WO2002020495A3 - Inhibiteurs de glycogene-synthase kinase 3 - Google Patents

Inhibiteurs de glycogene-synthase kinase 3 Download PDF

Info

Publication number
WO2002020495A3
WO2002020495A3 PCT/US2001/042081 US0142081W WO0220495A3 WO 2002020495 A3 WO2002020495 A3 WO 2002020495A3 US 0142081 W US0142081 W US 0142081W WO 0220495 A3 WO0220495 A3 WO 0220495A3
Authority
WO
WIPO (PCT)
Prior art keywords
gsk3
glycogen synthase
synthase kinase
disorders
compositions
Prior art date
Application number
PCT/US2001/042081
Other languages
English (en)
Other versions
WO2002020495A2 (fr
Inventor
John M Nuss
Stephen D Harrison
David B Ring
Rustum S Boyce
Kirk Johnson
Keith B Pfister
Savithri Ramurthy
Lynn Seely
Allan S Wagman
Manoj Desai
Barry H Levine
Original Assignee
Chiron Corp
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 Chiron Corp filed Critical Chiron Corp
Priority to AU9502601A priority Critical patent/AU9502601A/xx
Priority to JP2002525117A priority patent/JP2004514656A/ja
Priority to KR1020037003327A priority patent/KR100816769B1/ko
Priority to AU2001295026A priority patent/AU2001295026B2/en
Priority to EP01975734A priority patent/EP1317433A2/fr
Publication of WO2002020495A2 publication Critical patent/WO2002020495A2/fr
Publication of WO2002020495A3 publication Critical patent/WO2002020495A3/fr
Priority to HK05104683.9A priority patent/HK1072936A1/xx

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P37/04—Immunostimulants
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/79—Acids; Esters
    • C07D213/80—Acids; Esters in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/84—Nitriles
    • C07D213/85—Nitriles in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • 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
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)

Abstract

L'invention concerne de nouveaux composés à base de pyrimidine ou de pyridine, des compositions les renfermant, ainsi que des méthodes d'inhibition de l'activité de glycogène-synthase kinase (GSK3) in vitro et de traitement de maladies occasionnées par GSK3. Les méthodes, composés et compositions selon l'invention peuvent être employés seuls ou en combinaison avec d'autres agents pharmacologiquement actifs dans le traitement de maladies occasionnées par l'activité GSK3, telles que diabète, maladie d'Alzheimer et autres maladies neuro-dégénératives, obésité, maladies cardiovasculaires athéroscléreuses, hypertension artérielle essentielle, syndrome des ovaires polykystiques, syndrome X, ischémie, lésions cérébrales traumatiques, affections bipolaires, immunodéficience ou cancer.
PCT/US2001/042081 2000-09-06 2001-09-06 Inhibiteurs de glycogene-synthase kinase 3 WO2002020495A2 (fr)

Priority Applications (6)

Application Number Priority Date Filing Date Title
AU9502601A AU9502601A (en) 2000-09-06 2001-09-06 Inhibitors of glycogen synthase kinase 3
JP2002525117A JP2004514656A (ja) 2000-09-06 2001-09-06 グリコゲンシンターゼキナーゼ３のインヒビター
KR1020037003327A KR100816769B1 (ko) 2000-09-06 2001-09-06 글리코겐 합성효소 키나아제 3의 억제제
AU2001295026A AU2001295026B2 (en) 2000-09-06 2001-09-06 Inhibitors of glycogen synthase kinase 3
EP01975734A EP1317433A2 (fr) 2000-09-06 2001-09-06 Inhibiteurs de glycogene-synthase kinase 3
HK05104683.9A HK1072936A1 (en) 2000-09-06 2005-06-03 Inhibitors of glycogen synthase kinase 3

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US23048000P 2000-09-06 2000-09-06
US60/230,480 2000-09-06

Publications (2)

Publication Number Publication Date
WO2002020495A2 WO2002020495A2 (fr) 2002-03-14
WO2002020495A3 true WO2002020495A3 (fr) 2002-06-20

Family

ID=22865391

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2001/042081 WO2002020495A2 (fr) 2000-09-06 2001-09-06 Inhibiteurs de glycogene-synthase kinase 3

Country Status (7)

Country Link
EP (1) EP1317433A2 (fr)
JP (1) JP2004514656A (fr)
KR (2) KR100816769B1 (fr)
CN (1) CN100506801C (fr)
AU (2) AU2001295026B2 (fr)
HK (1) HK1072936A1 (fr)
WO (1) WO2002020495A2 (fr)

Families Citing this family (60)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE416175T1 (de) * 2001-02-20 2008-12-15 Astrazeneca Ab 2-arylaminopyrimidine zur behandlung von mit gsk3 in zusammenhang stehenden erkrankungen
EP1373257B9 (fr) 2001-03-29 2008-10-15 Vertex Pharmaceuticals Incorporated Inhibiteurs de kinases n-terminales c-jun (jnk) et autres proteineskinases
TWI330183B (fr) 2001-10-22 2010-09-11 Eisai R&D Man Co Ltd
CA2487948A1 (fr) 2002-06-14 2003-12-24 Applied Research Systems Ars Holding N.V. Derives de cyanure d'azole methylidene et leur utilisation comme modulateurs de proteine kinase
US7304071B2 (en) * 2002-08-14 2007-12-04 Vertex Pharmaceuticals Incorporated Protein kinase inhibitors and uses thereof
CN1717391A (zh) 2002-10-21 2006-01-04 希龙公司 糖元合成酶激酶3的抑制剂
ATE454378T1 (de) * 2002-11-01 2010-01-15 Vertex Pharma Verbindungen, die sich als inhibitoren vonjak und anderen proteinkinasen eignen
ES2289349T3 (es) * 2002-11-04 2008-02-01 Vertex Pharmaceuticals Incorporated Derivados de heteroaril-pirimidina como inhibidores de jak.
JP2006508107A (ja) * 2002-11-05 2006-03-09 バーテックス　ファーマシューティカルズ　インコーポレイテッド Ｊａｋおよび他のプロテインキナーゼのインヒビターとして有用な化合物
MXPA05005477A (es) * 2002-11-21 2005-07-25 Chiron Corp Pirimidinas 2,4,6-trisustituidas como inhibidores de fosfotidilinositol (pi) 3-cinasa y su uso en el tratamiento del cancer.
JPWO2004054617A1 (ja) * 2002-12-13 2006-04-20 協和醗酵工業株式会社 中枢疾患の予防および／または治療剤
CA2524161C (fr) 2003-05-08 2013-01-15 Applied Research Systems Ars Holding N.V. Acetonitriles de pyridinyle
TWI334868B (en) * 2003-06-03 2010-12-21 Nippon Kayaku Kk [1,2,4] triazoro [1,5-a] pyrimidine-2-ylurea derivative and use thereof
AU2004272306A1 (en) * 2003-09-12 2005-03-24 Merck Serono Sa Benzimidazole acetonitriles
EP1668004A1 (fr) * 2003-09-12 2006-06-14 Applied Research Systems ARS Holding N.V. Derives de benzoxazole-acetonitrile
US20070129383A1 (en) * 2003-10-17 2007-06-07 Hiroshi Kuramochi Substituted 2-amino-[1,2,4]triazolo[1,5-a]pyrimidine derivative and use thereof
GB0324551D0 (en) * 2003-10-21 2003-11-26 Karobio Ab Novel compounds
WO2005040135A1 (fr) * 2003-10-24 2005-05-06 Ono Pharmaceutical Co., Ltd. Medicament antistress et usage medical correspondant
ZA200602664B (en) * 2003-12-03 2007-06-27 Cytopia Res Pty Ltd Tubulin inhibitors
HUP0400405A3 (en) * 2004-02-10 2009-03-30 Sanofi Synthelabo Pyrimidine derivatives, process for producing them, their use, pharmaceutical compositions containing them and their intermediates
EP1768679B1 (fr) * 2004-07-09 2012-08-22 Agency for Science, Technology and Research Modulation de gsk-3beta et procede de traitement des maladies proliferatives
WO2006066172A1 (fr) 2004-12-17 2006-06-22 Amgen, Inc. Composes d'aminopyrimidine et procedes d'utilisation correspondants
US7759342B2 (en) 2005-01-13 2010-07-20 Signal Pharmaceuticals, Llc Methods of treatment and prevention using haloaryl substituted aminopurines
US7723340B2 (en) 2005-01-13 2010-05-25 Signal Pharmaceuticals, Llc Haloaryl substituted aminopurines, compositions thereof, and methods of treatment therewith
US7521446B2 (en) 2005-01-13 2009-04-21 Signal Pharmaceuticals, Llc Haloaryl substituted aminopurines, compositions thereof, and methods of treatment therewith
US9101722B2 (en) 2005-02-28 2015-08-11 Novo Nordisk A/S Dose setting mechanism for an injection device capable of presetting a maximum dose
ES2270715B1 (es) 2005-07-29 2008-04-01 Laboratorios Almirall S.A. Nuevos derivados de pirazina.
WO2007025177A2 (fr) 2005-08-26 2007-03-01 Braincells, Inc. Neurogenese par modulation du recepteur muscarinique
EP2258359A3 (fr) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenèse par modulation des récepteurs muscariniques avec sabcomeline
ES2274712B1 (es) 2005-10-06 2008-03-01 Laboratorios Almirall S.A. Nuevos derivados imidazopiridina.
WO2007047978A2 (fr) 2005-10-21 2007-04-26 Braincells, Inc. Modulation de la neurogenese par inhibition de la pde
US20070112017A1 (en) 2005-10-31 2007-05-17 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
WO2007117399A2 (fr) 2006-03-31 2007-10-18 Janssen Pharmaceutica N.V. Benzoimidazol-2-yl pyrimidines et pyrazines modulatrices du récepteur de l'histamine h4
EP2004188B1 (fr) 2006-03-31 2010-09-01 Janssen Pharmaceutica NV Benzoimidazol-2-yl pyridines modulatrices du récepteur de l'histamine h4
JP2009536669A (ja) 2006-05-09 2009-10-15 ブレインセルス，インコーポレイティド アンジオテンシン調節による神経新生
KR20090115866A (ko) 2007-03-05 2009-11-09 교와 핫꼬 기린 가부시키가이샤 의약 조성물
US8084466B2 (en) 2007-12-18 2011-12-27 Janssen Pharmaceutica Nv Bicyclic heteroaryl-substituted imidazoles as modulators of the histamine H4 receptor
US9371311B2 (en) 2008-06-30 2016-06-21 Janssen Pharmaceutica Nv Benzoimidazol-2-yl pyrimidine derivatives
DE102008035552A1 (de) * 2008-07-30 2010-02-04 Bayer Schering Pharma Aktiengesellschaft Substituierte Pyridine und ihre Verwendung
WO2010099217A1 (fr) 2009-02-25 2010-09-02 Braincells, Inc. Modulation de neurogenèse à l'aide de combinaisons de d-cyclosérine
DK2401010T3 (en) 2009-02-26 2018-07-23 Shl Group Ab DOSE ADJUSTMENT MECHANISM
WO2011082268A2 (fr) 2009-12-30 2011-07-07 Arqule Inc. Composés naphthalényl-pyrimidine substitués
WO2012175711A1 (fr) 2011-06-24 2012-12-27 INSERM (Institut National de la Santé et de la Recherche Médicale) Procédé pour prédire la réponse à une chimiothérapie d'un patient atteint d'un ostéosarcome
EP2554662A1 (fr) 2011-08-05 2013-02-06 M Maria Pia Cosma Procédés pour le traitement de maladies rétiniennes dégénératives
MX342326B (es) 2011-09-27 2016-09-26 Novartis Ag 3-pirimidin-4-il-oxazolidin-2-onas como inhibidoras de idh mutante.
UY34632A (es) 2012-02-24 2013-05-31 Novartis Ag Compuestos de oxazolidin- 2- ona y usos de los mismos
BR112015007182A2 (pt) * 2012-10-05 2017-07-04 Rigel Pharmaceuticals Inc inibidores de gdf-8
US9296733B2 (en) 2012-11-12 2016-03-29 Novartis Ag Oxazolidin-2-one-pyrimidine derivative and use thereof for the treatment of conditions, diseases and disorders dependent upon PI3 kinases
UY35370A (es) 2013-03-06 2014-09-30 Janssen Pharmaceutica Nv Moduladores benzoimidazol-2-il pirimidina del receptor de histamina h4
WO2014141104A1 (fr) 2013-03-14 2014-09-18 Novartis Ag 3-pyrimidin-4-yl-oxazolidin-2-ones comme inhibiteurs d'idh mutante
GB201312800D0 (en) 2013-07-17 2013-08-28 Heptares Therapeutics Ltd mGlu5 modulators
WO2015155738A2 (fr) 2014-04-09 2015-10-15 Christopher Rudd Utilisation d'inhibiteurs ou d'activateurs de gsk -3 qui modulent l'expression de pd -1 ou de t-bet pour moduler l'immunité due aux lymphocytes t
EP3313420B1 (fr) 2015-06-25 2024-03-13 The Children's Medical Center Corporation Procédés et compositions se rapportant à l'expansion, l'enrichissement et la conservation de cellules souches hématopoïétiques
AU2017235461B2 (en) 2016-03-15 2023-02-23 Children's Medical Center Corporation Methods and compositions relating to hematopoietic stem cell expansion
EP3231434A1 (fr) 2016-04-14 2017-10-18 Fundacio Centre de Regulacio Genomica Procédé de traitement de la maladie de parkinson
US11331313B2 (en) 2017-05-22 2022-05-17 Whitehead Institute For Biomedical Research KCC2 expression enhancing compounds and uses thereof
EP3920885A1 (fr) 2019-02-08 2021-12-15 Frequency Therapeutics, Inc. Composés d'acide valproïque et agonistes wnt pour le traitement de troubles de l'oreille
CN113293046B (zh) * 2021-05-26 2021-11-30 安徽博洋润滑科技有限公司 一种低发尘润滑脂及其制备方法

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0710659A1 (fr) * 1994-11-02 1996-05-08 Takeda Chemical Industries, Ltd. Dérivés d'oxazolidinedione, leur fabrication et leur application
US5741796A (en) * 1994-05-27 1998-04-21 Merck & Co., Inc. Pyridyl and naphthyridyl compounds for inhibiting osteoclast-mediated bone resorption
WO1998024782A2 (fr) * 1996-12-05 1998-06-11 Amgen Inc. Composes pyrimidines substitues et leur utilisation
WO1999065897A1 (fr) * 1998-06-19 1999-12-23 Chiron Corporation Inhibiteurs de glycogene synthase kinase 3

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3627922A1 (de) * 1986-08-18 1988-03-03 Henkel Kgaa Neue tetraaminopyrimidin-derivate und deren verwendung in haarfaerbemitteln
ZA959204B (en) * 1994-11-02 1997-04-30 Takeda Chemical Industries Ltd Oxazolidinedioe derivatives their production and use
NZ335997A (en) * 1996-12-05 2001-08-31 Amgen Inc Substituted pyrimidine compounds for treating TNF and interleukin diseases

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5741796A (en) * 1994-05-27 1998-04-21 Merck & Co., Inc. Pyridyl and naphthyridyl compounds for inhibiting osteoclast-mediated bone resorption
EP0710659A1 (fr) * 1994-11-02 1996-05-08 Takeda Chemical Industries, Ltd. Dérivés d'oxazolidinedione, leur fabrication et leur application
WO1998024782A2 (fr) * 1996-12-05 1998-06-11 Amgen Inc. Composes pyrimidines substitues et leur utilisation
WO1999065897A1 (fr) * 1998-06-19 1999-12-23 Chiron Corporation Inhibiteurs de glycogene synthase kinase 3

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
S.C.CONNOR: "ANTIDIABETIC EFFICACY OF BRL 49653", J. PHARM. PHARMACOL., vol. 49, no. 3, 1 March 1997 (1997-03-01), ENGL., pages 336 - 344, XP002080751 *

Also Published As

Publication number Publication date
EP1317433A2 (fr) 2003-06-11
KR20080013026A (ko) 2008-02-12
KR100860827B1 (ko) 2008-09-30
AU9502601A (en) 2002-03-22
HK1072936A1 (en) 2005-09-16
JP2004514656A (ja) 2004-05-20
KR20040030404A (ko) 2004-04-09
CN1592743A (zh) 2005-03-09
KR100816769B1 (ko) 2008-03-26
AU2001295026B2 (en) 2008-04-03
WO2002020495A2 (fr) 2002-03-14
CN100506801C (zh) 2009-07-01

Similar Documents

Publication Publication Date Title
WO2002020495A3 (fr) Inhibiteurs de glycogene-synthase kinase 3
AU4956699A (en) Inhibitors of glycogen synthase kinase 3
WO2001044246A8 (fr) Inhibiteurs bicycliques de synthase kinase 3 de glycogene
PT1237880E (pt) Inibidores baseados em pirazina da cinase 3 da glicogénio sintase
AU2003268184A1 (en) Pyrrole based inhibitors of glycogen synthase kinase 3
WO2004078116A3 (fr) Inhibiteurs de la p 38 et leurs procedes d'utilisation
WO2007041365A3 (fr) Composes organiques
IL161829A (en) 1,2,4 - thiadiazole derivatives, some of which are novel and pharmaceutical compositions comprising the same for treating disorders mediated by melanocortin receptor modulators
WO2007056163A3 (fr) Aminopyrimidines utiles en tant qu'inhibiteurs de kinases
WO2006034235A3 (fr) Inhibiteurs quinoline et quinazoline a substitution inhibant la quinone reductase 2
WO2007079214A3 (fr) Antagonistes du recepteur de la prokineticine 2
WO2004078747A8 (fr) Nouveaux derives de cyanopyridine utiles dans le traitement du cancer et d'autres troubles
WO2000006085A3 (fr) Composes et procedes
WO2002096361A3 (fr) Derives de 5-aralkylsulfonyl-3-(pyrrol-2-ylmethylidene)-2-indolinone utilises comme inhibiteurs de kinase
WO2004058769A3 (fr) Compositions utiles en tant qu'inhibiteurs des proteine kinases
WO2001012199A3 (fr) Effet synergique de la methoxyamide sur l'activite anticancereuse de la temozolomide
WO2005086656A3 (fr) Derives d'heteroarylaminopyrazole utilises pour traiter le diabete
WO2004009549A3 (fr) Piperidines utiles pour traiter des maladies du systeme nerveux central
WO2007079163A3 (fr) Antagonistes du recepteur de la prokineticine 1
WO2006034491A3 (fr) Composes a base de quinoleine et de quinazoline a substitution phenylique pour le traitement du diabete
WO2002078745A3 (fr) Compositions et utilisations d'antagonistes de mglur5
WO2003020280A3 (fr) Compositions et methodes de traitement du cancer
WO2007022305A3 (fr) 2-aminoimidazopyridines destinees a traiter des maladies neurodegeneratives
WO2003057149A3 (fr) Heteropyrimidines et hetero-4-pyrimidones fusionnees substituees en position 4, compositions pharmaceutiques les contenant et leur utilisation dans le traitement ou la prevention de maladies et de troubles a mediation par de7¿b?
WO2005121102A3 (fr) Inhibiteur du facteur viia

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A2

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY BZ CA CH CN CO CR CU CZ DE DK DM DZ EC EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NO NZ PH PL PT RO RU SD SE SG SI SK SL TJ TM TR TT TZ UA UG UZ VN YU ZA ZW

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE TR BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG

121 Ep: the epo has been informed by wipo that ep was designated in this application
AK Designated states

Kind code of ref document: A3

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY BZ CA CH CN CO CR CU CZ DE DK DM DZ EC EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NO NZ PH PL PT RO RU SD SE SG SI SK SL TJ TM TR TT TZ UA UG UZ VN YU ZA ZW

AL Designated countries for regional patents

Kind code of ref document: A3

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE TR BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG

DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
WWE Wipo information: entry into national phase

Ref document number: 2002525117

Country of ref document: JP

WWE Wipo information: entry into national phase

Ref document number: 277/KOLNP/2003

Country of ref document: IN

WWE Wipo information: entry into national phase

Ref document number: 1020037003327

Country of ref document: KR

WWE Wipo information: entry into national phase

Ref document number: 2001295026

Country of ref document: AU

WWE Wipo information: entry into national phase

Ref document number: 2001975734

Country of ref document: EP

WWE Wipo information: entry into national phase

Ref document number: 018184251

Country of ref document: CN

WWP Wipo information: published in national office

Ref document number: 2001975734

Country of ref document: EP

REG Reference to national code

Ref country code: DE

Ref legal event code: 8642

WWP Wipo information: published in national office

Ref document number: 1020037003327

Country of ref document: KR