ATE284885T1 - 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
ATE284885T1
ATE284885T1 AT01974083T AT01974083T ATE284885T1 AT E284885 T1 ATE284885 T1 AT E284885T1 AT 01974083 T AT01974083 T AT 01974083T AT 01974083 T AT01974083 T AT 01974083T AT E284885 T1 ATE284885 T1 AT E284885T1
Authority
AT
Austria
Prior art keywords
pyrrol
indolyl
phenyl
glycogen synthase
synthase kinase
Prior art date
Application number
AT01974083T
Other languages
English (en)
Inventor
Leyi Gong
Andrew Grupe
Gary Allen Peltz
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Application granted granted Critical
Publication of ATE284885T1 publication Critical patent/ATE284885T1/de

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    • 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
    • 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
    • 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • C07D403/14Heterocyclic 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)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (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)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Immunology (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Dermatology (AREA)
  • Reproductive Health (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
AT01974083T 2000-07-27 2001-07-18 3-indolyl-4-phenyl-1h-pyrrol-2,5-dion derivate als glycogen synthase kinase 3beta inhibitoren ATE284885T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US22105800P 2000-07-27 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 (1)

Publication Number Publication Date
ATE284885T1 true ATE284885T1 (de) 2005-01-15

Family

ID=22826151

Family Applications (1)

Application Number Title Priority Date Filing Date
AT01974083T ATE284885T1 (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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KR100916613B1 (ko) * 2000-11-07 2009-09-14 노파르티스 아게 단백질 키나제 c 억제제로서의 인돌릴말레이미드 유도체
US6645970B2 (en) * 2000-11-07 2003-11-11 Novartis Ag Indolylmaleimide derivatives
WO2003027069A1 (en) * 2001-09-24 2003-04-03 Bayer Pharmaceuticals Corporation Preparation and use of pyrrole derivatives for treating obesity
AU2003235798A1 (en) * 2002-01-10 2003-07-24 F. Hoffmann-La Roche Ag Use of a gsk-3beta inhibitor in the manufacture of a medicament for increasing bone formation
AU2003215325B8 (en) 2002-03-05 2008-10-09 Eli Lilly And Company Purine derivatives as kinase inhibitors
DE60315270T2 (de) 2002-03-08 2008-04-17 Eli Lilly And Co., Indianapolis Pyrrol-2,5-dion derivate und deren verwendung als gsk-3 inhibitoren
SE0302546D0 (sv) 2003-09-24 2003-09-24 Astrazeneca Ab New compounds
SE0200979D0 (sv) 2002-03-28 2002-03-28 Astrazeneca Ab New compounds
AR039209A1 (es) * 2002-04-03 2005-02-09 Novartis Ag Derivados de indolilmaleimida
CA2488602A1 (en) 2002-06-05 2003-12-18 Janssen Pharmaceutica N.V. Substituted pyrrolines as kinase inhibitors
WO2003103663A2 (en) 2002-06-05 2003-12-18 Janssen Pharmaceutica N.V. Substituted pyrrolines as kinase inhibitors
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
JP2007509185A (ja) * 2003-10-27 2007-04-12 ノバルティス アクチエンゲゼルシャフト βアミロイド産生および/または凝集と関係がある神経障害および血管障害の処置のためのインドリル−ピロールジオン誘導体
US20100152044A1 (en) * 2004-05-12 2010-06-17 Bayer Cropscience Gmbh Plant growth regulation
JP5289769B2 (ja) 2004-12-08 2013-09-11 ヨハネス、グーテンベルク−ウニフェルジテート、マインツ 3−(インドリル)−4−アリールマレイミド誘導体および脈管形成阻害剤としてのそれらの使用
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
US20080207594A1 (en) 2005-05-04 2008-08-28 Davelogen Aktiengesellschaft Use of Gsk-3 Inhibitors for Preventing and Treating Pancreatic Autoimmune Disorders
EP2275095A3 (de) 2005-08-26 2011-08-17 Braincells, Inc. Neurogenese durch modulation des Muscarinrezeptors
EP2258358A3 (de) 2005-08-26 2011-09-07 Braincells, Inc. Neurogenese mit Acetylcholinesterasehemmer
JP2009512711A (ja) 2005-10-21 2009-03-26 ブレインセルス,インコーポレイティド Pde阻害による神経新生の調節
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
WO2007134136A2 (en) 2006-05-09 2007-11-22 Braincells, Inc. Neurogenesis by modulating angiotensin
WO2008077138A1 (en) 2006-12-19 2008-06-26 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
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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
AR082912A1 (es) * 2010-09-08 2013-01-16 Sumitomo Chemical Co Metodo para producir compuestos de piridazinona y un intermediario de sintesis
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
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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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Also Published As

Publication number Publication date
HUP0301431A2 (hu) 2003-08-28
CA2417277A1 (en) 2002-02-07
IL153851A0 (en) 2003-07-31
JP3984157B2 (ja) 2007-10-03
CZ2003555A3 (en) 2004-03-17
US20020052397A1 (en) 2002-05-02
BR0112965A (pt) 2003-07-08
PE20020338A1 (es) 2002-04-23
ECSP034452A (es) 2003-03-10
GT200100151A (es) 2002-05-23
JO2293B1 (en) 2005-09-12
EP1307447A2 (de) 2003-05-07
KR20030017655A (ko) 2003-03-03
ES2233691T3 (es) 2005-06-16
CN1185229C (zh) 2005-01-19
PL366701A1 (en) 2005-02-07
EP1307447B1 (de) 2004-12-15
DE60107857T2 (de) 2005-12-08
AR033989A1 (es) 2004-01-21
UY26857A1 (es) 2002-01-31
DE60107857D1 (de) 2005-01-20
JP2004505078A (ja) 2004-02-19
YU4403A (sh) 2006-05-25
HRP20030030A2 (en) 2005-02-28
HK1058670A1 (en) 2004-05-28
AU2001293702A1 (en) 2002-02-13
NO20030328D0 (no) 2003-01-22
US6479490B2 (en) 2002-11-12
ZA200300216B (en) 2004-04-08
NO20030328L (no) 2003-01-22
MXPA03000695A (es) 2003-06-04
PA8523001A1 (es) 2002-10-24
MA26936A1 (fr) 2004-12-20
CN1444581A (zh) 2003-09-24
WO2002010158A2 (en) 2002-02-07
WO2002010158A3 (en) 2002-05-16
NZ523462A (en) 2004-09-24
RU2003104796A (ru) 2004-08-20
US20020188018A1 (en) 2002-12-12

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