CA2927920A1 - Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7) - Google Patents

Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7) Download PDF

Info

Publication number
CA2927920A1
CA2927920A1 CA2927920A CA2927920A CA2927920A1 CA 2927920 A1 CA2927920 A1 CA 2927920A1 CA 2927920 A CA2927920 A CA 2927920A CA 2927920 A CA2927920 A CA 2927920A CA 2927920 A1 CA2927920 A1 CA 2927920A1
Authority
CA
Canada
Prior art keywords
optionally substituted
certain embodiments
compound
alkyl
unsubstituted
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Abandoned
Application number
CA2927920A
Other languages
English (en)
French (fr)
Inventor
Nathanael Gray
Tinghu Zhang
Stephane Ciblat
Melissa Leblanc
Jason J. Marineau
Joel Moore
Kevin Sprott
M. Arshad Siddiqui
Anzhelika KABRO
Tom Miller
Stephanie ROY
Darby Schmidt
Dana K. WINTER
Michael Bradley
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Dana Farber Cancer Institute Inc
Original Assignee
Dana Farber Cancer Institute Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Dana Farber Cancer Institute Inc filed Critical Dana Farber Cancer Institute Inc
Publication of CA2927920A1 publication Critical patent/CA2927920A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/0803Compounds with Si-C or Si-Si linkages
    • C07F7/081Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
    • C07F7/0812Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CA2927920A 2013-10-18 2014-10-17 Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7) Abandoned CA2927920A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361893005P 2013-10-18 2013-10-18
US61/893,005 2013-10-18
PCT/US2014/061232 WO2015058140A1 (en) 2013-10-18 2014-10-17 Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7)

Publications (1)

Publication Number Publication Date
CA2927920A1 true CA2927920A1 (en) 2015-04-23

Family

ID=51904230

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2927920A Abandoned CA2927920A1 (en) 2013-10-18 2014-10-17 Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7)

Country Status (7)

Country Link
US (2) US10047070B2 (enExample)
EP (1) EP3057956B1 (enExample)
JP (1) JP6491202B2 (enExample)
CN (1) CN105849099B (enExample)
AU (2) AU2014337044A1 (enExample)
CA (1) CA2927920A1 (enExample)
WO (1) WO2015058140A1 (enExample)

Families Citing this family (63)

* 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
US9382239B2 (en) 2011-11-17 2016-07-05 Dana-Farber Cancer Institute, Inc. Inhibitors of c-Jun-N-terminal kinase (JNK)
US10112927B2 (en) 2012-10-18 2018-10-30 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
US10000483B2 (en) 2012-10-19 2018-06-19 Dana-Farber Cancer Institute, Inc. Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
US9758522B2 (en) 2012-10-19 2017-09-12 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
CN105849099B (zh) 2013-10-18 2020-01-17 达纳-法伯癌症研究所股份有限公司 周期蛋白依赖性激酶7(cdk7)的多环抑制剂
EP3057955B1 (en) 2013-10-18 2018-04-11 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of prolferative diseases
CN110229142A (zh) 2014-04-04 2019-09-13 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
US10017477B2 (en) 2014-04-23 2018-07-10 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
US9862688B2 (en) 2014-04-23 2018-01-09 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged janus kinase inhibitors and uses thereof
US10308648B2 (en) * 2014-10-16 2019-06-04 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
WO2016105528A2 (en) 2014-12-23 2016-06-30 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
CA2978518C (en) 2015-03-27 2023-11-21 Nathanael S. Gray Inhibitors of cyclin-dependent kinases
JP6469518B2 (ja) * 2015-05-14 2019-02-13 丸善製薬株式会社 血管新生促進剤
WO2016201370A1 (en) 2015-06-12 2016-12-15 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
US10273252B2 (en) 2015-06-15 2019-04-30 Ube Industries, Ltd. Substituted dihydropyrrolopyrazole derivative
WO2016210291A1 (en) * 2015-06-26 2016-12-29 Dana-Farber Cancer Institute, Inc. Fused bicyclic pyrimidine derivatives and uses thereof
EP3313530B1 (en) 2015-06-26 2022-10-05 Dana Farber Cancer Institute, Inc. 4,6-pyrimidinylene derivatives and uses thereof
PT3331877T (pt) * 2015-08-04 2021-12-27 Yissum Res Dev Co Of Hebrew Univ Jerusalem Ltd Derivado de pirimidina pirazol e usos do mesmo
WO2017044858A2 (en) 2015-09-09 2017-03-16 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
JOP20190024A1 (ar) 2016-08-26 2019-02-19 Gilead Sciences Inc مركبات بيروليزين بها استبدال واستخداماتها
SI3512833T1 (sl) 2016-09-15 2020-11-30 Boehringer Ingelheim International Gmbh Heteroarilne karboksamidne spojine kot inhibitorji RIPK2
US11306070B2 (en) 2016-11-22 2022-04-19 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 12 (CDK12) and uses thereof
EP3362471B1 (en) * 2016-12-19 2021-11-17 Sumitomo Dainippon Pharma Oncology, Inc. Profiling peptides and methods for sensitivity profiling
WO2018119395A1 (en) * 2016-12-23 2018-06-28 Aquinnah Pharmaceuticals, Inc. Compouns, compositions and methods of use
CN108276382B (zh) * 2017-01-06 2022-10-18 南京圣和药物研发有限公司 细胞周期蛋白依赖性激酶抑制剂及其应用
CN110475771B (zh) 2017-02-01 2022-09-02 耶路撒冷希伯来大学伊森姆研究发展有限公司 Ck1和/或irak1抑制剂、药物组合物和用于癌症治疗的治疗应用
EP3630079A4 (en) 2017-05-31 2021-02-24 The Children's Medical Center Corporation TARGETING LYSINE DEMETHYLASE (KDMS) AS A THERAPEUTIC STRATEGY FOR DIFFUSED LARGE B-CELL LYMPHOMA
US10913983B2 (en) 2017-07-18 2021-02-09 University Of South Carolina Sensitivity markers and uses for CDK7 inhibitors in breast cancers
ES2962605T3 (es) 2018-02-26 2024-03-20 Gilead Sciences Inc Compuestos de pirrolizina sustituidos como inhibidores de la replicación del VHB
BR112020019595A2 (pt) * 2018-03-29 2021-01-05 Takeda Pharmaceutical Company Limited Composto, e, medicamento.
CN110590747B (zh) * 2018-06-12 2022-03-22 隆泰申医药科技(南京)有限公司 一种化合物、其制备方法、药物组合物和应用
CN112367991A (zh) 2018-06-25 2021-02-12 达纳-法伯癌症研究所股份有限公司 Taire家族激酶抑制剂及其用途
BR112021004999A2 (pt) 2018-09-17 2021-06-08 Yungjin Pharm. Co., Ltd. composto e método de inibição de cdk7 em um sujeito
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
US20210401859A1 (en) 2018-11-01 2021-12-30 Syros Pharmaceuticals, Inc. Methods of treating cancer in biomarker-identified patients with non-covalent inhibitors of cyclin-dependent kinase 7 (cdk7)
US12304913B2 (en) 2018-11-14 2025-05-20 Ube Industries, Ltd. Dihydropyrrolopyrazole derivative
US11034669B2 (en) 2018-11-30 2021-06-15 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
CN113164477A (zh) * 2018-12-14 2021-07-23 达纳-法伯癌症研究所股份有限公司 C-jun-n-末端激酶的吡唑并吡啶抑制剂及其用途
WO2020140098A1 (en) 2018-12-28 2020-07-02 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 and uses thereof
WO2020168197A1 (en) 2019-02-15 2020-08-20 Incyte Corporation Pyrrolo[2,3-d]pyrimidinone compounds as cdk2 inhibitors
WO2020180959A1 (en) 2019-03-05 2020-09-10 Incyte Corporation Pyrazolyl pyrimidinylamine compounds as cdk2 inhibitors
WO2020205560A1 (en) 2019-03-29 2020-10-08 Incyte Corporation Sulfonylamide compounds as cdk2 inhibitors
WO2020223558A1 (en) 2019-05-01 2020-11-05 Incyte Corporation Tricyclic amine compounds as cdk2 inhibitors
WO2020223469A1 (en) 2019-05-01 2020-11-05 Incyte Corporation N-(1-(methylsulfonyl)piperidin-4-yl)-4,5-di hydro-1h-imidazo[4,5-h]quinazolin-8-amine derivatives and related compounds as cyclin-dependent kinase 2 (cdk2) inhibitors for treating cancer
CN114127058B (zh) * 2019-07-04 2024-06-25 深圳国顺康医药科技有限公司 一种杂环化合物、其药物组合物及用途
TW202115024A (zh) 2019-08-14 2021-04-16 美商英塞特公司 作為cdk2 抑制劑之咪唑基嘧啶基胺化合物
PE20221905A1 (es) 2019-10-11 2022-12-23 Incyte Corp Aminas biciclicas como inhibidoras de la cdk2
US20230095043A1 (en) * 2020-01-10 2023-03-30 Hangzhou Innogate Pharma Co., Ltd. Polycyclic compound acting as kinase inhibitor
WO2021182914A1 (ko) 2020-03-13 2021-09-16 영진약품 주식회사 신규한 cdk7 억제 화합물 및 이의 약제학적으로 허용가능한 염
US20230095520A1 (en) 2020-03-13 2023-03-30 Yungjin Pharm. Co., Ltd. Pharmaceutical composition for preventing or treating cancer comprising azole derivatives or pharmaceutically acceptable salt thereof
CN112661745A (zh) * 2020-07-24 2021-04-16 浙江同源康医药股份有限公司 用作cdk7激酶抑制剂的化合物及其应用
CN114133394B (zh) * 2020-08-12 2023-12-08 赛诺哈勃药业(成都)有限公司 一种选择性针对细胞周期依赖性激酶12活性的化合物、制备方法及医药用途
EP4313053A4 (en) * 2021-03-24 2025-03-05 Yissum Research Development Company of the Hebrew University of Jerusalem, Ltd. Pyrazolylpyrimidines for treating malignant solid tumor
US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
WO2023078451A1 (zh) * 2021-11-05 2023-05-11 浙江同源康医药股份有限公司 用作cdk7激酶抑制剂的化合物及其应用
US12084453B2 (en) 2021-12-10 2024-09-10 Incyte Corporation Bicyclic amines as CDK12 inhibitors
US11976073B2 (en) 2021-12-10 2024-05-07 Incyte Corporation Bicyclic amines as CDK2 inhibitors
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
CN117384135A (zh) * 2022-07-04 2024-01-12 浙江同源康医药股份有限公司 用作cdk7激酶抑制剂的化合物及其应用
WO2024066984A1 (zh) * 2022-09-30 2024-04-04 楚浦创制(武汉)医药科技有限公司 三并环类衍生物、药物组合物以及应用
WO2024153053A1 (zh) * 2023-01-17 2024-07-25 石药集团中奇制药技术(石家庄)有限公司 Cdk抑制剂及其可药用盐的晶型以及其用途

Family Cites Families (260)

* 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
WO1984002131A1 (fr) 1982-11-22 1984-06-07 Sandoz Ag Produits analogues de mevalolactone et leurs derives, leurs procedes de production, compositions pharmaceutiques les contenant ainsi que leur utilisation en tant que produits pharmaceutiques
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
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
US4790824A (en) 1987-06-19 1988-12-13 Bioject, Inc. Non-invasive hypodermic injection device
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
EP0763537A3 (en) 1993-05-14 1997-10-22 Genentech Inc Non-peptides farnesyl transfer inhibitors
US5602098A (en) 1993-05-18 1997-02-11 University Of Pittsburgh Inhibition of farnesyltransferase
US5571902A (en) 1993-07-29 1996-11-05 Isis Pharmaceuticals, Inc. Synthesis of oligonucleotides
EP0670314A4 (en) 1993-09-22 1996-04-10 Kyowa Hakko Kogyo Kk FARNESYL TRANSFERASE INHIBITORS.
TW308594B (enExample) 1993-10-15 1997-06-21 Schering Corp
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
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
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
WO1995010514A1 (en) 1993-10-15 1995-04-20 Schering Corporation Tricyclic sulfonamide compounds useful for inhibition of g-protein function and for treatment of proliferative diseases
ATE200677T1 (de) 1993-10-25 2001-05-15 Parke Davis & Co Substituierte tetra- und pentapeptid hemmstoffe der farnesyl protein transferase
ES2130452T3 (es) 1993-11-04 1999-07-01 Abbott Lab Derivados de ciclobutano utilizados como inhibidores de la escualeno-sintetasa y de la farnesiltransferasa proteica.
US5783593A (en) 1993-11-04 1998-07-21 Abbott Laboratories Inhibitors of squalene synthetase and protein farnesyltransferase
WO1995012612A1 (en) 1993-11-05 1995-05-11 Warner-Lambert Company Substituted di- and tripeptide inhibitors of protein: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
FI963597A7 (fi) 1994-03-15 1996-11-14 Eisai Co Ltd Isoprenyylitransferaasi-inhibiittoreita
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
TW365602B (en) 1994-06-10 1999-08-01 Rhone Poulenc Rorer Sa New farnesyl transferase inhibitors, their preparation and the pharmaceutical compositions which contain them
US5571792A (en) 1994-06-30 1996-11-05 Warner-Lambert Company Histidine and homohistidine derivatives as inhibitors of protein farnesyltransferase
WO1996005529A1 (en) 1994-08-09 1996-02-22 Micron Optics, Inc. Temperature compensated fiber fabry-perot filters
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
AU3192495A (en) 1994-08-12 1996-03-07 Banyu Pharmaceutical Co., Ltd. N,n-disubstituted amic acid derivative
DE4429506B4 (de) 1994-08-19 2007-09-13 Degussa Gmbh Verfahren zur Extraktion natürlicher Carotinoid-Farbstoffe
DE4429653C2 (de) 1994-08-20 1997-04-03 Anton Dr More Konverter und Verfahren zum Frischen von Metallschmelzen insbesondere von Roheisen zu Stahl
EP0740853B1 (en) 1994-11-22 1999-01-13 Koninklijke Philips Electronics N.V. Semiconductor device with a carrier body on which a substrate with a semiconductor element is fastened by means of a glue layer and on which a pattern of conductor tracks is fastened
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
BR9606896A (pt) 1995-01-09 1997-10-21 Magla Int Ltd Impressão de imagem resistente á água em superficies de látex
AU4915796A (en) 1995-01-12 1996-07-31 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
ES2194986T3 (es) 1995-04-07 2003-12-01 Schering Corp Compuestos de carbonil-piperazinilo y piperidinilo que inhiben la farnesil-protein-transferasa.
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
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
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
US5730723A (en) 1995-10-10 1998-03-24 Visionary Medical Products Corporation, Inc. Gas pressured needle-less injection device and method
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.
BR9611157A (pt) 1995-11-01 1999-03-30 Novartis Ag Derivados de purina e processos para sua preparação
ZA969273B (en) 1995-11-06 1998-05-05 Univ Pittsburgh Inhibitors of protein isoprenyl transferases.
AU704139B2 (en) 1995-11-22 1999-04-15 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
KR100272676B1 (ko) 1995-12-08 2000-11-15 디르크 반테 파르네실 단백질 트랜스퍼라제 억제 기능을 갖는 (이미다졸-5-일)메틸-2-퀴놀리논 유도체
CA2358394C (en) 1995-12-22 2006-05-02 Schering Corporation 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
WO1997026246A1 (en) 1996-01-16 1997-07-24 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
EP0944388A4 (en) 1996-04-03 2001-08-16 Merck & Co Inc INHIBITORS OF FARNESYL PROTEIN TRANSFERASE
GB9607549D0 (en) 1996-04-11 1996-06-12 Weston Medical Ltd Spring-powered dispensing device
BR9709354A (pt) 1996-05-22 1999-08-10 Warner Lambert Co Inibidores de proteína farnesil 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
EP0951285A1 (en) 1996-12-30 1999-10-27 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
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
US5993412A (en) 1997-05-19 1999-11-30 Bioject, Inc. Injection apparatus
IT1298087B1 (it) 1998-01-08 1999-12-20 Fiderm S R L Dispositivo per il controllo della profondita' di penetrazione di un ago, in particolare applicabile ad una siringa per iniezioni
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
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
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
AU2001287654B2 (en) 2000-08-10 2006-12-14 Pfizer Italia S.R.I. Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
BR0115080A (pt) 2000-10-31 2003-09-23 Aventis Pharma Inc Derivados de acila e sulfonila de 2-(trans-1,4-diaminocicloexil)-purinas 6,9-dissubstituìdas e o uso destes como agentes antiproliferativos
US7429599B2 (en) 2000-12-06 2008-09-30 Signal Pharmaceuticals, Llc Methods for treating or preventing an inflammatory or metabolic condition or inhibiting JNK
CA2432131C (en) 2000-12-21 2008-07-08 Vertex Pharmaceuticals Incorporated 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.
DE60223790T4 (de) 2001-03-29 2009-05-07 Vertex Pharmaceuticals Inc., Cambridge Hemmer von c-jun-terminal kinase (jnk) und andere protein kinase
EP1401469A2 (en) 2001-04-09 2004-03-31 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
ES2274035T3 (es) 2001-06-01 2007-05-16 Vertex Pharmaceuticals Incorporated Compuestos de tiazol utiles como inhibidores de proteina quinasas.
WO2002102800A1 (en) 2001-06-15 2002-12-27 Vertex Pharmaceuticals Incorporated 5-(2-aminopyrimidin-4-yl) benzisoxazoles as protein kinase inhibitors
US6939874B2 (en) 2001-08-22 2005-09-06 Amgen Inc. Substituted pyrimidinyl derivatives and methods of use
US7115617B2 (en) 2001-08-22 2006-10-03 Amgen Inc. Amino-substituted pyrimidinyl derivatives and methods of use
WO2003026666A1 (en) 2001-09-26 2003-04-03 Bayer Pharmaceuticals Corporation 2-phenylamino-4- (5-pyrazolylamino)-pyrimidine derivatives as kinase inhibitors, in particular, as 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
AU2003231231A1 (en) 2002-05-06 2003-11-11 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
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
ATE469903T1 (de) 2002-09-04 2010-06-15 Schering Corp Zur behandlung von krebserkrankungen geeignete pyrazolopyrimidine
US7205308B2 (en) 2002-09-04 2007-04-17 Schering Corporation Trisubstituted 7-aminopyrazolopyrimidines as cyclin dependent kinase inhibitors
US7119200B2 (en) 2002-09-04 2006-10-10 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
JP4790265B2 (ja) 2002-09-04 2011-10-12 シェーリング コーポレイション サイクリン依存性キナーゼインヒビターとしての新規ピラゾロピリミジン
US20050250837A1 (en) 2002-10-18 2005-11-10 D Mello Santosh R Use of C-Raf inhibitors for the treatment of neurodegenerative diseases
WO2004039796A1 (de) 2002-10-28 2004-05-13 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
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
GB0304665D0 (en) 2003-02-28 2003-04-02 Teijin Ltd Compounds
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
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
WO2004087699A2 (en) 2003-03-25 2004-10-14 Vertex Pharmaceuticals Incorporated Thiazoles useful as inhibitors of protein kinases
WO2004087707A1 (en) 2003-03-31 2004-10-14 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
PL1638941T3 (pl) 2003-05-22 2010-11-30 Abbvie Bahamas Ltd Indazolowe, benzizoksazolowe i benzizotiazolowe inhibitory kinaz
SE0301906D0 (sv) 2003-06-26 2003-06-26 Astrazeneca Ab New compounds
WO2005012256A1 (en) 2003-07-22 2005-02-10 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
MXPA06001098A (es) 2003-07-29 2006-04-24 Irm Llc Compuestos y composiciones utiles como inhibidores de proteina cinasa.
PL2287156T3 (pl) 2003-08-15 2013-11-29 Novartis Ag 2,4-Di(fenyloamino)-pirymidyny stosowane w leczeniu chorób nowotworowych, chorób zapalnych i zaburzeń układu immunologicznego
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
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
EP1735322B1 (en) 2004-04-02 2011-09-14 Novartis AG Sulfonamide-thiazolpyridine derivatives as glucokinase activators useful for 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
CA2574418A1 (en) 2004-07-23 2006-02-02 Susan Marie Royalty Peptidase inhibitors
CN101048388A (zh) 2004-08-31 2007-10-03 阿斯利康(瑞典)有限公司 喹唑啉酮衍生物及其作为B-Raf抑制剂的用途
US20060100226A1 (en) 2004-09-10 2006-05-11 Sikorski James A 2-Thiopyrimidinones as therapeutic agents
AR051094A1 (es) 2004-09-20 2006-12-20 Xenon Pharmaceuticals Inc Derivados heterociclicos y su uso como inhibidores de la estearoil-coa desaturasa
CA2583096A1 (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
JP5208516B2 (ja) 2004-12-30 2013-06-12 エグゼリクシス, インコーポレイテッド キナーゼモジュレーターとしてのピリミジン誘導体および使用方法
KR100919905B1 (ko) 2005-01-26 2009-10-06 아이알엠 엘엘씨 단백질 키나제 억제제로서의 화합물 및 조성물
TW200639163A (en) 2005-02-04 2006-11-16 Genentech Inc RAF inhibitor compounds and methods
US20090156582A1 (en) 2005-02-09 2009-06-18 Tetsuya Tsukamoto Pyrazole Compound
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
PT1893612E (pt) 2005-06-22 2011-11-21 Plexxikon Inc Derivados de pirrolo [2,3-b]piridina como inibidores de proteína quinase
AU2006283592A1 (en) 2005-08-22 2007-03-01 Amgen Inc. Pyrazolopyridine and pyrazolopyrimidine compounds useful as kinase enzymes modulators
US7880004B2 (en) 2005-09-15 2011-02-01 Bristol-Myers Squibb Company Met kinase inhibitors
WO2007037534A1 (ja) 2005-09-30 2007-04-05 Banyu Pharmaceutical Co., Ltd. 2-へテロアリール置換インドール誘導体
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
CA2634381C (en) 2005-12-21 2011-03-08 Pfizer Products Inc. Carbonylamino pyrrolopyrazoles, potent kinase inhibitors
AU2006331673B2 (en) 2005-12-23 2013-02-28 Takeda Pharmaceuticals U.S.A., Inc. Bicyclic heteroaryl compounds
WO2007129195A2 (en) * 2006-05-04 2007-11-15 Pfizer Products Inc. 4-pyrimidine-5-amino-pyrazole compounds
JP2009538304A (ja) 2006-05-22 2009-11-05 シェーリング コーポレイション CDK阻害剤としてのピラゾロ[1,5−a]ピリミジン
US20100063049A1 (en) 2006-05-26 2010-03-11 Clifford Jones 2-carbocycloamino-4-imidazolylpyrimidines as agents for the inhbition of cell proliferation
HUE028086T2 (en) 2006-09-22 2016-11-28 Pharmacyclics Llc Inhibitors of bruton's tyrosine kinase
EP2089394B1 (en) 2006-10-11 2011-06-29 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
ES2403546T3 (es) 2006-11-03 2013-05-20 Pharmacyclics, Inc. Sonda de actividad de la tirosina-cinasa de Bruton y procedimiento de utilización
WO2008063888A2 (en) 2006-11-22 2008-05-29 Plexxikon, Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor
WO2008068171A1 (en) 2006-12-08 2008-06-12 F. Hoffmann-La Roche Ag Substituted pyrimidines and their use as jnk modulators
DK2120932T3 (da) 2006-12-20 2014-10-13 Nerviano Medical Sciences Srl Indazolderivater som kinasehæmmere til behandling af kræft
CA2673736A1 (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
BRPI0808772A2 (pt) 2007-03-14 2014-08-12 Exelixis Inc Inibidores da via de hedgehog
WO2008124393A1 (en) 2007-04-04 2008-10-16 Irm Llc Benzothiazole derivatives and their use as protein kinase inhibitors
CN104370914B (zh) 2007-04-12 2018-09-07 辉瑞大药厂 作为蛋白酶c抑制剂的3-酰氨基-吡咯并[3,4-c]吡唑-5(1h,4h,6h)甲醛衍生物
WO2008144253A1 (en) 2007-05-14 2008-11-27 Irm Llc Protein kinase inhibitors and methods for using thereof
EP2152079A4 (en) 2007-06-04 2011-03-09 Avila Therapeutics Inc HETEROCYCLIC COMPOUNDS AND USES THEREOF
CA2688616A1 (en) 2007-06-05 2008-12-11 Emory University Selective inhibitors for cyclin-dependent kinases
JP5561702B2 (ja) 2007-08-02 2014-07-30 アムジエン・インコーポレーテツド Pi3キナーゼ調節剤および使用方法
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
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
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
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
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
US8394818B2 (en) 2008-10-17 2013-03-12 Dana-Farber Cancer Institute, Inc. Soluble mTOR complexes and modulators thereof
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
MX2011008444A (es) * 2009-02-12 2011-09-06 Astellas Pharma Inc Derivado de heteroanillo.
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
CN102480966B (zh) 2009-06-12 2015-09-16 达娜-法勃肿瘤研究所公司 融合的杂环化合物及其用途
AU2010270831A1 (en) 2009-07-07 2012-02-02 Merck Sharp & Dohme Corp. Platelet-activating factor receptor antagonists
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
US8586584B2 (en) 2009-10-14 2013-11-19 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
US8987275B2 (en) 2010-03-16 2015-03-24 Dana-Farber Cancer Institute, Inc. Indazole compounds and their uses
PL2571503T3 (pl) 2010-05-14 2015-06-30 Dana Farber Cancer Inst Inc Kompozycje i sposoby leczenia nowotworu, choroby zapalnej i innych zaburzeń
US8546443B2 (en) 2010-12-21 2013-10-01 Boehringer Ingelheim International Gmbh Benzylic oxindole pyrimidines
DE102011078841A1 (de) * 2011-07-08 2013-01-10 Robert Bosch Gmbh Verfahren zur Ansteuerung einer mehrphasigen Maschine
BR112014000360A2 (pt) 2011-07-28 2017-02-14 Cellzome Ltd análogos de heterociclil pirimidina como inibidores jak
WO2013040436A2 (en) 2011-09-16 2013-03-21 The Regents Of The University Of Michgian Esx-mediated transcription modulators and related methods
US9382239B2 (en) 2011-11-17 2016-07-05 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
US9879003B2 (en) 2012-04-11 2018-01-30 Dana-Farber Cancer Institute, Inc. Host targeted inhibitors of dengue virus and other viruses
US10112927B2 (en) 2012-10-18 2018-10-30 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
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
US10000483B2 (en) 2012-10-19 2018-06-19 Dana-Farber Cancer Institute, Inc. Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
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)
WO2015013635A2 (en) 2013-07-25 2015-01-29 Dana-Farber Cancer Institute, Inc. Inhibitors of transcription factors and uses thereof
EP3057955B1 (en) 2013-10-18 2018-04-11 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of prolferative diseases
CN105849099B (zh) 2013-10-18 2020-01-17 达纳-法伯癌症研究所股份有限公司 周期蛋白依赖性激酶7(cdk7)的多环抑制剂
MX2016009976A (es) 2014-01-31 2016-11-15 Dana Farber Cancer Inst Inc Derivados de diazepam y sus usos.
WO2015117087A1 (en) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Uses of diazepane derivatives
EP3099171A4 (en) 2014-01-31 2017-08-09 Dana-Farber Cancer Institute, Inc. Dihydropteridinone derivatives and uses thereof
KR20160115953A (ko) 2014-01-31 2016-10-06 다나-파버 캔서 인스티튜트 인크. 디아미노피리미딘 벤젠술폰 유도체 및 그의 용도
CN110229142A (zh) 2014-04-04 2019-09-13 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
EP3805218A1 (en) 2014-04-05 2021-04-14 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
WO2016014551A1 (en) 2014-07-21 2016-01-28 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
US20170224700A1 (en) 2014-08-08 2017-08-10 Dana-Farber Cancer Institute, Inc. Uses of salt-inducible kinase (sik) inhibitors
US10308648B2 (en) 2014-10-16 2019-06-04 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
WO2016105528A2 (en) 2014-12-23 2016-06-30 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
ES2899196T3 (es) 2015-03-09 2022-03-10 Aurigene Discovery Tech Ltd Derivados de pirazolo[1,5-a][1,3,5]triazina y de pirazolo[1,5-a]pirimidina como inhibidores de CDK
CA2978518C (en) 2015-03-27 2023-11-21 Nathanael S. Gray Inhibitors of cyclin-dependent kinases
WO2016201370A1 (en) 2015-06-12 2016-12-15 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
CN108348522A (zh) 2015-08-28 2018-07-31 诺华股份有限公司 含(a)周期素依赖性激酶4/6(cdk4/6)抑制剂lee011(=ribociclib)和(b)表皮生长因子受体(egfr)抑制剂厄洛替尼的药物组合,用于治疗或预防癌症
WO2017044858A2 (en) 2015-09-09 2017-03-16 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases

Also Published As

Publication number Publication date
US20190031642A1 (en) 2019-01-31
AU2014337044A1 (en) 2016-05-05
EP3057956B1 (en) 2021-05-05
US20160264554A1 (en) 2016-09-15
CN105849099B (zh) 2020-01-17
CN105849099A (zh) 2016-08-10
EP3057956A1 (en) 2016-08-24
JP2016533379A (ja) 2016-10-27
US10906889B2 (en) 2021-02-02
AU2019200372B2 (en) 2020-07-23
WO2015058140A1 (en) 2015-04-23
AU2019200372A1 (en) 2019-02-07
US10047070B2 (en) 2018-08-14
JP6491202B2 (ja) 2019-03-27

Similar Documents

Publication Publication Date Title
AU2019200372B2 (en) Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7)
US10787436B2 (en) Inhibitors of cyclin-dependent kinase 7 (CDK7)
CA3041563C (en) Pyrimidin-2-amine derivatives and pharmaceutical compositions thereof useful as inhibitors of cyclin-dependent kinase 12 (cdk12)
US11040957B2 (en) Heteroaromatic compounds useful for the treatment of proliferative diseases
US20210061803A1 (en) Inhibitors of cyclin-dependent kinase 7 (cdk7)
EP2822935B1 (en) Inhibitors of c-jun-n-terminal kinase (jnk)
EP3126352B1 (en) Inhibitors of cyclin-dependent kinase 7 (cdk7)
CA2918910A1 (en) Inhibitors of transcription factors and uses thereof
CA2897942A1 (en) Ras inhibitors and uses thereof
JP2018522866A (ja) 4,6−ピリミジニレン誘導体およびこれらの使用
WO2014063054A1 (en) Bone marrow on x chromosome kinase (bmx) inhibitors and uses thereof
CA2988330C (en) 4,6-pyrimidinylene derivatives and uses thereof
HK1229328A1 (en) Inhibitors of cyclin-dependent kinase 7 (cdk7)
HK1229328B (en) Inhibitors of cyclin-dependent kinase 7 (cdk7)

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20191009

EEER Examination request

Effective date: 20191009

FZDE Discontinued

Effective date: 20230601