WO1995018616B1 - 8-aza, 6-aza et 6,8-diaza-1,4-dihydroquinoxaline-2,3-diones et leur utilisation comme antagonistes du recepteur de la glycine ou du nmda - Google Patents
8-aza, 6-aza et 6,8-diaza-1,4-dihydroquinoxaline-2,3-diones et leur utilisation comme antagonistes du recepteur de la glycine ou du nmdaInfo
- Publication number
- WO1995018616B1 WO1995018616B1 PCT/US1995/000214 US9500214W WO9518616B1 WO 1995018616 B1 WO1995018616 B1 WO 1995018616B1 US 9500214 W US9500214 W US 9500214W WO 9518616 B1 WO9518616 B1 WO 9518616B1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- hydrogen
- aryl
- alkyl
- alkoxy
- amino
- Prior art date
Links
- 230000003042 antagnostic Effects 0.000 title claims 3
- HNSVDKLARSSFGE-UHFFFAOYSA-N 5,8-dihydropteridine-6,7-dione Chemical class N1=CN=C2NC(=O)C(=O)NC2=C1 HNSVDKLARSSFGE-UHFFFAOYSA-N 0.000 title abstract 2
- 102000011714 Glycine Receptors Human genes 0.000 title abstract 2
- 108010076533 Glycine Receptors Proteins 0.000 title abstract 2
- 102000004868 N-methyl-D-aspartate receptors Human genes 0.000 title 1
- 108090001041 N-methyl-D-aspartate receptors Proteins 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- 150000003839 salts Chemical class 0.000 claims abstract 16
- 239000011780 sodium chloride Substances 0.000 claims abstract 16
- 230000002265 prevention Effects 0.000 claims abstract 10
- 206010002091 Anaesthesia Diseases 0.000 claims abstract 5
- 230000037005 anaesthesia Effects 0.000 claims abstract 5
- 206010001897 Alzheimer's disease Diseases 0.000 claims abstract 3
- 206010002026 Amyotrophic lateral sclerosis Diseases 0.000 claims abstract 3
- 206010002855 Anxiety Diseases 0.000 claims abstract 3
- 206010057666 Anxiety disease Diseases 0.000 claims abstract 3
- 208000000094 Chronic Pain Diseases 0.000 claims abstract 3
- 206010010904 Convulsion Diseases 0.000 claims abstract 3
- 201000010374 Down syndrome Diseases 0.000 claims abstract 3
- 201000001971 Huntington's disease Diseases 0.000 claims abstract 3
- 206010020993 Hypoglycaemia Diseases 0.000 claims abstract 3
- 206010022114 Injury Diseases 0.000 claims abstract 3
- 206010061255 Ischaemia Diseases 0.000 claims abstract 3
- 206010053643 Neurodegenerative disease Diseases 0.000 claims abstract 3
- 208000002193 Pain Diseases 0.000 claims abstract 3
- 206010044688 Trisomy 21 Diseases 0.000 claims abstract 3
- 230000002411 adverse Effects 0.000 claims abstract 3
- 230000036506 anxiety Effects 0.000 claims abstract 3
- 230000036461 convulsion Effects 0.000 claims abstract 3
- 239000003257 excitatory amino acid Substances 0.000 claims abstract 3
- 230000002461 excitatory amino acid Effects 0.000 claims abstract 3
- 230000002218 hypoglycaemic Effects 0.000 claims abstract 3
- 230000001939 inductive effect Effects 0.000 claims abstract 3
- 230000001537 neural Effects 0.000 claims abstract 3
- 238000001356 surgical procedure Methods 0.000 claims abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 329
- 239000001257 hydrogen Substances 0.000 claims 329
- 150000002431 hydrogen Chemical group 0.000 claims 152
- 125000004435 hydrogen atoms Chemical group [H]* 0.000 claims 120
- 125000000217 alkyl group Chemical group 0.000 claims 108
- 125000003118 aryl group Chemical group 0.000 claims 73
- -1 nitro, amino Chemical group 0.000 claims 66
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 57
- 125000003545 alkoxy group Chemical group 0.000 claims 53
- 125000004104 aryloxy group Chemical group 0.000 claims 52
- 125000001153 fluoro group Chemical group F* 0.000 claims 52
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 45
- 125000004432 carbon atoms Chemical group C* 0.000 claims 44
- 150000001875 compounds Chemical class 0.000 claims 27
- 125000004438 haloalkoxy group Chemical group 0.000 claims 26
- 125000005553 heteroaryloxy group Chemical group 0.000 claims 26
- 125000005843 halogen group Chemical group 0.000 claims 25
- 125000001188 haloalkyl group Chemical group 0.000 claims 24
- 125000003342 alkenyl group Chemical group 0.000 claims 23
- 125000000304 alkynyl group Chemical group 0.000 claims 23
- 125000000852 azido group Chemical group *N=[N+]=[N-] 0.000 claims 23
- 125000004093 cyano group Chemical group *C#N 0.000 claims 23
- 125000000753 cycloalkyl group Chemical group 0.000 claims 23
- 125000001072 heteroaryl group Chemical group 0.000 claims 23
- 125000004442 acylamino group Chemical group 0.000 claims 22
- 125000003710 aryl alkyl group Chemical group 0.000 claims 22
- 125000003107 substituted aryl group Chemical group 0.000 claims 14
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 7
- 206010061920 Psychotic disease Diseases 0.000 claims 2
- HOKKHZGPKSLGJE-GSVOUGTGSA-N NMDA Chemical compound CN[C@@H](C(O)=O)CC(O)=O HOKKHZGPKSLGJE-GSVOUGTGSA-N 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 1
- 230000000926 neurological Effects 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 206010037211 Psychomotor hyperactivity Diseases 0.000 abstract 1
Abstract
La présente invention concerne des procédés de traitement ou de prévention des pertes neuronales associées à l'ictus, à l'ischémie, au traumatisme du système nerveux central, à l'hypoglycémie et à la chirurgie. L'invention concerne également, d'une part le traitement des affections neurodégénératives, notamment la maladie d'Alzheimer, la sclérose amyotrophique latérale, la chorée de Huntington, le syndrome de Down, et d'autre part le traitement ou la prévention des conséquences néfastes de l'hyperactivité des acides aminés excitateurs. L'invention concerne en outre le traitement de l'anxiété, des douleurs chroniques, des convulsions, l'induction de l'anesthésie et le traitement ou la prévention de la tolérance aux opiacés. Le procédé consiste à administrer, à l'animal nécessitant un tel traitement ou une telle prévention, un 8-aza, 6-aza ou 6,8-diaza-1,4-dihydroquinoxaline-2,3-dione substitué ou non substitué, ou l'un de ses sels et N-oxydes pharmaceutiquement acceptables, cette substance présentant une fixation élevée au récepteur de la glycine.
Priority Applications (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AU15993/95A AU1599395A (en) | 1994-01-03 | 1995-01-03 | 8-aza, 6-aza and 6,8-diaza-1,4-dihydroquinoxaline-2,3-diones and the use thereof as antagonists for the glycine/nmda receptor |
| JP7518626A JPH09510695A (ja) | 1994-01-03 | 1995-01-03 | ８−アザ、６−アザ、および６，８−ジアザ−１，４−ジヒドロキノキサリン−２，３−ジオン類およびそのグリシン／ｎｍｄａリセプターに対するアンタゴニストとしての使用 |
| EP95907997A EP0743855A1 (fr) | 1994-01-03 | 1995-01-03 | 8-aza, 6-aza et 6,8-diaza-1,4-dihydroquinoxaline-2,3-diones et leur utilisation comme antagonistes du recepteur de la glycine ou du nmda |
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US17627894A | 1994-01-03 | 1994-01-03 | |
| US08/176,278 | 1994-01-03 | ||
| US28936694A | 1994-08-11 | 1994-08-11 | |
| US08/289,366 | 1994-08-11 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| WO1995018616A2 WO1995018616A2 (fr) | 1995-07-13 |
| WO1995018616A3 WO1995018616A3 (fr) | 1995-12-21 |
| WO1995018616B1 true WO1995018616B1 (fr) | 1996-02-29 |
Family
ID=26872063
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/US1995/000214 WO1995018616A2 (fr) | 1994-01-03 | 1995-01-03 | 8-aza, 6-aza et 6,8-diaza-1,4-dihydroquinoxaline-2,3-diones et leur utilisation comme antagonistes du recepteur de la glycine ou du nmda |
Country Status (7)
| Country | Link |
|---|---|
| US (2) | US5620978A (fr) |
| EP (1) | EP0743855A1 (fr) |
| JP (2) | JPH09510695A (fr) |
| AU (1) | AU1599395A (fr) |
| CA (1) | CA2180122A1 (fr) |
| IL (1) | IL112235A (fr) |
| WO (1) | WO1995018616A2 (fr) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AUPN842196A0 (en) * | 1996-03-05 | 1996-03-28 | Fujisawa Pharmaceutical Co., Ltd. | New compound |
| US6455554B1 (en) | 1999-06-07 | 2002-09-24 | Targacept, Inc. | Oxopyridinyl pharmaceutical compositions and methods for use |
| SK11952003A3 (sk) | 2001-03-26 | 2004-03-02 | Novartis Ag | Deriváty pyridínu, spôsoby ich prípravy, farmaceutická kompozícia, ktorá ich obsahuje, a ich použitie |
| SE0101387D0 (sv) * | 2001-04-20 | 2001-04-20 | Astrazeneca Ab | Novel compounds |
| US6638981B2 (en) * | 2001-08-17 | 2003-10-28 | Epicept Corporation | Topical compositions and methods for treating pain |
| GB0412769D0 (en) | 2004-06-08 | 2004-07-07 | Novartis Ag | Organic compounds |
| KR20070033032A (ko) | 2004-07-16 | 2007-03-23 | 프로테오시스 악티엔게젤샤프트 | 세포보호제로서 ｐａｒｐ 및 ｓｉｒ 조절 활성을 갖는무스카린 길항제 |
| WO2009000038A1 (fr) * | 2007-06-28 | 2008-12-31 | Cnsbio Pty Ltd | Procédés et compositions de combinaison pour le traitement d'une douleur neuropathique |
| CA2716080C (fr) | 2008-02-20 | 2016-12-13 | Targia Pharmaceuticals | Compositions pharmaceutiques actives sur le snc et methodes d'utilisation |
| KR101687841B1 (ko) | 2008-12-09 | 2016-12-19 | 길리애드 사이언시즈, 인코포레이티드 | 톨-유사 수용체의 조절제 |
| EP2387405A2 (fr) | 2009-01-13 | 2011-11-23 | ProteoSys AG | Pirenzépine en tant qu'agent utilisé dans le traitement du cancer |
| PL2477987T3 (pl) * | 2009-09-14 | 2018-06-29 | Gilead Sciences, Inc. | Modulatory receptorów toll-podobnych |
| EP2935215B1 (fr) * | 2012-12-20 | 2019-11-13 | Lu, Qing-Bin | Composés radiosensibilisateurs destinés à être utilisés en association avec des rayonnements |
| CN103435561B (zh) * | 2013-08-19 | 2016-08-10 | 上海交通大学 | 一种新型d-氨基酸氧化酶抑制剂及其制备和应用 |
| US10463662B2 (en) * | 2013-10-08 | 2019-11-05 | Qing-Bin Lu | Non-platinum-based anti-cancer compounds for use in targeted chemotherapy |
| FR3015482B1 (fr) | 2013-12-20 | 2016-01-08 | Oreal | Composition tinctoriale comprenant un compose 1,2,3,4-tetrahydropyrido[2,3-b]pyrazin-7-amine |
| CA2954056C (fr) | 2014-07-11 | 2020-04-28 | Gilead Sciences, Inc. | Modulateurs de recepteurs de type toll pour le traitement du vih |
| ES2706527T3 (es) | 2014-09-16 | 2019-03-29 | Gilead Sciences Inc | Métodos para preparar moduladores de receptores tipo Toll |
| JP2017526730A (ja) | 2014-09-16 | 2017-09-14 | ギリアード サイエンシーズ， インコーポレイテッド | Ｔｏｌｌ様受容体モジュレーターの固体形態 |
| WO2016196012A1 (fr) | 2015-05-29 | 2016-12-08 | The Board Of Trustees Of The Leland Stanford Junior University | Agents nucléosidiques pour la réduction de l'activité délétère de gènes contenant une répétition de nucléotide étendue |
| CN116322696A (zh) | 2020-05-04 | 2023-06-23 | 安进公司 | 作为髓样细胞上表达的触发受体2激动剂的杂环化合物和使用方法 |
| TW202208355A (zh) | 2020-05-04 | 2022-03-01 | 美商安進公司 | 作為骨髓細胞觸發受體2促效劑之雜環化合物及使用方法 |
| EP4321515A1 (fr) * | 2021-04-09 | 2024-02-14 | Simcere Zaiming Pharmaceutical Co., Ltd. | Inhibiteur de la protéase spécifique de l'ubiquitine 1 (usp1) |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0008864A1 (fr) * | 1978-08-15 | 1980-03-19 | FISONS plc | Dérivés de la pyridopyrazine et de la quinoxaline, procédés pour leur préparation, et compositions pharmaceutiques les contenant |
| ZA794209B (en) * | 1978-08-15 | 1980-07-30 | Fisons Ltd | Pharmaceutically active heterocyclic compounds |
| EP0039920B1 (fr) * | 1980-05-09 | 1984-07-25 | Usv Pharmaceutical Corporation | Triazoloquinoxalin-1,4-diones |
| GB8513639D0 (en) * | 1985-05-30 | 1985-07-03 | Ici America Inc | Cinnoline compounds |
| DK155524C (da) * | 1987-03-18 | 1989-09-11 | Ferrosan As | Kondenserede imidazolderivater og farmaceutiske praeparater indeholdende disse |
| IT1204612B (it) * | 1987-05-14 | 1989-03-10 | Bioresearch Spa | Pteridine atte alla preparazione di composizioni farmaceutiche ad attivita' antiamnesica |
| DK160876C (da) * | 1987-12-08 | 1991-10-14 | Novo Nordisk As | Imidazoquinoxalinforbindelser, fremgangsmaade til deres fremstilling, anvendelse af forbindelserne og farmaceutiske praeparater, hvori forbindelserne indgaar |
| ES2058527T3 (es) * | 1988-06-16 | 1994-11-01 | Smith Kline French Lab | Derivados de pirimidina condensados procedimiento y compuestos intermedios para su preparacion y composiciones farmaceuticas que los contienen. |
| DK716188D0 (da) * | 1988-12-22 | 1988-12-22 | Ferrosan As | Quinoxalinforbindelser, deres fremstilling og anvendelse |
| GB8907865D0 (en) * | 1989-04-07 | 1989-05-24 | Wyeth John & Brother Ltd | Tetrahydroquinoline derivatives |
| US5055465A (en) * | 1989-05-31 | 1991-10-08 | Berlex Laboratories, Inc. | Imidazoquinoxalinones, their aza analogs and process for their preparation |
| DK69790D0 (da) * | 1990-03-16 | 1990-03-16 | Novo Nordisk As | Heterocykliske forbindelser, deres fremstilling af anvendelse |
| DK0556393T3 (da) * | 1990-11-06 | 2000-10-16 | Yamanouchi Pharma Co Ltd | Tilkondenseret pyrazinderivat |
| JPH04178385A (ja) * | 1990-11-09 | 1992-06-25 | Yamanouchi Pharmaceut Co Ltd | ジケトピリドピラジン誘導体 |
| EP0581805A1 (fr) * | 1991-04-26 | 1994-02-09 | Byk Gulden Lomberg Chemische Fabrik Gmbh | Nouvelles pyridazines |
| JPH05310732A (ja) * | 1992-03-12 | 1993-11-22 | Mitsubishi Kasei Corp | シンノリン−３−カルボン酸誘導体 |
| DE69334237D1 (de) * | 1992-06-22 | 2008-09-25 | State Of Oregon Through Oregon | Glycinrezeptorantagonisten und ihre verwendung |
| TW274550B (fr) * | 1992-09-26 | 1996-04-21 | Hoechst Ag |
-
1995
- 1995-01-03 JP JP7518626A patent/JPH09510695A/ja active Pending
- 1995-01-03 IL IL11223595A patent/IL112235A/xx not_active IP Right Cessation
- 1995-01-03 CA CA002180122A patent/CA2180122A1/fr not_active Abandoned
- 1995-01-03 US US08/368,163 patent/US5620978A/en not_active Expired - Lifetime
- 1995-01-03 AU AU15993/95A patent/AU1599395A/en not_active Abandoned
- 1995-01-03 WO PCT/US1995/000214 patent/WO1995018616A2/fr not_active Application Discontinuation
- 1995-01-03 EP EP95907997A patent/EP0743855A1/fr not_active Withdrawn
-
1997
- 1997-02-04 US US08/795,387 patent/US5863916A/en not_active Expired - Fee Related
-
2005
- 2005-04-19 JP JP2005121174A patent/JP2005247864A/ja not_active Withdrawn
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