IN2012DN02534A - - Google Patents

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IN2012DN02534A
IN2012DN02534A IN2534DEN2012A IN2012DN02534A IN 2012DN02534 A IN2012DN02534 A IN 2012DN02534A IN 2534DEN2012 A IN2534DEN2012 A IN 2534DEN2012A IN 2012DN02534 A IN2012DN02534 A IN 2012DN02534A
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India
Prior art keywords
irreversibly
protein
relates
cysteine residue
protein kinase
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English (en)
Inventor
Singh Juswinder
Colyn Petter Russel
Niu Deqiang
Qiao Lixin
Kluge Arthur
Lobb Roy
Ghosh Shomir
Zhu Zhendong
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Avila Therapeutics Inc
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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=IN2012DN02534(A) "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 IN2012DN02534A publication Critical patent/IN2012DN02534A/en

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    • C07D487/04Ortho-condensed systems
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    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
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    • C07D213/04Heterocyclic 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
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Families Citing this family (70)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL2529621T3 (pl) 2006-09-22 2017-06-30 Pharmacyclics Llc Inhibitory kinazy tyrozynowej brutona
US8809273B2 (en) 2007-03-28 2014-08-19 Pharmacyclics, Inc. Inhibitors of Bruton's tyrosine kinase
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
EA029131B1 (ru) 2008-05-21 2018-02-28 Ариад Фармасьютикалз, Инк. Фосфорсодержащие производные в качестве ингибиторов киназы
CN102159214A (zh) 2008-07-16 2011-08-17 药品循环公司 用于实体肿瘤的治疗的布鲁顿酪氨酸激酶的抑制剂
CN102405284B (zh) * 2008-09-05 2016-01-20 新基阿维罗米克斯研究公司 设计不可逆抑制剂的算法
CN105063001A (zh) 2009-09-16 2015-11-18 新基阿维罗米克斯研究公司 蛋白激酶复合物和含有该复合物的药物组合物以及它们的用途
US8946197B2 (en) 2009-11-16 2015-02-03 Chdi Foundation, Inc. Transglutaminase TG2 inhibitors, pharmaceutical compositions, and methods of use thereof
CN102812167A (zh) 2009-12-30 2012-12-05 阿维拉制药公司 蛋白的配体-介导的共价修饰
AU2011261185A1 (en) 2010-06-03 2013-01-10 Pharmacyclics, Inc. The use of inhibitors of Bruton's tyrosine kinase (Btk)
RS54865B1 (sr) 2010-06-04 2016-10-31 Hoffmann La Roche Derivati aminopirimidina kao modulatori lrrk2
SG189043A1 (en) 2010-11-10 2013-05-31 Hoffmann La Roche Pyrazole aminopyrimidine derivatives as lrrk2 modulators
US9834518B2 (en) 2011-05-04 2017-12-05 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in EGFR-driven cancers
US8889716B2 (en) 2011-05-10 2014-11-18 Chdi Foundation, Inc. Transglutaminase TG2 inhibitors, pharmaceutical compositions, and methods of use thereof
WO2013009812A1 (en) * 2011-07-13 2013-01-17 Tempero Pharmaceuticals, Inc Methods of treatment
WO2013009827A1 (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
WO2013009830A1 (en) * 2011-07-13 2013-01-17 Tempero Pharmaceuticals, Inc. Methods of treatment
ME02382B (me) 2011-07-27 2016-06-20 Astrazeneca Ab 2-(2,4,5-supstituisani-anilino) piramidisnki derivati kao egfr modulatori korisni za tretman raka
US9382239B2 (en) 2011-11-17 2016-07-05 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
JP5736507B2 (ja) * 2012-04-17 2015-06-17 富士フイルム株式会社 含窒素複素環化合物またはその塩
WO2013169401A1 (en) 2012-05-05 2013-11-14 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
CA3218491A1 (en) 2012-06-04 2013-12-12 Pharmacyclics Llc Crystalline forms of a bruton's tyrosine kinase inhibitor
AU2013290074A1 (en) 2012-07-11 2015-01-29 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor
KR20180088926A (ko) 2012-07-24 2018-08-07 파마싸이클릭스 엘엘씨 브루톤 티로신 키나제(btk)의 억제제에 대한 내성과 관련된 돌연변이
JP2015537033A (ja) 2012-11-15 2015-12-24 ファーマサイクリックス,インク. キナーゼ阻害剤としてのピロロピリミジン化合物
DK2970205T3 (da) 2013-03-14 2019-07-29 Tolero Pharmaceuticals Inc JAK2- og ALK2-inhibitorer og fremgangsmåder til anvendelse deraf
KR102350704B1 (ko) 2013-03-15 2022-01-13 셀젠 카르 엘엘씨 헤테로아릴 화합물 및 이의 용도
TWI647220B (zh) 2013-03-15 2019-01-11 美商西建卡爾有限責任公司 雜芳基化合物及其用途
EP2968337B1 (en) * 2013-03-15 2021-07-21 Celgene CAR LLC 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
TWI649081B (zh) 2013-08-02 2019-02-01 製藥公司 治療固態腫瘤之方法
WO2015023703A1 (en) 2013-08-12 2015-02-19 Pharmacyclics, Inc. 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
RS63405B1 (sr) 2013-10-25 2022-08-31 Blueprint Medicines Corp Inhibitori receptora faktora rasta fibroblasta
US9695165B2 (en) 2014-01-15 2017-07-04 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor
CA2942528A1 (en) 2014-03-20 2015-09-24 Pharmacyclics Inc. Phospholipase c gamma 2 and resistance associated mutations
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
EP3174539A4 (en) 2014-08-01 2017-12-13 Pharmacyclics, LLC Inhibitors of bruton's tyrosine kinase
CN106573002A (zh) 2014-08-07 2017-04-19 药品循环有限责任公司 布鲁顿氏酪氨酸激酶抑制剂的新型制剂
IL315294A (en) 2015-03-03 2024-10-01 Pharmacyclics Llc Pharmaceutical formulations of proton tyrosine kinase inhibitor
CA2987335A1 (en) 2015-06-03 2016-12-08 David Goldstein Bruton tyrosine kinase inhibitors
AU2016366680B2 (en) 2015-12-09 2021-06-24 The Board Of Trustees Of The University Of Illinois Benzothiophene-based selective estrogen receptor downregulators
WO2017197055A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Heterocyclic degronimers for target protein degradation
EP3454862B1 (en) 2016-05-10 2024-09-11 C4 Therapeutics, Inc. Spirocyclic degronimers for target protein degradation
AU2017281903B2 (en) 2016-06-23 2020-12-24 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
AU2017290748A1 (en) 2016-07-01 2019-01-17 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
FI3645001T3 (fi) 2017-06-29 2024-09-25 G1 Therapeutics Inc Git38:n morfisia muotoja ja niiden valmistusmenetelmiä
WO2019024876A1 (zh) * 2017-08-04 2019-02-07 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
JP2021519337A (ja) 2018-03-26 2021-08-10 シー4 セラピューティクス, インコーポレイテッド Ikarosの分解のためのセレブロン結合剤
IL259810A (en) * 2018-06-04 2018-07-31 Yeda Res & Dev Mitogen-activated protein kinase kinase 7 inhibitors
US11040038B2 (en) 2018-07-26 2021-06-22 Sumitomo Dainippon 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
CN113453679A (zh) 2018-12-20 2021-09-28 C4医药公司 靶向蛋白降解
US20220288069A1 (en) * 2019-07-19 2022-09-15 Bridgene Biosciences, Inc. Inhibitors of tyrosine kinase
AU2020405237A1 (en) 2019-12-20 2022-07-07 C4 Therapeutics, Inc. Isoindolinone and indazole compounds for the degradation of EGFR
BR112022017393A2 (pt) 2020-03-05 2022-10-18 C4 Therapeutics Inc Composto, composição farmacêutica, método para tratar um transtorno mediado por brd9, e, uso de um composto
JP2023525047A (ja) 2020-05-06 2023-06-14 エイジャックス セラピューティクス, インコーポレイテッド Jak2阻害薬としての6-ヘテロアリールオキシベンゾイミダゾール及びアザベンゾイミダゾール
US12043632B2 (en) 2020-12-23 2024-07-23 Ajax Therapeutics, Inc. 6-heteroaryloxy benzimidazoles and azabenzimidazoles as JAK2 inhibitors
EP4430042A1 (en) 2021-11-09 2024-09-18 Ajax Therapeutics, Inc. 6-he tero aryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors
US12084453B2 (en) 2021-12-10 2024-09-10 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
WO2024030968A1 (en) 2022-08-03 2024-02-08 Brystol-Myers Squibb Company Compounds for modulating ret protein
WO2024097980A1 (en) 2022-11-04 2024-05-10 Bristol-Myers Squibb Company Ret-ldd protein inhibitors
WO2024097989A1 (en) 2022-11-04 2024-05-10 Bristol-Myers Squibb Company Ret-ldd protein degraders

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
US5650270A (en) 1982-02-01 1997-07-22 Northeastern University Molecular analytical release tags and their use in chemical analysis
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
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
US5756466A (en) * 1994-06-17 1998-05-26 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1β converting enzyme
US5856116A (en) * 1994-06-17 1999-01-05 Vertex Pharmaceuticals, Incorporated Crystal structure and mutants of interleukin-1 beta converting enzyme
US5760041A (en) * 1996-02-05 1998-06-02 American Cyanamid Company 4-aminoquinazoline EGFR Inhibitors
RO121900B1 (ro) 1996-04-12 2008-07-30 Warner-Lambert Company Compuşi inhibitori, ireversibili, ai tirozin kinazelor, compoziţie farmaceutică care îi conţine şi utilizarea acestora
CA2261974A1 (en) * 1996-07-25 1998-02-05 Biogen, Inc. Molecular model for vla-4 inhibitors
US6686350B1 (en) * 1996-07-25 2004-02-03 Biogen, Inc. Cell adhesion inhibitors
WO1998024805A1 (en) 1996-12-06 1998-06-11 Vertex Pharmaceuticals Incorporated INHIBITORS OF INTERLEUKIN-1β CONVERTING ENZYME
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
US6919178B2 (en) 2000-11-21 2005-07-19 Sunesis Pharmaceuticals, Inc. Extended tethering approach for rapid identification of ligands
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
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
HUP0104211A3 (en) 1998-11-19 2003-01-28 Warner Lambert Co N-[4-(3-chloro-4-fluoro-phenylamino)-7-(3-morpholin-4-yl-propoxy)-quinazolin-6-yl]-acrylamide, an irreversible inhibitor of tyrosine kinases and pharmaceutical composition containing it
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
AU2001236720A1 (en) * 2000-02-05 2001-08-14 Bemis, Guy 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
MXPA03001256A (es) 2000-08-11 2004-12-06 Vertex Pharma Inhibidores de p38.
JP4160395B2 (ja) 2000-12-21 2008-10-01 バーテックス ファーマシューティカルズ インコーポレイテッド プロテインキナーゼインヒビターとして有用なピラゾール化合物
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
EP1456840B1 (en) 2001-12-07 2008-02-20 Research Investment Network, Inc A solid state microoptical electromechanical system (moems) for reading a photonics diffractive memory
EP1472536A4 (en) 2002-01-07 2007-02-14 Sequoia Pharmaceuticals VERSATILE INHIBITORS
AU2003228345B2 (en) * 2002-03-21 2009-02-05 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
AU2003288198A1 (en) 2002-11-28 2004-06-18 Schering Aktiengesellschaft CHK-,PDK- and AKT-inhibitory pyrimidines, their production and use as pharmaceutical agents
PE20040945A1 (es) 2003-02-05 2004-12-14 Warner Lambert Co Preparacion de quinazolinas substituidas
AU2004210972A1 (en) * 2003-02-11 2004-08-26 Immusol Incorporated siRNA libraries optimized for predetermined protein families
JP4594925B2 (ja) 2003-02-28 2010-12-08 ニッポネックス インコーポレイテッド 増殖亢進性、血管新生性及び炎症性疾患の治療に有用な2−オキソ−1,3,5−パーヒドロトリアザピン誘導体
JP4927533B2 (ja) 2003-02-28 2012-05-09 ニッポネックス インコーポレイテッド 癌その他の疾患の治療に有用な置換ピリジン誘導体
US7557129B2 (en) * 2003-02-28 2009-07-07 Bayer Healthcare Llc Cyanopyridine derivatives useful in the treatment of cancer and other disorders
JP5503837B2 (ja) * 2003-03-26 2014-05-28 ポール,サッドヒル 非共有結合により誘導される求核性タンパク質へのリガンドの共有結合
US8748601B2 (en) 2003-04-11 2014-06-10 The Regents Of The University Of California Selective serine/threonine kinase inhibitors
WO2005000197A2 (en) 2003-04-11 2005-01-06 The Regents Of The University Of California Selective serine/threonine kinase inhibitors
JP2007511203A (ja) 2003-05-20 2007-05-10 バイエル、ファーマシューテイカルズ、コーポレイション キナーゼ阻害活性を有するジアリール尿素
EP1648516A2 (en) * 2003-08-01 2006-04-26 Wyeth Holdings Corporation Use of combination of an epidermal growth factor receptor kinase inhibitor and cytotoxic agents for treatment and inhibition of cancer
GB0321710D0 (en) 2003-09-16 2003-10-15 Novartis Ag Organic compounds
WO2005034840A2 (en) * 2003-09-17 2005-04-21 Sunesis Pharmaceuticals, Inc. Identification of kinase inhibitors
US8187874B2 (en) * 2003-10-27 2012-05-29 Vertex Pharmaceuticals Incorporated Drug discovery method
WO2005069894A2 (en) 2004-01-16 2005-08-04 The Regents Of The University Of Michigan Conformationally constrained smac mimetics and the uses thereof
US20070161677A1 (en) * 2004-01-30 2007-07-12 Merck Patent Gmbh Bisarylurea derivatives
WO2005114219A2 (en) 2004-05-20 2005-12-01 Wyeth Assays to identify irreversibly binding inhibitors of receptor tyrosine kinases
WO2005115145A2 (en) * 2004-05-20 2005-12-08 Wyeth Quinone substituted quinazoline and quinoline kinase inhibitors
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
CA2584185C (en) 2004-10-13 2014-07-15 Frank Stieber Heterocyclic substituted bisarylurea derivates as kinase inhibitors
CN113975393A (zh) 2005-02-03 2022-01-28 综合医院公司 治疗吉非替尼耐药性癌症的方法
KR20080002826A (ko) * 2005-04-14 2008-01-04 와이어쓰 게피티니브 내성 환자에서의 표피 성장 인자 수용체(egfr) 키나제 억제제의 용도
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
JP2008545670A (ja) 2005-05-27 2008-12-18 バイエル・ヘルスケア・アクチェンゲゼルシャフト 疾患を処置するためのジアリールウレア類を含む組合せ治療
MY167260A (en) 2005-11-01 2018-08-14 Targegen Inc Bi-aryl meta-pyrimidine inhibitors of kinases
JP5249771B2 (ja) 2005-11-03 2013-07-31 バーテックス ファーマシューティカルズ インコーポレイテッド キナーゼインヒビターとして有用なアミノピリミジン
WO2007062459A1 (en) 2005-11-29 2007-06-07 Cytopia Research Pty Ltd Selective kinase inhibitors based on pyridine scaffold
JP2009520038A (ja) 2005-12-19 2009-05-21 ジェネンテック・インコーポレーテッド ピリミジンキナーゼインヒビター
TW200736232A (en) 2006-01-26 2007-10-01 Astrazeneca Ab Pyrimidine derivatives
CA2647271A1 (en) * 2006-04-07 2007-10-18 Modpro Ab Binder for c-reactive protein
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
AU2007254179B2 (en) * 2006-05-18 2013-03-21 Pharmacyclics Llc Intracellular kinase inhibitors
PE20080403A1 (es) * 2006-07-14 2008-04-25 Amgen Inc Derivados heterociclicos fusionados y metodos de uso
US8198448B2 (en) * 2006-07-14 2012-06-12 Amgen Inc. Fused heterocyclic derivatives and methods of use
US8217177B2 (en) * 2006-07-14 2012-07-10 Amgen Inc. Fused heterocyclic derivatives and methods of use
PL2529621T3 (pl) 2006-09-22 2017-06-30 Pharmacyclics Llc Inhibitory kinazy tyrozynowej brutona
CA2673125C (en) 2006-10-19 2015-04-21 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
EP2091918B1 (en) 2006-12-08 2014-08-27 Irm Llc Compounds and compositions as protein kinase inhibitors
EP2099771A1 (en) 2006-12-19 2009-09-16 Genentech, Inc. Pyrimidine kinase inhibitors
EP2114900B1 (en) 2007-01-31 2018-10-10 YM BioSciences Australia Pty Ltd Thiopyrimidine-based compounds and uses thereof
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
US7982036B2 (en) 2007-10-19 2011-07-19 Avila Therapeutics, Inc. 4,6-disubstitued pyrimidines useful as kinase inhibitors
US7989465B2 (en) 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
AU2008340257B2 (en) 2007-12-21 2015-06-11 Celgene Avilomics Research, Inc. HCV protease inhibitors and uses thereof
NZ586232A (en) 2007-12-21 2012-12-21 Avila Therapeutics Inc HCV protease inhibitors comprising a functionalised proline derivative
US8293705B2 (en) 2007-12-21 2012-10-23 Avila Therapeutics, Inc. HCV protease inhibitors and uses thereof
US8309685B2 (en) 2007-12-21 2012-11-13 Celgene Avilomics Research, Inc. HCV protease inhibitors and uses thereof
EP2244721A4 (en) 2008-01-14 2017-01-18 Bayer Intellectual Property GmbH Sulfone substituted 2,3-dihydroimidazo ý1,2-c¨quinazoline derivatives useful for treating hyper-proliferative disorders and diseases with angiogenesis
MX2010014029A (es) 2008-06-27 2011-01-21 Avila Therapeutics Inc Compuestos de heteroarilo y usos de los mismos.
US8338439B2 (en) 2008-06-27 2012-12-25 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
CN102405284B (zh) 2008-09-05 2016-01-20 新基阿维罗米克斯研究公司 设计不可逆抑制剂的算法
US8603737B2 (en) 2008-09-19 2013-12-10 Celgene Avilomics Research, Inc. Methods for identifying HCV protease inhibitors
MX339584B (es) 2009-09-09 2016-06-01 Avila Therapeutics Inc Inhibidores de pi3 cinasa y usos de los mismos.
CN105063001A (zh) 2009-09-16 2015-11-18 新基阿维罗米克斯研究公司 蛋白激酶复合物和含有该复合物的药物组合物以及它们的用途
CN102812167A (zh) 2009-12-30 2012-12-05 阿维拉制药公司 蛋白的配体-介导的共价修饰
MX336875B (es) 2010-08-10 2016-02-04 Celgene Avilomics Res Inc Sal de besilato de un inhibidor de tirosina cinasa de bruton (btk).

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