SG179172A1 - Protein kinase conjugates and inhibitors - Google Patents

Protein kinase conjugates and inhibitors

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Publication number
SG179172A1
SG179172A1 SG2012018545A SG2012018545A SG179172A1 SG 179172 A1 SG179172 A1 SG 179172A1 SG 2012018545 A SG2012018545 A SG 2012018545A SG 2012018545 A SG2012018545 A SG 2012018545A SG 179172 A1 SG179172 A1 SG 179172A1
Authority
SG
Singapore
Prior art keywords
protein kinase
inhibitors
irreversibly
conjugates
protein
Prior art date
Application number
SG2012018545A
Other languages
English (en)
Inventor
Juswinder Singh
Russell Colyn Petter
Deqiang Niu
Lixin Qiao
Arthur Kluge
Roy Lobb
Shomir Ghosh
Zhendong Zhu
Original Assignee
Avila Therapeutics 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43759252&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=SG179172(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Avila Therapeutics Inc filed Critical Avila Therapeutics Inc
Publication of SG179172A1 publication Critical patent/SG179172A1/en

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    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
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    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
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    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
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Families Citing this family (83)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2529621B1 (en) 2006-09-22 2016-10-05 Pharmacyclics LLC Inhibitors of bruton's tyrosine kinase
US20120101114A1 (en) 2007-03-28 2012-04-26 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
WO2009143389A1 (en) 2008-05-21 2009-11-26 Ariad Pharmaceuticals, Inc. Phosphorous derivatives as kinase inhibitors
EP3311818A3 (en) 2008-07-16 2018-07-18 Pharmacyclics, LLC Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors
MX2011002484A (es) * 2008-09-05 2011-09-26 Avila Therapeutics Inc Algoritmo para diseñar inhibidores irreversibles.
NZ620174A (en) 2009-09-16 2016-08-26 Celgene Avilomics Res Inc Protein kinase conjugates and inhibitors
WO2011060321A1 (en) 2009-11-16 2011-05-19 Chdi, Inc. Transglutaminase tg2 inhibitors, pharmaceutical compositions, and methods of use thereof
EP2519664A4 (en) 2009-12-30 2014-03-12 Avila Therapeutics Inc LIGAND-RELATED COVALENTS MODIFYING A PROTEIN
EA031737B1 (ru) 2010-06-03 2019-02-28 Фармасайкликс, Инк. Применение ингибиторов тирозинкиназы брутона (btk) для лечения лейкоза и лимфомы
AU2011260323A1 (en) * 2010-06-04 2012-11-15 F. Hoffmann-La Roche Ag Aminopyrimidine derivatives as LRRK2 modulators
DK2638031T3 (en) 2010-11-10 2017-12-11 Genentech Inc PYRAZOLAMINOPYRIMIDINE DERIVATIVES AS LRRK2 MODULATORS
CN103501612B (zh) 2011-05-04 2017-03-29 阿里亚德医药股份有限公司 抑制表皮生长因子受体导致的癌症中细胞增殖的化合物
US8889716B2 (en) 2011-05-10 2014-11-18 Chdi Foundation, Inc. Transglutaminase TG2 inhibitors, pharmaceutical compositions, and methods of use thereof
WO2013009827A1 (en) * 2011-07-13 2013-01-17 Tempero Pharmaceuticals, Inc. Methods of treatment
WO2013009830A1 (en) * 2011-07-13 2013-01-17 Tempero Pharmaceuticals, Inc. Methods of treatment
WO2013009810A1 (en) * 2011-07-13 2013-01-17 Tempero Pharmaceuticals, Inc. Methods of treatment
WO2013009812A1 (en) * 2011-07-13 2013-01-17 Tempero Pharmaceuticals, Inc Methods of treatment
ME02887B (me) 2011-07-27 2018-04-20 Astrazeneca Ab 2-(2,4,5-supstituisani-anilino) pirimidinski derivati kao egfr modulatori korisni za tretman raka
EP3569598A1 (en) 2011-11-17 2019-11-20 Dana Farber Cancer Institute, Inc. Inhibitors of c-jun-n-terminal kinase (jnk)
AR089182A1 (es) * 2011-11-29 2014-08-06 Hoffmann La Roche Derivados de aminopirimidina como moduladores de lrrk2
HUE036582T2 (hu) * 2012-04-17 2018-07-30 Fujifilm Corp Nitrogéntartalmú heterociklusos vegyület vagy annak sója
JP6469567B2 (ja) 2012-05-05 2019-02-13 アリアド・ファーマシューティカルズ・インコーポレイテッド Ｅｇｆｒ発動性がんの細胞増殖阻害用化合物
US9296753B2 (en) 2012-06-04 2016-03-29 Pharmacyclics Llc Crystalline forms of a Bruton's tyrosine kinase inhibitor
RU2679130C2 (ru) * 2012-07-11 2019-02-06 Блюпринт Медсинс Корпорейшн Ингибиторы рецептора фактора роста фибробластов
EP3550031A1 (en) 2012-07-24 2019-10-09 Pharmacyclics, LLC Mutations associated with resistance to inhibitors of bruton's tyrosine kinase (btk)
BR112015011171A2 (pt) 2012-11-15 2017-07-11 Pharmacyclics Inc compostos de pirrolopirimidina como inibidores da quinase
JP6433974B2 (ja) 2013-03-14 2018-12-05 トレロ ファーマシューティカルズ， インコーポレイテッド Ｊａｋ２およびａｌｋ２阻害剤およびその使用方法
SG11201507478VA (en) 2013-03-15 2015-10-29 Celgene Avilomics Res Inc Heteroaryl compounds and uses thereof
AR095464A1 (es) 2013-03-15 2015-10-21 Celgene Avilomics Res Inc Compuestos de heteroarilo y usos de los mismos
MY181020A (en) 2013-03-15 2020-12-16 Sanofi Sa Heteroaryl compounds and uses thereof
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
EP3027192A4 (en) 2013-08-02 2017-03-22 Pharmacyclics, LLC Methods for the treatment of solid tumors
US9415050B2 (en) 2013-08-12 2016-08-16 Pharmacyclics Llc Methods for the treatment of HER2 amplified cancer
EP3044338B1 (en) 2013-09-12 2021-11-24 Dana-Farber Cancer Institute, Inc. Methods for evaluating and treating waldenstrom's macroglobulinemia
EP3060560A1 (en) 2013-10-25 2016-08-31 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor
US9695165B2 (en) 2014-01-15 2017-07-04 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor
EP3119910A4 (en) 2014-03-20 2018-02-21 Pharmacyclics LLC Phospholipase c gamma 2 and resistance associated mutations
RS58175B1 (sr) * 2014-04-04 2019-03-29 Syros Pharmaceuticals Inc Inhibitori ciklin-zavisne kinaze 7 (cdk7)
EP3174539A4 (en) 2014-08-01 2017-12-13 Pharmacyclics, LLC Inhibitors of bruton's tyrosine kinase
AU2015300798A1 (en) 2014-08-07 2017-02-02 Pharmacyclics Llc Novel formulations of a Bruton's tyrosine kinase inhibitor
IL315294A (en) 2015-03-03 2024-10-01 Pharmacyclics Llc Pharmaceutical formulations of bruton's tyrosine kinase inhibitor
SI3303334T1 (sl) 2015-06-03 2021-09-30 Principia Biopharma Inc. Zaviralci tirozin kinaz
WO2017100715A1 (en) 2015-12-09 2017-06-15 The Board Of Trustees Of The University Of Illinois Benzothiophene-based selective estrogen receptor downregulator compounds
WO2017197055A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Heterocyclic degronimers for target protein degradation
CN109790143A (zh) 2016-05-10 2019-05-21 C4医药公司 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体
EP3454862B1 (en) 2016-05-10 2024-09-11 C4 Therapeutics, Inc. Spirocyclic degronimers for target protein degradation
US11285218B2 (en) 2016-06-23 2022-03-29 Dana-Farber Cancer Institute, Inc. Degradation of bromodomain-containing protein 9 (BRD9) by conjugation of BRD9 inhibitors with E3 ligase ligand and methods of use
WO2018005860A1 (en) 2016-07-01 2018-01-04 G1 Therapeutics, Inc. Pyrimidine-based antiproliferative agents
WO2018049233A1 (en) 2016-09-08 2018-03-15 Nicolas Stransky Inhibitors of the fibroblast growth factor receptor in combination with cyclin-dependent kinase inhibitors
WO2018187294A1 (en) * 2017-04-03 2018-10-11 Asana Biosciences, Llc Pyrimido-pyridazinone compound combinations, methods, kits and formulations thereof
CN110769822A (zh) 2017-06-20 2020-02-07 C4医药公司 用于蛋白降解的n/o-连接的降解决定子和降解决定子体
MX392531B (es) 2017-06-29 2025-03-24 G1 Therapeutics Inc Formas morficas de g1t38 y metodos de preparacion de las mismas.
CN110691775B (zh) * 2017-08-04 2021-04-23 上海和誉生物医药科技有限公司 一种具有fgfr4抑制活性的醛基吡啶衍生物、其制备方法和应用
WO2019191112A1 (en) 2018-03-26 2019-10-03 C4 Therapeutics, Inc. Cereblon binders for the degradation of ikaros
IL259810A (en) * 2018-06-04 2018-07-31 Yeda Res & Dev Mitogen-activated protein kinase kinase 7 inhibitors
AU2019310590A1 (en) 2018-07-26 2021-01-14 Sumitomo Pharma Oncology, Inc. Methods for treating diseases associated with abnormal acvr1 expression and acvr1 inhibitors for use in the same
KR102328682B1 (ko) 2018-08-27 2021-11-18 주식회사 대웅제약 신규한 헤테로사이클릭아민 유도체 및 이를 포함하는 약학 조성물
WO2020045941A1 (ko) * 2018-08-27 2020-03-05 주식회사 대웅제약 신규한 헤테로사이클릭아민 유도체 및 이를 포함하는 약학 조성물
WO2020051235A1 (en) 2018-09-04 2020-03-12 C4 Therapeutics, Inc. Compounds for the degradation of brd9 or mth1
EP3876939A4 (en) 2018-11-07 2022-08-10 Dana-Farber Cancer Institute, Inc. Benzothiazole derivatives and 7-aza-benzothiazole derivatives as janus kinase 2 inhibitors and uses thereof
CN120698985A (zh) 2018-12-20 2025-09-26 C4医药公司 靶向蛋白降解
US20230065740A1 (en) 2018-12-28 2023-03-02 Spv Therapeutics Inc. Cyclin-dependent kinase inhibitors
AU2020250832A1 (en) 2019-03-29 2021-11-11 Astrazeneca Ab Osimertinib for use in the treatment of non-small cell lung cancer
EA202192738A1 (ru) 2019-04-12 2022-03-17 С4 Терапьютикс, Инк. Трициклические соединения, обеспечивающие разрушение белка ikaros и белка aiolos
US20220288069A1 (en) * 2019-07-19 2022-09-15 Bridgene Biosciences, Inc. Inhibitors of tyrosine kinase
CN114901277B (zh) 2019-12-20 2024-05-17 C4医药公司 用于egfr降解的异吲哚啉酮和吲唑化合物
MX2022010952A (es) 2020-03-05 2022-10-07 C4 Therapeutics Inc Compuestos para la degradacion dirigida de brd9.
US11691963B2 (en) 2020-05-06 2023-07-04 Ajax Therapeutics, Inc. 6-heteroaryloxy benzimidazoles and azabenzimidazoles as JAK2 inhibitors
MX2022014573A (es) 2020-05-19 2022-12-15 G1 Therapeutics Inc Compuestos inhibidores de cinasa dependiente de ciclina para el tratamiento de trastornos medicos.
WO2022032026A1 (en) 2020-08-05 2022-02-10 C4 Therapeutics, Inc. Compounds for targeted degradation of ret
US20250171423A1 (en) 2020-09-23 2025-05-29 Achillion Pharmaceuticals, Inc. Pharmaceutical compounds for the treatment of complement mediated disorders
TW202241889A (zh) 2020-12-23 2022-11-01 美商雅捷可斯治療公司 作為ｊａｋ２抑制劑之６－雜芳基氧基苯并咪唑及氮雜苯并咪唑
AU2022290851A1 (en) 2021-06-08 2023-11-23 C4 Therapeutics, Inc. Therapeutics for the degradation of mutant braf
US12162881B2 (en) 2021-11-09 2024-12-10 Ajax Therapeutics, Inc. Forms and compositions of inhibitors of JAK2
AU2022388555A1 (en) 2021-11-09 2024-05-02 Ajax Therapeutics, Inc. 6-he tero aryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors
WO2023107705A1 (en) 2021-12-10 2023-06-15 Incyte Corporation Bicyclic amines as cdk12 inhibitors
TW202345806A (zh) 2022-03-31 2023-12-01 美商艾伯維有限公司 噻唑并〔５，４－ｂ〕吡啶ｍａｌｔ－１抑制劑
CN119998285A (zh) 2022-08-03 2025-05-13 百时美施贵宝公司 用于调控ret蛋白的化合物
CN120569388A (zh) 2022-11-04 2025-08-29 百时美施贵宝公司 Ret-ldd蛋白降解剂
CN120530116A (zh) 2022-11-04 2025-08-22 百时美施贵宝公司 Ret-ldd蛋白抑制剂
WO2025006753A2 (en) 2023-06-30 2025-01-02 Merck Patent Gmbh Heterobifunctional compounds for the degradation of kras protein
CN118766549A (zh) * 2024-06-24 2024-10-15 重庆医科大学附属第一医院 脊柱转移性肿瘤微创切吸治疗系统

Family Cites Families (104)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3710795A (en) 1970-09-29 1973-01-16 Alza Corp Drug-delivery device with stretched, rate-controlling membrane
US4709016A (en) 1982-02-01 1987-11-24 Northeastern University Molecular analytical release tags and their use in chemical analysis
US5516931A (en) 1982-02-01 1996-05-14 Northeastern University Release tag compounds producing ketone signal groups
US4650750A (en) 1982-02-01 1987-03-17 Giese Roger W Method of chemical analysis employing molecular release tag compounds
US5650270A (en) 1982-02-01 1997-07-22 Northeastern University Molecular analytical release tags and their use in chemical analysis
US5262564A (en) 1992-10-30 1993-11-16 Octamer, Inc. Sulfinic acid adducts of organo nitroso compounds useful as retroviral inactivating agents anti-retroviral agents and anti-tumor agents
US5856116A (en) 1994-06-17 1999-01-05 Vertex Pharmaceuticals, Incorporated Crystal structure and mutants of interleukin-1 beta converting enzyme
US5756466A (en) 1994-06-17 1998-05-26 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1β converting enzyme
US5760041A (en) 1996-02-05 1998-06-02 American Cyanamid Company 4-aminoquinazoline EGFR Inhibitors
EA001595B1 (ru) 1996-04-12 2001-06-25 Варнер-Ламберт Компани Необратимые ингибиторы тирозинкиназ
US6686350B1 (en) 1996-07-25 2004-02-03 Biogen, Inc. Cell adhesion inhibitors
DE69737769T2 (de) 1996-07-25 2008-05-15 Biogen Idec Ma Inc., Cambridge Molekülmodell für vla-4-inhibitoren
ATE290545T1 (de) 1996-12-06 2005-03-15 Vertex Pharma Inhibitoren des interleukin-1beta konvertierenden enzyms
US6002008A (en) 1997-04-03 1999-12-14 American Cyanamid Company Substituted 3-cyano quinolines
ZA986732B (en) 1997-07-29 1999-02-02 Warner Lambert Co Irreversible inhibitiors of tyrosine kinases
US6251912B1 (en) 1997-08-01 2001-06-26 American Cyanamid Company Substituted quinazoline derivatives
US6162613A (en) 1998-02-18 2000-12-19 Vertex Pharmaceuticals, Inc. Methods for designing inhibitors of serine/threonine-kinases and tyrosine kinases
US7383135B1 (en) 1998-05-04 2008-06-03 Vertex Pharmaceuticals Incorporated Methods of designing inhibitors for JNK kinases
US6335155B1 (en) 1998-06-26 2002-01-01 Sunesis Pharmaceuticals, Inc. Methods for rapidly identifying small organic molecule ligands for binding to biological target molecules
US6919178B2 (en) 2000-11-21 2005-07-19 Sunesis Pharmaceuticals, Inc. Extended tethering approach for rapid identification of ligands
CA2343934A1 (en) * 1998-09-25 2000-04-06 The Children's Medical Center Corporation Short peptides which selectively modulate the activity of protein kinases
US6288082B1 (en) 1998-09-29 2001-09-11 American Cyanamid Company Substituted 3-cyanoquinolines
PT1131304E (pt) 1998-11-19 2003-04-30 Warner Lambert Co N-¬4-(3-cloro-4-fluoro-fenilamino)-7-(3-morfolin-4-il-propoxi)-quinazolin-6-il|-acrilamida um inibidor irreversivel de tirosino quinases
US6569876B1 (en) 1999-06-17 2003-05-27 John C. Cheronis Method and structure for inhibiting activity of serine elastases
US6420364B1 (en) 1999-09-13 2002-07-16 Boehringer Ingelheim Pharmaceuticals, Inc. Compound useful as reversible inhibitors of cysteine proteases
WO2001056557A2 (en) 2000-02-05 2001-08-09 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of erk
US6384051B1 (en) 2000-03-13 2002-05-07 American Cyanamid Company Method of treating or inhibiting colonic polyps
US6667300B2 (en) 2000-04-25 2003-12-23 Icos Corporation Inhibitors of human phosphatidylinositol 3-kinase delta
US7427689B2 (en) 2000-07-28 2008-09-23 Georgetown University ErbB-2 selective small molecule kinase inhibitors
CA2418389A1 (en) 2000-08-11 2002-02-21 Vertex Pharmaceuticals Incorporated Pyridine derivatives as inhibitors of p38
WO2002068415A1 (en) 2000-12-21 2002-09-06 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US7235576B1 (en) 2001-01-12 2007-06-26 Bayer Pharmaceuticals Corporation Omega-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
IL144583A0 (en) * 2001-07-26 2002-05-23 Peptor Ltd Chimeric protein kinase inhibitors
JP4391237B2 (ja) 2001-11-21 2009-12-24 サネシス ファーマシューティカルズ， インコーポレイテッド リガンド発見のための方法
AU2002224970A1 (en) 2001-12-07 2003-06-17 Discovision Associates A solid state microoptical electromechanical system (moens) for reading a photonics diffractive memory
WO2003064406A1 (en) 2002-01-07 2003-08-07 Sequoia Pharmaceuticals Resistance-repellent retroviral protease inhibitors
CA2478981A1 (en) 2002-03-21 2003-10-02 Sunesis Pharmaceuticals, Inc. Identification of kinase inhibitors
GB0213186D0 (en) 2002-06-08 2002-07-17 Univ Dundee Methods
MY141867A (en) 2002-06-20 2010-07-16 Vertex Pharma Substituted pyrimidines useful as protein kinase inhibitors
EP1375517A1 (en) 2002-06-21 2004-01-02 Smithkline Beecham Corporation Structure of a glucocorticoid receptor ligand binding domain comprising an expanded binding pocket and methods employing same
GB0221169D0 (en) 2002-09-12 2002-10-23 Univ Bath Crystal
BR0316680A (pt) 2002-11-28 2005-10-18 Schering Ag Pirimidinas inibidoras de chk, pdk e akt, sua produção e uso como agentes farmacêuticos
PE20040945A1 (es) 2003-02-05 2004-12-14 Warner Lambert Co Preparacion de quinazolinas substituidas
US20050026172A1 (en) * 2003-02-11 2005-02-03 Immusol, Inc. siRNA libraries optimized for predetermined protein families
EP1603879A2 (en) 2003-02-28 2005-12-14 Bayer Pharmaceuticals Corporation Substituted pyridine derivatives useful in the treatment of cancer and other disorders
US7557129B2 (en) 2003-02-28 2009-07-07 Bayer Healthcare Llc Cyanopyridine derivatives useful in the treatment of cancer and other disorders
WO2004078746A2 (en) 2003-02-28 2004-09-16 Bayer Pharmaceuticals Corporation 2-oxo-1,3,5-perhydrotriazapine derivatives useful in the treatment of hyper-proliferative, angiogenesis, and inflammatrory disorders
CA2520392C (en) 2003-03-26 2014-08-12 Sudhir Paul Covalent attachment of ligands to nucleophilic proteins guided by non-covalent binding
US8748601B2 (en) 2003-04-11 2014-06-10 The Regents Of The University Of California Selective serine/threonine kinase inhibitors
US7687506B2 (en) 2003-04-11 2010-03-30 The Regents Of The University Of California Selective serine/threonine kinase inhibitors
EP1626714B1 (en) 2003-05-20 2007-07-04 Bayer Pharmaceuticals Corporation Diaryl ureas for diseases mediated by pdgfr
MXPA06001110A (es) 2003-08-01 2006-04-11 Wyeth Corp Uso de una combinacion de un inhibidor de la cinasa del receptor del factor de crecimiento epidermico y agentes citotoxicos para el tratamiento e inhibicion del cancer.
GB0321710D0 (en) 2003-09-16 2003-10-15 Novartis Ag Organic compounds
CA2539064A1 (en) * 2003-09-17 2005-04-21 Sunesis Pharmaceuticals, Inc. Identification of kinase inhibitors
WO2005043118A2 (en) 2003-10-27 2005-05-12 Vertex Pharmaceuticals Incorporated Drug discovery method
CA2553874A1 (en) 2004-01-16 2005-08-04 The Regents Of The University Of Michigan Conformationally constrained smac mimetics and the uses thereof
BRPI0507198A (pt) * 2004-01-30 2007-06-26 Merck Patent Gmbh derivados de bisariluréia
US20070299092A1 (en) 2004-05-20 2007-12-27 Wyeth Quinone Substituted Quinazoline and Quinoline Kinase Inhibitors
WO2005114219A2 (en) 2004-05-20 2005-12-01 Wyeth Assays to identify irreversibly binding inhibitors of receptor tyrosine kinases
US7521457B2 (en) 2004-08-20 2009-04-21 Boehringer Ingelheim International Gmbh Pyrimidines as PLK inhibitors
WO2006036941A2 (en) 2004-09-27 2006-04-06 Kosan Biosciences Incorporated Specific kinase inhibitors
AU2005293839B2 (en) 2004-10-13 2012-08-23 Merck Patent Gmbh Heterocyclic substituted bisarylurea derivatives as kinase inhibitors
CN113952459B (zh) 2005-02-03 2025-02-11 综合医院公司 治疗吉非替尼耐药性癌症的方法
JP2008536847A (ja) 2005-04-14 2008-09-11 ワイス ゲフィニチブ耐性患者における上皮増殖因子レセプター（ｅｇｆｒ）キナーゼインヒビターの使用
AR053602A1 (es) 2005-05-03 2007-05-09 Smithkline Beecham Corp Compuesto de 2- arilamino -4-oxo-1,3-tiazol-5(4h)- substituido, composicion farmaceutica que lo comprende, proceso para prepararla y uso del compuesto para preparar un medicamento
GB0509224D0 (en) 2005-05-05 2005-06-15 Chroma Therapeutics Ltd Inhibitors of intracellular enzymatic activity
EP1964578A3 (en) 2005-05-05 2008-11-05 Chroma Therapeutics Limited Alpha aminoacid ester-drug conjugates hydrolysable by carboxylesterase
KR20080012902A (ko) 2005-05-27 2008-02-12 바이엘 헬스케어 아게 질병을 치료하기 위한 디아릴 우레아를 포함하는 병용요법
MX362412B (es) 2005-11-01 2019-01-15 Targegen Inc Inhibidores de biaril meta-pirimidina de cinasas.
WO2007056163A2 (en) 2005-11-03 2007-05-18 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
WO2007062459A1 (en) 2005-11-29 2007-06-07 Cytopia Research Pty Ltd Selective kinase inhibitors based on pyridine scaffold
WO2007120339A1 (en) 2005-12-19 2007-10-25 Genentech, Inc. Pyrimidine kinase inhibitors
TW200736232A (en) 2006-01-26 2007-10-01 Astrazeneca Ab Pyrimidine derivatives
JP5232769B2 (ja) 2006-04-07 2013-07-10 モドプロ アーベー Ｃ−反応性タンパク質についての結合剤
CN101054380B (zh) 2006-04-13 2011-07-20 沈阳药科大学 用作细胞周期依赖性蛋白激酶抑制剂的吡唑并嘧啶类衍生物
US7601852B2 (en) 2006-05-11 2009-10-13 Kosan Biosciences Incorporated Macrocyclic kinase inhibitors
CA2651732C (en) * 2006-05-18 2014-10-14 Mannkind Corporation Intracellular kinase inhibitors
PE20121506A1 (es) * 2006-07-14 2012-11-26 Amgen Inc Compuestos triazolopiridinas como inhibidores de c-met
US8217177B2 (en) * 2006-07-14 2012-07-10 Amgen Inc. Fused heterocyclic derivatives and methods of use
US8198448B2 (en) * 2006-07-14 2012-06-12 Amgen Inc. Fused heterocyclic derivatives and methods of use
EP2529621B1 (en) 2006-09-22 2016-10-05 Pharmacyclics LLC Inhibitors of bruton's tyrosine kinase
CA2673125C (en) 2006-10-19 2015-04-21 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
PT2091918E (pt) 2006-12-08 2014-11-24 Irm Llc Compostos e composições como inibidores de proteína cinase
EP2099771A1 (en) 2006-12-19 2009-09-16 Genentech, Inc. Pyrimidine kinase inhibitors
PT2114900T (pt) 2007-01-31 2019-01-17 Ym Biosciences Australia Pty Compostos à base de tiopirimidina e as suas utilizações
PE20090717A1 (es) 2007-05-18 2009-07-18 Smithkline Beecham Corp Derivados de quinolina como inhibidores de la pi3 quinasa
EP2152079A4 (en) 2007-06-04 2011-03-09 Avila Therapeutics Inc HETEROCYCLIC COMPOUNDS AND USES THEREOF
WO2009030890A1 (en) 2007-09-03 2009-03-12 University Court Of The University Of Dundee Pyrimidine compounds for the treatment of cancer, septic shock and/or primary open angle glaucoma
TWI475996B (zh) 2007-10-19 2015-03-11 Celgene Avilomics Res Inc 雜芳基化合物及其用途
US7989465B2 (en) 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
TW201546079A (zh) 2007-12-21 2015-12-16 Celgene Avilomics Res Inc Ｈｃｖ蛋白酶抑制劑及其用途（一）
US8309685B2 (en) 2007-12-21 2012-11-13 Celgene Avilomics Research, Inc. HCV protease inhibitors and uses thereof
US8293705B2 (en) 2007-12-21 2012-10-23 Avila Therapeutics, Inc. HCV protease inhibitors and uses thereof
WO2009082697A1 (en) 2007-12-21 2009-07-02 Avila Therapeutics, Inc. Hcv protease inhibitors and uses thereof
US8859572B2 (en) 2008-01-14 2014-10-14 Bayer Intellectual Property Gmbh Sulfone substituted 2,3-dihydroimidazo [1,2-C] quinazoline derivatives useful for treating hyper-proliferative disorders and diseases with angiogenesis
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
US8450335B2 (en) 2008-06-27 2013-05-28 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
US8188137B2 (en) 2008-08-15 2012-05-29 Avila Therapeutics, Inc. HCV protease inhibitors and uses thereof
MX2011002484A (es) 2008-09-05 2011-09-26 Avila Therapeutics Inc Algoritmo para diseñar inhibidores irreversibles.
US8603737B2 (en) 2008-09-19 2013-12-10 Celgene Avilomics Research, Inc. Methods for identifying HCV protease inhibitors
CN102625708A (zh) 2009-09-09 2012-08-01 阿维拉制药公司 Pi3激酶抑制剂及其用途
NZ620174A (en) 2009-09-16 2016-08-26 Celgene Avilomics Res Inc Protein kinase conjugates and inhibitors
EP2519664A4 (en) 2009-12-30 2014-03-12 Avila Therapeutics Inc LIGAND-RELATED COVALENTS MODIFYING A PROTEIN
JP6068340B2 (ja) 2010-08-10 2017-01-25 セルジーン アヴィロミクス リサーチ， インコーポレイテッド Ｂｔｋ阻害剤のベシル酸塩

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