公开(公告)号：US5468750A

公开(公告)日：1995-11-21

申请号：US273943

申请日：1994-07-12

申请人： Andre Bachy ,  Laurent Fraisse ,  Peter Keane ,  Etienne Mendes ,  Jean-Claude Vernieres ,  Jacques Simiand

发明人： Andre Bachy ,  Laurent Fraisse ,  Peter Keane ,  Etienne Mendes ,  Jean-Claude Vernieres ,  Jacques Simiand

IPC分类号： A61K31/435 ,  A61P3/00 ,  A61P3/08 ,  C07D471/04 ,  C07D471/14 ,  C07D495/04 ,  C07D495/14 ,  A61K31/44 ,  A61K31/495

CPC分类号： C07D471/04 ,  C07D471/14 ,  C07D495/04 ,  C07D495/14

摘要： A compound of formula ##STR1## in which A represents S;R.sub.1 is selected from the group consisting of OH, (C.sub.1 -C.sub.12)alkyl, (C.sub.1 -C.sub.12)alkoxy, benzyloxy, phenyl, benzyl (C.sub.1 -C.sub.4)alkyl NZ.sub.1 Z.sub.2, and NZ.sub.1 Z.sub.2 ;R.sub.2 is selected from the group consisting of OH, SH, (C.sub.1 -C.sub.4)alkoxy, (C.sub.1 -C.sub.4)alkylthio, and NZ.sub.1 Z.sub.2 ;R.sub.3 is selected from the group consisting of H, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkylthio, (C.sub.1 -C.sub.4)alkoxy, phenyl, and benzyl;B is selected from the group consisting of phenyl; pyridyl; phenyl substituted by one or more groups selected from halo, (C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkoxy, CF.sub.3, CH.sub.2 NZ.sub.1 Z.sub.2, and NZ.sub.1 Z.sub.2 wherein Z.sub.1 and Z.sub.2 are selected, independently of each other, from the group consisting of H, (C.sub.1 -C.sub.6)alkyl, formyl, and benzyl or --NZ.sub.1 Z.sub.2 is selected from the group consisting of pyrrolidinyl, piperidinyl, morpholino, hexahydroazepino, ##STR2## piperazino, piperazino substituted in position 4 by (C.sub.1 -C.sub.8)alkyl, benzyl or diphenylmethyl; and pyridyl substituted by one or more groups selected from halo, (C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkoxy, CF.sub.3, CH.sub.2 NZ.sub.1 Z.sub.2, and NZ.sub.1 Z.sub.2 wherein Z.sub.1 and Z.sub.2 are selected, independently of each other, from the group consisting of H, (C.sub.1 -C.sub.6)alkyl, formyl, and benzyl, or NZ.sub.1 Z.sub.2 is selected from the group consisting of pyrrolidinyl, piperidinyl, morpholino, hyxahydroazepino, ##STR3## piperazino, and piperazino substituted in position 4 by (C.sub.1 -C.sub.8)alkyl, benzyl or diphenylmethyl; or its salt with an acid or a base.

摘要翻译： 其中A表示S的式（Ⅰ）化合物; R1选自OH，（C1-C12）烷基，（C1-C12）烷氧基，苄氧基，苯基，苄基（C1-C4）烷基NZ1Z2和NZ1Z2; R2选自OH，SH，（C1-C4）烷氧基，（C1-C4）烷硫基和NZ1Z2; R 3选自H，（C 1 -C 4）烷基，（C 1 -C 4）烷硫基，（C 1 -C 4）烷氧基，苯基和苄基; B选自苯基; 吡啶基 被选自卤素，（C1-C6）烷基，（C1-C6）烷氧基，CF3，CH2NZ1Z2和NZ1Z2中的一个或多个基团取代的苯基，其中Z1和Z2彼此独立地选自H， （C 1 -C 6）烷基，甲酰基和苄基或-NZ 1 Z 2选自吡咯烷基，哌啶基，吗啉代，六氢氮杂环庚烷，哌嗪子基，哌嗪基，其在第4位被（C 1 -C 8）烷基取代，苄基或二苯基甲基 ; 和被一个或多个选自卤素，（C 1 -C 6）烷基，（C 1 -C 6）烷氧基，CF 3，CH 2 NZ 1 Z 2和NZ 1 Z 2的基团取代的吡啶基，其中Z 1和Z 2彼此独立地选自H ，（C 1 -C 6）烷基，甲酰基和苄基，或NZ 1 Z 2选自吡咯烷基，哌啶基，吗啉代，杂环吖庚因，哌嗪子基和在位置4上被（C 1 -C 8）烷基取代的哌嗪基，苄基 或二苯基甲基; 或其与酸或碱的盐。

公开(公告)号：US5360799A

公开(公告)日：1994-11-01

申请号：US109073

申请日：1993-08-19

申请人： Andre Bachy ,  Laurent Fraisse ,  Peter Keane ,  Etienne Mendes ,  Jean-Claude Vernieres ,  Jacques Simiand

发明人： Andre Bachy ,  Laurent Fraisse ,  Peter Keane ,  Etienne Mendes ,  Jean-Claude Vernieres ,  Jacques Simiand

IPC分类号： A61K31/435 ,  A61P3/00 ,  A61P3/08 ,  C07D471/04 ,  C07D471/14 ,  C07D495/04 ,  C07D495/14 ,  A61K31/44 ,  A61K31/55 ,  C07D413/14

CPC分类号： C07D471/04 ,  C07D471/14 ,  C07D495/04 ,  C07D495/14

摘要： Compounds of formula ##STR1## in which R.sub.1 represents OH, (C.sub.1 -C.sub.12)alkyl, (C.sub.1 -C.sub.12)alkoxy, benzyloxy, benzyl, phenyl, (C.sub.1 -C.sub.4)alkylNZ.sub.1 Z.sub.2 or NZ.sub.1 Z.sub.2 ; R.sub.2 represents OH, SH, (C.sub.1 -C.sub.4)alkoxy, (C.sub.1 -C.sub.4)alkylthio or NZ.sub.1 Z.sub.2 ; R.sub.3 represents H, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkylthio, (C.sub.1 -C.sub.4)alkoxy, phenyl or benzyl; A represents N and R represents H or (C.sub.1 -C.sub.4)alkyl which can be substituted by phenyl or NZ.sub.1 Z.sub.2 ; B represents phenyl which is coupled to the pyridyl ring and is optionally substituted by one or more groups chosen from halo, (C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkoxy, CF.sub.3, CH.sub.2 NZ.sub.1 Z.sub.2 or NZ.sub.1 Z.sub.2 ; and Z.sub.1 and Z.sub.2 represent, independently of each other, H, (C.sub.1 -C.sub.6) alkyl, formyl or benzyl, or they form with the nitrogen atom to which they are attached an optionally substituted saturated heterocycle and their salts.

摘要翻译： 其中R 1表示OH，（C 1 -C 12）烷基，（C 1 -C 12）烷氧基，苄氧基，苄基，苯基，（C 1 -C 4）烷基NZ 1 Z 2或NZ 1 Z 2的式I化合物; R2代表OH，SH，（C1-C4）烷氧基，（C1-C4）烷硫基或NZ1Z2; R3表示H，（C1-C4）烷基，（C1-C4）烷硫基，（C1-C4）烷氧基，苯基或苄基; A表示N，R表示H或可被苯基或NZ1Z2取代的（C1-C4）烷基; B表示与吡啶基环偶联并且任选被一个或多个选自卤素，（C 1 -C 6）烷基，（C 1 -C 6）烷氧基，CF 3，CH 2 NZ 1 Z 2或NZ 1 Z 2的基团取代的苯基; 并且Z 1和Z 2彼此独立地表示H，（C 1 -C 6）烷基，甲酰基或苄基，或者与它们所连接的氮原子一起形成任选取代的饱和杂环及其盐。

公开(公告)号：US5026711A

公开(公告)日：1991-06-25

申请号：US362105

申请日：1989-06-06

申请人： Etienne Mendes ,  Jean-Claude Vernieres ,  Peter E. Keane ,  Andre Bachy

发明人： Etienne Mendes ,  Jean-Claude Vernieres ,  Peter E. Keane ,  Andre Bachy

IPC分类号： A61K31/435 ,  A61K31/47 ,  A61P9/08 ,  A61P9/10 ,  A61P25/20 ,  A61P31/04 ,  A61P37/00 ,  A61P37/08 ,  C07D215/42 ,  C07D215/54 ,  C07D215/60 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06 ,  C07D471/04 ,  C07D491/04 ,  C07D491/056 ,  C07D491/147

CPC分类号： C07D401/06 ,  C07D215/42 ,  C07D215/54 ,  C07D215/60 ,  C07D471/04 ,  C07D491/04

摘要： Compounds represented by the general formula: ##STR1## in which R.sub.1 and R.sub.2 are selected from hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkenyl , phenyl or benzyl or R.sub.1 and R.sub.2 form together with the nitrogen atom to which they are attached a C.sub.4 -C.sub.8 saturated heterocycle, R.sub.3 is selected from hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl or C.sub.7 -C.sub.9 phenyl-alkyl, R.sub.4 is selected from hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.5 and R.sub.6 are selected from hydrogen or halogen, C.sub.1 -C.sub.3 or alkoxy, nitro or trifluoromethyl; Z is selected from OH, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.4 alkyl, benzyl, C.sub.4 -C.sub.6 aryl with or without a heteroatom, or NR.sub.8 R.sub.9, R.sub.8 and R.sub.9 being selected from hydrogen, C.sub.1 -C.sub.4 alkyl, phenyl or benzyl; R.sub.10 is selected from hydrogen, C.sub.1 -C.sub.4 alkyl or phenyl; n is 0, 1 or 3, p is 0 or 1 and one of the symbols A, B, C, D represents N and the others CH or A, B, C, D all represent CH and their acid addition salts, and their salts with bases. The compounds are useful in the prevention and treatment of cardiovascular diseases, as anti-allergic drugs, in the prevention and treatment of infectious states, and for the treatment of anxiety.

摘要翻译： 由以下通式表示的化合物：其中R 1和R 2选自氢，C 1 -C 6烷基或C 2 -C 6烯基，苯基或苄基或R 1和R 2与它们所连接的氮原子一起形成C4 -C8饱和杂环，R3选自氢，C1-C6烷基，苯基或C7-C9苯基 - 烷基，R4选自氢或C1-C4烷基，R5和R6选自氢或卤素，C1-C3或 烷氧基，硝基或三氟甲基; Z选自OH，C 1 -C 6烷氧基，C 1 -C 4烷基，苄基，具有或不具有杂原子的C 4 -C 6芳基，或NR 8 R 9，R 8和R 9选自氢，C 1 -C 4烷基，苯基或苄基; R 10选自氢，C 1 -C 4烷基或苯基; n为0,1或3，p为0或1，符号A，B，C，D中的一个为N，其余CH或A，B，C，D全部为CH及其酸加成盐， 与碱的盐。 该化合物可用于预防和治疗心血管疾病，作为抗过敏药物，预防和治疗感染状态以及治疗焦虑症。