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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Pending
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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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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

Family

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)

Cited By (7)

* 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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US7196078B2 (en) * 2002-09-04 2007-03-27 Schering Corpoartion Trisubstituted and tetrasubstituted pyrazolopyrimidines as cyclin dependent kinase inhibitors
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
JP5052518B2 (ja) 2005-10-06 2012-10-17 シェーリング コーポレイション プロテインキナーゼインヒビターとしてのピラゾロピリミジン
BRPI0616985B1 (pt) * 2005-10-06 2021-10-26 Merck Sharp & Dohme Corp. Composto de pirazolo[1,5-a]pirimidina, e, uso de um composto
EA034598B1 (ru) 2005-12-23 2020-02-25 Ариад Фармасьютикалз, Инк. Применение бициклических гетероарильных соединений для лечения рака
US20090069315A1 (en) * 2006-03-08 2009-03-12 Rajeev Sivasankaran Use of Pyrazolo(1,5A)Pyrimidin-7-YL Amine Derivatives in the Treatment of Neurological Disorders
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
CA2664375A1 (fr) * 2006-09-28 2008-04-03 Novartis Ag Derives pyrazolo[1,5-a]pyrimidine et leur utilisation therapeutique
WO2008037477A1 (fr) 2006-09-29 2008-04-03 Novartis Ag PYRAZOLOPYRIMIDINES UTILISÉES COMME INHIBITEURS DES LIPIDES KINASES Pl3K
EP1918291A1 (fr) * 2006-10-30 2008-05-07 Novartis AG Dérives de pyrazole fusionnes substitués de 3-aminocarbonyle comme modulateurs de protéine kinase
CA2689667A1 (fr) * 2007-06-07 2008-12-18 Schering Corporation Synthese d'aminopyrazoles substitues en position 3
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JP2013506669A (ja) 2009-09-30 2013-02-28 メルク・シャープ・アンド・ドーム・コーポレーション Ｅｒｋ阻害剤である新規化合物
ME03376B (fr) 2010-05-20 2020-01-20 Array Biopharma Inc Composés macrocycliques comme inhibiteurs de la kinase trk
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US20150038500A1 (en) * 2011-11-25 2015-02-05 Catholic University Industry-Academic Cooperation Foundation Pharmaceutical composition for preventing and treating ophthalmic disorders
BR112018000808A2 (pt) 2015-07-16 2018-09-04 Array Biopharma Inc compostos de pirazolo[1,5-a]piridina substituída como inibidores de ret cinase
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
TWI752098B (zh) 2016-10-10 2022-01-11 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
WO2018136661A1 (fr) 2017-01-18 2018-07-26 Andrews Steven W Composés de pyrazolo[1,5-a]pyrazine substitués utilisés en tant qu'inhibiteurs de la kinase ret
WO2018136663A1 (fr) 2017-01-18 2018-07-26 Array Biopharma, Inc. Inhibiteurs de ret
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
US11472802B2 (en) 2018-01-18 2022-10-18 Array Biopharma Inc. Substituted pyrazolyl[4,3-c]pyridine compounds as RET kinase inhibitors
JP7060694B2 (ja) 2018-01-18 2022-04-26 アレイ バイオファーマ インコーポレイテッド Ｒｅｔキナーゼ阻害剤としての置換ピロロ［２，３－ｄ］ピリミジン化合物
EP3740490A1 (fr) 2018-01-18 2020-11-25 Array Biopharma, Inc. Composés de pyrazolo[3,4-d]pyrimidine substitués utilisés en tant qu'inhibiteurs de la kinase ret
BR112020015396A2 (pt) 2018-01-29 2020-12-08 Merck Patent Gmbh Inididores de gcn2 e usos dos mesmos
JP7229257B2 (ja) * 2018-01-29 2023-02-28 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
CN112996794A (zh) 2018-09-10 2021-06-18 阿雷生物药品公司 作为ret激酶抑制剂的稠合杂环化合物
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CN114728167B (zh) 2019-11-25 2024-03-19 安进公司 作为δ-5脱饱和酶抑制剂的杂环化合物以及使用方法
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Cited By (11)

* 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
CN117843642B (zh) * 2022-10-09 2026-04-10 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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PE20051089A1 (es) 2006-01-25
MA28400B1 (fr) 2007-01-02
NO20063758L (no) 2006-10-23
BRPI0507071A (pt) 2007-06-19
WO2005070431A1 (fr) 2005-08-04
AR049769A1 (es) 2006-09-06
KR20070009546A (ko) 2007-01-18
IL176737A0 (en) 2006-10-31
CA2552885A1 (fr) 2005-08-04
AU2005205915B2 (en) 2009-05-21
RU2006130003A (ru) 2008-04-10
JP2007519662A (ja) 2007-07-19
EP1708710A1 (fr) 2006-10-11
TW200528103A (en) 2005-09-01
AU2005205915A1 (en) 2005-08-04
TNSN06226A1 (en) 2007-12-03

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