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

Info

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
Authority
JP
Japan
Prior art keywords
substituted
unsubstituted
compound
alkyl
abl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
JP2011532279A
Other languages
English (en)
Japanese (ja)
Other versions
JP2012505916A5 (enExample
JP2012505916A (ja
Inventor
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
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
University of California
University of California Los Angeles UCLA
Original Assignee
University of California San Diego UCSD
University of California Los Angeles UCLA
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by University of California San Diego UCSD, University of California Los Angeles UCLA filed Critical University of California San Diego UCSD
Publication of JP2012505916A publication Critical patent/JP2012505916A/ja
Publication of JP2012505916A5 publication Critical patent/JP2012505916A5/ja
Application granted granted Critical
Publication of JP5819195B2 publication Critical patent/JP5819195B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)

Application Number Title Priority Date Filing Date
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

Family

ID=42107267

Family Applications (2)

Application Number Title Priority Date Filing Date
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

Family Applications After (1)

Application Number Title Priority Date Filing Date
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

Country Status (8)

Country Link
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 (33)

* 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
MX2008014618A (es) * 2006-05-15 2008-11-28 Irm Llc Composiciones y metodos para inhibidores de cinasas del receptor fgf.
US20110224223A1 (en) 2008-07-08 2011-09-15 The Regents Of The University Of California, A California Corporation MTOR Modulators and Uses Thereof
WO2010045542A2 (en) * 2008-10-16 2010-04-22 The Regents Of The University Of California Fused ring heteroaryl kinase inhibitors
GEP201706639B (en) 2009-08-17 2017-03-27 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
BR112012024380A2 (pt) 2010-03-25 2015-09-15 Glaxosmithkline Llc compostos químicos
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
RS58326B1 (sr) 2011-05-04 2019-03-29 Rhizen Pharmaceuticals S A Nova jedinjenja kao modulatori proteinskih kinaza
BR112014000653A2 (pt) * 2011-07-13 2017-02-14 Pharmacyclics Inc inibidores de tirosina quinase de bruton
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
CN105594216B (zh) 2014-08-01 2019-02-19 Lg电子株式会社 广播信号发送方法、广播信号发送设备
CN113620978A (zh) 2014-09-11 2021-11-09 加利福尼亚大学董事会 mTORC1抑制剂
EP3430017B1 (en) 2016-03-17 2023-01-25 The Regents of The University of California Compositions and methods for treating parasitic diseases
WO2017220477A1 (en) 2016-06-21 2017-12-28 Nerviano Medical Sciences S.R.L. N-(substituted-phenyl)-sulfonamide derivatives as kinase inhibitors
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
KR102526964B1 (ko) 2018-02-26 2023-04-28 길리애드 사이언시즈, 인코포레이티드 Hbv 복제 억제제로서의 치환된 피롤리진 화합물
MX2020011564A (es) 2018-05-01 2021-01-29 Revolution Medicines Inc Analogos de rapamicina unidos a c26 como inhibidores de mtor.
HRP20230488T1 (hr) 2018-05-01 2023-08-04 Revolution Medicines, Inc. C40-, C28- I C-32-VEZANI ANALOZI RAPAMICINA KAO INHIBITORI mTOR
US12324807B2 (en) 2018-06-01 2025-06-10 Cornell University Combination therapy for 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
JP2023549540A (ja) 2020-11-18 2023-11-27 デシフェラ・ファーマシューティカルズ,エルエルシー Gcn2およびperkキナーゼ阻害剤およびその使用方法
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
JP2024544632A (ja) 2021-12-03 2024-12-03 デシフェラ・ファーマシューティカルズ,エルエルシー Gcn2及びperkキナーゼ阻害剤としての複素環式化合物
US12539305B2 (en) 2022-05-25 2026-02-03 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
US5442039A (en) 1989-07-17 1995-08-15 The Dow Chemical Company Mesogenic polycyanates and thermosets thereof
US5428125A (en) 1989-07-17 1995-06-27 The Dow Chemical Company Mesogenic polycyanates and thermosets thereof
US5674998A (en) 1989-09-15 1997-10-07 Gensia 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
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
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
SG80526A1 (en) 1990-09-25 2001-05-22 Rhone Poulenc Rorer Int Compounds having antihypertensive and anti- ischemic properies
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
GB9103839D0 (en) 1991-02-23 1991-04-10 Smithkline Beecham Plc Pharmaceuticals
US5916891A (en) 1992-01-13 1999-06-29 Smithkline Beecham Corporation Pyrimidinyl imidazoles
IL104369A0 (en) 1992-01-13 1993-05-13 Smithkline Beecham Corp Novel compounds and compositions
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
DE69333955D1 (de) 1992-04-24 2006-02-02 Stanford Res Inst Int Targeting homologer sequenzen in eukaryotenzellen
EP0672325B2 (en) 1992-06-19 2008-08-27 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
TW444018B (en) * 1992-12-17 2001-07-01 Pfizer Pyrazolopyrimidines
AU673055B2 (en) 1993-02-03 1996-10-24 Gensia, Inc. Adenosine kinase inhibitors comprising lyxofuranosyl derivatives
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
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
DK0783505T3 (da) * 1994-09-29 2001-07-02 Novartis Ag Pyrrolo[2,3-d]pyrimidiner og deres anvendelse
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
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
US5665721A (en) 1995-06-07 1997-09-09 Abbott Laboratories Heterocyclic substituted cyclopentane compounds
IL122246A (en) 1995-06-07 2004-06-01 Searle & Co Combination of spironolactone and angiotensin II antagonist for the treatment of heart failure
WO1996040256A1 (en) 1995-06-07 1996-12-19 G.D. Searle & Co. Method to treat cardiofibrosis with a combination of an angiotensin ii antagonist and spironolactone
KR100618466B1 (ko) 1995-06-07 2006-12-13 지.디. 썰 엘엘씨 울혈성심마비의치료를위한에폭시-스테로이드계알도스테론길항제및앤지오탠신ii길항제복합요법
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
BR9711805A (pt) 1996-06-20 2002-01-15 Regents The Univesity Of Texas Compostos e métodos para providenciar preparações farmacologicamente ativas e uso dos mesmos
US5948776A (en) 1996-10-23 1999-09-07 Zymogenetic, 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
US5922753A (en) 1996-10-23 1999-07-13 Zymogenetics, Inc. Methods for treating bone deficit conditions with benzothiazole
US5965573A (en) 1996-10-23 1999-10-12 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
US5990169A (en) 1996-10-23 1999-11-23 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
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
WO1998035048A2 (en) 1997-02-07 1998-08-13 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
ATE242245T1 (de) 1997-03-19 2003-06-15 Basf Ag Pyrrolo(2,3-d)pyrimidine und ihre verwendung als tyrosinkinase-inhibitoren
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
WO1999024432A1 (fr) 1997-11-12 1999-05-20 Mitsubishi Chemical Corporation Derives de purine et medicament les renfermant en tant qu'ingredient actif
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
JP2002527359A (ja) 1998-09-18 2002-08-27 ビーエーエスエフ アクチェンゲゼルシャフト キナーゼインヒビターとしての4−アミノピロリピリミジン
US6713474B2 (en) * 1998-09-18 2004-03-30 Abbott Gmbh & Co. Kg Pyrrolopyrimidines as therapeutic agents
SK3842001A3 (en) * 1998-09-18 2002-04-04 Basf Ag Pyrrolopyrimidines as protein kinase inhibitors (revised)
AU779008C (en) 1999-01-11 2005-06-30 Princeton University High affinity inhibitors for target validation and uses thereof
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
HK1046402A1 (zh) 1999-06-03 2003-01-10 Basf Aktiengesellschaft Benzothiazinone和benzoxazinone化合物
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
AU7080500A (en) 1999-08-27 2001-03-26 Chemocentryx, Inc. Compounds and methods for modulating cxcr3 function
EP1216234B1 (en) 1999-09-16 2004-12-29 Curis, Inc. Mediators of hedgehog signaling pathways, compositions and uses related thereto
IL148718A0 (en) 1999-09-17 2002-09-12 Abbott Gmbh & Co Kg Pyrazolopyrimidines as therapeutic agents
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
ES2225231T3 (es) 1999-10-06 2005-03-16 Boehringer Ingelheim Pharmaceuticals Inc. Compuestos heterociclicos, utiles como inhibidores de tirosina quinasas.
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
JP2004514405A (ja) * 2000-03-29 2004-05-20 アボット ゲーエムベーハー ウント カンパニー カーゲー Tie−2阻害薬の特定方法
AU2000240570A1 (en) * 2000-03-29 2001-10-08 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
MXPA02010618A (es) 2000-04-25 2004-05-05 Icos Corp Inhibidores de fosfatidilinositol 3-quinasa delta.
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
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
AU2002213467A1 (en) 2000-10-11 2002-04-22 Chemocentryx, Inc. Modulation of ccr4 function
US6811979B2 (en) 2000-10-11 2004-11-02 Applera Corporation Fluorescent nucleobase conjugates having anionic linkers
US6890747B2 (en) 2000-10-23 2005-05-10 Warner-Lambert Company Phosphoinositide 3-kinases
US6964967B2 (en) 2000-12-11 2005-11-15 Amgen, Inc. Substituted pyrido[2,3-d]pyrimidines and methods for their use
TWI312779B (enExample) 2000-12-28 2009-08-01 Daiichi Seiyaku Co
DZ3487A1 (fr) 2001-01-22 2002-07-25 Merck Sharp & Dohme Derives de nucleoside comme inhibiteurs de l'arn polymerase virale d'arn-dependant
US7105499B2 (en) 2001-01-22 2006-09-12 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
EP1397350B1 (en) 2001-05-08 2007-02-28 Kudos Pharmaceuticals Limited Isoquinolinone derivatives as parp inhibitors
US7144903B2 (en) 2001-05-23 2006-12-05 Amgen Inc. CCR4 antagonists
US20030236198A1 (en) 2001-06-13 2003-12-25 Genesoft, Inc. Antipathogenic benzamide compounds
WO2002100832A1 (en) 2001-06-13 2002-12-19 Genesoft Pharmaceuticals, Inc. Isoquinoline compounds having antiinfective activity
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
EP1463742A4 (en) 2001-06-21 2006-05-10 Ariad Pharma Inc NEW PYRAZOLO AND PYRROLO PYRIMIDINES AND THEIR USES
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
JP4338192B2 (ja) 2001-08-10 2009-10-07 塩野義製薬株式会社 抗ウイルス剤
WO2004043335A2 (en) 2001-09-13 2004-05-27 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 (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
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
US7998986B2 (en) 2001-12-21 2011-08-16 Exelixis Patent Company Llc Modulators of LXR
WO2003057212A1 (en) 2001-12-26 2003-07-17 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
AU2003225933A1 (en) 2002-03-22 2003-10-13 Cellular Genomics, Inc. AN IMPROVED FORMULATION OF CERTAIN PYRAZOLO(3,4-d) PYRIMIDINES AS KINASE MODULATORS
WO2003080582A2 (de) 2002-03-26 2003-10-02 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
JP2005529889A (ja) 2002-04-26 2005-10-06 ファイザー・プロダクツ・インク ピリミジン−2,4,6−トリオンメタロ−プロテイナーゼ阻害剤
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
EP1556357A4 (en) 2002-06-14 2006-09-13 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
KR101124245B1 (ko) 2002-06-27 2012-07-02 노보 노르디스크 에이/에스 치료제로서 아릴 카르보닐 유도체
AU2003243921B2 (en) 2002-06-27 2009-05-07 Novo Nordisk A/S Aryl carbonyl derivatives as therapeutic 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
BR0313460A (pt) 2002-08-13 2005-07-05 Warner Lambert Co Derivados de naftaleno como inibidores de metaloproteinase da matriz
NZ538420A (en) 2002-08-16 2007-06-29 Kinacia Pty Ltd Inhibition of phosphoinositide 3-kinase beta
AU2003262747A1 (en) 2002-08-21 2004-03-11 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
WO2004031177A1 (ja) 2002-09-30 2004-04-15 Banyu Pharmaceutical Co., Ltd. 2−アミノベンズイミダゾール誘導体
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
ATE496893T1 (de) 2002-12-20 2011-02-15 X Ceptor Therapeutics Inc Isochinolinonderivate und deren verwendung als medikamente
WO2004056746A1 (en) 2002-12-23 2004-07-08 4Sc Ag Cycloalkene dicarboxylic acid compounds as anti-inflammatory, immunomodulatory and anti-proliferatory 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
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
WO2004103270A2 (en) 2003-04-02 2004-12-02 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
EP1646615B1 (en) 2003-06-06 2009-08-26 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
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
US7208601B2 (en) 2003-08-08 2007-04-24 Mjalli Adnan M M Aryl and heteroaryl compounds, compositions, and methods of use
US7501538B2 (en) 2003-08-08 2009-03-10 Transtech Pharma, Inc. 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
US20050124637A1 (en) 2003-08-15 2005-06-09 Irm Llc Compounds and compositions as inhibitors of receptor tyrosine kinase activity
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
EP1687002A4 (en) 2003-11-10 2008-07-23 Synta Pharmaceuticals Corp CONDENSED HETEROCYCLIC COMPOUNDS
CA2546192C (en) 2003-11-17 2010-04-06 Pfizer Products Inc. Pyrrolopyrimidine compounds useful in treatment of cancer
JP2007513154A (ja) 2003-12-08 2007-05-24 サイトキネティクス・インコーポレーテッド 化合物、組成物及び方法
WO2005063258A1 (en) 2003-12-22 2005-07-14 Gilead Sciences, Inc. Kinase inhibitor phosphonate conjugates
DE602004025504D1 (de) 2003-12-23 2010-03-25 Novartis Ag Bicyclische heterocyclische p-38-kinase-inhibitoren
CA2552664A1 (en) 2004-01-08 2005-07-28 Michigan State University Methods for treating and preventing hypertension and hypertension-related disorders
JP2007520559A (ja) * 2004-02-03 2007-07-26 アボット・ラボラトリーズ 治療薬としてのアミノベンゾオキサゾール類
CA2555824C (en) 2004-02-13 2011-06-07 Banyu Pharmaceutical Co., Ltd. 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
CA2557575A1 (en) 2004-02-27 2005-09-15 F. Hoffmann-La Roche Ag Fused derivatives of pyrazole
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
AU2005238386A1 (en) 2004-04-30 2005-11-10 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
PL1761540T3 (pl) 2004-05-13 2017-06-30 Icos Corporation Chinazolinony jako inhibitory ludzkiej kinazy 3-fosfatydyloinozytolu delta
CA2566436C (en) 2004-05-13 2011-05-10 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
BRPI0511512A (pt) * 2004-05-27 2007-12-26 Pfizer Prod Inc derivados pirrolpirimidina úteis no tratamento do cáncer
EP1750715A1 (en) 2004-06-04 2007-02-14 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
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
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
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
JP2008520742A (ja) 2004-11-23 2008-06-19 ピーティーシー セラピューティクス, インコーポレイテッド Vegf産生の阻害に有用なカルバゾール誘導体、カルボリン誘導体およびインドール誘導体
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
EP1885356A2 (en) 2005-02-17 2008-02-13 Icos Corporation 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
RU2007138264A (ru) * 2005-03-17 2009-09-10 Новартис АГ (CH) N-[3-(1-АМИНО-5,6,7,8-ТЕТРАГИДРО-2,4,4b-ТРИАЗАФЛУОРЕН-9-ИЛ)ФЕНИЛ]БЕНЗАМИДЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ТИРОЗИН/ТРЕОНИНКИНАЗ, ПРЕЖДЕ ВСЕГО КИНАЗ В-RAF
WO2006108107A1 (en) 2005-04-06 2006-10-12 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
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
MX2007015917A (es) 2005-06-22 2008-03-10 Chemocentryx Inc Compuestos de azaindazol y metodos de uso.
ATE474829T1 (de) 2005-06-27 2010-08-15 Amgen Inc Entzündungshemmende arylnitrilverbindungen
WO2007006547A1 (en) 2005-07-11 2007-01-18 Devgen N.V. Amide derivatives as kinase inhibitors
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
AU2006283940A1 (en) 2005-08-25 2007-03-01 F. Hoffmann-La Roche Ag P38 MAP kinase inhibitors and methods for using the same
WO2007025090A2 (en) 2005-08-25 2007-03-01 Kalypsys, Inc. Heterobicyclic and - tricyclic inhibitors of mapk/erk kinase
WO2007025534A1 (de) 2005-09-01 2007-03-08 Bioagency Ag Fredericamycin-derivate
JP2009510066A (ja) 2005-09-29 2009-03-12 ワイス 血管運動症状(vms)の治療のためのモノアミン再取り込みのモジュレータである1−(1h−インドール−1−イル)−3−(メチルアミノ)−1−フェニルプロパン−2−オール誘導体および関連の化合物
AU2006316605B2 (en) 2005-11-17 2012-04-26 Osi Pharmaceuticals, Inc. Fused bicyclic mTOR inhibitors
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
WO2007079164A2 (en) 2005-12-29 2007-07-12 Abbott Laboratories 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
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
HRP20160990T1 (hr) 2006-03-24 2016-10-07 Biogen Hemophilia Inc. Pc5 kao enzim obrade faktor ix propeptida
JP2009531443A (ja) 2006-03-29 2009-09-03 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 α−シヌクレイン毒性の抑制
KR101499783B1 (ko) 2006-04-04 2015-03-09 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
PE20080361A1 (es) 2006-04-21 2008-06-03 Novartis Ag Compuestos derivados de purina como activadores del receptor de adenosina a2a
GB0607950D0 (en) 2006-04-21 2006-05-31 Novartis Ag Organic compounds
US20090082370A1 (en) 2006-04-25 2009-03-26 Neil Thomas Thompson 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
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
CA2661307C (en) 2006-08-22 2016-07-19 Technion Research And Development Foundation Ltd. Heterocyclic derivatives binding to the peripheral-type benzodiazepine receptor (pbr)
EP2069325A2 (en) 2006-08-24 2009-06-17 Serenex, Inc. Isoquinoline, quinazoline and phthalazine derivatives
CA2974246C (en) 2006-09-01 2020-02-25 Senhwa Biosciences, Inc. Tricyclic heteroaryl compounds and their use as protein modulators
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
JP5306818B2 (ja) 2006-10-18 2013-10-02 武田薬品工業株式会社 縮合複素環化合物
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
CN101611007A (zh) 2006-12-20 2009-12-23 先灵公司 新颖的jnk抑制剂
KR20090101278A (ko) 2006-12-22 2009-09-24 인더스트리얼 리서치 리미티드 누클레오시다제 및 포스포릴라제 억제제의 아제티딘 유사체
EP2124954A2 (en) 2007-01-26 2009-12-02 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
AU2008231304B2 (en) 2007-03-23 2011-05-12 Amgen Inc. Heterocyclic compounds and their uses
US7705018B2 (en) 2007-03-23 2010-04-27 Amgen Inc. Substituted quinolines and their uses in treatment of inflammatory and related conditions
EP2132207A2 (en) 2007-03-23 2009-12-16 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
KR20100015546A (ko) 2007-04-13 2010-02-12 사노피-아벤티스 N-아미노인돌의 전이 금속 촉매된 합성
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
US20090214529A9 (en) 2007-05-22 2009-08-27 Taigen Biotechnology Co., Ltd. Kinesin inhibitors
US9603848B2 (en) 2007-06-08 2017-03-28 Senomyx, Inc. Modulation of chemosensory receptors and ligands associated therewith
US7928111B2 (en) 2007-06-08 2011-04-19 Senomyx, Inc. Compounds including substituted thienopyrimidinone derivatives as ligands for modulating chemosensory receptors
ATE538120T1 (de) 2007-06-26 2012-01-15 Sanofi Sa Regioselektive, metallkatalysierte synthese annelierter benzimidazole und azabenzimidazole
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
US20090053192A1 (en) 2007-08-10 2009-02-26 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
WO2009044707A1 (ja) 2007-10-03 2009-04-09 Riken 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
JP2011500657A (ja) 2007-10-15 2011-01-06 アストラゼネカ アクチボラグ 組合せ059
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
AU2008323694A1 (en) * 2007-11-07 2009-05-14 Foldrx Pharmaceuticals, Inc. Modulation of protein trafficking
NZ585460A (en) 2007-11-13 2013-02-22 Icos Corp Inhibitors of human phosphatidyl-inositol 3-kinase delta
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
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
AU2009204483B2 (en) 2008-01-04 2014-03-13 Intellikine, Llc Certain chemical entities, compositions and methods
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
EP2244709A4 (en) 2008-02-07 2012-02-29 Synta Pharmaceuticals Corp TOPICAL FORMULATIONS FOR THE TREATMENT OF PSORIASIS
EP2259790A1 (en) 2008-02-07 2010-12-15 Gilead Palo Alto, Inc. Abca-1 elevating compounds and the use thereof
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
WO2009117157A1 (en) 2008-03-20 2009-09-24 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.
EP2328897A1 (en) 2008-07-16 2011-06-08 Schering Corporation 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
EP2331525A4 (en) 2008-08-11 2013-01-02 Harvard College HALOFUGINONE ANALOGUE FOR INHIBITING TRNA SYNTHETASES AND APPLICATIONS 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
WO2010045542A2 (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
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

Also Published As

Publication number Publication date
US20110275651A1 (en) 2011-11-10
EP2358720B1 (en) 2016-03-02
AU2020200597A1 (en) 2020-02-20
WO2010045542A2 (en) 2010-04-22
EP2358720A2 (en) 2011-08-24
AU2018201842A1 (en) 2018-04-12
CA2740885C (en) 2018-04-03
CA2740885A1 (en) 2010-04-22
ES2570429T3 (es) 2016-05-18
WO2010045542A3 (en) 2010-08-19
US8697709B2 (en) 2014-04-15
AU2016202455A1 (en) 2016-05-12
DK2358720T3 (en) 2016-06-06
JP2014193925A (ja) 2014-10-09
EP2358720A4 (en) 2012-08-15
AU2009305669A1 (en) 2010-04-22
JP2012505916A (ja) 2012-03-08

Similar Documents

Publication Publication Date Title
JP5819195B2 (ja) 融合環ヘテロアリールキナーゼ阻害剤
AU2011217199B2 (en) Deuterated pyrrolopyrimidine compounds as inhibitors of CDK4/6
JP7397452B2 (ja) ヘテロアリールカルボキシアミド化合物
WO2021091956A1 (en) Ras inhibitors
US10829492B2 (en) Amino pyrazolopyrimidine compound used as neurotrophic factor tyrosine kinase receptor inhibitor
TW201811794A (zh) (s)-7-(1-丙烯醯基六氫吡啶-4-基)-2-(4-苯氧基苯基)-4,5,6,7-四氫吡唑並[1,5-a]嘧啶-3-甲醯胺的晶型、其製備和用途
WO2021057867A1 (zh) 一类基于有机胂的cdk抑制剂及其制备方法和用途
EA024984B1 (ru) Производные 6-циклоалкил-1,5-дигидропиразоло[3,4-d]пиримидин-4-она и их применение в качестве ингибиторов pde9a
JP6916185B2 (ja) Btk阻害剤としてのイソキノロン類
CN103582643A (zh) 蛋白激酶抑制剂
WO2013170671A1 (zh) 蝶啶酮衍生物及其作为egfr、blk、flt3抑制剂的应用
ES2324837T3 (es) Derivados de piridina utiles como inhibidores de la pkc-theta.
CN104844566A (zh) 一种新型结构的激酶抑制剂
IL293107A (en) Adenosine receptor antagonist compounds
JP7430656B2 (ja) Cdk4/6活性阻害化合物の結晶形およびその使用
CA2610166C (en) Benzoquinolinesulfonamide derivatives useful as rho-kinase inhibitors
CN115702146B (zh) 5-((1,2,3,4-四氢异喹啉-7-基)氨基)吡啶-2(1h)-酮衍生物及其应用
Qhobosheane et al. Exploration of 7-azaindole-coumaranone hybrids and their analogues as protein kinase inhibitors
WO2011082271A2 (en) Substituted triazolo-pyrimidine compounds
WO2021174581A1 (zh) 吲唑类化合物的新用途
KR20210102388A (ko) 퀴놀린 구조를 갖는 pan-kit 키나제 억제제 및 이의 용도
WO2019178801A1 (zh) 一类新型的苯氧基哌啶衍生物及其用途
KR20220007447A (ko) Trap1 선택적 억제제로서의 화합물 및 이를 포함하는 암 예방 또는 치료용 조성물
BR122024019067A2 (pt) Forma cristalina de (s) -7- (1-acriloilpiperidin-4-il) -2- (4-fenoxifenil) -4,5,6,7-tetra-hidropirazol [1,5-a] pirimidina-3-carboxamida, sua preparação e seus usos
BR122024019068A2 (pt) Método de preparação de forma cristalina de (s) -7- (1- acriloilpiperidin- 4-il) -2- (4-fenoxifenil) -4,5,6,7-tetra-hidropirazol [1,5-a] pirimidina- 3-carboxamida

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20121015

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20121015

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20140130

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20140218

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20140515

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20140522

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20140618

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20150120

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20150519

A911 Transfer to examiner for re-examination before appeal (zenchi)

Free format text: JAPANESE INTERMEDIATE CODE: A911

Effective date: 20150707

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20150901

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20150930

R150 Certificate of patent or registration of utility model

Ref document number: 5819195

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

LAPS Cancellation because of no payment of annual fees