DE60017894T2 - Diaminothiazole und ihre verwendung zur inhibierung von proteinkinasen - Google Patents

Diaminothiazole und ihre verwendung zur inhibierung von proteinkinasen Download PDF

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Publication number
DE60017894T2
DE60017894T2 DE60017894T DE60017894T DE60017894T2 DE 60017894 T2 DE60017894 T2 DE 60017894T2 DE 60017894 T DE60017894 T DE 60017894T DE 60017894 T DE60017894 T DE 60017894T DE 60017894 T2 DE60017894 T2 DE 60017894T2
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Prior art keywords
aryl
amino
heteroaryl
alkyl
unsubstituted
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Expired - Fee Related
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DE60017894T
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German (de)
English (en)
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DE60017894D1 (de
Inventor
Song Shao CHU
Andrew Larry ALEGRIA
Lee Steven BENDER
Pritchett Suzanne BENEDICT
J. Allen BORCHARDT
Steven Robert KANIA
David Mitchell NAMBU
Anna Maria Tempczyk-Russell
Sepehr Sarshar
Dilip San Diego BHUMRALKAR
Peng San Diego ZHENGWEI
Michelle Yi San Diego YANG
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Agouron Pharmaceuticals LLC
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Agouron Pharmaceuticals LLC
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
    • C07D277/38Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62Benzothiazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6536Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and sulfur atoms with or without oxygen atoms, as the only ring hetero atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6536Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and sulfur atoms with or without oxygen atoms, as the only ring hetero atoms
    • C07F9/6539Five-membered rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
DE60017894T 1999-06-04 2000-06-02 Diaminothiazole und ihre verwendung zur inhibierung von proteinkinasen Expired - Fee Related DE60017894T2 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US13781099P 1999-06-04 1999-06-04
US137810P 1999-06-04
PCT/US2000/015188 WO2000075120A1 (en) 1999-06-04 2000-06-02 Diaminothiazoles and their use for inhibiting protein kinases

Publications (2)

Publication Number Publication Date
DE60017894D1 DE60017894D1 (de) 2005-03-10
DE60017894T2 true DE60017894T2 (de) 2005-12-29

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DE60017894T Expired - Fee Related DE60017894T2 (de) 1999-06-04 2000-06-02 Diaminothiazole und ihre verwendung zur inhibierung von proteinkinasen

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Country Link
US (1) US6620828B2 (https=)
EP (1) EP1181283B1 (https=)
JP (1) JP2003501420A (https=)
KR (1) KR20020015333A (https=)
CN (1) CN1359380A (https=)
AP (1) AP2001002341A0 (https=)
AT (1) ATE288424T1 (https=)
AU (1) AU778071B2 (https=)
BG (1) BG106276A (https=)
BR (1) BR0011585A (https=)
CA (1) CA2371158A1 (https=)
CZ (1) CZ20014213A3 (https=)
DE (1) DE60017894T2 (https=)
EA (1) EA200101268A1 (https=)
EE (1) EE200100659A (https=)
ES (1) ES2234628T3 (https=)
HR (1) HRP20020008A2 (https=)
HU (1) HUP0202897A3 (https=)
IL (1) IL146094A0 (https=)
IS (1) IS6183A (https=)
MA (1) MA25530A1 (https=)
MX (1) MXPA01012483A (https=)
NO (1) NO20015045L (https=)
NZ (1) NZ514881A (https=)
OA (1) OA11959A (https=)
PE (1) PE20010211A1 (https=)
PL (1) PL352714A1 (https=)
SK (1) SK17302001A3 (https=)
SV (1) SV2002000096A (https=)
UA (1) UA71971C2 (https=)
UY (1) UY26190A1 (https=)
WO (1) WO2000075120A1 (https=)
YU (1) YU85601A (https=)
ZA (1) ZA200108291B (https=)

Families Citing this family (66)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20020150921A1 (en) * 1996-02-09 2002-10-17 Francis Barany Detection of nucleic acid sequence differences using the ligase detection reaction with addressable arrays
PL342447A1 (en) * 1997-10-27 2001-06-04 Agouron Pharma Substituted 4-amino thiazol-2-yl compounds as inhibitors of cyclin-dependent kinases
US6262096B1 (en) 1997-11-12 2001-07-17 Bristol-Myers Squibb Company Aminothiazole inhibitors of cyclin dependent kinases
US20040226056A1 (en) * 1998-12-22 2004-11-11 Myriad Genetics, Incorporated Compositions and methods for treating neurological disorders and diseases
EP1169038B9 (en) 1999-04-15 2013-07-10 Bristol-Myers Squibb Company Cyclic protein tyrosine kinase inhibitors
US7125875B2 (en) 1999-04-15 2006-10-24 Bristol-Myers Squibb Company Cyclic protein tyrosine kinase inhibitors
WO2002050071A1 (en) 2000-12-21 2002-06-27 Bristol-Myers Squibb Company Thiazolyl inhibitors of tec family tyrosine kinases
US6756374B2 (en) 2001-01-22 2004-06-29 Hoffmann-La Roche Inc. Diaminothiazoles having antiproliferative activity
UA76977C2 (en) 2001-03-02 2006-10-16 Icos Corp Aryl- and heteroaryl substituted chk1 inhibitors and their use as radiosensitizers and chemosensitizers
JP2005504014A (ja) * 2001-06-08 2005-02-10 サイトビア インコーポレイテッド カスパーゼの活性化因子およびアポトーシスの誘導因子としての置換された3−アリール−5−アリール−[1,2,4]−オキサジアゾール類および類似体、並びにその使用法
EP1467981A1 (en) * 2002-01-25 2004-10-20 Kylix Pharmaceuticals B.V. 4(hetero-) aryl substituted (thia-/oxa-/pyra) zoles for inhibition of tie-2
US6818663B2 (en) * 2002-05-17 2004-11-16 Hoffmann-La Roches Diaminothiazoles
MXPA05001277A (es) * 2002-08-02 2005-10-06 Ab Science 2-(3-aminoaril)amino-4-aril-tiazoles y su uso como inhibidores del c-kit.
US8450302B2 (en) 2002-08-02 2013-05-28 Ab Science 2-(3-aminoaryl) amino-4-aryl-thiazoles and their use as c-kit inhibitors
AU2003278600A1 (en) * 2002-11-01 2004-05-25 Takeda Pharmaceutical Company Limited Agent for preventing or treating neuropathy
MXPA05008878A (es) * 2003-02-21 2005-10-05 Pfizer Derivados de aminotiazol sustituidos con cicloalquilo que contiene n y composiciones farmaceuticas para inhibir la proliferacion celular, y metodos para su uso.
US7078419B2 (en) 2003-03-10 2006-07-18 Boehringer Ingelheim Pharmaceuticals, Inc. Cytokine inhibitors
HUE047569T2 (hu) 2003-04-11 2020-04-28 Ptc Therapeutics Inc 1,2,4-oxadiazol-benzoesav vegyület és nonszensz szupresszióra történõ alkalmazása
WO2004092217A1 (en) * 2003-04-17 2004-10-28 Pfizer Inc. Crystal structure of vegfrkd: ligand complexes and methods of use thereof
WO2005007091A2 (en) * 2003-07-07 2005-01-27 Georgetown University Histone deacetylase inhibitors and methods of use thereof
EP1663204B1 (en) * 2003-08-29 2014-05-07 Exelixis, Inc. C-kit modulators and methods of use
EP2060270A3 (en) * 2003-10-16 2009-12-09 Imclone LLC Fibroblast growth factor receptor-1 inhibitors and methods of treatment thereof
AU2005205201B2 (en) 2004-01-12 2011-05-12 Merck Serono Sa Thiazole derivatives and use thereof
JPWO2005108370A1 (ja) * 2004-04-16 2008-03-21 味の素株式会社 ベンゼン化合物
US7211576B2 (en) 2004-04-20 2007-05-01 Hoffmann-La Roche Inc. Diaminothiazoles
AU2005271843A1 (en) * 2004-07-12 2006-02-16 Merck Sharp & Dohme Corp. Histone deacetylase inhibitors
WO2006125807A1 (en) 2005-05-24 2006-11-30 Laboratoires Serono S.A. Thiazole derivatives and use thereof
CN101248054B (zh) * 2005-05-24 2012-05-09 默克雪兰诺有限公司 噻唑衍生物及其应用
EP1945632B1 (en) 2005-11-08 2013-09-18 Vertex Pharmaceuticals Incorporated Heterocyclic modulators of atp-binding cassette transporters
AU2006336504C9 (en) * 2005-12-28 2015-05-14 Vertex Pharmaceuticals Incorporated 1-(benzo [D] [1,3] dioxol-5-yl) -N- (phenyl) cyclopropane- carboxamide derivatives and related compounds as modulators of ATP-Binding Cassette transporters for the treatment of Cystic Fibrosis
AU2012244242B2 (en) * 2005-12-28 2015-05-21 Vertex Pharmaceuticals Incorporated 1-(benzo [D] [1,3] dioxol-5-yl) -N- (phenyl) cyclopropane- carboxamide derivatives and related compounds as modulators of ATP-Binding Cassette transporters for the treatment of Cystic Fibrosis
WO2007084391A2 (en) * 2006-01-18 2007-07-26 Amgen Inc. Thiazole compounds as protein kinase b ( pkb) inhibitors
CN101484433A (zh) * 2006-02-15 2009-07-15 艾博特公司 新的乙酰辅酶a羧化酶(acc)抑制剂及其在糖尿病、肥胖症和代谢综合征中的应用
JP2009526868A (ja) * 2006-02-15 2009-07-23 アボット・ラボラトリーズ 新規なアセチル−CoAカルボキシラーゼ(ACC)阻害薬およびこれらの糖尿病、肥満および代謝症候群における使用
RU2462246C2 (ru) 2006-03-30 2012-09-27 ПиТиСи ТЕРАПЬЮТИКС, ИНК. Способы получения функционального белка из днк, имеющей нонсенс-мутацию, и лечения нарушений, ассоциированных с ней
CN101501023A (zh) * 2006-07-07 2009-08-05 贝林格尔.英格海姆国际有限公司 苯基取代的杂芳基衍生物及其作为抗肿瘤剂的用途
WO2008080134A2 (en) 2006-12-22 2008-07-03 Rigel Pharmaceuticals, Inc. 4-amin0-2- (hetero) arylamino-5- (hetero) arylthiazoles useful as axl inhibitors
US8969386B2 (en) 2007-05-09 2015-03-03 Vertex Pharmaceuticals Incorporated Modulators of CFTR
CA2692379A1 (en) * 2007-07-02 2009-01-08 Boehringer Ingelheim International Gmbh Antiproliferative compounds based on 5-membered heterocycles
CL2008001943A1 (es) 2007-07-02 2009-09-11 Boehringer Ingelheim Int Compuestos derivados de fenil-triazol, inhibidores de enzimas de señales especificas que participan del control de la proliferacion celular; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar cancer, infecciones, enfermedades inflamatorias y autoinmunes.
US7919504B2 (en) * 2007-07-17 2011-04-05 Amgen Inc. Thiadiazole modulators of PKB
EP2173728A2 (en) 2007-07-17 2010-04-14 Amgen Inc. Heterocyclic modulators of pkb
EP2639224B1 (en) 2007-12-07 2016-08-24 Vertex Pharmaceuticals Incorporated Process for producing cycloalkylcarboxiamido-pyridine benzoic acids
SI2225230T1 (sl) 2007-12-07 2017-03-31 Vertex Pharmaceuticals Incorporated Trdne oblike 3-(6-(1-2,2-difluorobenzo(d)(1,3)dioxol-5-il)ciklopropan- karboksamido)-3-metilpiridin-2-il) benzojske kisline
WO2009076140A1 (en) * 2007-12-13 2009-06-18 Smithkline Beecham Corporation Thiazole and oxazole kinase inhibitors
NZ720282A (en) 2008-02-28 2017-12-22 Vertex Pharma Heteroaryl derivatives as cftr modulators
UA103319C2 (en) 2008-05-06 2013-10-10 Глаксосмитклайн Ллк Thiazole- and oxazole-benzene sulfonamide compounds
US8778929B2 (en) 2008-09-29 2014-07-15 Boehringer Ingelheim International Gmbh Substituted heteroaryl inhibitors of B-RAF
PL2387395T3 (pl) 2009-01-16 2015-03-31 Rigel Pharmaceuticals Inc Inhibitory Axl do zastosowania w terapii skojarzonej do zapobiegania, leczenia lub postępowania z nowotworem przerzutowym
EP2492269A4 (en) * 2009-10-19 2013-08-07 Taisho Pharmaceutical Co Ltd aminothiazole
WO2011117382A1 (en) 2010-03-26 2011-09-29 Boehringer Ingelheim International Gmbh Pyridyltriazoles
WO2011117381A1 (en) 2010-03-26 2011-09-29 Boehringer Ingelheim International Gmbh B-raf kinase inhibitors
HRP20211752T1 (hr) 2010-04-07 2022-02-18 Vertex Pharmaceuticals Incorporated Farmaceutski pripravci 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioksol-5-il)ciklopropankarboksamido)-3-metilpiridin-2-il)benzojeve kiseline i njihova primjena
US8710055B2 (en) 2010-12-21 2014-04-29 Boehringer Ingelheim International Gmbh Triazolylphenyl sulfonamides as serine/threonine kinase inhibitors
WO2013112804A1 (en) 2012-01-25 2013-08-01 Vertex Pharmaceuticals Incorporated Formulations of 3-(6-(1-(2.2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid
TW201350479A (zh) 2012-04-26 2013-12-16 Ono Pharmaceutical Co Trk阻害化合物
AU2014219855B2 (en) 2013-02-19 2017-09-28 Ono Pharmaceutical Co., Ltd. Trk-inhibiting compound
GB201309333D0 (en) 2013-05-23 2013-07-10 Agency Science Tech & Res Purine diones as WNT pathway modulators
JP6963896B2 (ja) 2013-11-12 2021-11-10 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Vertex Pharmaceuticals Incorporated Cftr媒介性疾患の処置のための医薬組成物を調製する方法
KR102497273B1 (ko) 2014-03-06 2023-02-07 피티씨 테라퓨틱스, 인크. 1,2,4-옥사디아졸 벤조산의 약학 조성물 및 염
PT3221692T (pt) 2014-11-18 2021-09-10 Vertex Pharma Processo de realização de testagem de alta produtividade por cromatografia líquida de alta eficiência
JP2018531975A (ja) 2015-10-30 2018-11-01 ピーティーシー セラピューティクス,インコーポレーテッド てんかんの治療方法
WO2018052967A1 (en) * 2016-09-13 2018-03-22 Arbutus Biopharma, Inc. Substituted chromane-8-carboxamide compounds and analogues thereof, and methods using same
CN111233786B (zh) * 2020-02-04 2021-11-26 中国人民解放军军事科学院军事医学研究院 含五元杂环的苯磺酰胺类化合物及其制备方法和用途
CN121443601A (zh) * 2023-07-03 2026-01-30 英矽智能科技知识产权有限公司 作为cdk2/4/6抑制剂的取代的噻唑化合物及其使用方法
CN116874442B (zh) * 2023-07-27 2025-10-24 武汉呈瑞生物医药科技有限公司 一种有机化合物及其应用

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE273062C (de) 1912-04-19 1914-04-20 Deylen Sohn Firma Vorrichtung zum Schränken von Plattenzündspänen
AU558132B2 (en) 1981-05-27 1987-01-22 Labatt Brewing Co. Ltd. Malt sterilisation with hydrogen peroxide
EP0218728A1 (en) 1985-04-03 1987-04-22 Yamanouchi Pharmaceutical Co. Ltd. Phenylene derivatives
SG64322A1 (en) * 1991-05-10 1999-04-27 Rhone Poulenc Rorer Int Bis mono and bicyclic aryl and heteroaryl compounds which inhibit egf and/or pdgf receptor tyrosine kinase
JPH07505155A (ja) 1992-03-24 1995-06-08 メルク シヤープ エンド ドーム リミテツド コレシストキニン及び/又はガストリン拮抗活性を有する3−ウレイド置換ベンゾジアゼピン−2−オン及び治療におけるその使用
US5631156A (en) 1994-06-21 1997-05-20 The University Of Michigan DNA encoding and 18 KD CDK6 inhibiting protein
WO1996014843A2 (en) 1994-11-10 1996-05-23 Cor Therapeutics, Inc. Pharmaceutical pyrazole compositions useful as inhibitors of protein kinases
DK0808312T3 (da) 1995-02-02 2001-02-12 Smithkline Beecham Plc Indolderivater som 5-HT-receptorantagonist
US5710173A (en) 1995-06-07 1998-01-20 Sugen, Inc. Thienyl compounds for inhibition of cell proliferative disorders
AU6526896A (en) 1995-07-22 1997-02-18 Rhone-Poulenc Rorer Limited Substituted aromatic compounds and their pharmaceutical use
US5705499A (en) 1995-10-06 1998-01-06 Boehringer Ingelheim Pharmaceuticals, Inc. 8-arylalkyl- and 8-arylheteroalkyl-5,11-dihydro-6H-dipyrido 3,2-B:2',3'-e! 1!diazepines and their use in the treatment of HIV-1 infection
US5733920A (en) 1995-10-31 1998-03-31 Mitotix, Inc. Inhibitors of cyclin dependent kinases
US5760028A (en) 1995-12-22 1998-06-02 The Dupont Merck Pharmaceutical Company Integrin receptor antagonists
AU2103097A (en) 1996-03-15 1997-10-10 Zeneca Limited Cinnoline derivatives and use as medicine
EP0816357B1 (en) 1996-06-27 2002-01-09 Pfizer Inc. Substituted indazole derivatives
EA002113B1 (ru) 1996-09-04 2001-12-24 Пфайзер Инк. Производные индазола и их использование в качестве ингибиторов фосфодиэстеразы (фдэ) типа iv и продуцирования фактора некроза опухоли (фно)
ID18494A (id) 1996-10-02 1998-04-16 Novartis Ag Turunan pirazola leburan dan proses pembuatannya
PL342447A1 (en) * 1997-10-27 2001-06-04 Agouron Pharma Substituted 4-amino thiazol-2-yl compounds as inhibitors of cyclin-dependent kinases
IL135714A0 (en) 1997-11-04 2001-05-20 Pfizer Prod Inc Therapeutically active compounds based on indazole bioisostere replacement of catechol in pde4 inhibitors
IL135900A0 (en) 1997-11-04 2001-05-20 Pfizer Prod Inc Indazole bioisostere replacement of catechol in therapeuticaly active compounds
US6040321A (en) * 1997-11-12 2000-03-21 Bristol-Myers Squibb Company Aminothiazole inhibitors of cyclin dependent kinases
EP1087951B9 (en) * 1998-06-18 2006-09-13 Bristol-Myers Squibb Company Carbon substituted aminothiazole inhibitors of cyclin dependent kinases
ATE255575T1 (de) 1998-09-29 2003-12-15 Wyeth Corp Substituierte 3-cyanochinoline als protein tyrosine kinase inhibitoren

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EP1181283A1 (en) 2002-02-27
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YU85601A (sh) 2004-09-03
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AU5725400A (en) 2000-12-28
EA200101268A1 (ru) 2002-06-27
KR20020015333A (ko) 2002-02-27
CN1359380A (zh) 2002-07-17
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NO20015045D0 (no) 2001-10-17
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HUP0202897A2 (hu) 2002-12-28
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OA11959A (en) 2006-04-17
CA2371158A1 (en) 2000-12-14
ZA200108291B (en) 2002-12-24
ATE288424T1 (de) 2005-02-15
US20020025976A1 (en) 2002-02-28
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UA71971C2 (en) 2005-01-17
AU778071B2 (en) 2004-11-11
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