JP2018515434A5 - - Google Patents

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JP2018515434A5
JP2018515434A5 JP2017550748A JP2017550748A JP2018515434A5 JP 2018515434 A5 JP2018515434 A5 JP 2018515434A5 JP 2017550748 A JP2017550748 A JP 2017550748A JP 2017550748 A JP2017550748 A JP 2017550748A JP 2018515434 A5 JP2018515434 A5 JP 2018515434A5
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optionally substituted
alkyl
protecting group
pharmaceutically acceptable
solvate
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JP2017550748A
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JP2018515434A (ja
JP6861166B2 (ja
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Priority claimed from PCT/US2016/024345 external-priority patent/WO2016160617A2/en
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Publication of JP2018515434A5 publication Critical patent/JP2018515434A5/ja
Priority to JP2021054539A priority Critical patent/JP7200282B2/ja
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Publication of JP6861166B2 publication Critical patent/JP6861166B2/ja
Priority to JP2022204259A priority patent/JP2023052006A/ja
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JP2017550748A 2015-03-27 2016-03-25 サイクリン依存性キナーゼの阻害剤 Active JP6861166B2 (ja)

Priority Applications (2)

Application Number Priority Date Filing Date Title
JP2021054539A JP7200282B2 (ja) 2015-03-27 2021-03-29 サイクリン依存性キナーゼの阻害剤
JP2022204259A JP2023052006A (ja) 2015-03-27 2022-12-21 サイクリン依存性キナーゼの阻害剤

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562139352P 2015-03-27 2015-03-27
US62/139,352 2015-03-27
PCT/US2016/024345 WO2016160617A2 (en) 2015-03-27 2016-03-25 Inhibitors of cyclin-dependent kinases

Related Child Applications (1)

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JP2021054539A Division JP7200282B2 (ja) 2015-03-27 2021-03-29 サイクリン依存性キナーゼの阻害剤

Publications (3)

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JP2018515434A JP2018515434A (ja) 2018-06-14
JP2018515434A5 true JP2018515434A5 (cg-RX-API-DMAC7.html) 2019-05-09
JP6861166B2 JP6861166B2 (ja) 2021-04-21

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JP2017550748A Active JP6861166B2 (ja) 2015-03-27 2016-03-25 サイクリン依存性キナーゼの阻害剤
JP2021054539A Active JP7200282B2 (ja) 2015-03-27 2021-03-29 サイクリン依存性キナーゼの阻害剤
JP2022204259A Pending JP2023052006A (ja) 2015-03-27 2022-12-21 サイクリン依存性キナーゼの阻害剤

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JP2021054539A Active JP7200282B2 (ja) 2015-03-27 2021-03-29 サイクリン依存性キナーゼの阻害剤
JP2022204259A Pending JP2023052006A (ja) 2015-03-27 2022-12-21 サイクリン依存性キナーゼの阻害剤

Country Status (8)

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US (3) US10550121B2 (cg-RX-API-DMAC7.html)
EP (1) EP3273966B1 (cg-RX-API-DMAC7.html)
JP (3) JP6861166B2 (cg-RX-API-DMAC7.html)
CN (1) CN107427521B (cg-RX-API-DMAC7.html)
AU (1) AU2016243529B2 (cg-RX-API-DMAC7.html)
CA (1) CA2978518C (cg-RX-API-DMAC7.html)
HK (1) HK1246645A1 (cg-RX-API-DMAC7.html)
WO (1) WO2016160617A2 (cg-RX-API-DMAC7.html)

Families Citing this family (54)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2784807C (en) 2009-12-29 2021-12-14 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
WO2013074986A1 (en) 2011-11-17 2013-05-23 Dana-Farber Cancer Institute, Inc. Inhibitors of c-jun-n-terminal kinase (jnk)
EP2909194A1 (en) 2012-10-18 2015-08-26 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
USRE48175E1 (en) 2012-10-19 2020-08-25 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
ES2676734T3 (es) 2013-10-18 2018-07-24 Syros Pharmaceuticals, Inc. Compuestos heteroatómicos útiles para el tratamiento de enfermedades proliferativas
US10047070B2 (en) 2013-10-18 2018-08-14 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7)
EP3236959B1 (en) 2014-12-23 2025-09-24 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
EP3268000B1 (en) * 2015-03-09 2021-08-04 Aurigene Discovery Technologies Limited Pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives as cdk inhibitors
WO2016160617A2 (en) * 2015-03-27 2016-10-06 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
AU2016276963C1 (en) 2015-06-12 2021-08-05 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
JP7028766B2 (ja) 2015-09-09 2022-03-02 ダナ－ファーバー キャンサー インスティテュート， インコーポレイテッド サイクリン依存性キナーゼの阻害剤
US11306070B2 (en) * 2016-11-22 2022-04-19 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 12 (CDK12) and uses thereof
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
MX2020007797A (es) * 2018-01-29 2020-09-18 Merck Patent Gmbh Inhibidores de la cinasa 2 de control general no desrepresible (gcn2) y usos de los mismos.
EP3787629A4 (en) 2018-05-02 2022-01-05 Kinnate Biopharma Inc. CYCLINE-DEPENDENT KINASE INHIBITORS
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
WO2020006497A1 (en) 2018-06-29 2020-01-02 Kinnate Biopharma Inc. Inhibitors of cyclin-dependent kinases
MX2021000895A (es) 2018-07-27 2021-08-24 California Inst Of Techn Inhibidores de cinasas dependientes de ciclinas (cdk) y usos de los mismos.
EP3873911A4 (en) 2018-10-30 2022-06-22 Kronos Bio, Inc. COMPOUNDS, COMPOSITIONS AND METHODS OF MODULATING CDK9 ACTIVITY
CA3118330A1 (en) * 2018-11-01 2020-05-07 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
CN111217814B (zh) * 2018-11-26 2022-08-26 天津科技大学 一类联哌啶衍生物及其作为抗肿瘤药物的应用
EP3902542A4 (en) 2018-12-28 2022-09-07 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 and uses thereof
CN109988172B (zh) * 2019-01-10 2020-09-29 石家庄学院 一种吡唑并[1,5-a]嘧啶类杂环化合物及衍生物的合成方法
US20220144841A1 (en) * 2019-03-13 2022-05-12 The Translational Genomics Research Institute Trisubstituted pyrazolo [1,5-a] pyrimidine compounds as cdk7 inhibitors
EP3947382B1 (en) * 2019-03-26 2025-09-24 Academia Sinica Compounds for uses in pharmacological induction of hbf for treatment of sickle cell disease and beta-thalassemia
CN110075116A (zh) * 2019-04-23 2019-08-02 昆明医科大学 Sox4的抑制剂的应用及包含sox4的抑制剂的药物
CN110613850A (zh) * 2019-05-24 2019-12-27 中国医学科学院北京协和医院 周期蛋白依赖性激酶1抑制剂及其用途
CA3147106A1 (en) * 2019-07-23 2021-01-28 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 and uses thereof
CN111253371B (zh) * 2019-11-29 2023-01-31 中国药科大学 靶向cdk9的小分子调控剂、及其合成方法与应用
WO2021138391A1 (en) 2019-12-30 2021-07-08 Tyra Biosciences, Inc. Indazole compounds
US20230158159A1 (en) * 2020-04-24 2023-05-25 Massachusetts Institute Of Technology Chimeric degraders of cyclin-dependent kinase 9 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
WO2022033552A1 (zh) * 2020-08-12 2022-02-17 隆泰申医药科技(南京) 有限公司 Cdk激酶抑制剂、其制备方法、药物组合物和应用
CN112716957B (zh) * 2020-12-28 2022-10-14 复旦大学附属肿瘤医院 Cdk7靶向抑制剂在制备治疗car-t治疗引起的细胞因子释放综合征药物中的用途
JP7657943B2 (ja) * 2021-01-22 2025-04-07 上海海雁医薬科技有限公司 置換ピラゾロ［１，５－ａ］ピリミジン－７－アミン誘導体、その組成物及び医薬上の使用
US20240254138A1 (en) * 2021-03-09 2024-08-01 Janssen Pharmaceutica Nv Tricyclic pyrimidines as cyclin-dependent kinase 7 (cdk7) inhibitors
WO2022206795A1 (en) * 2021-04-02 2022-10-06 Taizhou Eoc Pharma Co., Ltd. A cyclin-dependent kinase inhibitor
CN117916235A (zh) * 2021-08-11 2024-04-19 泰州亿腾景昂药业股份有限公司 周期蛋白依赖性激酶抑制剂
WO2023046128A1 (en) * 2021-09-27 2023-03-30 Taizhou Eoc Pharma Co., Ltd. A cyclin-dependent kinase inhibitor
US20250019382A1 (en) 2021-11-23 2025-01-16 Origenis Gmbh Novel inhibitors of cyclin-dependent kinases
WO2023107705A1 (en) 2021-12-10 2023-06-15 Incyte Corporation Bicyclic amines as cdk12 inhibitors
WO2023109876A1 (en) * 2021-12-16 2023-06-22 Edigene Therapeutics (Beijing) Inc. Biomarkers for colorectal cancer treatment
CN114452391B (zh) * 2022-01-28 2023-08-25 深圳市泰尔康生物医药科技有限公司 Cdk16作为靶标在制备用于治疗三阴性乳腺癌的药物中的应用
CN116693538A (zh) * 2022-03-04 2023-09-05 成都苑东生物制药股份有限公司 一种吡唑并嘧啶类衍生物、其制备方法及用途
WO2023186065A1 (en) * 2022-04-02 2023-10-05 Taizhou Eoc Pharma Co., Ltd. A cyclin-dependent kinase inhibitor
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
WO2024017365A1 (zh) * 2022-07-22 2024-01-25 上海海雁医药科技有限公司 取代的吡唑并[1,5-a]嘧啶-7-胺衍生物的药学上可接受的盐和多晶型物及其应用
CN118126043B (zh) * 2022-12-02 2025-01-28 沈阳药科大学 一种高选择性的plk4抑制剂及制备方法和应用
WO2024127350A1 (en) 2022-12-16 2024-06-20 Astrazeneca Ab 2,6,9-trisubstituted purines
CN120712267A (zh) * 2023-02-21 2025-09-26 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
WO2024242416A1 (ko) * 2023-05-22 2024-11-28 주식회사 셀러스 신규한 cdk7 억제 화합물 및 이의 용도
WO2025040170A1 (zh) * 2023-08-24 2025-02-27 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
WO2025153034A1 (zh) * 2024-01-19 2025-07-24 上海海雁医药科技有限公司 一种吡唑并嘧啶衍生物的磷酸盐多晶型物及其应用
CN119462661A (zh) * 2024-09-24 2025-02-18 烟台皓元生物医药科技有限公司 一种azd-8421及其中间体的制备方法

Family Cites Families (341)

* 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
CA1283827C (en) 1986-12-18 1991-05-07 Giorgio Cirelli Appliance for injection of liquid formulations
GB8704027D0 (en) 1987-02-20 1987-03-25 Owen Mumford Ltd Syringe needle combination
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
US4940460A (en) 1987-06-19 1990-07-10 Bioject, Inc. Patient-fillable and non-invasive hypodermic injection device assembly
US4782084A (en) 1987-06-29 1988-11-01 Merck & Co., Inc. HMG-COA reductase inhibitors
US4885314A (en) 1987-06-29 1989-12-05 Merck & Co., Inc. Novel HMG-CoA reductase inhibitors
US5339163A (en) 1988-03-16 1994-08-16 Canon Kabushiki Kaisha Automatic exposure control device using plural image plane detection areas
FR2638359A1 (fr) 1988-11-03 1990-05-04 Tino Dalto Guide de seringue avec reglage de la profondeur de penetration de l'aiguille dans la peau
US5064413A (en) 1989-11-09 1991-11-12 Bioject, Inc. Needleless hypodermic injection device
US5312335A (en) 1989-11-09 1994-05-17 Bioject Inc. Needleless hypodermic injection device
US5420245A (en) 1990-04-18 1995-05-30 Board Of Regents, The University Of Texas Tetrapeptide-based inhibitors of farnesyl transferase
US5190521A (en) 1990-08-22 1993-03-02 Tecnol Medical Products, Inc. Apparatus and method for raising a skin wheal and anesthetizing skin
US5527288A (en) 1990-12-13 1996-06-18 Elan Medical Technologies Limited Intradermal drug delivery device and method for intradermal delivery of drugs
US5747469A (en) 1991-03-06 1998-05-05 Board Of Regents, The University Of Texas System Methods and compositions comprising DNA damaging agents and p53
GB9118204D0 (en) 1991-08-23 1991-10-09 Weston Terence E Needle-less injector
SE9102652D0 (sv) 1991-09-13 1991-09-13 Kabi Pharmacia Ab Injection needle arrangement
US5328483A (en) 1992-02-27 1994-07-12 Jacoby Richard M Intradermal injection device with medication and needle guard
US5383851A (en) 1992-07-24 1995-01-24 Bioject Inc. Needleless hypodermic injection device
US5569189A (en) 1992-09-28 1996-10-29 Equidyne Systems, Inc. hypodermic jet injector
US5334144A (en) 1992-10-30 1994-08-02 Becton, Dickinson And Company Single use disposable needleless injector
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
JPH09500615A (ja) 1993-05-14 1997-01-21 ジェネンテク，インコーポレイテッド Ｒａｓ−ファルネシル転移酵素阻害剤
US5602098A (en) 1993-05-18 1997-02-11 University Of Pittsburgh Inhibition of farnesyltransferase
EP0670314A4 (en) 1993-09-22 1996-04-10 Kyowa Hakko Kogyo Kk FARNESYL TRANSFERASE INHIBITORS.
ATE210652T1 (de) 1993-10-15 2001-12-15 Schering Corp Tricyclische carbamat-derivate zur inhibierung der g-protein funktion und für die behandlung von proliferativen erkrankungen
IL111235A (en) 1993-10-15 2001-03-19 Schering Plough Corp Medicinal preparations for inhibiting protein G activity and for the treatment of malignant diseases, containing tricyclic compounds, some such new compounds and a process for the preparation of some of them
US5719148A (en) 1993-10-15 1998-02-17 Schering Corporation Tricyclic amide and urea compounds useful for inhibition of g-protein function and for treatment of proliferative diseases
ZA947969B (en) 1993-10-15 1996-07-12 Schering Corp Tricyclic sulfonamide compounds useful for inhibition of g-protein function and for treatment of proliferative diseases
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
ES2157994T3 (es) 1993-10-25 2001-09-01 Parke Davis & Co Inhibidores tetra y pentapeptidos sustituidos de la proteina farnesiltransferasa.
DK0677039T3 (da) 1993-11-04 1999-09-27 Abbott Lab Cyclobutanderivater som squalen-syntetase- og protein-farnesyltransferaseinhibitorer
US5783593A (en) 1993-11-04 1998-07-21 Abbott Laboratories Inhibitors of squalene synthetase and protein farnesyltransferase
KR100362338B1 (ko) 1993-11-05 2003-04-08 워너-램버트 캄파니 단백질:파르네실트랜스퍼라아제의치환디-및트리펩티드억제제
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
WO1995024612A1 (de) 1994-03-07 1995-09-14 International Business Machines Corporation Verfahren und vorrichtung zur schnellen interpolation von zwischenwerten aus periodischen phasenverschobenen signalen und zur erkennung von defekten in einem drehkörper
US5466220A (en) 1994-03-08 1995-11-14 Bioject, Inc. Drug vial mixing and transfer device
HUT77406A (hu) 1994-03-15 1998-04-28 Eisai Co., Ltd., 1-(4-Amino-5-tio-pent-2-en)-il oldalláncot tartalmazó peptidomimetikumok és az ezeket tartalmazó gyógyszerkészítmények
US6312699B1 (en) 1994-03-28 2001-11-06 Uab Research Foundation Ligands added to adenovirus fiber
RU95104898A (ru) 1994-03-31 1996-12-27 Бристоль-Мейерз Сквибб Компани (US) Имидазолсодержащие ингибиторы фарнезид-протеинтрансферазы, способ лечения связанных с ней заболеваний
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
AU2742195A (en) 1994-06-10 1996-01-05 Rhone-Poulenc Rorer S.A. Novel farnesyl transferase inhibitors, their preparation and pharmaceutical compositions containing same
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
CA2155448A1 (en) 1994-08-11 1996-02-12 Katerina Leftheris Inhibitors of farnesyl protein transferase
AU3192395A (en) 1994-08-11 1996-03-07 Banyu Pharmaceutical Co., Ltd. Substituted amide derivative
WO1996005169A1 (en) 1994-08-12 1996-02-22 Banyu Pharmaceutical Co., Ltd. N,n-disubstituted amic acid derivative
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
JP4319251B2 (ja) 1994-11-22 2009-08-26 エヌエックスピー ビー ヴィ 半導体素子を有し導体トラックが形成されている基板が接着層により結合されている支持本体を有する半導体装置
WO1996017861A1 (en) 1994-12-09 1996-06-13 Warner-Lambert Company Substituted tetra- and pentapeptide inhibitors of protein:farnesyl transferase
EA000164B1 (ru) 1995-01-09 1998-10-29 Магла Интернэшнл Лтд. Состав для печати изображения на поверхности изделия из каучукового латекса, способ печати изображения и изделия из каучукового латекса
US5599302A (en) 1995-01-09 1997-02-04 Medi-Ject Corporation Medical injection system and method, gas spring thereof and launching device using gas spring
JP3929069B2 (ja) 1995-01-12 2007-06-13 ユニバーシティ オブ ピッツバーグ プレニルトランスフェラーゼの阻害剤
FR2729390A1 (fr) 1995-01-18 1996-07-19 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
FR2730491B1 (fr) 1995-02-09 1997-03-14 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
FR2730492B1 (fr) 1995-02-09 1997-03-14 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
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
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
IL117580A0 (en) 1995-03-29 1996-07-23 Merck & Co Inc Inhibitors of farnesyl-protein transferase and pharmaceutical compositions containing them
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
AU5432696A (en) 1995-04-07 1996-10-23 Pharmacopeia, Inc. Carbonyl-piperazinyl and piperidinil compounds which inhibit farnesyl protein transferase
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
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
AT402617B (de) 1995-07-11 1997-07-25 Datacon Schweitzer & Zeindl Gm Anlage zum automatisierten, hermetischen anlage zum automatisierten, hermetischen verschliessen von gehäusen verschliessen von gehäusen
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.
DE69627195T2 (de) * 1995-11-01 2004-01-29 Novartis Ag Purinderivate und verfahren zu ihrer herstellung
WO1997017070A1 (en) 1995-11-06 1997-05-15 University Of Pittsburgh Inhibitors of protein isoprenyl transferases
EP0862435A4 (en) 1995-11-22 1999-02-03 Merck & Co Inc Inhibitors of farnesyl-protein transferase
SI0865440T1 (en) 1995-12-08 2002-08-31 Janssen Pharmaceutica N.V. Farnesyl protein transferase inhibiting (imidazol-5-yl)methyl-2-quinolinone derivatives
CA2240846C (en) 1995-12-22 2002-07-16 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
AU1529997A (en) 1996-01-16 1997-08-11 Warner-Lambert Company Substituted histidine inhibitors of protein farnesyltransferase
US6673927B2 (en) 1996-02-16 2004-01-06 Societe De Conseils De Recherches Et D'applications Scientifiques, S.A.S. Farnesyl transferase inhibitors
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
AU709409B2 (en) 1996-07-15 1999-08-26 Bristol-Myers Squibb Company Thiadioxobenzodiazepine inhibitors of farnesyl protein transferase
US5866702A (en) * 1996-08-02 1999-02-02 Cv Therapeutics, Incorporation Purine inhibitors of cyclin dependent kinase 2
EP1003374A4 (en) 1996-12-30 2000-05-31 Merck & Co Inc INHIBITORS OF FARNESYL PROTEIN TRANSFERASE
JP2001507699A (ja) 1996-12-30 2001-06-12 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
US6040321A (en) 1997-11-12 2000-03-21 Bristol-Myers Squibb Company Aminothiazole inhibitors of cyclin dependent kinases
US6262096B1 (en) 1997-11-12 2001-07-17 Bristol-Myers Squibb Company Aminothiazole inhibitors of cyclin dependent kinases
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
WO2000044777A1 (en) 1999-01-29 2000-08-03 Imclone Systems Incorporated Antibodies specific to kdr and uses thereof
GB9903762D0 (en) * 1999-02-18 1999-04-14 Novartis Ag Organic compounds
GB9904387D0 (en) 1999-02-25 1999-04-21 Pharmacia & Upjohn Spa Antitumour synergistic composition
WO2000061186A1 (en) 1999-04-08 2000-10-19 Arch Development Corporation Use of anti-vegf antibody to enhance radiation in cancer therapy
US6329380B1 (en) 1999-06-30 2001-12-11 Merck & Co., Inc. SRC kinase inhibitor compounds
PE20010306A1 (es) 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa
PL355639A1 (en) 1999-09-10 2004-05-04 Merck & Co, Inc. Tyrosine kinase inhibitors
JP2003509428A (ja) 1999-09-17 2003-03-11 アボツト・ゲー・エム・ベー・ハー・ウント・コンパニー・カーゲー 治療薬としてのピラゾロピリミジン
US6921763B2 (en) 1999-09-17 2005-07-26 Abbott Laboratories Pyrazolopyrimidines as therapeutic agents
CN1391562A (zh) 1999-09-21 2003-01-15 阿斯特拉曾尼卡有限公司 用作药物的喹唑啉衍生物
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
NZ524475A (en) 2000-08-10 2004-11-26 Pharmacia Italia S Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
ATE426603T1 (de) * 2000-10-31 2009-04-15 Aventis Pharma Inc Acyl- und sulfonylderivative 6,9- disubstitutierter 2-(trans-1,4-diaminocyclohexyl)-purine und ihre verwendung als antiproliferative mittel
US7429599B2 (en) 2000-12-06 2008-09-30 Signal Pharmaceuticals, Llc Methods for treating or preventing an inflammatory or metabolic condition or inhibiting JNK
DE60117605T2 (de) 2000-12-21 2006-12-07 Bristol-Myers Squibb Co. Thiazolyl-inhibitoren von tyrosinkinasen der tec-familie
PT1355905E (pt) 2000-12-21 2007-05-31 Vertex Pharma Compostos de pirazole úteis como inibidores de proteínaquinase
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.
ES2292753T4 (es) 2001-03-29 2009-02-16 Vertex Pharmaceuticals Incorporated Inhibidores de quinasas n-terminales c-jun (jnk) y otras proteina quinasas.
AU2002247847A1 (en) 2001-04-09 2002-10-21 Lorantis Limited Therapeutic use and identification of modulators of a hedgehog signalling pathway or one of its target pathways
US6881737B2 (en) 2001-04-11 2005-04-19 Amgen Inc. Substituted triazinyl acrylamide derivatives and methods of use
JP2002338537A (ja) 2001-05-16 2002-11-27 Mitsubishi Pharma Corp アミド化合物およびその医薬用途
FR2825278A1 (fr) * 2001-05-30 2002-12-06 Sod Conseils Rech Applic Produit comprenant du mikanolide, du dihydromikanolide ou un analogue de ceux-ci en association avec un autre agent anti-cancereux pour une utilisation therapeutique dans le traitement du cancer
CA2446756C (en) 2001-06-01 2011-03-08 Vertex Pharmaceuticals Incorporated Thiazole compounds useful as inhibitors of protein kinase
ATE432929T1 (de) 2001-06-15 2009-06-15 Vertex Pharma 5-(2-aminopyrimidin-4-yl)benzisoxazole als proteinkinasehemmer
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
WO2003026665A1 (en) 2001-09-26 2003-04-03 Bayer Pharmaceuticals Corporation 2-phenylamino-4-(5-pyrazolylamino)-pyrimidine derivatives as kinase inhibitors, in particular, src kinase inhibitors
AU2002353186A1 (en) 2001-12-19 2003-06-30 Smithkline Beecham P.L.C. (1-h-indazol-3-yl) -amide derivatives as gsk-3 inhibitors
FR2836915B1 (fr) 2002-03-11 2008-01-11 Aventis Pharma Sa Derives d'aminoindazoles, procede de preparation et intermediaires de ce procede a titre de medicaments et compositions pharmaceutiques les renfermant
AU2003231231A1 (en) 2002-05-06 2003-11-11 Bayer Pharmaceuticals Corporation Pyridinyl amino pyrimidine derivatives useful for treating hyper-proliferative disorders
BR0311291A (pt) 2002-05-17 2005-03-29 Pharmacia Italia Spa Derivados de aminoindazol ativos como inibidores da cinase, processo para sua preparação e composições farmacêuticas compreendendo os mesmos
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
CA2491895C (en) 2002-07-09 2011-01-18 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
TWI329112B (en) 2002-07-19 2010-08-21 Bristol Myers Squibb Co Novel inhibitors of kinases
GB0217757D0 (en) 2002-07-31 2002-09-11 Glaxo Group Ltd Novel compounds
DE10239042A1 (de) 2002-08-21 2004-03-04 Schering Ag Makrozyclische Pyrimidine, deren Herstellung und Verwendung als Arzneimittel
US7196078B2 (en) * 2002-09-04 2007-03-27 Schering Corpoartion Trisubstituted and tetrasubstituted pyrazolopyrimidines as cyclin dependent kinase inhibitors
CN1880317B (zh) * 2002-09-04 2012-10-10 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
ATE469903T1 (de) * 2002-09-04 2010-06-15 Schering Corp Zur behandlung von krebserkrankungen geeignete pyrazolopyrimidine
ES2283868T3 (es) * 2002-09-04 2007-11-01 Schering Corporation Compuestos pirazol(1,5-a) pirimidina como inhibidores de quinasa dependiente de ciclina.
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
JP4845380B2 (ja) * 2002-09-19 2011-12-28 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
EP1562935B1 (de) 2002-10-28 2006-09-06 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
ATE479667T1 (de) 2003-02-06 2010-09-15 Bristol Myers Squibb Co Als kinaseinhibitoren geeignete verbindungen auf thiazolylbasis
EP1597256A1 (en) 2003-02-21 2005-11-23 Pfizer Inc. N-heterocyclyl-substituted amino-thiazole derivatives as protein kinase inhibitors
GB0304665D0 (en) * 2003-02-28 2003-04-02 Teijin Ltd Compounds
BRPI0407834A (pt) * 2003-02-28 2006-02-14 Teijin Pharma Ltd composto, processo para a manufatura do mesmo, composição, processo para a manufatura da mesma, método de tratamento ou prevenção de um distúrbio mediado por proteìna quinase em um indivìduo, uso de um composto, ensaio para determinar a atividade dos compostos, e, método de inibição da atividade ou função de uma proteìna quinase
GB0305142D0 (en) 2003-03-06 2003-04-09 Eisai London Res Lab Ltd Synthesis
GB0305559D0 (en) * 2003-03-11 2003-04-16 Teijin Ltd Compounds
ATE396731T1 (de) 2003-03-25 2008-06-15 Vertex Pharma Thiazole zur verwendung als inhibitoren von protein-kinasen
WO2004087707A1 (en) 2003-03-31 2004-10-14 Vernalis (Cambridge) Limited Pyrazolopyrimidine compounds and their use in medicine
WO2004100868A2 (en) 2003-04-23 2004-11-25 Abbott Laboratories Method of treating transplant rejection
EP1638941B1 (en) 2003-05-22 2010-06-02 Abbott Laboratories Indazole, benzisoxazole, and benzisothiazole kinase inhibitors
SE0301906D0 (sv) 2003-06-26 2003-06-26 Astrazeneca Ab New compounds
GB0315657D0 (en) 2003-07-03 2003-08-13 Astex Technology Ltd Pharmaceutical compounds
PL1651612T3 (pl) 2003-07-22 2012-09-28 Astex Therapeutics Ltd Związki 3,4-pochodne 1h-pirazolu i ich zastosowanie jako kinazy zależne od cyklin (cdk) i modulatory kinazy syntazy glikogenu-3 (gsk-3)
US7442698B2 (en) 2003-07-24 2008-10-28 Amgen Inc. Substituted heterocyclic compounds and methods of use
CA2533774A1 (en) 2003-07-29 2005-02-10 Irm Llc Compounds and compositions as protein kinase inhibitors
SI2287156T1 (sl) 2003-08-15 2013-09-30 Novartis Ag 2,4-di(fenilamino)-pirimidini, uporabni pri zdravljenju neoplastičnih bolezni, vnetnih motenj in motenj imunskega sistema
WO2005037845A1 (en) 2003-10-17 2005-04-28 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
ATE465731T1 (de) 2003-10-23 2010-05-15 Ab Science 2-aminoaryloxazol-verbindungen als tyrosinkinase- hemmer
DE10357510A1 (de) 2003-12-09 2005-07-07 Bayer Healthcare Ag Heteroarylsubstituierte Benzole
US20070281907A1 (en) 2003-12-22 2007-12-06 Watkins William J Kinase Inhibitor Phosphonate Conjugates
ES2651615T3 (es) 2003-12-25 2018-01-29 Nippon Shinyaku Co., Ltd. Amidoderivado y medicamento
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
CA2567662C (en) 2004-06-10 2012-11-27 Irm Llc Compounds and compositions as protein kinase inhibitors
DE102004028862A1 (de) 2004-06-15 2005-12-29 Merck Patent Gmbh 3-Aminoindazole
AU2005278959A1 (en) 2004-08-31 2006-03-09 Astrazeneca Ab Quinazolinone derivatives and their use as B-Raf inhibitors
WO2006031806A2 (en) 2004-09-10 2006-03-23 Atherogenics, Inc. 2-thiopyrimidinones as therapeutic agents
TW200626155A (en) 2004-09-20 2006-08-01 Xenon Pharmaceuticals Inc Heterocyclic derivatives and their use as therapeutic agents
BRPI0518126A (pt) 2004-10-15 2008-10-28 Astrazeneca Ab composto, processo para preparar o mesmo, composição farmacêutica, uso de um composto, e, métodos para produzir um efeito inibitório de b-raf e um efeito anti-cáncer em um animal de sangue quente, e para tratar uma doença ou condição
US7632854B2 (en) 2004-11-17 2009-12-15 Pfizer Italia S.R.L. Aminoindazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
EP1841760B1 (en) 2004-12-30 2011-08-10 Exelixis, Inc. Pyrimidine derivatives as kinase modulators and method of use
JP4250195B2 (ja) 2005-01-10 2009-04-08 ファイザー・インク ピロロピラゾール類、強力なキナーゼ阻害剤
AR052660A1 (es) 2005-01-21 2007-03-28 Astex Therapeutics Ltd Derivados de pirazol para inhibir la cdk's y gsk's
CN101106990B (zh) 2005-01-26 2010-12-08 Irm责任有限公司 用作蛋白激酶抑制剂的化合物和组合物
TW200639163A (en) 2005-02-04 2006-11-16 Genentech Inc RAF inhibitor compounds and methods
JPWO2006085685A1 (ja) 2005-02-09 2008-06-26 武田薬品工業株式会社 ピラゾール化合物
DE102005008310A1 (de) 2005-02-17 2006-08-24 Schering Ag Verwendung von CDKII Inhibitoren zur Fertilitätskontrolle
CA2599544A1 (en) 2005-02-28 2006-09-08 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
CN101218241B (zh) 2005-05-16 2011-02-16 Irm责任有限公司 用作蛋白激酶抑制剂的吡咯并吡啶衍生物
CN102603581B (zh) 2005-06-22 2015-06-24 普莱希科公司 作为蛋白质激酶抑制剂的吡咯并[2,3-b]吡啶衍生物
WO2007024680A1 (en) 2005-08-22 2007-03-01 Amgen Inc. Pyrazolopyridine and pyrazolopyrimidine compounds useful as kinase enzymes modulators
WO2007035428A1 (en) 2005-09-15 2007-03-29 Bristol-Myers Squibb Company Met kinase inhibitors
US7799820B2 (en) 2005-09-30 2010-09-21 Banyu Pharmaceutical Co., Ltd. 2-Heterocycle-substituted indole derivatives for treating diabetes and associated conditions
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
US20070161645A1 (en) 2005-11-02 2007-07-12 Targegen, Inc. Thiazole inhibitors targeting resistant kinase mutations
RS20080281A (sr) 2005-12-21 2009-09-08 Pfizer Products Inc., Karbonilamino pirolopirazoli, snažni inhibitori kinaza
WO2007071963A2 (en) 2005-12-22 2007-06-28 Astrazeneca Ab Quinazoline derivatives, process for their preparation and their use as anti-cancer agents
DK2495016T3 (da) 2005-12-23 2019-12-16 Ariad Pharma Inc Bicykliske heteroarylforbindelser
WO2007076474A1 (en) 2005-12-23 2007-07-05 Kalypsys, Inc. Novel substituted pyridinyloxy and pyrimidinyloxy amides useful as inhibitors of protein kinases
WO2007076161A2 (en) 2005-12-27 2007-07-05 Myriad Genetics, Inc Compounds with therapeutic activity
WO2007086584A1 (ja) 2006-01-30 2007-08-02 Meiji Seika Kaisha, Ltd. 新規ＦａｂＫおよびＦａｂＩ／Ｋ阻害剤
WO2007129195A2 (en) 2006-05-04 2007-11-15 Pfizer Products Inc. 4-pyrimidine-5-amino-pyrazole compounds
PE20080071A1 (es) * 2006-05-22 2008-02-11 Schering Corp PIRAZOLO[1,5-a]PIRIMIDINAS
JP2009538352A (ja) 2006-05-26 2009-11-05 アストラゼネカ アクチボラグ 細胞増殖を阻害するための薬剤としての２−カルボシクロアミノ−４−イミダゾリルピリミジン類
US20090318430A1 (en) 2006-07-21 2009-12-24 Astex Therapeutics Limited Medical use of cyclin dependent kinases inhibitors
EP2063882A4 (en) 2006-09-05 2010-03-03 Univ Emory TYROSINKINASE INHIBITOR FOR PREVENTING OR TREATING INFECTIONS
ES2616789T3 (es) 2006-09-22 2017-06-14 Pharmacyclics, Inc. Inhibidores de tirosina cinasa de Bruton
US8227472B2 (en) 2006-10-11 2012-07-24 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
EP2089391B1 (en) 2006-11-03 2013-01-16 Pharmacyclics, Inc. Bruton's tyrosine kinase activity probe and method of using
WO2008063888A2 (en) 2006-11-22 2008-05-29 Plexxikon, Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor
MX2009005508A (es) 2006-12-08 2009-06-03 Hoffmann La Roche Pirimidinas substituidas y su uso como moduladores de cinasas c-jun n-terminales.
US8148400B2 (en) 2006-12-20 2012-04-03 Bristol-Myers Squibb Company Thiazolyl compounds useful as kinase inhibitors
SI2120932T1 (sl) 2006-12-20 2014-09-30 Nerviano Medical Sciences S.R.L. Indazolni derivati kot kinazni inhibitorji za zdravljenje raka
BRPI0720695A2 (pt) 2006-12-21 2014-02-18 Plexxikon Inc Compostos e métodos para modulação de cinase, e indicações para estes
JP5161245B2 (ja) 2007-02-07 2013-03-13 ファイザー・インク ＰＫＣ阻害剤としての３−アミノ−ピロロ［３，４−ｃ］ピラゾール−５（１Ｈ，４Ｈ，６Ｈ）カルボアルデヒド誘導体
MX2009009786A (es) 2007-03-14 2009-09-24 Exelixis Inc Inhibidores de la via de hedgehog.
WO2008124393A1 (en) 2007-04-04 2008-10-16 Irm Llc Benzothiazole derivatives and their use as protein kinase inhibitors
CN101675052A (zh) 2007-04-12 2010-03-17 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
US8242271B2 (en) 2007-06-04 2012-08-14 Avila Therapeutics, Inc. Heterocyclic compounds and uses thereof
JP2010529140A (ja) * 2007-06-05 2010-08-26 エモリー・ユニバーシテイ サイクリン依存性キナーゼの選択的阻害剤
EP2170852A1 (en) 2007-06-11 2010-04-07 Bristol-Myers Squibb Company 1, 3 - dihydroxy substituted phenylamide glucokinase activators
WO2009017822A2 (en) 2007-08-02 2009-02-05 Amgen Inc. Pi3 kinase modulators and methods of use
US20090054392A1 (en) 2007-08-20 2009-02-26 Wyeth Naphthylpyrimidine, naphthylpyrazine and naphthylpyridazine analogs and their use as agonists of the wnt-beta-catenin cellular messaging system
WO2009032703A1 (en) 2007-08-28 2009-03-12 Irm Llc 2- (het) arylamino-6-aminopyridine derivatives and fused forms thereof as anaplastic lymphoma kinase inhibitors
WO2009028655A1 (ja) 2007-08-30 2009-03-05 Takeda Pharmaceutical Company Limited 複素環化合物およびその用途
TW200922564A (en) 2007-09-10 2009-06-01 Curis Inc CDK inhibitors containing a zinc binding moiety
KR100923540B1 (ko) 2007-11-23 2009-10-27 한국과학기술연구원 5-아실하이드라진카르보닐-3,4-디치환 피라졸 유도체 및이의 제조방법
KR20130040258A (ko) 2008-03-21 2013-04-23 노파르티스 아게 신규한 헤테로시클릭 화합물 및 그의 용도
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
ES2554772T3 (es) 2008-05-30 2015-12-23 Merck Sharp & Dohme Corp. Azabenzoxazoles sustituidos novedosos
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
EP2311842A3 (en) 2008-06-24 2011-07-13 Takeda Pharmaceutical Company Limited PI3K/M TOR inhibitors
GB0812031D0 (en) 2008-07-01 2008-08-06 7Tm Pharma As Thiazole derivatives
TWI450898B (zh) 2008-07-04 2014-09-01 Sigma Tau Res Switzerland Sa 具有抗腫瘤活性之芳基異唑化合物
EP2303881A2 (en) 2008-07-14 2011-04-06 Gilead Sciences, Inc. Fused heterocyclyc inhibitors of histone deacetylase and/or cyclin-dependent kinases
WO2010017047A1 (en) 2008-08-05 2010-02-11 Merck & Co., Inc. Therapeutic compounds
EP2350053B1 (en) 2008-10-17 2013-12-11 Whitehead Institute For Biomedical Research Modulators of MTOR Complexes
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
EP2361254A1 (en) 2008-12-05 2011-08-31 ArQule, Inc. Raf inhibitors and their uses
WO2010075542A1 (en) 2008-12-23 2010-07-01 Curis, Inc. Cdk inhibitors
WO2010092962A1 (ja) 2009-02-12 2010-08-19 アステラス製薬株式会社 へテロ環誘導体
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
US20120178758A1 (en) 2009-06-09 2012-07-12 California Capital Equity, Llc Styryl-triazine derivatives and their therapeutical applications
EP2440058A4 (en) 2009-06-12 2012-11-21 Dana Farber Cancer Inst Inc MELTED HETEROCYCLIC COMPOUNDS AND APPLICATIONS THEREOF
FR2948367A1 (fr) 2009-07-24 2011-01-28 Centre Nat Rech Scient Derives d'acyl-guanidines modulateurs de la voie de signalisation des proteines hedgehog
EP2488526B1 (en) 2009-10-14 2013-07-24 Bristol-Myers Squibb Company Compounds for the treatment of hepatitis c
WO2011079231A1 (en) * 2009-12-23 2011-06-30 Gatekeeper Pharmaceutical, Inc. Compounds that modulate egfr activity and methods for treating or preventing conditions therewith
CA2784807C (en) 2009-12-29 2021-12-14 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
AU2011227643A1 (en) 2010-03-16 2012-09-20 Dana-Farber Cancer Institute, Inc. Indazole compounds and their uses
BR122014024883A2 (pt) 2010-05-14 2019-08-20 Dana-Farber Cancer Institute, Inc. Compostos no tratamento de neoplasia
UY33539A (es) 2010-08-02 2012-02-29 Astrazeneca Ab Compuestos químicos alk
CN102408408A (zh) 2010-09-20 2012-04-11 北大方正集团有限公司 具有抗肿瘤作用的芳基脲衍生物
CN102406644A (zh) 2010-09-20 2012-04-11 北大方正集团有限公司 芳基脲衍生物用于制备治疗移植排斥药物的新用途
CN102406646B (zh) 2010-09-20 2015-09-09 北大方正集团有限公司 芳基脲衍生物用于制备治疗移植排斥药物的用途
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
JP2014521623A (ja) 2011-07-28 2014-08-28 セルゾーム リミティッド Ｊａｋ阻害剤としてのヘテロシクリルピリミジンアナログ
WO2013040436A2 (en) 2011-09-16 2013-03-21 The Regents Of The University Of Michgian Esx-mediated transcription modulators and related methods
ES2575710T3 (es) * 2011-09-22 2016-06-30 Pfizer Inc Derivados de pirrolopirimidina y purina
ES2616242T3 (es) 2011-09-28 2017-06-12 Euro-Celtique S.A. Derivados de mostaza de nitrógeno
WO2013074986A1 (en) 2011-11-17 2013-05-23 Dana-Farber Cancer Institute, Inc. Inhibitors of c-jun-n-terminal kinase (jnk)
HK1203927A1 (en) * 2012-01-13 2015-11-06 Acea Biosciences, Inc. Heterocyclic compounds and uses as anticancer agents
GB201204384D0 (en) 2012-03-13 2012-04-25 Univ Dundee Anti-flammatory agents
US9879003B2 (en) 2012-04-11 2018-01-30 Dana-Farber Cancer Institute, Inc. Host targeted inhibitors of dengue virus and other viruses
ES2776365T3 (es) 2012-07-09 2020-07-30 Novartis Ag Biomarcadores asociados con inhibidores de CDK
WO2014015523A1 (en) * 2012-07-27 2014-01-30 Hutchison Medipharma Limited Novel heteroaryl and heterocycle compounds, compositions and methods
EP2909194A1 (en) * 2012-10-18 2015-08-26 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
USRE48175E1 (en) 2012-10-19 2020-08-25 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
WO2014063054A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Bone marrow on x chromosome kinase (bmx) inhibitors and uses thereof
CN103319483B (zh) 2012-10-19 2016-08-03 药源药物化学（上海）有限公司 一种利拉列汀重要中间体的制备方法
PL2935248T3 (pl) 2012-12-21 2018-07-31 Plexxikon Inc Związki i sposoby modulacji kinaz i wskazania dla nich
TW201444821A (zh) 2013-03-13 2014-12-01 Janssen Pharmaceutica Nv 經取代之哌啶化合物及其作為食慾素受體調節劑之用途
KR20150133172A (ko) * 2013-03-15 2015-11-27 셀진 아빌로믹스 리서치, 인코포레이티드 Mk2 억제제 및 이의 용도
JP2016519674A (ja) 2013-03-20 2016-07-07 バイエル・ファルマ・アクティエンゲゼルシャフト 過剰増殖障害を治療または予防するための３−アセチルアミノ−１−（フェニル−ヘテロアリール−アミノカルボニルまたはフェニル−ヘテロアリール−カルボニルアミノ）ベンゼン誘導体
US9938279B2 (en) * 2013-04-09 2018-04-10 Energenesis Biomedical Co., Ltd Method for treating disease or condition susceptible to amelioration by AMPK activators and compounds of formula which are useful to activate AMP-activated protein kinase (AMPK)
CN103242341B (zh) 2013-04-19 2015-12-09 中国科学院广州生物医药与健康研究院 噻吩并2，4取代嘧啶类化合物及其药物组合物与应用
CN104177363B (zh) 2013-05-24 2018-06-05 江苏先声药业有限公司 双环杂环胺类Hedgehog信号通路抑制剂
CN117486865A (zh) * 2013-07-11 2024-02-02 艾森医药公司 嘧啶衍生物作为激酶抑制剂
EP3024327B1 (en) 2013-07-25 2019-09-04 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
US10047070B2 (en) 2013-10-18 2018-08-14 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7)
ES2676734T3 (es) 2013-10-18 2018-07-24 Syros Pharmaceuticals, Inc. Compuestos heteroatómicos útiles para el tratamiento de enfermedades proliferativas
USRE50030E1 (en) 2013-12-13 2024-07-02 Dana-Farber Cancer Institute, Inc. Methods to treat lymphoplasmacytic lymphoma
WO2015117083A1 (en) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Diazepane derivatives and uses thereof
WO2015117055A1 (en) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Dihydropteridinone derivatives and uses thereof
WO2015117087A1 (en) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Uses of diazepane derivatives
RU2016134947A (ru) 2014-01-31 2018-03-01 Дана-Фарбер Кансер Институт, Инк. Производные диаминопиримидин бензолсульфона и их применение
CN104860941B (zh) 2014-02-25 2017-03-22 上海海雁医药科技有限公司 2,4‑二取代苯‑1,5‑二胺衍生物及其应用以及由其制备的药物组合物和药用组合物
SG11201608242XA (en) 2014-04-04 2016-10-28 Syros Pharmaceuticals Inc Inhibitors of cyclin-dependent kinase 7 (cdk7)
WO2015154022A1 (en) 2014-04-05 2015-10-08 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
WO2015164614A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
WO2015164604A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged janus kinase inhibitors and uses thereof
CN104829610B (zh) 2014-06-20 2017-03-15 中国科学院合肥物质科学研究院 一种新型布鲁顿酪氨酸激酶抑制剂
CA2954187C (en) 2014-07-21 2022-08-16 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
EP3191469B1 (en) 2014-07-24 2021-12-15 Beta Pharma, Inc. 2-h-indazole derivatives as cyclin-dependent kinase (cdk) inhibitors and therapeutic uses thereof
EP3536323A1 (en) 2014-08-08 2019-09-11 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)
AU2015337607B2 (en) 2014-10-31 2020-04-09 Ube Corporation Substituted dihydropyrrolopyrazole compound
EP3236959B1 (en) 2014-12-23 2025-09-24 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
EP3253764B1 (en) 2015-02-05 2021-06-09 Merck Patent GmbH Macrocyclic compounds as irak1/4 inhibitors and uses thereof
EP3268000B1 (en) 2015-03-09 2021-08-04 Aurigene Discovery Technologies Limited Pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives as cdk inhibitors
WO2016160617A2 (en) 2015-03-27 2016-10-06 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
AU2016276963C1 (en) 2015-06-12 2021-08-05 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
US10695346B2 (en) 2015-06-26 2020-06-30 Dana-Farber Cancer Institute, Inc. 4,6-pyrimidinylene derivatives and uses thereof
HK1254469A1 (zh) 2015-06-26 2019-07-19 Dana Farber Cancer Institute, Inc. 稠合双环嘧啶衍生物及其用途
ES2761885T3 (es) 2015-08-28 2020-05-21 Novartis Ag Combinaciones farmacéuticas que comprenden (a) el inhibidor de la cinasa dependiente de ciclina 4/6 (CDK4/6) LEE011 (= ribociclib) y (b) el inhibidor del receptor del factor de crecimiento epidérmico (EGFR) erlotinib, para el tratamiento o la prevención del cáncer
JP7028766B2 (ja) 2015-09-09 2022-03-02 ダナ－ファーバー キャンサー インスティテュート， インコーポレイテッド サイクリン依存性キナーゼの阻害剤
WO2017160717A2 (en) 2016-03-15 2017-09-21 Memorial Sloan Kettering Cancer Center Method of treating diseases using kinase modulators
US11306070B2 (en) 2016-11-22 2022-04-19 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 12 (CDK12) and uses thereof
CA3043222A1 (en) 2016-11-28 2018-05-31 Dana-Farber Cancer Institute, Inc. Reagents and methods for analysis of proteins and metabolites targeted by covalent probes
CN107235906B (zh) 2017-06-28 2020-05-01 郑州大学第一附属医院 一组吡唑酰胺类衍生物及其应用
CN107686477B (zh) 2017-09-30 2020-01-31 武汉九州钰民医药科技有限公司 作为cdk4/6抑制剂的新型化合物及其应用
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
JP7530297B2 (ja) 2018-11-14 2024-08-07 Ｕｂｅ株式会社 ジヒドロピロロピラゾール誘導体
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
EP3902542A4 (en) 2018-12-28 2022-09-07 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 and uses thereof
US12365696B2 (en) 2019-05-10 2025-07-22 Dana-Farber Cancer Institute, Inc. Small-molecule focal adhesion kinase (FAK) inhibitors
CA3147106A1 (en) 2019-07-23 2021-01-28 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 and uses thereof
AU2020324408A1 (en) 2019-08-05 2021-12-16 Dana-Farber Cancer Institute, Inc. Degraders of cyclin-dependent kinase 7 (CDK7) and uses thereof
AU2020414418A1 (en) 2019-12-24 2022-07-21 Dana-Farber Cancer Institute, Inc. The combination of cyclin dependent kinase 7 inhibitor and immunotherapy for treatment of cancer

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