JP4623962B2 - タンパク質キナーゼおよびホスファターゼ阻害剤、それらを設計する方法、ならびにそれらを使用する方法 - Google Patents

タンパク質キナーゼおよびホスファターゼ阻害剤、それらを設計する方法、ならびにそれらを使用する方法 Download PDF

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JP4623962B2
JP4623962B2 JP2003538137A JP2003538137A JP4623962B2 JP 4623962 B2 JP4623962 B2 JP 4623962B2 JP 2003538137 A JP2003538137 A JP 2003538137A JP 2003538137 A JP2003538137 A JP 2003538137A JP 4623962 B2 JP4623962 B2 JP 4623962B2
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inhibitors
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peptide
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JP2005514339A (ja
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デビッド ジー. ジュニア ハンガー
マウスタファ イー. エル−アラバイ
カレン エル. ミルキーウィックス
トーマス ニコテラ
ドナルド ヘンダーソン
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Research Foundation of the State University of New York
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
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    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P27/00Drugs for disorders of the senses
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    • A61P3/04Anorexiants; Antiobesity agents
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    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/30Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Immunology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Peptides Or Proteins (AREA)
JP2003538137A 2001-10-22 2002-10-19 タンパク質キナーゼおよびホスファターゼ阻害剤、それらを設計する方法、ならびにそれらを使用する方法 Expired - Lifetime JP4623962B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US33619101P 2001-10-22 2001-10-22
US41072602P 2002-09-13 2002-09-13
PCT/US2002/033660 WO2003035621A1 (en) 2001-10-22 2002-10-19 Protein kinase and phosphatase inhibitors, methods for designing them, and methods of using them

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JP2009160619A Division JP2009263394A (ja) 2001-10-22 2009-07-07 タンパク質キナーゼおよびホスファターゼ阻害剤、それらを設計する方法、ならびにそれらを使用する方法

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JP2005514339A JP2005514339A (ja) 2005-05-19
JP4623962B2 true JP4623962B2 (ja) 2011-02-02

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JP2009160619A Pending JP2009263394A (ja) 2001-10-22 2009-07-07 タンパク質キナーゼおよびホスファターゼ阻害剤、それらを設計する方法、ならびにそれらを使用する方法

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US (2) US7129225B2 (2)
EP (1) EP1444204A4 (2)
JP (2) JP4623962B2 (2)
CA (1) CA2464214C (2)
MX (1) MXPA04003758A (2)
WO (1) WO2003035621A1 (2)

Families Citing this family (50)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4865129B2 (ja) * 1999-01-13 2012-02-01 ザ・リサーチ・ファウンデーション・オブ・ステイト・ユニバーシティ・オブ・ニューヨーク タンパク質キナーゼ阻害剤を設計するための新規の方法
US7005445B2 (en) * 2001-10-22 2006-02-28 The Research Foundation Of State University Of New York Protein kinase and phosphatase inhibitors and methods for designing them
US7129225B2 (en) * 2001-10-22 2006-10-31 The Research Foundation Of State University Of New York Protection against and treatment of hearing loss
JP4595059B2 (ja) 2002-04-18 2010-12-08 株式会社医薬分子設計研究所 アミド誘導体
US20060128783A1 (en) * 2002-08-09 2006-06-15 Dinsmore Christopher J Tyrosine kinase inhibitors
WO2004014851A2 (en) 2002-08-09 2004-02-19 Merck & Co., Inc. Tyrosine kinase inhibitors
DE60323876D1 (de) * 2002-12-17 2008-11-13 Centre Nat Rech Scient Verwendung von purinderivaten zur induktion der differenzierung überzähliger haarzellen und deiter-zellen im entwickelnden corti-organ zur behandlung von taubheit
TWI328009B (en) 2003-05-21 2010-08-01 Glaxo Group Ltd Quinoline derivatives as phosphodiesterase inhibitors
WO2005004863A1 (en) * 2003-07-11 2005-01-20 Merck Patent Gmbh Benzimidazole carboxamides as raf kinase inhibitors
US20050089936A1 (en) * 2003-10-23 2005-04-28 Jianping Cai Combinatorial library of 3-aryl-1H-indole-2-carboxylic acid amides
EP1532980A1 (en) 2003-11-24 2005-05-25 Novo Nordisk A/S N-heteroaryl indole carboxamides and analogues thereof, for use as glucokinase activators in the treatment of diabetes
WO2005114197A2 (en) * 2004-04-15 2005-12-01 Albert Einstein College Of Medicine Of Yeshiva University Activity-based probes for protein tyrosine phosphatases
WO2006053274A2 (en) 2004-11-15 2006-05-18 Bristol-Myers Squibb Company 2-amino-1-functionalized tetralin derivatives and related glycogen phosphorylase inhibitors
WO2006055462A1 (en) 2004-11-15 2006-05-26 Bristol-Myers Squibb Company 2-amino-4-functionalized tetralin derivatives and related glycogen phosphorylase inhibitors
US7223786B2 (en) * 2004-11-15 2007-05-29 Bristol-Myers Squibb Company 2-aminonaphthalene derivatives and related glycogen phosphorylase inhibitors
US7365061B2 (en) 2004-11-15 2008-04-29 Bristol-Myers Squibb Company 2-Amino-3-functionalized tetralin derivatives and related glycogen phosphorylase inhibitors
GB0425919D0 (en) * 2004-11-25 2004-12-29 Prosidion Ltd Indole-2-carboxylic acid amides
FR2878849B1 (fr) * 2004-12-06 2008-09-12 Aventis Pharma Sa Indoles substitues, compositions les contenant, procede de fabrication et utilisation
BRPI0515811A (pt) * 2004-12-06 2008-08-05 Aventis Pharma Sa indóis substituìdos, processo para preparação, bem como utilização dos mesmos, medicamento e composição farmacêutica
EP1838690A2 (en) * 2004-12-21 2007-10-03 Devgen N.V. Compounds with kv4 ion channel activity
EP2308839B1 (en) * 2005-04-20 2017-03-01 Takeda Pharmaceutical Company Limited Fused heterocyclic compounds
FR2884821B1 (fr) * 2005-04-26 2007-07-06 Aventis Pharma Sa Pyrrolopyridines substitues, compositions les contenant, procede de fabrication et utilisation
MY148644A (en) 2005-07-18 2013-05-15 Orion Corp New pharmaceutical compounds
BRPI0620415A2 (pt) * 2005-12-23 2011-11-08 Astrazeneca Ab composto e sais farmaceuticamente e farmacologicamente aceitáveis do mesmo, e enantiÈmeros do composto e sais do mesmo, composição farmaceutica, e, uso de um composto opcionalmente em combinação com um agonista do receptor de gabab, e, métodos para o tratamento de doença, de um distúrbio, e de sìndrome
US7838542B2 (en) * 2006-06-29 2010-11-23 Kinex Pharmaceuticals, Llc Bicyclic compositions and methods for modulating a kinase cascade
ATE478847T1 (de) 2006-09-15 2010-09-15 Pfizer Substituierte pyridylmethylbicyclocarboxyamidverbindungen
EP2222631B1 (en) 2006-10-23 2011-08-17 Pfizer Inc. Substituted phenylmethyl bicyclocarboxyamide compounds
JP2010510202A (ja) 2006-11-17 2010-04-02 ファイザー株式会社 置換ビシクロカルボキシアミド化合物
EP2079687A1 (en) * 2006-12-18 2009-07-22 Ambrx, Inc. Compositions containing, methods involving, and uses of non-natural amino acids and polypeptides
WO2008127199A1 (en) 2007-04-13 2008-10-23 Agency For Science, Technology And Research Methods of controlling tumorigenesis and diagnosing the risk thereof
CN101808995A (zh) * 2007-07-27 2010-08-18 百时美施贵宝公司 新颖的葡糖激酶激活剂及其使用方法
US8513422B2 (en) 2007-08-31 2013-08-20 Astellas Pharma Inc. Piperidine derivative
PL2242491T3 (pl) 2008-02-19 2012-12-31 Dsm Ip Assets Bv Nowatorskie zastosowanie 3,3'-diinodolilometanu
JP5421366B2 (ja) 2008-07-21 2014-02-19 オトノミ―,インク. 制御放出性の耳の構造体調節および生来の免疫システム調節化合物および耳の障害の処置のための方法
KR101258331B1 (ko) 2008-09-11 2013-04-26 화이자 인코포레이티드 헤테로아릴 아미드 유도체 및 글루코키나제 활성화제로서의 그의 용도
MY151246A (en) 2009-03-11 2014-04-30 Pfizer Benzofuranyl derivatives
BR112015004666B1 (pt) 2012-09-07 2022-04-26 Novartis Ag Derivados de indol carboxamida, seu uso, e composição farmacêutica
CN103044311B (zh) * 2012-12-26 2015-04-22 山东大学 一种多取代吲哚类化合物及其制备方法和应用
AU2014256984B2 (en) 2013-04-26 2019-02-14 Indiana University Research & Technology Corporation Hydroxyindole carboxylic acid based inhibitors for oncogenic Src homology-2 domain containing protein tyrosine phosphatase-2 (SHP2)
NZ725860A (en) * 2014-04-04 2019-08-30 Iomet Pharma Ltd Indole derivatives for use in medicine
CN104876851A (zh) * 2015-05-15 2015-09-02 南京大学 一类含吲哚-3羧酸骨架的哌嗪类衍生物的制备方法及在抗癌药物中的应用
EP4234552A3 (en) * 2016-03-09 2023-10-18 Raze Therapeutics, Inc. 3-phosphoglycerate dehydrogenase inhibitors and uses thereof
LT3426243T (lt) 2016-03-09 2021-08-10 Raze Therapeutics, Inc. 3-fosfogliceratdehidrogenazės inhibitoriai ir jų panaudojimas
CA3089678A1 (en) 2018-01-31 2019-08-08 Heparegenix Gmbh Protein kinase mkk4 inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death
WO2019243315A1 (en) 2018-06-21 2019-12-26 Heparegenix Gmbh Tricyclic protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death
US11912701B2 (en) 2018-07-16 2024-02-27 Heparegenix Gmbh Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death
AU2021207236A1 (en) 2020-01-15 2022-08-11 Heparegenix Gmbh 3-benzoyl-1h-pyrrolo[2,3-b]pyridine derivatives as MKK4 inhibitors for treating liver diseases
WO2021225980A1 (en) * 2020-05-04 2021-11-11 Dna-Seq, Inc. Methods and systems for determination of an effective therapeutic regimen and drug discovery
US11857551B1 (en) 2020-07-10 2024-01-02 Ting Therapeutics Llc Methods for the prevention and treatment of hearing loss
WO2024109642A1 (zh) * 2023-07-28 2024-05-30 常州大学 一种苯并氮杂环类化合物作为β2-肾上腺素受体别构调节剂的应用

Family Cites Families (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH01132579A (ja) * 1987-11-19 1989-05-25 Ss Pharmaceut Co Ltd インドール誘導体
GB8827189D0 (en) * 1988-11-21 1988-12-29 Fujisawa Pharmaceutical Co 2(1h)-quinolinone compounds processes for preparation thereof & pharmaceutical composition comprising same
HK1002235A1 (en) * 1989-12-28 1998-08-07 Pharmacia & Upjohn Company Diaromatic substituted anti-aids compounds
US5552534A (en) 1991-08-22 1996-09-03 The Trustees Of The University Of Pennsylvania Non-Peptide peptidomimetics
DE4307883A1 (en) * 1992-03-12 1993-09-23 Westarp Martin Egon Dr Med Use of anti-retroviral substances - to treat motor-neuronal diseases
US5705585A (en) 1993-06-30 1998-01-06 Arqule, Inc. Aminimide-containing molecules and materials as molecular recognition agents
WO1994003427A1 (en) 1992-08-06 1994-02-17 Warner-Lambert Company 2-thioindoles (selenoindoles) and related disulfides (selenides) which inhibit protein tyrosine kinases and which have antitumor properties
US6011175A (en) 1993-05-18 2000-01-04 University Of Pittsburgh Inhibition of farnesyltransferase
US5532167A (en) 1994-01-07 1996-07-02 Beth Israel Hospital Substrate specificity of protein kinases
US5712171A (en) 1995-01-20 1998-01-27 Arqule, Inc. Method of generating a plurality of chemical compounds in a spatially arranged array
FR2733995B1 (fr) * 1995-05-09 1997-07-25 Inst Nat Sante Rech Med Inhibiteurs de l'inactivation de neuropeptides endogenes notamment la cholecystokinine, leurs procedes de preparation leur utilisation comme medicaments et procede de criblage de medicaments
FI974437A7 (fi) 1995-06-06 1997-12-05 Pfizer Substituoituja N-(indoli-2-karbonyyli)amideja ja johdannaisia glykogee nifosforylaasi-inhibiittoreina
CA2224062C (en) 1995-06-06 2001-09-04 Pfizer Limited Substituted n-(indole-2-carbonyl)-glycinamides and derivatives as glycogen phosphorylase inhibitors
US5648378A (en) 1995-06-07 1997-07-15 Research Corporation Technologies, Inc. 2-iminochromene derivatives as inhibitors of protein tyrosine kinase
JPH11512708A (ja) 1995-09-11 1999-11-02 オステオアルスリィティス サイエンシズ,インコーポレイテッド 変形性関節炎を治療するためのプロテインチロシンキナーゼインヒビター
EP0922042A1 (en) * 1996-08-09 1999-06-16 Smithkline Beecham Corporation Novel piperazine containing compounds
US5952322A (en) * 1996-12-05 1999-09-14 Pfizer Inc. Method of reducing tissue damage associated with non-cardiac ischemia using glycogen phosphorylase inhibitors
EP0946587A2 (en) * 1996-12-16 1999-10-06 Fujisawa Pharmaceutical Co., Ltd. New amide compounds
WO1998037070A1 (en) * 1997-02-21 1998-08-27 Takeda Chemical Industries, Ltd. Fused ring compounds, process for producing the same and use thereof
US6420338B1 (en) 1997-06-13 2002-07-16 New York University Medical Center Inhibition of the Src kinase family pathway as a method of treating HBV infection and hepatocellular carcinoma
GB9718913D0 (en) * 1997-09-05 1997-11-12 Glaxo Group Ltd Substituted oxindole derivatives
WO1999054309A1 (en) * 1998-04-23 1999-10-28 Takeda Chemical Industries, Ltd. Naphthalene derivatives, their production and use
JP2002515488A (ja) * 1998-05-15 2002-05-28 ギルフォード ファーマシューティカルズ インコーポレイテッド カルボキサミド化合物、組成物、及びparp活性の抑制方法
WO2000018407A1 (en) * 1998-09-25 2000-04-06 Cephalon, Inc. Methods for preventing/treating damage to sensory hair cells and cochlear neurons
JP4865129B2 (ja) 1999-01-13 2012-02-01 ザ・リサーチ・ファウンデーション・オブ・ステイト・ユニバーシティ・オブ・ニューヨーク タンパク質キナーゼ阻害剤を設計するための新規の方法
US7070936B1 (en) * 1999-01-13 2006-07-04 The Research Foundation Of State University Of New York Method for designing protein kinase inhibitors
DE60023920T2 (de) * 1999-08-27 2006-07-20 Sugen, Inc., South San Francisco Phosphatmimetika und Verfahren zur Behandlung mit Phosphataseinhibitoren HIBITOREN
US6921763B2 (en) * 1999-09-17 2005-07-26 Abbott Laboratories Pyrazolopyrimidines as therapeutic agents
HN2001000008A (es) * 2000-01-21 2003-12-11 Inc Agouron Pharmaceuticals Compuesto de amida y composiciones farmaceuticas para inhibir proteinquinasas, y su modo de empleo
AU2868601A (en) * 2000-01-27 2001-08-07 Ribotargets Ltd Biaryl compounds, their preparation and their use in therapy
SI1255752T1 (sl) * 2000-02-15 2007-12-31 Pharmacia & Upjohn Co Llc S pirolom substituirani zaviralci 2-indolinon protein kinaza
KR100423899B1 (ko) 2000-05-10 2004-03-24 주식회사 엘지생명과학 세포 증식 억제제로 유용한 1,1-디옥소이소티아졸리딘을갖는 인다졸
IL152771A0 (en) * 2000-06-26 2003-06-24 Pfizer Prod Inc PYRROLO(2,3-d) PYRIMIDINE COMPOUNDS AS IMMUNOSUPPRESSIVE AGENTS
EP1301516B1 (en) * 2000-07-07 2006-03-22 Novo Nordisk A/S Modulators of protein tyrosine phosphatases (ptpases)
WO2002072548A2 (en) * 2001-03-09 2002-09-19 Ortho-Mcneil Pharmaceutical, Inc. Heterocyclic compounds and their use as histamine h4 ligands.
KR100429841B1 (ko) 2001-07-19 2004-05-04 삼성전자주식회사 Grin 렌즈를 구비하는 광 기록헤드
US7129225B2 (en) 2001-10-22 2006-10-31 The Research Foundation Of State University Of New York Protection against and treatment of hearing loss
US7005445B2 (en) 2001-10-22 2006-02-28 The Research Foundation Of State University Of New York Protein kinase and phosphatase inhibitors and methods for designing them
JP3975272B2 (ja) 2002-02-21 2007-09-12 独立行政法人産業技術総合研究所 超微細流体ジェット装置
EP1501514B1 (en) 2002-05-03 2012-12-19 Exelixis, Inc. Protein kinase modulators and methods of use
JP4539538B2 (ja) * 2005-11-17 2010-09-08 トヨタ自動車株式会社 エネルギ回収装置
US7838542B2 (en) 2006-06-29 2010-11-23 Kinex Pharmaceuticals, Llc Bicyclic compositions and methods for modulating a kinase cascade

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