JP6854762B2 - サイクリン依存性キナーゼ7(cdk7)の阻害剤 - Google Patents

サイクリン依存性キナーゼ7(cdk7)の阻害剤 Download PDF

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JP6854762B2
JP6854762B2 JP2017534308A JP2017534308A JP6854762B2 JP 6854762 B2 JP6854762 B2 JP 6854762B2 JP 2017534308 A JP2017534308 A JP 2017534308A JP 2017534308 A JP2017534308 A JP 2017534308A JP 6854762 B2 JP6854762 B2 JP 6854762B2
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alkyl
optionally substituted
carbamate
formula
ring
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JP2018502098A (ja
JP2018502098A5 (cg-RX-API-DMAC7.html
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グレイ,ナサニエル,エス.
リアン,ヤンケ
チャン,ティンフー
クウィアトコウスキ,ニコラス,ポール
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Dana Farber Cancer Institute Inc
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • A61K31/41621,2-Diazoles condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10Spiro-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2017534308A 2014-12-23 2015-12-23 サイクリン依存性キナーゼ7(cdk7)の阻害剤 Active JP6854762B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462096040P 2014-12-23 2014-12-23
US62/096,040 2014-12-23
PCT/US2015/000297 WO2016105528A2 (en) 2014-12-23 2015-12-23 Inhibitors of cyclin-dependent kinase 7 (cdk7)

Publications (3)

Publication Number Publication Date
JP2018502098A JP2018502098A (ja) 2018-01-25
JP2018502098A5 JP2018502098A5 (cg-RX-API-DMAC7.html) 2020-07-09
JP6854762B2 true JP6854762B2 (ja) 2021-04-07

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JP2017534308A Active JP6854762B2 (ja) 2014-12-23 2015-12-23 サイクリン依存性キナーゼ7(cdk7)の阻害剤

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US (2) US10870651B2 (cg-RX-API-DMAC7.html)
EP (1) EP3236959B1 (cg-RX-API-DMAC7.html)
JP (1) JP6854762B2 (cg-RX-API-DMAC7.html)
AU (1) AU2015371251B2 (cg-RX-API-DMAC7.html)
HK (1) HK1245260A1 (cg-RX-API-DMAC7.html)
WO (1) WO2016105528A2 (cg-RX-API-DMAC7.html)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011090738A2 (en) 2009-12-29 2011-07-28 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
AU2012340200B2 (en) 2011-11-17 2017-10-12 Dana-Farber Cancer Institute, Inc. Inhibitors of c-Jun-N-Terminal Kinase (JNK)
WO2014063068A1 (en) 2012-10-18 2014-04-24 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
WO2014063054A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Bone marrow on x chromosome kinase (bmx) inhibitors and uses thereof
WO2014063061A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
CA2927920A1 (en) 2013-10-18 2015-04-23 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
EP3129371B1 (en) * 2014-04-05 2020-07-29 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
WO2015164604A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged janus kinase inhibitors and uses thereof
WO2015164614A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
AU2015371251B2 (en) 2014-12-23 2020-06-11 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
US10550121B2 (en) 2015-03-27 2020-02-04 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
HRP20240101T1 (hr) 2015-06-04 2024-03-29 Aurigene Oncology Limited Supstituirani heterociklil derivati kao cdk inhibitori
CA2986441A1 (en) 2015-06-12 2016-12-15 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
WO2017044858A2 (en) 2015-09-09 2017-03-16 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
ES2968227T3 (es) 2016-12-23 2024-05-08 Aquinnah Pharmaceuticals Inc Compuestos, composiciones y procedimientos de uso
US10913983B2 (en) 2017-07-18 2021-02-09 University Of South Carolina Sensitivity markers and uses for CDK7 inhibitors in breast cancers
US11447493B2 (en) 2018-05-02 2022-09-20 Kinnate Biopharma Inc. Inhibitors of cyclin-dependent kinases
CA3099763A1 (en) 2018-06-25 2020-01-02 Dana-Farber Cancer Institute, Inc. Taire family kinase inhibitors and uses thereof
AU2019291935A1 (en) 2018-06-29 2021-02-04 Kinnate Biopharma Inc. Inhibitors of cyclin-dependent kinases
WO2020100944A1 (ja) * 2018-11-14 2020-05-22 宇部興産株式会社 ジヒドロピロロピラゾール誘導体
CA3124422A1 (en) * 2018-12-28 2020-07-02 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 and uses thereof
JP7680999B2 (ja) * 2019-07-23 2025-05-21 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
CN114174281B (zh) * 2019-08-05 2025-02-07 达纳-法伯癌症研究公司 细胞周期蛋白依赖性激酶7(cdk7)的降解剂及其用途
CA3156610A1 (en) * 2019-10-29 2021-05-06 J. Graeme HODGSON Methods of treating cancer in biomarker-identified patients with inhibitors of cyclin-dependent kinase 7 (cdk7)
CA3166135A1 (en) * 2019-12-24 2021-07-01 Dana-Farber Cancer Institute, Inc. The combination of cyclin dependent kinase 7 inhibitor and immunotherapy for treatment of cancer
WO2021138391A1 (en) 2019-12-30 2021-07-08 Tyra Biosciences, Inc. Indazole compounds
CN116194103A (zh) * 2020-09-25 2023-05-30 詹森药业有限公司 细胞周期蛋白依赖性激酶7(cdk7)非共价抑制剂
WO2023109876A1 (en) * 2021-12-16 2023-06-22 Edigene Therapeutics (Beijing) Inc. Biomarkers for colorectal cancer treatment
WO2023227125A1 (zh) * 2022-05-26 2023-11-30 杭州德睿智药科技有限公司 作为CDKs抑制剂的新型并杂环类新化合物及其应用
KR20250091232A (ko) * 2022-10-25 2025-06-20 투오지에 바이오텍 (상하이) 컴퍼니 리미티드 피페리디노피리미딘계 유도체, 이의 제조 방법 및 이의 의학적 응용

Family Cites Families (333)

* 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
US4941880A (en) 1987-06-19 1990-07-17 Bioject, Inc. Pre-filled ampule and non-invasive hypodermic injection device assembly
US4940460A (en) 1987-06-19 1990-07-10 Bioject, Inc. Patient-fillable 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
EP0604181A1 (en) 1992-12-21 1994-06-29 Eli Lilly And Company Antitumor compositions and method 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
JPH09500615A (ja) 1993-05-14 1997-01-21 ジェネンテク,インコーポレイテッド Ras−ファルネシル転移酵素阻害剤
US5602098A (en) 1993-05-18 1997-02-11 University Of Pittsburgh Inhibition of farnesyltransferase
WO1995008542A1 (en) 1993-09-22 1995-03-30 Kyowa Hakko Kogyo Co., Ltd. Farnesyltransferase inhibitor
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
HUT76066A (en) 1993-10-15 1997-06-30 Schering Corp Tricyclic amide and urea compounds useful for inhibition of g-protein function and for treatment of proliferative diseases, pharmaceutical compositions containing them and process for producing them
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
DE69429440T2 (de) 1993-10-15 2002-08-08 Schering Corp., Kenilworth Tricyclische sulfonamide-derivate zur inhibierung der g-protein funktion und fur die bekandlung von proliferativen erkrantungen
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
CA2173590A1 (en) 1993-10-25 1995-05-04 Gary Louis Bolton Substituted tetra- and pentapeptide inhibitors of protein:farnesyl transferase
US5783593A (en) 1993-11-04 1998-07-21 Abbott Laboratories Inhibitors of squalene synthetase and protein farnesyltransferase
JPH08505646A (ja) 1993-11-04 1996-06-18 アボツト・ラボラトリーズ スクアレンシンテターゼ及びプロテインファルネシルトランスフェラーゼのインヒビターとしてのシクロブタン誘導体
JP3597863B2 (ja) 1993-11-05 2004-12-08 ワーナー−ランバート・コンパニー タンパク質:ファルネシルトランスフェラーゼの置換されたジ‐およびトリペプチド阻害剤
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
CA2185441A1 (en) 1994-03-15 1995-09-21 Michael D. Lewis Isoprenyl transferase inhibitors
US6312699B1 (en) 1994-03-28 2001-11-06 Uab Research Foundation Ligands added to adenovirus fiber
HUT72440A (en) 1994-03-31 1996-04-29 Bristol Myers Squibb Co Imidazole-containing inhibitors of farnesyl protein transferase and pharmaceutical compositions containing them
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
EP0764149B1 (fr) 1994-06-10 1999-01-20 Aventis Pharma S.A. Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
US5571792A (en) 1994-06-30 1996-11-05 Warner-Lambert Company Histidine and homohistidine derivatives as inhibitors of protein farnesyltransferase
EP0776884B1 (en) 1994-08-11 2000-01-05 Banyu Pharmaceutical Co., Ltd. Substituted amide derivative
CA2155448A1 (en) 1994-08-11 1996-02-12 Katerina Leftheris Inhibitors of farnesyl protein transferase
EP0805154A1 (en) 1994-08-12 1997-11-05 Banyu Pharmaceutical Co., Ltd. N,n-disubstituted amic acid derivative
WO1996017861A1 (en) 1994-12-09 1996-06-13 Warner-Lambert Company Substituted tetra- and pentapeptide inhibitors of protein:farnesyl transferase
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
CA2207252C (en) 1995-01-12 2014-02-25 University Of Pittsburgh Inhibitors of prenyl transferases
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
WO1996031501A1 (en) 1995-04-07 1996-10-10 Schering Corporation Carbonyl-piperazinyl and piperidinil compounds which inhibit farnesyl protein transferase
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
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
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
WO1997000252A1 (en) 1995-06-16 1997-01-03 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.
US7091346B1 (en) 1995-11-01 2006-08-15 Novartis Ag Purine derivatives and processes for their preparation
CA2235986C (en) 1995-11-06 2006-09-12 University Of Pittsburgh Inhibitors of protein isoprenyl transferases
EP0862435A4 (en) 1995-11-22 1999-02-03 Merck & Co Inc Inhibitors of farnesyl-protein transferase
BR9610745A (pt) 1995-12-08 1999-07-13 Janssen Pharmaceutica Nv Derivados de (imidazol-5-il) metil-2-quinolinona inibindo a transferase da proteina farnesil
DE69635424T2 (de) 1995-12-22 2006-08-03 Schering Corp. Zur hemming der g-protein-funktion und zur behandlung proliferativer krankheiten geeignete tricyclische amide
US5893397A (en) 1996-01-12 1999-04-13 Bioject Inc. Medication vial/syringe liquid-transfer apparatus
AU1529997A (en) 1996-01-16 1997-08-11 Warner-Lambert Company Substituted 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
WO1997038665A2 (en) 1996-04-03 1997-10-23 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
IL126833A0 (en) 1996-05-22 1999-08-17 Warner Lambert Co Inhibitors of protein farnesyl transferase
JP2000514456A (ja) 1996-07-15 2000-10-31 ブリストル―マイヤーズ・スクイブ・カンパニー ファルネシルプロテイントランスフェラーゼのチアジオキソベンゾジアゼピン阻害剤
US5866702A (en) 1996-08-02 1999-02-02 Cv Therapeutics, Incorporation Purine inhibitors of cyclin dependent kinase 2
JP2002511054A (ja) 1996-12-30 2002-04-09 メルク エンド カンパニー インコーポレーテッド ファルネシル蛋白トランスフェラーゼ阻害薬
AU5719598A (en) 1996-12-30 1998-07-31 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5993412A (en) 1997-05-19 1999-11-30 Bioject, Inc. Injection apparatus
US6262096B1 (en) 1997-11-12 2001-07-17 Bristol-Myers Squibb Company Aminothiazole inhibitors of cyclin dependent kinases
US6040321A (en) 1997-11-12 2000-03-21 Bristol-Myers Squibb Company Aminothiazole inhibitors of cyclin dependent kinases
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
AU3475100A (en) 1999-01-29 2000-08-18 Imclone Systems Incorporated Antibodies specific to kdr and uses thereof
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
WO2000061186A1 (en) 1999-04-08 2000-10-19 Arch Development Corporation Use of anti-vegf antibody to enhance radiation in cancer therapy
AU6605200A (en) 1999-06-30 2001-01-31 Merck & Co., Inc. Src kinase inhibitor compounds
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
ES2250186T3 (es) 1999-09-10 2006-04-16 MERCK & CO., INC. Inhibidores de tirosina quinasa.
US6921763B2 (en) 1999-09-17 2005-07-26 Abbott Laboratories Pyrazolopyrimidines as therapeutic agents
IL148718A0 (en) 1999-09-17 2002-09-12 Abbott Gmbh & Co Kg Pyrazolopyrimidines as therapeutic agents
MY125768A (en) 1999-12-15 2006-08-30 Bristol Myers Squibb Co N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases
TWI284639B (en) 2000-01-24 2007-08-01 Shionogi & Co A compound having thrombopoietin receptor agonistic effect
CA2416527C (en) * 2000-08-10 2009-12-22 Pharmacia Italia S.P.A. Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
WO2002042303A2 (en) 2000-10-31 2002-05-30 Aventis Pharmaceuticals 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
EP1345926B1 (en) 2000-12-21 2006-05-17 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
PT1347971E (pt) 2000-12-21 2006-06-30 Bristol Myers Squibb Co Inibidores tiazolilicos de tirosina-cinases da familia tec
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
WO2002080952A2 (en) 2001-04-09 2002-10-17 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
JP2002338537A (ja) 2001-05-16 2002-11-27 Mitsubishi Pharma Corp アミド化合物およびその医薬用途
FR2825278A1 (fr) 2001-05-30 2002-12-06 Sod Conseils Rech Applic Produit comprenant du mikanolide, du dihydromikanolide ou un analogue de ceux-ci en association avec un autre agent anti-cancereux pour une utilisation therapeutique dans le traitement du cancer
DE60214703T2 (de) 2001-06-01 2007-09-13 Vertex Pharmaceuticals Inc., Cambridge Thiazolverbindungen, die sich als inhibitoren von proteinkinasen eignen
MXPA03011652A (es) 2001-06-15 2004-05-31 Vertex Pharma 5-(2-aminopirimidin-4-il) benzioxazoles como inhibidores de proteinas cinasa.
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
AU2002353186A1 (en) 2001-12-19 2003-06-30 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
AU2003231231A1 (en) 2002-05-06 2003-11-11 Bayer Pharmaceuticals Corporation Pyridinyl amino pyrimidine derivatives useful for treating hyper-proliferative disorders
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
US7041692B2 (en) 2002-06-19 2006-05-09 Bristol-Myers Squibb Company Methods of treating factor VIIa-associated conditions with compounds having an amine nucleus
TW200401638A (en) 2002-06-20 2004-02-01 Bristol Myers Squibb Co Heterocyclic inhibitors of kinases
JP4570955B2 (ja) 2002-07-09 2010-10-27 バーテクス ファーマスーティカルズ インコーポレイテッド プロテインキナーゼ阻害活性を持つイミダゾール類
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
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
CA2497544C (en) 2002-09-04 2010-11-02 Schering Corporation Pyrazolo[1,5-a]pyrimidines compounds as cyclin dependent kinase inhibitors
CA2497440C (en) 2002-09-04 2011-03-22 Schering Corporation Pyrazolopyrimidines as cyclin-dependent kinase inhibitors
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
US20050250837A1 (en) 2002-10-18 2005-11-10 D Mello Santosh R Use of C-Raf inhibitors for the treatment of neurodegenerative diseases
DE50304983D1 (de) 2002-10-28 2006-10-19 Bayer Healthcare Ag Heteroaryloxy-substituierte phenylaminopyrimidine als rho-kinaseinhibitoren
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
WO2004071440A2 (en) 2003-02-06 2004-08-26 Bristol-Myers Squibb Company Thiazolyl-based compounds useful as kinase inhibitors
EP1597256A1 (en) 2003-02-21 2005-11-23 Pfizer Inc. N-heterocyclyl-substituted amino-thiazole derivatives as protein kinase inhibitors
GB0304665D0 (en) 2003-02-28 2003-04-02 Teijin Ltd Compounds
MXPA05008955A (es) 2003-02-28 2006-02-22 Teijin Pharma Ltd Derivados de pirazolo [1,5-a] pirimidina.
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
EP1608652A1 (en) 2003-03-31 2005-12-28 Vernalis (Cambridge) Limited Pyrazolopyrimidine compounds and their use in medicine
US20050008640A1 (en) 2003-04-23 2005-01-13 Wendy Waegell Method of treating transplant rejection
SI1638941T1 (sl) 2003-05-22 2010-11-30 Abbott Lab Inhibitorji indazol benzizoksazol in benzizotiazol kinaze
SE0301906D0 (sv) 2003-06-26 2003-06-26 Astrazeneca Ab New compounds
GB0315657D0 (en) 2003-07-03 2003-08-13 Astex Technology Ltd Pharmaceutical compounds
EP1651612B9 (en) 2003-07-22 2012-09-05 Astex Therapeutics Limited 3,4-disubstituted 1h-pyrazole compounds and their use as cyclin dependent kinases (cdk) and glycogen synthase kinase-3 (gsk-3) modulators
US7442698B2 (en) 2003-07-24 2008-10-28 Amgen Inc. Substituted heterocyclic compounds and methods of use
CA2533774A1 (en) 2003-07-29 2005-02-10 Irm Llc Compounds and compositions as protein kinase inhibitors
BRPI0413616B8 (pt) 2003-08-15 2021-05-25 Irm Llc 2,4-pirimidinadiaminas, seus usos, e composição farmacêutica
EP1680431A1 (en) 2003-10-17 2006-07-19 Rigel Pharmaceuticals, Inc. Benzothiazole and thiazole'5,5-b!pyridine 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
US7718676B2 (en) 2003-10-23 2010-05-18 Ab Science 2-aminoaryloxazole compounds as tyrosine kinase inhibitors
DE10357510A1 (de) 2003-12-09 2005-07-07 Bayer Healthcare Ag Heteroarylsubstituierte Benzole
BRPI0418031A (pt) 2003-12-22 2007-04-17 Gilead Sciences Inc inibidores de quinase fosfonato-substituìdos
RU2410375C9 (ru) 2003-12-25 2017-08-02 Ниппон Синяку Ко., Лтд. Амидное производное и лекарственное средство
WO2005095418A1 (en) 2004-04-02 2005-10-13 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
US20050228031A1 (en) 2004-04-13 2005-10-13 Bilodeau Mark T Tyrosine kinase inhibitors
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
CA2567662C (en) 2004-06-10 2012-11-27 Irm Llc Compounds and compositions as protein kinase inhibitors
DE102004028862A1 (de) 2004-06-15 2005-12-29 Merck Patent Gmbh 3-Aminoindazole
US20090118261A1 (en) 2004-08-31 2009-05-07 Astrazeneca Ab Quinazolinone derivatives and their use as b-raf inhibitors
US20060100226A1 (en) 2004-09-10 2006-05-11 Sikorski James A 2-Thiopyrimidinones as therapeutic agents
CA2580845A1 (en) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Pyridazine derivatives for inhibiting human stearoyl-coa-desaturase
WO2006038001A1 (en) 2004-10-06 2006-04-13 Celltech R & D Limited Aminopyrimidine derivatives as jnk inhibitors
MX2007004480A (es) 2004-10-15 2007-05-08 Astrazeneca Ab Quinoxalinas como inhibidores b raf.
JP2008517064A (ja) 2004-10-19 2008-05-22 アークル インコーポレイテッド P38mapキナーゼのイミダゾオキサゾールおよびイミダゾチアゾール阻害剤の合成
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
EP1841760B1 (en) 2004-12-30 2011-08-10 Exelixis, Inc. Pyrimidine derivatives as kinase modulators and method of use
ES2365245T3 (es) 2005-01-10 2011-09-27 Pfizer, Inc. Pirrolopirazoles, potentes inhibidores de quinasas.
AR053662A1 (es) 2005-01-21 2007-05-16 Astex Therapeutics Ltd Compuestos de pirazol inhibidores de la actividad quinasa cdk y gsk
CA2593803A1 (en) 2005-01-26 2006-08-03 Irm Llc Thiazole-amide compounds and compsitions as protein kinase inhibitors
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
DE102005008310A1 (de) 2005-02-17 2006-08-24 Schering Ag Verwendung von CDKII Inhibitoren zur Fertilitätskontrolle
NZ561000A (en) 2005-02-28 2010-01-29 Japan Tobacco Inc Novel aminopyridine compound with Syk inhibitory activity
FR2884516B1 (fr) 2005-04-15 2007-06-22 Cerep Sa Antagonistes npy, preparation et utilisations
WO2006124731A2 (en) 2005-05-12 2006-11-23 Irm Llc Compounds and compositions as protein kinase inhibitors
WO2006124863A2 (en) 2005-05-16 2006-11-23 Irm Llc Pyrrolopyridine derivatives as protein kinase inhibitors
BRPI0611863B1 (pt) 2005-06-22 2021-11-23 Plexxikon, Inc Composto, bem como composição e kit compreendendo o mesmo, composto intermediário na preparação do mesmo, método para tratamento e uso do mesmo
WO2007024680A1 (en) 2005-08-22 2007-03-01 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
CA2623958C (en) 2005-09-30 2013-05-28 Banyu Pharmaceutical Co., Ltd. 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
WO2007056023A2 (en) 2005-11-02 2007-05-18 Targegen, Inc. Thiazole inhibitors targeting resistant kinase mutations
BRPI0620354A2 (pt) 2005-12-21 2011-11-08 Pfizer Prod Inc compostos pirrolopirazóis de carbonilamino e composição farmaceutica que os contém
HUE047422T2 (hu) 2005-12-23 2020-04-28 Ariad Pharma Inc Biciklusos heteroaril vegyületek
US20070155746A1 (en) 2005-12-23 2007-07-05 Kalypsys, Inc. Novel substituted pyridinyloxy and pyrimidinyloxy amides useful as inhibitors of protein kinases
WO2007076161A2 (en) 2005-12-27 2007-07-05 Myriad Genetics, Inc Compounds with therapeutic activity
WO2007086584A1 (ja) 2006-01-30 2007-08-02 Meiji Seika Kaisha, Ltd. 新規FabKおよびFabI/K阻害剤
WO2007129195A2 (en) 2006-05-04 2007-11-15 Pfizer Products Inc. 4-pyrimidine-5-amino-pyrazole compounds
PE20080071A1 (es) 2006-05-22 2008-02-11 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
WO2008009954A1 (en) 2006-07-21 2008-01-24 Astex Therapeutics Limited Medical use of cyclin dependent kinases inhibitors
CA2662677C (en) 2006-09-05 2016-05-31 Emory University Kinase inhibitors for preventing or treating pathogen infection and method of use thereof
NZ601278A (en) 2006-09-22 2013-09-27 Pharmacyclics Inc Inhibitors of Bruton's tyrosine kinase
JP5415271B2 (ja) 2006-10-11 2014-02-12 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ キナーゼ阻害剤としての置換ピロロ−ピラゾール誘導体
WO2008049856A2 (en) 2006-10-25 2008-05-02 Ingenium Pharmaceuticals Gmbh Methods of treating pain using cdk inhibitors
WO2008054827A2 (en) 2006-11-03 2008-05-08 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
EP2102194A1 (en) 2006-12-08 2009-09-23 F. Hoffmann-Roche AG Substituted pyrimidines and their use as jnk modulators
WO2008079873A2 (en) 2006-12-20 2008-07-03 Bristol-Myers Squibb Company Thiazolyl compounds useful as kinase inhibitors
CA2673095C (en) 2006-12-20 2016-03-15 Nerviano Medical Sciences S.R.L. Indazole derivatives as kinase inhibitors for the treatment of cancer
RU2009122670A (ru) 2006-12-21 2011-01-27 Плекссикон, Инк. (Us) Соединения и способы для модуляции киназ и показания к их применению
AU2008212625B2 (en) 2007-02-07 2012-07-19 Pfizer Inc. 3-amino-pyrrolo[3,4-c] pyrazole- 5 (1H, 4H, 6H) carbaldehyde derivatives as PKC inhibitors
JP5577104B2 (ja) 2007-03-14 2014-08-20 エクセリクシス パテント カンパニー エルエルシー ヘッジホッグ経路の阻害剤
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
WO2008151183A1 (en) 2007-06-04 2008-12-11 Avila Therapeutics, Inc. Heterocyclic compounds and uses thereof
JP2010529140A (ja) 2007-06-05 2010-08-26 エモリー・ユニバーシテイ サイクリン依存性キナーゼの選択的阻害剤
WO2008154563A1 (en) 2007-06-11 2008-12-18 Bristol-Myers Squibb Company 1, 3 - dihydroxy substituted phenylamide glucokinase activators
ES2401557T3 (es) 2007-08-02 2013-04-22 Amgen, Inc Moduladores de Pl3 cinasas y métodos de uso
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
TW200922564A (en) 2007-09-10 2009-06-01 Curis Inc CDK inhibitors containing a zinc binding moiety
KR100923540B1 (ko) 2007-11-23 2009-10-27 한국과학기술연구원 5-아실하이드라진카르보닐-3,4-디치환 피라졸 유도체 및이의 제조방법
AU2009227013B2 (en) 2008-03-21 2013-01-10 Novartis Ag Novel heterocyclic compounds and uses therof
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
JP2011524864A (ja) 2008-05-30 2011-09-08 メルク・シャープ・エンド・ドーム・コーポレイション 新規な置換されたアザベンゾオキサゾール
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
US20110212053A1 (en) 2008-06-19 2011-09-01 Dapeng Qian Phosphatidylinositol 3 kinase inhibitors
US20110178070A1 (en) 2008-06-24 2011-07-21 Takeda Pharmaceutical Company Limited PI3K/mTOR INHIBITORS
GB0812031D0 (en) 2008-07-01 2008-08-06 7Tm Pharma As Thiazole derivatives
TWI450898B (zh) 2008-07-04 2014-09-01 Sigma Tau Res Switzerland Sa 具有抗腫瘤活性之芳基異唑化合物
EP2303881A2 (en) 2008-07-14 2011-04-06 Gilead Sciences, Inc. Fused heterocyclyc inhibitors of histone deacetylase and/or cyclin-dependent kinases
CA2732520A1 (en) 2008-08-05 2010-02-11 Merck Sharp & Dohme Corp. 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
JP2012511021A (ja) 2008-12-05 2012-05-17 アークル インコーポレイテッド Rafの阻害剤およびその使用
WO2010075542A1 (en) 2008-12-23 2010-07-01 Curis, Inc. Cdk inhibitors
CN102317282A (zh) 2009-02-12 2012-01-11 安斯泰来制药有限公司 杂环衍生物
WO2010125799A1 (ja) 2009-04-27 2010-11-04 塩野義製薬株式会社 Pi3k阻害活性を有するウレア誘導体
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
US20120178758A1 (en) 2009-06-09 2012-07-12 California Capital Equity, Llc Styryl-triazine derivatives and their therapeutical applications
WO2010144909A1 (en) 2009-06-12 2010-12-16 Novartis Ag Fused heterocyclic compounds and their uses
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
WO2011079231A1 (en) 2009-12-23 2011-06-30 Gatekeeper Pharmaceutical, Inc. Compounds that modulate egfr activity and methods for treating or preventing conditions therewith
WO2011090738A2 (en) 2009-12-29 2011-07-28 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
MX2012010617A (es) 2010-03-16 2012-10-05 Dana Farber Cancer Inst Inc Compuestos de imidazol y sus usos.
MX384074B (es) 2010-05-14 2025-03-12 Dana Farber Cancer Inst Inc Composiciones y métodos para tratar neoplasias, enfermedades inflamatorias y otros trastornos.
UY33539A (es) 2010-08-02 2012-02-29 Astrazeneca Ab Compuestos químicos alk
CN102406644A (zh) 2010-09-20 2012-04-11 北大方正集团有限公司 芳基脲衍生物用于制备治疗移植排斥药物的新用途
CN102408408A (zh) 2010-09-20 2012-04-11 北大方正集团有限公司 具有抗肿瘤作用的芳基脲衍生物
CN102406646B (zh) 2010-09-20 2015-09-09 北大方正集团有限公司 芳基脲衍生物用于制备治疗移植排斥药物的用途
CN103313987A (zh) 2010-11-19 2013-09-18 弗·哈夫曼-拉罗切有限公司 吡唑并吡啶化合物、吡唑并吡啶化合物以及它们作为tyk2抑制剂的用途
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
KR20140047092A (ko) 2011-07-28 2014-04-21 셀좀 리미티드 Jak 억제제로서의 헤테로시클릴 피리미딘 유사체
WO2013040436A2 (en) 2011-09-16 2013-03-21 The Regents Of The University Of Michgian Esx-mediated transcription modulators and related methods
BR112014006840A2 (pt) 2011-09-22 2017-04-04 Pfizer derivados de pirrolopirimidina e purina
SI2760860T1 (sl) 2011-09-28 2017-04-26 Euro-Celtique S.A. Derivati dušikove gorčice
AU2012340200B2 (en) 2011-11-17 2017-10-12 Dana-Farber Cancer Institute, Inc. Inhibitors of c-Jun-N-Terminal Kinase (JNK)
WO2013106792A1 (en) 2012-01-13 2013-07-18 Acea Biosciences Inc. Heterocyclic compounds and uses as anticancer agents.
GB201204384D0 (en) 2012-03-13 2012-04-25 Univ Dundee Anti-flammatory agents
US9879003B2 (en) 2012-04-11 2018-01-30 Dana-Farber Cancer Institute, Inc. Host targeted inhibitors of dengue virus and other viruses
ES2776365T3 (es) 2012-07-09 2020-07-30 Novartis Ag Biomarcadores asociados con inhibidores de CDK
WO2014015523A1 (en) 2012-07-27 2014-01-30 Hutchison Medipharma Limited Novel heteroaryl and heterocycle compounds, compositions and methods
WO2014063068A1 (en) 2012-10-18 2014-04-24 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
WO2014063054A1 (en) 2012-10-19 2014-04-24 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
WO2014063061A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
ES2664985T3 (es) 2012-12-21 2018-04-24 Plexxikon Inc. Compuestos y métodos para modulación de quinasa, e indicaciones de los mismos
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
TW201444821A (zh) 2013-03-13 2014-12-01 Janssen Pharmaceutica Nv 經取代之哌啶化合物及其作為食慾素受體調節劑之用途
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
JP2016519674A (ja) 2013-03-20 2016-07-07 バイエル・ファルマ・アクティエンゲゼルシャフト 過剰増殖障害を治療または予防するための3−アセチルアミノ−1−(フェニル−ヘテロアリール−アミノカルボニルまたはフェニル−ヘテロアリール−カルボニルアミノ)ベンゼン誘導体
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)
CN103242341B (zh) 2013-04-19 2015-12-09 中国科学院广州生物医药与健康研究院 噻吩并2,4取代嘧啶类化合物及其药物组合物与应用
CN104177363B (zh) 2013-05-24 2018-06-05 江苏先声药业有限公司 双环杂环胺类Hedgehog信号通路抑制剂
CN105916851A (zh) 2013-07-11 2016-08-31 艾森生物科学公司 嘧啶衍生物作为激酶抑制剂
CA2918910A1 (en) 2013-07-25 2015-01-29 Dana-Farber Cancer Institute, Inc. Inhibitors of transcription factors and uses thereof
US10273224B2 (en) 2013-08-22 2019-04-30 Jubilant Biosys Limited Substituted pyrimidine compounds, compositions and medicinal applications thereof
EP3057954A2 (en) 2013-10-18 2016-08-24 Syros Pharmaceuticals, Inc. Heteromaromatic compounds useful for the treatment of proliferative diseases
EP3057955B1 (en) 2013-10-18 2018-04-11 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of prolferative diseases
CA2927920A1 (en) 2013-10-18 2015-04-23 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7)
USRE50030E1 (en) 2013-12-13 2024-07-02 Dana-Farber Cancer Institute, Inc. Methods to treat lymphoplasmacytic lymphoma
EP3099693A4 (en) 2014-01-31 2017-08-16 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
WO2015117083A1 (en) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Diazepane derivatives and uses thereof
US10150756B2 (en) 2014-01-31 2018-12-11 Dana-Farber Cancer Institute, Inc. Diaminopyrimidine benzenesulfone derivatives and uses thereof
CN104860941B (zh) 2014-02-25 2017-03-22 上海海雁医药科技有限公司 2,4‑二取代苯‑1,5‑二胺衍生物及其应用以及由其制备的药物组合物和药用组合物
EP3489232A3 (en) 2014-04-04 2019-07-31 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
EP3129371B1 (en) 2014-04-05 2020-07-29 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
WO2015164614A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
WO2015164604A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged 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
AU2015292827B2 (en) 2014-07-21 2019-11-14 Dana-Farber Cancer Institute, Inc. Macrocyclic kinase inhibitors and uses thereof
CA2954186A1 (en) 2014-07-21 2016-01-28 Dana-Farber Cancer Institute, Inc. Imidazolyl kinase inhibitors and uses thereof
WO2016014904A1 (en) 2014-07-24 2016-01-28 Beta Pharma, Inc. 2-h-indazole derivatives as cyclin-dependent kinase (cdk) inhibitors and therapeutic uses thereof
WO2016058544A1 (en) 2014-10-16 2016-04-21 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
EP3214086B1 (en) 2014-10-31 2021-09-22 Ube Industries, Ltd. Substituted dihydropyrrolopyrazole compound
AU2015371251B2 (en) 2014-12-23 2020-06-11 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
ES2886577T3 (es) 2015-02-05 2021-12-20 Merck Patent Gmbh Compuestos macrólidos como inhibidores de irak1/4 y sus usos
WO2016142855A2 (en) 2015-03-09 2016-09-15 Aurigene Discovery Technologies Limited Pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives as cdk inhibitors
US10550121B2 (en) 2015-03-27 2020-02-04 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
HRP20240101T1 (hr) 2015-06-04 2024-03-29 Aurigene Oncology Limited Supstituirani heterociklil derivati kao cdk inhibitori
CA2986441A1 (en) 2015-06-12 2016-12-15 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
JP2018522867A (ja) 2015-06-26 2018-08-16 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 縮合二環式ピリミジン誘導体およびこれらの使用
WO2016210296A1 (en) 2015-06-26 2016-12-29 Dana-Farber Cancer Institute, Inc. 4,6-pyrimidinylene derivatives and uses thereof
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
WO2017044858A2 (en) 2015-09-09 2017-03-16 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
US20190077856A1 (en) 2016-03-15 2019-03-14 Memorial Sloan Kettering Cancer Center Method of treating diseases using kinase modulators
AU2017363307B2 (en) 2016-11-22 2021-07-29 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 12 (CDK12) and uses thereof
CA3043222A1 (en) 2016-11-28 2018-05-31 Dana-Farber Cancer Institute, Inc. Reagents and methods for analysis of proteins and metabolites targeted by covalent probes
CN107235906B (zh) 2017-06-28 2020-05-01 郑州大学第一附属医院 一组吡唑酰胺类衍生物及其应用
CN107686477B (zh) 2017-09-30 2020-01-31 武汉九州钰民医药科技有限公司 作为cdk4/6抑制剂的新型化合物及其应用
CA3099763A1 (en) 2018-06-25 2020-01-02 Dana-Farber Cancer Institute, Inc. Taire family kinase inhibitors and uses thereof
WO2020100944A1 (ja) 2018-11-14 2020-05-22 宇部興産株式会社 ジヒドロピロロピラゾール誘導体
JP7642540B2 (ja) 2018-12-14 2025-03-10 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 C-jun-n末キナーゼのピラゾロピリジンインヒビターおよびそれらの使用
CA3124422A1 (en) 2018-12-28 2020-07-02 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 and uses thereof
EP3965803B1 (en) 2019-05-10 2025-08-20 Dana-Farber Cancer Institute, Inc. Small-molecule focal adhesion kinase (fak) inhibitors
JP7680999B2 (ja) 2019-07-23 2025-05-21 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
CN114174281B (zh) 2019-08-05 2025-02-07 达纳-法伯癌症研究公司 细胞周期蛋白依赖性激酶7(cdk7)的降解剂及其用途
CA3166135A1 (en) 2019-12-24 2021-07-01 Dana-Farber Cancer Institute, Inc. The combination of cyclin dependent kinase 7 inhibitor and immunotherapy for treatment of cancer

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