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1. 发明授权

US5424328A Phenyl-imidazolidinone derivatives 失效
标题翻译：苯基咪唑啉酮衍生物
公开(公告)号：US5424328A
公开(公告)日：1995-06-13
申请号：US144514
申请日：1993-11-02
申请人： Mario Varasi , Franco Heidempergher , Carla Caccia , Claudio Arrigoni
发明人： Mario Varasi , Franco Heidempergher , Carla Caccia , Claudio Arrigoni
IPC分类号： C07D403/06 , A61K31/415 , A61K31/4178 , A61P1/00 , A61P1/08 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/20 , A61P25/26 , C07D233/32 , C07D233/54 , C07D233/56 , C07D233/61 , C07D401/06
CPC分类号： C07D233/64 , Y02P20/55
摘要： The invention relates to new derivatives of 1-imidazolylalkyl-3-phenyl-imidazolidin-2-ones of general formula (I) ##STR1## wherein n is 1, 2 or 3; each of R, R.sub.1 and R.sub.2, which may be the same or different, is hydrogen, halogen, hydroxy, cyano, C.sub.1 -C.sub.6 alkyl, CF.sub.3, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, formyl, C.sub.2 -C.sub.6 alkanoyl, carboxy, C.sub.1 -C.sub.6 alkoxy-carbonyl, nitro, --N(R.sub.4 R.sub.5) in which each of R.sub.4 and R.sub.5 independently is hydrogen C.sub.1 -C.sub.6 alkyl formyl or C.sub.2 -C.sub.6 alkanoyl; or a (R.sub.6 R.sub.7)N--SO.sub.2 group, in which each of R.sub.6 and R.sub.7 independently is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.3 is an imidazolyl group of formula ##STR2## wherein each of R.sub.8 and R.sub.10 which may be the same or different is hydrogen or C.sub.1 -C.sub.6 alkyl, R.sub.9 is hydrogen, C.sub.1 -C.sub.6 alkyl or a nitrogen protecting group, or pharmaceutically acceptable salts thereof, which are useful in the treatment of CNS disorders, such as, e.g., anxiety and psychosis, and in the treatment of gut motility disorders, and/or emesis.
摘要翻译：本发明涉及通式（I）的单咪唑烷基-3-苯基 - 咪唑烷-2-酮的新衍生物，其中n为1,2或3; R，R 1和R 2可以相同或不同，为氢，卤素，羟基，氰基，C 1 -C 6烷基，CF 3，C 1 -C 6烷氧基，C 1 -C 6烷硫基，甲酰基，C 2 -C 6烷酰基，羧基，其中R 4和R 5各自独立地是C 1 -C 6烷基甲酰基或C 2 -C 6烷酰基的C 1 -C 6烷氧基羰基，硝基，-N（R 4 R 5）或（R6R7）N-SO2基团，其中R6和R7各自独立地为氢或C1-C6烷基; R3是式IMAMA的咪唑基，其中R 8和R 10可以相同或不同的是氢或C 1 -C 6烷基，R 9是氢，C 1 -C 6烷基或氮保护基，或其药学上可接受的盐，其可用于治疗中枢神经系统疾病，例如焦虑和精神病，以及肠道运动障碍和/或呕吐的治疗。

2. 发明授权

US5364854A Derivatives of substituted imidazo benzoxazin-1-one and process for their preparation 失效
标题翻译：取代的咪唑并苯并恶嗪-1-酮的衍生物及其制备方法
公开(公告)号：US5364854A
公开(公告)日：1994-11-15
申请号：US70860
申请日：1993-06-03
申请人： Mario Varasi , Franco Heidempergher , Claudio Arrigoni , Carla Caccia
发明人： Mario Varasi , Franco Heidempergher , Claudio Arrigoni , Carla Caccia
IPC分类号： A61K31/535 , A61P25/26 , C07D498/04 , C07D519/00 , C07D487/04 , A61K35/00
CPC分类号： C07D519/00 , Y10S514/872
摘要： Derivatives of 2,3,3a,4-tetrahydro-2-azabicyclo alkyl-1H-imidazo[5,1,-c][1,4]benzoxazin-1-one are provided of general formula (I) ##STR1## in which inter alia R.sub.3 represents ##STR2## wherein n is an integer of 1 or 2 and R.sub.8 is hydrogen, C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, formyl or C.sub.2 -C.sub.6 alkanoyl; and the pharmaceutically acceptable salts thereof, which are useful in the treatment of CNS disorders, gut motility disorders, emesis and migraine, as cognition activators, anti-drug addiction agents and analgesic.
摘要翻译： 2,3,3a，4-四氢-2-氮杂双环烷基-1H-咪唑并[5,1，-c] [1,4]苯并恶嗪-1-酮的衍生物由通式（I）提供。 I），其中特别是R3表示其中n是1或2的整数，R8是氢，未被取代或被苯基，C 2 -C 4烯基，C 2 -C 4炔基，甲酰基或C 2 -C 6取代的C 1 -C 6烷基烷酰基; 及其药学上可接受的盐，其可用于治疗CNS障碍，肠蠕动障碍，呕吐和偏头痛，作为认知激活剂，抗药成瘾剂和止痛剂。

3. 发明授权

US5637596A Azabicycloalkyl derivatives of imidazo[1,5-a]indol-3-one and process for their preparation 失效
标题翻译：咪唑并[1,5-a]吲哚-3-酮的氮杂双环烷基衍生物及其制备方法
公开(公告)号：US5637596A
公开(公告)日：1997-06-10
申请号：US578548
申请日：1996-01-24
申请人： Mario Varasi , Franco Heidempergher , Carla Caccia , Patricia Salvati
发明人： Mario Varasi , Franco Heidempergher , Carla Caccia , Patricia Salvati
IPC分类号： A61K31/41 , A61K31/435 , A61K31/439 , A61K31/46 , A61P1/00 , A61P1/08 , A61P25/00 , A61P25/06 , A61P25/18 , A61P25/22 , A61P25/28 , A61P25/36 , A61P43/00 , C07D451/04 , C07D451/14 , C07D453/02 , C07D519/00
CPC分类号： C07D453/02 , C07D451/04 , C07D451/14
摘要： Novel 5-HT.sub.3 receptor antagonist compounds having the general formula (I) ##STR1## wherein each of R, R.sub.1 and R.sub.2, which may be the same or different, is hydrogen, halogen, hydroxy, cyano, C.sub.1 -C.sub.6 alkyl, CF.sub.3, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, formyl, C.sub.2 -C.sub.6 alkanoyl, carboxy, C.sub.1 -C.sub.6 alkoxy-carbonyl, nitro, --N(R.sub.4 R.sub.5) in which each of R.sub.4 and R.sub.5 independently is hydrogen, C.sub.1 -C.sub.6 alkyl, formyl or C.sub.2 -C.sub.6 alkanoyl; or a (R.sub.6 R.sub.7)N--SO.sub.2 group, in which each of R.sub.6 and R.sub.7 independently is hydrogen or C.sub.1 -C.sub.6 alkyl; ##STR2## wherein n is an integer of 1 or 2 and R.sub.8 is hydrogen, C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, formyl or C.sub.2 -C.sub.6 alkanoyl; and the pharmaceutically acceptable salts thereof, are provided.
摘要翻译： PCT No.PCT / EP95 / 01652 Sec。 371日期：1996年1月24日 102（e）日期1996年1月24日PCT 1995年5月2日PCT PCT。公开号WO95 / 32209 日期1995年11月30日具有通式（I）的图像的新型5-HT 3受体拮抗剂化合物（I）其中R，R 1和R 2可以相同或不同，为氢，卤素，羟基，氰基，C 1 -C 6烷基，CF 3，C 1 -C 6烷氧基，C 1 -C 6烷硫基，甲酰基，C 2 -C 6烷酰基，羧基，C 1 -C 6烷氧羰基，硝基，-N（R 4 R 5）是氢，C 1 -C 6烷基，甲酰基或C 2 -C 6烷酰基; 或（R6R7）N-SO2基团，其中R6和R7各自独立地为氢或C1-C6烷基; R3是a，a）或b）其中n是1或2的整数，R8是氢，未被取代或被苯基取代的C1-C6烷基，C2-C4烯基，C2-C4炔基，或C 2 -C 6烷酰基; 及其药学上可接受的盐。

4. 发明授权

US5874457A Imidazolylalkyl derivatives of imidazo�1,5-a!indol-3-one 失效
标题翻译：咪唑并[1,5-a]吲哚-3-酮的咪唑基烷基衍生物
公开(公告)号：US5874457A
公开(公告)日：1999-02-23
申请号：US578550
申请日：1996-01-24
申请人： Mario Varasi , Franco Heidempergher , Carla Caccia , Patricia Salvati
发明人： Mario Varasi , Franco Heidempergher , Carla Caccia , Patricia Salvati
IPC分类号： A61K31/415 , A61K31/4188 , A61P1/00 , A61P1/08 , A61P1/12 , A61P25/06 , A61P25/18 , A61P25/22 , A61P25/28 , A61P25/36 , A61P43/00 , C07D487/04
CPC分类号： C07D487/04 , Y02P20/55
摘要： Novel 5-HT.sub.3 receptor antagonist compounds having following formula (I) ##STR1## wherein n is 1, 2 or 3;each of R, R.sub.1 and R.sub.2, which may be the same or different, is hydrogen, halogen, hydroxy, cyano, C.sub.1 -C.sub.6 alkyl, CF.sub.3, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, formyl, C.sub.2 -C.sub.6 alkanoyl, carboxy, C.sub.1 -C.sub.6 alkoxy-carbonyl, nitro, --N (R.sub.4 R.sub.5) in which each of R.sub.4 and R.sub.5 independently is hydrogen, C.sub.1 -C.sub.6 alkyl, formyl or C.sub.2 -C.sub.6 alkanoyl; or a (R.sub.6 R.sub.7) N--SO.sub.2 group, in which each of R.sub.6 and R.sub.7 independently is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.3 is an imidazolyl group of formula ##STR2## wherein each of R.sub.8 and R.sub.10 which may be the same or different is hydrogen or C.sub.1 -C.sub.6 alkyl, R.sub.9 is hydrogen, C.sub.1 -C.sub.6 alkyl or a nitrogen protecting group; and the pharmaceutically acceptable salts thereof, are disclosed.
摘要翻译： PCT No.PCT / EP95 / 01651 Sec。 371日期：1996年1月24日 102（e）日期1996年1月24日PCT 1995年5月2日PCT PCT。出版物WO95 / 32204 日期：1995年11月30日具有下式（I）的新型5-HT 3受体拮抗剂化合物其中n为1,2或3; R，R 1和R 2可以相同或不同，为氢，卤素，羟基，氰基，C 1 -C 6烷基，CF 3，C 1 -C 6烷氧基，C 1 -C 6烷硫基，甲酰基，C 2 -C 6烷酰基，羧基，其中R 4和R 5各自独立地为氢，C 1 -C 6烷基，甲酰基或C 2 -C 6烷酰基的C 1 -C 6烷氧羰基，硝基，-N（R 4 R 5）或（R6R7）N-SO2基团，其中R6和R7各自独立地为氢或C1-C6烷基; R 3是式（I）的咪唑基，其中R 8和R 10各自可以相同或不同，是氢或C 1 -C 6烷基，R 9是氢，C 1 -C 6烷基或氮保护基; 及其药学上可接受的盐。

5. 发明授权

US5783574A Imidazolylakyl derivatives of imidazo �5,1-c!�1,4!benzoxazin-1-one process for their preparation 失效
标题翻译：咪唑并[5,1-c] [1,4]苯并恶嗪-1-酮的咪唑基]甲基衍生物的制备方法
公开(公告)号：US5783574A
公开(公告)日：1998-07-21
申请号：US578549
申请日：1996-01-24
申请人： Mario Varasi , Franco Heidempergher , Carla Caccia , Patricia Salvati
发明人： Mario Varasi , Franco Heidempergher , Carla Caccia , Patricia Salvati
IPC分类号： A61K31/535 , A61K31/5383 , A61P1/00 , A61P1/08 , A61P25/00 , A61P25/06 , A61P25/18 , A61P25/22 , A61P25/28 , A61P25/36 , A61P43/00 , C07D498/04
CPC分类号： C07D498/04 , Y02P20/55
摘要： Novel 5-HT.sub.3 receptor antagonist compounds having following formula (I) ##STR1## wherein n is 1, 2 or 3; each of R, R.sub.1 and R.sub.2, which may be the same or different, is hydrogen, halogen, hydroxy, cyano, C.sub.1 -C.sub.6 alkyl, CF.sub.3, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, formyl, C.sub.2 -C.sub.6 alkanoyl, carboxy, C.sub.1 -C.sub.6 alkoxy-carbonyl, nitro, --N (R.sub.4 R.sub.5) in which each of R.sub.4 and R.sub.5 independently is hydrogen, C.sub.1 -C.sub.6 alkyl, formyl or C.sub.2 -C.sub.6 alkanoyl; or a (R.sub.6 R.sub.7) N--SO.sub.2 group, in which each of R6 and R.sub.7 independently is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.3 is an imidazolyl group of formula ##STR2## wherein each of R.sub.8 and R.sub.10 which may be the same or different is hydrogen or C.sub.1 -C.sub.6 alkyl, R.sub.9 is hydrogen, C.sub.1 -C.sub.6 alkyl or a nitrogen protecting group; and the pharmaceutically acceptable salts thereof, are disclosed.
摘要翻译： PCT No.PCT / EP95 / 01650 Sec。 371日期：1996年1月24日 102（e）日期1996年1月24日PCT 1995年5月2日PCT PCT。公开号WO95 / 32208 PCT 日期：1995年11月30日具有下式（I）的新型5-HT 3受体拮抗剂化合物其中n为1,2或3; R，R 1和R 2可以相同或不同，为氢，卤素，羟基，氰基，C 1 -C 6烷基，CF 3，C 1 -C 6烷氧基，C 1 -C 6烷硫基，甲酰基，C 2 -C 6烷酰基，羧基，其中R 4和R 5各自独立地为氢，C 1 -C 6烷基，甲酰基或C 2 -C 6烷酰基的C 1 -C 6烷氧羰基，硝基，-N（R 4 R 5）或（R6R7）N-SO2基团，其中R6和R7各自独立地为氢或C1-C6烷基; R 3是式A的咪唑基a）其中R 8和R 10可以相同或不同的是氢或C 1 -C 6烷基，R 9是氢，C 1 -C 6烷基或氮保护组; 及其药学上可接受的盐。

6. 发明授权

US5236957A N-phenylalkyl substituted .alpha.-amino carboxamide derivatives and process for their preparation 失效
标题翻译：取代（α-氨基）氨基甲酰胺衍生物及其制备方法
公开(公告)号：US5236957A
公开(公告)日：1993-08-17
申请号：US646596
申请日：1991-01-25
申请人： Philippe Dostert , Paolo Pevarello , Franco Heidempergher , Mario Varasi , Alberto Bonsignori , Romeo Roncucci
发明人： Philippe Dostert , Paolo Pevarello , Franco Heidempergher , Mario Varasi , Alberto Bonsignori , Romeo Roncucci
IPC分类号： C07C237/06 , A61K31/16 , A61K31/33 , A61K31/34 , A61K31/341 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61P25/00 , A61P25/08 , A61P25/20 , A61P25/24 , A61P25/26 , C07C231/02 , C07C231/10 , C07C323/63 , C07D213/30 , C07D307/42 , C07D307/58 , C07D333/16 , C07D333/32
CPC分类号： C07D213/30 , C07C237/06 , C07C323/63 , C07D307/58 , C07D333/32
摘要： N-phenylalkyl substituted .alpha.-amino carboxamide derivatives of formula (I) ##STR1## wherein R is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, furyl, thienyl, pyridyl or unsubstituted or substituted phenyl; A is a --(CH.sub.2).sub.m -- or --(CH.sub.2).sub.p --X--(CH.sub.2).sub.q -- group wherein X is --O--, --S-- or --NR.sub.4 --; R.sub.1, R.sub.2, R.sub.3, R'.sub.3, R.sub.4, n, m, p and q are as herein defined; and each of R.sub.5 and R.sub.6 is independently hydrogen or C.sub.1 -C.sub.6 alkyl, and the pharmaceutically acceptable salts thereof, are active on the central nervous system and can be used as anti-epileptic, anti-Parkinson, neuroprotective, antidepressant, antispastic and/or hypnotic agents in mammals.

7. 发明授权

US5391577A N-phenylalkyl substituted .alpha.-amino carboxamide derivatives and process for their preparation 失效
标题翻译： N-苯基烷基取代的α-氨基甲酰胺衍生物及其制备方法
公开(公告)号：US5391577A
公开(公告)日：1995-02-21
申请号：US065888
申请日：1993-05-25
申请人： Philippe Dostert , Paolo Pevarello , Franco Heidempergher , Mario Varasi , Alberto Bonsignori , Romeo Roncucci
发明人： Philippe Dostert , Paolo Pevarello , Franco Heidempergher , Mario Varasi , Alberto Bonsignori , Romeo Roncucci
IPC分类号： C07C237/06 , A61K31/16 , A61K31/33 , A61K31/34 , A61K31/341 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61P25/00 , A61P25/08 , A61P25/20 , A61P25/24 , A61P25/26 , C07C231/02 , C07C231/10 , C07C323/63 , C07D213/30 , C07D307/42 , C07D307/58 , C07D333/16 , C07D333/32 , A61K31/165
CPC分类号： C07D213/30 , C07C237/06 , C07C323/63 , C07D307/58 , C07D333/32
摘要： N-phenylalkyl substituted .alpha.-amino carboxamide derivatives of formula (I) ##STR1## wherein R is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, furyl, thienyl, pyridyl or unsubstituted or substituted phenyl; A is a --(CH.sub.2).sub.m -- or --(CH.sub.2).sub.p --X--(CH.sub.2).sub.q -- group wherein X is --O--, --S-- or --NR.sub.4 --; R.sub.1, R.sub.2, R.sub.3, R'.sub.3, R.sub.4, n, m, p and q are as herein defined; and each of R.sub.5 and R.sub.6 is independently hydrogen or C.sub.1 -C.sub.6 alkyl, and the pharmaceutically acceptable salts thereof, are active on the central nervous system and can be used as anti-epileptic, anti-Parkinson, neuroprotective, antidepressant, antispastic and/or hypnotic agents in mammals.
摘要翻译：式（I）的N-苯基烷基取代的α-氨基甲酰胺衍生物其中R为C1-C8烷基，C3-C8环烷基，呋喃基，噻吩基，吡啶基或未取代或取代的苯基; A是 - （CH 2）m - 或 - （CH 2）p -X-（CH 2）q-基，其中X是-O - ， - S-或-NR 4 - ; R1，R2，R3，R'3，R4，n，m，p和q如本文所定义; 并且R 5和R 6各自独立地为氢或C 1 -C 6烷基，并且其药学上可接受的盐在中枢神经系统上具有活性，可用作抗癫痫药，抗帕金森综合征，神经保护药，抗抑郁药，抗痉挛药和/或哺乳动物催眠药。

8. 发明授权

US5401750A Derivatives of substituted imidazol-2-one and process for their preparation 失效
标题翻译：取代咪唑-2-酮的衍生物及其制备方法
公开(公告)号：US5401750A
公开(公告)日：1995-03-28
申请号：US76153
申请日：1993-06-14
申请人： Mario Varasi , Franco Heidempergher , Nicola Carfagna , Ruggero Fariello
发明人： Mario Varasi , Franco Heidempergher , Nicola Carfagna , Ruggero Fariello
IPC分类号： A61K31/435 , A61K31/4166 , A61K31/429 , A61P1/00 , A61P1/08 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/28 , A61P25/30 , A61P29/00 , A61P43/00 , C07D233/32 , C07D403/04 , C07D451/02 , C07D451/04 , C07D451/14 , C07D453/02 , C07D401/04 , A61K31/46
CPC分类号： C07D451/04 , C07D451/14 , C07D453/02 , Y10S514/81 , Y10S514/872
摘要： Derivatives of 1-phenyl-3-azabicycloalkylimidazolidin-2-ones are provided of general formula (I) ##STR1## in which inter alia R.sub.3 represents a group ##STR2## wherein n is an integer of 1 or 2 and R.sub.8 is hydrogen, C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, formyl or C.sub.2 -C.sub.6 alkanoyl; and the pharmaceutically acceptable salts thereof, which are useful in the treatment of CNS disorders, gut motility disorders, emesis and migraine, as cognition activators, anti-drug addition agents and analgesic.
摘要翻译： 1-苯基-3-氮杂双环烷基咪唑烷-2-酮的衍生物由通式（I）提供，其中特别是R 3表示基团，其中n为1或2的整数，R 8为氢，未取代或被苯基取代的C 1 -C 6烷基，C 2 -C 4烯基，C 2 -C 4炔基，甲酰基或C 2 -C 6烷酰基; 其药学上可接受的盐，其可用于治疗CNS障碍，肠蠕动障碍，呕吐和偏头痛，作为认知激活剂，抗药物添加剂和止痛剂。

9. 发明授权

US5502079A N-phenylalkyl substituted .alpha.-amino carboxamide derivatives and process for their preparation 失效
公开(公告)号：US5502079A
公开(公告)日：1996-03-26
申请号：US343853
申请日：1994-11-17
申请人： Philippe Dostert , Paolo Pevarello , Franco Heidempergher , Mario Varasi , Alberto Bonsignori , Romeo Roncucci
发明人： Philippe Dostert , Paolo Pevarello , Franco Heidempergher , Mario Varasi , Alberto Bonsignori , Romeo Roncucci
IPC分类号： C07C237/06 , A61K31/16 , A61K31/33 , A61K31/34 , A61K31/341 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61P25/00 , A61P25/08 , A61P25/20 , A61P25/24 , A61P25/26 , C07C231/02 , C07C231/10 , C07C323/63 , C07D213/30 , C07D307/42 , C07D307/58 , C07D333/16 , C07D333/32 , A61K31/165
CPC分类号： C07D213/30 , C07C237/06 , C07C323/63 , C07D307/58 , C07D333/32
摘要： N-phenylalkyl substituted .alpha.-amino carboxamide derivatives of formula (I) ##STR1## wherein R is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, furyl, thienyl, pyridyl or unsubstituted or substituted phenyl; A is a --(CH.sub.2).sub.m -- or --(CH.sub.2).sub.p --X--(CH.sub.2).sub.q -- group wherein X is --O--, --S-- or --NR.sub.4 --; R.sub.1, R.sub.2, R.sub.3, R'.sub.3, R.sub.4, n, m, p and q are as herein defined; and each of R.sub.5 and R.sub.6 is independently hydrogen or C.sub.1 -C.sub.6 alkyl, and the pharmaceutically acceptable salts thereof, are active on the central nervous system and can be used as anti-epileptic, anti-Parkinson, neuroprotective, antidepressant, antispastic and/or hypnotic agents in mammals.

10. 发明授权

US5242929A Derivatives of substituted imidazol-2-one and process for their preparation 失效
标题翻译：取代的咪唑烷-2-酮的衍生物及其制备方法
公开(公告)号：US5242929A
公开(公告)日：1993-09-07
申请号：US843339
申请日：1992-02-28
申请人： Mario Varasi , Franco Heidempergher , Nicola Carfagna , Ruggero Fariello
发明人： Mario Varasi , Franco Heidempergher , Nicola Carfagna , Ruggero Fariello
IPC分类号： A61K31/435 , A61K31/4166 , A61K31/429 , A61P1/00 , A61P1/08 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/28 , A61P25/30 , A61P29/00 , A61P43/00 , C07D233/32 , C07D403/04 , C07D451/02 , C07D451/04 , C07D451/14 , C07D453/02
CPC分类号： C07D451/04 , C07D451/14 , C07D453/02 , Y10S514/81 , Y10S514/872
摘要： Derivatives of 1-phenyl-3-azabicycloalkylimidazolidin-2-ones are provided of general formula (1) ##STR1## in which inter alia R represents a group ##STR2## wherein n is an integer of 1 or 2 and R.sub.8 is hydrogen, C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, formyl or C.sub.2 -C.sub.6 alkanoyl; and the pharmaceutically acceptable salts thereof. which are useful in the treatment of CNS disorders, gut motility disorders, emesis and migraine, as cognition activators, anti-drug addition agents and analgesic.

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