| 主权项 |
1. 一种式(I)化合物: 式中 A@su1为N-R@su1或CHR@su1; A@su4为N-R@su4; R@su2为CH@ss2CO@ss2R'、H、C@ss1@ss-@ss4烷基、CONR' R"、(CH@ss2)@ss1@ss-@ss4OH; R@su1及R@su4为H、C@ss1@ss-@ss4烷基、Ar-C@ss1@ss-@ ss4烷基或C@ss3@ss-@ss6环烷基-C@ss1@ss-@ss4烷基; R'及R"为H或C@ss1@ss-@ss4烷基;R@su6为 R@ss2N(CH@ss2)@ss1@ss-@ss5NHCO-,(R=H,CH@ss3,或 其医药上可接受之盐。2. 根据申请专利范围第1项 之化合物,其系选自一列任一 者: (R,S)-8-[[[4-(胺亚胺甲基)苯基]胺基]羰基]-2, 3,4,5-四氢-4-(2-苯乙基)-1H-1,4-苯并二氮七圜-2- 乙酸; (R,S)-7- [[4-(胺亚胺甲基)苯醯基]甲胺基]-2,3, 4,5-四氢-1-甲-3-氧-4-(2-苯乙基)-1H-1,4-苯并二氮 七圜-2-乙酸; (R,S)-2,3,4,5-四氢-3-氧-4-(2-苯乙基)-8-[[[2- (4- 啶基)乙基]胺基]羰基]-1H-1,4-苯并二氮七圜- 2-乙酸; (R,S)-2,3,4,5-四氢-3-氧-4-(2-苯乙基)-8-[[[2- (2- 啶基)乙基]胺基]羰基]-1H-1,4-苯并二氮七圜- 2-乙酸; (R,S)-8-[[(5-胺戊基)胺基]羰基]-2,3,4,5-四氢 -3-氧-4-(2-苯乙基)-1H-1,4-苯并二氮七圜-2-乙酸; (R,S)-8-[[[4-(丙基)胺甲基]苯基]胺基]羰基]-2 ,3,4,5-四氢-3-氧-4-(2-苯乙基)-1H-1,4-苯并二氮 七圜-2-乙酸; (R,S)-8[[[[3-(胺甲基)苯基]甲基]胺基]羰基]- 2,3,4,5-四氢-3-氧-4-(2-苯乙基)-1H-,4-苯并二氮 七圜-2-乙酸; (R,S)-8-[[[3-[4-[六氢 啶基]丙基]胺基]羰基 ]-2,3,4,5-四氢-3-氧-4-(2-苯乙基)-1H-1,4-苯并 二氮七圜-2-乙酸; (R,S)-2,3,4,5-四氢-3-氧-4-(2-苯乙基)-8-[[[4- ( 啶基)甲基]胺基]羰基]-1H-1,4-苯并二氮七圜-2- 乙酸; (R,S)-2,3,4,5-四氢-3-氧-4-(2-苯乙基)-8-[[[4- (3- 啶基)丁基]甲胺基]羰基]-1H-1,4-苯并二氮七 圜-2-乙酸; (R,S)-2,3,4,5-四氢-8-[[[2-(1H-咪唑-1-基)乙基 ]胺基]羰基]-3-氧-4-(2-苯乙基)-1H-1,4-苯并二氮 七圜-2-乙酸; (R,S)-2,3,4,5-四氢-8-[[[3-(1H-咪唑-1-基)丙基 ]胺基]羰基]-3-氧-4-(2-苯乙基)-1H-1,4-苯并二氮 七圜-2-乙酸; (R,S)-8-[[[6-胺己基)胺基]羰基]-2,3,4,5-四 氢-3-氧-4-(2-苯乙基)-1H-1,4-苯并二氮七圜-2-乙酸; (R,S)-8-[[[6-胺丁基)胺基]羰基]-2,3,4,5-四 氢-3-氧-4-(2-苯乙基)-1H-1,4-苯并二氮七圜-2-乙酸; (R,S)-2,3,4,5-四氢-8-[[[2-(1H-咪唑-4-基)乙基 ]胺基]羰基]-3-氧-4-(2-苯乙基)-1H-1,4-苯并二氮 七圜-2-乙酸; (R,S)-2,3,4,5-四氢-8-[[[2-(1-甲-1H咪唑-5-基) 乙基]胺基]羰基]-3-氧-4-(2-苯乙基)-1H-1,4-苯并 二氮七圜-2-乙酸; (R,S)-7-[[[4-胺甲基)苯基]羰基]胺基]-2,3,4 ,5-四氢-1-甲-3-氧-4-(2-苯乙基)-1H-1,4-苯并二氮七 圜-2-乙酸; (R,S)-8-[[[2-(4- 啶基)乙基]甲胺基]羰基]-2, 3,4,5-四氢-3-氧-4-(2-苯乙基)-1H-1,4-苯并二氮七 圜-2-乙酸; (R,S)-8-[[2-[4-[1-(甲基) 锭]乙基]甲胺基]羰 基]-4-[2-苯乙基)-2,3,4,5-四氢-3-氧-4-(2-苯乙 基)-1H-1,4-苯并二氮七圜-2-乙酸酯氢碘酸盐; (R,S)-2,3,4,5,-四氢-3-氧-4-[2-(环己基)乙基]- 8-[[[2-(1-甲-4-六氢 啶基)乙基]甲胺基]羰基]- 1H-1,4-苯并二氮七圜-2-乙酸; (R,S)-2,3,4,5-四氢-3-氧-4-(2-苯乙基-8-[[[2-( 1-甲-4-六氢 啶基)乙基]甲胺基]羰基]-1H-1,4-苯 并二氮七圜-2-乙酸; (S-(R,S)]-8-[[[4-[N-(丙胺醯)胺甲基]苯基]胺 基]羰基]-2,3,4,5,-四氢-3-氧-4-(2-苯乙基)-1H- 1,4-苯并二氮七圜-2-乙酸; 8-[[4-(胺亚胺甲基)苯醯]胺基]-4,5-二氢-2-甲-3- 氧-4-(2-苯乙基)-3H-1,4-苯并二氮七圜; (R,S)-8-[[[4-(胺亚胺甲基)苯基]甲胺基]羰基]-2 ,3,4,5-四氢-2-甲-3-氧-4-(2-苯乙基)-1H-1,4-苯并 二氮七圜; (R,S)-8-[[[[4-(胺亚胺甲基)苯基]甲胺基]羰基] -2,3,4,5-四氢-3-氧-4-(2-苯乙基)-1H-1,4-苯并二 氮七圜-2-乙酸乙酯; (R,S)-[[8-[4-(胺亚胺甲基)苯基]甲胺基]羰基]-2 ,3,4,5-四氢-3-氧-4-(2-苯乙基)-1H-1,4-苯并二氮 七圜-2-乙醯胺; (R,S)-8-[[[4-(胺亚胺甲基)苯基]甲胺基]羰基]-2 ,3,4,5-四氢-3-氧-4-(2-苯乙基)-1H-1,4-苯并二氮 七圜-2-乙醇; (R,S)-8-[2-[4-(胺甲基)苯基]乙基]-2,3,4,5-四 氢-3-氧-4-(2-苯乙基)-1H-1,4-苯并二氮七圜-2-乙酸; 7-[3-(4- 啶基)丙氧基-2-(2-苯乙基)-3-氧-2,3,4, 5-四氢-1H-2-苯并一氮七圜-4-乙酸; 7-[3(4-六氢 啶基)丙氧基]-2-(2-苯乙基)-3-氧-2,3 ,4,5-四氢-1H-2-苯并一氮七圜-4-乙酸; (R,S)-8-[[[3-(胺甲基)苯基]胺基]羰基]-2,3,4 ,5-四氢-3-氧-4-(2-苯乙基)-1H-1,4-苯并二氮七圜-2- 乙酸; 8-[1-[4-(4- 啶基)六氢 基]羰基]-2,3,4,5- 四氢-3-氧-4-(2-苯乙基)-1H-1,4-苯并二氮七圜-2-乙酸 ; (R,S)-8-[[[4-(胺甲基)-3-氯-苯基]羰基]胺基]-2 ,3,4,5-四氢-3-氧-4-(2-苯乙基)-1H-1,4-苯并二氮 七圜-2-乙酸; 2-[3-(4-六氢 啶基)丙氧基]-7-氧-6,7,8,9-四氢-5H- 苯并环庚烯-6-乙酸; 3-[3-(4-六氢 啶基)丙氧基]-7-氧-6,7,8,9-四氢-5H- 苯并环庚烯-6-乙酸;或 (R,S)-8-[[[2-[4-(2-胺 啶基)乙基]胺基]羰基] -2,3,4,5-四氢-3-氧-4-(2-苯乙基)-1H-1,4-苯并二氮七 圜-2-乙酸。3. 根据申请专利范围第1项之化合物, 其系选自一列任一 者: (R,S)-8-[[[4-(胺亚胺甲基)苯基]甲胺基]羰基]-2 ,3,4,5-四氢-1-甲-3-氧-4-(2-苯乙基)-1H-1,4-苯并二氮 七圜-2-乙酸; (R,S)-2,3,4,5-四氢-3-氧-4-(2-苯乙基)-8-[[[2-(1- 六氢 基)乙基]胺基]羰基]-1H-1,4-苯并二氮七圜- 2-乙酸; (R,S)-2,3,4,5-四氢-3-氧-4-(2-苯乙基)-8-[[[2-(4- 六氢 啶基)乙基]胺基]羰基]-1H-1,4-苯并二氮七圜- 2-乙酸; (R,S)-7-[[[4-(胺亚胺甲基)苯基]甲胺基]羰基]-2 ,3,4,5-四氢-3-氧-2-(2-苯乙基)-1H-2-苯并一氮七圜-4- 乙酸; (R,S)-8-[[[(4-胺亚胺甲基)苯基]甲胺基]羰基]-2 ,3,4,5-四氢-3-氧-1H-1,4-苯并二氮七圜-2-乙酸; (R,S)-8-[[[4-(胺亚胺甲基)苯基]甲胺基]羰基]-2 ,3,4,5-四氢-4-甲-3-氧-1H-1,4-苯并二氮七圜-2-乙酸; (R,S)-2,3,4,5-四氢-3-氧-4-(2-苯乙基)-8-[[[2-(1- 六氢 基)乙基]甲胺基]羰基]-1H-1,4-苯并二氮七 圜-2-乙酸; (R,S)-2,3,4,5-四氢-3-氧-4-(2-苯乙基)-8-[[[2-(4- 六氢 啶基)乙基]甲胺基]羰基]-1H-1,4-苯并二氮七 圜-2-乙酸;或 (R,S)-2,3,4,5-四氢-3-氧-4-(2-(环己基)乙基]-8-[[ [2-(4-六氢 啶基)乙基]甲胺基]羰基]-1H-1,4-苯并 二氮七圜-2-乙酸。4. 根据申请专利范围第1项之化 合物,其系选自一列任一 者: (R,S)-8-[[[4-(胺甲基)苯基]甲胺基]羰基]-2,3,4 ,5-四氢-3-氧-4-(2-苯乙基)-1H-1,4-苯并二氮七圜-2-乙 酸; (R,S)-2,3,4,5-四氢-8-[[[2-[1-甲-1,2,5,6-四氢 啶-4-基]乙基]甲胺基]羰基]-3-氧-4-(2-苯乙基)-1H -1,4-苯并二氮七圜-2-乙酸; (R,S)-2,3,4,5-四氢-3-氧-4-(2-苯乙基)-8-[4-(六氢 啶-4-基)-1-(E)-丁烯基]-1H-1,4-苯并二氮七圜-2-乙酸 ; (R,S)-2,3,4,5-四氢-3-氧-2-(环己乙基)-7-[[[2-(六 氢 啶-4-基)乙基]甲胺基]羰基-1H-2-苯并一氮七圜-4 -乙酸;及 (R,S)-2,3,4,5-四氢-3-氧-4-(2-苯乙基)-8-[4-(六氢 啶-4-基)丁基」-1H-1, 4-苯并二氮七圜-2-乙酸; (R,S)-2,3,4,5-四氢-3-氧-4-(2-苯乙基)-7-[[4-( 啶 -4-基)六氢 -1-基]羰基]-1H-1,4-苯并二氮七圜-2-乙 酸; (R,S)-2,3,4,5-四氢-3-氧-7-[[[2-(六氢 啶-4-基) 乙基]甲胺基]羰基]]-1H-2-苯并一氮七圜-2-乙酸; (R,S)-2,3,4,5-四氢-3-氧-2-(2-苯乙基)-7-[[[2-(六 氢 啶-4-基)乙基]甲胺基]羰基]-1H-2-苯并一氮七圜 -4-乙酸; (R,S)-7-[[[2-[(2-胺基) 啶-3-基]乙基]甲胺基 ]羰基]-2,3,4,5-四氢-3-氧-2-(2-苯乙基)-1H-2-苯并 一氮七圜-2-乙酸; 7-[1-[4-(六氢 -1-基)丁-1-炔基]]-2-(2-苯乙基 )-3-氧-2,3,4,5-四氢-1H-2-苯并一氮七圜-4-乙酸; (R,S)-7-[[[2-(六氢 啶-4-基)乙基]甲胺基]羰基 ]-2,3,4,5-四氢-2-甲-3-氧-1H-2-苯并一氮七圜-4-乙酸 ; (R,S)-7-[[[4-胺甲苯基]甲胺基]羰基]-2,3,4,5- 四氢-3-氧-2-(2-苯乙基)-1H-2-苯并一氮七圜-4-乙酸; (R,S)-8-[[[4-(N,N-二甲胺甲基)苯基]胺基]羰基] -2,3,4,5-四氢-3-氧-4-(2-苯乙基)-1H-1,4-苯并二氮七 圜-2-乙酸; 8-[[[2-(2-胺基 啶-4-基)乙基]甲胺基]羰基]-2, 3,4,5-四氢-3-氧-4-(2-苯乙基)-1H-1,4-苯并二氮七圜-2 -乙酸;或 (R,S)-7-[(4,4'-二六氢 啶-1-基)羰基)-2,3,4,5-四氢 -3-氧-4-(苯乙基)-1H-1,4-苯并二氮七圜-2-乙酸。5. 一 种下式之中间化合物: 式中 E为N或CH, R@su2@su0为氢、胺基、单或二-C@ss1@ss-@ss4烷胺基、 羟基或C@ss1@ss-@ss4烷基, R@sup为氮保护基, L@su2为CHO、CO@ss2R'、C≡C-H、OH、Cl、Br、I、CH@ ss2-T或NR'R",及 T为CF@ss3SO@ss3.OH、NHR"、Cl、Br或I。6. 一种抑制血小 板聚集之医药组合物,其系含根据申请 专利范围第1至4项中任一项之化合物及医药上可 接受之载 剂。7. 根据申请专利范围第1至4项中任一项之化 合物,供用 |
