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
inhibitor
group
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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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic 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
    • A61K31/403—Heterocyclic 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
    • A61K31/404—Indoles, e.g. pindolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/47—Quinolines; Isoquinolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; 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
    • C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/12—Heterocyclic 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Emergency Medicine (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)
  • Peptides Or Proteins (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (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 (enExample)
EP (1) EP1444204A4 (enExample)
JP (2) JP4623962B2 (enExample)
CA (1) CA2464214C (enExample)
MX (1) MXPA04003758A (enExample)
WO (1) WO2003035621A1 (enExample)

Families Citing this family (50)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR0007532A (pt) * 1999-01-13 2001-11-20 Univ New York State Res Found Métodos para identificar inibidores de proteìnaquinase, para testar compostos para umacapacidade de inibir a atividade de proteìnaquinase e para inibir uma proteìna quinase, inibidorde proteìna tirosina quinase não peptìdica, e,método de tratar uma condição responsiva a uminibidor de proteìna quinase em um paciente
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
CA2464214C (en) * 2001-10-22 2011-02-08 The Research Foundation Of State University Of New York Protein kinase and phosphatase inhibitors, methods for designing them, and methods of using them
WO2003086377A1 (en) 2002-04-18 2003-10-23 Institute Of Medicinal Molecular Design. Inc. Amide derivatives
AU2003261415C1 (en) 2002-08-09 2010-01-14 Merck Sharp & Dohme Corp. Tyrosine kinase inhibitors
EP1534268A4 (en) * 2002-08-09 2006-11-02 Merck & Co Inc TYROSINE KINASE INHIBITORS
ATE409484T1 (de) * 2002-12-17 2008-10-15 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
US7736911B2 (en) 2004-04-15 2010-06-15 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
WO2006055463A2 (en) 2004-11-15 2006-05-26 Bristol-Myers Squibb Company 2-amino-3-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
WO2006055462A1 (en) 2004-11-15 2006-05-26 Bristol-Myers Squibb Company 2-amino-4-functionalized tetralin derivatives and related glycogen phosphorylase inhibitors
GB0425919D0 (en) * 2004-11-25 2004-12-29 Prosidion Ltd Indole-2-carboxylic acid amides
MX2007006764A (es) * 2004-12-06 2007-08-15 Aventis Pharma Sa Indoles sustituidos, composiciones que los contienen, procedimiento de fabricacion y utilizacion.
FR2878849B1 (fr) * 2004-12-06 2008-09-12 Aventis Pharma Sa Indoles substitues, compositions les contenant, procede de fabrication et utilisation
WO2006066879A2 (en) * 2004-12-21 2006-06-29 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
EP1966150A4 (en) * 2005-12-23 2011-07-20 Astrazeneca Ab PYRAZOLE FOR THE TREATMENT OF GERD AND IBS
US7838542B2 (en) * 2006-06-29 2010-11-23 Kinex Pharmaceuticals, Llc Bicyclic compositions and methods for modulating a kinase cascade
JP2010503657A (ja) 2006-09-15 2010-02-04 ファイザー株式会社 置換ピリジルメチルビシクロカルボキサミド化合物
EP2222631B1 (en) 2006-10-23 2011-08-17 Pfizer Inc. Substituted phenylmethyl bicyclocarboxyamide compounds
EP2091944B1 (en) 2006-11-17 2011-05-18 Pfizer Inc. Substituted bicyclocarboxyamide compounds
KR20090100407A (ko) * 2006-12-18 2009-09-23 암브룩스, 인코포레이티드 비천연 아미노산 및 폴리펩티드를 함유하는 조성물, 비천연 아미노산 및 폴리펩티드를 포함하는 방법, 및 비천연 아미노산 및 폴리펩티드의 용도
WO2008127199A1 (en) 2007-04-13 2008-10-23 Agency For Science, Technology And Research Methods of controlling tumorigenesis and diagnosing the risk thereof
EP2173717B9 (en) 2007-07-27 2013-06-26 Bristol-Myers Squibb Company Novel glucokinase activators and methods of using same
US8513422B2 (en) 2007-08-31 2013-08-20 Astellas Pharma Inc. Piperidine derivative
US8420677B2 (en) 2008-02-19 2013-04-16 Dsm Ip Assets B.V. Use of 3,3′-diindolylmethane
CA2731769C (en) 2008-07-21 2013-09-10 Otonomy, Inc. Controlled-release otic structure modulating and innate immune system modulating compositions and methods for the treatment of otic disorders
MX2011002613A (es) 2008-09-11 2011-05-23 Pfizer Derivados de heteroarilamida y su uso como activadores de glucoquinasa.
HRP20130661T1 (en) 2009-03-11 2013-08-31 Pfizer Inc. Benzofuranyl derivatives used as glucokinase inhibitors
CN104603106B (zh) 2012-09-07 2017-05-10 诺华股份有限公司 吲哚甲酰胺衍生物及其用途
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
EP2988741B1 (en) 2013-04-26 2019-11-27 Indiana University Research&Technology Corporation Hydroxyindole carboxylic acid based inhibitors for oncogenic src homology-2 domain containing protein tyrosine phosphatase-2 (shp2)
HRP20201621T1 (hr) * 2014-04-04 2021-03-05 Iomet Pharma Ltd. Derivati indola za uporabu u medicini
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
PL3426244T3 (pl) * 2016-03-09 2023-09-25 Raze Therapeutics, Inc. Inhibitory dehydrogenazy 3-fosfoglicerynianowej i ich zastosowania
HUE055197T2 (hu) 2016-03-09 2021-11-29 Raze Therapeutics Inc 3-Foszfoglicerát-dehidrogenáz inhibitorok és alkalmazásuk
ES3000465T3 (en) 2018-01-31 2025-02-28 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
JP7365393B2 (ja) 2018-07-16 2023-10-19 ヘパリジェニックス ゲーエムベーハー 肝再生促進又は肝細胞死の抑制もしくは防止のためのプロテインキナーゼ阻害剤
CA3164361A1 (en) 2020-01-15 2021-07-22 Heparegenix Gmbh 3-benzoyl-1h-pyrrolo[2,3-b]pyridine derivatives as mkk4 inhibitors for treating liver diseases
US20230183810A1 (en) * 2020-05-04 2023-06-15 Dna-Seq, Inc. Methods and systems for determination of an effective therapeutic regimen and drug discovery
WO2022020114A2 (en) 2020-07-10 2022-01-27 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
CA2071529C (en) * 1989-12-28 2001-03-20 Donna Lee Romero 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
JPH08503450A (ja) 1992-08-06 1996-04-16 ワーナー−ランバート・コンパニー 蛋白チロシンキナーゼを阻害し、かつ抗腫瘍特性を有する２−チオインドール（セレノインドール）および関連ジスルフィド（セレニド）
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
FI974437L (fi) 1995-06-06 1997-12-05 Pfizer Substituoituja N-(indoli-2-karbonyyli)amideja ja johdannaisia glykogeenifosforylaasi-inhibiittoreina
DK0832065T3 (da) 1995-06-06 2001-11-19 Pfizer Substituerede N-(indol-2-carbonyl)glycinamider og derivater som glycogenphosphorylaseinhibitorer
US5648378A (en) 1995-06-07 1997-07-15 Research Corporation Technologies, Inc. 2-iminochromene derivatives as inhibitors of protein tyrosine kinase
WO1997011692A2 (en) 1995-09-11 1997-04-03 Osteoarthritis Sciences, Inc. Protein tyrosine kinase inhibitors for treating osteoarthritis
JP2001506230A (ja) * 1996-08-09 2001-05-15 スミスクライン・ビーチャム・コーポレイション 新規ピペラジン含有化合物
US5952322A (en) * 1996-12-05 1999-09-14 Pfizer Inc. Method of reducing tissue damage associated with non-cardiac ischemia using glycogen phosphorylase inhibitors
WO1998027108A2 (en) 1996-12-16 1998-06-25 Fujisawa Pharmaceutical Co., Ltd. New amide compounds and their use as nitric oxide synthase inhibitors
AU6229698A (en) * 1997-02-21 1998-09-09 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
US6573289B1 (en) * 1998-04-23 2003-06-03 Takeda Chemical Industries, Ltd. Naphthalene derivatives, their production and use
AU9297998A (en) * 1998-05-15 1999-12-06 Guilford Pharmaceuticals Inc. Carboxamide compounds, compositions, and methods for inhibiting parp activity
CA2345295C (en) * 1998-09-25 2009-12-15 Cephalon, Inc. Use of fused pyrrolocarbazoles in preventing/treating damage to sensory hair cells and cochlear neurons
US7070936B1 (en) * 1999-01-13 2006-07-04 The Research Foundation Of State University Of New York Method for designing protein kinase inhibitors
BR0007532A (pt) 1999-01-13 2001-11-20 Univ New York State Res Found Métodos para identificar inibidores de proteìnaquinase, para testar compostos para umacapacidade de inibir a atividade de proteìnaquinase e para inibir uma proteìna quinase, inibidorde proteìna tirosina quinase não peptìdica, e,método de tratar uma condição responsiva a uminibidor de proteìna quinase em um paciente
EP1212296B9 (en) * 1999-08-27 2006-05-10 Sugen, Inc. Phosphate mimics and methods of treatment using phosphatase inhibitors
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
ATE369359T1 (de) * 2000-02-15 2007-08-15 Sugen Inc Pyrrol substituierte indolin-2-on protein kinase inhibitoren
KR100423899B1 (ko) 2000-05-10 2004-03-24 주식회사 엘지생명과학 세포 증식 억제제로 유용한 1,1-디옥소이소티아졸리딘을갖는 인다졸
DK1686130T3 (da) * 2000-06-26 2009-04-06 Pfizer Prod Inc Pyrrolo-[2,3-d]-pyrimidinforbindelser som immunsuppressive midler
ATE321052T1 (de) * 2000-07-07 2006-04-15 Novo Nordisk As Modulatoren von protein tyrosin phosphatasen (ptpasen)
EP1373204B1 (en) * 2001-03-09 2016-10-26 Janssen Pharmaceuticals, Inc. Heterocyclic compounds
KR100429841B1 (ko) 2001-07-19 2004-05-04 삼성전자주식회사 Ｇｒｉｎ 렌즈를 구비하는 광 기록헤드
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
CA2464214C (en) 2001-10-22 2011-02-08 The Research Foundation Of State University Of New York Protein kinase and phosphatase inhibitors, methods for designing them, and methods of using 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
CA2484209C (en) 2002-05-03 2013-06-11 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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US7427608B2 (en) 2008-09-23
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WO2003035621A1 (en) 2003-05-01
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