DE60107857D1 - 3-indolyl-4-phenyl-1h-pyrrol-2,5-dion derivate als glycogen synthase kinase 3beta inhibitoren - Google Patents

3-indolyl-4-phenyl-1h-pyrrol-2,5-dion derivate als glycogen synthase kinase 3beta inhibitoren

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Publication number
DE60107857D1
DE60107857D1 DE60107857T DE60107857T DE60107857D1 DE 60107857 D1 DE60107857 D1 DE 60107857D1 DE 60107857 T DE60107857 T DE 60107857T DE 60107857 T DE60107857 T DE 60107857T DE 60107857 D1 DE60107857 D1 DE 60107857D1
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DE
Germany
Prior art keywords
pyrrol
indolyl
phenyl
glycogen synthase
synthase kinase
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
Application number
DE60107857T
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English (en)
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DE60107857T2 (de
Inventor
Leyi Gong
Andrew Grupe
Allen Peltz
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F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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Publication of DE60107857D1 publication Critical patent/DE60107857D1/de
Application granted granted Critical
Publication of DE60107857T2 publication Critical patent/DE60107857T2/de
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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    • 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
    • C07D401/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
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    • A61P17/00Drugs for dermatological disorders
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    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • 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
    • C07D403/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Obesity (AREA)
  • Immunology (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Reproductive Health (AREA)
  • Otolaryngology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
DE60107857T 2000-07-27 2001-07-18 3-Indolyl-4-Phenyl-1H-Pyrrol-2,5-Dion-Derivate als Glycogen Synthase-Kinase 3Beta Inhibitoren Expired - Fee Related DE60107857T2 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US22105800P 2000-07-27 2000-07-27
US221058P 2000-07-27
PCT/EP2001/008293 WO2002010158A2 (en) 2000-07-27 2001-07-18 3-indolyl-4-phenyl-1h-pyrrole-2,5-dione derivatives as inhibitors of glycogen synthase kinase-3beta

Publications (2)

Publication Number Publication Date
DE60107857D1 true DE60107857D1 (de) 2005-01-20
DE60107857T2 DE60107857T2 (de) 2005-12-08

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Family Applications (1)

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DE60107857T Expired - Fee Related DE60107857T2 (de) 2000-07-27 2001-07-18 3-Indolyl-4-Phenyl-1H-Pyrrol-2,5-Dion-Derivate als Glycogen Synthase-Kinase 3Beta Inhibitoren

Country Status (32)

Country Link
US (2) US6479490B2 (de)
EP (1) EP1307447B1 (de)
JP (1) JP3984157B2 (de)
KR (1) KR20030017655A (de)
CN (1) CN1185229C (de)
AR (1) AR033989A1 (de)
AT (1) ATE284885T1 (de)
AU (1) AU2001293702A1 (de)
BR (1) BR0112965A (de)
CA (1) CA2417277A1 (de)
CZ (1) CZ2003555A3 (de)
DE (1) DE60107857T2 (de)
EC (1) ECSP034452A (de)
ES (1) ES2233691T3 (de)
GT (1) GT200100151A (de)
HK (1) HK1058670A1 (de)
HR (1) HRP20030030A2 (de)
HU (1) HUP0301431A2 (de)
IL (1) IL153851A0 (de)
JO (1) JO2293B1 (de)
MA (1) MA26936A1 (de)
MX (1) MXPA03000695A (de)
NO (1) NO20030328L (de)
NZ (1) NZ523462A (de)
PA (1) PA8523001A1 (de)
PE (1) PE20020338A1 (de)
PL (1) PL366701A1 (de)
RU (1) RU2003104796A (de)
UY (1) UY26857A1 (de)
WO (1) WO2002010158A2 (de)
YU (1) YU4403A (de)
ZA (1) ZA200300216B (de)

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EP1224932A4 (de) * 1999-08-20 2002-10-16 Sagami Chem Res Wirkstoffe zur hemmung des zelltods
US6900041B2 (en) * 2000-10-02 2005-05-31 Reddy Us Therapeutics Inc. Methods and compositions for the treatment of inflammatory diseases
NZ525656A (en) * 2000-11-07 2004-12-24 Novartis Ag Indolylmaleimide derivatives as protein kinase C inhibitors
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US20040267028A1 (en) * 2001-09-24 2004-12-30 Smith Roger A Preparation and use of pyrrole derivatives for treating obesity
CA2471565C (en) * 2002-01-10 2009-10-27 Patricia Ann Day-Lollini Use of a gsk-3beta inhibitor in the manufacture of a medicament for increasing bone formation
ATE346070T1 (de) 2002-03-05 2006-12-15 Lilly Co Eli Purinderivate als kinaseinhibitoren
AU2003217596A1 (en) 2002-03-08 2003-09-22 Eli Lilly And Company Pyrrole-2, 5-dione derivatives and their use as GSK-3 inhibitors
SE0302546D0 (sv) 2003-09-24 2003-09-24 Astrazeneca Ab New compounds
SE0200979D0 (sv) * 2002-03-28 2002-03-28 Astrazeneca Ab New compounds
TW200918046A (en) 2002-04-03 2009-05-01 Novartis Ag Indolylmaleimide derivatives
AU2003238874A1 (en) 2002-06-05 2003-12-22 Janssen Pharmaceutica N.V. Bisindolyl-maleimid derivatives as kinase inhibitors
ES2312785T3 (es) 2002-06-05 2009-03-01 Janssen Pharmaceutica Nv Pirrolinas sustituidas utiles como inhibidores de quinasa.
GB0303319D0 (en) 2003-02-13 2003-03-19 Novartis Ag Organic compounds
US7250444B2 (en) * 2003-08-11 2007-07-31 Pfizer Inc. Pyrrole-based HMG-CoA reductase inhibitors
US7109436B2 (en) * 2003-08-29 2006-09-19 General Electric Company Laser shock peening target
AR045595A1 (es) * 2003-09-04 2005-11-02 Vertex Pharma Composiciones utiles como inhibidores de proteinas quinasas
EP1682103A1 (de) * 2003-10-27 2006-07-26 Novartis AG Indolyl-pyrroldion-derivate zur behandlung von neurologischen und vaskulären störungen im zusammenhang mit der beta-amyloid-erzeugung und/oder aggregation
CN1949967B (zh) * 2004-05-12 2012-02-01 拜尔作物科学有限公司 植物生长调节作用
WO2006061212A1 (en) 2004-12-08 2006-06-15 Johannes Gutenberg-Universität Mainz 3-(indolyl)-4-arylmaleimide derivatives and their use as angiogenesis inhibitors
JP4747364B2 (ja) * 2005-04-04 2011-08-17 独立行政法人産業技術総合研究所 紫外線皮膚炎抑止剤およびアトピー性皮膚炎抑止剤
WO2006117212A2 (en) 2005-05-04 2006-11-09 Develogen Aktiengesellschaft Use of gsk-3 inhibitors for preventing and treating pancreatic autoimmune disorders
EP2258358A3 (de) 2005-08-26 2011-09-07 Braincells, Inc. Neurogenese mit Acetylcholinesterasehemmer
CA2620333A1 (en) 2005-08-26 2007-03-01 Braincells, Inc. Neurogenesis by muscarinic receptor modulation
EP1940389A2 (de) 2005-10-21 2008-07-09 Braincells, Inc. Modulation von neurogenese durch pde-hemmung
CA2625210A1 (en) 2005-10-31 2007-05-10 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
AU2007249399A1 (en) 2006-05-09 2007-11-22 Braincells, Inc. Neurogenesis by modulating angiotensin
CA2673368C (en) 2006-12-19 2014-10-28 The Board Of Trustees Of The University Of Illinois 3-benzofuranyl-4-indolyl maleimides as potent gsk3 inhibitors for neurogenerative disorders
WO2008080824A1 (en) * 2006-12-29 2008-07-10 F. Hoffmann-La Roche Ag Aromatic sulfonated ketals
AU2009262241B2 (en) * 2008-06-25 2014-05-22 Forum Pharmaceuticals Inc. 1, 2 disubstituted heterocyclic compounds
US20100216805A1 (en) 2009-02-25 2010-08-26 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
EP2343291A1 (de) 2009-12-18 2011-07-13 Johannes Gutenberg-Universität Mainz 3-(Indolyl)- oder 3-(Azaindolyl)-4-Arylmaleimid-Verbindungen und ihre Verwendung bei der Behandlung von Tumoren
AU2011299811B2 (en) * 2010-09-08 2016-03-03 Sumitomo Chemical Company, Limited Method for producing pyridazinone compounds and intermediate thereof
EP2474541A1 (de) 2010-12-23 2012-07-11 Johannes- Gutenberg-Universität Mainz Konjugierte 3-(Indolyl)- und 3-(Azaindolyl)-4-arylmaleinimid-Verbindungen und deren Verwendung bei der Behandlung von Tumoren
KR20130034672A (ko) * 2011-09-28 2013-04-08 김동식 보텍스타입 열교환기
KR101440724B1 (ko) * 2013-03-29 2014-09-18 중앙대학교 산학협력단 글리코겐 신타아제 키나아제-3베타 억제물질을 유효성분으로 포함하는 난소과립세포종양의 예방 또는 치료용 약학적 조성물 및 건강기능성식품 조성물
CA2945263A1 (en) 2014-04-09 2015-10-15 Christopher Rudd Use of gsk-3 inhibitors or activators which modulate pd-1 or t-bet expression to modulate t cell immunity
TWI744723B (zh) 2014-06-20 2021-11-01 美商基利科學股份有限公司 多環型胺甲醯基吡啶酮化合物之合成
EP3187495A1 (de) 2015-12-30 2017-07-05 Johannes Gutenberg-Universität Mainz 3-(5-fluorindolyl)-4-arylmaleimid-verbindungen und deren verwendung bei der tumorbehandlung
WO2018132636A1 (en) * 2017-01-12 2018-07-19 The Research Foundation For The State University Of New York [18f]maleimide-based glycogen synthase kinase-3beta ligands for positron emission tomography imaging and radiosynthesis method
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GB9828640D0 (en) * 1998-12-23 1999-02-17 Smithkline Beecham Plc Novel method and compounds

Also Published As

Publication number Publication date
PE20020338A1 (es) 2002-04-23
WO2002010158A3 (en) 2002-05-16
WO2002010158A2 (en) 2002-02-07
US20020188018A1 (en) 2002-12-12
YU4403A (sh) 2006-05-25
IL153851A0 (en) 2003-07-31
DE60107857T2 (de) 2005-12-08
UY26857A1 (es) 2002-01-31
AU2001293702A1 (en) 2002-02-13
US20020052397A1 (en) 2002-05-02
KR20030017655A (ko) 2003-03-03
NZ523462A (en) 2004-09-24
RU2003104796A (ru) 2004-08-20
HUP0301431A2 (hu) 2003-08-28
ECSP034452A (es) 2003-03-10
NO20030328D0 (no) 2003-01-22
ZA200300216B (en) 2004-04-08
US6479490B2 (en) 2002-11-12
JP2004505078A (ja) 2004-02-19
EP1307447A2 (de) 2003-05-07
ES2233691T3 (es) 2005-06-16
GT200100151A (es) 2002-05-23
BR0112965A (pt) 2003-07-08
MA26936A1 (fr) 2004-12-20
MXPA03000695A (es) 2003-06-04
CZ2003555A3 (en) 2004-03-17
CA2417277A1 (en) 2002-02-07
EP1307447B1 (de) 2004-12-15
PL366701A1 (en) 2005-02-07
CN1444581A (zh) 2003-09-24
NO20030328L (no) 2003-01-22
PA8523001A1 (es) 2002-10-24
JO2293B1 (en) 2005-09-12
ATE284885T1 (de) 2005-01-15
CN1185229C (zh) 2005-01-19
AR033989A1 (es) 2004-01-21
HK1058670A1 (en) 2004-05-28
JP3984157B2 (ja) 2007-10-03
HRP20030030A2 (en) 2005-02-28

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