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

Info

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
German (de)
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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    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P25/28—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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • 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
    • 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
    • C07D403/14—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 three or more hetero rings
    • 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

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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)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Immunology (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Vascular Medicine (AREA)
  • Dermatology (AREA)
  • Otolaryngology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (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 (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) NO20030328D0 (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
DE60325551D1 (de) * 2002-01-10 2009-02-12 Hoffmann La Roche Verwendung eines gsk-3beta-hemmers bei der herstellung eines arzneimittel zur erhöhung der knochenbildung
CN1312154C (zh) 2002-03-05 2007-04-25 伊莱利利公司 作为激酶抑制剂的嘌呤衍生物
IL163777A0 (en) * 2002-03-08 2005-12-18 Lilly Co Eli Kinase inhibitors
SE0200979D0 (sv) * 2002-03-28 2002-03-28 Astrazeneca Ab New compounds
SE0302546D0 (sv) 2003-09-24 2003-09-24 Astrazeneca Ab New compounds
PE20040079A1 (es) * 2002-04-03 2004-04-19 Novartis Ag Derivados de indolilmaleimida
JP2005531609A (ja) 2002-06-05 2005-10-20 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ キナーゼ阻害剤としてのシスインドリル−マレイミド誘導体
EP1513520B1 (en) * 2002-06-05 2008-09-24 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
WO2005039549A1 (en) * 2003-10-27 2005-05-06 Novartis Ag Indolyl-pyrroledione derivatives for the treatment of neurological and vascular disorders related to beta-amyloid generation and/or aggregation
EP1746886A1 (en) * 2004-05-12 2007-01-31 Bayer CropScience GmbH Plant growth regulation
AU2005313485B2 (en) 2004-12-08 2011-02-03 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
EP1885454A2 (en) 2005-05-04 2008-02-13 DeveloGen Aktiengesellschaft Use of gsk-3 inhibitors for preventing and treating pancreatic autoimmune disorders
EP2258359A3 (en) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenesis by muscarinic receptor modulation with sabcomelin
JP2009506069A (ja) 2005-08-26 2009-02-12 ブレインセルス，インコーポレイティド ムスカリン性受容体調節による神経発生
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
EP2314289A1 (en) 2005-10-31 2011-04-27 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
MX2011000175A (es) * 2008-06-25 2011-06-27 Envivo Pharmaceuticals Inc Compuestos heterociclicos 1,2-di-substituidos.
US20100216805A1 (en) 2009-02-25 2010-08-26 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
TWI507381B (zh) 2010-09-08 2015-11-11 Sumitomo Chemical Co 製造嗒酮化合物的方法及其中間物
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
US20170165230A1 (en) 2014-04-09 2017-06-15 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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Also Published As

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

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