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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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
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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 Berkeley
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University of California San Diego UCSD
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs 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)

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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 (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
CN101460175A (zh) * 2006-05-15 2009-06-17 Irm责任有限公司 用于fgf受体激酶抑制剂的组合物和方法
US20110224223A1 (en) 2008-07-08 2011-09-15 The Regents Of The University Of California, A California Corporation MTOR Modulators and Uses Thereof
ES2570429T3 (es) * 2008-10-16 2016-05-18 Univ California Inhibidores de heteroaril quinasa de anillo condensado
NZ598220A (en) 2009-08-17 2014-02-28 Intellikine Llc Heterocyclic compounds and uses thereof
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
JP6130305B2 (ja) 2011-02-23 2017-05-17 インテリカイン, エルエルシー キナーゼ阻害剤の組み合わせおよびそれらの使用
PH12013502240B1 (en) 2011-05-04 2018-06-27 Rhizen Pharmaceuticals Sa Novel compounds as modulators of protein kinase
KR20140048968A (ko) 2011-07-13 2014-04-24 파마시클릭스, 인코포레이티드 브루톤형 티로신 키나제의 억제제
WO2014052669A1 (en) 2012-09-26 2014-04-03 The Regents Of The University Of California Modulation of ire1
JP2015531395A (ja) 2012-10-04 2015-11-02 ファイザー・リミテッドPfizer Limited ピロロ[3,2−c]ピリジントロポミオシン関連キナーゼ阻害剤
EP3026918B1 (en) 2014-08-01 2019-02-27 LG Electronics Inc. Broadcast signal transmission method and broadcast signal transmission apparatus using encapsulation in link layer packets
CA2960992C (en) 2014-09-11 2024-04-09 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
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
TW201920184A (zh) * 2017-08-17 2019-06-01 美國華盛頓大學 Cdpk1抑制劑、組合物及與其相關之方法
KR102526964B1 (ko) 2018-02-26 2023-04-28 길리애드 사이언시즈, 인코포레이티드 Hbv 복제 억제제로서의 치환된 피롤리진 화합물
CR20240382A (es) 2018-05-01 2025-08-29 Revolution Medicines Inc ANÁLOGOS DE RAPAMICINA A C40, C28 Y C32 COMO INHIBIDORES DE MTOR (Divisional 2020-578)
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
US11767321B2 (en) * 2020-10-05 2023-09-26 Enliven 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
WO2022261352A1 (en) * 2021-06-09 2022-12-15 Icahn School Of Medicine At Mount Sinai Perfluoroalkane substituted pyrazolo[3,4-d]pyrimidin and pyrrolo[2,3-d]pyrimidin compounds and uses thereof
JP2025522296A (ja) 2022-05-25 2025-07-15 レヴォリューション・メディスンズ,インコーポレイテッド mTOR阻害剤によりがんを処置する方法

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
US5763596A (en) 1989-09-15 1998-06-09 Metabasis Therapeutics, Inc. C-4' modified adenosine kinase inhibitors
US5795977A (en) 1989-09-15 1998-08-18 Metabasis Therapeutics, Inc. Water soluble adenosine kinase inhibitors
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
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
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
US5652366A (en) 1990-09-25 1997-07-29 Rhone-Poulenc Rorer Pharmaceuticals Inc. DI (1R)-(-)camphosulfonic acid) salt, preparation thereof and use thereof
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.
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
JPH07506252A (ja) 1992-04-24 1995-07-13 エス・アール・アイ・インターナシヨナル 真核細胞内でのイン・ビボ相同配列ターゲッティング
WO1994000950A1 (en) 1992-06-19 1994-01-06 Honeywell Inc. Infrared camera with thermoelectric temperature stabilization
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
WO1995012588A1 (en) 1993-11-05 1995-05-11 Biochem Pharma Inc. Antineoplastic heteronaphthoquinones
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
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
ES2157344T3 (es) * 1994-09-29 2001-08-16 Novartis Ag Pirrolo(2,3-d)pirimidinas y su uso.
US6323201B1 (en) 1994-12-29 2001-11-27 The Regents Of The University Of California Compounds for inhibition of ceramide-mediated signal transduction
ATE195123T1 (de) 1995-04-03 2000-08-15 Novartis Erfind Verwalt Gmbh Pyrazolderivate und verfahren zu deren herstellung
US6312894B1 (en) 1995-04-03 2001-11-06 Epoch Pharmaceuticals, Inc. Hybridization and mismatch discrimination using oligonucleotides conjugated to minor groove binders
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
IL122246A (en) 1995-06-07 2004-06-01 Searle & Co Combination of spironolactone and angiotensin II antagonist for the treatment of heart failure
US5665721A (en) 1995-06-07 1997-09-09 Abbott Laboratories Heterocyclic substituted cyclopentane compounds
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
JPH11507627A (ja) 1995-06-07 1999-07-06 ジー.ディー.サール アンド カンパニー 充血性心不全症を処置するためのエポキシ−ステロイド系アルドステロン拮抗物質とアンギオテンシンii拮抗物質との組合せ治療
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
DE19603576A1 (de) 1996-02-01 1997-08-07 Bayer Ag Acylierte 4-Amino und 4-Hydrazinopyrimidine
CH690773A5 (de) 1996-02-01 2001-01-15 Novartis Ag Pyrrolo(2,3-d)pyrimide und ihre Verwendung.
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
KR20000022040A (ko) 1996-06-20 2000-04-25 보오드 오브 리젠츠, 더 유니버시티 오브 텍사스 시스템 약학적 활성 제제를 제공하기 위한 화합물, 방법 및 그의 용도
US5948776A (en) 1996-10-23 1999-09-07 Zymogenetic, 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
US5965573A (en) 1996-10-23 1999-10-12 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
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
US6153631A (en) 1996-10-23 2000-11-28 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
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
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
US7863444B2 (en) 1997-03-19 2011-01-04 Abbott Laboratories 4-aminopyrrolopyrimidines as kinase inhibitors
AU748884B2 (en) 1997-03-19 2002-06-13 Abbott Gmbh & Co. Kg Pyrrolo(2,3d)pyrimidines and their use as tyrosine kinase inhibitors
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
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
US6713474B2 (en) * 1998-09-18 2004-03-30 Abbott Gmbh & Co. Kg Pyrrolopyrimidines as therapeutic agents
CN1326457A (zh) * 1998-09-18 2001-12-12 巴斯福股份公司 作为激酶抑制剂的4-氨基吡咯并嘧啶
PL346700A1 (en) * 1998-09-18 2002-02-25 Basf Ag Pyrrolopyrimidines as protein kinase inhibitors
ES2206191T3 (es) 1999-01-11 2004-05-16 Princeton University Inhibidores de alta afinidad para validacion de dianas y usos de los mismos.
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
AU5179000A (en) 1999-06-03 2000-12-28 Basf Aktiengesellschaft 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
WO2001016114A2 (en) 1999-08-27 2001-03-08 Chemocentryx, Inc. Heterocyclic compounds and methods for modulating cxcr3 function
ATE286033T1 (de) 1999-09-16 2005-01-15 Curis Inc Vermittler von igel signalwegen, deren zusammenstellungen und verwendungen
CA2385747A1 (en) * 1999-09-17 2001-03-22 Gavin C. Hirst Pyrazolopyrimidines as therapeutic agents
US6921763B2 (en) * 1999-09-17 2005-07-26 Abbott Laboratories Pyrazolopyrimidines as therapeutic agents
MXPA02003364A (es) 1999-10-06 2002-08-23 Boehringer Ingelheim Pharma Compuestos heterociclicos utiles como inhibidores de las cinasas de tirosina.
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
EP1268257B1 (de) * 2000-03-27 2006-07-26 Continental Teves AG & Co. oHG Fahrzeuglenkung und achslenkmodul für eine fahrzeuglenkung
WO2001072778A2 (en) * 2000-03-29 2001-10-04 Knoll Gesellschaft Mit Beschraenkter Haftung Method of identifying inhibitors of tie-2
AU2000240570A1 (en) * 2000-03-29 2001-10-08 Knoll Gesellschaft Mit Beschraenkter Haftung Pyrrolopyrimidines as tyrosine kinase inhibitors
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
EP1278748B1 (en) 2000-04-25 2011-03-23 ICOS Corporation Inhibitors of human phosphatidyl-inositol 3-kinase delta
US6667300B2 (en) 2000-04-25 2003-12-23 Icos Corporation Inhibitors of human phosphatidylinositol 3-kinase delta
WO2001091699A2 (en) 2000-05-30 2001-12-06 Advanced Research & Technology Institute Compositions and methods for identifying agents which modulate pten function and pi-3 kinase pathways
KR20030011371A (ko) 2000-06-27 2003-02-07 진랩스 테크놀러지스, 인크. 항세균, 항진균 또는 항암 활성을 갖는 신규 화합물
US6534691B2 (en) 2000-07-18 2003-03-18 E. I. Du Pont De Nemours And Company Manufacturing process for α-olefins
WO2002030944A2 (en) 2000-10-11 2002-04-18 Applera Corporation Fluorescent nucleobase conjugates having anionic linkers
WO2002030358A2 (en) 2000-10-11 2002-04-18 Tularik Inc. Modulation of ccr4 function
US6890747B2 (en) 2000-10-23 2005-05-10 Warner-Lambert Company Phosphoinositide 3-kinases
SK8752003A3 (en) 2000-12-11 2003-11-04 Tularik Inc CXCR3 antagonists, pharmaceutical composition comprising same and use thereof
MXPA03005838A (es) 2000-12-28 2003-09-10 Daichi Pharmaceutical Co Ltd Inhibidores de antigenos de aparicion muy tardia-4.
EA007491B1 (ru) 2001-01-22 2006-10-27 Мерк Энд Ко., Инк. Производные нуклеозидов в качестве ингибиторов рнк-зависимой рнк вирусной полимеразы
US7105499B2 (en) 2001-01-22 2006-09-12 Merck & Co., Inc. Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase
US20030165873A1 (en) * 2001-03-02 2003-09-04 Come Jon H. 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
DE60218458T2 (de) 2001-05-08 2007-11-15 Kudos Pharmaceuticals Ltd. Isochinolinon derivate als parp inhibitoren
WO2002094264A1 (en) 2001-05-23 2002-11-28 Tularik Inc. Ccr4 antagonists
JP2005505508A (ja) 2001-06-13 2005-02-24 ジーンソフト ファーマシューティカルズ インコーポレイテッド 抗感染活性を有するベンゾチオフェン化合物
WO2002100832A1 (en) 2001-06-13 2002-12-19 Genesoft Pharmaceuticals, Inc. Isoquinoline compounds having antiinfective activity
WO2002101007A2 (en) 2001-06-13 2002-12-19 Genesoft Pharmaceuticals, Inc Antipathogenic benzamide compounds
US20030114467A1 (en) 2001-06-21 2003-06-19 Shakespeare William C. 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
BR0211750A (pt) 2001-08-10 2004-10-13 Shionogi & Co Agente antiviral
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
US7101884B2 (en) 2001-09-14 2006-09-05 Merck & Co., Inc. Tyrosine kinase inhibitors
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
AU2002350217A1 (en) 2001-12-04 2003-06-17 Bristol-Myers Squibb Company Glycinamides as factor xa inhibitors
EP1465869B1 (en) 2001-12-21 2013-05-15 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
AU2002364209A1 (en) 2001-12-26 2003-07-24 Genelabs Technologies, Inc. Polyamide derivatives 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
US8247424B2 (en) 2002-03-26 2012-08-21 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
AU2003223012A1 (en) 2002-04-26 2003-11-10 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
JP2006506401A (ja) 2002-05-23 2006-02-23 メルク エンド カムパニー インコーポレーテッド 有糸分裂キネシン阻害薬
US7041676B2 (en) 2002-06-14 2006-05-09 Cytokinetics, Inc. Compounds, compositions, and methods
RU2340605C2 (ru) 2002-06-27 2008-12-10 Ново Нордиск А/С Арилкарбонильные производные в качестве терапевтических средств
AU2003243921B2 (en) 2002-06-27 2009-05-07 Novo Nordisk A/S Aryl carbonyl derivatives as therapeutic agents
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
MXPA05001642A (es) 2002-08-13 2005-04-25 Warner Lambert Co Derivados de naftaleno como inhibidores de metaloproteinasas de matriz.
US7598377B2 (en) 2002-08-16 2009-10-06 Astrazeneca Ab Inhibition of phosphoinositide 3-kinase β
US20040048853A1 (en) 2002-08-21 2004-03-11 Gustave Bergnes 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
AU2003301020A1 (en) 2002-12-20 2004-07-22 Sankyo Company, Limited Isoquinolinone derivatives and their use as therapeutic agents
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
CN1756735A (zh) 2003-03-06 2006-04-05 帝斯曼知识产权资产管理有限公司 α-氨羰基化合物的制备方法
KR20050122220A (ko) 2003-03-25 2005-12-28 다케다 샌디에고, 인코포레이티드 디펩티딜 펩티다제 억제제
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
US20050008640A1 (en) * 2003-04-23 2005-01-13 Wendy Waegell Method of treating transplant rejection
WO2004111014A1 (en) 2003-06-06 2004-12-23 Vertex Pharmaceuticals Incorporated Pyrimidine derivatives as modulators of atp-binding cassette transporters
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
CA2572324A1 (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
US7459472B2 (en) 2003-08-08 2008-12-02 Transtech Pharma, Inc. Aryl and heteroaryl compounds, compositions, and methods of use
WO2005016349A1 (en) 2003-08-14 2005-02-24 Icos Corporation Methods of inhibiting leukocyte accumulation
WO2005016348A1 (en) 2003-08-14 2005-02-24 Icos Corporation Method of inhibiting immune responses stimulated by an endogenous factor
SG145748A1 (en) 2003-08-15 2008-09-29 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
JP2007510745A (ja) 2003-11-10 2007-04-26 シンタ ファーマシューティカルズ コーポレーション 縮合複素環式化合物
MXPA06005578A (es) 2003-11-17 2006-08-11 Pfizer Prod Inc Compuestos de pirrolopirimidina utiles en el tratamiento del cancer.
WO2005061460A1 (en) 2003-12-08 2005-07-07 Cytokinetics, Inc. Compounds, compositions, and methods
WO2005063258A1 (en) 2003-12-22 2005-07-14 Gilead Sciences, Inc. Kinase inhibitor phosphonate conjugates
RU2006126791A (ru) 2003-12-23 2008-01-27 Новартис АГ (CH) Бициклические гетероциклические ингибиторы р-38 киназы
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
UA83416C2 (en) 2004-02-13 2008-07-10 Баниу Фармасьютикал Ко., Лтд. 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
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
PL2168968T3 (pl) 2004-04-02 2018-02-28 OSI Pharmaceuticals, LLC Inhibitory kinazy białkowej stanowiące związki heterobicykliczne z podstawionym pierścieniem 6,6-bicyklicznym
TW200538453A (en) * 2004-04-26 2005-12-01 Bristol Myers Squibb Co Bicyclic heterocycles as kinase inhibitors
ZA200609259B (en) 2004-04-30 2008-07-30 Takeda Pharmaceutical Heterocyclic amide compound and use thereof as an mmp-13 inhibitor
DE102004022897A1 (de) 2004-05-10 2005-12-08 Bayer Cropscience Ag Azinyl-imidazoazine
CN102229609A (zh) 2004-05-13 2011-11-02 艾科斯有限公司 作为人磷脂酰肌醇3-激酶δ抑制剂的喹唑啉酮
WO2005112935A1 (en) 2004-05-13 2005-12-01 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
WO2005116035A1 (en) * 2004-05-27 2005-12-08 Pfizer Products Inc. Pyrrolopyrimidine derivatives useful in cancer treatment
WO2005120511A1 (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
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
US8212012B2 (en) 2004-11-03 2012-07-03 University Of Kansas Novobiocin analogues having modified sugar moieties
CA2585091C (en) 2004-11-03 2016-07-19 University Of Kansas Novobiocin analogues as anticancer agents
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
WO2006089106A2 (en) 2005-02-17 2006-08-24 Icos Corporation 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
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
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
WO2006114064A2 (en) 2005-04-25 2006-11-02 Institute Of Organic Chemistry And Biochemistry Ofthe 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
EP1917250B1 (en) 2005-06-27 2010-07-21 Amgen, Inc Anti-inflammatory aryl nitrile compounds
US20100190788A1 (en) 2005-07-11 2010-07-29 Olivier Defert Amide derivatives as kinase inhitors
BRPI0615524A2 (pt) 2005-07-11 2010-04-06 Devgen Nv derivados da amida como inibidores da quinase
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
JP2009506006A (ja) 2005-08-25 2009-02-12 エフ.ホフマン−ラ ロシュ アーゲー p38MAPキナーゼ阻害剤およびその使用方法
US20080318942A1 (en) 2005-09-01 2008-12-25 Bioagency Ag Fredericamycin Derivatives
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
EA015463B1 (ru) 2005-11-17 2011-08-30 Оси Фармасьютикалз, Инк. КОНДЕНСИРОВАННОЕ БИЦИКЛИЧЕСКОЕ СОЕДИНЕНИЕ - ИНГИБИТОР mTOR, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, ЕГО СОДЕРЖАЩАЯ, И СПОСОБ ЛЕЧЕНИЯ РАКА
AU2006316321A1 (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
EP1979002A2 (en) 2005-12-19 2008-10-15 OSI Pharmaceuticals, Inc. Combination of igfr inhibitor and anti-cancer agent
US7772231B2 (en) 2005-12-29 2010-08-10 Abbott Laboratories Substituted pyrazolo[3,4-d]pyrimidines as protein kinase inhibitors
WO2007089669A2 (en) 2006-01-26 2007-08-09 Wyeth Processes for the preparation of compounds which modulate cell proliferation
CA2645137A1 (en) 2006-03-07 2007-09-13 James F. Blake Heterobicyclic pyrazole compounds and methods of use
EP1996193A2 (en) 2006-03-13 2008-12-03 OSI Pharmaceuticals, Inc. Combined treatment with an egfr kinase inhibitor and an agent that sensitizes tumor cells to the effects of egfr kinase inhibitors
US7566565B2 (en) 2006-03-24 2009-07-28 Syntonix Pharmaceuticals, Inc. PC5 as a factor IX propeptide processing enzyme
WO2007126841A2 (en) 2006-03-29 2007-11-08 Foldrx Pharmaceuticals, Inc. Inhibition of alpha-synuclein toxicity
DK2004654T3 (da) 2006-04-04 2013-07-22 Univ California Pyrazolopyrimidin derivater til anvendelse som kinase antagonister
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
SI2013211T1 (sl) 2006-04-21 2012-07-31 Novartis Ag Purinski derivati za uporabo kot agonisti receptorja adenozina A A
GB0607950D0 (en) 2006-04-21 2006-05-31 Novartis Ag Organic compounds
US20090253718A1 (en) 2006-04-25 2009-10-08 Astex Therapeutics Limited Pharmaceutical Compounds
EP2037931A2 (en) 2006-04-25 2009-03-25 Astex Therapeutics Limited Pharmaceutical combinations of pk inhibitors and other active agents
DE102006020327A1 (de) 2006-04-27 2007-12-27 Bayer Healthcare Ag Heterocyclisch substituierte, anellierte Pyrazol-Derivate und ihre Verwendung
EP2029593A1 (en) 2006-05-22 2009-03-04 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)
US7678803B2 (en) 2006-08-24 2010-03-16 Serenex, Inc. Quinazoline derivatives for the treatment of cancer
WO2008025755A1 (de) 2006-09-01 2008-03-06 Basf Se Verwendung von n-haltigen heterozyklen in dermokosmetika
ES2528316T3 (es) 2006-09-01 2015-02-06 Senhwa Biosciences, Inc. Moduladores de la serina-treonina proteína quinasa y de PARP
EP1903044A1 (en) 2006-09-14 2008-03-26 Novartis AG Adenosine Derivatives as A2A Receptor Agonists
US8492405B2 (en) 2006-10-18 2013-07-23 Takeda Pharmaceutical Company Limited Glucokinase-activating fused heterocyclic compounds and methods of treating diabetes and obesity
US7772180B2 (en) 2006-11-09 2010-08-10 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
SG178786A1 (en) 2006-11-13 2012-03-29 Lilly Co Eli 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
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
DK2114925T3 (da) 2006-12-22 2012-05-29 Ind Res Ltd Azetidin-analoger af nucleosidase- og phosphorylase-inhibitorer
AU2008210904A1 (en) 2007-01-26 2008-08-07 Irm Llc Purine compounds and compositions as kinase inhibitors for the treatment of Plasmodium related diseases
WO2008112715A2 (en) 2007-03-12 2008-09-18 Vm Discovery Inc. Novel agents of calcium ion channel modulators
DK2139882T3 (en) 2007-03-23 2014-03-10 Amgen Inc 3-substituted quinoline or quinoxaline derivatives and their use as inhibitors of phosphatidylinositol 3-kinase (PI3K)
PL2137186T3 (pl) 2007-03-23 2016-09-30 Związki heterocykliczne i ich zastosowania
EP2132207A2 (en) 2007-03-23 2009-12-16 Amgen Inc. Heterocyclic compounds and their uses
WO2008156513A2 (en) 2007-03-29 2008-12-24 University Of Connecticut Methods to protect skeletal muscle against injury
EP2134682B1 (en) 2007-04-13 2011-12-14 Sanofi A transition metal catalyzed synthesis of n-aminoindoles
WO2008125014A1 (fr) 2007-04-13 2008-10-23 Institute Of Pharmacology And Toxicology Academy Of Military Medical Sciences P.L.A. Composés d'urée, leurs procédés de préparation et leurs utilisations pharmaceutiques
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
CN101687865A (zh) 2007-06-26 2010-03-31 塞诺菲-安万特股份有限公司 稠合的苯并咪唑和氮杂苯并咪唑的区域选择性金属催化合成
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
CN106279283A (zh) 2007-08-13 2017-01-04 症变治疗公司 新颖的葡糖激酶活化剂
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
CN101952292A (zh) 2007-11-13 2011-01-19 艾科斯有限公司 人磷脂酰肌醇3-激酶δ的抑制剂
CA2708391A1 (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
KR101660050B1 (ko) 2008-01-04 2016-09-26 인텔리카인, 엘엘씨 특정 화학 물질, 조성물 및 방법
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
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
WO2009100326A1 (en) 2008-02-07 2009-08-13 Cv Therapeutics, 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
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
EP3009436B1 (en) 2008-07-08 2019-06-05 Intellikine, LLC Kinase inhibitors and methods of use
US20110224223A1 (en) 2008-07-08 2011-09-15 The Regents Of The University Of California, A California Corporation MTOR Modulators and Uses Thereof
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
JP2011530596A (ja) 2008-08-11 2011-12-22 プレジデント アンド フェロウズ オブ ハーバード カレッジ tRNA合成酵素の阻害のためのハロフジノン類似体およびそれらの使用
CA2738313A1 (en) 2008-09-23 2010-04-08 Georgetown University Viral and fungal inhibitors
CA2738429C (en) 2008-09-26 2016-10-25 Intellikine, Inc. Heterocyclic kinase inhibitors
ES2570429T3 (es) * 2008-10-16 2016-05-18 Univ California Inhibidores de heteroaril quinasa de anillo condensado
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
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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