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 PDFInfo
- 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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- Canada
- Prior art keywords
- heteroalkyl
- compound
- hydrogen
- dione
- alkyl
- 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.)
- Abandoned
Links
- 108010014905 Glycogen Synthase Kinase 3 Proteins 0.000 title claims abstract description 61
- 239000003112 inhibitor Substances 0.000 title claims abstract description 22
- LKDTVSJUXXGXKE-UHFFFAOYSA-N 3-(1h-indol-2-yl)-4-phenylpyrrole-2,5-dione Chemical class C=1C2=CC=CC=C2NC=1C=1C(=O)NC(=O)C=1C1=CC=CC=C1 LKDTVSJUXXGXKE-UHFFFAOYSA-N 0.000 title abstract description 7
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- 239000000203 mixture Substances 0.000 claims description 67
- 125000004404 heteroalkyl group Chemical group 0.000 claims description 65
- 125000000217 alkyl group Chemical group 0.000 claims description 63
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- 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
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- 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
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Landscapes
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| 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 |
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| CA2417277A1 true CA2417277A1 (en) | 2002-02-07 |
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| BR0114411A (pt) * | 2000-10-02 | 2006-05-09 | Reddy Us Therapeutics Inc | métodos e composições para o tratamento de doenças inflamatórias |
| CA2428133C (en) * | 2000-11-07 | 2009-12-29 | Novartis Ag | Indolylmaleimide derivatives as protein kinase c inhibitors |
| US6645970B2 (en) | 2000-11-07 | 2003-11-11 | Novartis Ag | Indolylmaleimide derivatives |
| 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 |
| 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 |
| 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 |
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| PE20040079A1 (es) * | 2002-04-03 | 2004-04-19 | Novartis Ag | Derivados de indolilmaleimida |
| US6987110B2 (en) | 2002-06-05 | 2006-01-17 | Janssen Pharmaceutica N.V. | Substituted pyrrolines as kinase inhibitors |
| JP2005531607A (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置換ピロリン |
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| 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 |
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| CA2566392A1 (en) * | 2004-05-12 | 2005-11-17 | Bayer Cropscience Gmbh | Plant growth regulation |
| EP1819697B1 (en) | 2004-12-08 | 2012-08-01 | 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 |
| US20080207594A1 (en) | 2005-05-04 | 2008-08-28 | Davelogen Aktiengesellschaft | Use of Gsk-3 Inhibitors for Preventing and Treating Pancreatic Autoimmune Disorders |
| US7678363B2 (en) | 2005-08-26 | 2010-03-16 | Braincells Inc | Methods of treating psychiatric conditions comprising administration of muscarinic agents in combination with SSRIs |
| EP2258359A3 (en) | 2005-08-26 | 2011-04-06 | Braincells, Inc. | Neurogenesis by muscarinic receptor modulation with sabcomelin |
| WO2007047978A2 (en) | 2005-10-21 | 2007-04-26 | Braincells, Inc. | Modulation of neurogenesis by pde inhibition |
| AU2006308889A1 (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 |
| CA2651813A1 (en) | 2006-05-09 | 2007-11-22 | Braincells, Inc. | Neurogenesis by modulating angiotensin |
| ES2446269T3 (es) | 2006-12-19 | 2014-03-06 | The Board Of Trustees Of The University Of Illinois | 3-Benzofuranil-4-indolil-maleimidas como potentes inhibidores de GSK-3 para trastornos neurodegenerativos |
| 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. |
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| 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 |
| JP5790348B2 (ja) | 2010-09-08 | 2015-10-07 | 住友化学株式会社 | ピリダジノン化合物の製造法およびその製造中間体 |
| 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 |
| TWI677489B (zh) | 2014-06-20 | 2019-11-21 | 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 |
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| 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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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ227850A (en) * | 1988-02-10 | 1991-11-26 | Hoffmann La Roche | Indole substituted pyrrole derivatives; preparatory process and medicaments for use against inflammatory immunological, bronchopulmonary or vascular disorders |
| MC2096A1 (fr) | 1989-02-23 | 1991-02-15 | Hoffmann La Roche | Pyrroles substitues |
| GB8904161D0 (en) | 1989-02-23 | 1989-04-05 | Hoffmann La Roche | Substituted pyrroles |
| GB9123396D0 (en) | 1991-11-04 | 1991-12-18 | Hoffmann La Roche | A process for the manufacture of substituted maleimides |
| CA2116460A1 (en) | 1993-03-02 | 1994-09-03 | Mitsubishi Chemical Corporation | Preventive or therapeutic agents for alzheimer's disease, a screening method of alzheimer's disease and tau-protein kinase i originated from human being |
| US5721230A (en) | 1993-05-10 | 1998-02-24 | Hoffmann-La Roche Inc. | Substituted pyrroles |
| AU678435B2 (en) | 1993-05-10 | 1997-05-29 | F. Hoffmann-La Roche Ag | Substituted pyrroles |
| AU1200497A (en) | 1995-12-20 | 1997-07-14 | Medical Research Council | Control of protein synthesis, and screening method for agents |
| WO1997041854A1 (en) | 1996-05-07 | 1997-11-13 | The Trustees Of The University Of Pennsylvania | Inhibitors of glycogen synthase kinase-3 and methods for identifying and using the same |
| SE9603285D0 (sv) | 1996-09-10 | 1996-09-10 | Astra Ab | New compounds |
| DE69922526T2 (de) * | 1998-10-08 | 2005-06-02 | Smithkline Beecham Plc, Brentford | 3-(3-chloro-4-hydroxyphenylamino)-4-(2-nitrophenyl)-1h-pyrrol-2,5-dion als glykogen synthase kinase-3 inhibitor (gsk-3) |
| GB9828640D0 (en) * | 1998-12-23 | 1999-02-17 | Smithkline Beecham Plc | Novel method and compounds |
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