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。

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.

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.

公开(公告)号：US5446066A

公开(公告)日：1995-08-29

申请号：US215628

申请日：1994-03-22

申请人： Mario Varasi ,  Philippe Dostert ,  Paolo Pevarello ,  Alberto Bonsignori

发明人： Mario Varasi ,  Philippe Dostert ,  Paolo Pevarello ,  Alberto Bonsignori

IPC分类号： A61K31/165 ,  A61P25/00 ,  A61P25/08 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  C07C231/10 ,  C07C237/00 ,  C07C237/06 ,  C07C233/04

CPC分类号： C07C237/00

摘要： The invention provides new compounds of formula (I) ##STR1## wherein, subject to a proviso, n is zero or an integer of 1 to 3; each of R and R.sub.1, which may be the same or different, is hydrogen, halogen, trifluoromethyl or C.sub.1 -C.sub.4 alkoxy; R.sub.2 is hydrogen or C.sub.1 -C.sub.4 alkyl optionally substituted by hydroxy; each of R.sub.3 and R.sub.4 independently is hydrogen or C.sub.1 -C.sub.4 alkyl; or a pharmaceutically acceptable salt thereof; and of formula (IA) ##STR2## wherein R.sub.5 is hydrogen, halogen, trifluoromethyl or C.sub.1 -C.sub.4 alkoxy, or a pharmaceutically acceptable salt thereof, which are active on the central nervous system (CNS) and can be used in therapy as anti-epileptics, anti-Parkinson, neuroprotective, antidepressant, anti-spastic and hypnotic agents.

摘要翻译： 本发明提供新的式（I）化合物其中，条件是n为0或1〜3的整数; R和R 1可以相同或不同，为氢，卤素，三氟甲基或C 1 -C 4烷氧基; R2是氢或任选被羟基取代的C 1 -C 4烷基; R 3和R 4各自独立地是氢或C 1 -C 4烷基; 或其药学上可接受的盐; 和式（IA）的化合物（IA）其中R5是氢，卤素，三氟甲基或C1-C4烷氧基，或其药学上可接受的盐，其在中枢神经系统（CNS）上是有活性的并且可以用于治疗 作为抗癫痫药，抗帕金森综合征，神经保护药，抗抑郁药，抗痉挛药和催眠药。

公开(公告)号：US5449692A

公开(公告)日：1995-09-12

申请号：US215694

申请日：1994-03-22

申请人： Mario Varasi ,  Philippe Dostert ,  Paolo Pevarello ,  Alberto Bonsignori

发明人： Mario Varasi ,  Philippe Dostert ,  Paolo Pevarello ,  Alberto Bonsignori

IPC分类号： A61K31/165 ,  A61P25/00 ,  A61P25/08 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P43/00 ,  C07C231/10 ,  C07C237/06 ,  C07C233/05

CPC分类号： C07C237/06

摘要： The invention provides new compounds of formula (I) ##STR1## wherein n is an integer of 1 to 4; each of R and R.sub.1, which may be the same or different, is hydrogen, halogen, trifluoromethyl or C.sub.1 -C.sub.4 alkoxy; R2 is hydrogen or C.sub.1 -C.sub.4 alkyl; and a pharmaceutically acceptable salts thereof; and wherein when, at the same time, R is hydrogen, R.sub.1 is hydrogen or halogen and n is one, then R.sub.2 is other than hydrogen or methyl; and of formula (IA) ##STR2## wherein R.sub.3 is halogen, and a pharmaceutical acceptable salt thereof, which are active on the central nervous system (CNS) and can be used in therapy as anti-epileptics, anti-Parkinson, neuroprotective, antidepressant, anti-spastic and hypnotic agents.

摘要翻译： 本发明提供新的式（I）化合物其中n为1至4的整数; R和R 1可以相同或不同，为氢，卤素，三氟甲基或C 1 -C 4烷氧基; R2是氢或C1-C4烷基; 及其药学上可接受的盐; 并且其中当R同时为氢时，R 1为氢或卤素且n为1，则R 2为氢或甲基; 和式（IA）其中R 3是卤素的式（IA）及其药学上可接受的盐，其在中枢神经系统（CNS）上是有活性的，可用于治疗作为抗癫痫药，抗帕金森病， 神经保护，抗抑郁药，抗痉挛药和催眠药。

公开(公告)号：US5272144A

公开(公告)日：1993-12-21

申请号：US499257

申请日：1991-06-13

申请人： Piero Melloni ,  Philippe Dostert ,  Arturo D. Torre ,  Alberto Bonsignori

发明人： Piero Melloni ,  Philippe Dostert ,  Arturo D. Torre ,  Alberto Bonsignori

IPC分类号： A61K31/13 ,  A61K31/135 ,  A61K31/357 ,  A61K31/36 ,  A61K31/38 ,  A61K31/381 ,  A61K31/40 ,  A61P3/04 ,  A61P25/24 ,  A61P25/26 ,  A61P25/30 ,  C07C47/277 ,  C07C217/46 ,  C07C217/48 ,  C07C217/54 ,  C07C217/72 ,  C07C217/84 ,  C07C255/54 ,  C07C275/10 ,  C07C275/32 ,  C07C317/22 ,  C07D207/335 ,  C07D317/54 ,  C07D317/58 ,  C07D317/64 ,  C07D333/20 ,  C07D333/32 ,  C07D521/00 ,  A61K31/54 ,  C07D279/12

CPC分类号： C07C255/54 ,  C07C217/48 ,  C07C217/72 ,  C07C217/84 ,  C07C275/10 ,  C07C317/22 ,  C07D317/58 ,  C07D317/64 ,  C07D333/20 ,  C07D333/32

摘要： Aryloxy- and heteroaryloxy-alkylene derivatives of amines of formula ##STR1## wherein each of A and B is a group of formula (i) to (iii): ##STR2## wherein Y is --O--, --S-- or --NR-- in which R is hydrogen or C.sub.1 -C.sub.6 alkyl; each of R.sub.3, R.sub.4, R.sub.5 and R.sub.6 is independently:a) hydrogen, halogen, hydroxy, cyano or nitro;b) C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by halogen,c) C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkylthio;d) C.sub.1 -C.sub.6 alkyl-sulfonyl;e) a substituted amine group --NR.sub.7 R.sub.8 ;f) a --COR.sub.12 group; org) two adjacent groups of R.sub.3, R.sub.4, R.sub.5 and R.sub.6, taken together, form a C.sub.1 -C.sub.4 alkylenedioxy group;each of R.sub.1 and R.sub.2 independently is hydrogen, C.sub.3 -C.sub.6 alkynyl, C.sub.3 -C.sub.6 alkenyl or C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl; or R.sub.1 and R.sub.2 taken together with the nitrogen atom to which they are linked, form a substituted or unsubstituted, saturated heterocyclic ring; and the pharmaceutically acceptable salts thereof; are active on the central nervous nervous system, in particular as antidepressant, antiobesity antismoking and anti-alcoholabuse agents.

公开(公告)号：US4863956A

公开(公告)日：1989-09-05

申请号：US886790

申请日：1986-07-18

申请人： Bruno Gabetta ,  Maria J. Magistretti ,  Philippe Dostert

发明人： Bruno Gabetta ,  Maria J. Magistretti ,  Philippe Dostert

IPC分类号： A61K31/35 ,  A61P1/04 ,  A61P3/06 ,  A61P9/14 ,  A61P43/00 ,  C07D493/18

CPC分类号： C07D493/18 ,  A61K31/35 ,  A61K36/77 ,  A61K9/4858 ,  A61K2236/00 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/0056 ,  Y10S514/926 ,  Y10S514/927

摘要： There is described a process for preparing proanthocyanidine A2 by extraction from cortex or fruits of Aesculus hippocastanum and related species and its activity for stimulating healing processes, e.g. healing wounds and injuries of various origins, gastric and duodenal ulcers for modifying conditions of impaired capillary permeability and resistance and for obtaining an anti-lipid peroxidation effect.There are also described pharmaceutical formulations suitable for use by topical and systemic routes.

摘要翻译： 描述了通过从眉毛和相关物种的皮质或果实中提取原花青素A2的方法及其刺激愈合过程的活性，例如， 治愈各种原因的伤口和伤口，胃和十二指肠溃疡，用于修饰毛细血管通透性和抗性受损的病症，并获得抗脂质过氧化作用。 还描述了适用于局部和全身途径的药物制剂。

公开(公告)号：US4138482A

公开(公告)日：1979-02-06

申请号：US840790

申请日：1977-10-11

申请人： Philippe Dostert

发明人： Philippe Dostert

IPC分类号： A61K31/00 ,  A61K31/55 ,  A61P25/24 ,  A61P25/26 ,  C07D223/22 ,  C07D223/28

CPC分类号： C07D223/22 ,  C07D223/28

摘要： 3-Cyano-N-(N,N-dimethylaminopropyl)-iminodibenzyl, and its salts, prepared, inter alia, by heating 3-cyano-iminodibenzyl-5-carboxylic acid (N,N-dimethylaminopropyl ester) are described. The end product and its salts are useful as antidepressants.

摘要翻译： 描述了3-氰基-N-（N，N-二甲基氨基丙基） - 亚氨基二苄基及其盐，特别是通过加热3-氰基 - 亚氨基二苄基-5-羧酸（N，N-二甲基氨基丙酯）制备。 最终产物及其盐可用作抗抑郁药。

公开(公告)号：US4003915A

公开(公告)日：1977-01-18

申请号：US588268

申请日：1975-06-19

申请人： Philippe Dostert ,  Emilio Kyburz

发明人： Philippe Dostert ,  Emilio Kyburz

IPC分类号： C07C65/36 ,  C07D337/12

CPC分类号： C07C65/36

摘要： Tricyclic imines of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, X, m and n are as hereinafter described, prepared from the corresponding ketones of the formula ##STR2## wherein R.sup.1, X and m are as hereinafter described, are disclosed. The compounds of formula I are useful as antidepressants, as well as anticonvulsants and agents for the treatment of Parkinsonism.

摘要翻译： 其中R 1，R 2，R 3，R 4，X，m和n如下文所述，由下式其中R 1，X和m如下文所述的相应的酮制备的式（I）所示的三环亚胺 ，被披露。 式I的化合物可用作抗抑郁药，以及抗惊厥药和用于治疗帕金森综合征的药剂。

公开(公告)号：US4925870A

公开(公告)日：1990-05-15

申请号：US356895

申请日：1989-05-25

申请人： Bruno Gabetta ,  Maria J. Magistretti ,  Philippe Dostert

发明人： Bruno Gabetta ,  Maria J. Magistretti ,  Philippe Dostert

IPC分类号： A61K31/35 ,  A61P1/04 ,  A61P3/06 ,  A61P9/14 ,  A61P43/00 ,  C07D493/18

CPC分类号： C07D493/18 ,  A61K31/35 ,  A61K36/77 ,  A61K9/4858 ,  A61K2236/00 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/0056 ,  Y10S514/926 ,  Y10S514/927

摘要： There is described a process for preparing proanthocyanidine A2 by extraction from cortex or fruits of Aesculus hippocastanum and related species and its activity for stimulating healing processes, e.g. healing wounds and injuries of various origins, gastric and duodenal ulcers for modifying conditions of impaired capillary permeability and resistance and for obtaining an anti-lipid peroxidation effect.There are also described pharmaceutical formulations suitable for use by topical and systemic routes.