JP5581219B2 - チオフェンおよびホスファチジルイノシトール３−キナーゼ（ｐｉ３ｋ）阻害薬としてのその使用 - Google Patents

チオフェンおよびホスファチジルイノシトール３−キナーゼ（ｐｉ３ｋ）阻害薬としてのその使用 Download PDF

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Publication number
JP5581219B2
JP5581219B2 JP2010544359A JP2010544359A JP5581219B2 JP 5581219 B2 JP5581219 B2 JP 5581219B2 JP 2010544359 A JP2010544359 A JP 2010544359A JP 2010544359 A JP2010544359 A JP 2010544359A JP 5581219 B2 JP5581219 B2 JP 5581219B2
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membered
nitrogen
sulfur
oxygen
optionally substituted
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JP2011510080A (ja
JP2011510080A5 (https=
Inventor
ロバート ダウンハム，
マシュー オー． ダフィー，
クリステル シー． ルノー，
トリシア ジェイ． ボス，
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Millennium Pharmaceuticals Inc
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Millennium Pharmaceuticals Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur 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
    • C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur 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
    • C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D333/40—Thiophene-2-carboxylic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Transplantation (AREA)
  • Hospice & Palliative Care (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2010544359A 2008-01-25 2009-01-26 チオフェンおよびホスファチジルイノシトール３−キナーゼ（ｐｉ３ｋ）阻害薬としてのその使用 Active JP5581219B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US6243908P 2008-01-25 2008-01-25
US61/062,439 2008-01-25
PCT/US2009/000513 WO2009094224A1 (en) 2008-01-25 2009-01-26 Thiophenes and their use as phosphatidylinositol 3-kinase (pi3k) inhibitors

Publications (3)

Publication Number Publication Date
JP2011510080A JP2011510080A (ja) 2011-03-31
JP2011510080A5 JP2011510080A5 (https=) 2013-03-07
JP5581219B2 true JP5581219B2 (ja) 2014-08-27

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Family Applications (1)

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JP2010544359A Active JP5581219B2 (ja) 2008-01-25 2009-01-26 チオフェンおよびホスファチジルイノシトール３−キナーゼ（ｐｉ３ｋ）阻害薬としてのその使用

Country Status (4)

Country Link
US (1) US9029411B2 (https=)
EP (1) EP2250160B1 (https=)
JP (1) JP5581219B2 (https=)
WO (1) WO2009094224A1 (https=)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9029411B2 (en) 2008-01-25 2015-05-12 Millennium Pharmaceuticals, Inc. Thiophenes and uses thereof
ES2491522T3 (es) 2008-06-19 2014-09-08 Millennium Pharmaceuticals, Inc. Derivados de tiofeno o tiazol y su uso como inhibidores de PI3K
TWI378933B (en) 2008-10-14 2012-12-11 Daiichi Sankyo Co Ltd Morpholinopurine derivatives
US8546405B2 (en) 2008-12-23 2013-10-01 Abbott Laboratories Anti-viral compounds
SG172352A1 (en) 2008-12-23 2011-07-28 Abbott Lab Anti-viral compounds
US8796314B2 (en) 2009-01-30 2014-08-05 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
US9090601B2 (en) 2009-01-30 2015-07-28 Millennium Pharmaceuticals, Inc. Thiazole derivatives
WO2010090716A1 (en) 2009-01-30 2010-08-12 Millennium Pharmaceuticals, Inc. Heteroaryls and their use as pi3k inhibitors
US9278922B2 (en) 2009-04-15 2016-03-08 Abbvie Inc. Anti-viral compounds
US9394279B2 (en) 2009-06-11 2016-07-19 Abbvie Inc. Anti-viral compounds
US8716454B2 (en) 2009-06-11 2014-05-06 Abbvie Inc. Solid compositions
EA020031B1 (ru) 2009-06-11 2014-08-29 Эббви Бахамаз Лтд. Противовирусные соединения
US8937150B2 (en) 2009-06-11 2015-01-20 Abbvie Inc. Anti-viral compounds
MX2012002059A (es) * 2009-08-20 2012-04-19 Karus Therapeutics Ltd Compestos heterociclicos triciclicos como inhibidores de fosfoionositida 3-quinasa.
NZ605440A (en) 2010-06-10 2014-05-30 Abbvie Bahamas Ltd Solid compositions comprising an hcv inhibitor
WO2012021611A1 (en) 2010-08-11 2012-02-16 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
TW201217365A (en) 2010-08-11 2012-05-01 Millennium Pharm Inc Heteroaryls and uses thereof
US8859768B2 (en) 2010-08-11 2014-10-14 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
TW201307309A (zh) 2010-10-13 2013-02-16 Millennium Pharm Inc 雜芳基化合物及其用途
US10201584B1 (en) 2011-05-17 2019-02-12 Abbvie Inc. Compositions and methods for treating HCV
US9034832B2 (en) 2011-12-29 2015-05-19 Abbvie Inc. Solid compositions
HK1201270A1 (en) 2012-01-11 2015-08-28 Bayer Intellectual Property Gmbh Tetrazol-5-yl- and triazol-5-yl-aryl compounds and use thereof as herbicides
US11484534B2 (en) 2013-03-14 2022-11-01 Abbvie Inc. Methods for treating HCV
WO2015103490A1 (en) 2014-01-03 2015-07-09 Abbvie, Inc. Solid antiviral dosage forms
EP3418275B1 (en) * 2016-02-16 2021-03-17 Korea Institute of Science and Technology Novel 2,3,5-substituted thiophene compound as protein kinase inhibitor
ES2946917T3 (es) 2017-07-21 2023-07-27 Antabio Sas Compuestos químicos

Family Cites Families (103)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL242505A (https=) 1958-08-20
US3852293A (en) 1972-06-21 1974-12-03 Uniroyal Inc 4-phenyl-2-(3-pyridyl)-thiazole carboxamides
US3821384A (en) 1972-10-06 1974-06-28 Uniroyal Inc Pharmaceutical compositions containing a4-aryl-2-(3-pyridyl)thiazole and methods of using same
DE3021590A1 (de) 1980-06-09 1981-12-17 Hoechst Ag, 6000 Frankfurt 4-halogen-5-(halogenmethyl-phenyl)-oxazol-derivate, ein verfahren zu ihrer herstellung und sie enthaltenden strahlungsempfindliche massen
DD275870A1 (de) 1988-09-27 1990-02-07 Univ Leipzig Verfahren zur herstellung von in 5-position verschiedenartig substituierten 3-aminothiophen-4-carbonitrilen
PH27357A (en) 1989-09-22 1993-06-21 Fujisawa Pharmaceutical Co Pyrazole derivatives and pharmaceutical compositions comprising the same
AU6966696A (en) 1995-10-05 1997-04-28 Warner-Lambert Company Method for treating and preventing inflammation and atherosclerosis
US6268308B1 (en) 1996-08-27 2001-07-31 Syngenta Crop Protection, Inc. Herbicidal S-substituted 1,2,4,6-thiatriazines
JPH1087490A (ja) 1996-09-10 1998-04-07 Sagami Chem Res Center インターロイキン６生産抑制剤、骨吸収抑制剤、抗骨粗鬆症剤、及びチアゾール化合物
PT853083E (pt) 1997-01-06 2001-12-28 Pfizer Composto de piridilfurano e piridiltiofeno e sua utilizacao farmaceutica
ES2167882T3 (es) 1997-04-24 2002-05-16 Dow Agrosciences Llc 3-(fenil sustituido)-5-(tienil o furil)-1,2,4-triazoles pesticidas.
CA2336848A1 (en) 1998-07-10 2000-01-20 Merck & Co., Inc. Novel angiogenesis inhibitors
DE19858192A1 (de) 1998-12-17 2000-06-21 Aventis Cropscience Gmbh 4-Trifluormethyl-3-oxazolylpyridine, Verfahren zu ihrer Herstellung, sie enthaltende Mittel und ihre Verwendung als Schädlingsbekämpfungsmittel
CO5170501A1 (es) 1999-04-14 2002-06-27 Novartis Ag AZOLES SUSTITUIDOS UTILES PARA EL TRATAMIENTO DE ENFERMEDADES MEDIADAS POR TNFa eIL-1 Y ENFERMEDADES DEL METABOLISMO OSEO
JP2003520233A (ja) 2000-01-18 2003-07-02 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 ジャイレースインヒビターおよびそれらの使用
AU2002338642A1 (en) 2001-04-13 2002-10-28 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
US7074801B1 (en) 2001-04-26 2006-07-11 Eisai Co., Ltd. Nitrogen-containing condensed cyclic compound having a pyrazolyl group as a substituent group and pharmaceutical composition thereof
US7405235B2 (en) 2001-05-04 2008-07-29 Paratek Pharmaceuticals, Inc. Transcription factor modulating compounds and methods of use thereof
ATE325608T1 (de) 2001-08-13 2006-06-15 Janssen Pharmaceutica Nv 2,4,5-trisubstituted thiazolyl derivative und deren antiinflammatorische wirkung
US7375105B2 (en) 2001-09-05 2008-05-20 Smithkline Beecham P.L.C. Pyridine substituted furan derivatives as Raf kinase inhibitors
US20040198773A1 (en) 2001-09-26 2004-10-07 Barry Hart Substituted 3-pyridyl oxazoles as c17,20 lyase inhibitors
EP1432706A2 (en) 2001-09-26 2004-06-30 Bayer Pharmaceuticals Corporation 3-pyridyl or 4-isoquinolinyl thiazoles as c17,20 lyase inhibitors
AU2002359376B2 (en) 2001-11-08 2008-01-10 Elan Pharmaceuticals, Inc. N, N'-substituted-1,3-diamino-2-hydroxypropane derivatives
BR0313160A (pt) 2002-08-08 2005-07-12 Smithkline Beecham Corp Composto, composição farmacêutica, métodos para tratar uma condição e um neoplasmo suscetìvel em um animal em um animal, processo para preparar um composto e uso de um composto
AU2003265395A1 (en) 2002-08-14 2004-03-03 Ppd Discovery, Inc. Prenylation inhibitors and methods of their synthesis and use
WO2004016741A2 (en) 2002-08-14 2004-02-26 Ppd Discovery, Inc. Prenylation inhibitors containing dimethyl-cyclobutane and methods of their synthesis and use
ATE411996T1 (de) 2002-09-30 2008-11-15 Bayer Healthcare Ag Kondensierte azolpyrimidinderivate
AR044519A1 (es) 2003-05-02 2005-09-14 Novartis Ag Derivados de piridin-tiazol amina y de pirimidin-tiazol amina
US7122560B2 (en) 2003-06-18 2006-10-17 Bristol-Myers Squibb Company Lactam derivatives as inhibitors of matrix metalloproteinases and/or TNF-α converting enzyme
US6984652B2 (en) 2003-09-05 2006-01-10 Warner-Lambert Company Llc Gyrase inhibitors
RU2006125441A (ru) * 2003-12-15 2008-01-27 Джапан Тобакко Инк. (Jp) Производные циклопропана и их фармацевтическое применение
EP1711496A4 (en) 2004-01-28 2009-02-11 Smithkline Beecham Corp THIAZOLE COMPOUNDS
JP2007519753A (ja) 2004-01-30 2007-07-19 スミスクライン ビーチャム コーポレーション 化合物
WO2005079791A1 (en) * 2004-02-12 2005-09-01 Boehringer Ingelheim Pharmaceuticals, Inc. Thiophene -2- carboxylic acid - (1h - benzimidazol - 2 yl) - amide derivatives and related compounds as inhibitors of the tec kinase itk (interleukin -2- inducible t cell kinase) for the treatment of inflammation, immunological and allergic disorders
WO2005095386A1 (en) 2004-03-30 2005-10-13 Chiron Corporation Substituted thiophene derivatives as anti-cancer agents
EP1742627A4 (en) * 2004-05-06 2009-08-26 Plexxikon Inc PDE4B HEMMER AND ITS USE
GB0423653D0 (en) 2004-10-25 2004-11-24 Piramed Ltd Pharmaceutical compounds
DK1836201T4 (da) 2004-12-20 2013-11-11 Genentech Inc Pyrrolidininhibitorer af IAP.
CA2589827A1 (en) 2004-12-21 2006-06-29 Merck & Co., Inc. Mitotic kinesin inhibitors
MX2007008781A (es) 2005-01-21 2007-09-11 Astex Therapeutics Ltd Compuestos farmaceuticos.
CA2599320A1 (en) 2005-02-25 2006-08-31 Kudos Pharmaceuticals Limited Hydrazinomethyl, hydr zonomethyl and 5-membered heterocylic compounds which act as mtor inhibitors and their use as anti cancer agents
GB0503962D0 (en) 2005-02-25 2005-04-06 Kudos Pharm Ltd Compounds
CN1834095B (zh) 2005-03-18 2011-04-20 中国科学院上海药物研究所 一类非核苷类抗病毒抑制剂及其制备方法和用途
EP1869049B1 (en) 2005-03-21 2009-03-04 Eli Lilly And Company Imidazopyridazine compounds
GB0508472D0 (en) 2005-04-26 2005-06-01 Glaxo Group Ltd Compounds
GB0508471D0 (en) 2005-04-26 2005-06-01 Celltech R&D Ltd Therapeutic agents
BRPI0612287A8 (pt) 2005-06-27 2019-01-22 Exelixis Inc composição para uso farmacêutico no tratamento de doenças através da medicina nuclear e métodos de uso e para modulação de atividade de receptor nuclear
JP5222561B2 (ja) 2005-10-07 2013-06-26 キッセイ薬品工業株式会社 含窒素芳香族複素環化合物およびそれを含有する医薬組成物
US7618982B2 (en) 2005-12-19 2009-11-17 Nerviano Medical Sciences S.R.L. Heteroarylpyrrolopyridinones active as kinase inhibitors
JP2007197324A (ja) 2006-01-23 2007-08-09 Toray Ind Inc ２，４，５−置換−１，３−アゾール誘導体
CA2637933C (en) 2006-01-24 2013-03-12 Eli Lilly And Company Indole sulfonamide modulators of progesterone receptors
US7504513B2 (en) 2006-02-27 2009-03-17 Hoffman-La Roche Inc. Thiazolyl-benzimidazoles
BRPI0709680B8 (pt) 2006-03-27 2021-05-25 Nerviano Medical Sciences Srl derivados de pirrol, tiofeno e furano substituídos por piridil e piridimil como inibidores de quinase
WO2007129161A2 (en) 2006-04-26 2007-11-15 F. Hoffmann-La Roche Ag Thieno [3, 2-d] pyrimidine derivative useful as pi3k inhibitor
JP2009535386A (ja) * 2006-05-03 2009-10-01 アストラゼネカ アクチボラグ チアゾール誘導体および抗腫瘍剤としてのその使用
WO2007139816A2 (en) 2006-05-23 2007-12-06 Vertex Pharmaceuticals Incorporated Thiophene-carboxamides useful as inhibitors of protein kinases
WO2007138110A2 (en) 2006-06-01 2007-12-06 Devgen N.V. Compounds that interact with ion channels, in particular with ion channels from the kv family
AU2007275221A1 (en) 2006-07-20 2008-01-24 Allen J. Borchardt Benzothiophene inhibitors of RHO kinase
US20100143499A1 (en) 2006-07-24 2010-06-10 Tetralogic Pharmaceuticals Corporation Dimeric iap inhibitors
BRPI0715051A2 (pt) 2006-08-14 2015-05-19 Schering Corp Processo e intermediários para a síntese de derivados de 2-(quinolin-5il)-4,5 dissubstituído-azol
AU2007287428B2 (en) 2006-08-24 2011-08-11 Astrazeneca Ab Morpholino pyrimidine derivatives useful in the treatment of proliferative disorders
WO2008024980A2 (en) 2006-08-24 2008-02-28 Serenex, Inc. Pyrrole, thiophene, furan, imidazole, oxazole, and thiazole derivatives
JP5184536B2 (ja) 2006-09-20 2013-04-17 イーライ リリー アンド カンパニー チオフェンピラゾロピリミジン化合物
GB0620818D0 (en) 2006-10-19 2006-11-29 Ucb Sa Therapeutic agents
RU2469034C2 (ru) 2006-12-04 2012-12-10 Астразенека Аб Химические соединения
WO2008083070A1 (en) 2006-12-29 2008-07-10 Neurogen Corporation Crf1 receptor ligands comprising fused bicyclic heteroaryl moieties
GB0701426D0 (en) 2007-01-25 2007-03-07 Univ Sheffield Compounds and their use
JP5461197B2 (ja) 2007-02-02 2014-04-02 ベイラー カレッジ オブ メディスン 代謝障害を処置するための組成物および方法
UY30892A1 (es) 2007-02-07 2008-09-02 Smithkline Beckman Corp Inhibidores de la actividad akt
US8420690B2 (en) 2007-02-07 2013-04-16 Glaxosmithkline Llc Inhibitors of Akt activity
WO2008134679A1 (en) 2007-04-30 2008-11-06 Genentech, Inc. Inhibitors of iap
GB0709031D0 (en) 2007-05-10 2007-06-20 Sareum Ltd Pharmaceutical compounds
WO2008157273A1 (en) 2007-06-14 2008-12-24 Smithkline Beecham Corporation Chemical compounds
WO2009006577A2 (en) 2007-07-03 2009-01-08 The Regents Of The University Of Michigan Compositions and methods for inhibiting ezh2
US8067613B2 (en) 2007-07-16 2011-11-29 Abbott Laboratories Benzimidazole poly(ADP ribose)polymerase inhibitors
CA2704711C (en) 2007-09-24 2016-07-05 Genentech, Inc. Thiazolopyrimidine p13k inhibitor compounds and methods of use
JP2010540429A (ja) 2007-09-24 2010-12-24 アクテリオン ファーマシューティカルズ リミテッド オレキシン受容体拮抗薬としてのピロリジン類及びピペリジン類
WO2009049028A1 (en) 2007-10-09 2009-04-16 Targegen Inc. Pyrrolopyrimidine compounds and their use as janus kinase modulators
US9029411B2 (en) 2008-01-25 2015-05-12 Millennium Pharmaceuticals, Inc. Thiophenes and uses thereof
TW200940537A (en) 2008-02-26 2009-10-01 Astrazeneca Ab Heterocyclic urea derivatives and methods of use thereof
MX2010010659A (es) 2008-03-31 2010-10-26 Genentech Inc Compuestos de benzopirano y benzoxepina, inhibidores de fosfoinoinositida 3-cinasas y metodos para utilizarlos.
GB0805818D0 (en) 2008-03-31 2008-04-30 Ucb Pharma Sa Therapeutic agents
ES2491522T3 (es) 2008-06-19 2014-09-08 Millennium Pharmaceuticals, Inc. Derivados de tiofeno o tiazol y su uso como inhibidores de PI3K
EP2303852A4 (en) 2008-06-26 2011-12-28 Glaxosmithkline Llc ACTIVITY INHIBITORS AKT
GB0812309D0 (en) 2008-07-03 2008-08-13 Ucb Pharma Sa Therapeutic agents
US8420695B2 (en) 2008-07-09 2013-04-16 Merck Sharp & Dohme Corp. Inhibitors of janus kinases
AU2009279874B2 (en) 2008-08-04 2015-02-12 Merck Sharp & Dohme Corp. Oxazole derivatives useful as inhibitors of FAAH
AU2009314544C1 (en) 2008-11-11 2015-11-12 Xcovery Holding Company Llc PI3K/mTOR kinase inhibitors
GB0820819D0 (en) 2008-11-13 2008-12-24 Sareum Ltd Pharmaceutical compounds
WO2010071741A1 (en) 2008-12-16 2010-06-24 Merck Sharp & Dohme Corp. Triazole derivatives for treatment of alzheimer's disease
WO2010121675A2 (en) 2008-12-18 2010-10-28 F. Hoffmann-La Roche Ag Thiazolyl-benzimidazoles
WO2010080873A1 (en) 2009-01-08 2010-07-15 Glaxo Group Limited Oxazoles as modulators of chemokine receptors
US9090601B2 (en) 2009-01-30 2015-07-28 Millennium Pharmaceuticals, Inc. Thiazole derivatives
US8796314B2 (en) 2009-01-30 2014-08-05 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
WO2010090716A1 (en) 2009-01-30 2010-08-12 Millennium Pharmaceuticals, Inc. Heteroaryls and their use as pi3k inhibitors
EP2430013B1 (en) 2009-05-13 2014-10-15 Amgen Inc. Heteroaryl compounds as pikk inhibitors
US20110021531A1 (en) 2009-07-27 2011-01-27 Chobanian Harry Oxazole derivatives useful as inhibitors of faah
JP2012254939A (ja) 2009-10-07 2012-12-27 Astellas Pharma Inc オキサゾール化合物
WO2012021611A1 (en) 2010-08-11 2012-02-16 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
US8859768B2 (en) 2010-08-11 2014-10-14 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
TW201217365A (en) 2010-08-11 2012-05-01 Millennium Pharm Inc Heteroaryls and uses thereof
TW201307309A (zh) 2010-10-13 2013-02-16 Millennium Pharm Inc 雜芳基化合物及其用途
TW201332989A (zh) 2011-12-23 2013-08-16 Millennium Pharm Inc 雜芳基化合物及其用途

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