ATE529109T1 - Hemmung der p38 kinase aktivität durch substituierte heterocyclische harnstoffe - Google Patents

Hemmung der p38 kinase aktivität durch substituierte heterocyclische harnstoffe

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Publication number
ATE529109T1
ATE529109T1 AT98964709T AT98964709T ATE529109T1 AT E529109 T1 ATE529109 T1 AT E529109T1 AT 98964709 T AT98964709 T AT 98964709T AT 98964709 T AT98964709 T AT 98964709T AT E529109 T1 ATE529109 T1 AT E529109T1
Authority
AT
Austria
Prior art keywords
inhibition
kinase activity
substituted heterocyclic
heterocyclic ureas
ureas
Prior art date
Application number
AT98964709T
Other languages
English (en)
Inventor
Jacques Dumas
Uday Khire
Timothy Lowinger
Holger Paulsen
Bernd Riedl
William Scott
Roger Smith
Jill Wood
Holia Hatoum-Mokdad
Jeffrey Johnson
Wendy Lee
Aniko Redman
Original Assignee
Bayer Healthcare Llc
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Publication date
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Publication of ATE529109T1 publication Critical patent/ATE529109T1/de

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    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
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    • C07D277/48—Acylated amino or imino radicals by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof, e.g. carbonylguanidines
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    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
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    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D333/30—Hetero atoms other than halogen
    • C07D333/36—Nitrogen atoms
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
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AT98964709T 1997-12-22 1998-12-22 Hemmung der p38 kinase aktivität durch substituierte heterocyclische harnstoffe ATE529109T1 (de)

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Families Citing this family (149)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1019040B1 (de) * 1997-05-23 2004-09-29 Bayer Corporation Arylharnstoffderivate zur behandlung von inflammatorischen oder immunomodulatorischen erkrankungen
EP1473292A1 (de) * 1997-11-03 2004-11-03 Boehringer Ingelheim Pharmaceuticals, Inc. Aromatische heterocyclische Verbindungen als antiinflammatorische Mittel
AU2006201959B2 (en) * 1997-12-22 2008-09-04 Bayer Healthcare Llc Inhibition of Raf Kinase using Substituted Heterocyclic Ureas
US7329670B1 (en) 1997-12-22 2008-02-12 Bayer Pharmaceuticals Corporation Inhibition of RAF kinase using aryl and heteroaryl substituted heterocyclic ureas
JP4437270B2 (ja) * 1997-12-22 2010-03-24 バイエル コーポレイション 置換複素環式尿素を用いたrafキナーゼの阻害
US7517880B2 (en) 1997-12-22 2009-04-14 Bayer Pharmaceuticals Corporation Inhibition of p38 kinase using symmetrical and unsymmetrical diphenyl ureas
US20020065296A1 (en) * 1999-01-13 2002-05-30 Bayer Corporation Heteroaryl ureas containing nitrogen hetero-atoms as p38 kinase inhibitors
EP1690853B1 (de) * 1999-01-13 2010-03-10 Bayer HealthCare LLC Verwendung von Omega-Carboxyaryl-substituierten Diphenylharnstoffen als raf-Kinase-Inhibitoren
EP1140840B1 (de) 1999-01-13 2006-03-22 Bayer Pharmaceuticals Corp. -g(v)-carboxyaryl substituierte diphenyl harnstoffe als raf kinase inhibitoren
US7351834B1 (en) 1999-01-13 2008-04-01 Bayer Pharmaceuticals Corporation ω-Carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
US8124630B2 (en) 1999-01-13 2012-02-28 Bayer Healthcare Llc ω-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
EP2298311B1 (de) * 1999-01-13 2012-05-09 Bayer HealthCare LLC Omega-carboxyarylsubstituierte-Diphenyl-Harnstoffe als p38-Kinasehemmer
UA73492C2 (en) 1999-01-19 2005-08-15 Aromatic heterocyclic compounds as antiinflammatory agents
MXPA01008440A (es) 1999-02-22 2002-04-24 Boehringer Ingelheim Pharma Derivados heterociclicos policiclos como agentes anti-inflamatorios..
TR200102817T2 (tr) 1999-03-12 2002-05-21 Boehringer Ingelheim Pharmaceuticals, Inc. Antiinflamatuar ajanlar olarak faydalı bileşikler
WO2000055152A1 (en) * 1999-03-12 2000-09-21 Boehringer Ingelheim Pharmaceuticals, Inc. Aromatic heterocyclic compounds as anti-inflammatory agents
CA2374737C (en) 1999-07-09 2008-02-12 Boehringer Ingelheim Pharmaceuticals, Inc. Novel process for synthesis of heteroaryl-substituted urea compounds
MXPA02001498A (es) 1999-08-12 2003-07-21 Pharmacia & Italia S P A Derivados de 3(5)-amino-pirazol, procedimiento para la preparacion de los mismos y usos como agentes antitumorales.
US6387900B1 (en) 1999-08-12 2002-05-14 Pharmacia & Upjohn S.P.A. 3(5)-ureido-pyrazole derivatives process for their preparation and their use as antitumor agents
ES2292488T3 (es) 1999-11-16 2008-03-16 Boehringer Ingelheim Pharmaceuticals Inc. Derivados de la urea, como agentes antiinflamatorios.
SE9904177D0 (sv) * 1999-11-18 1999-11-18 Astra Ab Novel compounds
US6525046B1 (en) 2000-01-18 2003-02-25 Boehringer Ingelheim Pharmaceuticals, Inc. Aromatic heterocyclic compounds as antiinflammatory agents
US6608052B2 (en) 2000-02-16 2003-08-19 Boehringer Ingelheim Pharmaceuticals, Inc. Compounds useful as anti-inflammatory agents
GB0010757D0 (en) 2000-05-05 2000-06-28 Astrazeneca Ab Chemical compounds
GB0016787D0 (en) 2000-07-07 2000-08-30 Pfizer Ltd Compounds useful in therapy
FR2812633A1 (fr) * 2000-08-04 2002-02-08 Aventis Cropscience Sa Derives de phenyl(thio)urees et phenyl(thio)carbamates fongicides
US6645990B2 (en) 2000-08-15 2003-11-11 Amgen Inc. Thiazolyl urea compounds and methods of uses
FR2815030A1 (fr) * 2000-10-05 2002-04-12 Lipha Derives nitroso de la diphenylamine, compositions pharmaceutiques les contenant et leur utilisation pour la preparation de medicaments
KR100600550B1 (ko) 2000-10-20 2006-07-13 에자이 가부시키가이샤 질소 함유 방향환 유도체
US7238813B2 (en) 2000-11-29 2007-07-03 Smithkline Beecham Corporation Chemical compounds
SG138463A1 (en) * 2000-12-21 2008-01-28 Schering Corp Heteroaryl urea neuropeptide y y5 receptor antagonists
US6946476B2 (en) 2000-12-21 2005-09-20 Schering Corporation Heteroaryl urea neuropeptide Y Y5 receptor antagonists
US7235576B1 (en) 2001-01-12 2007-06-26 Bayer Pharmaceuticals Corporation Omega-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
US7371763B2 (en) 2001-04-20 2008-05-13 Bayer Pharmaceuticals Corporation Inhibition of raf kinase using quinolyl, isoquinolyl or pyridyl ureas
EP1382604B1 (de) * 2001-04-27 2005-12-28 Kirin Beer Kabushiki Kaisha Chinolinderivate mit einer azolylgruppe und chinazolinderivate
JP2004530690A (ja) 2001-05-16 2004-10-07 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド 抗炎症性薬剤として有用なジアリールウレア誘導体
MXPA03010724A (es) 2001-05-25 2004-03-02 Boehringer Ingelheim Pharma Compuestos de carbamato y oxamida como inhibidores de la produccion de citocina.
ATE338035T1 (de) 2001-06-05 2006-09-15 Boehringer Ingelheim Pharma 1,4-disubstituierte benzokondensierte cycloalkyl harnstoffverbindungen
ES2284887T3 (es) 2001-07-11 2007-11-16 Boehringer Ingelheim Pharmaceuticals Inc. Metodos para tratar enfermedades transmitidas por citocinas.
JP4825375B2 (ja) * 2001-08-28 2011-11-30 株式会社 資生堂 ジチアゾール化合物及びマトリックスメタロプロテアーゼ活性阻害剤、皮膚外用剤
GB0121941D0 (en) 2001-09-11 2001-10-31 Astrazeneca Ab Chemical compounds
KR20040047869A (ko) 2001-09-26 2004-06-05 파마시아 이탈리아 에스.피.에이. 키나제 억제제로서 활성인 아미노인다졸 유도체, 이의제조방법 및 이를 함유하는 약제학적 조성물
WO2003032989A1 (en) 2001-10-18 2003-04-24 Boehringer Ingelheim Pharmaceuticals, Inc. 1,4-disubstituted benzo-fused urea compounds as cytokine inhibitors
US10653684B2 (en) 2002-02-11 2020-05-19 Bayer Healthcare Llc Aryl ureas with angiogenisis inhibiting activity
WO2003068223A1 (en) * 2002-02-11 2003-08-21 Bayer Corporation Aryl ureas with raf kinase and angiogenesis inhibiting activity
ATE529406T1 (de) 2002-02-11 2011-11-15 Bayer Healthcare Llc Aryl-harnstoffe als kinase inhibitoren
DK1478358T3 (da) 2002-02-11 2013-10-07 Bayer Healthcare Llc Sorafenibtosylat til behandling af sygdomme kendetegnet ved unormal angiogenese
EP1480973B1 (de) 2002-02-25 2008-02-13 Boehringer Ingelheim Pharmaceuticals Inc. 1,4-disubstituierte benzokondensierte cycloalkyl-harnstoffverbindungen zur behandlung von zytokinvermittelten erkrankungen
WO2003097610A1 (en) * 2002-05-17 2003-11-27 Pharmacia Italia S.P.A. Aminoindazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
KR101124245B1 (ko) 2002-06-27 2012-07-02 노보 노르디스크 에이/에스 치료제로서 아릴 카르보닐 유도체
CA2744893A1 (en) 2002-06-27 2004-01-08 Novo Nordisk A/S Aryl carbonyl derivatives as glucokinase activators
AU2003245989A1 (en) 2002-07-09 2004-01-23 Boehringer Ingelheim Pharma Gmbh And Co. Kg Pharmaceutical compositions of anticholinergics and p38 kinase inhibitors in the treatment of respiratory diseases
CA2495284A1 (en) * 2002-09-05 2004-03-18 Neurosearch A/S Diarylurea derivatives and their use as chloride channel blockers
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
US7399866B2 (en) * 2003-01-14 2008-07-15 Cytokinetics, Inc. Compounds, compositions, and methods
EP1603879A2 (de) * 2003-02-28 2005-12-14 Bayer Pharmaceuticals Corporation Zur behandlung von krebs und anderen erkrankungen geeignete substituierte pyridinderivate
CA2516931C (en) 2003-02-28 2014-09-09 Bayer Pharmaceuticals Corporation Novel bicyclic urea derivatives useful in the treatment of cancer and other disorders
JP2006521345A (ja) * 2003-03-28 2006-09-21 ファルマシア・アンド・アップジョン・カンパニー・エルエルシー ニコチン性アセチルコリン受容体の正のアロステリック調節剤
EP1636585B2 (de) 2003-05-20 2012-06-13 Bayer HealthCare LLC Diaryl-harnstoffe mit kinasehemmender wirkung
PL1663978T3 (pl) 2003-07-23 2008-04-30 Bayer Healthcare Llc Fluoropodstawiony omega-karboksyarylodifenylomocznik do leczenia i profilaktyki chorób i stanów
JP4303726B2 (ja) 2003-11-11 2009-07-29 エーザイ・アール・アンド・ディー・マネジメント株式会社 ウレア誘導体およびその製造方法
WO2005048953A2 (en) * 2003-11-13 2005-06-02 Ambit Biosciences Corporation Amide derivatives as kinase modulators
GB0330042D0 (en) 2003-12-24 2004-01-28 Pharmacia Italia Spa Pyrrolo [2,3-b] pyridine derivatives active as kinase inhibitors process for their preparation and pharmaceutical compositions them
GB0330043D0 (en) 2003-12-24 2004-01-28 Pharmacia Italia Spa Pyrrolo [2,3-b] pyridine derivatives active as kinase inhibitors process for their preparation and pharmaceutical compositions comprising them
BRPI0506662B8 (pt) 2004-01-06 2021-05-25 Novo Nordisk As compostos ativadores de glucoquinase
RU2006131045A (ru) * 2004-01-30 2008-03-10 Мерк Патент ГмбХ (DE) Производные бисарилмочевины
TW200530236A (en) 2004-02-23 2005-09-16 Chugai Pharmaceutical Co Ltd Heteroaryl phenylurea
US20060211752A1 (en) 2004-03-16 2006-09-21 Kohn Leonard D Use of phenylmethimazoles, methimazole derivatives, and tautomeric cyclic thiones for the treatment of autoimmune/inflammatory diseases associated with toll-like receptor overexpression
US7838524B2 (en) 2004-04-30 2010-11-23 Bayer Healthcare Llc Substituted pyrazolyl urea derivatives useful in the treatment of cancer
US7507735B2 (en) 2004-06-17 2009-03-24 Cytokinetics, Inc. Compounds, compositions and methods
EP1609789A1 (de) * 2004-06-23 2005-12-28 Eli Lilly And Company Ureido-pyrazolderivate und ihre verwendung als kinaseinhibitoren
US20060035893A1 (en) 2004-08-07 2006-02-16 Boehringer Ingelheim International Gmbh Pharmaceutical compositions for treatment of respiratory and gastrointestinal disorders
US8969379B2 (en) 2004-09-17 2015-03-03 Eisai R&D Management Co., Ltd. Pharmaceutical compositions of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7=methoxy-6-quinolinecarboxide
WO2006062982A2 (en) 2004-12-07 2006-06-15 Locus Pharmaceuticals, Inc. Urea inhibitors of map kinases
US7612200B2 (en) 2004-12-07 2009-11-03 Locus Pharmaceuticals, Inc. Inhibitors of protein kinases
PE20060777A1 (es) 2004-12-24 2006-10-06 Boehringer Ingelheim Int Derivados de indolinona para el tratamiento o la prevencion de enfermedades fibroticas
DE602006017188D1 (de) 2005-03-07 2010-11-11 Bayer Schering Pharma Ag Pharmazeutische zusammensetzung mit einem omega-carboxyaryl-substituierten diphenylharnstoff zur behandlung von krebs
DE102005015253A1 (de) * 2005-04-04 2006-10-05 Merck Patent Gmbh Pyrazolderivate
JP4989476B2 (ja) 2005-08-02 2012-08-01 エーザイ・アール・アンド・ディー・マネジメント株式会社 血管新生阻害物質の効果を検定する方法
US7538223B2 (en) 2005-08-04 2009-05-26 Cytokinetics, Inc. Compounds, compositions and methods
DE102005037499A1 (de) 2005-08-09 2007-02-15 Merck Patent Gmbh Pyrazolderivate
EP1790342A1 (de) 2005-11-11 2007-05-30 Zentaris GmbH Pyridopyrazin-Derivate und deren Verwendung als Modulatoren der Signaltransduktionswege
AU2006313701B2 (en) 2005-11-11 2012-05-31 Aeterna Zentaris Gmbh Novel pyridopyrazines and their use as modulators of kinases
US8217042B2 (en) 2005-11-11 2012-07-10 Zentaris Gmbh Pyridopyrazines and their use as modulators of kinases
US7825120B2 (en) 2005-12-15 2010-11-02 Cytokinetics, Inc. Certain substituted ((piperazin-1-ylmethyl)benzyl)ureas
TW200808321A (en) 2005-12-15 2008-02-16 Cytokinetics Inc Certain chemical entities, compositions and methods
WO2007078815A2 (en) 2005-12-16 2007-07-12 Cytokinetics, Inc. Certain chemical entities, compositions, and methods
WO2007078839A2 (en) 2005-12-19 2007-07-12 Cytokinetics, Inc. Compounds, compositions and methods
ES2480440T3 (es) * 2005-12-21 2014-07-28 Bayer Intellectual Property Gmbh Derivados sustituidos de pirimidina útiles en el tratamiento del cáncer y de otros trastornos
WO2007076460A2 (en) * 2005-12-23 2007-07-05 Kalypsys, Inc. Substituted thiazole ureas useful as inhibitors of protein kinases
CN104706637A (zh) 2006-05-18 2015-06-17 卫材R&D管理有限公司 针对甲状腺癌的抗肿瘤剂
US20080045589A1 (en) 2006-05-26 2008-02-21 Susan Kelley Drug Combinations with Substituted Diaryl Ureas for the Treatment of Cancer
DE102006029795A1 (de) * 2006-06-27 2008-01-03 Schebo Biotech Ag Neue Harnstoff-Derivate und deren Verwendungen
JP5368096B2 (ja) 2006-08-28 2013-12-18 エーザイ・アール・アンド・ディー・マネジメント株式会社 未分化型胃癌に対する抗腫瘍剤
US7897762B2 (en) 2006-09-14 2011-03-01 Deciphera Pharmaceuticals, Llc Kinase inhibitors useful for the treatment of proliferative diseases
WO2008079972A2 (en) 2006-12-20 2008-07-03 Bayer Healthcare Llc 4-{4- [ ({3-tert-butyl-1- [3- (hydroxymethyl) phenyl] - 1h- pyrazol- 5 -yl } carbamoyl) -amin o] -3-chlorophenoxy} -n-methylpyridine-2-carboxamide as an inhibitor of the vegfr kinase for the treatment of cancer
WO2008093855A1 (ja) 2007-01-29 2008-08-07 Eisai R & D Management Co., Ltd. 未分化型胃癌治療用組成物
CN101636397B (zh) * 2007-04-13 2012-06-13 中国人民解放军军事医学科学院毒物药物研究所 脲类化合物、其制备方法及其医药用途
WO2008140895A1 (en) 2007-04-20 2008-11-20 Deciphera Pharmaceuticals, Llc Kinase inhibitors useful for the treatment of myleoproliferative diseases and other proliferative diseases
EP1992344A1 (de) 2007-05-18 2008-11-19 Institut Curie P38 Alpha als therapeutisches Target für Erkrankungen, die mit einer FGFR3- Mutation assoziiert sind
CA2704000C (en) 2007-11-09 2016-12-13 Eisai R&D Management Co., Ltd. Combination of anti-angiogenic substance and anti-tumor platinum complex
GB0818033D0 (en) 2008-10-02 2008-11-05 Respivert Ltd Novel compound
BRPI0920707A2 (pt) * 2008-10-02 2015-12-29 Respivert Ltd compostos
MX2011006219A (es) * 2008-12-11 2011-06-28 Respivert Ltd Inhibidores de la proteina cinasa activada por el mitogeno p38.
GB0905955D0 (en) 2009-04-06 2009-05-20 Respivert Ltd Novel compounds
KR20120059558A (ko) * 2009-08-19 2012-06-08 암비트 바이오사이언시즈 코포레이션 바이아릴 화합물 및 이의 사용 방법
CA2771403C (en) 2009-08-19 2015-02-24 Eisai R&D Management Co. Ltd. Quinoline derivative-containing pharmaceutical composition
CN102958523B (zh) 2010-06-25 2014-11-19 卫材R&D管理有限公司 使用具有激酶抑制作用的组合的抗肿瘤剂
JP2013531067A (ja) 2010-07-19 2013-08-01 バイエル ヘルスケア リミティド ライアビリティ カンパニー 疾病及び状態の処置及び予防のためのフルオロ置換オメガ−カルボキシアリールジフェニル尿素を用いた組み合わせ薬
EP2508184A1 (de) 2011-04-06 2012-10-10 Æterna Zentaris GmbH Pyridopyrazinderivate und ihre Verwendungen
AU2012246490B2 (en) 2011-04-18 2016-08-04 Eisai R&D Management Co., Ltd. Therapeutic agent for tumor
JP6038128B2 (ja) 2011-06-03 2016-12-07 エーザイ・アール・アンド・ディー・マネジメント株式会社 レンバチニブ化合物に対する甲状腺癌対象及び腎臓癌対象の反応性を予測及び評価するためのバイオマーカー
CN103172648B (zh) * 2011-12-20 2016-05-25 上海迪诺医药科技有限公司 三杂环衍生物、制备方法及应用
US20150044178A1 (en) 2011-12-28 2015-02-12 Kyoto Prefectural Public University Corporation Normalization of culture of corneal endothelial cells
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
WO2014033447A2 (en) * 2012-08-29 2014-03-06 Respivert Limited Kinase inhibitors
ME02990B (de) 2012-11-13 2018-10-20 Array Biopharma Inc N-pyrrolidinyl-, n'-pyrazolyl-harnstoff-, thioharnstoff-, guanidin- und cyanoguanidinverbindungen als trka-kinaseinhibitoren
CA2891334C (en) 2012-11-13 2021-10-19 Array Biopharma Inc. Bicyclic urea, thiourea, guanidine and cyanoguanidine compounds useful for the treatment of pain
JPWO2014098176A1 (ja) 2012-12-21 2017-01-12 エーザイ・アール・アンド・ディー・マネジメント株式会社 キノリン誘導体のアモルファス及びその製造方法
MX362181B (es) * 2013-02-19 2019-01-08 Ono Pharmaceutical Co Compuesto inhibidor de cinasa del receptor de tropomiosina (trk).
CA2912219C (en) 2013-05-14 2021-11-16 Eisai R&D Management Co., Ltd. Biomarkers for predicting and assessing responsiveness of endometrial cancer subjects to lenvatinib compounds
US9750723B2 (en) 2013-10-31 2017-09-05 Ohio University Prevention and treatment of non-alcoholic fatty liver disease
US10813920B2 (en) 2013-11-14 2020-10-27 The Doshisha Drug for treating corneal endothelium by promoting cell proliferation or inhibiting cell damage
CN106459013B (zh) 2014-05-15 2019-10-25 阵列生物制药公司 作为trka激酶抑制剂的化合物及其用途
WO2016010610A2 (en) 2014-07-18 2016-01-21 Ohio University Imidazole and thiazole compositions for modifying biological signaling
CA2957785C (en) 2014-08-11 2023-01-03 Angion Biomedica Corporation Cytochrome p450 inhibitors and uses thereof
EP3187491A4 (de) 2014-08-28 2018-08-01 Eisai R&D Management Co., Ltd. Hochreines chinolinderivat und verfahren zur herstellung davon
EP3517526B1 (de) 2014-09-10 2020-08-19 GlaxoSmithKline Intellectual Property Development Limited Pyridinone als rearranged-during-transfection (ret)-inhibitoren
BR112017004897A2 (pt) 2014-09-10 2017-12-12 Glaxosmithkline Ip Dev Ltd compostos inovadores como inibidores rearranjados durante a transfecção (ret)
US9638690B2 (en) 2014-11-07 2017-05-02 The University Of British Columbia Compounds and compositions for use as alkylating agent sensors and methods of use thereof
CA2970819A1 (en) 2014-12-31 2016-07-07 Angion Biomedica Corp. Methods and agents for treating disease
US20180028662A1 (en) 2015-02-25 2018-02-01 Eisai R&D Management Co., Ltd. Method for Suppressing Bitterness of Quinoline Derivative
KR20240064733A (ko) 2015-03-04 2024-05-13 머크 샤프 앤드 돔 코포레이션 암을 치료하기 위한 pd-1 길항제 및 vegfr/fgfr/ret 티로신 키나제 억제제의 조합
CA2988707C (en) 2015-06-16 2023-10-10 Eisai R&D Management Co., Ltd. Combination of cbp/catenin inhibitor and immune checkpoint inhibitor for treating cancer
CN108135894B (zh) 2015-08-20 2021-02-19 卫材R&D管理有限公司 肿瘤治疗剂
CN110072528B (zh) 2017-02-08 2022-04-26 卫材R&D管理有限公司 治疗肿瘤的药物组合物
WO2018212202A1 (en) 2017-05-16 2018-11-22 Eisai R&D Management Co., Ltd. Treatment of hepatocellular carcinoma
KR102708177B1 (ko) 2018-01-31 2024-09-23 데시페라 파마슈티칼스, 엘엘씨. 위장관 기질 종양의 치료를 위한 병용 요법
CN118903436A (zh) 2018-01-31 2024-11-08 德西费拉制药有限责任公司 治疗肥大细胞增多症的组合疗法
CA3093025A1 (en) 2018-06-12 2019-12-19 Vtv Therapeutics Llc Therapeutic uses of glucokinase activators in combination with insulin or insulin analogs
IL330104A (en) 2019-03-11 2026-08-01 Deciphera Pharmaceuticals Llc Crystalline forms of rifatinib
US12691108B2 (en) 2019-08-12 2026-07-28 Deciphera Pharmaceuticals, Llc Methods for treating vascular malformations
HRP20260411T1 (hr) 2019-08-12 2026-05-08 Deciphera Pharmaceuticals, Llc Ripretinib za liječenje gastrointestinalnih stromalnih tumora
FI4084779T3 (fi) 2019-12-30 2024-12-16 Deciphera Pharmaceuticals Llc 1-(4-bromi-5-(1-etyyli-7-(metyyliamino)-2-okso-1,2-dihydro-1,6-naftyridin-3-yyli)-2-fluorifenyyli)-3-fenyyliurean koostumuksia
US12391658B2 (en) 2020-02-18 2025-08-19 Vtv Therapeutics Llc Sulfoxide and sulfone glucokinase activators and methods of use thereof
CN116102522A (zh) * 2021-11-09 2023-05-12 河南省化工研究所有限责任公司 一种阳离子蓝染料中间体的制备方法
US11779572B1 (en) 2022-09-02 2023-10-10 Deciphera Pharmaceuticals, Llc Methods of treating gastrointestinal stromal tumors
WO2024112854A1 (en) 2022-11-22 2024-05-30 Odyssey Therapeutics, Inc. Inhibitors of ripk2 and medical uses thereof

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3646059A (en) * 1969-05-05 1972-02-29 Du Pont Plant growth regulatory ureidopyrazoles
AU646722B2 (en) * 1991-01-21 1994-03-03 Shionogi Seiyaku Kabushiki Kaisha 3-benzylidene-1-carbamoyl-2-pyrrolidone analog
US5162360A (en) * 1991-06-24 1992-11-10 Warner-Lambert Company 2-heteroatom containing urea and thiourea ACAT inhibitors
DE4227989A1 (de) 1992-08-21 1994-06-09 Schering Ag Mittel zur transdermalen Applikation enthaltend 3-Keto-desogestrel
US5871934A (en) * 1993-09-17 1999-02-16 Smithkline Beecham Corporation Screening methods using cytokine suppressive anti-inflammatory drug (CSAID) binding proteins
US5559137A (en) * 1994-05-16 1996-09-24 Smithkline Beecham Corp. Compounds
US5932576A (en) * 1997-05-22 1999-08-03 G. D. Searle & Company 3(5)-heteroaryl substituted pyrazoles as p38 kinase inhibitors
US6087381A (en) * 1997-05-22 2000-07-11 G. D. Searle & Company Pyrazole derivatives as p38 kinase inhibitors
EP1019040B1 (de) * 1997-05-23 2004-09-29 Bayer Corporation Arylharnstoffderivate zur behandlung von inflammatorischen oder immunomodulatorischen erkrankungen
US20020156104A1 (en) * 1997-06-13 2002-10-24 Jerry L. Adams Novel pyrazole and pyrazoline substituted compounds
AU1367599A (en) * 1997-11-03 1999-05-24 Boehringer Ingelheim Pharmaceuticals, Inc. Aromatic heterocyclic compounds as anti-inflammatory agents
JP4437270B2 (ja) * 1997-12-22 2010-03-24 バイエル コーポレイション 置換複素環式尿素を用いたrafキナーゼの阻害
NZ505845A (en) * 1997-12-22 2003-10-31 Bayer Ag Inhibition of RAF kinase using aryl and heteroaryl substituted heterocyclic ureas
IL136768A0 (en) * 1997-12-22 2001-06-14 Bayer Ag INHIBITION OF p38 KINASE ACTIVITY USING ARYL AND HETEROARYL SUBSTITUTED HETEROCYCLIC UREAS

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AU739642B2 (en) 2001-10-18
JP2001526223A (ja) 2001-12-18
ES2154253T1 (es) 2001-04-01
IL136738A0 (en) 2001-06-14
IL170201A (en) 2006-12-31
JP4403482B2 (ja) 2010-01-27
EP1041982A4 (de) 2006-06-14
EP1041982A1 (de) 2000-10-11
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EP1041982B1 (de) 2011-10-19

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