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1. 发明授权

US5192770A Serotonergic alpha-oxoacetamides 失效
标题翻译： SEROTONERGIC ALPHA-OXOACETAMIDES
公开(公告)号：US5192770A
公开(公告)日：1993-03-09
申请号：US624028
申请日：1990-12-07
申请人： Robin D. Clark , Richard M. Eglen , Joseph M. Muchowski , William L. Smith , Klaus K. Weinhardt
发明人： Robin D. Clark , Richard M. Eglen , Joseph M. Muchowski , William L. Smith , Klaus K. Weinhardt
IPC分类号： A61K31/435 , A61K31/46 , A61P1/00 , A61P1/08 , A61P9/00 , A61P25/00 , A61P25/04 , C07D451/04 , C07D451/08 , C07D451/14 , C07D453/02 , C07D453/06 , C07D471/08 , C07D487/08
CPC分类号： C07D451/04 , C07D451/14 , C07D453/02 , C07D471/08 , C07D487/08
摘要： .alpha.-Oxoacetamides of the formula R.sup.1 C(O)C(O)NR.sup.2 R.sup.3 in which R.sup.1 is optionally substituted phenyl, 1-indolyl, 2,3-dihydro-1-indolyl, 1-benzimidazolidinonyl, 3-benzofuranyl, 3-benzothiophenyl, 3-indolyl, and 1,2-alkano-3-indolyl; R.sup.2 is selected from: ##STR1## and R.sup.3 is selected from hydrogen or lower alkyl; and the pharmaceutically acceptable salts, individual isomers, mixtures of isomers, processes for preparation, compositions, and methods of use thereof.

2. 发明授权

US5202318A Tricyclic compounds acting at serotonin receptor subtypes 失效
标题翻译：作用于血清素受体亚型的三环化合物
公开(公告)号：US5202318A
公开(公告)日：1993-04-13
申请号：US708260
申请日：1991-05-28
申请人： Jacob Berger , Robin D. Clark , Richard M. Eglen , William L. Smith , Klaus K. Weinhardt
发明人： Jacob Berger , Robin D. Clark , Richard M. Eglen , William L. Smith , Klaus K. Weinhardt
IPC分类号： C07D401/04 , C07D451/04 , C07D451/14 , C07D453/02 , C07D471/08
CPC分类号： C07D401/04 , C07D451/04 , C07D451/14 , C07D453/02 , C07D471/08 , Y10S514/872
摘要： Compounds of Formula I: ##STR1## in which Z is CH.sub.2 or C.dbd.O;X and Y are independently selected from hydrogen, halogen, hydroxy, lower alkoxy, lower alkyl, nitro, amino, aminocarbonyl, (lower alkyl)amino, di(lower alkyl)amino and (lower alkanoyl)amino; and R.sup.1 is a group selected from Formulae (a), (b), (c) (d) and (e): ##STR2## in which p is 0 or 1;n is 1, 2 or 3;R.sup.2 is hydrogen, lower alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl-C.sub.12 alkyl, or a group R.sup.6 -C.sub.1-2 alkyl in which R.sup.6 is thienyl, pyrrolyl or furyl optionally substituted by one or two substituents selected from lower alkyl, lower alkoxy, trifluoromethyl or halogen, or is phenyl optionally substituted by one or two substituents selected from C.sub.1-4 alkoxy, trifluoromethyl, halogen, nitro, carboxy, esterified carboxy, and C.sub.1-4 alkyl optionally further substituted by hydroxy, C.sub.1-4 alkoxy, carboxy, esterified carboxy or in vivo hydrolyzable acyloxy;each R.sup.3 is independently selected from hydrogen, hydroxy, alkyl and alkoxy;each R.sup.4 is independently hydrogen or alkyl; andR.sup.5 is hydrogen, lower alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl-C.sub.1-2 alkyl, alkenyl, alkynyl or a group R.sup.7 -C.sub.1-3 alkyl in which R.sup.7 is phenyl or phenoxy optionally substituted by one or two substituents selected from C.sub.1-4 alkoxy, trifluoromethyl, halogen, nitro, carboxy, esterified carboxy, and C.sub.1-4 alkyl optionally further substituted by hydroxy, C.sub.1-4 alkoxy, carboxy, esterified carboxy or in vivo hydrolyzable acyloxy; and the pharmaceutically acceptable salts, individual isomers, mixtures of isomers, processes for preparation, compositions, and methods of use thereof.
摘要翻译：式I化合物：其中Z为CH 2或C = O; X和Y独立地选自氢，卤素，羟基，低级烷氧基，低级烷基，硝基，氨基，氨基羰基，（低级烷基）氨基，二（低级烷基）氨基和（低级烷酰基）氨基; （a），（b），（c）（d）和（e）所示的基团：（a）（e）其中p为0或1; n为1,2或3; R 2是氢，低级烷基，C 3-8环烷基，C 3-8环烷基-C 12烷基或其中R 6是噻吩基的R6-C 1-2烷基，任选地被一个或两个选自下列的取代基取代的吡咯基或呋喃基：低级烷基，低级烷氧基，三氟甲基或卤素，或者是被一个或两个选自C 1-4烷氧基，三氟甲基，卤素，硝基，羧基，酯化羧基和任选进一步被羟基，C 1-4烷氧基取代的C 1-4烷基取代的苯基，羧基，酯化羧基或体内可水解酰氧基; 每个R 3独立地选自氢，羟基，烷基和烷氧基; 每个R 4独立地是氢或烷基; R 5是氢，低级烷基，C 3-8环烷基，C 3-8环烷基-C 1-2烷基，链烯基，炔基或其中R 7是任选被一个或两个取代基所取代的苯基或苯氧基的基团由C 1-4烷氧基，三氟甲基，卤素，硝基，羧基，酯化羧基和任选进一步被羟基，C 1-4烷氧基，羧基，酯化羧基或体内可水解酰氧基进一步取代的C 1-4烷基; 和其药学上可接受的盐，各异构体，异构体的混合物，制备方法，组合物及其使用方法。

3. 发明授权

US5202333A Tricyclic 5-HT.sub.3 receptor antagonists 失效
标题翻译：三环5-HT 3受体拮抗剂
公开(公告)号：US5202333A
公开(公告)日：1993-04-13
申请号：US704565
申请日：1991-05-22
申请人： Jacob Berger , Robin D. Clark , Richard M. Eglen , William L. Smith , Klaus K. Weinhardt
发明人： Jacob Berger , Robin D. Clark , Richard M. Eglen , William L. Smith , Klaus K. Weinhardt
IPC分类号： C07D487/08 , A61K31/47 , A61K31/55 , A61P1/00 , A61P1/08 , A61P1/14 , A61P9/00 , A61P25/00 , A61P25/04 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P43/00 , C07D205/12 , C07D209/52 , C07D221/22 , C07D401/04 , C07D403/04 , C07D451/02 , C07D451/04 , C07D451/14 , C07D453/02 , C07D453/06 , C07D471/06 , C07D471/08
CPC分类号： C07D451/04 , C07D451/14 , C07D453/02 , C07D453/06 , C07D471/06 , C07D471/08 , Y10S514/872
摘要： The present invention is directed to 5-HT.sub.3 receptor antagonist compounds of formula I: ##STR1## in which the dashed line denotes an optional double bond;n is 1, 2 or 3;p is 0, 1, 2 or 3;q is 0, 1 or 2;each R.sup.1 is independently selected from halogen, hydroxy, lower alkoxy, lower alkyl, nitro, amino, amino carbonyl, (lower alkyl)amino, di(lower alkyl)amino, and (lower alkanoyl)amino;each R.sup.2 is lower alkyl; andR.sup.3 is a group selected from Formulae (a), (b), (c) and (d): ##STR2## in which u is 0 or 1;z is 1, 2 or 3; andR.sup.4 is C.sub.1-7 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl-C.sub.1-2 alkyl, or a group (CH.sub.2).sub.t R.sup.5 where t is 1 or 2 and R.sup.5 is thienyl, pyrrolyl, or furyl, each optionally further substituted by one or two substituents selected from C.sub.1-6 alkyl, C.sub.1-6 alkoxy, trifluoromethyl or halogen, or is phenyl optionally substituted by one or two substituents selected from C.sub.1-4 alkoxy, trifluoromethyl, halogen, nitro, carboxy, esterified carboxy, and C.sub.1-4 alkyl optionally substituted by hydroxy, C.sub.1-4 alkoxy, carboxy, esterified carboxy or in vivo hydrolyzable acyloxy; and the pharmaceutically acceptable salts, individual isomers, mixtures of isomers, processes for preparation, compositions, and methods of use thereof.
摘要翻译：本发明涉及式I的5-HT 3受体拮抗剂化合物：其中虚线表示任选的双键; n为1,2或3; p为0,1,2或3; q是0,1或2; 每个R 1独立地选自卤素，羟基，低级烷氧基，低级烷基，硝基，氨基，氨基羰基，（低级烷基）氨基，二（低级烷基）氨基和（低级烷酰基）氨基; 每个R 2是低级烷基; （a），（b），（c）和（d）所示的基团：其中，（a），（c）你是0或1; z为1,2或3; 和R 4是C 1-7烷基，C 3-8环烷基，C 3-8环烷基-C 1-2烷基或基团（CH 2）t R 5，其中t是1或2，R 5是噻吩基，吡咯基或呋喃基，选自C 1-6烷基，C 1-6烷氧基，三氟甲基或卤素的一个或两个取代基，或被任选被一个或两个选自C 1-4烷氧基，三氟甲基，卤素，硝基，羧基，酯化羧基的取代基取代的苯基和任选被羟基，C 1-4烷氧基，羧基，酯化羧基或体内可水解酰氧基取代的C 1-4烷基; 和其药学上可接受的盐，各异构体，异构体的混合物，制备方法，组合物及其使用方法。

4. 发明授权

US4957914A 1,9-alkano-bridged-2,3,4,5-tetrahydro-1H-3-benzazepines 失效
标题翻译： 1,9-链烷基-2,3,4,5-四氢-1H-3-苯并氮杂
公开(公告)号：US4957914A
公开(公告)日：1990-09-18
申请号：US231818
申请日：1988-08-12
申请人： Robin D. Clark , Jacob Berger , Klaus K. Weinhardt
发明人： Robin D. Clark , Jacob Berger , Klaus K. Weinhardt
IPC分类号： C07D223/14 , C07D223/32
CPC分类号： C07D223/32 , C07D223/14
摘要： 1,9-Alkano-bridged-2,3,4,5-tetrahydro-1H-3-benzazepines and the derivatives thereof, i.e., the compounds of Formula I: ##STR1## wherein: R is selected from the group consisting of: hydrogen, cyano, lower alkyl, lower alkenyl, and aralkyl;each of R.sup.1, R.sup.2 and R.sup.3 is independently selected from the group consisting of: hydrogen, hydroxy, halo, trifluoromethyl, nitro, amido, lower alkoxy, lower alkyl, and lower alkylthio; andY is lower alkylene having from two to four carbon atoms;and the pharmaceutically acceptable salts thereof, are useful as CNS agents, e.g., as antidepressants, anxiolytics and antihypertensives, and/or as precursors thereto.
摘要翻译： 1,9-烷基桥-2,3,4,5-四氢-1H-3-苯并吖庚因及其衍生物，即式I化合物：其中：R选自由氢，氰基，低级烷基，低级烯基和芳烷基组成的基团; R 1，R 2和R 3各自独立地选自：氢，羟基，卤素，三氟甲基，硝基，酰氨基，低级烷氧基，低级烷基和低级烷硫基; Y是具有2至4个碳原子的低级亚烷基; 和其药学上可接受的盐可用作CNS剂，例如作为抗抑郁药，抗焦虑药和抗高血压药，和/或作为其前体。

5. 发明授权

US5739336A 1,3,8-triaza- and 3,8-diaza-1-oxaspiro �4,5! decane derivatives 失效
标题翻译： 1,3,8-三氮杂 - 和3,8-二氮杂-1-氧杂螺[4,5]癸烷衍生物
公开(公告)号：US5739336A
公开(公告)日：1998-04-14
申请号：US667247
申请日：1996-06-20
申请人： Klaus K. Weinhardt , Jacob Berger , David S. Carter , Lee A. Flippin
发明人： Klaus K. Weinhardt , Jacob Berger , David S. Carter , Lee A. Flippin
IPC分类号： C07D471/10 , C07D498/10 , A61K31/395
CPC分类号： C07D471/10
摘要： Heterocyclic compounds of Formula I: ##STR1## in which n is 2, 3, 4, 5 or 6; t is 1, 2, 3 or 4; u is 0 or 1 (provided that t is not 1 when u is 0); X is O or N(R.sup.4); Y and Z are independently C(O), C(S) or CH.sub.2 (provided that Y and Z are not both CH.sub.2); R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are as defined in the specification; and their pharmaceutically acceptable salts and N-oxides, formulations containing them, their uses as therapeutic agents, and their synthesis.
摘要翻译：式I的杂环化合物：其中n为2,3,4,5或6; t为1,2,3或4; u为0或1（假设当u为0时t不为1）; X是O或N（R4）; Y和Z独立地为C（O），C（S）或CH 2（条件是Y和Z不同时为CH 2）; R1，R2，R3和R4如说明书中所定义; 及其药学上可接受的盐和N-氧化物，含有它们的制剂，它们作为治疗剂的用途及其合成。

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