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

Info

Publication number
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
Authority
JP
Japan
Prior art keywords
src
inhibitors
inhibitor
group
peptide
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 - Lifetime
Application number
JP2003538137A
Other languages
English (en)
Japanese (ja)
Other versions
JP2005514339A (ja
Inventor
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
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.)
Research Foundation of the State University of New York
Original Assignee
Research Foundation of the State University of New York
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 Research Foundation of the State University of New York filed Critical Research Foundation of the State University of New York
Publication of JP2005514339A publication Critical patent/JP2005514339A/ja
Application granted granted Critical
Publication of JP4623962B2 publication Critical patent/JP4623962B2/ja
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Images

Classifications

    • CCHEMISTRY; METALLURGY
    • 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
    • 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
    • A61K31/435Heterocyclic 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/16Otologicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • 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
    • CCHEMISTRY; METALLURGY
    • 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
    • CCHEMISTRY; METALLURGY
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • 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

Landscapes

  • 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)
  • Rheumatology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Emergency Medicine (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (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

Related Child Applications (1)

Application Number Title Priority Date Filing Date
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

Publications (2)

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

Family

ID=26990085

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2003538137A Expired - Lifetime JP4623962B2 (ja) 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
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

Family Applications After (1)

Application Number Title Priority Date Filing Date
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

Country Status (6)

Country Link
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
WO2000042213A1 (en) * 1999-01-13 2000-07-20 The Research Foundation Of State University Of New York A novel method for designing protein kinase inhibitors
WO2003035621A1 (en) * 2001-10-22 2003-05-01 The Research Foundation Of State University Of New York Protein kinase and phosphatase inhibitors, methods for designing them, and methods of using them
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
US7598418B2 (en) 2002-04-18 2009-10-06 Institute Of Medicinal Molecular Design, Inc. Amide derivatives
WO2004014300A2 (en) 2002-08-09 2004-02-19 Merck & Co., Inc. Tyrosine kinase inhibitors
CA2494962C (en) 2002-08-09 2011-06-14 Merck & Co., Inc. Tyrosine kinase inhibitors
WO2004055154A2 (en) * 2002-12-17 2004-07-01 Centre National De La Recherche Scientifique (Cnrs) Use of purine derivatives for inducing differentiation of supernumerary hair cells and deiters' cells in the developing organ of corti for treating deafness
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
US7223786B2 (en) * 2004-11-15 2007-05-29 Bristol-Myers Squibb Company 2-aminonaphthalene derivatives and related glycogen phosphorylase inhibitors
WO2006053274A2 (en) 2004-11-15 2006-05-18 Bristol-Myers Squibb Company 2-amino-1-functionalized tetralin 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
US7226942B2 (en) 2004-11-15 2007-06-05 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
FR2878849B1 (fr) * 2004-12-06 2008-09-12 Aventis Pharma Sa Indoles substitues, compositions les contenant, procede de fabrication et utilisation
KR20070100277A (ko) * 2004-12-06 2007-10-10 아벤티스 파마 소시에떼아노님 치환된 인돌, 그를 함유하는 조성물, 그의 제조 방법 및그의 용도
CN101084209A (zh) * 2004-12-21 2007-12-05 德福根有限公司 具有Kv4离子通道活性的化合物
CA2605778A1 (en) * 2005-04-20 2006-10-26 Takeda Pharmaceutical Company Limited Fused heterocyclic compound
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
CA2632011A1 (en) * 2005-12-23 2007-06-28 Astrazeneca Ab Pyrazoles 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
WO2008032204A1 (en) 2006-09-15 2008-03-20 Pfizer Japan Inc. Substituted pyridylmethyl bicyclocarboxyamide compounds
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
CA2672205A1 (en) * 2006-12-18 2008-06-26 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
JP2010534722A (ja) 2007-07-27 2010-11-11 ブリストル−マイヤーズ スクイブ カンパニー 新規グルコキナーゼ活性化薬およびその使用方法
SI2181990T1 (sl) 2007-08-31 2012-10-30 Astellas Pharma Inc Piperidinski derivat
WO2009103755A1 (en) * 2008-02-19 2009-08-27 Dsm Ip Assets B.V. Novel 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
KR101258331B1 (ko) 2008-09-11 2013-04-26 화이자 인코포레이티드 헤테로아릴 아미드 유도체 및 글루코키나제 활성화제로서의 그의 용도
UA99882C2 (uk) 2009-03-11 2012-10-10 Пфайзер Інк. Похідні бензофуранілу, фармацевтична композиція та спосіб лікування захворювань (варіанти)
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
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)
PT3125883T (pt) * 2014-04-04 2020-10-12 Iomet Pharma Ltd Derivados de indol para utilização na medicina
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
PL3426243T3 (pl) 2016-03-09 2021-10-04 Raze Therapeutics, Inc. Inhibitory dehydrogenazy 3-fosfoglicerynianowej i ich zastosowania
SG11202007143UA (en) 2018-01-31 2020-08-28 Heparegenix Gmbh Protein kinase mkk4 inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death
US11731968B2 (en) 2018-06-21 2023-08-22 Heparegenix Gmbh Tricyclic protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death
SG11202012732UA (en) 2018-07-16 2021-02-25 Heparegenix Gmbh Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death
ES2984974T3 (es) 2020-01-15 2024-10-31 Heparegenix Gmbh Derivados de 3-benzoil-1H-pirrolo[2,3-b]piridina como inhibidores de MKK4 para el tratamiento de hepatopatías
US20230183810A1 (en) * 2020-05-04 2023-06-15 Dna-Seq, Inc. Methods and systems for determination of an effective therapeutic regimen and drug discovery
US20240350492A1 (en) 2020-07-10 2024-10-24 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
ES2093090T3 (es) 1989-12-28 1996-12-16 Upjohn Co Compuestos sustituidos diaromaticos anti-sida.
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
US6297269B1 (en) * 1995-06-06 2001-10-02 Pfizer Inc. Substituted n-(indole-2-carbonyl-) amides and derivatives as glycogen phosphorylase inhibitors
JP3314938B2 (ja) * 1995-06-06 2002-08-19 ファイザー・インコーポレーテッド グリコーゲンホスホリラーゼ抑制剤としての置換されたn−(インドール−2−カルボニル)−グリシンアミド類および誘導体
US5648378A (en) 1995-06-07 1997-07-15 Research Corporation Technologies, Inc. 2-iminochromene derivatives as inhibitors of protein tyrosine kinase
CA2231509C (en) 1995-09-11 2008-07-08 Osteoarthritis Sciences, Inc. Protein tyrosine kinase inhibitors for treating osteoarthritis
WO1998006715A1 (en) * 1996-08-09 1998-02-19 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
WO1998027108A2 (en) 1996-12-16 1998-06-25 Fujisawa Pharmaceutical Co., Ltd. New amide compounds and their use as nitric oxide synthase inhibitors
DE69810760T2 (de) * 1997-02-21 2003-11-20 Takeda Chemical Industries, Ltd. Verbindungen mit kondensierten ringen, verfahren zu ihrer herstellung und ihre anwendung
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
CA2328973A1 (en) * 1998-04-23 1999-10-28 Akio Ojida 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
JP2002525329A (ja) * 1998-09-25 2002-08-13 セフアロン・インコーポレーテツド 感覚毛細胞及び蝸牛ニューロンへの損傷を予防する/処置するための方法
WO2000042213A1 (en) * 1999-01-13 2000-07-20 The Research Foundation Of State University Of New York A novel method for designing protein kinase inhibitors
US7070936B1 (en) * 1999-01-13 2006-07-04 The Research Foundation Of State University Of New York Method for designing protein kinase inhibitors
AU775625B2 (en) * 1999-08-27 2004-08-05 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
BRPI0117360B8 (pt) * 2000-02-15 2021-07-06 Upjohn Co inibidores de proteína de quinase de 2-indolinona de pirrol substituído, seus sais e composições farmacêuticas compreendendo os mesmos
KR100423899B1 (ko) 2000-05-10 2004-03-24 주식회사 엘지생명과학 세포 증식 억제제로 유용한 1,1-디옥소이소티아졸리딘을갖는 인다졸
UA74370C2 (uk) * 2000-06-26 2005-12-15 Пфайзер Продактс Інк. Піроло(2,3-d)піримідинові сполуки як імуносупресори
DE60118195T2 (de) * 2000-07-07 2006-12-14 Novo Nordisk A/S Modulatoren von protein tyrosin phosphatasen (ptpasen)
CA2440438C (en) * 2001-03-09 2011-05-03 Ortho-Mcneil Pharmaceutical, Inc. Heterocyclic compounds
KR100429841B1 (ko) 2001-07-19 2004-05-04 삼성전자주식회사 Grin 렌즈를 구비하는 광 기록헤드
WO2003035621A1 (en) * 2001-10-22 2003-05-01 The Research Foundation Of State University Of New York Protein kinase and phosphatase inhibitors, methods for designing them, and methods of using them
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

Also Published As

Publication number Publication date
US7129225B2 (en) 2006-10-31
JP2009263394A (ja) 2009-11-12
CA2464214C (en) 2011-02-08
CA2464214A1 (en) 2003-05-01
EP1444204A1 (en) 2004-08-11
EP1444204A4 (en) 2009-11-04
US7427608B2 (en) 2008-09-23
US20060172971A1 (en) 2006-08-03
WO2003035621A1 (en) 2003-05-01
JP2005514339A (ja) 2005-05-19
US20040019015A1 (en) 2004-01-29
MXPA04003758A (es) 2005-06-20

Similar Documents

Publication Publication Date Title
JP4623962B2 (ja) 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
JP4865129B2 (ja) 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
Zhang et al. Proteolysis targeting chimeras (PROTACs) of anaplastic lymphoma kinase (ALK)
US8088768B2 (en) Protein kinase and phosphatase inhibitors
CN110423212B (zh) Shp2的基于羟基吲哚羧酸的抑制剂
CA2656165A1 (en) Bicyclic compositions and methods for modulating a kinase cascade
JP7749263B2 (ja) Kat6阻害剤としての化合物
KR20210065097A (ko) 치환된 인돌 및 이의 사용 방법
AU2007341977B2 (en) Targeting of EWS-FLI1 as anti-tumor therapy
Zhao et al. Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors
JP2009242437A (ja) スルホンアミド誘導体
TW200812970A (en) Inhibitors of AKT (protein kinase B)
Edraki et al. 2-Imino 2 H-chromene and 2-(phenylimino) 2 H-chromene 3-aryl carboxamide derivatives as novel cytotoxic agents: synthesis, biological assay, and molecular docking study
AboulMagd et al. Saccharomonosporine A inspiration; synthesis of potent analogues as potential PIM kinase inhibitors
Liu et al. Synthesis and SAR of derivatives based on 2-biarylethylimidazole as bombesin receptor subtype-3 (BRS-3) agonists for the treatment of obesity
KR20220122597A (ko) 약학적 화합물
EP4393908A1 (en) Bis-pyrazolyl-methane compounds affecting kras
US7662750B2 (en) Protein-protein interaction antagonist screening libraries based upon 1,4-disubstituted naphthalenes and related scaffolds
JP7779908B2 (ja) アリールピロール誘導体の薬学的塩
Tosso Design and synthesis of small molecule disruptors of EWS-FLI1 in Ewing's sarcoma
WO2025184565A1 (en) Targeted protein modification
Jones The design and synthesis of novel epigenetic modulators
Deschamps Targeting HDAC6 with chemical modulators: catalytic inhibition and beyond

Legal Events

Date Code Title Description
A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20050803

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20090107

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20090107

RD04 Notification of resignation of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7424

Effective date: 20090313

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20090406

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20090413

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20090707

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20090805

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20091104

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20091111

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20100204

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20100308

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20100625

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20100813

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20100823

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

Free format text: JAPANESE INTERMEDIATE CODE: A911

Effective date: 20100915

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: 20101004

A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20101102

R150 Certificate of patent or registration of utility model

Ref document number: 4623962

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

Free format text: JAPANESE INTERMEDIATE CODE: R150

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20131112

Year of fee payment: 3

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

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

EXPY Cancellation because of completion of term