NZ603644A - Bicyclic heteroaryl kinase inhibitors and methods of use - Google Patents

Bicyclic heteroaryl kinase inhibitors and methods of use

Info

Publication number
NZ603644A
NZ603644A NZ603644A NZ60364411A NZ603644A NZ 603644 A NZ603644 A NZ 603644A NZ 603644 A NZ603644 A NZ 603644A NZ 60364411 A NZ60364411 A NZ 60364411A NZ 603644 A NZ603644 A NZ 603644A
Authority
NZ
New Zealand
Prior art keywords
methods
mixed lineage
kinases
compounds
disease
Prior art date
Application number
NZ603644A
Other languages
English (en)
Inventor
Colin J Loweth
Torsten Wiemann
Harris A Gelbard
Stephen Dewhurst
Satheesh Babu Ravula
Val S Goodfellow
Original Assignee
Univ Rochester
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Univ Rochester filed Critical Univ Rochester
Publication of NZ603644A publication Critical patent/NZ603644A/en

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A—HUMAN NECESSITIES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Virology (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Vascular Medicine (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Psychology (AREA)
NZ603644A 2010-05-24 2011-05-24 Bicyclic heteroaryl kinase inhibitors and methods of use NZ603644A (en)

Applications Claiming Priority (2)

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

Publications (1)

Publication Number Publication Date
NZ603644A true NZ603644A (en) 2014-10-31

Family

ID=45004716

Family Applications (1)

Application Number Title Priority Date Filing Date
NZ603644A NZ603644A (en) 2010-05-24 2011-05-24 Bicyclic heteroaryl kinase inhibitors and methods of use

Country Status (8)

Country Link
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
CA2744498C (en) 2008-11-25 2017-10-24 University Of Rochester Mlk inhibitors and methods of use
AU2011258465B2 (en) 2010-05-24 2016-12-15 University Of Rochester Bicyclic heteroaryl kinase inhibitors and methods of use
KR20130124291A (ko) 2010-07-02 2013-11-13 길리애드 사이언시즈, 인코포레이티드 Ｈｉｖ 항바이러스 화합물로서의 2-퀴놀리닐-아세트산 유도체
AP2013006706A0 (en) 2010-07-02 2013-02-28 Gilead Sciences Inc Napht-2-ylacetic acid derivatives to treat AIDS
DE102011009961A1 (de) * 2011-02-01 2012-08-02 Merck Patent Gmbh 7-Azaindolderivate
BR112013027096A2 (pt) 2011-04-21 2016-12-27 Gilead Sciences Inc compostos de benzotiazol e seu uso farmacêutico
JP2014527981A (ja) 2011-09-23 2014-10-23 アドヴィナス・セラピューティックス・リミテッド アミド化合物、組成物およびその用途
WO2013103724A1 (en) 2012-01-04 2013-07-11 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
ES2571479T3 (es) 2012-04-20 2016-05-25 Gilead Sciences Inc Derivados del ácido benzotiazol-6-il acético y su uso para tratar una infección por VIH
CN106279202A (zh) * 2012-05-03 2017-01-04 霍夫曼-拉罗奇有限公司 作为lrrk2调节剂用于治疗帕金森病的吡唑氨基嘧啶衍生物
JP2015533151A (ja) * 2012-10-16 2015-11-19 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト セリン／スレオニンキナーゼ阻害剤
EP2925319B1 (en) 2012-11-30 2019-01-09 University Of Rochester Mixed lineage kinase inhibitors for hiv/aids therapies
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
CA2896187A1 (en) 2013-01-18 2014-07-24 F. Hoffmann-La Roche Ag 3-substituted pyrazoles and use as dlk inhibitors
PH12019502378A1 (en) 2013-05-01 2022-05-11 Hoffmann La Roche Biheteroaryl compounds and uses thereof
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
WO2017094026A1 (en) * 2015-11-30 2017-06-08 Council Of Scientific & Industrial Research 3-pyrimidinyl pyrrolo [2,3-b] pyridine as new 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
EP4183786A1 (en) * 2016-12-23 2023-05-24 Felicitex Therapeutics, Inc. Derivatives of quinolines as inhibitors of dyrk1a and/or dyrk1b kinases
WO2019169306A1 (en) 2018-03-01 2019-09-06 The Trustees Of Columbia University In The City Of New York Compounds, compositions, and methods for suppressing toxic endoplasmic reticulum stress
WO2020061377A1 (en) 2018-09-19 2020-03-26 Genentech, Inc. Spirocyclic 2,3-dihydro-7-azaindole compounds and uses thereof
TW202039483A (zh) * 2018-11-22 2020-11-01 英屬開曼群島商百濟神州有限公司 作為HPK1抑制劑的吡咯並[2,3-b]吡啶以及它們的用途
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
TW202116771A (zh) 2019-07-17 2021-05-01 英屬開曼群島商百濟神州有限公司 作為ｈｐｋ１抑制劑之三環化合物及其用途
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
CN117279923B (zh) * 2021-04-27 2025-09-30 南京明德新药研发有限公司 六元杂芳并脲环的衍生物及其应用
US20240293400A1 (en) * 2021-05-21 2024-09-05 Centre National De La Recherche Scientifique Novel azaindole derivatives as antiviral agents
WO2022243649A1 (fr) * 2021-05-21 2022-11-24 Centre National De La Recherche Scientifique (Cnrs) Nouveaux derives azaindole en tant qu'agents anticancereux
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

Family Cites Families (68)

* 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
EP0584185B1 (en) 1991-05-14 1999-08-11 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
CA2301883A1 (en) 1997-09-11 1999-03-18 Nycomed Danmark A/S Modified release multiple-units compositions of non-steroid anti-inflammatory drug substances (nsaids)
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
BR9914251A (pt) 1998-10-01 2001-06-19 Novartis Ag Formulações orais de liberação sustentada
US6248363B1 (en) 1999-11-23 2001-06-19 Lipocine, Inc. Solid carriers for improved delivery of active ingredients in pharmaceutical compositions
GB9904933D0 (en) 1999-03-04 1999-04-28 Glaxo Group Ltd Compounds
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
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
NZ516452A (en) 1999-07-21 2004-06-25 Astrazeneca Ab Spirooxindole Derivatives
US6562375B1 (en) 1999-08-04 2003-05-13 Yamanouchi Pharmaceuticals, Co., Ltd. Stable pharmaceutical composition for oral use
PT1207860E (pt) 1999-09-02 2008-01-24 Nostrum Pharmaceuticals Inc Formulação de peletes de libertação controlada
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
DE60239097D1 (de) 2001-03-02 2011-03-17 Gpc Biotech Ag Drei-hybrid-assaysystem
GB0115109D0 (en) * 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
US20030187026A1 (en) 2001-12-13 2003-10-02 Qun Li Kinase inhibitors
JP4787150B2 (ja) 2003-03-06 2011-10-05 エーザイ・アール・アンド・ディー・マネジメント株式会社 Ｊｎｋ阻害剤
GB2400101A (en) 2003-03-28 2004-10-06 Biofocus Discovery Ltd Compounds capable of binding to the active site of protein kinases
AR045595A1 (es) 2003-09-04 2005-11-02 Vertex Pharma Composiciones utiles como inhibidores de proteinas quinasas
US20060011139A1 (en) 2004-07-16 2006-01-19 Applied Materials, Inc. Heated substrate support for chemical vapor deposition
US7709645B2 (en) * 2004-07-27 2010-05-04 Sgx Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
US7626021B2 (en) * 2004-07-27 2009-12-01 Sgx Pharmaceuticals, Inc. Fused ring heterocycle kinase modulators
EP1781654A1 (en) 2004-07-27 2007-05-09 SGX Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
US7361764B2 (en) * 2004-07-27 2008-04-22 Sgx Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
WO2006036883A2 (en) 2004-09-24 2006-04-06 Janssen Pharmaceutica, N.V. Imidazo{4,5-b}pyrazinone inhibitors of protein kinases
EP1807425B1 (en) 2004-10-27 2014-07-30 Janssen Pharmaceutica NV Pyridine imidazoles and aza-indoles as progesterone receptor modulators
EP1828180A4 (en) * 2004-12-08 2010-09-15 Glaxosmithkline Llc 1H-pyrrolo [2,3-BETA] PYRIDINE
CA2598489A1 (en) 2005-02-16 2006-08-24 Schering Corporation Piperazine-piperidines with cxcr3 antagonist activity
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
ES2558517T3 (es) 2006-08-02 2016-02-04 Cytokinetics, Inc. Ciertas entidades químicas, composiciones y métodos que comprenden imidazopirimidinas
ATE543819T1 (de) * 2006-10-19 2012-02-15 Signal Pharm Llc Heteroarylverbindungen, zusammensetzungen daraus und behandlungsverfahren damit
GB0706168D0 (en) 2007-03-29 2007-05-09 Glaxo Group Ltd Compounds
WO2008124848A1 (en) 2007-04-10 2008-10-16 Sgx Pharmaceuticals, Inc. Fused ring heterocycle kinase modulators
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
US8183245B2 (en) 2007-10-25 2012-05-22 Merck Sharp & Dohme Corp. Pyrazine substituted pyrrolopyridines as inhibitors of JAK and PDK1
JP5368485B2 (ja) * 2008-02-25 2013-12-18 エフ．ホフマン−ラ ロシュ アーゲー ピロロピラジンキナーゼインヒビター
NZ590688A (en) 2008-08-05 2012-09-28 Daiichi Sankyo Co Ltd imidazo[4,5-b]pyridin-2-one derivatives
CA2744498C (en) * 2008-11-25 2017-10-24 University Of Rochester Mlk inhibitors and methods of use
AU2011258465B2 (en) 2010-05-24 2016-12-15 University Of Rochester Bicyclic heteroaryl kinase inhibitors and methods of use

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AU2011258465B2 (en) 2016-12-15
CN103153994B (zh) 2016-02-10
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CA2800176C (en) 2018-08-28
CN103153994A (zh) 2013-06-12
JP2013526609A (ja) 2013-06-24
AU2011258465A1 (en) 2012-12-06
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CA2800176A1 (en) 2011-12-01
US8846909B2 (en) 2014-09-30

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