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
abl
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Japanese (ja)
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JP2012505916A5 (OSRAM
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 Berkeley
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University of California San Diego UCSD
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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)
  • Hematology (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (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 (OSRAM) 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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Country Status (8)

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

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 (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2008520744A (ja) 2004-11-19 2008-06-19 ザ・レジェンツ・オブ・ザ・ユニバーシティ・オブ・カリフォルニア 抗炎症性ピラゾロピリミジン
EP2018167A4 (en) * 2006-05-15 2010-07-14 Irm Llc COMPOSITIONS AND METHODS AS INHIBITORS OF FGF RECEPTOR KINASES
WO2010006072A2 (en) 2008-07-08 2010-01-14 The Regents Of The University Of California Mtor modulators and uses thereof
JP5819195B2 (ja) * 2008-10-16 2015-11-18 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 融合環ヘテロアリールキナーゼ阻害剤
HRP20190016T1 (hr) 2009-08-17 2019-03-08 Intellikine, Llc Heterociklički spojevi i njihova upotreba
WO2011047384A2 (en) 2009-10-16 2011-04-21 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
EP2678018A4 (en) 2011-02-23 2015-09-30 Intellikine Llc COMBINATION OF CHINESE HEMMER AND USES THEREOF
KR101992311B1 (ko) 2011-05-04 2019-09-27 리젠 파마슈티컬스 소시에떼 아노님 단백질 키나아제의 조절제로서 신규한 화합물
PH12014500122A1 (en) 2011-07-13 2014-03-24 Pharmacyclics Inc Inhibitors of bruton's tyrosine kinase
RU2015115631A (ru) 2012-09-26 2016-11-20 Дзе Риджентс Оф Дзе Юниверсити Оф Калифорния Модулирование ire1
EP2912036A1 (en) 2012-10-04 2015-09-02 Pfizer Limited Pyrrolo[3,2-c]pyridine tropomyosin-related kinase inhibitors
KR101721884B1 (ko) 2014-08-01 2017-03-31 엘지전자 주식회사 방송신호 전송방법, 방송신호 수신방법, 방송신호 전송장치, 방송신호 수신장치
WO2016040806A1 (en) 2014-09-11 2016-03-17 The Regents Of The University Of California mTORC1 INHIBITORS
EP3430017B1 (en) 2016-03-17 2023-01-25 The Regents of The University of California Compositions and methods for treating parasitic diseases
CN109311894B (zh) 2016-06-21 2022-03-22 内尔维阿诺医学科学有限公司 作为激酶抑制剂的n-(取代的-苯基)-磺酰胺衍生物
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
US11518761B2 (en) 2017-08-17 2022-12-06 Vyera Pharmaceuticals, LLC CDPK1 inhibitors, compositions, and methods related thereto
CA3091142C (en) 2018-02-26 2023-04-11 Gilead Sciences, Inc. Substituted pyrrolizine compounds and uses thereof
CA3098692A1 (en) 2018-05-01 2019-11-07 Revolution Medicines, Inc. C40-, c28-, and c-32-linked rapamycin analogs as mtor inhibitors
WO2019212991A1 (en) 2018-05-01 2019-11-07 Revolution Medicines, Inc. C26-linked rapamycin analogs as mtor inhibitors
EP3801069A4 (en) 2018-06-01 2022-03-16 Cornell University MULTIPLE THERAPY FOR DISEASE OR DISORDER ASSOCIATED WITH PI3K
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
AU2021358123A1 (en) * 2020-10-05 2023-06-08 Enliven Inc. 5- and 6-azaindole compounds for inhibition of bcr-abl tyrosine kinases
IL302807A (en) 2020-11-18 2023-07-01 Deciphera Pharmaceuticals Llc Gcn2 and perk kinase inhibitors and methods of use thereof
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
AU2023275778A1 (en) 2022-05-25 2024-12-12 Revolution Medicines, Inc. Methods of treating cancer with an mtor inhibitor

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
US5506347A (en) 1993-02-03 1996-04-09 Gensia, Inc. Lyxofuranosyl analogues of adenosine
US5763597A (en) 1989-09-15 1998-06-09 Metabasis Therapeutics, 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
US5721356A (en) 1989-09-15 1998-02-24 Gensia, Inc. Orally active adenosine kinase inhibitors
US5795977A (en) 1989-09-15 1998-08-18 Metabasis Therapeutics, Inc. Water soluble adenosine kinase inhibitors
US5646128A (en) 1989-09-15 1997-07-08 Gensia, Inc. Methods for treating adenosine kinase related conditions
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
US5652366A (en) 1990-09-25 1997-07-29 Rhone-Poulenc Rorer Pharmaceuticals Inc. DI (1R)-(-)camphosulfonic acid) salt, preparation thereof and use thereof
EP0550631B1 (en) 1990-09-25 1997-01-02 Rhone-Poulenc Rorer International (Holdings) Inc. Compounds having antihypertensive and anti-ischemic properties
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
DE4204032A1 (de) 1992-02-12 1993-08-19 Boehringer Mannheim Gmbh Neue liponucleotide, deren herstellunmg sowie deren verwendung als antivirale arzneimittel
DE4204031A1 (de) 1992-02-12 1993-08-19 Boehringer Mannheim Gmbh Neue lipidphosphonsaeure-nucleosid-konjugate 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
WO1993022443A1 (en) 1992-04-24 1993-11-11 Sri International In vivo homologous sequence targeting in eukaryotic cells
DE69328440T3 (de) 1992-06-19 2009-05-07 Honeywell, Inc., Minneapolis Infrarot kamera mit thermoelektrischer temperaturstabilisierung
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
TW444018B (en) * 1992-12-17 2001-07-01 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
WO1995012588A1 (en) 1993-11-05 1995-05-11 Biochem Pharma Inc. Antineoplastic heteronaphthoquinones
US5679683A (en) 1994-01-25 1997-10-21 Warner-Lambert Company Tricyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family
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
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
NZ293249A (en) * 1994-09-29 1999-04-29 Novartis Ag 4-amino-5,7-diaryl-pyrrolo[2,3-d]pyrimidines and their use
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
AU711592B2 (en) 1995-04-03 1999-10-14 Novartis Ag Pyrazole derivatives and processes for the preparation thereof
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
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
WO1996037777A1 (en) 1995-05-23 1996-11-28 Nelson Randall W Mass spectrometric immunoassay
US5665721A (en) 1995-06-07 1997-09-09 Abbott Laboratories Heterocyclic substituted cyclopentane compounds
CZ297975B6 (cs) 1995-06-07 2007-05-09 G. D. Searle & Co. Farmaceutická kombinace antagonisty receptoru proangiotensin II a epoxymexrenonu pro lécení kardiovaskulárních poruch
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
ES2175098T3 (es) 1995-06-07 2002-11-16 Searle & Co Terapia de combinacion de espironolactona y antagonista de angiotensina hi para el tratamiento del fallo cardiaco congestivo.
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
US5914488A (en) 1996-03-05 1999-06-22 Mitsubishi Denki Kabushiki Kaisha Infrared detector
GB9611460D0 (en) 1996-06-01 1996-08-07 Ludwig Inst Cancer Res Novel lipid kinase
WO1997048694A1 (en) 1996-06-20 1997-12-24 Board Of Regents, The University Of Texas System Compounds and methods for providing pharmacologically active preparations and uses thereof
US5919808A (en) 1996-10-23 1999-07-06 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
US6342514B1 (en) 1996-10-23 2002-01-29 Zymogenetics, Inc. Compositions and methods for treating bone deficit conditions
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
US6153631A (en) 1996-10-23 2000-11-28 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
US5990169A (en) 1996-10-23 1999-11-23 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
US5858753A (en) 1996-11-25 1999-01-12 Icos Corporation Lipid kinase
ATE346085T1 (de) 1996-12-06 2006-12-15 Vertex Pharma Inhibitoren des interleukin-1-beta konvertierenden enzyms
US6093737A (en) 1996-12-30 2000-07-25 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
JP3784076B2 (ja) 1997-02-07 2006-06-07 プリンストン ユニヴァーシティ 変性ヌクレオチド三燐酸基質を利用できる組み換えタンパクキナーゼ
CA2283961A1 (en) 1997-03-19 1998-09-24 Basf Aktiengesellschaft Pyrrolo[2,3d]pyrimidines and their use as tyrosine kinase inhibitors
US7863444B2 (en) * 1997-03-19 2011-01-04 Abbott Laboratories 4-aminopyrrolopyrimidines as kinase inhibitors
AU7449598A (en) 1997-05-23 1998-12-11 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
EP1020445B1 (en) 1997-10-02 2008-08-13 Eisai R&D Management 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
US6127121A (en) 1998-04-03 2000-10-03 Epoch Pharmaceuticals, Inc. Oligonucleotides containing pyrazolo[3,4-D]pyrimidines for hybridization and mismatch discrimination
US7715989B2 (en) 1998-04-03 2010-05-11 Elitech Holding B.V. Systems and methods for predicting oligonucleotide melting temperature (TmS)
JP2000072773A (ja) 1998-08-28 2000-03-07 Zeria Pharmaceut Co Ltd プリン誘導体
SK3852001A3 (en) 1998-09-18 2003-03-04 Basf Ag 4-Aminopyrrolopyrimidines as kinase inhibitors
US6713474B2 (en) * 1998-09-18 2004-03-30 Abbott Gmbh & Co. Kg Pyrrolopyrimidines as therapeutic agents
JP2002526500A (ja) * 1998-09-18 2002-08-20 ビーエーエスエフ アクチェンゲゼルシャフト プロテインキナーゼ阻害剤としてのピロロピリミジン
DE1140938T1 (de) 1999-01-11 2003-01-09 Princeton University, Princeton Kinase-inhibitoren mit hoher affinität zur ziel detektion und ihre verwendung
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
CN1636005A (zh) 1999-06-03 2005-07-06 克诺尔股份有限公司 苯并噻嗪酮和苯并噁嗪酮化合物
US6387894B1 (en) 1999-06-11 2002-05-14 Pfizer Inc. Use of CRF antagonists and renin-angiotensin system inhibitors
TWI262914B (en) 1999-07-02 2006-10-01 Agouron Pharma Compounds and pharmaceutical compositions for inhibiting protein kinases
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
GB9919588D0 (en) 1999-08-18 1999-10-20 Hoechst Schering Agrevo Gmbh Fungicidal compounds
JP4831906B2 (ja) 1999-08-27 2011-12-07 ケモセントリックス， インコーポレイテッド Ｃｘｃｒ３機能を調節するための複素環式化合物および方法
WO2001019800A2 (en) 1999-09-16 2001-03-22 Curis, Inc. Mediators of hedgehog signaling pathways, compositions and uses related thereto
PT1212327E (pt) * 1999-09-17 2004-01-30 Abbott Gmbh & Co Kg Pirazolopirimidinas como agentes terapeuticos
US6921763B2 (en) 1999-09-17 2005-07-26 Abbott Laboratories Pyrazolopyrimidines as therapeutic agents
US6506769B2 (en) 1999-10-06 2003-01-14 Boehringer Ingelheim Pharmaceuticals, Inc. Heterocyclic compounds useful as inhibitors of tyrosine kinases
WO2001025238A2 (en) 1999-10-06 2001-04-12 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
EP1268257B1 (de) * 2000-03-27 2006-07-26 Continental Teves AG & Co. oHG Fahrzeuglenkung und achslenkmodul für eine fahrzeuglenkung
AU2001287268A1 (en) * 2000-03-29 2001-10-08 Knoll Gesellschaft Mit Beschraenkter Haftung Method of identifying inhibitors of tie-2
WO2001072751A1 (en) * 2000-03-29 2001-10-04 Knoll Gesellschaft Mit Beschraenkter Haftung Pyrrolopyrimidines as tyrosine kinase inhibitors
US7115653B2 (en) 2000-03-30 2006-10-03 Curis, Inc. Small organic molecule regulators of cell proliferation
US6613798B1 (en) 2000-03-30 2003-09-02 Curis, Inc. Small organic molecule regulators of cell proliferation
KR100785363B1 (ko) 2000-04-25 2007-12-18 이코스 코포레이션 인간 포스파티딜-이노시톨 3-키나제 델타의 억제제
US6667300B2 (en) 2000-04-25 2003-12-23 Icos Corporation Inhibitors of human phosphatidylinositol 3-kinase delta
US6777439B2 (en) 2000-05-30 2004-08-17 Advanced Research & Technology Institute, Inc. 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
AU2002213467A1 (en) 2000-10-11 2002-04-22 Chemocentryx, Inc. Modulation of ccr4 function
WO2002030944A2 (en) 2000-10-11 2002-04-18 Applera Corporation Fluorescent nucleobase conjugates having anionic linkers
US6890747B2 (en) 2000-10-23 2005-05-10 Warner-Lambert Company Phosphoinositide 3-kinases
BR0116096A (pt) 2000-12-11 2005-10-18 Tularik Inc Composto, composição farmacêutica, e, métodos para tratar uma condição ou doença inflamatória ou imune em um paciente, para tratar uma condição ou doença mediada por cxcr3 em um paciente, e para a modulação da função de cxcr3 em uma célula
US7157487B2 (en) 2000-12-28 2007-01-02 Daiichi Pharmaceutical Co., Ltd. Vla-4 inhibitors
US7105499B2 (en) 2001-01-22 2006-09-12 Merck & Co., Inc. Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase
HUP0400726A3 (en) 2001-01-22 2007-05-29 Merck & Co Inc Nucleoside derivatives as inhibitors of rna-dependent rna viral polymerase
CA2439263C (en) * 2001-03-02 2012-10-23 Frank Becker Three hybrid assay system
MXPA03008560A (es) 2001-03-22 2004-06-30 Abbot Gmbh & Co Kg Pirazolopirimidinas como agentes terapeuticos.
US7250569B2 (en) 2001-04-26 2007-07-31 New York University School Of Medicine Method for dissolving nanostructural materials
US6664269B2 (en) 2001-05-08 2003-12-16 Maybridge Plc Isoquinolinone derivatives
US7144903B2 (en) 2001-05-23 2006-12-05 Amgen Inc. CCR4 antagonists
EP1470119A4 (en) 2001-06-13 2005-10-19 Genesoft Pharmaceuticals Inc BENZOTHIOPHENE COMPOUNDS WITH ANTI-INFECTIOUS ACTIVITY
WO2002101007A2 (en) 2001-06-13 2002-12-19 Genesoft Pharmaceuticals, Inc Antipathogenic benzamide compounds
US6777425B2 (en) 2001-06-13 2004-08-17 Genesoft Pharmaceuticals, Inc. Isoquinoline compounds having antiinfective activity
AU2002315389A1 (en) 2001-06-21 2003-01-08 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
AU2002327422A1 (en) * 2001-08-03 2003-03-18 Abbott Laboratories Method of identifying inhibitors of lck
EP2181985B1 (en) 2001-08-10 2011-10-26 Shionogi & Co., Ltd. Antiviral Agent
US20030199516A1 (en) 2001-09-13 2003-10-23 Genesoft, Inc. Methods of treating infection by drug resistant bacteria
US7101884B2 (en) 2001-09-14 2006-09-05 Merck & Co., Inc. Tyrosine kinase inhibitors
AUPR769501A0 (en) 2001-09-14 2001-10-11 Biomolecular Research Institute Limited Cytokine receptor 1
TWI330183B (OSRAM) 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
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
EP1465869B1 (en) 2001-12-21 2013-05-15 Exelixis Patent Company LLC Modulators of lxr
US7064218B2 (en) 2001-12-26 2006-06-20 Genelabs Technologies, Inc. Aromatic compounds and poly(oxyalkylene) containing aromatic compounds possessing antibacterial, antifungal or antitumor activity
US7414036B2 (en) 2002-01-25 2008-08-19 Muscagen Limited Compounds useful as A3 adenosine receptor agonists
WO2003082341A1 (en) 2002-03-22 2003-10-09 Cellular Genomics, Inc. AN IMPROVED FORMULATION OF CERTAIN PYRAZOLO[3,4-d] PYRIMIDINES AS KINASE MODULATORS
AU2003219088A1 (en) 2002-03-26 2003-10-08 Zentopharm Gmbh Fredericamycin derivatives
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
EP1507535A1 (en) 2002-04-26 2005-02-23 Pfizer Products Inc. Pyrimidine-2,4,6-trione metallo-proteinase inhibitors
US6794562B2 (en) 2002-05-01 2004-09-21 Stine Seed Farm, Inc. Soybean cultivar 0332143
CA2485343A1 (en) 2002-05-23 2004-05-13 Merck & Co., Inc. Mitotic kinesin inhibitors
US7041676B2 (en) 2002-06-14 2006-05-09 Cytokinetics, Inc. Compounds, compositions, and methods
US7265111B2 (en) 2002-06-27 2007-09-04 Sanofi-Aventis Deutschland Gmbh Adenosine analogues and their use as pharmaceutical agents
CA2488642C (en) 2002-06-27 2011-09-06 Dharma Rao Polisetti Aryl carbonyl derivatives as glucokinase activators
CN1678311A (zh) 2002-06-27 2005-10-05 诺沃挪第克公司 用作治疗剂的芳基羰基衍生物
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
JP2006503008A (ja) 2002-08-13 2006-01-26 ワーナー−ランバート カンパニー リミティド ライアビリティー カンパニー マトリクスメタロプロテイナーゼ阻害物質としての４−ヒドロキシキノリン誘導体
CA2495661C (en) 2002-08-16 2011-06-14 Kinacia Pty Ltd. Inhibition 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
ES2361924T3 (es) 2002-12-20 2011-06-24 X-Ceptor Therapeutics, Inc. Derivados de isoquinolinona y su uso como agentes terapéuticos.
US7247736B2 (en) 2002-12-23 2007-07-24 4Sc Ag Method of identifying inhibitors of DHODH
US7071355B2 (en) 2002-12-23 2006-07-04 4 Sc Ag Compounds as anti-inflammatory, immunomodulatory and anti-proliferatory agents
US7365094B2 (en) 2002-12-23 2008-04-29 4Sc Ag 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
US20040242566A1 (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
WO2004089297A2 (en) 2003-04-02 2004-10-21 Suntory Pharmaceutical Research Laboratories, Llc Compounds and methods for treatment of thrombosis
US20050008640A1 (en) * 2003-04-23 2005-01-13 Wendy Waegell 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
EP1680125A1 (en) 2003-07-02 2006-07-19 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
WO2005014532A1 (en) 2003-08-08 2005-02-17 Transtech Pharma, Inc. Aryl and heteroaryl compounds, compositions and methods of use
US7208601B2 (en) 2003-08-08 2007-04-24 Mjalli Adnan M M Aryl and heteroaryl compounds, compositions, and methods of use
WO2005016348A1 (en) 2003-08-14 2005-02-24 Icos Corporation Method of inhibiting immune responses stimulated by an endogenous factor
WO2005016349A1 (en) 2003-08-14 2005-02-24 Icos Corporation Methods of inhibiting leukocyte accumulation
AU2004264419B2 (en) 2003-08-15 2009-01-15 Irm Llc 6-substituted anilino purines as RTK inhibitors
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
AU2004289303A1 (en) 2003-11-10 2005-05-26 Synta Pharmaceuticals, Corp. Fused heterocyclic compounds
JP2007511596A (ja) * 2003-11-17 2007-05-10 ファイザー・プロダクツ・インク 癌の治療において有用なピロロピリミジン化合物
EP1692112A4 (en) 2003-12-08 2008-09-24 Cytokinetics Inc COMPOUNDS, COMPOSITIONS, AND METHODS
AU2004308974A1 (en) 2003-12-22 2005-07-14 Gilead Sciences, Inc. Kinase inhibitor phosphonate conjugates
ES2339670T3 (es) 2003-12-23 2010-05-24 Novartis Ag Inhibidores heterociclicos biciclicos de la quinasa p-38.
CA2552664A1 (en) 2004-01-08 2005-07-28 Michigan State University Methods for treating and preventing hypertension and hypertension-related disorders
CA2553724A1 (en) 2004-02-03 2005-08-18 Abbott Laboratories Aminobenzoxazoles as therapeutic agents
AU2005212092B2 (en) 2004-02-13 2011-01-20 Msd K.K. Fused-ring 4-oxopyrimidine derivative
US20050187418A1 (en) 2004-02-19 2005-08-25 Small Brooke L. Olefin oligomerization
EP1720874A4 (en) 2004-02-24 2010-03-03 Bioaxone Therapeutique Inc 4-SUBSTITUTED PIPERIDINE DERIVATIVES
JP2007523938A (ja) 2004-02-27 2007-08-23 エフ．ホフマン−ラ　ロシュ　アーゲー ピラゾールの縮合誘導体
DE602005014964D1 (de) 2004-04-02 2009-07-30 Osi Pharm Inc Mit einem 6,6-bicyclischen ring substituierte heterobicyclische proteinkinaseinhibitoren
TW200538453A (en) * 2004-04-26 2005-12-01 Bristol Myers Squibb Co Bicyclic heterocycles as kinase inhibitors
CA2564085C (en) 2004-04-30 2013-04-02 Takeda Pharmaceutical Company Limited Heterocyclic amide compound and use thereof as an mmp-13 inhibitor
DE102004022897A1 (de) 2004-05-10 2005-12-08 Bayer Cropscience Ag Azinyl-imidazoazine
WO2005113556A1 (en) 2004-05-13 2005-12-01 Icos Corporation Quinazolinones as inhibitors of human phosphatidylinositol 3-kinase delta
EP1750714A1 (en) 2004-05-13 2007-02-14 Vanderbilt University Phosphoinositide 3-kinase delta selective inhibitors for inhibiting angiogenesis
JP2008500338A (ja) 2004-05-25 2008-01-10 イコス・コーポレイション 造血細胞の異常増殖を治療及び／又は予防する方法
CA2566160C (en) * 2004-05-27 2011-01-18 Pfizer Products Inc. Pyrrolopyrimidine derivatives useful in cancer treatment
CA2569406A1 (en) 2004-06-04 2005-12-22 Icos Corporation Methods for treating mast cell disorders
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
US7608594B2 (en) 2004-11-03 2009-10-27 University Of Kansas Novobiocin analogues as anticancer agents
US8212012B2 (en) 2004-11-03 2012-07-03 University Of Kansas Novobiocin analogues having modified sugar moieties
US8212011B2 (en) 2004-11-03 2012-07-03 University Of Kansas Novobiocin analogues
US7622451B2 (en) 2004-11-03 2009-11-24 University Of Kansas Novobiocin analogues as neuroprotective agents and in the treatment of autoimmune disorders
GB0425035D0 (en) * 2004-11-12 2004-12-15 Novartis Ag Organic compounds
JP2008520744A (ja) 2004-11-19 2008-06-19 ザ・レジェンツ・オブ・ザ・ユニバーシティ・オブ・カリフォルニア 抗炎症性ピラゾロピリミジン
CA2588607A1 (en) 2004-11-23 2006-06-01 Ptc Therapeutics, Inc. Carbazole, carboline and indole derivatives useful in the inhibition of vegf production
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
US7579348B2 (en) 2005-02-25 2009-08-25 Pgxhealth, 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
AU2006227447A1 (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
CN101184395A (zh) 2005-04-06 2008-05-21 Irm责任有限公司 包含二芳基胺的化合物和组合物及其作为类固醇激素核受体调节剂的用途
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
ES2543714T3 (es) 2005-06-22 2015-08-21 Chemocentryx, Inc. Compuestos de azaindazol y métodos de uso
WO2007002701A2 (en) 2005-06-27 2007-01-04 Amgen Inc. Anti-inflammatory aryl nitrile compounds
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
JP2009500437A (ja) 2005-07-11 2009-01-08 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
WO2007025090A2 (en) 2005-08-25 2007-03-01 Kalypsys, Inc. Heterobicyclic and - tricyclic inhibitors of mapk/erk kinase
KR101011957B1 (ko) 2005-08-25 2011-01-31 에프. 호프만-라 로슈 아게 Ｐ３８ ｍαｐ 키나아제 저해제 및 이의 사용 방법
US20080318942A1 (en) 2005-09-01 2008-12-25 Bioagency Ag Fredericamycin Derivatives
BRPI0616459A2 (pt) 2005-09-29 2011-06-21 Wyeth Corp compostos das fórmulas i, ii, e iii; processos para o tratamento ou para a prevenção de: um estado de saúde com melhora devido à recaptação de monoamina; pelo menos um sintoma vasomotor; pelo menos um distúrbio depressivo; pelo menos uma disfunção sexual; para a prevenção de dor; de distúrbio gastrointestinal ou genitourinário; de sìndrome de fadiga crÈnica; de sìndrome de fibromialgia; de esquizofrenia; e uso de um composto
PT2385053E (pt) 2005-11-17 2013-12-17 Osi Pharm Inc Intermediários para a preparação de compostos bicíclicos condensados como inibidores mtor
US20090088452A1 (en) 2005-11-22 2009-04-02 Coleman Paul J 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
WO2007075554A2 (en) 2005-12-19 2007-07-05 Osi Pharmaceuticals, Inc. Combination of igfr inhibitor and anti-cancer agent
TW201307354A (zh) 2005-12-29 2013-02-16 Abbott Lab 蛋白質激酶抑制劑
WO2007089669A2 (en) 2006-01-26 2007-08-09 Wyeth Processes for the preparation of compounds which modulate cell proliferation
RU2008139599A (ru) 2006-03-07 2010-04-20 Эррэй Биофарма Инк. (Us) Гетеробициклические производные пиразола и способы их применения
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
HUE067285T2 (hu) 2006-03-24 2024-10-28 Bioverativ Therapeutics Inc PC5 mint IX-es faktor propeptidet feldolgozó enzim
EA200870385A1 (ru) 2006-03-29 2009-04-28 Фолдркс Фармасьютикалз, Инк. Ингибирование токсичности альфа-синуклеина
KR20130087054A (ko) 2006-04-04 2013-08-05 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
GB0607950D0 (en) 2006-04-21 2006-05-31 Novartis Ag Organic compounds
AR060607A1 (es) 2006-04-21 2008-07-02 Novartis Ag Derivados de purina,composiciones farmaceuticas que los contienen, metodo de preparacion y usos en enfermedades obstructivas o inflamatorias de las vias respiratorias.
GB0607948D0 (en) 2006-04-21 2006-05-31 Novartis Ag Organic compounds
WO2007125310A2 (en) 2006-04-25 2007-11-08 Astex Therapeutics Limited Pharmaceutical combinations of pk inhibitors and other active agents
WO2007125315A2 (en) 2006-04-25 2007-11-08 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
CA2658462C (en) 2006-07-20 2011-09-27 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)
CA2661436A1 (en) 2006-08-24 2008-02-28 Serenex, Inc. Isoquinoline, quinazoline and phthalazine derivatives
WO2008025755A1 (de) 2006-09-01 2008-03-06 Basf Se Verwendung von n-haltigen heterozyklen in dermokosmetika
US7956064B2 (en) 2006-09-01 2011-06-07 Cylene Pharmaceuticals, Inc. Fused tricyclic compounds as serine-threonine protein kinase and PARP modulators
EP1903044A1 (en) 2006-09-14 2008-03-26 Novartis AG Adenosine Derivatives as A2A Receptor Agonists
EP2077267A4 (en) 2006-10-18 2010-04-07 Takeda Pharmaceutical CONDENSED HETEROCYCLIC COMPOUND
US7772180B2 (en) 2006-11-09 2010-08-10 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
CN101605797A (zh) 2006-11-13 2009-12-16 伊莱利利公司 治疗炎症疾病和癌症的噻吩并嘧啶酮
WO2008063625A2 (en) 2006-11-20 2008-05-29 Adolor Corporation Pyridine compounds and methods of their use
JP5178738B2 (ja) 2006-12-20 2013-04-10 メルク・シャープ・アンド・ドーム・コーポレーション 新規なｊｎｋ阻害剤
WO2008079028A1 (en) 2006-12-22 2008-07-03 Industrial Research Limited Azetidine analogues of nucleosidase and phosphorylase inhibitors
KR20090112732A (ko) 2007-01-26 2009-10-28 아이알엠 엘엘씨 플라스모듐 관련 질환의 치료를 위한 키나제 억제제로서의 퓨린 화합물 및 조성물
US8586619B2 (en) 2007-03-12 2013-11-19 Vm Therapeutics Llc Agents of calcium ion channel modulators
US7705018B2 (en) 2007-03-23 2010-04-27 Amgen Inc. Substituted quinolines and their uses in treatment of inflammatory and related conditions
US7919498B2 (en) 2007-03-23 2011-04-05 Amgen Inc. Substituted pyrazolo[3,4-d]pyrimidines as PI3K inhibitors
AU2008231304B2 (en) 2007-03-23 2011-05-12 Amgen Inc. Heterocyclic compounds and their uses
US7867983B2 (en) 2007-03-29 2011-01-11 The 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
TW200902016A (en) 2007-05-22 2009-01-16 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
BRPI0813273A2 (pt) 2007-06-26 2014-12-30 Sanofi Aventis Síntese catalisada por metal regiosseletivo de benzimidazóis e azabenzimidazóis anelados
WO2009004621A1 (en) 2007-07-02 2009-01-08 Technion Research & 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
EP2190466A4 (en) 2007-08-10 2011-12-21 Burnham Inst Medical Research Tissue-specific alkaline phosphatase (TNAP) activators and their use
MX2010001784A (es) 2007-08-13 2010-03-15 Metabasis Therapeutics Inc Activadores novedosos de la glucocinasa.
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
JP2011503103A (ja) * 2007-11-07 2011-01-27 フォールドアールエックス ファーマシューティカルズ インコーポレーティッド タンパク質輸送の調節方法
CA2716334A1 (en) 2007-11-13 2009-05-22 Icos Corporation Inhibitors of human phosphatidyl-inositol 3-kinase delta
US20090163481A1 (en) 2007-12-13 2009-06-25 Murphy Brian J 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
MX358640B (es) 2008-01-04 2018-08-29 Intellikine Llc Isoquinolin-1 (2h) -onas y tieno [2,3-d]pirimidin-4(3h) -onas substituidas, y metodos de uso de las mismas.
JP2011509305A (ja) 2008-01-09 2011-03-24 ピージーエックスヘルス、リミテッド、ライアビリティー、カンパニー Ａ２ａｒアゴニストによる神経障害性疼痛の髄腔内治療
CA2714516A1 (en) 2008-02-07 2009-08-13 Gilead Palo Alto, Inc. Abca-1 elevating compounds and the use thereof
WO2009100406A2 (en) 2008-02-07 2009-08-13 Synta Pharmaceuticals Corp. 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
WO2009114874A2 (en) 2008-03-14 2009-09-17 Intellikine, Inc. Benzothiazole kinase inhibitors and methods of use
MX2010010151A (es) 2008-03-20 2010-10-25 Amgen Inc Moduladores de cinasa aurora y metodo de uso.
US20090312406A1 (en) 2008-06-12 2009-12-17 Hsing-Pang Hsieh Coumarin compounds and their use for treating viral infection
WO2010006072A2 (en) 2008-07-08 2010-01-14 The Regents Of The University Of California Mtor modulators and uses thereof
US9096611B2 (en) 2008-07-08 2015-08-04 Intellikine Llc Kinase inhibitors and methods of use
US20110118286A1 (en) 2008-07-16 2011-05-19 Santhosh Francis Neelamkavil Bicyclic heterocycle derivatives and their use as gpcr modulators
US8450344B2 (en) 2008-07-25 2013-05-28 Aerie Pharmaceuticals, Inc. Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds
WO2010019210A2 (en) 2008-08-11 2010-02-18 President And Fellows Of Harvard College Halofuginone analogs for inhibition of trna synthetases and uses thereof
AU2009298877A1 (en) 2008-09-23 2010-04-08 Georgetown University Viral and fungal inhibitors
US8703778B2 (en) 2008-09-26 2014-04-22 Intellikine Llc Heterocyclic kinase inhibitors
JP5819195B2 (ja) * 2008-10-16 2015-11-18 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 融合環ヘテロアリールキナーゼ阻害剤
US8476431B2 (en) 2008-11-03 2013-07-02 Itellikine LLC Benzoxazole kinase inhibitors and methods of use
WO2010059593A1 (en) 2008-11-18 2010-05-27 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
WO2011047384A2 (en) * 2009-10-16 2011-04-21 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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