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1. 发明公开

EP0459561A3 Dioxo-tetrahydroquinoline derivatives 失效
标题翻译：二氧代四氢喹啉衍生物
公开(公告)号：EP0459561A3
公开(公告)日：1992-04-29
申请号：EP91201216.8
申请日：1991-05-22
申请人： MERCK SHARP & DOHME LTD.
发明人： Baker, Raymond , Stevenson, Graeme I. , Leeson, Paul D. , Rowley, Michael
IPC分类号： C07D409/06 , A61K31/47 , C07D409/04 , C07D401/04 , C07D215/22 , C07D405/04 , C07D401/12 , C07D409/12 , C07D413/04 , C07D404/04
CPC分类号： C07D215/22 , C07D215/56 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/06 , C07D409/04 , C07D409/06 , C07D409/12 , C07D413/04
摘要： A class of 2,4-dioxo-1,2,3,4-tetrahydroquinoline derivatives, substituted at the 3-position by a range of carbonyl-containing substituents or by a five- or six-membered heteroaromatic moiety, are selective non-competitive antagonists of NMDA receptors and/or are antagonists of AMPA receptors, and are therefore of utility in the treatment of conditions, such as neurodegenerative disorders, convulsions or schizophrenia, which require the administration of an NMDA and/or AMPA antagonist.

2. 发明公开

EP0318091A3 Resolved amino pyrrolidine neuroprotective agents 失效
标题翻译：解决的氨基吡咯烷神经保护剂
公开(公告)号：EP0318091A3
公开(公告)日：1989-08-30
申请号：EP88202602.4
申请日：1988-11-18
申请人： MERCK SHARP & DOHME LTD.
发明人： Leeson, Paul D. , Williams, Brian J.
IPC分类号： C07D207/46 , C07C259/00 , A61K31/40
CPC分类号： C07D207/46 , C07C323/47
摘要： The present invention provides R(+)-3-amino-1-hydroxypyrrolidin-2-one of formula I:
or a pharmaceutically acceptable acid addition salt thereof, which compound is useful as an anticonvulsant agent and in the treatment and/or prevention of neurodegenerative disorders.

3. 发明授权

EP0303512B1 Substituted dibenzocycloheptenimines 失效
标题翻译：取代二苯并咪唑啉酮
公开(公告)号：EP0303512B1
公开(公告)日：1992-09-30
申请号：EP88307515.2
申请日：1988-08-12
申请人： MERCK SHARP & DOHME LTD.
发明人： Baker, Raymond , Leeson, Paul D. , Britcher, Susan F.
IPC分类号： C07D451/00 , C07C239/00
CPC分类号： C07D451/00

4. 发明公开

EP0481676A1 Hydroxyquinolone derivatives 失效
标题翻译：羟基喹诺酮衍生物
公开(公告)号：EP0481676A1
公开(公告)日：1992-04-22
申请号：EP91309309.2
申请日：1991-10-10
申请人： MERCK SHARP & DOHME LTD.
发明人： Kulagowski, Janusz J. , Rowley, Michael , Leeson, Paul D. , Mawer, Ian Michael
IPC分类号： C07D215/22 , A61K31/47 , C07D405/04 , C07D409/10 , C07D405/10 , C07D401/10 , C07D401/12 , C07D409/12 , C07D405/12
CPC分类号： C07D215/22 , C07D401/12 , C07D403/10 , C07D405/04 , C07D405/10 , C07D405/12 , C07D409/10 , C07D409/12
摘要： A class of 4-hydroxy-2-(1 H)-quinolone derivatives, substituted at the 3-position by an optionally substituted aryl substituent, are selective non-competitive antagonists of NMDA receptors and/or are antagonists of AMPA receptors, and are therefore of utility in the treatment of conditions, such as neurodegenerative disorders, convulsions or schizophrenia, which require the administration of an NMDA and/or AMPA receptor antagonist.
摘要翻译：一类4-位羟基-2-（1H） - 喹诺酮衍生物，在3位被任选取代的芳基取代基取代，是NMDA受体的选择性非竞争性拮抗剂和/或是AMPA受体的拮抗剂，因此可用于治疗需要给予NMDA和/或AMPA受体拮抗剂的病症如神经变性疾病，惊厥或精神分裂症。

5. 发明公开

EP0319073A3 Cyclo-octane neuroprotective agents 失效
标题翻译： CYCLO-OCTANE神经保护剂
公开(公告)号：EP0319073A3
公开(公告)日：1990-12-19
申请号：EP88202618.0
申请日：1988-11-22
申请人： MERCK SHARP & DOHME LTD.
发明人： Baker, Raymond , Carling, William R. , James, Kim , Leeson, Paul D.
IPC分类号： C07D487/08 , A61K31/55
CPC分类号： C07D487/08
摘要： he present invention provides a compound of formula I:
or a salt thereof, wherein:
the dotted lines represent optional double bonds; R 1 represents hydrogen, hydroxy, alkenyl, alkyl, aminoalkyl or hydroxyalkyl; R 2 , R 3 , R 4 , R 5 and R 6 independently represent hydrogen, hydroxy, fluoro, alkenyl, aryl, alkyl, or alkyl substituted with aryl, amino, hydroxy, carboxy or fluoro; and R 7 , R 8 , R 9 and R 10 independently represent hydrogen, hydrocarbon or a heterocyclic group provided that R 7 , R 8 , R 9 and R 10 are not simultaneously hydrogen; or R 7 and R 8 and/or R 9 and R 10 may complete a saturated or unsaturated C 4 - 9 hydrocarbon or heterocyclic ring; which compounds are useful as anticonvulsant agents and in the treatment and/or prevention of neurodegenerative disorders.

6. 发明公开

EP0319073A2 Cyclo-octane neuroprotective agents 失效
标题翻译：环辛烷神经保护剂
公开(公告)号：EP0319073A2
公开(公告)日：1989-06-07
申请号：EP88202618.0
申请日：1988-11-22
申请人： MERCK SHARP & DOHME LTD.
发明人： Baker, Raymond , Carling, William R. , James, Kim , Leeson, Paul D.
IPC分类号： C07D487/08 , A61K31/55
CPC分类号： C07D487/08
摘要： he present invention provides a compound of formula I:
or a salt thereof, wherein:

the dotted lines represent optional double bonds;
R 1 represents hydrogen, hydroxy, alkenyl, alkyl, aminoalkyl or hydroxyalkyl;
R 2 , R 3 , R 4 , R 5 and R 6 independently represent hydrogen, hydroxy, fluoro, alkenyl, aryl, alkyl, or alkyl
substituted with aryl, amino, hydroxy, carboxy or fluoro; and
R 7 , R 8 , R 9 and R 10 independently represent hydrogen, hydrocarbon or a heterocyclic group provided that R 7 , R 8 , R 9 and R 10 are not simultaneously hydrogen; or
R 7 and R 8 and/or R 9 and R 10 may complete a saturated or unsaturated C 4 - 9 hydrocarbon or heterocyclic ring; which compounds are useful as anticonvulsant agents and in the treatment and/or prevention of neurodegenerative disorders.
摘要翻译：本发明提供了式I化合物或其盐：其中：虚线代表任选的双键; R1代表氢，羟基，链烯基，烷基，氨基烷基或羟烷基; R2，R3，R4，R5和R6独立地表示氢，羟基，氟，烯基，芳基，烷基或被芳基，氨基，羟基，羧基或氟取代的烷基; 且R7，R8，R9和R10独立地表示氢，烃或杂环基，条件是R7，R8，R9和R10不同时为氢; 或者R7和R8和/或R9和R10可以完成饱和或不饱和的C4-9烃或杂环; 这些化合物可用作抗惊厥剂并用于治疗和/或预防神经变性疾病。

7. 发明授权

EP0489458B1 Hydroxyquinolone derivatives 失效
标题翻译：羟基喹诺酮衍生物
公开(公告)号：EP0489458B1
公开(公告)日：1995-06-07
申请号：EP91203099.6
申请日：1991-11-27
申请人： MERCK SHARP & DOHME LTD.
发明人： Carling, William R. , Leeson, Paul D. , Moore, Kevin W.
IPC分类号： C07D401/04 , A61K31/47
CPC分类号： C07D401/04

8. 发明公开

EP0489458A1 Hydroxyquinolone derivatives 失效
标题翻译：羟基喹诺酮衍生物
公开(公告)号：EP0489458A1
公开(公告)日：1992-06-10
申请号：EP91203099.6
申请日：1991-11-27
申请人： MERCK SHARP & DOHME LTD.
发明人： Carling, William R. , Leeson, Paul D. , Moore, Kevin W.
IPC分类号： C07D401/04 , A61K31/47
CPC分类号： C07D401/04
摘要： A class of 4-hydroxy-2(1H)-quinolone derivatives, substituted at the 3-position by an N-linked heteroaromatic ring system, are selective non-competitive antagonists of NMDA receptors and/or are antagonists of AMPA receptors, and are therefore of utility in the treatment of conditions, such as neurodegenerative disorders, convulsions or schizophrenia, which require the administration of an NMDA and or AMPA receptor antagonist.
摘要翻译：一类4-位羟基-2（1H） - 喹诺酮衍生物，在3-位被N-连接的杂芳环体系取代，是NMDA受体的选择性非竞争性拮抗剂和/或是AMPA受体的拮抗剂，因此可用于治疗需要给予NMDA和/或AMPA受体拮抗剂的病症如神经变性疾病，惊厥或精神分裂症。

9. 发明公开

EP0459561A2 Dioxo-tetrahydroquinoline derivatives 失效
标题翻译：二氧tetrahydrochinolinderivate。
公开(公告)号：EP0459561A2
公开(公告)日：1991-12-04
申请号：EP91201216.8
申请日：1991-05-22
申请人： MERCK SHARP & DOHME LTD.
发明人： Baker, Raymond , Stevenson, Graeme I. , Leeson, Paul D. , Rowley, Michael
IPC分类号： C07D409/06 , A61K31/47 , C07D409/04 , C07D401/04 , C07D215/22 , C07D405/04 , C07D401/12 , C07D409/12 , C07D413/04 , C07D404/04
CPC分类号： C07D215/22 , C07D215/56 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/06 , C07D409/04 , C07D409/06 , C07D409/12 , C07D413/04
摘要： A class of 2,4-dioxo-1,2,3,4-tetrahydroquinoline derivatives, substituted at the 3-position by a range of carbonyl-containing substituents or by a five- or six-membered heteroaromatic moiety, are selective non-competitive antagonists of NMDA receptors and/or are antagonists of AMPA receptors, and are therefore of utility in the treatment of conditions, such as neurodegenerative disorders, convulsions or schizophrenia, which require the administration of an NMDA and/or AMPA antagonist.
摘要翻译：一类在3-位被一定范围的含羰基取代基或五元或六元杂芳族部分取代的2,4-二氧代-1,2,3,4-四氢喹啉衍生物是选择性非 - NMDA受体的竞争性拮抗剂和/或是AMPA受体的拮抗剂，因此可用于治疗需要施用NMDA和/或AMPA拮抗剂的诸如神经变性疾病，惊厥或精神分裂症的病症。

10. 发明公开

EP0303512A1 Substituted dibenzocycloheptenimines 失效
标题翻译：取代基二苯并环庚烯亚胺。
公开(公告)号：EP0303512A1
公开(公告)日：1989-02-15
申请号：EP88307515.2
申请日：1988-08-12
申请人： MERCK SHARP & DOHME LTD.
发明人： Baker, Raymond , Leeson, Paul D. , Britcher, Susan F.
IPC分类号： C07D451/00 , C07C239/00
CPC分类号： C07D451/00
摘要： The present invention provides a compound of formula (I):
or a pharmaceutically acceptable salt thereof, wherein one of R¹, R², R³ and R⁴ represents a hydrocarbon or hydrocarbyloxycarbonyl group and the remaining groups R¹, R², R³ and R⁴ independently represent hydrogen, hydrocarbon, hydrocarbyloxycarbonyl, halogen, hydroxy or C₁₋₆ alkoxy, or R¹ and R² or R³ and R⁴ may together represent the residue of a carbocyclic ring; R⁵ and R⁶ independently represent hydrogen, hydrocarbon, hydroxy or fluoro; R⁷ represents hydrogen or C₁₋₃ alkyl; and R⁸ represents methyl or ethyl; which compounds are useful as anticonvulsant agents and in the treatment of neurodegenerative diseases.
摘要翻译：本发明提供式（I）化合物：其中R 1，R 2，R 3和R 4中的一个代表烃或烃氧基羰基其余基团R 1，R 2，R 3和R 4独立地表示氢，烃，烃氧基羰基，卤素，羟基或C 1-6烷氧基，或R 1和R 2独立地是氢，或R 3和R 4可以一起代表碳环的残基; R 5和R 6独立地表示氢，烃，羟基或氟; R 7表示氢或C 1-3烷基; 并且R 8表示甲基或乙基; 哪些化合物可用作抗惊厥药和治疗神经变性疾病。

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