製藥股份有限公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物
CA3087578C (fr) 2018-01-18 2023-08-08 Array Biopharma Inc. Composes de pyrazolo[3,4-d]pyrimidine substitues utilises en tant qu'inhibiteurs de la kinase ret
CA3087972C (fr) 2018-01-18 2023-01-10 Array Biopharma Inc. Composes de pyrazolyl[4,3-c]pyridine substitues utilises en tant qu'inhibiteurs de la kinase ret
CA3087354C (fr) 2018-01-18 2023-01-03 Array Biopharma Inc. Composes de pyrrolo[2,3-d]pyrimidines substitues utilises en tant qu'inhibiteurs de la kinase ret
JP7377207B2 (ja) 2018-01-29 2023-11-09 メルク パテント ゲーエムベーハー Ｇｃｎ２阻害剤およびその使用
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WO2023154282A1 (fr) * 2022-02-08 2023-08-17 Theras, Inc. Composés ayant une structure t formée par au moins quatre cycles destinés à être utilisés dans le traitement du cancer et d'autres indications

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Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102918043A (zh) * 2010-02-19 2013-02-06 诺瓦提斯公司 作为cdk4/6抑制剂的吡咯并嘧啶化合物
CN102918043B (zh) * 2010-02-19 2015-07-29 诺华股份有限公司 作为cdk4/6抑制剂的吡咯并嘧啶化合物
CN103097380A (zh) * 2010-08-09 2013-05-08 株式会社创药分子设计 酪蛋白激酶1δ 及酪蛋白激酶1ε 抑制剂
CN103097380B (zh) * 2010-08-09 2015-06-03 株式会社创药分子设计 酪蛋白激酶1δ及酪蛋白激酶1ε抑制剂
CN105906630A (zh) * 2015-04-06 2016-08-31 四川百利药业有限责任公司 用作fgfr抑制剂的n-(1h-吡唑-5-基)嘧啶并吡唑-4,6-二取代胺类化合物
CN106588893A (zh) * 2016-12-01 2017-04-26 北京万全德众医药生物技术有限公司 维拉佐酮双氧化物的制备
CN109836428A (zh) * 2019-02-27 2019-06-04 华东师范大学 具有免疫抑制活性的吡唑[4,3-d]嘧啶衍生物及用途
CN114751910A (zh) * 2022-05-17 2022-07-15 重庆文理学院 一种可诱导细胞巨泡式死亡的化合物及其制备方法和应用
CN114751910B (zh) * 2022-05-17 2023-02-24 重庆文理学院 一种可诱导细胞巨泡式死亡的化合物及其制备方法和应用
CN117843642A (zh) * 2022-10-09 2024-04-09 麦科萨药业(苏州)有限公司 一种双官能化合物及其用途

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CA2552885A1 (fr) 2005-08-04
AU2005205915A1 (en) 2005-08-04
ECSP066718A (es) 2006-10-31
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