JP2008530011A - Rafインヒビター化合物および方法 - Google Patents

Rafインヒビター化合物および方法 Download PDF

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JP2008530011A
JP2008530011A JP2007554205A JP2007554205A JP2008530011A JP 2008530011 A JP2008530011 A JP 2008530011A JP 2007554205 A JP2007554205 A JP 2007554205A JP 2007554205 A JP2007554205 A JP 2007554205A JP 2008530011 A JP2008530011 A JP 2008530011A
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compound
pyridin
pyrazol
alkyl
oxime
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JP2008530011A5 (enExample
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エレン レアード,
ジョセフ ピー. リーシカトス,
マイク ウェルチ,
ジョナス グリナ,
ジョシュ ハンセン,
ブラッド ニューハウス,
アラン オリベーロ,
ジョージ トポラフ,
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Genentech Inc
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Genentech Inc
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    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • AHUMAN NECESSITIES
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    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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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JP2007554205A 2005-02-04 2006-02-02 Rafインヒビター化合物および方法 Pending JP2008530011A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US65005005P 2005-02-04 2005-02-04
PCT/US2006/003654 WO2006084015A2 (en) 2005-02-04 2006-02-02 Raf inhibitor compounds and methods

Publications (2)

Publication Number Publication Date
JP2008530011A true JP2008530011A (ja) 2008-08-07
JP2008530011A5 JP2008530011A5 (enExample) 2009-02-26

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US (2) US7491829B2 (enExample)
EP (1) EP1846391A2 (enExample)
JP (1) JP2008530011A (enExample)
KR (1) KR20070107104A (enExample)
CN (1) CN101282960A (enExample)
AR (1) AR053014A1 (enExample)
AU (1) AU2006210626A1 (enExample)
BR (1) BRPI0607346A2 (enExample)
CA (1) CA2596973A1 (enExample)
CR (1) CR9365A (enExample)
IL (1) IL185024A0 (enExample)
MA (1) MA29310B1 (enExample)
MX (1) MX2007009405A (enExample)
NO (1) NO20074473L (enExample)
RU (1) RU2007133111A (enExample)
TW (1) TW200639163A (enExample)
WO (1) WO2006084015A2 (enExample)
ZA (1) ZA200707289B (enExample)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013509384A (ja) * 2009-10-30 2013-03-14 ドメイン・セラピューティクス 新規オキシム誘導体及び代謝型グルタミン酸受容体のアロステリック調節因子としての利用
JP2016512498A (ja) * 2013-03-14 2016-04-28 イーライ リリー アンド カンパニー Cdc7阻害剤
JP2020504741A (ja) * 2016-12-23 2020-02-13 アルビナス・オペレーションズ・インコーポレイテッドArvinas Operations, Inc. Raf(急速進行性線維肉腫)ポリペプチドの標的分解のための化合物および方法

Families Citing this family (88)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103739595A (zh) 2006-10-02 2014-04-23 Irm责任有限公司 作为蛋白激酶抑制剂的化合物和组合物
MX2009004096A (es) 2006-10-17 2009-06-16 Stiefel Laboratories Metabolitos de talarozol.
US20090082354A1 (en) * 2007-09-20 2009-03-26 Wyeth Pyrazolo[5, 1-c] [1,2,4] triazines, methods for preparation and use thereof
WO2009111279A1 (en) * 2008-02-29 2009-09-11 Array Biopharma Inc. Pyrazole [3, 4-b] pyridine raf inhibitors
KR20100122505A (ko) * 2008-02-29 2010-11-22 어레이 바이오파마 인크. Raf 저해물질 화합물 및 이들의 이용 방법
WO2009111260A1 (en) * 2008-02-29 2009-09-11 Wyeth Phenylsulfonamide-substituted, pyrazolo[1, 5-a]pyrimidines, methods for preparation and uses thereof
WO2009108827A1 (en) * 2008-02-29 2009-09-03 Wyeth Fused tricyclic pyrazolo[1, 5-a]pyrimidines, methods for preparation and uses thereof
JP2011513332A (ja) * 2008-02-29 2011-04-28 アレイ バイオファーマ、インコーポレイテッド 癌の治療のためのraf阻害剤としてのn−(6−アミノピリジン−3−イル)−3−(スルホンアミド)ベンズアミド誘導体
US20110003809A1 (en) * 2008-02-29 2011-01-06 Array Biopharma Inc. Imidazo [4,5-b] pyridine derivatives used as raf inhibitors
JP2009286773A (ja) * 2008-03-14 2009-12-10 Bayer Cropscience Ag 殺虫性縮環式アリール類
PT2300013T (pt) 2008-05-21 2017-10-31 Ariad Pharma Inc Derivados de fósforo como inibidores de cinases
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
CA2744563A1 (en) * 2008-12-12 2010-06-17 Ariad Pharmaceuticals, Inc. Azaindole derivatives as kinase inhibitors
EP2440058A4 (en) 2009-06-12 2012-11-21 Dana Farber Cancer Inst Inc MELTED HETEROCYCLIC COMPOUNDS AND APPLICATIONS THEREOF
JP2013503188A (ja) 2009-08-28 2013-01-31 アレイ バイオファーマ、インコーポレイテッド Raf阻害化合物およびその使用方法
WO2011025938A2 (en) 2009-08-28 2011-03-03 Array Biopharma Inc. Raf inhibitor compounds and methods of use thereof
US20120214811A1 (en) 2009-08-28 2012-08-23 Ignacio Aliagas Raf inhibitor compounds and methods of use thereof
WO2011025947A1 (en) 2009-08-28 2011-03-03 Array Biopharma Inc. Raf inhibitor compounds and methods of use thereof
US20120157451A1 (en) 2009-08-28 2012-06-21 Genentech, Inc Raf inhibitor compounds and methods of use thereof
EP2470532A1 (en) 2009-08-28 2012-07-04 Array Biopharma, Inc. 1h-pyrazolo [ 3, 4-b]pyridine compounds for inhibiting raf kinase
CA2784807C (en) 2009-12-29 2021-12-14 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
PH12012501361A1 (en) 2009-12-31 2012-10-22 Centro Nac De Investigaciones Oncologicas Cnio Tricyclic compounds for use as kinase inhibitors
US20120122928A1 (en) 2010-08-11 2012-05-17 Bayer Cropscience Ag Heteroarylpiperidine and -Piperazine Derivatives as Fungicides
EP2423210A1 (de) 2010-08-25 2012-02-29 Bayer CropScience AG Heteroarylpiperidin- und -piperazinderivate als Fungizide
US8759527B2 (en) 2010-08-25 2014-06-24 Bayer Cropscience Ag Heteroarylpiperidine and -piperazine derivatives as fungicides
WO2012055837A1 (de) 2010-10-27 2012-05-03 Bayer Cropscience Ag Heteroarylpiperidin und -piperazinderivate als fungizide
EP2661434A4 (en) 2011-01-06 2014-07-09 Beta Pharma Canada Inc NEW URGES FOR THE TREATMENT AND PREVENTION OF CANCER
WO2012098387A1 (en) 2011-01-18 2012-07-26 Centro Nacional De Investigaciones Oncológicas (Cnio) 6, 7-ring-fused triazolo [4, 3 - b] pyridazine derivatives as pim inhibitors
WO2012104273A1 (de) 2011-02-01 2012-08-09 Bayer Cropscience Ag Heteroarylpiperidin und -piperazinderivate als fungizide
WO2012145503A1 (en) 2011-04-21 2012-10-26 Novartis Ag Pharmaceutical combinations
EP2704572B1 (en) 2011-05-04 2015-12-30 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
AR087405A1 (es) 2011-08-01 2014-03-19 Genentech Inc Metodos para tratar el cancer por el uso de antagonistas de union al eje pd-1 e inhibidores de mek
KR20140064971A (ko) 2011-09-19 2014-05-28 제넨테크, 인크. c-met 길항제 및 B-raf 길항제를 포함하는 조합 치료
WO2013074986A1 (en) 2011-11-17 2013-05-23 Dana-Farber Cancer Institute, Inc. Inhibitors of c-jun-n-terminal kinase (jnk)
US9408885B2 (en) 2011-12-01 2016-08-09 Vib Vzw Combinations of therapeutic agents for treating melanoma
EP2921481A1 (de) 2011-12-27 2015-09-23 Bayer Intellectual Property GmbH 4-piperidine carboxylic acid derivatives
EP2797888B1 (en) * 2011-12-31 2016-06-08 BeiGene, Ltd. Fused tricyclic compounds as raf kinase inhibitors
AU2013204563B2 (en) 2012-05-05 2016-05-19 Takeda Pharmaceutical Company Limited Compounds for inhibiting cell proliferation in EGFR-driven cancers
KR20240146112A (ko) 2012-08-17 2024-10-07 에프. 호프만-라 로슈 아게 코비메티닙 및 베무라피닙을 투여함을 포함하는 흑색종의 조합 치료법
US10112927B2 (en) 2012-10-18 2018-10-30 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
US10000483B2 (en) 2012-10-19 2018-06-19 Dana-Farber Cancer Institute, Inc. Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
US9758522B2 (en) 2012-10-19 2017-09-12 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
CN104994879A (zh) 2013-02-22 2015-10-21 霍夫曼-拉罗奇有限公司 治疗癌症和预防药物抗性的方法
MX2015011899A (es) 2013-03-15 2016-05-05 Genentech Inc Metodos para el tratamiento de cáncer y prevención de resistencia a los fármacos para el cáncer.
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
WO2014206344A1 (en) 2013-06-28 2014-12-31 Beigene, Ltd. Fused tricyclic amide compounds as multiple kinase inhibitors
ES2792183T3 (es) 2013-09-13 2020-11-10 Beigene Switzerland Gmbh Anticuerpos anti-PD1 y su uso como productos terapéuticos y de diagnóstico
EP3046557A1 (en) 2013-09-20 2016-07-27 Stichting Het Nederlands Kanker Instituut Rock in combination with mapk-pathway
WO2015041534A1 (en) 2013-09-20 2015-03-26 Stichting Het Nederlands Kanker Instituut P90rsk in combination with raf/erk/mek
CA2927917C (en) 2013-10-18 2022-08-09 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of proliferative diseases
JP6491202B2 (ja) 2013-10-18 2019-03-27 デイナ ファーバー キャンサー インスティチュート,インコーポレイテッド サイクリン依存性キナーゼ7(cdk7)の多環阻害剤
EP3122900A1 (en) 2014-03-24 2017-02-01 F. Hoffmann-La Roche AG Cancer treatment with c-met antagonists and correlation of the latter with hgf expression
US20170027940A1 (en) 2014-04-10 2017-02-02 Stichting Het Nederlands Kanker Instituut Method for treating cancer
US10017477B2 (en) 2014-04-23 2018-07-10 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
US9862688B2 (en) 2014-04-23 2018-01-09 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged janus kinase inhibitors and uses thereof
WO2015178770A1 (en) 2014-05-19 2015-11-26 Stichting Het Nederlands Kanker Instituut Compositions for cancer treatment
JP2017517552A (ja) 2014-06-13 2017-06-29 ジェネンテック, インコーポレイテッド 抗癌剤耐性の治療及び防止方法
US20170114323A1 (en) 2014-06-19 2017-04-27 Whitehead Institute For Biomedical Research Uses of kinase inhibitors for inducing and maintaining pluripotency
CN106604742B (zh) 2014-07-03 2019-01-11 百济神州有限公司 抗pd-l1抗体及其作为治疗剂及诊断剂的用途
AR101210A1 (es) 2014-07-15 2016-11-30 Genentech Inc Métodos de tratamiento de cáncer usando antagonistas de unión al eje pd-1 e inhibidores de mek
SG11201700496WA (en) 2014-07-22 2017-02-27 Cb Therapeutics Inc Anti-pd-1 antibodies
SG10201901057UA (en) 2014-08-05 2019-03-28 Cb Therapeutics Inc Anti-pd-l1 antibodies
EP3236959B1 (en) 2014-12-23 2025-09-24 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
CA2978518C (en) 2015-03-27 2023-11-21 Nathanael S. Gray Inhibitors of cyclin-dependent kinases
JP7320741B2 (ja) 2015-04-15 2023-08-04 ベイジーン リミテッド B-rafキナーゼのマレイン酸塩、結晶形、調整方法、及びその使用
CA2986441A1 (en) 2015-06-12 2016-12-15 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
JP7028766B2 (ja) 2015-09-09 2022-03-02 ダナ-ファーバー キャンサー インスティテュート, インコーポレイテッド サイクリン依存性キナーゼの阻害剤
JP6952691B2 (ja) 2015-11-19 2021-10-20 ジェネンテック, インコーポレイテッド B−raf阻害剤及び免疫チェックポイント阻害剤を使用してがんを治療する方法
CN109475536B (zh) 2016-07-05 2022-05-27 百济神州有限公司 用于治疗癌症的PD-l拮抗剂和RAF抑制剂的组合
PT3500299T (pt) 2016-08-19 2024-02-21 Beigene Switzerland Gmbh Combinação de zanubrutinib com um anticorpo anti-cd20 ou anti-pd-1 para utilização no tratamento do cancro
IL297717A (en) 2016-12-01 2022-12-01 Arvinas Operations Inc History of tetrahydronaphthalene and tetrahydroisoquinoline as estrogen receptor antagonists
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
CN110461847B (zh) 2017-01-25 2022-06-07 百济神州有限公司 (S)-7-(1-(丁-2-炔酰基)哌啶-4-基)-2-(4-苯氧基苯基)-4,5,6,7-四氢吡唑并[1,5-a]嘧啶-3-甲酰胺的结晶形式、其制备及用途
US11471538B2 (en) 2017-02-10 2022-10-18 INSERM (Institut National de la Santéet de la Recherche Medicale) Methods and pharmaceutical compositions for the treatment of cancers associated with activation of the MAPK pathway
TW202515616A (zh) 2017-06-26 2025-04-16 英屬開曼群島商百濟神州有限公司 抗pd-1抗體或其抗原結合片段在製備治療用於患有肝細胞癌(hcc)之藥物的用途
WO2019108795A1 (en) 2017-11-29 2019-06-06 Beigene Switzerland Gmbh Treatment of indolent or aggressive b-cell lymphomas using a combination comprising btk inhibitors
EP3732285A1 (en) 2017-12-28 2020-11-04 Tract Pharmaceuticals, Inc. Stem cell culture systems for columnar epithelial stem cells, and uses related thereto
WO2020005807A1 (en) 2018-06-25 2020-01-02 Dana-Farber Cancer Institute, Inc. Taire family kinase inhibitors and uses thereof
EP3902542A4 (en) 2018-12-28 2022-09-07 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 and uses thereof
EP4021450B1 (en) 2019-08-26 2025-11-05 Arvinas Operations, Inc. Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders
WO2021120890A1 (en) * 2019-12-20 2021-06-24 Novartis Ag Pyrazolyl derivatives useful as anti-cancer agents
EP4204418A1 (en) 2020-08-28 2023-07-05 Arvinas Operations, Inc. Rapidly accelerating fibrosarcoma protein degrading compounds and associated methods of use
EP4211128A1 (en) 2020-09-14 2023-07-19 Arvinas Operations, Inc. Crystalline forms of a compound for the targeted degradation of estrogen receptor
BR112023007912A2 (pt) * 2020-10-30 2024-01-02 Novartis Ag Formas cristalinas de um composto inibidor de kras g12c
US12371667B2 (en) 2021-05-13 2025-07-29 Washington University Enhanced methods for inducing and maintaining naive human pluripotent stem cells
KR20240090781A (ko) * 2021-11-30 2024-06-21 아비스코 테라퓨틱스 컴퍼니 리미티드 피라졸 유도체, 그 제조방법 및 약학에서의 응용
CN119301101A (zh) * 2022-07-29 2025-01-10 四川科伦博泰生物医药股份有限公司 甲基吡唑化合物、包含其的药物组合物及其制备方法和用途
TW202432544A (zh) 2022-09-07 2024-08-16 美商亞文納營運公司 快速加速纖維肉瘤降解化合物及相關使用方法

Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002088107A1 (fr) * 2001-04-26 2002-11-07 Eisai Co., Ltd. Compose azote a anneaux condenses possedant un groupe pyrazolyle et servant de substituant, et composition medicale le comprenant
WO2003055860A1 (en) * 2001-12-21 2003-07-10 Vernalis (Cambridge) Limited 3,4-diarylpyrazoles and their use in the therapy of cancer
WO2004014900A1 (en) * 2002-08-09 2004-02-19 Eli Lilly And Company Benzimidazoles and benzothiazoles as inhibitors of map kinase
WO2004022055A1 (en) * 2002-09-09 2004-03-18 Amgen Inc. 1, 4, 5-substituted 1, 2-dihydro-pyrazol-3-one and 3-alkoxy-1h-pyrazole derivatives s tnf-alpha and interleukin lowering agents for the treatment of inflammations
WO2004026871A1 (en) * 2002-09-17 2004-04-01 Eli Lilly And Company Novel pyrazolopyridine derivatves as pharmaceutical agents
WO2004050659A1 (en) * 2002-11-27 2004-06-17 Eli Lilly And Company Novel compounds as pharmaceutical agents
JP2004526727A (ja) * 2001-03-09 2004-09-02 ファイザー・プロダクツ・インク ベンゾイミダゾール抗炎症化合物
JP2004535404A (ja) * 2001-05-24 2004-11-25 イーライ・リリー・アンド・カンパニー 医薬物質としての新規ピロール誘導体
WO2004111036A1 (en) * 2003-06-16 2004-12-23 Smithkline Beecham Corporation 4- (heterocyclyl- fused phenyl)- 3- (phenyl or pyrid -2- yl) pyrazoles as inhibitors of the alk-5- receptor

Family Cites Families (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1245283A (en) 1968-10-04 1971-09-08 Labaz Pyrazole derivatives
JP2753659B2 (ja) 1990-09-03 1998-05-20 株式会社大塚製薬工場 ピラゾール誘導体
US5356897A (en) 1991-09-09 1994-10-18 Fujisawa Pharmaceutical Co., Ltd. 3-(heteroaryl)-pyrazololi[1,5-a]pyrimidines
JPH05125079A (ja) 1991-11-05 1993-05-21 Otsuka Pharmaceut Factory Inc ピラゾロ[1,5−aピリミジン誘導体
PT714898E (pt) 1994-06-21 2002-04-29 Otsuka Pharma Co Ltd Derivado de pirazolo¬1,5-a|pirimidina
US5486534A (en) 1994-07-21 1996-01-23 G. D. Searle & Co. 3,4-substituted pyrazoles for the treatment of inflammation
CN1169149A (zh) 1995-09-28 1997-12-31 株式会社大制药工场 止痛组合物
JPH10101672A (ja) 1996-08-06 1998-04-21 Otsuka Pharmaceut Factory Inc アデノシン増強剤
JPH10101671A (ja) 1996-08-08 1998-04-21 Otsuka Pharmaceut Factory Inc 一酸化窒素合成酵素阻害剤
US6514977B1 (en) 1997-05-22 2003-02-04 G.D. Searle & Company Substituted pyrazoles as p38 kinase inhibitors
RU2249591C2 (ru) 1997-05-22 2005-04-10 Дж.Д. Серл Энд Ко. 3(5)-гетероарилзамещенные пиразолы в качестве ингибиторов киназы p38
JP2000153671A (ja) 1998-11-20 2000-06-06 Fuji Photo Film Co Ltd 感熱記録材料
EP1173254A2 (en) 1999-04-27 2002-01-23 Smithkline Beecham Plc Novel treatment of neurotraumatic conditions with a raf inhibitor
TWI271406B (en) 1999-12-13 2007-01-21 Eisai Co Ltd Tricyclic condensed heterocyclic compounds, preparation method of the same and pharmaceuticals comprising the same
CA2369076A1 (en) 2000-02-05 2001-08-09 Vertex Pharmaceuticals Incorporated Pyrazole compositions useful as inhibitors of erk
AU2001236720A1 (en) 2000-02-05 2001-08-14 Bemis, Guy Compositions useful as inhibitors of erk
CZ20013540A3 (cs) 2000-02-05 2002-03-13 Vertex Pharmaceuticals Incorporated Deriváty pyrazolu jako inhibitory ERK a farmaceutický prostředek, který je obsahuje
JP2003525936A (ja) 2000-03-06 2003-09-02 スミスクライン ビーチャム パブリック リミテッド カンパニー Rafキナーゼ阻害物質としてのイミダゾール誘導体
CA2423154A1 (en) 2000-09-21 2002-03-28 David Kenneth Dean Imidazole derivatives as raf kinase inhibitors
KR100843281B1 (ko) 2000-12-28 2008-07-09 오노 야꾸힝 고교 가부시키가이샤 삼환식 복소환 유도체 화합물 및 그 화합물을 유효성분으로 하는 의약
ES2296910T3 (es) 2001-01-22 2008-05-01 Sankyo Company, Limited Compuestos sustituidos con grupo amino biciclicos.
GB0112348D0 (en) 2001-05-19 2001-07-11 Smithkline Beecham Plc Compounds
CA2456187A1 (en) 2001-08-03 2003-02-13 Qing Tang Pyrazole-derived kinase inhibitors and uses thereof
WO2003011855A2 (en) 2001-08-03 2003-02-13 Vertex Pharmaceuticals Incorporated Pyrazole-derived kinase inhibitors and uses thereof
GB0121490D0 (en) 2001-09-05 2001-10-24 Smithkline Beecham Plc Ciompounds
GB0121494D0 (en) 2001-09-05 2001-10-24 Smithkline Beecham Plc Compounds
US6897208B2 (en) 2001-10-26 2005-05-24 Aventis Pharmaceuticals Inc. Benzimidazoles
US20040010027A1 (en) 2001-12-17 2004-01-15 Pharmacia & Upjohn Spa Hydroxphenyl-pyrazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical comositions comprising them
JP4286146B2 (ja) * 2001-12-18 2009-06-24 メルク エンド カムパニー インコーポレーテッド メタボトロピックグルタミン酸受容体−5のヘテロアリール置換ピラゾール系調節剤
ATE365740T1 (de) 2002-05-10 2007-07-15 Smithkline Beecham Corp Substituierte pyrazolopyrimidine
GB0217786D0 (en) 2002-07-31 2002-09-11 Glaxo Group Ltd Compounds
TW200417547A (en) 2002-07-31 2004-09-16 Smithkline Beecham Corp Compounds
BR0314302A (pt) 2002-09-18 2005-07-05 Pfizer Producs Inc Compostos de pirazol como inibidores do fator de crescimento trnasformante (tgf)
WO2004026302A1 (en) 2002-09-19 2004-04-01 Eli Lilly And Company Methods of inhibiting tgf beta with substituted pyrazoles
US7176210B2 (en) 2003-02-10 2007-02-13 Pfizer Inc. Cannabinoid receptor ligands and uses thereof
CL2004000234A1 (es) 2003-02-12 2005-04-15 Biogen Idec Inc Compuestos derivados 3-(piridin-2-il)-4-heteroaril-pirazol sustituidos, antagonistas de aik5 y/o aik4; composicion farmaceutica y uso del compuesto en el tratamiento de desordenes fibroticos como esclerodermia, lupus nefritico, cicatrizacion de herid

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2004526727A (ja) * 2001-03-09 2004-09-02 ファイザー・プロダクツ・インク ベンゾイミダゾール抗炎症化合物
WO2002088107A1 (fr) * 2001-04-26 2002-11-07 Eisai Co., Ltd. Compose azote a anneaux condenses possedant un groupe pyrazolyle et servant de substituant, et composition medicale le comprenant
JP2004535404A (ja) * 2001-05-24 2004-11-25 イーライ・リリー・アンド・カンパニー 医薬物質としての新規ピロール誘導体
WO2003055860A1 (en) * 2001-12-21 2003-07-10 Vernalis (Cambridge) Limited 3,4-diarylpyrazoles and their use in the therapy of cancer
WO2004014900A1 (en) * 2002-08-09 2004-02-19 Eli Lilly And Company Benzimidazoles and benzothiazoles as inhibitors of map kinase
WO2004022055A1 (en) * 2002-09-09 2004-03-18 Amgen Inc. 1, 4, 5-substituted 1, 2-dihydro-pyrazol-3-one and 3-alkoxy-1h-pyrazole derivatives s tnf-alpha and interleukin lowering agents for the treatment of inflammations
WO2004026871A1 (en) * 2002-09-17 2004-04-01 Eli Lilly And Company Novel pyrazolopyridine derivatves as pharmaceutical agents
WO2004050659A1 (en) * 2002-11-27 2004-06-17 Eli Lilly And Company Novel compounds as pharmaceutical agents
WO2004111036A1 (en) * 2003-06-16 2004-12-23 Smithkline Beecham Corporation 4- (heterocyclyl- fused phenyl)- 3- (phenyl or pyrid -2- yl) pyrazoles as inhibitors of the alk-5- receptor

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013509384A (ja) * 2009-10-30 2013-03-14 ドメイン・セラピューティクス 新規オキシム誘導体及び代謝型グルタミン酸受容体のアロステリック調節因子としての利用
JP2016512498A (ja) * 2013-03-14 2016-04-28 イーライ リリー アンド カンパニー Cdc7阻害剤
JP2020504741A (ja) * 2016-12-23 2020-02-13 アルビナス・オペレーションズ・インコーポレイテッドArvinas Operations, Inc. Raf(急速進行性線維肉腫)ポリペプチドの標的分解のための化合物および方法
JP2023065395A (ja) * 2016-12-23 2023-05-12 アルビナス・オペレーションズ・インコーポレイテッド Raf(急速進行性線維肉腫)ポリペプチドの標的分解のための化合物および方法

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