CA2996978A1 - Inhibitors of cyclin-dependent kinases - Google Patents

Inhibitors of cyclin-dependent kinases Download PDF

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Publication number
CA2996978A1
CA2996978A1 CA2996978A CA2996978A CA2996978A1 CA 2996978 A1 CA2996978 A1 CA 2996978A1 CA 2996978 A CA2996978 A CA 2996978A CA 2996978 A CA2996978 A CA 2996978A CA 2996978 A1 CA2996978 A1 CA 2996978A1
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CA
Canada
Prior art keywords
optionally substituted
compound
pharmaceutically acceptable
acceptable salt
ring
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.)
Pending
Application number
CA2996978A
Other languages
English (en)
French (fr)
Inventor
Mingfeng HAO
Nathanael S. Gray
Tinghu Zhang
Nicholas P. Kwiatkowski
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 CA2996978A1 publication Critical patent/CA2996978A1/en
Pending legal-status Critical Current

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/38Nitrogen atoms
    • C07D277/44Acylated amino or imino radicals
    • C07D277/46Acylated amino or imino radicals by carboxylic acids, or sulfur or nitrogen analogues thereof
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • 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
    • 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
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CA2996978A 2015-09-09 2016-09-09 Inhibitors of cyclin-dependent kinases Pending CA2996978A1 (en)

Applications Claiming Priority (3)

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

Publications (1)

Publication Number Publication Date
CA2996978A1 true CA2996978A1 (en) 2017-03-16

Family

ID=58240329

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2996978A Pending CA2996978A1 (en) 2015-09-09 2016-09-09 Inhibitors of cyclin-dependent kinases

Country Status (6)

Country Link
US (2) US11142507B2 (enExample)
EP (2) EP3347018B1 (enExample)
JP (2) JP7028766B2 (enExample)
AU (1) AU2016319125B2 (enExample)
CA (1) CA2996978A1 (enExample)
WO (1) WO2017044858A2 (enExample)

Families Citing this family (25)

* 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)
US9758522B2 (en) 2012-10-19 2017-09-12 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
EP3057955B1 (en) 2013-10-18 2018-04-11 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of prolferative diseases
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
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
WO2016201370A1 (en) 2015-06-12 2016-12-15 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
JP6927999B2 (ja) * 2016-04-22 2021-09-01 デイナ ファーバー キャンサー インスティチュート,インコーポレイテッド サイクリン依存性キナーゼ9(cdk9)阻害剤のe3リガーゼリガンドとのコンジュゲーションによるcdk9の分解および使用法
AU2017358901B2 (en) * 2016-11-03 2023-01-05 Corvus Pharmaceuticals, Inc. Compounds and methods for modulating interleukin-2-inducible T-cell kinase
US11306070B2 (en) 2016-11-22 2022-04-19 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 12 (CDK12) and uses thereof
WO2019075386A1 (en) * 2017-10-13 2019-04-18 The Regents Of The University Of California MODULATORS OF MTORC1
TWI703149B (zh) 2017-11-16 2020-09-01 美商美國禮來大藥廠 用於抑制cdk7之化合物
WO2019213403A1 (en) 2018-05-02 2019-11-07 Kinnate Biopharma Inc. Inhibitors of cyclin-dependent kinases
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
CN112638373A (zh) 2018-06-29 2021-04-09 金耐特生物制药公司 细胞周期蛋白依赖性激酶抑制剂
WO2020046770A1 (en) * 2018-08-31 2020-03-05 Institute For Cancer Research D/B/A The Research Institute Of Fox Chase Cancer Center Kinase activity in tumors
WO2020140098A1 (en) 2018-12-28 2020-07-02 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 and uses thereof
TWI783480B (zh) 2020-05-27 2022-11-11 美商美國禮來大藥廠 用於抑制cdk7之化合物
CN116802178A (zh) * 2020-11-20 2023-09-22 耶路撒冷希伯来大学伊萨姆研发有限公司 Igf2bp1-rna结合的抑制剂
EP4247808A1 (en) * 2020-11-20 2023-09-27 Yissum Research Development Company of the Hebrew University of Jerusalem Ltd. Inhibitors of igf2bp1-rna binding
TW202317546A (zh) 2021-07-09 2023-05-01 美商普萊克斯姆公司 調節ikzf2之芳基化合物及醫藥組合物
US12084453B2 (en) 2021-12-10 2024-09-10 Incyte Corporation Bicyclic amines as CDK12 inhibitors
CN118255746A (zh) * 2022-12-27 2024-06-28 南京圣和药业股份有限公司 选择性cdk12/13抑制剂及其应用

Family Cites Families (280)

* 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
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
US5312335A (en) 1989-11-09 1994-05-17 Bioject Inc. Needleless hypodermic injection device
US5064413A (en) 1989-11-09 1991-11-12 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
EP0670314A4 (en) 1993-09-22 1996-04-10 Kyowa Hakko Kogyo Kk FARNESYL TRANSFERASE INHIBITORS.
US5661152A (en) 1993-10-15 1997-08-26 Schering Corporation Tricyclic sulfonamide compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
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
TW308594B (enExample) 1993-10-15 1997-06-21 Schering Corp
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
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
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
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
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
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
CA2155448A1 (en) 1994-08-11 1996-02-12 Katerina Leftheris Inhibitors of farnesyl protein transferase
EP0776884B1 (en) 1994-08-11 2000-01-05 Banyu Pharmaceutical Co., Ltd. Substituted amide derivative
AU3192495A (en) 1994-08-12 1996-03-07 Banyu Pharmaceutical Co., Ltd. N,n-disubstituted amic acid derivative
JPH10510261A (ja) 1994-12-09 1998-10-06 ワーナー−ランバート・カンパニー タンパク質:ファルネシルトランスフェラーゼの置換テトラーおよびペンタペプチド阻害剤
US5599302A (en) 1995-01-09 1997-02-04 Medi-Ject Corporation Medical injection system and method, gas spring thereof and launching device using gas spring
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
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
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
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.
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
US5891872A (en) 1995-04-07 1999-04-06 Schering Corporation Tricyclic compounds
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
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
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
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
EP0951285A1 (en) 1996-12-30 1999-10-27 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
IL144578A0 (en) 1999-01-29 2002-05-23 Imclone Systems Inc 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
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
JP3892296B2 (ja) 1999-09-10 2007-03-14 メルク エンド カムパニー インコーポレーテッド チロシンキナーゼ阻害薬
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
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
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
ES2257461T3 (es) 2000-12-21 2006-08-01 Bristol-Myers Squibb Company Inhibidores de tiazolilo de tirosina quinasas de la familia tec.
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
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
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
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
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
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
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
ATE469903T1 (de) 2002-09-04 2010-06-15 Schering Corp Zur behandlung von krebserkrankungen geeignete pyrazolopyrimidine
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
CN100376580C (zh) 2002-09-04 2008-03-26 先灵公司 作为细胞周期蛋白依赖性激酶抑制剂的吡唑并嘧啶
US20050250837A1 (en) 2002-10-18 2005-11-10 D Mello Santosh R Use of C-Raf inhibitors for the treatment of neurodegenerative diseases
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
WO2005040139A2 (en) 2003-10-23 2005-05-06 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
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
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
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
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
AU2006219231B2 (en) 2005-02-28 2010-01-14 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
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
GT200600429A (es) 2005-09-30 2007-04-30 Compuestos organicos
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
GB0520955D0 (en) 2005-10-14 2005-11-23 Cyclacel Ltd Compound
US8247556B2 (en) 2005-10-21 2012-08-21 Amgen Inc. Method for preparing 6-substituted-7-aza-indoles
US20070149508A1 (en) * 2005-11-02 2007-06-28 Targegen, Inc. Six membered heteroaromatic inhibitors targeting resistant kinase mutations
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
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
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
US8148400B2 (en) 2006-12-20 2012-04-03 Bristol-Myers Squibb Company Thiazolyl compounds useful as kinase inhibitors
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
TW200922564A (en) 2007-09-10 2009-06-01 Curis Inc CDK inhibitors containing a zinc binding moiety
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
GB0812031D0 (en) 2008-07-01 2008-08-06 7Tm Pharma As Thiazole derivatives
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
WO2010075542A1 (en) * 2008-12-23 2010-07-01 Curis, Inc. Cdk inhibitors
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
WO2010144416A1 (en) 2009-06-08 2010-12-16 Gaeta Federico C A SUBSTITUTED PYRAZOLO [1,5-a] PYRIDINE COMPOUNDS HAVING MULTI-TARGET ACTIVITY
KR20120026613A (ko) 2009-06-09 2012-03-19 아브락시스 바이오사이언스, 엘엘씨 스티릴-트리아진 유도체와 이들의 치료적 용도
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
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
WO2012066061A1 (en) 2010-11-19 2012-05-24 F. Hoffmann-La Roche Ag Pyrazolopyridines and pyrazolopyridines and their use as tyk2 inhibitors
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
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
ES2616242T3 (es) * 2011-09-28 2017-06-12 Euro-Celtique S.A. Derivados de mostaza de nitrógeno
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)
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
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
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
CN110746424A (zh) 2013-03-15 2020-02-04 西建卡尔有限责任公司 Mk2抑制剂和其用途
WO2014147021A2 (en) 2013-03-20 2014-09-25 Bayer Pharma Aktiengesellschaft Novel compounds
US9938279B2 (en) 2013-04-09 2018-04-10 Energenesis Biomedical Co., Ltd Method for treating disease or condition susceptible to amelioration by AMPK activators and compounds of formula which are useful to activate AMP-activated protein kinase (AMPK)
WO2015013635A2 (en) 2013-07-25 2015-01-29 Dana-Farber Cancer Institute, Inc. Inhibitors of transcription factors and uses thereof
EP3036231B1 (en) 2013-08-22 2020-02-26 Jubilant Biosys Ltd. Substituted pyrimidine compounds, compositions and medicinal applications thereof
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
MX2016009976A (es) 2014-01-31 2016-11-15 Dana Farber Cancer Inst Inc Derivados de diazepam y sus usos.
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
WO2015117087A1 (en) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Uses of diazepane derivatives
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
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)
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

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