JP5819195B2 - 融合環ヘテロアリールキナーゼ阻害剤 - Google Patents

融合環ヘテロアリールキナーゼ阻害剤 Download PDF

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Publication number
JP5819195B2
JP5819195B2 JP2011532279A JP2011532279A JP5819195B2 JP 5819195 B2 JP5819195 B2 JP 5819195B2 JP 2011532279 A JP2011532279 A JP 2011532279A JP 2011532279 A JP2011532279 A JP 2011532279A JP 5819195 B2 JP5819195 B2 JP 5819195B2
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substituted
unsubstituted
compound
alkyl
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Japanese (ja)
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JP2012505916A5 (enExample
JP2012505916A (ja
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ダル，アルヴィン
エム． ショカット，ケバン
エム． ショカット，ケバン
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University of California
University of California, Los Angeles
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University of California, San Diego
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    • 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
    • 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
    • A61K31/495—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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2011532279A 2008-10-16 2009-10-16 融合環ヘテロアリールキナーゼ阻害剤 Expired - Fee Related JP5819195B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US10613708P 2008-10-16 2008-10-16
US61/106,137 2008-10-16
US10645308P 2008-10-17 2008-10-17
US61/106,453 2008-10-17
PCT/US2009/060985 WO2010045542A2 (en) 2008-10-16 2009-10-16 Fused ring heteroaryl kinase inhibitors

Related Child Applications (1)

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JP2014125313A Division JP2014193925A (ja) 2008-10-16 2014-06-18 融合環ヘテロアリールキナーゼ阻害剤

Publications (3)

Publication Number Publication Date
JP2012505916A JP2012505916A (ja) 2012-03-08
JP2012505916A5 JP2012505916A5 (enExample) 2012-11-29
JP5819195B2 true JP5819195B2 (ja) 2015-11-18

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JP2011532279A Expired - Fee Related JP5819195B2 (ja) 2008-10-16 2009-10-16 融合環ヘテロアリールキナーゼ阻害剤
JP2014125313A Withdrawn JP2014193925A (ja) 2008-10-16 2014-06-18 融合環ヘテロアリールキナーゼ阻害剤

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US (1) US8697709B2 (enExample)
EP (1) EP2358720B1 (enExample)
JP (2) JP5819195B2 (enExample)
AU (4) AU2009305669A1 (enExample)
CA (1) CA2740885C (enExample)
DK (1) DK2358720T3 (enExample)
ES (1) ES2570429T3 (enExample)
WO (1) WO2010045542A2 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2014525464A (ja) * 2011-09-02 2014-09-29 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア 置換ピラゾロ［３，４−ｄ］ピリミジンおよびその用途

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9512125B2 (en) 2004-11-19 2016-12-06 The Regents Of The University Of California Substituted pyrazolo[3.4-D] pyrimidines as anti-inflammatory agents
JP2009537520A (ja) * 2006-05-15 2009-10-29 アイアールエム・リミテッド・ライアビリティ・カンパニー Ｆｇｆ受容体キナーゼ阻害剤のための組成物および方法
US20110224223A1 (en) 2008-07-08 2011-09-15 The Regents Of The University Of California, A California Corporation MTOR Modulators and Uses Thereof
AU2009305669A1 (en) * 2008-10-16 2010-04-22 The Regents Of The University Of California Fused ring heteroaryl kinase inhibitors
UA111579C2 (uk) 2009-08-17 2016-05-25 Інтеллікіне Ллк ГЕТЕРОЦИКЛІЧНІ ПОХІДНІ 2-АМІНОБЕНЗО[d]ОКСАЗОЛУ, ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ НА ЇХ ОСНОВІ ТА ЇХ ЗАСТОСУВАННЯ ДЛЯ ЛІКУВАННЯ ЗАХВОРЮВАННЯ, ПОВ'АНОГО З РІ3-КІНАЗОЮ
US8980899B2 (en) 2009-10-16 2015-03-17 The Regents Of The University Of California Methods of inhibiting Ire1
US8598156B2 (en) 2010-03-25 2013-12-03 Glaxosmithkline Llc Chemical compounds
WO2011153553A2 (en) 2010-06-04 2011-12-08 The Regents Of The University Of California Methods and compositions for kinase inhibition
TWI592411B (zh) 2011-02-23 2017-07-21 英特爾立秦有限責任公司 激酶抑制劑之組合及其用途
PT2705029T (pt) 2011-05-04 2019-02-01 Rhizen Pharmaceuticals S A Novos compostos como moduladores de proteína quinases
KR20140048968A (ko) 2011-07-13 2014-04-24 파마시클릭스, 인코포레이티드 브루톤형 티로신 키나제의 억제제
CA2886240A1 (en) * 2012-09-26 2014-04-03 The Regents Of The University Of California Modulation of ire1
CA2885259A1 (en) 2012-10-04 2014-04-10 Pfizer Limited Pyrrolo[3,2-c]pyridine tropomyosin-related kinase inhibitors
PL3026918T3 (pl) 2014-08-01 2019-09-30 Lg Electronics Inc. Sposób nadawania sygnału rozgłaszania i urządzenie do nadawania sygnału rozgłaszania wykorzystujące hermetyzację w pakietach warstwy łącza
EP3193902A4 (en) 2014-09-11 2018-03-28 The Regents of The University of California mTORC1 INHIBITORS
WO2017161344A1 (en) * 2016-03-17 2017-09-21 The Regants Of The University Of California Compositions and methods for treating parasitic diseases
KR102500416B1 (ko) 2016-06-21 2023-02-17 네르비아노 메디칼 사이언시스 에스.알.엘. 키나제 억제제로서의 n-(치환된-페닐)-설폰아미드 유도체
JOP20190024A1 (ar) 2016-08-26 2019-02-19 Gilead Sciences Inc مركبات بيروليزين بها استبدال واستخداماتها
TW201837040A (zh) * 2017-03-15 2018-10-16 美商微拉製藥公司 Cdpk1抑制劑及與其相關之組合物及方法
WO2019036001A1 (en) * 2017-08-17 2019-02-21 Vyera Pharmaceuticals, LLC CDPK1 INHIBITOR, COMPOSITIONS AND RELATED METHODS
JP7050165B2 (ja) 2018-02-26 2022-04-07 ギリアード サイエンシーズ， インコーポレイテッド Ｈｂｖ複製阻害剤としての置換ピロリジン化合物
PL3788049T3 (pl) 2018-05-01 2023-06-19 Revolution Medicines, Inc. Połączone z C40, C28 i C32 analogi rapamycyny jako inhibitory mTOR
EP3788050B1 (en) 2018-05-01 2024-08-28 Revolution Medicines, Inc. C26-linked rapamycin analogs as mtor inhibitors
EP3801069A4 (en) 2018-06-01 2022-03-16 Cornell University COMBINATION THERAPY FOR A PI3K-ASSOCIATED DISEASE OR DISORDER
CN111646995B (zh) * 2019-03-04 2023-03-21 四川大学 4-氨基-嘧啶并氮杂环-苯基脲类衍生物及其制备方法和用途
CN112961158B (zh) * 2020-03-05 2022-07-01 四川大学华西医院 氨基嘧啶并吡唑/吡咯类衍生物及其制备方法和用途
CA3196620A1 (en) * 2020-10-05 2022-04-14 Enliven Therapeutics, Inc. 5- and 6-azaindole compounds for inhibition of bcr-abl tyrosine kinases
PE20231311A1 (es) 2020-11-18 2023-08-24 Deciphera Pharmaceuticals Llc Inhibidores de gcn2 y perk quinasas y metodos de uso de los mismos
CN112574200B (zh) * 2021-02-26 2021-06-11 安润医药科技（苏州）有限公司 Btk和/或btk的突变体c481s的小分子抑制剂
CN115028633B (zh) * 2021-03-08 2023-12-22 药雅科技(上海)有限公司 吡咯并嘧啶类化合物的制备及其应用
US20240287081A1 (en) * 2021-06-09 2024-08-29 Icahn School Of Medicine At Mount Sinai Perfluoroalkane substituted pyrazolo[3,4-d]pyrimidin and pyrrolo[2,3-d]pyrimidin compounds and uses thereof
MX2024006627A (es) 2021-12-03 2024-08-22 Deciphera Pharmaceuticals Llc Inhibidores de gcn2 y perk quinasa y metodos de uso de los mismos.
EP4531859A4 (en) 2022-05-25 2026-05-27 Revolution Medicines Inc CANCER TREATMENT METHODS USING AN MTOR INHIBITOR
WO2024040081A2 (en) * 2022-08-15 2024-02-22 Jasper Therapeutics, Inc. Transgenic animals expressing chimeric c-kit protein

Family Cites Families (309)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB812366A (en) 1955-08-18 1959-04-22 Wellcome Found Improvements in and relating to derivatives of pyrimidine and the preparation thereof
GB937725A (en) 1960-05-11 1963-09-25 Ciba Ltd Pyrazolo[3:4-d]pyrimidines
IT1153216B (it) 1981-10-16 1987-01-14 Schering Ag Procedimento per la preparazione di composti cianoeterociclici
DE3406533A1 (de) 1984-02-23 1985-08-29 Boehringer Mannheim Gmbh, 6800 Mannheim Verwendung von adenosin-derivaten als antiallergica und arzneimittel, die diese enthalten
US5310731A (en) 1984-06-28 1994-05-10 Whitby Research, Inc. N-6 substituted-5'-(N-substitutedcarboxamido)adenosines as cardiac vasodilators and antihypertensive agents
WO1990003370A1 (en) 1988-09-28 1990-04-05 Microprobe Corporation DERIVATIVES OF PYRAZOLO[3,4-d]PYRIMIDINE
US5428125A (en) 1989-07-17 1995-06-27 The Dow Chemical Company Mesogenic polycyanates and thermosets thereof
US5442039A (en) 1989-07-17 1995-08-15 The Dow Chemical Company Mesogenic polycyanates and thermosets thereof
US5795977A (en) 1989-09-15 1998-08-18 Metabasis Therapeutics, Inc. Water soluble adenosine kinase inhibitors
US5763597A (en) 1989-09-15 1998-06-09 Metabasis Therapeutics, Inc. Orally active adenosine kinase inhibitors
US5646128A (en) 1989-09-15 1997-07-08 Gensia, Inc. Methods for treating adenosine kinase related conditions
US5721356A (en) 1989-09-15 1998-02-24 Gensia, Inc. Orally active adenosine kinase inhibitors
US5674998A (en) 1989-09-15 1997-10-07 Gensia Inc. C-4' modified adenosine kinase inhibitors
US5763596A (en) 1989-09-15 1998-06-09 Metabasis Therapeutics, Inc. C-4' modified adenosine kinase inhibitors
GB9009542D0 (en) 1990-04-27 1990-06-20 Beecham Group Plc Novel compounds
GB9113137D0 (en) 1990-07-13 1991-08-07 Ici Plc Thioxo heterocycles
US5563257A (en) 1990-08-20 1996-10-08 Boehringer Mannheim Gmbh Phospholipid derivatives of nucleosides
DE4026265A1 (de) 1990-08-20 1992-02-27 Boehringer Mannheim Gmbh Neue phospholipid-derivate von nucleosiden, deren herstellung sowie deren verwendung als antivirale arzneimittel
US5561134A (en) 1990-09-25 1996-10-01 Rhone-Poulenc Rorer Pharmaceuticals Inc. Compounds having antihypertensive, cardioprotective, anti-ischemic and antilipolytic properties
ES2095960T3 (es) 1990-09-25 1997-03-01 Rhone Poulenc Rorer Int Compuestos que tienen propiedades antihipertensivas y antiisquemicas.
US5652366A (en) 1990-09-25 1997-07-29 Rhone-Poulenc Rorer Pharmaceuticals Inc. DI (1R)-(-)camphosulfonic acid) salt, preparation thereof and use thereof
GB9103839D0 (en) 1991-02-23 1991-04-10 Smithkline Beecham Plc Pharmaceuticals
IL104369A0 (en) 1992-01-13 1993-05-13 Smithkline Beecham Corp Novel compounds and compositions
US5916891A (en) 1992-01-13 1999-06-29 Smithkline Beecham Corporation Pyrimidinyl imidazoles
DE4204031A1 (de) 1992-02-12 1993-08-19 Boehringer Mannheim Gmbh Neue lipidphosphonsaeure-nucleosid-konjugate sowie deren verwendung als antivirale arzneimittel
DE4204032A1 (de) 1992-02-12 1993-08-19 Boehringer Mannheim Gmbh Neue liponucleotide, deren herstellunmg sowie deren verwendung als antivirale arzneimittel
WO1993018035A1 (en) 1992-03-04 1993-09-16 Abbott Laboratories Angiotensin ii receptor antagonists
GB9208135D0 (en) 1992-04-13 1992-05-27 Ludwig Inst Cancer Res Polypeptides having kinase activity,their preparation and use
AU4115693A (en) 1992-04-24 1993-11-29 Sri International In vivo homologous sequence targeting in eukaryotic cells
RU2121766C1 (ru) 1992-06-19 1998-11-10 Ханивелл Инк. Инфракрасная камера и способ считывания изменений удельного сопротивления пассивных принимающих излучение элементов
US6057305A (en) 1992-08-05 2000-05-02 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Antiretroviral enantiomeric nucleotide analogs
TW370529B (en) * 1992-12-17 1999-09-21 Pfizer Pyrazolopyrimidines
IL108523A0 (en) 1993-02-03 1994-05-30 Gensia Inc Pharmaceutical compositions containing adenosine kinase inhibitors for preventing or treating conditions involving inflammatory responses and pain
WO1994018215A1 (en) 1993-02-03 1994-08-18 Gensia, Inc. Adenosine kinase inhibitors comprising lyxofuranosyl derivatives
AU6672794A (en) 1993-11-05 1995-05-23 Biochem Pharma Inc. Antineoplastic heteronaphthoquinones
IL112249A (en) 1994-01-25 2001-11-25 Warner Lambert Co Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds
US5654307A (en) 1994-01-25 1997-08-05 Warner-Lambert Company Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family
US6632789B1 (en) 1994-04-29 2003-10-14 The United States Of America As Represented By The Secretary Of The Navy Methods for modulating T cell responses by manipulating intracellular signal transduction
DE4418690A1 (de) 1994-05-28 1996-01-11 Boehringer Mannheim Gmbh Neue Lipidester von Nucleosid-Monophosphaten und deren Verwendung als immunsuppressive Arzneimittel
PT783505E (pt) * 1994-09-29 2001-08-30 Novartis Ag Pirrolo¬2,3-d|pirimidinas e sua utilizacao
US6323201B1 (en) 1994-12-29 2001-11-27 The Regents Of The University Of California Compounds for inhibition of ceramide-mediated signal transduction
US6312894B1 (en) 1995-04-03 2001-11-06 Epoch Pharmaceuticals, Inc. Hybridization and mismatch discrimination using oligonucleotides conjugated to minor groove binders
JP4249804B2 (ja) 1995-04-03 2009-04-08 ノバルティス・アクチエンゲゼルシャフト ピラゾール誘導体およびその製造法
US5977061A (en) 1995-04-21 1999-11-02 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic N6 - substituted nucleotide analagues and their use
WO1996037777A1 (en) 1995-05-23 1996-11-28 Nelson Randall W Mass spectrometric immunoassay
US5593997A (en) 1995-05-23 1997-01-14 Pfizer Inc. 4-aminopyrazolo(3-,4-D)pyrimidine and 4-aminopyrazolo-(3,4-D)pyridine tyrosine kinase inhibitors
AU5982296A (en) 1995-06-07 1996-12-30 G.D. Searle & Co. Method to treat cardiofibrosis with a combination of an angi otensin ii antagonist and spironolactone
AU6158096A (en) 1995-06-07 1996-12-30 G.D. Searle & Co. Spironolactone and angiotensin ii antagonist combination the rapy for treatment of congestive heart failure
US5665721A (en) 1995-06-07 1997-09-09 Abbott Laboratories Heterocyclic substituted cyclopentane compounds
CN1142793C (zh) 1995-06-07 2004-03-24 G·D·瑟尔公司 环氧-甾族化合物醛甾酮拮抗剂和血管紧张肽ⅱ拮抗剂联合治疗用于治疗充血性心衰
US5763885A (en) 1995-12-19 1998-06-09 Loral Infrared & Imaging Systems, Inc. Method and apparatus for thermal gradient stabilization of microbolometer focal plane arrays
US5747235A (en) 1996-01-26 1998-05-05 Eastman Kodak Company Silver halide light sensitive emulsion layer having enhanced photographic sensitivity
CH690773A5 (de) 1996-02-01 2001-01-15 Novartis Ag Pyrrolo(2,3-d)pyrimide und ihre Verwendung.
DE19603576A1 (de) 1996-02-01 1997-08-07 Bayer Ag Acylierte 4-Amino und 4-Hydrazinopyrimidine
GB2310952B (en) 1996-03-05 1998-08-19 Mitsubishi Electric Corp Infrared detector
GB9611460D0 (en) 1996-06-01 1996-08-07 Ludwig Inst Cancer Res Novel lipid kinase
IL127559A0 (en) 1996-06-20 1999-10-28 Univ Texas Compounds and methods for providing pharmacologically active preparations and uses thereof
US5965573A (en) 1996-10-23 1999-10-12 Zymogenetics, Inc. Compositions and methods for treating bone deficit conditions
US5994358A (en) 1996-10-23 1999-11-30 Zymogenetics, Inc. Compositions and methods for treating bone deficit conditions
US5990169A (en) 1996-10-23 1999-11-23 Zymogenetics, Inc. Compositions and methods for treating bone deficit conditions
US5922753A (en) 1996-10-23 1999-07-13 Zymogenetics, Inc. Methods for treating bone deficit conditions with benzothiazole
US6153631A (en) 1996-10-23 2000-11-28 Zymogenetics, Inc. Compositions and methods for treating bone deficit conditions
US5919808A (en) 1996-10-23 1999-07-06 Zymogenetics, Inc. Compositions and methods for treating bone deficit conditions
US6342514B1 (en) 1996-10-23 2002-01-29 Zymogenetics, Inc. Compositions and methods for treating bone deficit conditions
US6251901B1 (en) 1996-10-23 2001-06-26 Zymogenetics, Inc. Compositions and methods for treating bone deficit conditions
US5948776A (en) 1996-10-23 1999-09-07 Zymogenetic, Inc. Compositions and methods for treating bone deficit conditions
US5858753A (en) 1996-11-25 1999-01-12 Icos Corporation Lipid kinase
JP4094066B2 (ja) 1996-12-06 2008-06-04 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 インターロイキン−１β変換酵素のインヒビター
US6093737A (en) 1996-12-30 2000-07-25 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
EP1017823B1 (en) 1997-02-07 2004-07-14 Princeton University Engineered protein kinases which can utilize modified nucleotide triphosphate substrates
US7863444B2 (en) 1997-03-19 2011-01-04 Abbott Laboratories 4-aminopyrrolopyrimidines as kinase inhibitors
BR9808281A (pt) * 1997-03-19 2000-05-16 Basf Ag Compostos, composições farmacêuticas, processo para tratar doenças proliferativas e/ou distúrbios do sistema imune e para preparar um composto, e, uso de um composto
WO1998052611A1 (en) 1997-05-23 1998-11-26 Nippon Shinyaku Co., Ltd. Medicinal composition for prevention or treatment of hepatopathy
US6207679B1 (en) 1997-06-19 2001-03-27 Sepracor, Inc. Antimicrobial agents uses and compositions related thereto
WO1999018077A1 (en) 1997-10-02 1999-04-15 Eisai Co., Ltd. Fused pyridine derivatives
US6649631B1 (en) 1997-10-23 2003-11-18 The Board Of Regents Of The University Of Texas System Compositions and methods for treating bone deficit conditions
DE69824632T2 (de) 1997-11-12 2005-06-09 Mitsubishi Chemical Corp. Purinderivate und medikamente, welche dieselben als aktiven bestandteil enthalten
US6191170B1 (en) 1998-01-13 2001-02-20 Tularik Inc. Benzenesulfonamides and benzamides as therapeutic agents
US7715989B2 (en) 1998-04-03 2010-05-11 Elitech Holding B.V. Systems and methods for predicting oligonucleotide melting temperature (TmS)
US6127121A (en) 1998-04-03 2000-10-03 Epoch Pharmaceuticals, Inc. Oligonucleotides containing pyrazolo[3,4-D]pyrimidines for hybridization and mismatch discrimination
JP2000072773A (ja) 1998-08-28 2000-03-07 Zeria Pharmaceut Co Ltd プリン誘導体
NZ510588A (en) * 1998-09-18 2003-08-29 Abbott Gmbh & Co Pyrrolopyrimidines as protein kinase inhibitors
US6713474B2 (en) * 1998-09-18 2004-03-30 Abbott Gmbh & Co. Kg Pyrrolopyrimidines as therapeutic agents
CZ2001959A3 (cs) 1998-09-18 2001-12-12 Basf Aktiengesellschaft 4-Aminopyrrolopyrimidiny jako inhibitory kinasy
DK1140938T3 (da) 1999-01-11 2003-12-22 Univ Princeton Højaffinitetsinhibitorer for målvalidering og anvendelser heraf
CZ27399A3 (cs) 1999-01-26 2000-08-16 Ústav Experimentální Botaniky Av Čr Substituované dusíkaté heterocyklické deriváty, způsob jejich přípravy, tyto deriváty pro použití jako léčiva, farmaceutická kompozice a kombinovaný farmaceutický přípravek tyto deriváty obsahující a použití těchto derivátů pro výrobu léčiv
EP1040831A3 (en) 1999-04-02 2003-05-02 Pfizer Products Inc. Use of corticotropin releasing factor (CRF) antagonists to prevent sudden death
SE515856C2 (sv) 1999-05-19 2001-10-22 Ericsson Telefon Ab L M Bärare för elektronikkomponenter
PL352680A1 (en) 1999-06-03 2003-09-08 Knoll Gmbh Benzothiazinone and benzoxazinone compounds
US6387894B1 (en) 1999-06-11 2002-05-14 Pfizer Inc. Use of CRF antagonists and renin-angiotensin system inhibitors
PE20010306A1 (es) 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa
TWI262914B (en) 1999-07-02 2006-10-01 Agouron Pharma Compounds and pharmaceutical compositions for inhibiting protein kinases
GB9919588D0 (en) 1999-08-18 1999-10-20 Hoechst Schering Agrevo Gmbh Fungicidal compounds
US6559160B1 (en) 1999-08-27 2003-05-06 Chemocentryx, Inc. Compounds and methods for modulating cxcr3 function
DE60017157T2 (de) 1999-09-16 2005-12-22 Curis, Inc., Cambridge Vermittler von igel signalwegen, deren zusammenstellungen und verwendungen
US6921763B2 (en) 1999-09-17 2005-07-26 Abbott Laboratories Pyrazolopyrimidines as therapeutic agents
KR20020088406A (ko) 1999-09-17 2002-11-27 애보트 게엠베하 운트 콤파니 카게 치료제로서의 피라졸로피리미딘
DE60014130T2 (de) 1999-10-06 2006-03-09 Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield Heterocyclische verbindungen verwendbar als tyrosinkinase inhibitoren
US6506769B2 (en) 1999-10-06 2003-01-14 Boehringer Ingelheim Pharmaceuticals, Inc. Heterocyclic compounds useful as inhibitors of tyrosine kinases
US6472153B1 (en) 1999-10-26 2002-10-29 Epoch Biosciences, Inc. Hybridization-triggered fluorescent detection of nucleic acids
US6660845B1 (en) 1999-11-23 2003-12-09 Epoch Biosciences, Inc. Non-aggregating, non-quenching oligomers comprising nucleotide analogues; methods of synthesis and use thereof
GB0002032D0 (en) 2000-01-28 2000-03-22 Zeneca Ltd Chemical compounds
US7217722B2 (en) 2000-02-01 2007-05-15 Kirin Beer Kabushiki Kaisha Nitrogen-containing compounds having kinase inhibitory activity and drugs containing the same
JP4988119B2 (ja) * 2000-03-27 2012-08-01 コンティネンタル・テーベス・アクチエンゲゼルシヤフト・ウント・コンパニー・オッフェネ・ハンデルスゲゼルシヤフト 車両操舵装置
AU2000240570A1 (en) * 2000-03-29 2001-10-08 Knoll Gesellschaft Mit Beschraenkter Haftung Pyrrolopyrimidines as tyrosine kinase inhibitors
EP1268549A2 (en) * 2000-03-29 2003-01-02 Knoll GmbH Method of identifying inhibitors of tie-2
US6613798B1 (en) 2000-03-30 2003-09-02 Curis, Inc. Small organic molecule regulators of cell proliferation
US7115653B2 (en) 2000-03-30 2006-10-03 Curis, Inc. Small organic molecule regulators of cell proliferation
DE60144277D1 (de) 2000-04-25 2011-05-05 Icos Corp Hemmer der menschlichen phosphatidyl-inositol-3-kinase delta
US6667300B2 (en) 2000-04-25 2003-12-23 Icos Corporation Inhibitors of human phosphatidylinositol 3-kinase delta
AU2001265137B2 (en) 2000-05-30 2007-06-14 Indiana University Research And Technology Corporation Compositions and methods for identifying agents which modulate PTEN function and PI-3 kinase pathways
EP1294713A2 (en) 2000-06-27 2003-03-26 Genelabs Technologies, Inc. Compounds possessing antibacterial, antifungal or antitumor activity
US6534691B2 (en) 2000-07-18 2003-03-18 E. I. Du Pont De Nemours And Company Manufacturing process for α-olefins
AU1312502A (en) 2000-10-11 2002-04-22 Pe Corp Ny Fluorescent nucleobase conjugates having anionic linkers
AU2002213467A1 (en) 2000-10-11 2002-04-22 Chemocentryx, Inc. Modulation of ccr4 function
US6890747B2 (en) 2000-10-23 2005-05-10 Warner-Lambert Company Phosphoinositide 3-kinases
NZ526622A (en) 2000-12-11 2006-07-28 Amgen Sf Llc CXCR3 antagonists
CA2430978C (en) 2000-12-28 2012-05-15 Daiichi Pharmaceutical Co., Ltd. Vla-4 inhibitors
MXPA03006514A (es) 2001-01-22 2004-12-02 Merck & Co Inc Derivados de nucleosidos como inhibidores de polimerasa de acido ribonucleico viral dependiente de acido ribonucleico.
US7105499B2 (en) 2001-01-22 2006-09-12 Merck & Co., Inc. Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase
ATE497603T1 (de) * 2001-03-02 2011-02-15 Gpc Biotech Ag Drei-hybrid-assaysystem
MXPA03008560A (es) * 2001-03-22 2004-06-30 Abbot Gmbh & Co Kg Pirazolopirimidinas como agentes terapeuticos.
WO2002088025A1 (en) 2001-04-26 2002-11-07 New York University Method for dissolving carbon nanotubes
WO2002090334A1 (en) 2001-05-08 2002-11-14 Kudos Pharmaceuticals Limited Isoquinolinone derivatives as parp inhibitors
WO2002094264A1 (en) 2001-05-23 2002-11-28 Tularik Inc. Ccr4 antagonists
US6825228B2 (en) 2001-06-13 2004-11-30 Genesoft Pharmaceuticals, Inc. Benzothiophene compounds having antiinfective activity
AU2002312370A1 (en) 2001-06-13 2002-12-23 Roland W. Burli Antipathogenic benzamide compounds
CA2450625A1 (en) 2001-06-13 2002-12-19 Genesoft Pharmaceuticals, Inc. Isoquinoline compounds having antiinfective activity
WO2003000187A2 (en) 2001-06-21 2003-01-03 Ariad Pharmaceuticals, Inc. Novel pyrazolo-and pyrrolo-pyrimidines and uses thereof
CA2455181C (en) 2001-08-01 2010-04-06 Merck & Co., Inc. Benzimidazo[4,5-f]isoquinolinone derivatives
WO2003020880A2 (en) 2001-08-03 2003-03-13 Abbott Laboratories Method of identifying inhibitors of lck
ATE530520T1 (de) 2001-08-10 2011-11-15 Shionogi & Co Antivirales mittel
WO2003024969A1 (en) 2001-09-14 2003-03-27 Merck & Co., Inc. Tyrosine kinase inhibitors
AU2002368274A1 (en) 2001-09-13 2004-06-03 Genesoft, Inc. Methods of treating infection by drug resistant bacteria
AUPR769501A0 (en) 2001-09-14 2001-10-11 Biomolecular Research Institute Limited Cytokine receptor 1
TWI330183B (enExample) 2001-10-22 2010-09-11 Eisai R&D Man Co Ltd
US7319858B2 (en) 2001-11-16 2008-01-15 Cingular Wireless Ii, Llc System and method for querying message information
WO2003048081A2 (en) 2001-12-04 2003-06-12 Bristol-Myers Squibb Company Glycinamides as factor xa inhibitors
US7998986B2 (en) 2001-12-21 2011-08-16 Exelixis Patent Company Llc Modulators of LXR
JP4085237B2 (ja) 2001-12-21 2008-05-14 日本電気株式会社 携帯電話の利用契約システムと通信方法
BR0207583A (pt) 2001-12-26 2004-04-27 Genelabs Tech Inc Derivados de poliamida possuindo atividade antibacteriana, antifungo ou antitumor
US7414036B2 (en) 2002-01-25 2008-08-19 Muscagen Limited Compounds useful as A3 adenosine receptor agonists
AU2003225933A1 (en) 2002-03-22 2003-10-13 Cellular Genomics, Inc. AN IMPROVED FORMULATION OF CERTAIN PYRAZOLO(3,4-d) PYRIMIDINES AS KINASE MODULATORS
EP1503988B1 (de) 2002-03-26 2009-07-22 Biofrontera Discovery Gmbh Fredericamycin-derivate
US7166293B2 (en) 2002-03-29 2007-01-23 Carlsbad Technology, Inc. Angiogenesis inhibitors
DE10217046A1 (de) 2002-04-17 2003-11-06 Bioleads Gmbh Fredericamycin-Derivate
MXPA04010550A (es) 2002-04-26 2005-01-25 Pfizer Prod Inc Inhibidores de metaloproteinasa de pirimidina-2,4,6-triona.
US6794562B2 (en) 2002-05-01 2004-09-21 Stine Seed Farm, Inc. Soybean cultivar 0332143
EP1517904A4 (en) 2002-05-23 2007-02-21 Merck & Co Inc INHIBITORS OF MITOTIC KINESINE
CA2489367A1 (en) 2002-06-14 2003-12-24 Cytokinetics, Inc. Compounds, compositions, and methods
CA2744893A1 (en) 2002-06-27 2004-01-08 Novo Nordisk A/S Aryl carbonyl derivatives as glucokinase activators
KR101124245B1 (ko) 2002-06-27 2012-07-02 노보 노르디스크 에이/에스 치료제로서 아릴 카르보닐 유도체
US7265111B2 (en) 2002-06-27 2007-09-04 Sanofi-Aventis Deutschland Gmbh Adenosine analogues and their use as pharmaceutical agents
DE10230917A1 (de) 2002-07-09 2004-02-05 Bioleads Gmbh Fredericamycin-Derivate
WO2004006906A2 (en) 2002-07-15 2004-01-22 Combinatorx, Incorporated Methods for the treatment of neoplasms
WO2004014377A1 (en) 2002-08-13 2004-02-19 Warner-Lambert Company Llc 4-hydroxyquinoline derivatives as matrix metalloproteinase inhibitors
EP1537102A4 (en) 2002-08-16 2010-12-08 Astrazeneca Ab INHIBITORS OF PHOSPHOINOSITIDE-3-KINASE BETA
EP1539180A4 (en) 2002-08-21 2006-08-30 Cytokinetics Inc COMPOUNDS, COMPOSITIONS AND METHODS
US20030139427A1 (en) 2002-08-23 2003-07-24 Osi Pharmaceuticals Inc. Bicyclic pyrimidinyl derivatives and methods of use thereof
AU2003266668A1 (en) 2002-09-30 2004-04-23 Banyu Pharmaceutical Co., Ltd. 2-aminobenzimidazole derivative
JP2004161716A (ja) 2002-11-15 2004-06-10 Takeda Chem Ind Ltd Ｊｎｋ阻害剤
UA80171C2 (en) * 2002-12-19 2007-08-27 Pfizer Prod Inc Pyrrolopyrimidine derivatives
WO2004058717A1 (en) 2002-12-20 2004-07-15 X-Ceptor Therapeutics, Inc. Isoquinolinone derivatives and their use as therapeutic agents
US7247736B2 (en) 2002-12-23 2007-07-24 4Sc Ag Method of identifying inhibitors of DHODH
US7365094B2 (en) 2002-12-23 2008-04-29 4Sc Ag Compounds as anti-inflammatory, immunomodulatory and anti-proliferatory agents
WO2004056746A1 (en) 2002-12-23 2004-07-08 4Sc Ag Cycloalkene dicarboxylic acid compounds as anti-inflammatory, immunomodulatory and anti-proliferatory agents
WO2004078702A1 (en) 2003-03-06 2004-09-16 Dsm Ip Assets B.V. PROCESS FOR THE PREPARATION OF AN α-AMINO CARBONYL COMPOUND
US20040242568A1 (en) 2003-03-25 2004-12-02 Syrrx, Inc. Dipeptidyl peptidase inhibitors
GB0306907D0 (en) 2003-03-26 2003-04-30 Angiogene Pharm Ltd Boireductively-activated prodrugs
US7217794B2 (en) 2003-04-02 2007-05-15 Daiamed, Inc. Compounds and methods for treatment of thrombosis
WO2004100868A2 (en) * 2003-04-23 2004-11-25 Abbott Laboratories Method of treating transplant rejection
ATE440825T1 (de) 2003-06-06 2009-09-15 Vertex Pharma Pyrimidin-derivate zur verwendung als modulatoren von atp-bindende kassette transportern
US7429596B2 (en) 2003-06-20 2008-09-30 The Regents Of The University Of California 1H-pyrrolo [2,3-D] pyrimidine derivatives and methods of use thereof
WO2005002585A1 (en) 2003-07-02 2005-01-13 Warner-Lambert Company Llc Combination of an allosteric inhibitor of matrix metalloproteinase-13 and a ligand to an alpha-2-delta receptor
GB0317951D0 (en) 2003-07-31 2003-09-03 Trigen Ltd Compounds
US7208601B2 (en) 2003-08-08 2007-04-24 Mjalli Adnan M M Aryl and heteroaryl compounds, compositions, and methods of use
WO2005014532A1 (en) 2003-08-08 2005-02-17 Transtech Pharma, Inc. Aryl and heteroaryl compounds, compositions and methods of use
US20050054614A1 (en) 2003-08-14 2005-03-10 Diacovo Thomas G. Methods of inhibiting leukocyte accumulation
US20050043239A1 (en) 2003-08-14 2005-02-24 Jason Douangpanya Methods of inhibiting immune responses stimulated by an endogenous factor
JP2007502776A (ja) 2003-08-15 2007-02-15 アイアールエム・リミテッド・ライアビリティ・カンパニー Ｒｔｋ阻害剤としての６−置換アニリノプリン類
US7390820B2 (en) 2003-08-25 2008-06-24 Amgen Inc. Substituted quinolinone derivatives and methods of use
WO2005044181A2 (en) 2003-09-09 2005-05-19 Temple University-Of The Commonwealth System Of Higher Education Protection of tissues and cells from cytotoxic effects of ionizing radiation by abl inhibitors
GB0322409D0 (en) 2003-09-25 2003-10-29 Astrazeneca Ab Quinazoline derivatives
CA2545340A1 (en) 2003-11-10 2005-05-26 Synta Pharmaceuticals, Corp. Fused heterocyclic compounds
MXPA06005578A (es) * 2003-11-17 2006-08-11 Pfizer Prod Inc Compuestos de pirrolopirimidina utiles en el tratamiento del cancer.
EP1692112A4 (en) 2003-12-08 2008-09-24 Cytokinetics Inc COMPOUNDS, COMPOSITIONS, AND METHODS
MXPA06007095A (es) 2003-12-22 2006-09-04 Gilead Sciences Inc Conjugados de fosfonato inhibidores de cinasa.
JP2007517052A (ja) 2003-12-23 2007-06-28 ノバルティス アクチエンゲゼルシャフト 二環式ヘテロ環式ｐ−３８キナーゼ阻害剤
CA2552664A1 (en) 2004-01-08 2005-07-28 Michigan State University Methods for treating and preventing hypertension and hypertension-related disorders
WO2005074603A2 (en) 2004-02-03 2005-08-18 Abbott Laboratories Aminobenzoxazoles as therapeutic agents
BRPI0507629A (pt) 2004-02-13 2007-07-03 Banyu Pharma Co Ltd composto, antagonista do receptor e agonista inverso do receptor da histamina h3, agente profilático ou terapêutico para uma doença metabólica, uma doença circulatória ou uma doença do sistema nervoso, ou um seu sal farmaceuticamente aceitável
US20050187418A1 (en) 2004-02-19 2005-08-25 Small Brooke L. Olefin oligomerization
WO2005080394A1 (en) 2004-02-24 2005-09-01 Bioaxone Therapeutique Inc. 4-substituted piperidine derivatives
CN1926139A (zh) 2004-02-27 2007-03-07 霍夫曼-拉罗奇有限公司 稠合吡唑衍生物
MXPA06011423A (es) 2004-04-02 2007-01-23 Osi Pharm Inc Inhibidores de proteina cinasa heterobiciclica sustituida en el anillo 6,6-biciclico.
TW200538453A (en) * 2004-04-26 2005-12-01 Bristol Myers Squibb Co Bicyclic heterocycles as kinase inhibitors
MXPA06012333A (es) 2004-04-30 2007-01-17 Takeda Pharmaceutical Compuesto de amida heterociclico y uso del mismo como un inhibidor mmp-13.
DE102004022897A1 (de) 2004-05-10 2005-12-08 Bayer Cropscience Ag Azinyl-imidazoazine
LT2612862T (lt) 2004-05-13 2017-01-25 Icos Corporation Chinazolinonai kaip žmogaus fosfatidilinozitol-3-kinazės delta inhibitoriai
EP1750714A1 (en) 2004-05-13 2007-02-14 Vanderbilt University Phosphoinositide 3-kinase delta selective inhibitors for inhibiting angiogenesis
WO2005117889A1 (en) 2004-05-25 2005-12-15 Icos Corporation Methods for treating and/or preventing aberrant proliferation of hematopoietic
JP4842929B2 (ja) * 2004-05-27 2011-12-21 ファイザー・プロダクツ・インク 癌治療に有用なピロロピリミジン誘導体
JP2008501707A (ja) 2004-06-04 2008-01-24 アイコス、コーポレーション マスト細胞障害を処置するための方法
GB0420722D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
WO2006038865A1 (en) 2004-10-01 2006-04-13 Betagenon Ab Nucleotide derivatives for the treatment of type 2 diabetes and other disorders
US8212012B2 (en) 2004-11-03 2012-07-03 University Of Kansas Novobiocin analogues having modified sugar moieties
US7622451B2 (en) 2004-11-03 2009-11-24 University Of Kansas Novobiocin analogues as neuroprotective agents and in the treatment of autoimmune disorders
AU2005301957B2 (en) 2004-11-03 2012-02-23 Department Of Health And Human Services Novobiocin analogues as anticancer agents
US8212011B2 (en) 2004-11-03 2012-07-03 University Of Kansas Novobiocin analogues
GB0425035D0 (en) * 2004-11-12 2004-12-15 Novartis Ag Organic compounds
US9512125B2 (en) 2004-11-19 2016-12-06 The Regents Of The University Of California Substituted pyrazolo[3.4-D] pyrimidines as anti-inflammatory agents
EP1817025A2 (en) 2004-11-23 2007-08-15 PTC Therapeutics, Inc. Tetrahydrocarbazoles as active agents for inhibiting vegf production by translational control
US20060156485A1 (en) 2005-01-14 2006-07-20 The Procter & Gamble Company Keratin dyeing compounds, keratin dyeing compositions containing them, and use thereof
GB0501999D0 (en) 2005-02-01 2005-03-09 Sentinel Oncology Ltd Pharmaceutical compounds
US20080287469A1 (en) 2005-02-17 2008-11-20 Diacovo Thomas G Phosphoinositide 3-Kinase Inhibitors for Inhibiting Leukocyte Accumulation
WO2006091897A2 (en) 2005-02-25 2006-08-31 Adenosine Therapeutics, Llc Derivatives of 8-substituted xanthines
US20090124654A1 (en) 2005-03-01 2009-05-14 Mjalli Adnan M M Aryl and Heteroaryl Compounds, Compositions, Methods of Use
WO2006102079A1 (en) * 2005-03-17 2006-09-28 Novartis Ag N- [3- (1-amin0-5, 6, 7, 8-tetrahydro-2 , 4, 4b-triazafluoren-9-yl)-phenyl] benzamides as tyrosine/threonine kinase inhibitors, in particular b-raf kinase
EP1865775A1 (en) 2005-04-06 2007-12-19 Irm, Llc Diarylamine-containing compounds and compositions, and their use as modulators of steroid hormone nuclear receptors
KR100781704B1 (ko) 2005-04-20 2007-12-03 에스케이케미칼주식회사 피리딘 유도체와 이의 제조방법, 및 이를 포함하는약제조성물
EP1879657A2 (en) 2005-04-25 2008-01-23 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Use of compounds to enhance processivity of telomerase
US20070010523A1 (en) 2005-06-22 2007-01-11 Chemocentryx, Inc. Azaindazole compounds and methods of use
DE602006015658D1 (de) 2005-06-27 2010-09-02 Amgen Inc Entzündungshemmende arylnitrilverbindungen
US20100190788A1 (en) 2005-07-11 2010-07-29 Olivier Defert Amide derivatives as kinase inhitors
JP2009505948A (ja) 2005-07-11 2009-02-12 デブジェン エヌブイ キナーゼ阻害剤としてのアミド誘導体
GB0516723D0 (en) 2005-08-15 2005-09-21 Novartis Ag Organic compounds
EP1919913A2 (en) 2005-08-25 2008-05-14 F.Hoffmann-La Roche Ag P38 map kinase inhibitors and methods for using the same
US20070049591A1 (en) 2005-08-25 2007-03-01 Kalypsys, Inc. Inhibitors of MAPK/Erk Kinase
EP1919873A1 (de) 2005-09-01 2008-05-14 BioAgency AG Fredericamycin-derivate
CN101309904A (zh) 2005-09-29 2008-11-19 惠氏公司 作为单胺再摄取调节剂用于治疗血管舒缩症状(vasomotorsymptoms，vms)的1－(1h－吲哚－1－基)－3－(甲基氨基)－1－苯基丙－2－醇衍生物和相关化合物
CA2630271C (en) 2005-11-17 2014-04-08 Osi Pharmaceuticals, Inc. Fused bicyclic mtor inhibitors
WO2007061763A2 (en) 2005-11-22 2007-05-31 Merck & Co., Inc. Indole orexin receptor antagonists
WO2007066189A2 (en) * 2005-12-09 2007-06-14 Pfizer Products Inc. Salts, prodrugs and formulations of 1-[5-(4-amino-7-isopropyl-7h-pyrrolo[2,3-d]pyrimidine-5-carbonyl)-2-methoxy-phenyl]-3-(2,4-dichloro-phenyl)-urea
US20080299113A1 (en) 2005-12-19 2008-12-04 Arnold Lee D Combined treatment with and composition of 6,6-bicyclic ring substituted heterobicyclic protein kinase inhibitor and anti-cancer agents
US7772231B2 (en) 2005-12-29 2010-08-10 Abbott Laboratories Substituted pyrazolo[3,4-d]pyrimidines as protein kinase inhibitors
US20080058521A1 (en) 2006-01-26 2008-03-06 Wyeth Processes for the preparation of compounds
US7723330B2 (en) 2006-03-07 2010-05-25 Array Biopharma Inc. Heterobicyclic pyrazole compounds and methods of use
WO2007106503A2 (en) 2006-03-13 2007-09-20 Osi Pharmaceuticals, Inc. Combined treatment with an egfr kinase inhibitor and an agent that sensitizes tumor cells to the effects of egfr kinase inhibitors
TWI428448B (zh) 2006-03-24 2014-03-01 Syntonix Pharmaceuticals Inc 作為第九因子（ｆａｃｔｏｒ ｉｘ）原肽處理酶之ｐｃ５
US20100273776A1 (en) 2006-03-29 2010-10-28 FOLDRx PHARMACEUTICALS, INC Inhibition of alpha-synuclein toxicity
KR20150038395A (ko) 2006-04-04 2015-04-08 더 리젠트스 오브 더 유니이버시티 오브 캘리포니아 키나제 길항물질
WO2007121453A2 (en) 2006-04-17 2007-10-25 The Regents Of The University Of California 2-hydroxy-1-oxo 1,2 dihydro isoquinoline chelating agents
GB0607948D0 (en) 2006-04-21 2006-05-31 Novartis Ag Organic compounds
GB0607950D0 (en) 2006-04-21 2006-05-31 Novartis Ag Organic compounds
HRP20120494T1 (hr) 2006-04-21 2012-08-31 Novartis Ag Derivati purina za uporabu kao agonista adenozin a2a receptora
EP2037931A2 (en) 2006-04-25 2009-03-25 Astex Therapeutics Limited Pharmaceutical combinations of pk inhibitors and other active agents
US20090253718A1 (en) 2006-04-25 2009-10-08 Astex Therapeutics Limited Pharmaceutical Compounds
DE102006020327A1 (de) 2006-04-27 2007-12-27 Bayer Healthcare Ag Heterocyclisch substituierte, anellierte Pyrazol-Derivate und ihre Verwendung
WO2007135398A1 (en) 2006-05-22 2007-11-29 Astrazeneca Ab Indole derivatives
GB0610242D0 (en) 2006-05-23 2006-07-05 Novartis Ag Organic compounds
GB0610317D0 (en) 2006-05-24 2006-07-05 Medical Res Council Antiparasitic compounds and compositions
EP2079724B1 (en) 2006-07-20 2010-05-26 Amgen Inc. Substituted pyridone compounds and methods of use
EP2589597B1 (en) 2006-08-22 2019-03-06 Technion Research & Development Foundation Heterocyclic derivatives binding to the peripheral-type benzodiazepine receptor (PBR)
JP2010501593A (ja) 2006-08-24 2010-01-21 セレネックス， インコーポレイテッド イソキノリン、キナゾリンおよびフタラジン誘導体
DK2061765T3 (en) 2006-09-01 2015-01-26 Senhwa Biosciences Inc Serine-threonine protein kinase AND PARP-MODULATOR
WO2008025755A1 (de) 2006-09-01 2008-03-06 Basf Se Verwendung von n-haltigen heterozyklen in dermokosmetika
EP1903044A1 (en) 2006-09-14 2008-03-26 Novartis AG Adenosine Derivatives as A2A Receptor Agonists
EP2298772A1 (en) 2006-10-18 2011-03-23 Takeda Pharmaceutical Company Limited Fused heterocyclic compounds
US7772180B2 (en) 2006-11-09 2010-08-10 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
EP2441768A1 (en) 2006-11-13 2012-04-18 Eli Lilly & Co. Thienopyrimidinones for treatment of inflammatory disorders and cancers
WO2008063625A2 (en) 2006-11-20 2008-05-29 Adolor Corporation Pyridine compounds and methods of their use
CN101611007A (zh) 2006-12-20 2009-12-23 先灵公司 新颖的jnk抑制剂
DK2114925T3 (da) 2006-12-22 2012-05-29 Ind Res Ltd Azetidin-analoger af nucleosidase- og phosphorylase-inhibitorer
CA2676138A1 (en) 2007-01-26 2008-08-07 Irm Llc Compounds and compositions as kinase inhibitors
EP2073799A4 (en) 2007-03-12 2009-08-19 Vm Discovery Inc NOVEL ACTIVE SUBSTANCES FROM CALCIUMIONAL CHANNEL MODULATORS
CA2680783C (en) 2007-03-23 2012-04-24 Amgen Inc. Heterocyclic compounds and their uses
MX2009010050A (es) 2007-03-23 2009-10-12 Amgen Inc Derivados de quinolina o quinoxalina 3-sustituidos y su uso como inhibidores de fosfotidilinositol 3-cinasa (p13k).
HRP20160350T1 (hr) 2007-03-23 2016-05-06 Amgen Inc. Heterociklički spojevi i njihove uporabe
WO2008156513A2 (en) 2007-03-29 2008-12-24 University Of Connecticut Methods to protect skeletal muscle against injury
CN101636397B (zh) 2007-04-13 2012-06-13 中国人民解放军军事医学科学院毒物药物研究所 脲类化合物、其制备方法及其医药用途
AU2008238379A1 (en) 2007-04-13 2008-10-23 Sanofi-Aventis A transition metal catalyzed synthesis of N-aminoindoles
JP2010163361A (ja) 2007-04-27 2010-07-29 Dainippon Sumitomo Pharma Co Ltd キノリン誘導体
US7960353B2 (en) 2007-05-10 2011-06-14 University Of Kansas Novobiocin analogues as neuroprotective agents and in the treatment of autoimmune disorders
WO2008147852A1 (en) 2007-05-22 2008-12-04 Taigen Biotechnology Co., Ltd. Kinesin inhibitors
US7928111B2 (en) 2007-06-08 2011-04-19 Senomyx, Inc. Compounds including substituted thienopyrimidinone derivatives as ligands for modulating chemosensory receptors
US9603848B2 (en) 2007-06-08 2017-03-28 Senomyx, Inc. Modulation of chemosensory receptors and ligands associated therewith
ATE538120T1 (de) 2007-06-26 2012-01-15 Sanofi Sa Regioselektive, metallkatalysierte synthese annelierter benzimidazole und azabenzimidazole
EP2170274A1 (en) 2007-07-02 2010-04-07 Technion Research and Development Foundation, Ltd. Compositions, articles and methods comprising tspo ligands for preventing or reducing tobacco-associated damage
RU2345996C1 (ru) 2007-07-17 2009-02-10 Андрей Александрович Иващенко Аннелированные азагетероциклические амиды, включающие пиримидиновый фрагмент, способ их получения и применения
WO2009042294A2 (en) 2007-08-10 2009-04-02 Burnham Institute For Medical Research Tissue-nonspecific alkaline phosphatase (tnap) activators and uses thereof
CA2695583A1 (en) 2007-08-13 2009-02-19 Metabasis Therapeutics, Inc. Novel activators of glucokinase
JP5227965B2 (ja) 2007-10-03 2013-07-03 独立行政法人理化学研究所 ニトロトリアゾール誘導体、およびそれを用いる化合物の製造方法
BRPI0818426A2 (pt) 2007-10-15 2017-06-13 Astrazeneca Ab produto de combinação, uso de um produto de combinação, e, método para tratar câncer
JP5256693B2 (ja) 2007-10-31 2013-08-07 信越化学工業株式会社 酸化チタン系光触媒薄膜の製造法
WO2009062118A2 (en) * 2007-11-07 2009-05-14 Foldrx Pharmaceuticals, Inc. Modulation of protein trafficking
SG185996A1 (en) 2007-11-13 2012-12-28 Icos Corp Inhibitors of human phosphatidyl-inositol 3-kinase delta
AU2008338963A1 (en) 2007-12-13 2009-06-25 Sri International PPAR-delta ligands and methods of their use
US7960397B2 (en) 2007-12-28 2011-06-14 Institute Of Experimental Botany, Academy Of Sciences Of The Czech Republic 6,9-disubstituted purine derivatives and their use as cosmetics and cosmetic compositions
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
BRPI0906473A8 (pt) 2008-01-04 2016-02-10 Intellikine Inc Certas entidades químicas, composições e métodos
CN101938904A (zh) 2008-01-09 2011-01-05 PGx健康有限责任公司 用a2ar激动剂鞘内治疗神经性疼痛
CA2714516A1 (en) 2008-02-07 2009-08-13 Gilead Palo Alto, Inc. Abca-1 elevating compounds and the use thereof
US20110098267A1 (en) 2008-02-07 2011-04-28 Synta Pharmaceuticals Corporation Topical formulations for the treatment of psoriasis
TWI444384B (zh) 2008-02-20 2014-07-11 Gilead Sciences Inc 核苷酸類似物及其在治療惡性腫瘤上的用途
US8993580B2 (en) 2008-03-14 2015-03-31 Intellikine Llc Benzothiazole kinase inhibitors and methods of use
AU2009226024B2 (en) 2008-03-20 2012-07-12 Amgen Inc. Aurora kinase modulators and method of use
US20090312406A1 (en) 2008-06-12 2009-12-17 Hsing-Pang Hsieh Coumarin compounds and their use for treating viral infection
US20110224223A1 (en) 2008-07-08 2011-09-15 The Regents Of The University Of California, A California Corporation MTOR Modulators and Uses Thereof
MX2011000216A (es) 2008-07-08 2011-03-29 Intellikine Inc Inhibidores de cinasa y metodos para su uso.
JP2011528368A (ja) 2008-07-16 2011-11-17 シェーリング コーポレイション 二環式ヘテロ環誘導体およびｇｐｃｒモジュレーターとしてのその使用
US8450344B2 (en) 2008-07-25 2013-05-28 Aerie Pharmaceuticals, Inc. Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds
CA2737219C (en) 2008-08-11 2017-02-28 Tracy Keller Halofuginone analogs for inhibition of trna synthetases and uses thereof
AU2009298877A1 (en) 2008-09-23 2010-04-08 Georgetown University Viral and fungal inhibitors
WO2010036380A1 (en) 2008-09-26 2010-04-01 Intellikine, Inc. Heterocyclic kinase inhibitors
AU2009305669A1 (en) * 2008-10-16 2010-04-22 The Regents Of The University Of California Fused ring heteroaryl kinase inhibitors
US8476431B2 (en) 2008-11-03 2013-07-02 Itellikine LLC Benzoxazole kinase inhibitors and methods of use
US20110269779A1 (en) 2008-11-18 2011-11-03 Intellikine, Inc. Methods and compositions for treatment of ophthalmic conditions
CN101602768B (zh) 2009-07-17 2012-05-30 河南省农科院农副产品加工研究所 一种芝麻素和芝麻林素的提纯方法
US8980899B2 (en) * 2009-10-16 2015-03-17 The Regents Of The University Of California Methods of inhibiting Ire1

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2014525464A (ja) * 2011-09-02 2014-09-29 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア 置換ピラゾロ［３，４−ｄ］ピリミジンおよびその用途

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