JP7028766B2 - サイクリン依存性キナーゼの阻害剤 - Google Patents

サイクリン依存性キナーゼの阻害剤 Download PDF

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JP7028766B2
JP7028766B2 JP2018512916A JP2018512916A JP7028766B2 JP 7028766 B2 JP7028766 B2 JP 7028766B2 JP 2018512916 A JP2018512916 A JP 2018512916A JP 2018512916 A JP2018512916 A JP 2018512916A JP 7028766 B2 JP7028766 B2 JP 7028766B2
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JP2018526413A5 (https=
JP2018526413A (ja
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グレイ，ナサニエル，エス．
チャン，ティンフウ
クフャトコフスキ，ニコラス，ピー．
ハオ，ミンフェン
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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
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic 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
    • C07D277/32—Heterocyclic 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
    • C07D277/38—Nitrogen atoms
    • C07D277/44—Acylated amino or imino radicals
    • C07D277/46—Acylated amino or imino radicals by carboxylic acids, or sulfur or nitrogen analogues thereof
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/12—Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2018512916A 2015-09-09 2016-09-09 サイクリン依存性キナーゼの阻害剤 Active JP7028766B2 (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2021127000A JP2022020611A (ja) 2015-09-09 2021-08-02 サイクリン依存性キナーゼの阻害剤

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562216271P 2015-09-09 2015-09-09
US62/216,271 2015-09-09
PCT/US2016/051118 WO2017044858A2 (en) 2015-09-09 2016-09-09 Inhibitors of cyclin-dependent kinases

Related Child Applications (1)

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JP2021127000A Division JP2022020611A (ja) 2015-09-09 2021-08-02 サイクリン依存性キナーゼの阻害剤

Publications (3)

Publication Number Publication Date
JP2018526413A JP2018526413A (ja) 2018-09-13
JP2018526413A5 JP2018526413A5 (https=) 2019-10-24
JP7028766B2 true JP7028766B2 (ja) 2022-03-02

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JP2018512916A Active JP7028766B2 (ja) 2015-09-09 2016-09-09 サイクリン依存性キナーゼの阻害剤
JP2021127000A Pending JP2022020611A (ja) 2015-09-09 2021-08-02 サイクリン依存性キナーゼの阻害剤

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US (2) US11142507B2 (https=)
EP (2) EP3347018B1 (https=)
JP (2) JP7028766B2 (https=)
AU (1) AU2016319125B2 (https=)
CA (1) CA2996978A1 (https=)
WO (1) WO2017044858A2 (https=)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9180127B2 (en) 2009-12-29 2015-11-10 Dana-Farber Cancer Institute, Inc. Type II Raf kinase inhibitors
CA2856291C (en) 2011-11-17 2020-08-11 Dana-Farber Cancer Institute, Inc. Inhibitors of c-jun-n-terminal kinase (jnk)
EP2909194A1 (en) 2012-10-18 2015-08-26 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
US9758522B2 (en) 2012-10-19 2017-09-12 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
EP3057955B1 (en) 2013-10-18 2018-04-11 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of prolferative diseases
US10047070B2 (en) 2013-10-18 2018-08-14 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7)
AU2015371251B2 (en) 2014-12-23 2020-06-11 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
HK1246645A1 (zh) 2015-03-27 2018-09-14 达纳-法伯癌症研究所股份有限公司 细胞周期蛋白依赖性激酶的抑制剂
US10702527B2 (en) 2015-06-12 2020-07-07 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
CA3018429A1 (en) * 2016-04-22 2017-10-26 Dana-Farber Cancer Institute, Inc. Degradation of cyclin-dependent kinase 9 (cdk9) by conjugation of cdk9 inhibitors with e3 ligase ligand and methods of use
CN110099684B (zh) * 2016-11-03 2022-11-11 科尔沃斯制药股份有限公司 用于调节白介素-2诱导性t细胞激酶的化合物和方法
WO2018098361A1 (en) 2016-11-22 2018-05-31 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 12 (cdk12) and uses thereof
WO2019075386A1 (en) * 2017-10-13 2019-04-18 The Regents Of The University Of California MODULATORS OF MTORC1
TWI703149B (zh) 2017-11-16 2020-09-01 美商美國禮來大藥廠 用於抑制cdk7之化合物
EP3787629A4 (en) 2018-05-02 2022-01-05 Kinnate Biopharma Inc. CYCLINE-DEPENDENT KINASE INHIBITORS
US12187701B2 (en) 2018-06-25 2025-01-07 Dana-Farber Cancer Institute, Inc. Taire family kinase inhibitors and uses thereof
SG11202013175SA (en) 2018-06-29 2021-01-28 Kinnate Biopharma Inc Inhibitors of cyclin-dependent kinases
WO2020046770A1 (en) * 2018-08-31 2020-03-05 Institute For Cancer Research D/B/A The Research Institute Of Fox Chase Cancer Center Kinase activity in tumors
JP7660063B2 (ja) 2018-12-28 2025-04-10 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７のインヒビターおよびそれらの使用
TWI783480B (zh) 2020-05-27 2022-11-11 美商美國禮來大藥廠 用於抑制cdk7之化合物
CA3199617A1 (en) * 2020-11-20 2022-05-27 Vladimir Spiegelman Inhibitors of igf2bp1-rna binding
CN116802178A (zh) * 2020-11-20 2023-09-22 耶路撒冷希伯来大学伊萨姆研发有限公司 Igf2bp1-rna结合的抑制剂
KR20240035820A (ko) 2021-07-09 2024-03-18 플렉시움 인코포레이티드 Ikzf2를 조절하는 아릴 화합물 및 약학 조성물
WO2023107705A1 (en) 2021-12-10 2023-06-15 Incyte Corporation Bicyclic amines as cdk12 inhibitors
CN117447466A (zh) * 2022-07-19 2024-01-26 中国科学院上海药物研究所 噁唑类化合物及其制备方法和用途
WO2024140653A1 (zh) * 2022-12-27 2024-07-04 南京圣和药业股份有限公司 选择性cdk12/13抑制剂及其应用

Citations (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001053267A1 (en) 2000-01-24 2001-07-26 Shionogi & Co., Ltd. Compounds exhibiting thrombopoietin receptor agonism
JP2001522842A (ja) 1997-11-12 2001-11-20 ブリストル−マイヤーズ スクイブ カンパニー サイクリン依存性キナーゼのアミノチアゾール系阻害剤
JP2003509342A (ja) 1999-09-10 2003-03-11 メルク エンド カムパニー インコーポレーテッド チロシンキナーゼ阻害薬
JP2003516987A (ja) 1999-12-15 2003-05-20 ブリストル−マイヤーズ スクイブ カンパニー サイクリン依存性キナーゼのｎ−［５−［［［５−アルキル−２−オキサゾリル］メチル］チオ−２−チアゾリル］カルボキサミドインヒビター
JP2003516981A (ja) 1999-12-15 2003-05-20 ブリストル−マイヤーズ スクイブ カンパニー サイクリン依存キナーゼのアミノチアゾール阻害剤
WO2004002948A1 (ja) 2001-05-16 2004-01-08 Mitsubishi Pharma Corporation アミド化合物およびその医薬用途
JP2005506950A (ja) 2000-12-21 2005-03-10 ブリストル−マイヤーズ　スクイブ　カンパニー Ｔｅｃファミリーチロシンキナーゼのチアゾリルインヒビター
US20050228031A1 (en) 2004-04-13 2005-10-13 Bilodeau Mark T Tyrosine kinase inhibitors
JP2005533808A (ja) 2002-06-20 2005-11-10 ブリストル−マイヤーズ　スクイブ　カンパニー キナーゼ類のヘテロ環阻害剤
JP2006518368A (ja) 2003-02-21 2006-08-10 ファイザー・インク プロテインキナーゼ阻害剤としてのｎ−ヘテロシクリル置換アミノチアゾール誘導体
WO2006093247A1 (ja) 2005-02-28 2006-09-08 Japan Tobacco Inc. Ｓｙｋ阻害活性を有する新規なアミノピリジン化合物
JP2007509130A (ja) 2003-10-23 2007-04-12 アブ サイエンス チロシンキナーゼ阻害薬としての２−アミノアリールオキサゾール化合物
WO2007086584A1 (ja) 2006-01-30 2007-08-02 Meiji Seika Kaisha, Ltd. 新規ＦａｂＫおよびＦａｂＩ／Ｋ阻害剤
JP2008538749A (ja) 2005-04-15 2008-11-06 セレプ・ソシエテ・アノニム Ｎｐｙ拮抗物質、調製および使用
WO2009036016A1 (en) 2007-09-10 2009-03-19 Curis, Inc. Cdk inhibitors containing a zinc binding moiety
WO2010001166A1 (en) 2008-07-01 2010-01-07 Prosidion Limited Thiazole derivatives as gpr 119 modulators
JP2010514686A (ja) 2006-12-20 2010-05-06 ブリストル−マイヤーズ スクイブ カンパニー キナーゼ阻害剤として有用なチアゾリル化合物
JP2012529519A (ja) 2009-06-09 2012-11-22 アブラクシス バイオサイエンス リミテッド ライアビリティー カンパニー スチリル−トリアジン誘導体類及びそれらの治療応用
WO2015025197A1 (en) 2013-08-22 2015-02-26 Jubilant Biosys Limited Substituted pyrimidine compounds, compositions and medicinal applications thereof

Family Cites Families (261)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB796524A (en) 1956-03-21 1958-06-11 Hickson & Welch Ltd Improvements in or relating to optical whitening agents
US4231938A (en) 1979-06-15 1980-11-04 Merck & Co., Inc. Hypocholesteremic fermentation products and process of preparation
US4270537A (en) 1979-11-19 1981-06-02 Romaine Richard A Automatic hypodermic syringe
HU204253B (en) 1982-11-22 1991-12-30 Sandoz Ag Process for producing mevalonolactone analogues and derivatives and pharmaceutical compositions containing them
US4828991A (en) 1984-01-31 1989-05-09 Akzo N.V. Tumor specific monoclonal antibodies
US4596556A (en) 1985-03-25 1986-06-24 Bioject, Inc. Hypodermic injection apparatus
US4886499A (en) 1986-12-18 1989-12-12 Hoffmann-La Roche Inc. Portable injection appliance
GB8704027D0 (en) 1987-02-20 1987-03-25 Owen Mumford Ltd Syringe needle combination
US4790824A (en) 1987-06-19 1988-12-13 Bioject, Inc. Non-invasive hypodermic injection device
US4940460A (en) 1987-06-19 1990-07-10 Bioject, Inc. Patient-fillable and non-invasive hypodermic injection device assembly
US4941880A (en) 1987-06-19 1990-07-17 Bioject, Inc. Pre-filled ampule and non-invasive hypodermic injection device assembly
US4782084A (en) 1987-06-29 1988-11-01 Merck & Co., Inc. HMG-COA reductase inhibitors
US4885314A (en) 1987-06-29 1989-12-05 Merck & Co., Inc. Novel HMG-CoA reductase inhibitors
US5339163A (en) 1988-03-16 1994-08-16 Canon Kabushiki Kaisha Automatic exposure control device using plural image plane detection areas
FR2638359A1 (fr) 1988-11-03 1990-05-04 Tino Dalto Guide de seringue avec reglage de la profondeur de penetration de l'aiguille dans la peau
US5064413A (en) 1989-11-09 1991-11-12 Bioject, Inc. Needleless hypodermic injection device
US5312335A (en) 1989-11-09 1994-05-17 Bioject Inc. Needleless hypodermic injection device
US5420245A (en) 1990-04-18 1995-05-30 Board Of Regents, The University Of Texas Tetrapeptide-based inhibitors of farnesyl transferase
US5190521A (en) 1990-08-22 1993-03-02 Tecnol Medical Products, Inc. Apparatus and method for raising a skin wheal and anesthetizing skin
US5527288A (en) 1990-12-13 1996-06-18 Elan Medical Technologies Limited Intradermal drug delivery device and method for intradermal delivery of drugs
US5747469A (en) 1991-03-06 1998-05-05 Board Of Regents, The University Of Texas System Methods and compositions comprising DNA damaging agents and p53
GB9118204D0 (en) 1991-08-23 1991-10-09 Weston Terence E Needle-less injector
SE9102652D0 (sv) 1991-09-13 1991-09-13 Kabi Pharmacia Ab Injection needle arrangement
US5328483A (en) 1992-02-27 1994-07-12 Jacoby Richard M Intradermal injection device with medication and needle guard
US5383851A (en) 1992-07-24 1995-01-24 Bioject Inc. Needleless hypodermic injection device
US5569189A (en) 1992-09-28 1996-10-29 Equidyne Systems, Inc. hypodermic jet injector
US5334144A (en) 1992-10-30 1994-08-02 Becton, Dickinson And Company Single use disposable needleless injector
CA2111902A1 (en) 1992-12-21 1994-06-22 Jack Beuford Campbell Antitumor compositions and methods of treatment
WO1994019357A1 (en) 1993-02-23 1994-09-01 Merrell Dow Pharmaceuticals Inc. Farnesyl:protein transferase inhibitors as anticancer agents
CA2118985A1 (en) 1993-04-02 1994-10-03 Dinesh V. Patel Heterocyclic inhibitors of farnesyl protein transferase
WO1994026723A2 (en) 1993-05-14 1994-11-24 Genentech, Inc. ras FARNESYL TRANSFERASE INHIBITORS
US5602098A (en) 1993-05-18 1997-02-11 University Of Pittsburgh Inhibition of farnesyltransferase
EP0670314A4 (en) 1993-09-22 1996-04-10 Kyowa Hakko Kogyo Kk FARNESYL TRANSFERASE INHIBITORS.
US5661152A (en) 1993-10-15 1997-08-26 Schering Corporation Tricyclic sulfonamide compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
SG48750A1 (en) 1993-10-15 1998-05-18 Schering Corp Tricyclic carbonate compounds useful for inhabition of g-protein function for treatment of proliferative diseases
ZA947969B (en) 1993-10-15 1996-07-12 Schering Corp Tricyclic sulfonamide compounds useful for inhibition of g-protein function and for treatment of proliferative diseases
US5721236A (en) 1993-10-15 1998-02-24 Schering Corporation Tricyclic carbamate compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
IL111235A (en) 1993-10-15 2001-03-19 Schering Plough Corp Medicinal preparations for inhibiting protein G activity and for the treatment of malignant diseases, containing tricyclic compounds, some such new compounds and a process for the preparation of some of them
US5719148A (en) 1993-10-15 1998-02-17 Schering Corporation Tricyclic amide and urea compounds useful for inhibition of g-protein function and for treatment of proliferative diseases
ES2157994T3 (es) 1993-10-25 2001-09-01 Parke Davis & Co Inhibidores tetra y pentapeptidos sustituidos de la proteina farnesiltransferasa.
DE69417012T2 (de) 1993-11-04 1999-10-07 Abbott Laboratories, Abbott Park Cyclobutan-derivate als inhibitoren der squalen-synthetase und der protein-farnesyltransferase
US5783593A (en) 1993-11-04 1998-07-21 Abbott Laboratories Inhibitors of squalene synthetase and protein farnesyltransferase
NZ275691A (en) 1993-11-05 1998-03-25 Warner Lambert Co Di and tripeptides and compositions thereof which inhibit farnesyl transferase
US5484799A (en) 1993-12-09 1996-01-16 Abbott Laboratories Antifungal dorrigocin derivatives
WO1995024176A1 (en) 1994-03-07 1995-09-14 Bioject, Inc. Ampule filling device
US5466220A (en) 1994-03-08 1995-11-14 Bioject, Inc. Drug vial mixing and transfer device
JP3969737B2 (ja) 1994-03-15 2007-09-05 エーザイ株式会社 イソプレニルトランスフェラーゼ阻害剤
US6312699B1 (en) 1994-03-28 2001-11-06 Uab Research Foundation Ligands added to adenovirus fiber
IL113196A0 (en) 1994-03-31 1995-06-29 Bristol Myers Squibb Co Imidazole derivatives and pharmaceutical compositions containing the same
US5523430A (en) 1994-04-14 1996-06-04 Bristol-Myers Squibb Company Protein farnesyl transferase inhibitors
US5510510A (en) 1994-05-10 1996-04-23 Bristol-Meyers Squibb Company Inhibitors of farnesyl protein transferase
US5563255A (en) 1994-05-31 1996-10-08 Isis Pharmaceuticals, Inc. Antisense oligonucleotide modulation of raf gene expression
CN1150419A (zh) 1994-06-10 1997-05-21 罗纳-布朗克罗莱尔股份有限公司 新的法呢基转移酶抑制剂、其制法及其药物组合物
US5571792A (en) 1994-06-30 1996-11-05 Warner-Lambert Company Histidine and homohistidine derivatives as inhibitors of protein farnesyltransferase
CA2155448A1 (en) 1994-08-11 1996-02-12 Katerina Leftheris Inhibitors of farnesyl protein transferase
EP0776884B1 (en) 1994-08-11 2000-01-05 Banyu Pharmaceutical Co., Ltd. Substituted amide derivative
WO1996005169A1 (en) 1994-08-12 1996-02-22 Banyu Pharmaceutical Co., Ltd. N,n-disubstituted amic acid derivative
JPH10510261A (ja) 1994-12-09 1998-10-06 ワーナー−ランバート・カンパニー タンパク質：ファルネシルトランスフェラーゼの置換テトラーおよびペンタペプチド阻害剤
US5599302A (en) 1995-01-09 1997-02-04 Medi-Ject Corporation Medical injection system and method, gas spring thereof and launching device using gas spring
JP3929069B2 (ja) 1995-01-12 2007-06-13 ユニバーシティ オブ ピッツバーグ プレニルトランスフェラーゼの阻害剤
FR2729390A1 (fr) 1995-01-18 1996-07-19 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
FR2730491B1 (fr) 1995-02-09 1997-03-14 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
FR2730492B1 (fr) 1995-02-09 1997-03-14 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
US5700806A (en) 1995-03-24 1997-12-23 Schering Corporation Tricyclic amide and urea compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
US5684013A (en) 1995-03-24 1997-11-04 Schering Corporation Tricyclic compounds useful for inhibition of g-protein function and for treatment of proliferative diseases
IL117580A0 (en) 1995-03-29 1996-07-23 Merck & Co Inc Inhibitors of farnesyl-protein transferase and pharmaceutical compositions containing them
MX9707561A (es) 1995-04-07 1997-12-31 Schering Corp Compuestos de carbonil piperazinilo y piperidinilo.
IL117798A (en) 1995-04-07 2001-11-25 Schering Plough Corp Tricyclic compounds useful for inhibiting the function of protein - G and for the treatment of malignant diseases, and pharmaceutical preparations containing them
US5712280A (en) 1995-04-07 1998-01-27 Schering Corporation Tricyclic compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
US5891872A (en) 1995-04-07 1999-04-06 Schering Corporation Tricyclic compounds
US5831115A (en) 1995-04-21 1998-11-03 Abbott Laboratories Inhibitors of squalene synthase and protein farnesyltransferase
IL118101A0 (en) 1995-05-03 1996-09-12 Abbott Lab Inhibitors of farnesyltransferase
US5919780A (en) 1995-06-16 1999-07-06 Warner Lambert Company Tricyclic inhibitors of protein farnesyltransferase
FR2736641B1 (fr) 1995-07-10 1997-08-22 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
FR2736638B1 (fr) 1995-07-12 1997-08-22 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
CH690163A5 (fr) 1995-07-28 2000-05-31 Symphar Sa Dérivés gem-diphosphonates substitués utiles en tant qu'agents anti-cancers.
BR9611157A (pt) 1995-11-01 1999-03-30 Novartis Ag Derivados de purina e processos para sua preparação
JP4533466B2 (ja) 1995-11-06 2010-09-01 ユニバーシティ オブ ピッツバーグ 蛋白質イソプレニルトランスフェラーゼの阻害剤
CA2238081A1 (en) 1995-11-22 1997-05-29 S. Jane Desolms Inhibitors of farnesyl-protein transferase
DE69620445T2 (de) 1995-12-08 2002-12-12 Janssen Pharmaceutica N.V., Beerse (imidazol-5-yl)methyl-2-chinolinoderivate als farnesyl protein transferase inhibitoren
SK86198A3 (en) 1995-12-22 1999-02-11 Schering Corp Tricyclic amides useful for inhibition of g-protein function and for treatment of proliferative diseases
US5893397A (en) 1996-01-12 1999-04-13 Bioject Inc. Medication vial/syringe liquid-transfer apparatus
US6008372A (en) 1996-01-16 1999-12-28 Warner-Lambert Company Substituted dinaphthylmethyl and diheteroarylmethylacetyl histidine inhibitors of protein farnesyltransferase
US6673927B2 (en) 1996-02-16 2004-01-06 Societe De Conseils De Recherches Et D'applications Scientifiques, S.A.S. Farnesyl transferase inhibitors
JP2001519766A (ja) 1996-04-03 2001-10-23 メルク エンド カンパニー インコーポレーテッド ファルネシルタンパク質トランスフェラーゼの阻害剤
NZ332712A (en) 1996-05-22 2000-07-28 Warner Lambert Co Polypeptide inhibitors of protein farnesyl transferase
WO1998002436A1 (en) 1996-07-15 1998-01-22 Bristol-Myers Squibb Company Thiadioxobenzodiazepine inhibitors of farnesyl protein transferase
US5866702A (en) 1996-08-02 1999-02-02 Cv Therapeutics, Incorporation Purine inhibitors of cyclin dependent kinase 2
EP0951285A1 (en) 1996-12-30 1999-10-27 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
CA2276081A1 (en) 1996-12-30 1998-07-09 Lekhanh O. Tran Inhibitors of farnesyl-protein transferase
US5993412A (en) 1997-05-19 1999-11-30 Bioject, Inc. Injection apparatus
US6214852B1 (en) 1998-10-21 2001-04-10 Bristol-Myers Squibb Company N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases
CN1345334A (zh) 1999-01-29 2002-04-17 伊姆克罗尼系统公司 对kdr特异的抗体及其应用
GB9903762D0 (en) 1999-02-18 1999-04-14 Novartis Ag Organic compounds
GB9904387D0 (en) 1999-02-25 1999-04-21 Pharmacia & Upjohn Spa Antitumour synergistic composition
EP1187633A4 (en) 1999-04-08 2005-05-11 Arch Dev Corp USE OF ANTI-VEGF ANTIBODIES TO ENHANCE RADIATION IN ANTICANCER THERAPY
PE20010306A1 (es) 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa
US6921763B2 (en) 1999-09-17 2005-07-26 Abbott Laboratories Pyrazolopyrimidines as therapeutic agents
CA2385747A1 (en) 1999-09-17 2001-03-22 Gavin C. Hirst Pyrazolopyrimidines as therapeutic agents
ES2349762T3 (es) 2000-08-10 2011-01-11 Pfizer Italia S.R.L. Biciclo-pirazoles activos como inhibidores de quinasas, procedimientos para su preparación y composiciones farmacéuticas que los comprenden.
AU3938802A (en) 2000-10-31 2002-06-03 Aventis Pharma Inc Acyl and sulfonyl derivatives of 6,9-disubstituted 2-(trans-1,4-diaminocyclohexyl)-purines and their use as antiproliferative agents
US7429599B2 (en) 2000-12-06 2008-09-30 Signal Pharmaceuticals, Llc Methods for treating or preventing an inflammatory or metabolic condition or inhibiting JNK
NZ526472A (en) 2000-12-21 2004-04-30 Vertex Pharma Pyrazole compounds useful as protein kinase inhibitors
FR2818642B1 (fr) 2000-12-26 2005-07-15 Hoechst Marion Roussel Inc Nouveaux derives de la purine, leur procede de preparation, leur application a titre de medicaments, compositions pharmaceutiques et nouvelle utilistion
MXPA03008560A (es) 2001-03-22 2004-06-30 Abbot Gmbh & Co Kg Pirazolopirimidinas como agentes terapeuticos.
EP1373257B9 (en) 2001-03-29 2008-10-15 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
AU2002247847A1 (en) 2001-04-09 2002-10-21 Lorantis Limited Therapeutic use and identification of modulators of a hedgehog signalling pathway or one of its target pathways
US6881737B2 (en) 2001-04-11 2005-04-19 Amgen Inc. Substituted triazinyl acrylamide derivatives and methods of use
CA2446756C (en) 2001-06-01 2011-03-08 Vertex Pharmaceuticals Incorporated Thiazole compounds useful as inhibitors of protein kinase
US6825190B2 (en) 2001-06-15 2004-11-30 Vertex Pharmaceuticals Incorporated Protein kinase inhibitors and uses thereof
US7115617B2 (en) 2001-08-22 2006-10-03 Amgen Inc. Amino-substituted pyrimidinyl derivatives and methods of use
US6939874B2 (en) 2001-08-22 2005-09-06 Amgen Inc. Substituted pyrimidinyl derivatives and methods of use
WO2003026664A1 (en) 2001-09-26 2003-04-03 Bayer Corporation 2-phenylamino-4- (5-pyrazolylamino) -pyramidine derivatives as kinase inhibitors, in particular, src kinase inhibitors
WO2003051847A1 (en) 2001-12-19 2003-06-26 Smithkline Beecham P.L.C. (1-h-indazol-3-yl) -amide derivatives as gsk-3 inhibitors
FR2836915B1 (fr) 2002-03-11 2008-01-11 Aventis Pharma Sa Derives d'aminoindazoles, procede de preparation et intermediaires de ce procede a titre de medicaments et compositions pharmaceutiques les renfermant
WO2003095448A1 (en) 2002-05-06 2003-11-20 Bayer Pharmaceuticals Corporation Pyridinyl amino pyrimidine derivatives useful for treating hyper-proliferative disorders
JP4751063B2 (ja) 2002-05-17 2011-08-17 ファイザー イタリア ソシエタ ア レスポンサビリタ リミタータ キナーゼ阻害剤として活性のアミノインダゾール誘導体、それらの調製方法、及びそれらを含む薬学的組成物
AU2003279182A1 (en) 2002-06-19 2004-01-06 Bristol-Myers Squibb Company Use of compounds having an amine nucleus in manufacture of a medicament useful for treating factor viia-associated conditions
CA2491895C (en) 2002-07-09 2011-01-18 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
TWI329112B (en) 2002-07-19 2010-08-21 Bristol Myers Squibb Co Novel inhibitors of kinases
GB0217757D0 (en) 2002-07-31 2002-09-11 Glaxo Group Ltd Novel compounds
DE10239042A1 (de) 2002-08-21 2004-03-04 Schering Ag Makrozyclische Pyrimidine, deren Herstellung und Verwendung als Arzneimittel
US7119200B2 (en) 2002-09-04 2006-10-10 Schering Corporation Pyrazolopyrimidines as cyclin dependent kinase inhibitors
US7205308B2 (en) 2002-09-04 2007-04-17 Schering Corporation Trisubstituted 7-aminopyrazolopyrimidines as cyclin dependent kinase inhibitors
MY137843A (en) 2002-09-04 2009-03-31 Schering Corp Pyrazolopyrimidines as cyclin dependent kinase inhibitors
WO2004022561A1 (en) 2002-09-04 2004-03-18 Schering Corporation Pyrazolopyrimidines as cyclin-dependent kinase inhibitors
CN100376580C (zh) 2002-09-04 2008-03-26 先灵公司 作为细胞周期蛋白依赖性激酶抑制剂的吡唑并嘧啶
US20050250837A1 (en) 2002-10-18 2005-11-10 D Mello Santosh R Use of C-Raf inhibitors for the treatment of neurodegenerative diseases
ES2273047T3 (es) 2002-10-28 2007-05-01 Bayer Healthcare Ag Fenilaminopirimidinas sustituidas con heteroariloxi como inhibidores de rho-cinasa.
UA81790C2 (uk) 2002-12-19 2008-02-11 Фармация Италия С.П.А. Заміщені піролопіразольні похідні як інгібітори кінази
FR2850022B1 (fr) 2003-01-22 2006-09-08 Centre Nat Rech Scient Nouvelle utilisation de la mifepristone et de ses derives comme modulateurs de la voie de signalisation des proteines hedgehog et ses applications
ES2349532T3 (es) 2003-02-06 2011-01-04 Bristol-Myers Squibb Company Compuestos basados en tiazolilo útiles como inhibidores de cinasa.
JP4564485B2 (ja) 2003-02-28 2010-10-20 帝人ファーマ株式会社 ピラゾロ［１，５−ａ］ピリミジン誘導体
GB0304665D0 (en) 2003-02-28 2003-04-02 Teijin Ltd Compounds
GB0305142D0 (en) 2003-03-06 2003-04-09 Eisai London Res Lab Ltd Synthesis
GB0305559D0 (en) 2003-03-11 2003-04-16 Teijin Ltd Compounds
ATE396731T1 (de) 2003-03-25 2008-06-15 Vertex Pharma Thiazole zur verwendung als inhibitoren von protein-kinasen
US20070179161A1 (en) 2003-03-31 2007-08-02 Vernalis (Cambridge) Limited. Pyrazolopyrimidine compounds and their use in medicine
WO2004100868A2 (en) 2003-04-23 2004-11-25 Abbott Laboratories Method of treating transplant rejection
JP4810427B2 (ja) 2003-05-22 2011-11-09 アボット・ラボラトリーズ インダゾール、ベンズイソオキサゾールおよびベンズイソチアゾールキナーゼ阻害剤
SE0301906D0 (sv) 2003-06-26 2003-06-26 Astrazeneca Ab New compounds
PL2256106T3 (pl) 2003-07-22 2015-08-31 Astex Therapeutics Ltd Związki 3,4-pochodne 1h-pirazolu i ich zastosowanie jako kinazy zależne od cyklin (cdk) i modulatory kinazy syntazy glikogenu-3 (gsk-3)
US7442698B2 (en) 2003-07-24 2008-10-28 Amgen Inc. Substituted heterocyclic compounds and methods of use
MXPA06001098A (es) 2003-07-29 2006-04-24 Irm Llc Compuestos y composiciones utiles como inhibidores de proteina cinasa.
NZ585188A (en) 2003-08-15 2011-09-30 Novartis Ag 2,4-Pyrimidinediamines useful in the treatment of neoplastic diseases, inflammatory and immune system disorders
US20050130974A1 (en) 2003-10-17 2005-06-16 Rigel Pharmaceuticals, Inc. Benzothiazole compositions and their use as ubiquitin ligase inhibitors
WO2005037797A1 (en) 2003-10-21 2005-04-28 Pharmacia Corporation Substituted pyrazole urea compounds for the treatment of inflammation
DE10357510A1 (de) 2003-12-09 2005-07-07 Bayer Healthcare Ag Heteroarylsubstituierte Benzole
US20070281907A1 (en) 2003-12-22 2007-12-06 Watkins William J Kinase Inhibitor Phosphonate Conjugates
US7750020B2 (en) 2004-04-02 2010-07-06 Novartis Ag Sulfonamide-thiazolpyridine derivatives as glucokinase activators useful the treatment of Type 2 diabetes
DE102004017438A1 (de) 2004-04-08 2005-11-03 Bayer Healthcare Ag Hetaryloxy-substituierte Phenylaminopyrimidine
DE102004020570A1 (de) 2004-04-27 2005-11-24 Bayer Healthcare Ag Substituierte Phenylaminopyrimidine
GB0411791D0 (en) 2004-05-26 2004-06-30 Cyclacel Ltd Compounds
FR2871158A1 (fr) 2004-06-04 2005-12-09 Aventis Pharma Sa Indazoles substitues, compositions les contenant, procede de fabrication et utilisation
JP4688876B2 (ja) 2004-06-10 2011-05-25 アイアールエム・リミテッド・ライアビリティ・カンパニー タンパク質キナーゼ阻害剤としての化合物および組成物
DE102004028862A1 (de) 2004-06-15 2005-12-29 Merck Patent Gmbh 3-Aminoindazole
BRPI0514691A (pt) 2004-08-31 2008-06-17 Astrazeneca Ab composto ou um sal farmaceuticamente aceitável do mesmo, processo para preparar o mesmo, composição farmacêutica, e, uso de um composto ou um sal farmaceuticamente aceitável do mesmo
US20060100226A1 (en) 2004-09-10 2006-05-11 Sikorski James A 2-Thiopyrimidinones as therapeutic agents
US7829712B2 (en) 2004-09-20 2010-11-09 Xenon Pharmaceuticals Inc. Pyridazine derivatives for inhibiting human stearoyl-CoA-desaturase
WO2006040568A1 (en) 2004-10-15 2006-04-20 Astrazeneca Ab Quinoxalines as b raf inhibitors
US7632854B2 (en) 2004-11-17 2009-12-15 Pfizer Italia S.R.L. Aminoindazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
AU2005322855B2 (en) 2004-12-30 2012-09-20 Exelixis, Inc. Pyrimidine derivatives as kinase modulators and method of use
RU2368602C2 (ru) 2005-01-26 2009-09-27 Айрм Ллк Соединения и композиции в качестве ингибиторов протеинкиназ
TW200639163A (en) 2005-02-04 2006-11-16 Genentech Inc RAF inhibitor compounds and methods
WO2006085685A1 (ja) 2005-02-09 2006-08-17 Takeda Pharmaceutical Company Limited ピラゾール化合物
WO2006124731A2 (en) 2005-05-12 2006-11-23 Irm Llc Compounds and compositions as protein kinase inhibitors
DE602006014540D1 (en) 2005-05-16 2010-07-08 Irm Llc Pyrrolopyridinderivate als proteinkinaseinhibitoren
CN102206216B (zh) 2005-06-22 2014-11-12 普莱希科公司 作为蛋白质激酶抑制剂的吡咯并[2,3-b]吡啶衍生物
EP1926734A1 (en) 2005-08-22 2008-06-04 Amgen Inc. Pyrazolopyridine and pyrazolopyrimidine compounds useful as kinase enzymes modulators
WO2007035428A1 (en) 2005-09-15 2007-03-29 Bristol-Myers Squibb Company Met kinase inhibitors
AU2006295645B2 (en) 2005-09-30 2011-09-29 Msd K.K. 2-heteroaryl-substituted indole derivative
GT200600429A (es) 2005-09-30 2007-04-30 Compuestos organicos
GB0520955D0 (en) 2005-10-14 2005-11-23 Cyclacel Ltd Compound
US8247556B2 (en) 2005-10-21 2012-08-21 Amgen Inc. Method for preparing 6-substituted-7-aza-indoles
US20070149508A1 (en) * 2005-11-02 2007-06-28 Targegen, Inc. Six membered heteroaromatic inhibitors targeting resistant kinase mutations
EA015513B1 (ru) 2005-12-21 2011-08-30 Пфайзер Продактс Инк. Карбониламинопирролопиразолы в качестве эффективных ингибиторов киназ
SI2495016T1 (sl) 2005-12-23 2020-04-30 Ariad Pharmaceuticals, Inc. Biciklične heteroarilne spojine
WO2007076161A2 (en) * 2005-12-27 2007-07-05 Myriad Genetics, Inc Compounds with therapeutic activity
WO2007129195A2 (en) 2006-05-04 2007-11-15 Pfizer Products Inc. 4-pyrimidine-5-amino-pyrazole compounds
BRPI0712016A2 (pt) 2006-05-22 2011-12-27 Schering Corp pirazolo[1,5-a]pirimidinas
JP2009538352A (ja) 2006-05-26 2009-11-05 アストラゼネカ アクチボラグ 細胞増殖を阻害するための薬剤としての２−カルボシクロアミノ−４−イミダゾリルピリミジン類
BRPI0622054B8 (pt) 2006-09-22 2021-05-25 Oxford Amherst Llc composto e composição farmacêutica
WO2008043745A1 (en) 2006-10-11 2008-04-17 Nerviano Medical Sciences S.R.L. Substituted pyrrolo-pyrazole derivatives as kinase inhibitors
US20080188524A1 (en) * 2006-10-25 2008-08-07 Martin Augustin Methods of treating pain
CA2668286C (en) 2006-11-03 2014-09-16 Pharmacyclics, Inc. Bruton's tyrosine kinase activity probe and method of using
WO2008063888A2 (en) 2006-11-22 2008-05-29 Plexxikon, Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor
CN101547917A (zh) 2006-12-08 2009-09-30 霍夫曼-拉罗奇有限公司 用作jnk调节剂的取代的嘧啶类化合物及它们的应用
EP2120932B1 (en) 2006-12-20 2014-07-09 Nerviano Medical Sciences S.r.l. Indazole derivatives as kinase inhibitors for the treatment of cancer
AU2007336811A1 (en) 2006-12-21 2008-07-03 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
NZ578876A (en) 2007-02-07 2012-12-21 Pfizer 3-amino-pyrrolo[3,4-c]pyrazole-5 (1h, 4h, 6h) carbaldehyde derivatives as pkc inhibitors
CN101679308B (zh) 2007-03-14 2014-05-07 埃克塞里艾克西斯公司 Hedgehog途径抑制剂
WO2008124393A1 (en) 2007-04-04 2008-10-16 Irm Llc Benzothiazole derivatives and their use as protein kinase inhibitors
EP2195321B1 (en) 2007-04-12 2016-10-19 Pfizer Inc. 3-amido-pyrrolo[3,4-c]pyrazole-5(1h, 4h,6h) carbaldehyde derivatives as inhibitors of protein kinase c
WO2008144253A1 (en) 2007-05-14 2008-11-27 Irm Llc Protein kinase inhibitors and methods for using thereof
US8242271B2 (en) 2007-06-04 2012-08-14 Avila Therapeutics, Inc. Heterocyclic compounds and uses thereof
CA2688616A1 (en) 2007-06-05 2008-12-11 Emory University Selective inhibitors for cyclin-dependent kinases
AU2008282728B2 (en) 2007-08-02 2012-04-19 Amgen Inc. Pl3 kinase modulators and methods of use
US20090054392A1 (en) 2007-08-20 2009-02-26 Wyeth Naphthylpyrimidine, naphthylpyrazine and naphthylpyridazine analogs and their use as agonists of the wnt-beta-catenin cellular messaging system
WO2009032703A1 (en) 2007-08-28 2009-03-12 Irm Llc 2- (het) arylamino-6-aminopyridine derivatives and fused forms thereof as anaplastic lymphoma kinase inhibitors
WO2009028655A1 (ja) 2007-08-30 2009-03-05 Takeda Pharmaceutical Company Limited 複素環化合物およびその用途
WO2009122180A1 (en) 2008-04-02 2009-10-08 Medical Research Council Pyrimidine derivatives capable of inhibiting one or more kinases
GB0806419D0 (en) 2008-04-09 2008-05-14 Ineos Fluor Holdings Ltd Process
US20100197688A1 (en) 2008-05-29 2010-08-05 Nantermet Philippe G Epha4 rtk inhibitors for treatment of neurological and neurodegenerative disorders and cancer
CA2725940A1 (en) 2008-05-30 2009-12-23 Merck Sharp & Dohme Corp. Novel substituted azabenzoxazoles
TWI490214B (zh) 2008-05-30 2015-07-01 艾德克 上野股份有限公司 苯或噻吩衍生物及該等作為ｖａｐ－１抑制劑之用途
WO2009152027A1 (en) 2008-06-12 2009-12-17 Merck & Co., Inc. 5,7-dihydro-6h-pyrrolo[2,3-d]pyrimidin-6-one derivatives for mark inhibition
EP2303890A4 (en) 2008-06-19 2012-04-11 Progenics Pharm Inc INHIBITORS OF PHOSPHATIDYLINOSITE-3-KINASE
WO2010008847A2 (en) 2008-06-24 2010-01-21 Takeda Pharmaceutical Company Limited Pi3k/m tor inhibitors
AU2009279936A1 (en) 2008-08-05 2010-02-11 Banyu Pharmaceutical Co., Ltd. Therapeutic compounds
CN102256966B (zh) 2008-10-17 2016-02-10 白头生物医学研究所 可溶性mTOR复合物和其调节剂
CN101723936B (zh) 2008-10-27 2014-01-15 上海睿星基因技术有限公司 激酶抑制剂及其在药学中的用途
WO2010075542A1 (en) * 2008-12-23 2010-07-01 Curis, Inc. Cdk inhibitors
US20120165309A1 (en) 2009-02-12 2012-06-28 Astellas Pharma Inc. Hetero ring derivative
TW201103943A (en) 2009-04-27 2011-02-01 Shionogi & Co Urea derivative having pi3k inhibitory activity
KR101705158B1 (ko) 2009-05-05 2017-02-09 다나-파버 캔서 인스티튜트 인크. Ｅｇｆｒ 억제제 및 질환 치료방법
TW201102387A (en) 2009-06-08 2011-01-16 Medicinova Inc Substituted pyrazolo[1,5-a]pyridine compounds having multi-target activity
EP2440058A4 (en) 2009-06-12 2012-11-21 Dana Farber Cancer Inst Inc MELTED HETEROCYCLIC COMPOUNDS AND APPLICATIONS THEREOF
FR2948367A1 (fr) 2009-07-24 2011-01-28 Centre Nat Rech Scient Derives d'acyl-guanidines modulateurs de la voie de signalisation des proteines hedgehog
AU2010306803A1 (en) 2009-10-14 2012-05-03 Bristol-Myers Squibb Company Compounds for the treatment of hepatitis C
US20110207736A1 (en) 2009-12-23 2011-08-25 Gatekeeper Pharmaceuticals, Inc. Compounds that modulate egfr activity and methods for treating or preventing conditions therewith
US9180127B2 (en) 2009-12-29 2015-11-10 Dana-Farber Cancer Institute, Inc. Type II Raf kinase inhibitors
BR112012023021A2 (pt) 2010-03-16 2016-05-31 Dana Farber Cancer Inst Inc compostos de indazol e seus usos
PL2902030T3 (pl) 2010-05-14 2017-07-31 Dana-Farber Cancer Institute, Inc. Związki tienotriazolodiazepinowe do leczenia nowotworu
MX2013005445A (es) 2010-11-19 2013-07-29 Hoffmann La Roche Pirazolopiridinas y el uso de pirazolopiridinas como inhibidores de tirosina cinasa 2 (tyk2).
US8546443B2 (en) 2010-12-21 2013-10-01 Boehringer Ingelheim International Gmbh Benzylic oxindole pyrimidines
WO2012090219A2 (en) 2010-12-31 2012-07-05 Jubilant Biosys Ltd. Thiazole compounds useful as acetyl-coa carboxylase (acc) inhibitors
CN103781780B (zh) 2011-07-28 2015-11-25 赛尔佐姆有限公司 作为jak抑制剂的杂环基嘧啶类似物
US20150017156A1 (en) 2011-09-16 2015-01-15 The Ohio State University Esx-mediated transcription modulators and related methods
US8962855B2 (en) * 2011-09-28 2015-02-24 Purdue Pharmaceutical Products, L.P. Nitrogen mustard derivatives
CA2856291C (en) 2011-11-17 2020-08-11 Dana-Farber Cancer Institute, Inc. Inhibitors of c-jun-n-terminal kinase (jnk)
GB201204384D0 (en) 2012-03-13 2012-04-25 Univ Dundee Anti-flammatory agents
WO2013154778A1 (en) 2012-04-11 2013-10-17 Dana-Farber Cancer Institute, Inc. Host targeted inhibitors of dengue virus and other viruses
EP2909194A1 (en) 2012-10-18 2015-08-26 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
CN103319483B (zh) 2012-10-19 2016-08-03 药源药物化学（上海）有限公司 一种利拉列汀重要中间体的制备方法
US9758522B2 (en) 2012-10-19 2017-09-12 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
TWI621618B (zh) 2013-03-13 2018-04-21 比利時商健生藥品公司 經取代２－氮雜雙環類及其作為食慾素受體調控劑之用途
JP2016518316A (ja) 2013-03-15 2016-06-23 セルジーン アビロミクス リサーチ， インコーポレイテッド Ｍｋ２阻害剤およびそれらの使用
US10130633B2 (en) * 2013-03-20 2018-11-20 Bayer Pharma Aktiengesellschaft Compounds
US9938279B2 (en) 2013-04-09 2018-04-10 Energenesis Biomedical Co., Ltd Method for treating disease or condition susceptible to amelioration by AMPK activators and compounds of formula which are useful to activate AMP-activated protein kinase (AMPK)
AU2014292888B2 (en) 2013-07-25 2018-03-22 Dana-Farber Cancer Institute, Inc. Inhibitors of transcription factors and uses thereof
US10047070B2 (en) 2013-10-18 2018-08-14 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7)
EP3057955B1 (en) 2013-10-18 2018-04-11 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of prolferative diseases
CA2936865A1 (en) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Diaminopyrimidine benzenesulfone derivatives and uses thereof
WO2015117087A1 (en) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Uses of diazepane derivatives
WO2015117055A1 (en) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Dihydropteridinone derivatives and uses thereof
BR112016017045A2 (pt) 2014-01-31 2017-08-08 Dana Farber Cancer Inst Inc Derivados de diazepano e usos dos mesmos
CN106458990B (zh) 2014-04-04 2019-06-07 希洛斯医药品股份有限公司 细胞周期蛋白依赖性激酶7(cdk7)的抑制剂
EP3129371B1 (en) * 2014-04-05 2020-07-29 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
US9862688B2 (en) 2014-04-23 2018-01-09 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged janus kinase inhibitors and uses thereof
US10017477B2 (en) 2014-04-23 2018-07-10 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
CN104829610B (zh) 2014-06-20 2017-03-15 中国科学院合肥物质科学研究院 一种新型布鲁顿酪氨酸激酶抑制剂
US10457691B2 (en) 2014-07-21 2019-10-29 Dana-Farber Cancer Institute, Inc. Macrocyclic kinase inhibitors and uses thereof
AU2015292818B2 (en) 2014-07-21 2020-01-16 Dana-Farber Cancer Institute, Inc. Imidazolyl kinase inhibitors and uses thereof
WO2016058544A1 (en) 2014-10-16 2016-04-21 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
JP6690543B2 (ja) 2014-10-31 2020-04-28 宇部興産株式会社 置換ジヒドロピロロピラゾール化合物
AU2015371251B2 (en) 2014-12-23 2020-06-11 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
CN107530329B (zh) 2015-03-09 2021-10-08 奥瑞基尼探索技术有限公司 用作CDK抑制剂的吡唑并[1，5-a][1，3，5]三嗪和吡唑并[1，5-a]嘧啶衍生物
HK1246645A1 (zh) 2015-03-27 2018-09-14 达纳-法伯癌症研究所股份有限公司 细胞周期蛋白依赖性激酶的抑制剂
US10702527B2 (en) 2015-06-12 2020-07-07 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
US20180243304A1 (en) 2015-08-28 2018-08-30 Novartis Ag Pharmaceutical combinations comprising (a) the cyclin dependent kinase 4/6 (cdk4/6) inhibitor lee011 (=ribociclib), and (b) the epidermal growth factor receptor (egfr) inhibitor erlotinib, for the treatment or prevention of cancer

Patent Citations (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2001522842A (ja) 1997-11-12 2001-11-20 ブリストル−マイヤーズ スクイブ カンパニー サイクリン依存性キナーゼのアミノチアゾール系阻害剤
JP2003509342A (ja) 1999-09-10 2003-03-11 メルク エンド カムパニー インコーポレーテッド チロシンキナーゼ阻害薬
JP2003516987A (ja) 1999-12-15 2003-05-20 ブリストル−マイヤーズ スクイブ カンパニー サイクリン依存性キナーゼのｎ−［５−［［［５−アルキル−２−オキサゾリル］メチル］チオ−２−チアゾリル］カルボキサミドインヒビター
JP2003516981A (ja) 1999-12-15 2003-05-20 ブリストル−マイヤーズ スクイブ カンパニー サイクリン依存キナーゼのアミノチアゾール阻害剤
WO2001053267A1 (en) 2000-01-24 2001-07-26 Shionogi & Co., Ltd. Compounds exhibiting thrombopoietin receptor agonism
JP2005506950A (ja) 2000-12-21 2005-03-10 ブリストル−マイヤーズ　スクイブ　カンパニー Ｔｅｃファミリーチロシンキナーゼのチアゾリルインヒビター
WO2004002948A1 (ja) 2001-05-16 2004-01-08 Mitsubishi Pharma Corporation アミド化合物およびその医薬用途
JP2005533808A (ja) 2002-06-20 2005-11-10 ブリストル−マイヤーズ　スクイブ　カンパニー キナーゼ類のヘテロ環阻害剤
JP2006518368A (ja) 2003-02-21 2006-08-10 ファイザー・インク プロテインキナーゼ阻害剤としてのｎ−ヘテロシクリル置換アミノチアゾール誘導体
JP2007509130A (ja) 2003-10-23 2007-04-12 アブ サイエンス チロシンキナーゼ阻害薬としての２−アミノアリールオキサゾール化合物
US20050228031A1 (en) 2004-04-13 2005-10-13 Bilodeau Mark T Tyrosine kinase inhibitors
WO2006093247A1 (ja) 2005-02-28 2006-09-08 Japan Tobacco Inc. Ｓｙｋ阻害活性を有する新規なアミノピリジン化合物
JP2008538749A (ja) 2005-04-15 2008-11-06 セレプ・ソシエテ・アノニム Ｎｐｙ拮抗物質、調製および使用
WO2007086584A1 (ja) 2006-01-30 2007-08-02 Meiji Seika Kaisha, Ltd. 新規ＦａｂＫおよびＦａｂＩ／Ｋ阻害剤
JP2010514686A (ja) 2006-12-20 2010-05-06 ブリストル−マイヤーズ スクイブ カンパニー キナーゼ阻害剤として有用なチアゾリル化合物
WO2009036016A1 (en) 2007-09-10 2009-03-19 Curis, Inc. Cdk inhibitors containing a zinc binding moiety
WO2010001166A1 (en) 2008-07-01 2010-01-07 Prosidion Limited Thiazole derivatives as gpr 119 modulators
JP2012529519A (ja) 2009-06-09 2012-11-22 アブラクシス バイオサイエンス リミテッド ライアビリティー カンパニー スチリル−トリアジン誘導体類及びそれらの治療応用
WO2015025197A1 (en) 2013-08-22 2015-02-26 Jubilant Biosys Limited Substituted pyrimidine compounds, compositions and medicinal applications thereof

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
ＰＬｏＳ Ｏｎｅ，2013年，Ｖｏｌ．８，Ｎｏ．３，ｅ５７８８８，ｐ１－９

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