JP2004505078A5 - - Google Patents
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- Publication number
- JP2004505078A5 JP2004505078A5 JP2002515887A JP2002515887A JP2004505078A5 JP 2004505078 A5 JP2004505078 A5 JP 2004505078A5 JP 2002515887 A JP2002515887 A JP 2002515887A JP 2002515887 A JP2002515887 A JP 2002515887A JP 2004505078 A5 JP2004505078 A5 JP 2004505078A5
- Authority
- JP
- Japan
- Prior art keywords
- heteroalkyl
- hydrogen
- compound according
- alkyl
- disease
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 27
- 229910052739 hydrogen Inorganic materials 0.000 claims 18
- 239000001257 hydrogen Substances 0.000 claims 18
- 125000000217 alkyl group Chemical group 0.000 claims 15
- 125000004404 heteroalkyl group Chemical group 0.000 claims 15
- -1 cyano, nitro, amino Chemical group 0.000 claims 13
- 201000010099 disease Diseases 0.000 claims 12
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 12
- 125000000623 heterocyclic group Chemical group 0.000 claims 11
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 11
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 10
- 208000006673 asthma Diseases 0.000 claims 10
- 150000002431 hydrogen Chemical class 0.000 claims 8
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims 7
- 102000019058 Glycogen Synthase Kinase 3 beta Human genes 0.000 claims 6
- 108010051975 Glycogen Synthase Kinase 3 beta Proteins 0.000 claims 6
- 239000003112 inhibitor Substances 0.000 claims 6
- 102000002254 Glycogen Synthase Kinase 3 Human genes 0.000 claims 5
- 108010014905 Glycogen Synthase Kinase 3 Proteins 0.000 claims 5
- 206010020751 Hypersensitivity Diseases 0.000 claims 5
- 125000002947 alkylene group Chemical group 0.000 claims 5
- 208000026935 allergic disease Diseases 0.000 claims 5
- 230000007815 allergy Effects 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 125000004442 acylamino group Chemical group 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 125000004414 alkyl thio group Chemical group 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 125000004663 dialkyl amino group Chemical group 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 125000001188 haloalkyl group Chemical group 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 125000004475 heteroaralkyl group Chemical group 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- 208000024827 Alzheimer disease Diseases 0.000 claims 3
- 206010003210 Arteriosclerosis Diseases 0.000 claims 3
- 201000001320 Atherosclerosis Diseases 0.000 claims 3
- 208000020925 Bipolar disease Diseases 0.000 claims 3
- 206010061598 Immunodeficiency Diseases 0.000 claims 3
- 208000029462 Immunodeficiency disease Diseases 0.000 claims 3
- 241000124008 Mammalia Species 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 208000008589 Obesity Diseases 0.000 claims 3
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 206010012601 diabetes mellitus Diseases 0.000 claims 3
- 230000007813 immunodeficiency Effects 0.000 claims 3
- 208000028867 ischemia Diseases 0.000 claims 3
- 230000001404 mediated effect Effects 0.000 claims 3
- 235000020824 obesity Nutrition 0.000 claims 3
- 201000010065 polycystic ovary syndrome Diseases 0.000 claims 3
- 208000011580 syndromic disease Diseases 0.000 claims 3
- 230000009529 traumatic brain injury Effects 0.000 claims 3
- QGZKDVFQNNGYKY-UHFFFAOYSA-N Ammonia Chemical compound N QGZKDVFQNNGYKY-UHFFFAOYSA-N 0.000 claims 2
- 206010039085 Rhinitis allergic Diseases 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- 201000010105 allergic rhinitis Diseases 0.000 claims 2
- 239000002585 base Substances 0.000 claims 2
- 238000006243 chemical reaction Methods 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical compound [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- MZUZXNZGBBUAIM-UHFFFAOYSA-N 3-(1h-indol-3-yl)-4-phenylfuran-2,5-dione Chemical compound C=1NC2=CC=CC=C2C=1C=1C(=O)OC(=O)C=1C1=CC=CC=C1 MZUZXNZGBBUAIM-UHFFFAOYSA-N 0.000 claims 1
- 102000004127 Cytokines Human genes 0.000 claims 1
- 108090000695 Cytokines Proteins 0.000 claims 1
- 229910021529 ammonia Inorganic materials 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 239000012458 free base Substances 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
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 (3)
| Publication Number | Publication Date |
|---|---|
| JP2004505078A JP2004505078A (ja) | 2004-02-19 |
| JP2004505078A5 true JP2004505078A5 (enExample) | 2005-03-03 |
| JP3984157B2 JP3984157B2 (ja) | 2007-10-03 |
Family
ID=22826151
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002515887A Expired - Lifetime JP3984157B2 (ja) | 2000-07-27 | 2001-07-18 | グリコーゲンシンターゼキナーゼ−３ベータのインヒビターとしての３−インドリル−４−フェニル−１ｈ−ピロール−２，５−ジオン誘導体 |
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) |
Families Citing this family (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001013916A1 (en) * | 1999-08-20 | 2001-03-01 | Sagami Chemical Research Center | Drugs inhibiting cell death |
| WO2002029091A2 (en) * | 2000-10-02 | 2002-04-11 | Reddy Us Therapeutics, Inc. | Methods and compositions for the treatment of inflammatory diseases |
| CN1253449C (zh) * | 2000-11-07 | 2006-04-26 | 诺瓦提斯公司 | 作为蛋白激酶c抑制剂的吲哚基马来酰亚胺衍生物 |
| US6645970B2 (en) | 2000-11-07 | 2003-11-11 | Novartis Ag | Indolylmaleimide derivatives |
| 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 |
| ES2276048T3 (es) | 2002-03-05 | 2007-06-16 | Eli Lilly And Company | Derivados de purina como inhibidores de cinasa. |
| ATE368657T1 (de) * | 2002-03-08 | 2007-08-15 | Lilly Co Eli | Pyrrol-2,5-dion derivate und deren verwendung als gsk-3 inhibitoren |
| SE0200979D0 (sv) * | 2002-03-28 | 2002-03-28 | Astrazeneca Ab | New compounds |
| SE0302546D0 (sv) | 2003-09-24 | 2003-09-24 | Astrazeneca Ab | New compounds |
| AR039209A1 (es) * | 2002-04-03 | 2005-02-09 | Novartis Ag | Derivados de indolilmaleimida |
| ES2312785T3 (es) | 2002-06-05 | 2009-03-01 | Janssen Pharmaceutica Nv | Pirrolinas sustituidas utiles como inhibidores de quinasa. |
| 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 |
| 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 |
| 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 |
| CA2566392A1 (en) * | 2004-05-12 | 2005-11-17 | 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 |
| EP2258357A3 (en) | 2005-08-26 | 2011-04-06 | Braincells, Inc. | Neurogenesis with acetylcholinesterase inhibitor |
| EP2275096A3 (en) | 2005-08-26 | 2011-07-13 | Braincells, Inc. | Neurogenesis via modulation of the muscarinic receptors |
| WO2007047978A2 (en) | 2005-10-21 | 2007-04-26 | Braincells, Inc. | Modulation of neurogenesis by pde inhibition |
| 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 |
| EP2021000A2 (en) | 2006-05-09 | 2009-02-11 | 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 |
| CN102131801B (zh) * | 2008-06-25 | 2015-04-08 | 福拉姆医药股份有限公司 | 1,2-二取代的杂环化合物 |
| 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 |
| CN103180300B (zh) * | 2010-09-08 | 2015-10-07 | 住友化学株式会社 | 制备哒嗪酮化合物的方法和其中间体 |
| 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 |
| 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 |
| CN120349967A (zh) | 2020-11-26 | 2025-07-22 | 北京孟眸生物科技有限公司 | 用于重编程细胞的方法 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CZ280738B6 (cs) * | 1988-02-10 | 1996-04-17 | F. Hoffmann - La Roche And Co., Aktiengesellschaft | Substituované pyrroly, jejich použití pro výrobu léčiv a léčiva na jejich bázi |
| 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 |
| AU678435B2 (en) | 1993-05-10 | 1997-05-29 | F. Hoffmann-La Roche Ag | Substituted pyrroles |
| US5721230A (en) | 1993-05-10 | 1998-02-24 | Hoffmann-La Roche Inc. | Substituted pyrroles |
| JP2000502097A (ja) | 1995-12-20 | 2000-02-22 | メディカル、リサーチ、カウンシル | タンパク質合成の制御、および作用薬のスクリーニング法 |
| EP1019043A4 (en) | 1996-05-07 | 2003-07-30 | Univ Pennsylvania | INHIBITORS OF GLYCOGEN SYNTHESIS KINASE 3 AND METHOD FOR THEIR IDENTIFICATION AND USE |
| SE9603285D0 (sv) | 1996-09-10 | 1996-09-10 | Astra Ab | New compounds |
| JP2002527419A (ja) * | 1998-10-08 | 2002-08-27 | スミスクライン・ビーチャム・パブリック・リミテッド・カンパニー | Ｇｓｋ−３阻害物質としてのピロール−２，５−ジオン類 |
| GB9828640D0 (en) * | 1998-12-23 | 1999-02-17 | Smithkline Beecham Plc | Novel method and compounds |
-
2001
- 2001-07-18 CA CA002417277A patent/CA2417277A1/en not_active Abandoned
- 2001-07-18 EP EP01974083A patent/EP1307447B1/en not_active Expired - Lifetime
- 2001-07-18 WO PCT/EP2001/008293 patent/WO2002010158A2/en not_active Ceased
- 2001-07-18 CN CNB018134068A patent/CN1185229C/zh not_active Expired - Fee Related
- 2001-07-18 IL IL15385101A patent/IL153851A0/xx unknown
- 2001-07-18 BR BR0112965-1A patent/BR0112965A/pt not_active IP Right Cessation
- 2001-07-18 ES ES01974083T patent/ES2233691T3/es not_active Expired - Lifetime
- 2001-07-18 NZ NZ523462A patent/NZ523462A/en unknown
- 2001-07-18 RU RU2003104796/04A patent/RU2003104796A/ru not_active Application Discontinuation
- 2001-07-18 YU YU4403A patent/YU4403A/sh unknown
- 2001-07-18 HU HU0301431A patent/HUP0301431A2/hu unknown
- 2001-07-18 PL PL01366701A patent/PL366701A1/xx not_active Application Discontinuation
- 2001-07-18 AT AT01974083T patent/ATE284885T1/de not_active IP Right Cessation
- 2001-07-18 MX MXPA03000695A patent/MXPA03000695A/es unknown
- 2001-07-18 JP JP2002515887A patent/JP3984157B2/ja not_active Expired - Lifetime
- 2001-07-18 CZ CZ2003555A patent/CZ2003555A3/cs unknown
- 2001-07-18 DE DE60107857T patent/DE60107857T2/de not_active Expired - Fee Related
- 2001-07-18 KR KR10-2003-7001111A patent/KR20030017655A/ko not_active Ceased
- 2001-07-18 HR HR20030030A patent/HRP20030030A2/hr not_active Application Discontinuation
- 2001-07-18 AU AU2001293702A patent/AU2001293702A1/en not_active Abandoned
- 2001-07-23 PE PE2001000742A patent/PE20020338A1/es not_active Application Discontinuation
- 2001-07-24 JO JO2001126A patent/JO2293B1/en active
- 2001-07-24 PA PA20018523001A patent/PA8523001A1/es unknown
- 2001-07-25 AR ARP010103541A patent/AR033989A1/es not_active Application Discontinuation
- 2001-07-26 UY UY26857A patent/UY26857A1/es not_active Application Discontinuation
- 2001-07-26 GT GT200100151A patent/GT200100151A/es unknown
- 2001-07-27 US US09/916,706 patent/US6479490B2/en not_active Expired - Fee Related
-
2002
- 2002-05-06 US US10/139,410 patent/US20020188018A1/en not_active Abandoned
-
2003
- 2003-01-08 ZA ZA200300216A patent/ZA200300216B/en unknown
- 2003-01-22 NO NO20030328A patent/NO20030328D0/no not_active Application Discontinuation
- 2003-01-24 MA MA27013A patent/MA26936A1/fr unknown
- 2003-01-24 EC EC2003004452A patent/ECSP034452A/es unknown
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