CA2464214C - Protein kinase and phosphatase inhibitors, methods for designing them, and methods of using them - Google Patents

Protein kinase and phosphatase inhibitors, methods for designing them, and methods of using them Download PDF

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Publication number
CA2464214C
CA2464214C CA2464214A CA2464214A CA2464214C CA 2464214 C CA2464214 C CA 2464214C CA 2464214 A CA2464214 A CA 2464214A CA 2464214 A CA2464214 A CA 2464214A CA 2464214 C CA2464214 C CA 2464214C
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CA
Canada
Prior art keywords
inhibitors
src
inhibitor
day
protein
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
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CA2464214A
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English (en)
French (fr)
Other versions
CA2464214A1 (en
Inventor
David G. Hangauer, Jr.
Moustafa E. El-Araby
Karen L. Milkiewicz
Thomas Nicotera
Donald Henderson
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.)
Park Roswell Cancer Institute
Research Foundation of the State University of New York
Original Assignee
Park Roswell Cancer Institute
Research Foundation of the State University of New York
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Publication of CA2464214A1 publication Critical patent/CA2464214A1/en
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Publication of CA2464214C publication Critical patent/CA2464214C/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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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)
  • Orthopedic Medicine & Surgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Emergency Medicine (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole 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)
CA2464214A 2001-10-22 2002-10-19 Protein kinase and phosphatase inhibitors, methods for designing them, and methods of using them Expired - Fee Related CA2464214C (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US33619101P 2001-10-22 2001-10-22
US60/336,191 2001-10-22
US41072602P 2002-09-13 2002-09-13
US60/410,726 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

Publications (2)

Publication Number Publication Date
CA2464214A1 CA2464214A1 (en) 2003-05-01
CA2464214C true CA2464214C (en) 2011-02-08

Family

ID=26990085

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2464214A Expired - Fee Related CA2464214C (en) 2001-10-22 2002-10-19 Protein kinase and phosphatase inhibitors, methods for designing them, and methods of using them

Country Status (6)

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

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9522881B2 (en) 2013-04-26 2016-12-20 Indiana University Research And Technology Corporation Hydroxyindole carboxylic acid based inhibitors for oncogenic Src homology-2 domain containing protein tyrosine phosphatase-2 (SHP2)

Families Citing this family (49)

* 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
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
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
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
WO2004014300A2 (en) * 2002-08-09 2004-02-19 Merck & Co., Inc. Tyrosine kinase inhibitors
EP1585523B1 (en) * 2002-12-17 2008-10-01 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
JP5001650B2 (ja) * 2003-07-11 2012-08-15 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング ベンズイミダゾールカルボキサミド
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
US7226942B2 (en) 2004-11-15 2007-06-05 Bristol-Myers Squibb Company 2-amino-4-functionalized tetralin 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
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
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
US8957070B2 (en) 2005-04-20 2015-02-17 Takeda Pharmaceutical Company Limited Glucokinase activator compounds, methods of activating glucokinase and methods of treating diabetes and obesity
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
CA2663408C (en) 2006-09-15 2011-11-01 Pfizer Inc. Substituted pyridylmethyl bicyclocarboxyamide compounds
ATE520651T1 (de) 2006-10-23 2011-09-15 Pfizer Substituierte phenylmethylbicyclocarbonsäureamidverbindungen
WO2008059370A2 (en) 2006-11-17 2008-05-22 Pfizer Japan Inc. Substituted bicyclocarboxyamide compounds
CN101578264A (zh) * 2006-12-18 2009-11-11 Ambrx公司 含有非天然氨基酸和多肽的组合物、涉及非天然氨基酸和多肽的方法以及非天然氨基酸和多肽的用途
WO2008127199A1 (en) 2007-04-13 2008-10-23 Agency For Science, Technology And Research Methods of controlling tumorigenesis and diagnosing the risk thereof
ES2408384T3 (es) * 2007-07-27 2013-06-20 Bristol-Myers Squibb Company Nuevos activadores de glucoquinasa y procedimientos de uso de los mismos
KR20100050444A (ko) 2007-08-31 2010-05-13 아스텔라스세이야쿠 가부시키가이샤 피페리딘 유도체
WO2009103755A1 (en) * 2008-02-19 2009-08-27 Dsm Ip Assets B.V. Novel use of 3,3'-diindolylmethane
EP2306975A4 (en) 2008-07-21 2012-10-31 Otonomy Inc COMPOSITIONS WITH A TAXED RELEASE FOR MODULATING THE EARM STRUCTURE AND THE BORN IMMUNE SYSTEM, AND METHODS OF TREATING EAR OR DISEASE
AU2009290474A1 (en) 2008-09-11 2010-03-18 Pfizer Inc. Heteroaryls amide derivatives and their use as glucokinase activators
EP2604604A1 (en) 2009-03-11 2013-06-19 Pfizer Inc Benzofuranyl derivatives used as glucokinase inhibitors
ES2660210T3 (es) 2012-09-07 2018-03-21 Novartis Ag Derivados de indolcarboxamida y usos de los mismos
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
US10167257B2 (en) * 2014-04-04 2019-01-01 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
DK3426243T3 (da) 2016-03-09 2021-07-19 Raze Therapeutics Inc 3-phosphoglyceratdehydrogenase-inhibitorer og anvendelser deraf
NZ766594A (en) 2018-01-31 2025-12-19 Heparegenix Gmbh Protein kinase mkk4 inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death
EP3810139A1 (en) 2018-06-21 2021-04-28 HepaRegeniX GmbH Tricyclic protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death
IL279641B2 (en) 2018-07-16 2024-04-01 Heparegenix Gmbh Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death
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
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
DE69028552T2 (de) 1989-12-28 1997-03-06 The Upjohn Co., Kalamazoo, Mich. Diaromatische substituierte verbindungen gegen den aids-virus
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
DE69523182T2 (de) * 1995-06-06 2002-02-07 Pfizer Substituierte n-(indol-2-carbonyl)-glycinamide und derivate als glycogen phosphorylase inhibitoren
FI974437A7 (fi) * 1995-06-06 1997-12-05 Pfizer Substituoituja N-(indoli-2-karbonyyli)amideja ja johdannaisia glykogee nifosforylaasi-inhibiittoreina
US5648378A (en) * 1995-06-07 1997-07-15 Research Corporation Technologies, Inc. 2-iminochromene derivatives as inhibitors of protein tyrosine kinase
AU709191B2 (en) * 1995-09-11 1999-08-26 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
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
EP1073640B1 (en) * 1998-04-23 2005-04-13 Takeda Pharmaceutical Company Limited Naphthalene derivatives, their production and use
CA2332279A1 (en) * 1998-05-15 1999-11-25 Jia-He Li Carboxamide compounds, compositions, and methods for inhibiting parp activity
EP1126855B1 (en) * 1998-09-25 2007-05-09 Cephalon, Inc. Use of fused pyrrolocarbazoles for 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
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
WO2001016097A1 (en) * 1999-08-27 2001-03-08 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
JP3663382B2 (ja) * 2000-02-15 2005-06-22 スージェン・インコーポレーテッド ピロール置換２−インドリノン蛋白質キナーゼ阻害剤
KR100423899B1 (ko) 2000-05-10 2004-03-24 주식회사 엘지생명과학 세포 증식 억제제로 유용한 1,1-디옥소이소티아졸리딘을갖는 인다졸
ATE423120T1 (de) * 2000-06-26 2009-03-15 Pfizer Prod Inc Pyrroloä2,3-düpyrimidin verbindungen als immunosuppressive wirkstoffe
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
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

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9522881B2 (en) 2013-04-26 2016-12-20 Indiana University Research And Technology Corporation Hydroxyindole carboxylic acid based inhibitors for oncogenic Src homology-2 domain containing protein tyrosine phosphatase-2 (SHP2)

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