CN103153994B - 双环杂芳基激酶抑制剂及使用方法 - Google Patents

双环杂芳基激酶抑制剂及使用方法 Download PDF

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CN103153994B
CN103153994B CN201180036376.2A CN201180036376A CN103153994B CN 103153994 B CN103153994 B CN 103153994B CN 201180036376 A CN201180036376 A CN 201180036376A CN 103153994 B CN103153994 B CN 103153994B
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phenyl
pyrrolo
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optionally substituted
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CN103153994A (zh
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H.A.杰尔巴德
S.久赫斯特
V.S.古德菲洛
T.维曼
S.B.拉乌拉
C.J.罗思
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University of Rochester
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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CN201180036376.2A 2010-05-24 2011-05-24 双环杂芳基激酶抑制剂及使用方法 Active CN103153994B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US34769410P 2010-05-24 2010-05-24
US61/347,694 2010-05-24
US61/347694 2010-05-24
PCT/US2011/037758 WO2011149950A2 (en) 2010-05-24 2011-05-24 Bicyclic heteroaryl kinase inhibitors and methods of use

Publications (2)

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CN103153994A CN103153994A (zh) 2013-06-12
CN103153994B true CN103153994B (zh) 2016-02-10

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US (1) US8846909B2 (https=)
EP (1) EP2576549A4 (https=)
JP (1) JP6086326B2 (https=)
CN (1) CN103153994B (https=)
AU (1) AU2011258465B2 (https=)
CA (1) CA2800176C (https=)
NZ (1) NZ603644A (https=)
WO (1) WO2011149950A2 (https=)

Families Citing this family (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010068483A2 (en) 2008-11-25 2010-06-17 University Of Rochester Mlk inhibitors and methods of use
JP6086326B2 (ja) 2010-05-24 2017-03-01 ユニヴァーシティー オブ ロチェスター 二環式ヘテロアリールキナーゼ阻害剤および使用方法
EP2588455B1 (en) 2010-07-02 2018-04-04 Gilead Sciences, Inc. 2-quinolinyl-acetic acid derivatives as hiv antiviral compounds
MX2012015097A (es) 2010-07-02 2013-05-28 Gilead Sciences Inc Derivados de acido naft-2-ilacetico para tratar sida.
DE102011009961A1 (de) * 2011-02-01 2012-08-02 Merck Patent Gmbh 7-Azaindolderivate
UA111841C2 (uk) 2011-04-21 2016-06-24 Гіліад Сайєнсіз, Інк. Сполуки бензотіазолу та їх фармацевтичне застосування
WO2013042139A1 (en) 2011-09-23 2013-03-28 Advinus Therapeutics Limited Amide compounds, compositions and applications thereof
US9376392B2 (en) 2012-01-04 2016-06-28 Gilead Sciences, Inc. 2-(tert-butoxy)-2-(7-methylquinolin-6-yl) acetic acid derivatives for treating AIDS
US9284323B2 (en) 2012-01-04 2016-03-15 Gilead Sciences, Inc. Naphthalene acetic acid derivatives against HIV infection
CN102627646A (zh) * 2012-03-19 2012-08-08 苏州四同医药科技有限公司 一种3-碘-5-溴-4,7-二氮杂吲哚的制备方法
UY34750A (es) 2012-04-20 2013-11-29 Gilead Sciences Inc ?compuestos para el tratamiento del hiv, composiciones,métodos de preparación, intermediarios y métodos terapéuticos?.
KR102091895B1 (ko) * 2012-05-03 2020-04-14 제넨테크, 인크. 파킨슨병의 치료에 사용하기 위한 lrrk2 조절제로서의 피라졸 아미노피리미딘 유도체
MX2015004615A (es) * 2012-10-16 2015-07-17 Hoffmann La Roche Inhibidores de serina/treonina cinasa.
CN104884059B (zh) 2012-11-30 2018-08-10 罗切斯特大学 用于hiv/aids治疗的混合谱系激酶抑制剂
FR2999575A1 (fr) * 2012-12-18 2014-06-20 Centre Nat Rech Scient 3,5-diaryl-azaindoles comme inhibiteurs de la proteine dyrk1a pour le traitement des deficiences cognitives liees au syndrome de down et a la maladie d'alzheimer
JP6199991B2 (ja) 2013-01-18 2017-09-20 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ ３置換ピラゾール及びｄｌｋ阻害剤としての使用
AR096151A1 (es) 2013-05-01 2015-12-09 Hoffmann La Roche Compuestos de biheteroarilo y usos de los mismos
MX2016008110A (es) 2013-12-20 2016-08-19 Hoffmann La Roche Derivados de pirazol como inhibidores de la cinasa de cremallera de leucina dual (dlk) y usos de los mismos.
CN104478909B (zh) * 2014-11-19 2017-01-04 上海泰坦科技股份有限公司 杂环硼酸类化合物的合成工艺
GB201509893D0 (en) * 2015-06-08 2015-07-22 Ucb Biopharma Sprl Therapeutic agents
EP3383875B1 (en) * 2015-11-30 2022-02-09 Council Of Scientific & Industrial Research 3-pyrimidinyl pyrrolo [2,3-b] pyridine as anticancer agents and the process for the preparation thereof
CN105859761B (zh) * 2016-04-26 2018-06-26 丽水学院 一种芳香硼酸酯化合物合成方法
PL3558321T3 (pl) * 2016-12-23 2023-10-23 Felicitex Therapeutics, Inc. Pochodne chinolin jako inhibitory kinaz dyrk1a i/lub dyrk1b
EP3759072A4 (en) * 2018-03-01 2021-11-03 The Trustees of Columbia University in the City of New York COMPOUNDS, COMPOSITIONS AND METHODS FOR RELATING TOXIC STRESS FROM ENDOPLASMIC RETICULUM
CN113015526A (zh) 2018-09-19 2021-06-22 豪夫迈·罗氏有限公司 螺环2,3-二氢-7-氮杂吲哚化合物及其用途
WO2020103896A1 (en) * 2018-11-22 2020-05-28 Beigene, Ltd. Pyrrolo[2,3-b]pyridines as hpk1 inhibitor and uses thereof
TWI848141B (zh) 2019-07-04 2024-07-11 英屬開曼群島商百濟神州有限公司 及其用途
US12459958B2 (en) 2019-07-17 2025-11-04 Beone Medicines I Gmbh Tricyclic compounds as HPK1 inhibitor and the use thereof
US11560366B2 (en) * 2019-10-21 2023-01-24 Board Of Regents, The University Of Texas System Bicyclo[1.1.1]pentane inhibitors of dual leucine zipper (DLK) kinase for the treatment of disease
WO2022216845A1 (en) * 2021-04-06 2022-10-13 Perceive Biotherapeutics, Inc. Gene therapy for hearing loss
JP7607799B2 (ja) * 2021-04-27 2024-12-27 メッドシャイン ディスカバリー インコーポレイテッド ６員芳香族ヘテロ尿素環の誘導体及びその使用
WO2022243649A1 (fr) * 2021-05-21 2022-11-24 Centre National De La Recherche Scientifique (Cnrs) Nouveaux derives azaindole en tant qu'agents anticancereux
WO2022243650A1 (fr) * 2021-05-21 2022-11-24 Centre National De La Recherche Scientifique (Cnrs) Nouveaux derives azaindole en tant qu'agents antiviraux
US20240425499A1 (en) * 2021-10-11 2024-12-26 Halia Therapeutics, Inc. Tyro3 inhibitors
US11479541B1 (en) 2022-01-31 2022-10-25 Pioneura Corporation Acid addition salts, compositions, and methods of treating thereof
US11661409B1 (en) * 2022-01-31 2023-05-30 Pioneura Corporation Acid addition salts, compositions, and methods of treating
CN118126036A (zh) * 2022-12-01 2024-06-04 复旦大学 7-氮杂吲哚类化合物及其制备方法和应用
WO2025229111A1 (en) 2024-05-01 2025-11-06 Basf Se Pyrimidinone derivatives as pesticidal compounds

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1665809A (zh) * 2001-06-21 2005-09-07 艾文蒂斯药品有限公司 氮杂吲哚
CN101939324A (zh) * 2008-02-25 2011-01-05 霍夫曼-拉罗奇有限公司 吡咯并吡嗪激酶抑制剂

Family Cites Families (66)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4933438A (en) 1984-02-29 1990-06-12 University Of Florida Brain-specific analogues of centrally acting amines
US6150354A (en) 1987-01-15 2000-11-21 Bonnie Davis Compounds for the treatment of Alzheimer's disease
US5133974A (en) 1989-05-05 1992-07-28 Kv Pharmaceutical Company Extended release pharmaceutical formulations
WO1992020327A1 (en) 1991-05-14 1992-11-26 Ernir Snorrason Treatment of fatigue syndrome with cholinesterase inhibitors
IT1250421B (it) 1991-05-30 1995-04-07 Recordati Chem Pharm Composizione farmaceutica a rilascio controllato con proprieta' bio-adesive.
US6537579B1 (en) 1993-02-22 2003-03-25 American Bioscience, Inc. Compositions and methods for administration of pharmacologically active compounds
FR2710265B1 (fr) 1993-09-22 1995-10-20 Adir Composition pharmaceutique bioadhésive pour la libération contrôlée de principes actifs.
US5618819A (en) 1994-07-07 1997-04-08 Adir Et Compagnie 1,3-dihydro-2H-pyrrolo[2,3-b]pyridin-2-one and oxazolo[4,5-b]pyridin-2-(3H)-one compounds
US6548084B2 (en) 1995-07-20 2003-04-15 Smithkline Beecham Plc Controlled release compositions
US6245347B1 (en) 1995-07-28 2001-06-12 Zars, Inc. Methods and apparatus for improved administration of pharmaceutically active compounds
DE19541260A1 (de) 1995-11-06 1997-05-07 Lohmann Therapie Syst Lts Therapeutische Zubereitung zur transdermalen Applikation von Wirkstoffen durch die Haut
US6512010B1 (en) 1996-07-15 2003-01-28 Alza Corporation Formulations for the administration of fluoxetine
CN1277550A (zh) 1997-09-11 2000-12-20 尼科梅德丹麦有限公司 非甾体抗炎药物(NSAIDs)的改进释放的复合型组合物
US6624200B2 (en) 1998-08-25 2003-09-23 Columbia Laboratories, Inc. Bioadhesive progressive hydration tablets
GB9721437D0 (en) 1997-10-10 1997-12-10 Glaxo Group Ltd Heteroaromatic compounds and their use in medicine
US6607751B1 (en) 1997-10-10 2003-08-19 Intellipharamaceutics Corp. Controlled release delivery device for pharmaceutical agents incorporating microbial polysaccharide gum
US6403597B1 (en) 1997-10-28 2002-06-11 Vivus, Inc. Administration of phosphodiesterase inhibitors for the treatment of premature ejaculation
US6248864B1 (en) 1997-12-31 2001-06-19 Adherex Technologies, Inc. Compounds and methods and modulating tissue permeability
US6613358B2 (en) 1998-03-18 2003-09-02 Theodore W. Randolph Sustained-release composition including amorphous polymer
US6312717B1 (en) 1998-07-07 2001-11-06 Bristol-Myers Squibb Company Method for treatment of anxiety and depression
US20020009478A1 (en) 1998-08-24 2002-01-24 Douglas Joseph Dobrozsi Oral liquid mucoadhesive compositions
SE9802864D0 (sv) 1998-08-27 1998-08-27 Pharmacia & Upjohn Ab Transdermally administered tolterodine as antimuscarinic agent for the treatment of overactive bladder
EP1121104B1 (en) 1998-10-01 2005-01-12 Novartis AG New controlled release oral formulations for rivastigmine
US6248363B1 (en) 1999-11-23 2001-06-19 Lipocine, Inc. Solid carriers for improved delivery of active ingredients in pharmaceutical compositions
GB9904995D0 (en) 1999-03-04 1999-04-28 Glaxo Group Ltd Substituted aza-oxindole derivatives
US6498176B1 (en) 1999-03-04 2002-12-24 Smithklinebeecham Corporation 3-(anilinomethylene) oxindoles as protein tyrosine kinase and protein serine/threonine kinase inhibitors
GB9904933D0 (en) 1999-03-04 1999-04-28 Glaxo Group Ltd Compounds
US6624171B1 (en) 1999-03-04 2003-09-23 Smithkline Beecham Corporation Substituted aza-oxindole derivatives
FR2792527B1 (fr) 1999-04-22 2004-08-13 Ethypharm Lab Prod Ethiques Microgranules de ketoprofene, procede de preparation et compositions pharmaceutiques
US6541020B1 (en) 1999-07-09 2003-04-01 Trimeris, Inc. Methods and compositions for administration of therapeutic reagents
HUP0203548A3 (en) 1999-07-21 2003-04-28 Astrazeneca Ab New spirooxindole derivatives, process for their preparation, pharmaceutical compositions containing them and their use
US6562375B1 (en) 1999-08-04 2003-05-13 Yamanouchi Pharmaceuticals, Co., Ltd. Stable pharmaceutical composition for oral use
EP1207860B1 (en) 1999-09-02 2007-10-24 Nostrum Pharmaceuticals, Inc. Controlled release pellet formulation
US6544548B1 (en) 1999-09-13 2003-04-08 Keraplast Technologies, Ltd. Keratin-based powders and hydrogel for pharmaceutical applications
US6080736A (en) 1999-10-27 2000-06-27 Janus Pharmaceuticals, Inc. Methods and compositions for treating and preventing anxiety and anxiety disorders using optically pure (R) tofisopam
US6461631B1 (en) 1999-11-16 2002-10-08 Atrix Laboratories, Inc. Biodegradable polymer composition
WO2001047501A1 (en) 1999-12-29 2001-07-05 Nanodelivery, Inc. Drug delivery system exhibiting permeability control
US6589549B2 (en) 2000-04-27 2003-07-08 Macromed, Incorporated Bioactive agent delivering system comprised of microparticles within a biodegradable to improve release profiles
US6524621B2 (en) 2000-05-01 2003-02-25 Aeropharm Technology Inc. Core formulation
US6482440B2 (en) 2000-09-21 2002-11-19 Phase 2 Discovery, Inc. Long acting antidepressant microparticles
US6524615B2 (en) 2001-02-21 2003-02-25 Kos Pharmaceuticals, Incorporated Controlled release pharmaceutical composition
ATE497603T1 (de) 2001-03-02 2011-02-15 Gpc Biotech Ag Drei-hybrid-assaysystem
US20030187026A1 (en) 2001-12-13 2003-10-02 Qun Li Kinase inhibitors
EP2295433A3 (en) 2003-03-06 2011-07-06 Eisai R&D Management Co., Ltd. JNK inhibitors
GB2400101A (en) 2003-03-28 2004-10-06 Biofocus Discovery Ltd Compounds capable of binding to the active site of protein kinases
TWI339206B (en) 2003-09-04 2011-03-21 Vertex Pharma Compositions useful as inhibitors of protein kinases
US20060011139A1 (en) 2004-07-16 2006-01-19 Applied Materials, Inc. Heated substrate support for chemical vapor deposition
WO2006015123A1 (en) 2004-07-27 2006-02-09 Sgx Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
US7626021B2 (en) 2004-07-27 2009-12-01 Sgx Pharmaceuticals, Inc. Fused ring heterocycle kinase modulators
US7361764B2 (en) * 2004-07-27 2008-04-22 Sgx Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
US7709645B2 (en) * 2004-07-27 2010-05-04 Sgx Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
AU2005289644A1 (en) * 2004-09-24 2006-04-06 Janssen Pharmaceutica, N.V. Imidazo{4,5-b}pyrazinone inhibitors of protein kinases
JP4953457B2 (ja) 2004-10-27 2012-06-13 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ プロゲステロン受容体モジュレーターとしてのピリジンイミダゾール及びアザ−インドール
EP1828180A4 (en) 2004-12-08 2010-09-15 Glaxosmithkline Llc 1H-pyrrolo [2,3-BETA] PYRIDINE
MX2007010068A (es) 2005-02-16 2007-10-10 Schering Corp Piperazino-piperidinas con actividad antagonista de cxcr3.
JP2007108926A (ja) 2005-10-12 2007-04-26 Denso Corp 運転支援装置及びプログラム
US7732447B2 (en) 2006-06-22 2010-06-08 Cephalon, Inc. Fused [d]pyridazin-7-ones
PL2069352T3 (pl) 2006-08-02 2014-03-31 Cytokinetics Inc Określone cząstki chemiczne, kompozycje i sposoby
MX337906B (es) * 2006-10-19 2016-03-28 Signal Pharm Llc Compuestos de heteroarilo, composiciones de los mismos, y su uso como inhibidores de proteina cinasas.
GB0706168D0 (en) 2007-03-29 2007-05-09 Glaxo Group Ltd Compounds
MX2009010984A (es) 2007-04-10 2010-01-15 Sgx Pharmaceuticals Inc Moduladores de heterociclo cinasa de anillo fusionado.
ES2441196T3 (es) 2007-04-18 2014-02-03 Kissei Pharmaceutical Co., Ltd. Derivado de anillo condensado nitrogenado, composiciones farmacéuticas que lo contienen, y su uso con fines médicos
EP2211620B1 (en) 2007-10-25 2013-12-25 Merck Sharp & Dohme Corp. 3-PYRAZIN SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AS JANUS KINASE INHIBITORS FOR THE TREATMENT OF CANCER DISEASES
BRPI0917540A2 (pt) 2008-08-05 2015-11-17 Daiichi Sankyo Co Ltd composto, sal farmacologicamente aceitavél, composição farmacêutica, e, uso de um composto ou sal farmacologicamente aceitável
WO2010068483A2 (en) 2008-11-25 2010-06-17 University Of Rochester Mlk inhibitors and methods of use
JP6086326B2 (ja) 2010-05-24 2017-03-01 ユニヴァーシティー オブ ロチェスター 二環式ヘテロアリールキナーゼ阻害剤および使用方法

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1665809A (zh) * 2001-06-21 2005-09-07 艾文蒂斯药品有限公司 氮杂吲哚
CN101939324A (zh) * 2008-02-25 2011-01-05 霍夫曼-拉罗奇有限公司 吡咯并吡嗪激酶抑制剂

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
A novel synthesis of aryl tethered imidazo[4,5-b]pyrazin-2-ones through in situ ring construction and contraction;Vishnu Ji Ram et al;《Tetrahedron Letters》;20070212;第48卷(第7期);第1282页表1化合物4a *

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