CN1222520C - c-JUN N-末端激酶(JNK)和其它蛋白激酶的抑制剂 - Google Patents

c-JUN N-末端激酶(JNK)和其它蛋白激酶的抑制剂 Download PDF

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Publication number
CN1222520C
CN1222520C CNB008141789A CN00814178A CN1222520C CN 1222520 C CN1222520 C CN 1222520C CN B008141789 A CNB008141789 A CN B008141789A CN 00814178 A CN00814178 A CN 00814178A CN 1222520 C CN1222520 C CN 1222520C
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China
Prior art keywords
iia
iiia
och
phenyl
substituted
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Expired - Fee Related
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CNB008141789A
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English (en)
Chinese (zh)
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CN1378541A (zh
Inventor
J·格林
G·比米斯
A-L·格里洛特
M·勒德鲍尔
F·萨里图罗
E·哈林顿
H·高
C·贝克
J·曹
M·黑尔
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/341Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
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    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
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    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • C07DHETEROCYCLIC COMPOUNDS
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    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Physical Education & Sports Medicine (AREA)
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  • Diabetes (AREA)
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  • Orthopedic Medicine & Surgery (AREA)
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  • Pulmonology (AREA)
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  • Urology & Nephrology (AREA)
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  • Pain & Pain Management (AREA)
  • Communicable Diseases (AREA)
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CNB008141789A 1999-08-12 2000-08-11 c-JUN N-末端激酶(JNK)和其它蛋白激酶的抑制剂 Expired - Fee Related CN1222520C (zh)

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
US60/148795 1999-08-12
US14879599P 1999-08-13 1999-08-13
US60/148,795 1999-08-13
US16692299P 1999-11-22 1999-11-22
US60/166,922 1999-11-22
US21151700P 2000-06-14 2000-06-14
US60/211517 2000-06-14
US60/211,517 2000-06-14

Publications (2)

Publication Number Publication Date
CN1378541A CN1378541A (zh) 2002-11-06
CN1222520C true CN1222520C (zh) 2005-10-12

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CNB008141789A Expired - Fee Related CN1222520C (zh) 1999-08-12 2000-08-11 c-JUN N-末端激酶(JNK)和其它蛋白激酶的抑制剂

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Country Link
US (2) US6693108B2 (enExample)
EP (1) EP1218369B1 (enExample)
JP (1) JP2003531103A (enExample)
KR (1) KR20020030791A (enExample)
CN (1) CN1222520C (enExample)
AR (1) AR032130A1 (enExample)
AT (1) ATE402163T1 (enExample)
AU (1) AU6909600A (enExample)
BR (1) BR0013551A (enExample)
CA (1) CA2381882C (enExample)
CO (1) CO5200770A1 (enExample)
CZ (1) CZ2002534A3 (enExample)
DE (1) DE60039616D1 (enExample)
HK (1) HK1045507A1 (enExample)
HU (1) HUP0300340A3 (enExample)
MX (1) MXPA02001565A (enExample)
MY (1) MY133159A (enExample)
NO (1) NO20020713L (enExample)
NZ (1) NZ517694A (enExample)
PL (1) PL366110A1 (enExample)
SK (1) SK3572002A3 (enExample)
WO (1) WO2001012621A1 (enExample)

Families Citing this family (102)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1348370A (zh) 1999-04-15 2002-05-08 布里斯托尔-迈尔斯斯奎布公司 环状蛋白酪氨酸激酶抑制剂
US7125875B2 (en) 1999-04-15 2006-10-24 Bristol-Myers Squibb Company Cyclic protein tyrosine kinase inhibitors
US7119114B1 (en) 1999-08-19 2006-10-10 Signal Pharmaceuticals, Llc Pyrazoloanthrone and derivatives thereof as JNK inhibitors and compositions and methods related thereto
US20040072888A1 (en) 1999-08-19 2004-04-15 Bennett Brydon L. Methods for treating inflammatory conditions or inhibiting JNK
US7211594B2 (en) 2000-07-31 2007-05-01 Signal Pharmaceuticals, Llc Indazole compounds and compositions thereof as JNK inhibitors and for the treatment of diseases associated therewith
US6897231B2 (en) 2000-07-31 2005-05-24 Signal Pharmaceuticals, Inc. Indazole derivatives as JNK inhibitors and compositions and methods related thereto
US7473691B2 (en) 2000-09-15 2009-01-06 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6660731B2 (en) 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
ATE346064T1 (de) 2000-09-15 2006-12-15 Vertex Pharma Pyrazolverbindungen als protein-kinasehemmer
US7122544B2 (en) 2000-12-06 2006-10-17 Signal Pharmaceuticals, Llc Anilinopyrimidine derivatives as IKK inhibitors and compositions and methods related thereto
US7429599B2 (en) 2000-12-06 2008-09-30 Signal Pharmaceuticals, Llc Methods for treating or preventing an inflammatory or metabolic condition or inhibiting JNK
US7129242B2 (en) 2000-12-06 2006-10-31 Signal Pharmaceuticals, Llc Anilinopyrimidine derivatives as JNK pathway inhibitors and compositions and methods related thereto
ATE354573T1 (de) 2000-12-21 2007-03-15 Vertex Pharma ßPYRAZOLVERBINDUNGEN, DIE SICH ALS PROTEINKINASEINHIBITOREN EIGNENß
US7199124B2 (en) 2001-02-02 2007-04-03 Takeda Pharmaceutical Company Limited JNK inhibitor
US6987184B2 (en) 2001-02-15 2006-01-17 Signal Pharmaceuticals, Llc Isothiazoloanthrones, isoxazoloanthrones, isoindolanthrones and derivatives thereof as JNK inhibitors and compositions and methods related
EP1377572A1 (en) * 2001-04-10 2004-01-07 Vertex Pharmaceuticals Incorporated Isoxaxole derivatives as inhibitors of src and other protein kinases
US6642227B2 (en) 2001-04-13 2003-11-04 Vertex Pharmaceuticals Incorporated Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases
CA2440842A1 (en) 2001-04-16 2002-10-24 Eisai Co., Ltd. Novel 1h-indazole compounds
US6787555B2 (en) 2001-04-30 2004-09-07 The Procter & Gamble Company Triazole compounds useful in treating diseases associated with unwanted cytokine activity
US6727364B2 (en) 2001-04-30 2004-04-27 The Procter & Gamble Company Triazole compounds useful in treating diseases associated with unwanted cytokine activity
US7018999B2 (en) 2001-05-16 2006-03-28 Cephalon, Inc. Methods for the treatment and prevention of pain
US6790846B2 (en) 2001-05-24 2004-09-14 The Procter & Gamble Company Isoxazolone compounds useful in treating diseases associated with unwanted cytokine activity
CA2450769A1 (en) 2001-06-15 2002-12-27 Vertex Pharmaceuticals Incorporated 5-(2-aminopyrimidin-4-yl) benzisoxazoles as protein kinase inhibitors
US6589997B2 (en) * 2001-06-29 2003-07-08 North Shore-Long Island Jewish Health System Small-molecule modulators of hepatocyte growth factor/scatter factor activities
JP4342937B2 (ja) * 2001-07-03 2009-10-14 バーテックス ファーマシューティカルズ インコーポレイテッド SrcおよびLckタンパク質キナーゼの阻害剤としてのイソキサゾールピリミジン
IL159767A0 (en) 2001-07-23 2004-06-20 Applied Research Systems Sulfonamide derivatives, their preparation and pharmacetuical compositions containing them
JP2005501073A (ja) * 2001-08-06 2005-01-13 フアルマシア・イタリア・エツセ・ピー・アー キナーゼ阻害薬活性を有するアミノイソオキサゾール誘導体
SE0102764D0 (sv) 2001-08-17 2001-08-17 Astrazeneca Ab Compounds
EA007298B1 (ru) * 2001-11-01 2006-08-25 Янссен Фармацевтика Н.В. Гетероариламины в качестве ингибиторов гликогенсинтаза-киназы 3-бета (ингибиторов gsk3)
CA2468544A1 (en) 2001-12-10 2003-06-19 Amgen Inc. Vanilloid receptor ligands
GB0129476D0 (en) * 2001-12-10 2002-01-30 Syngenta Participations Ag Organic compounds
ES2262996T3 (es) * 2002-01-07 2006-12-01 Eisai Co., Ltd. Deazapurinas y sus usos.
EP1476840A4 (en) * 2002-01-11 2007-05-09 Vertex Pharma CRYSTALLINE STRUCTURES OF JNK INHIBITION COMPLEXES AND BINDING POCKETS THEREOF
ES2321827T3 (es) 2002-02-12 2009-06-12 Pfizer Products Inc. Gen de streptomyces avermitilis que rige la relacion de avermectinas b2-b1.
WO2003075917A1 (en) 2002-03-08 2003-09-18 Signal Pharmaceuticals, Inc. Combination therapy for treating, preventing or managing proliferative disorders and cancers
WO2003099284A1 (en) * 2002-05-22 2003-12-04 Amgen Inc. Amino-pyridine, -pyridine and pyridazine derivatives for use as vanilloid receptor ligands for the treatment of pain
JP2005528105A (ja) * 2002-05-30 2005-09-22 セルジーン・コーポレーション 細胞分化をモジュレートするため、並びに骨髄増殖性疾患及び骨髄異形成症候群を治療するためのjnk又はmkk阻害剤の使用方法
TW200406385A (en) 2002-05-31 2004-05-01 Eisai Co Ltd Pyrazole compound and pharmaceutical composition containing the same
MY141867A (en) 2002-06-20 2010-07-16 Vertex Pharma Substituted pyrimidines useful as protein kinase inhibitors
GB0215844D0 (en) 2002-07-09 2002-08-14 Novartis Ag Organic compounds
EP1542972A4 (en) 2002-07-29 2008-01-23 Nitromed Inc CYCLOOXYGENASE-2 SELECTIVE INHIBITORS, COMPOSITION AND METHOD OF USE
CN1319968C (zh) 2002-08-02 2007-06-06 沃泰克斯药物股份有限公司 用作gsk-3的抑制剂的吡唑组合物
DE10237883A1 (de) * 2002-08-19 2004-03-04 Merckle Gmbh Chem.-Pharm. Fabrik Substituierte Isoxazolderivate und ihre Verwendung in der Pharmazie
WO2004022555A1 (en) * 2002-09-06 2004-03-18 Vertex Pharmaceuticals Incorporated Isoxazoles and their use in the treatment of ischemic diseases
US20040087642A1 (en) * 2002-10-24 2004-05-06 Zeldis Jerome B. Methods of using and compositions comprising a JNK inhibitor for the treatment, prevention, management and/or modification of pain
WO2004058749A1 (en) 2002-12-18 2004-07-15 Vertex Pharmaceuticals Incorporated Benzisoxazole derivatives useful as inhibitors of protein kinases
US7279576B2 (en) 2002-12-31 2007-10-09 Deciphera Pharmaceuticals, Llc Anti-cancer medicaments
US7202257B2 (en) 2003-12-24 2007-04-10 Deciphera Pharmaceuticals, Llc Anti-inflammatory medicaments
US7144911B2 (en) 2002-12-31 2006-12-05 Deciphera Pharmaceuticals Llc Anti-inflammatory medicaments
MXPA05008335A (es) 2003-02-11 2006-05-04 Vernalis Cambridge Ltd Compuestos de isoxazol como inhibidores de las proteinas de choque por calor.
GB0308466D0 (en) * 2003-04-11 2003-05-21 Novartis Ag Organic compounds
BRPI0412820A (pt) * 2003-07-25 2006-09-26 Pfizer compostos de aminopirazol e utilização como inibidores de chk1
AR045595A1 (es) * 2003-09-04 2005-11-02 Vertex Pharma Composiciones utiles como inhibidores de proteinas quinasas
NZ545917A (en) * 2003-10-24 2009-11-27 Lilly Co Eli Novel crystalline forms of {2-[1-(3,5-bis-trifluoromethylbenzyl)-5-pyridin-4-yl-1H-[1,2,3]triazol-4-yl]-pyridin-3-yl}-(2-chlorophenyl)-methanone
TW200533357A (en) * 2004-01-08 2005-10-16 Millennium Pharm Inc 2-(amino-substituted)-4-aryl pyrimidines and related compounds useful for treating inflammatory diseases
US7276050B2 (en) * 2004-03-02 2007-10-02 Alan Franklin Trans-scleral drug delivery method and apparatus
KR100793479B1 (ko) * 2004-04-28 2008-01-14 다나베 미츠비시 세이야꾸 가부시키가이샤 염증성 질환을 치료하기 위한 p38 MAP- 키나제억제제로서의4-2-(시클로알킬아미노)피리딘-4-일-(페닐)-이미다졸린-2-온 유도체
MY143245A (en) * 2004-04-28 2011-04-15 Mitsubishi Tanabe Pharma Corp 4- 2-(cycloalkylamino)pyrimidin-4-yl-(phenyl)-imidazolin-2-one derivatives as p38 map-kinase inhibitors for the treatment of inflammatory diseases
US20060018123A1 (en) * 2004-07-02 2006-01-26 Rose Eric P Curing light having a reflector
CN102731490A (zh) * 2004-09-10 2012-10-17 先正达有限公司 作为杀真菌剂的取代异*唑
AU2005295788A1 (en) 2004-10-13 2006-04-27 Wyeth N-benzenesulfonyl substituted anilino-pyrimidine analogs
US7803824B2 (en) 2004-10-29 2010-09-28 Alcon, Inc. Use of inhibitors of Jun N-terminal kinases to treat glaucoma
US20060094753A1 (en) 2004-10-29 2006-05-04 Alcon, Inc. Use of inhibitors of Jun N-terminal kinases for the treatment of glaucomatous retinopathy and ocular diseases
US20060223807A1 (en) 2005-03-29 2006-10-05 University Of Massachusetts Medical School, A Massachusetts Corporation Therapeutic methods for type I diabetes
NZ575512A (en) 2005-07-09 2009-11-27 Astrazeneca Ab Heteroaryl benzamide derivatives for use as GLK activators in the treatment of diabetes
KR20080044836A (ko) 2005-07-15 2008-05-21 라보라뚜와르 세로노 에스. 에이. 자궁내막증 치료용 jnk 억제제
BRPI0613042A2 (pt) 2005-07-15 2010-12-14 Serono Lab inibidores de jnk para o tratamento de endometriose
WO2007030617A1 (en) * 2005-09-09 2007-03-15 Vertex Pharmaceuticals Incorporated Inhibitors of bacterial impdh
JP5249770B2 (ja) 2005-11-03 2013-07-31 バーテックス ファーマシューティカルズ インコーポレイテッド キナーゼインヒビターとして有用なアミノピリジン
JP2009521931A (ja) 2005-12-29 2009-06-11 アントフロゲネシス コーポレーション 胎盤幹細胞を収集及び保存するための改善された組成物、及び該組成物の使用方法
US7737149B2 (en) 2006-12-21 2010-06-15 Astrazeneca Ab N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-2H-pyrazol-3-yl]-4-(3,5-dimethylpiperazin-1-yl)benzamide and salts thereof
EP2008656A1 (en) * 2007-06-28 2008-12-31 Bergen Teknologioverforing AS Compositions for the treatment of hyperphenylalaninemia
AU2008282156B2 (en) 2007-07-31 2014-07-17 Vertex Pharmaceuticals Incorporated Process for preparing 5-fluoro-1H-pyrazolo [3, 4-b] pyridin-3-amine and derivatives thereof
MX2010008926A (es) 2008-02-15 2011-02-23 Rigel Pharmaceuticals Inc Compuestos de pirimidin-2-amina y su uso como inhibidores de jak cinasas.
GB0823002D0 (en) * 2008-12-17 2009-01-28 Syngenta Participations Ag Isoxazoles derivatives with plant growth regulating properties
HUE029196T2 (en) 2010-06-04 2017-02-28 Hoffmann La Roche Aminoprimidine derivatives as LRRK2 modulators
BR112013011600B1 (pt) 2010-11-10 2022-01-11 Genentech, Inc Derivados de pirazol aminopirimidina, seu uso e composição que os compreende
US8461179B1 (en) 2012-06-07 2013-06-11 Deciphera Pharmaceuticals, Llc Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
US20140179712A1 (en) 2012-12-21 2014-06-26 Astrazeneca Ab Pharmaceutical formulation of n-[5-[2-(3,5-dimethoxyphenyl)ethyl]-2h-pyrazol-3-yl]-4-[(3r,5s)-3,5-dimethylpiperazin-1-yl]benzamide
SG11201704827UA (en) * 2014-12-16 2017-07-28 Signal Pharm Llc Formulations of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methycyclohexylamino)-pyrimidine-5-carboxamide
WO2016100308A1 (en) * 2014-12-16 2016-06-23 Signal Pharmaceuticals, Llc Methods for measurement of inhibition of c-jun n-terminal kinase in skin
EP3250557B1 (en) 2015-01-29 2024-11-20 Signal Pharmaceuticals, LLC Isotopologues of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide
CN107922287B (zh) 2015-07-24 2021-04-09 细胞基因公司 合成(1r,2r,5r)-5-氨基-2-甲基环己醇盐酸盐的方法和其中可用的中间体
CN105622537A (zh) * 2016-03-01 2016-06-01 青岛大学 一种3,4,5-三取代异恶唑类化合物的合成方法
AU2019216351B2 (en) 2018-01-31 2024-07-25 Deciphera Pharmaceuticals, Llc Combination therapy for the treatment of mastocytosis
CN111818915B (zh) 2018-01-31 2024-05-24 德西费拉制药有限责任公司 治疗胃肠道间质瘤的组合疗法
US20200383984A1 (en) * 2018-02-08 2020-12-10 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. Heteroaryl compounds, pharmaceutical compositions thereof, and their therapeutic use
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
US11384083B2 (en) 2019-02-15 2022-07-12 Incyte Corporation Substituted spiro[cyclopropane-1,5′-pyrrolo[2,3-d]pyrimidin]-6′(7′h)-ones as CDK2 inhibitors
WO2020180959A1 (en) 2019-03-05 2020-09-10 Incyte Corporation Pyrazolyl pyrimidinylamine compounds as cdk2 inhibitors
WO2020205560A1 (en) 2019-03-29 2020-10-08 Incyte Corporation Sulfonylamide compounds as cdk2 inhibitors
US11440914B2 (en) 2019-05-01 2022-09-13 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
US11447494B2 (en) 2019-05-01 2022-09-20 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
TWI878335B (zh) 2019-08-12 2025-04-01 美商迪賽孚爾製藥有限公司 治療胃腸道基質瘤方法
NZ784949A (en) 2019-08-12 2025-09-26 Deciphera Pharmaceuticals Llc Ripretinib for treating gastrointestinal stromal tumors
BR112022002698A2 (pt) 2019-08-14 2022-07-19 Incyte Corp Compostos de imidazolil pirimidinilamina como inibidores de cdk2
MX2022004390A (es) 2019-10-11 2022-08-08 Incyte Corp Aminas biciclicas como inhibidores de la cinasa dependiente de ciclina 2 (cdk2).
AU2020419197B2 (en) 2019-12-30 2023-08-31 Deciphera Pharmaceuticals, Llc Amorphous kinase inhibitor formulations and methods of use thereof
KR20250057151A (ko) 2019-12-30 2025-04-28 데시페라 파마슈티칼스, 엘엘씨 1-(4-브로모-5-(1-에틸-7-(메틸아미노)-2-옥소-1,2-디히드로-1,6-나프티리딘-3-일)-2-플루오로페닐)-3-페닐우레아의조성물
US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
US11976073B2 (en) 2021-12-10 2024-05-07 Incyte Corporation Bicyclic amines as CDK2 inhibitors
US11779572B1 (en) 2022-09-02 2023-10-10 Deciphera Pharmaceuticals, Llc Methods of treating gastrointestinal stromal tumors

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4876252A (en) * 1986-01-13 1989-10-24 American Cyanamid Company 4,5,6-substituted-N-(substituted-phenyl)-2-pyrimidinamines
US5356897A (en) * 1991-09-09 1994-10-18 Fujisawa Pharmaceutical Co., Ltd. 3-(heteroaryl)-pyrazololi[1,5-a]pyrimidines
US5646042A (en) * 1992-08-26 1997-07-08 Ribozyme Pharmaceuticals, Inc. C-myb targeted ribozymes
DE4408084A1 (de) * 1994-03-10 1995-09-14 Hoechst Ag 3,5-Disubstituierte und 3,4,5-trisubstituierte 2-Isoxazoline und Isoxazole, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
US5668148A (en) * 1995-04-20 1997-09-16 Merck & Co., Inc. Alpha1a adrenergic receptor antagonists
US6514977B1 (en) * 1997-05-22 2003-02-04 G.D. Searle & Company Substituted pyrazoles as p38 kinase inhibitors
EP1000055A1 (en) * 1997-05-22 2000-05-17 G.D. Searle & Co. SUBSTITUTED PYRAZOLES AS p38 KINASE INHIBITORS

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