CA2417277A1 - 3-indolyl-4-phenyl-1h-pyrrole-2,5-dione derivatives as inhibitors of glycogen synthase kinase-3.beta. - Google Patents

3-indolyl-4-phenyl-1h-pyrrole-2,5-dione derivatives as inhibitors of glycogen synthase kinase-3.beta. Download PDF

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Publication number
CA2417277A1
CA2417277A1 CA002417277A CA2417277A CA2417277A1 CA 2417277 A1 CA2417277 A1 CA 2417277A1 CA 002417277 A CA002417277 A CA 002417277A CA 2417277 A CA2417277 A CA 2417277A CA 2417277 A1 CA2417277 A1 CA 2417277A1
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Prior art keywords
heteroalkyl
compound
hydrogen
dione
alkyl
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Abandoned
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CA002417277A
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English (en)
French (fr)
Inventor
Leyi Gong
Andrew Grupe
Gary Allen Peltz
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F Hoffmann La Roche AG
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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
    • 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
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    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
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    • 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
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    • 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)
  • 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)
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  • General Health & Medical Sciences (AREA)
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  • Diabetes (AREA)
  • Biomedical Technology (AREA)
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  • Neurology (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Otolaryngology (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CA002417277A 2000-07-27 2001-07-18 3-indolyl-4-phenyl-1h-pyrrole-2,5-dione derivatives as inhibitors of glycogen synthase kinase-3.beta. Abandoned CA2417277A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US22105800P 2000-07-27 2000-07-27
US60/221,058 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
CA2417277A1 true CA2417277A1 (en) 2002-02-07

Family

ID=22826151

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CA002417277A Abandoned CA2417277A1 (en) 2000-07-27 2001-07-18 3-indolyl-4-phenyl-1h-pyrrole-2,5-dione derivatives as inhibitors of glycogen synthase kinase-3.beta.

Country Status (31)

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

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JP2005532982A (ja) * 2001-09-24 2005-11-04 バイエル・フアーマシユーチカルズ・コーポレーシヨン 肥満の処置のためのピロール誘導体の製造及び使用
EP1465610B1 (en) * 2002-01-10 2008-12-31 F. Hoffmann-La Roche Ag Use of a gsk-3beta inhibitor in the manufacture of a medicament for increasing bone formation
KR100974770B1 (ko) 2002-03-05 2010-08-06 일라이 릴리 앤드 캄파니 키나제 억제제로서의 퓨린 유도체
MXPA04008671A (es) 2002-03-08 2004-12-06 Lilly Co Eli Derivados de pirrol-2,5-diona y su uso como inhibidores de gsk-3.
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
RU2004135382A (ru) 2002-06-05 2005-06-27 Янссен Фармацевтика Н.В. (Be) Замещенные пирролины в качестве ингибиторов киназы
CA2488798A1 (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
TWI339206B (en) 2003-09-04 2011-03-21 Vertex Pharma Compositions useful as inhibitors of protein kinases
EP1682103A1 (en) * 2003-10-27 2006-07-26 Novartis AG Indolyl-pyrroledione derivatives for the treatment of neurological and vascular disorders related to beta-amyloid generation and/or aggregation
WO2005107465A1 (en) * 2004-05-12 2005-11-17 Bayer Cropscience Gmbh Plant growth regulation
CA2589127C (en) 2004-12-08 2013-02-05 Johannes Gutenberg-Universitat 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
EP2258357A3 (en) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenesis with acetylcholinesterase inhibitor
CA2620333A1 (en) 2005-08-26 2007-03-01 Braincells, Inc. Neurogenesis by muscarinic receptor modulation
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
US20070112017A1 (en) 2005-10-31 2007-05-17 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
EP2382975A3 (en) 2006-05-09 2012-02-29 Braincells, Inc. Neurogenesis by modulating angiotensin
EP2125683B1 (en) 2006-12-19 2013-10-23 The Board of Trustees of the University of Illinois 3-benzofuranyl-4-indolyl-maleimides as potent gsk-3 inhibitors for neurodegenerative disorders
WO2008080824A1 (en) * 2006-12-29 2008-07-10 F. Hoffmann-La Roche Ag Aromatic sulfonated ketals
WO2009158393A1 (en) * 2008-06-25 2009-12-30 Envivo Pharmaceuticals, Inc. 1, 2 disubstituted heterocyclic compounds
WO2010099217A1 (en) 2009-02-25 2010-09-02 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
EP2343291A1 (en) 2009-12-18 2011-07-13 Johannes Gutenberg-Universität Mainz 3-(Indolyl)- or 3-(Azaindolyl)-4-arylmaleimide compounds and their use in tumor treatment
EP3045450B1 (en) * 2010-09-08 2018-02-07 Sumitomo Chemical Co., Ltd. Intermediate compounds in processes for producing pyridazinone compounds
EP2474541A1 (en) 2010-12-23 2012-07-11 Johannes- Gutenberg-Universität Mainz Conjugated 3-(indolyl)- and 3-(azaindolyl)-4-arylmaleimide compounds and their use in tumor treatment
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
WO2015155738A2 (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 (en) 2015-12-30 2017-07-05 Johannes Gutenberg-Universität Mainz 3-(5-fluoroindolyl)-4-arylmaleimide compounds and their use in tumor treatment
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
CN112538458B (zh) 2020-11-26 2025-10-31 北京孟眸生物科技有限公司 用于重编程细胞的方法

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Publication number Publication date
DE60107857D1 (de) 2005-01-20
ZA200300216B (en) 2004-04-08
JO2293B1 (en) 2005-09-12
AU2001293702A1 (en) 2002-02-13
NZ523462A (en) 2004-09-24
RU2003104796A (ru) 2004-08-20
WO2002010158A3 (en) 2002-05-16
PA8523001A1 (es) 2002-10-24
YU4403A (sh) 2006-05-25
ATE284885T1 (de) 2005-01-15
HRP20030030A2 (en) 2005-02-28
US6479490B2 (en) 2002-11-12
NO20030328D0 (no) 2003-01-22
IL153851A0 (en) 2003-07-31
CN1185229C (zh) 2005-01-19
ECSP034452A (es) 2003-03-10
AR033989A1 (es) 2004-01-21
HK1058670A1 (en) 2004-05-28
EP1307447A2 (en) 2003-05-07
HUP0301431A2 (hu) 2003-08-28
KR20030017655A (ko) 2003-03-03
US20020052397A1 (en) 2002-05-02
GT200100151A (es) 2002-05-23
WO2002010158A2 (en) 2002-02-07
NO20030328L (no) 2003-01-22
MA26936A1 (fr) 2004-12-20
EP1307447B1 (en) 2004-12-15
US20020188018A1 (en) 2002-12-12
JP3984157B2 (ja) 2007-10-03
PE20020338A1 (es) 2002-04-23
BR0112965A (pt) 2003-07-08
ES2233691T3 (es) 2005-06-16
CZ2003555A3 (en) 2004-03-17
DE60107857T2 (de) 2005-12-08
CN1444581A (zh) 2003-09-24
JP2004505078A (ja) 2004-02-19
PL366701A1 (en) 2005-02-07
UY26857A1 (es) 2002-01-31
MXPA03000695A (es) 2003-06-04

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