SLIEESQNQQEKNEQELL ； (4) BAo-β Ala-NNYTSLIHSLIEESQNQQEKNEQELL ； (5) UAo-β Ala-NNYTSLIHSLIEESQNQQEKNEQELL ； (6) OAo-β Ala-NNYTSLIHSLIEESQNQQEKNEQELL ； (7) BApc-β Ala-NNYTSLIHSLIEESQNQQEKNEQELL ； (8) UApc-β Ala-NNYTSLIHSLIEESQNQQEKNEQELL ； (9) OApc-β Ala-NNYTSLIHSLIEESQNQQEKNEQELL ； (10) BApo-β Ala-NNYTSLIHSLIEESQNQQEKNEQELL ； (11) UApo-β Ala-NNYTSLIHSLIEESQNQQEKNEQELL ； (12) OApo-β Ala-NNYTSLIHSLIEESQNQQEKNEQELL ； (13) NNYTSLIHSLIEESQNQQEKNEQELL-K(β Ala-Bac); (14) NNYTSLIHSLIEESQNQQEKNEQELL-K(β Ala-UAc); (15) NNYTSLIHSLIEESQNQQEKNEQELL-K ( β Ala-OAc); (16) NNYTSLIHSLIEESQNQQEKNEQELL-K ( β Ala-BAo); (17) NNYTSLIHSLIEESQNQQEKNEQELL-K(β Ala-UAo); (18) NNYTSLIHSLIEESQNQQEKNEQELL-K(β Ala-OAo); (19) NNYTSLIHSLIEESQNQQEKNEQELL-K(β Ala-BApc); (20) NNYTSLIHSLIEESQNQQEKNEQELL-K(β Ala-UApc); (21) NNYTSLIHSLIEESQNQQEKNEQELL-K ( β Ala-OApc); (22 ) NNYTSLIHSLIEESQNQQEKNEQELL-K ( β Ala-BApo); (23) NNYTSLIHSLIEESQNQQEKNEQELL-K(β Ala-UApo); (24) NNYTSLIHSLIEESQNQQEKNEQELL-K ( β Ala-OApo)； (25) BAc-β Ala-NNYTSLIHSLIEESQNQQEKNEQELL-K(β Ala-BAc); (26) UAc-β Ala-NNYTSLIHSLIEESQNQQEKNEQELL-K(β Ala-UAc); (27) OAc-β Ala-NNYTSLIHSLIEESQNQQEKNEQELL-K(β Ala-OAc); (28) BAo-β Ala-NNYTSLIHSLIEESQNQQEKNEQELL-K(β Ala-BAo); (29) UAo-β Ala-NNYTSLIHSLIEESQNQQEKNEQELL-K(β Ala-UAo); (30) OAo-β Ala-NNYTSLIHSLIEESQNQQEKNEQELL-K(β Ala-OAo); (31) BApc-βAla-NNYTSLIHSLIEESQNQQEKNEQELL-K(^Ala-BApc)； (32) UApc-β Ala-NNYTSLIHSLIEESQNQQEKNEQELL-K(β Ala-UApc); (33 ) OApc-β Ala-NNYTSLIHSLIEESQNQQEKNEQELL-K ( β Ala-OApc); (34) ΒΑρο-βAla-NNYTSLIHSLIEESQNQQEKNEQELL-K(βAla-BApo)； (35 ) UApo-β Ala-NNYTSLIHSLIEESQNQQEKNEQELL-K ( β Ala-UApo); (36) OApo-β Ala-NNYTSLIHSLIEESQNQQEKNEQELL-K(β Ala-OApo); (37) BAc-β Ala-NNYTSLIHSLIEESQNQQEKNEQELL-K(β Ala-BApc); (38 ) UAc-β Ala-NNYTSLIHSLIEESQNQQEKNEQELL-K ( β Ala-UApc); (39) OAc-β Ala-NNYTSLIHSLIEESQNQQEKNEQELL-K(β Ala-OApc); (40) BAo-β Ala-NNYTSLIHSLIEESQNQQEKNEQELL-K(β Ala-BApo); (41) UAo-β Ala-NNYTSLIHSLIEESQNQQEKNEQELL-K(β Ala-UApo); (42) OAo-β Ala-NNYTSLIHSLIEESQNQQEKNEQELL-K(β Ala-OApo); (43) BAc-β Ala-INNYTSLIHSLIEESQNQQEKNEQELL ； (44) UAc-β Ala-INNYTSLIHSLIEESQNQQEKNEQELL ； (45) OAc-β Ala-INNYTSLIHSLIEESQNQQEKNEQELL ； (46) BAo-β Ala-INNYTSLIHSLIEESQNQQEKNEQELL ； (47) UAo-β Ala-INNYTSLIHSLIEESQNQQEKNEQELL ； (48) OAo-β Ala-INNYTSLIHSLIEESQNQQEKNEQELL ； (49) BApc-β Ala-INNYTSLIHSLIEESQNQQEKNEQELL ； (50) UApc-β Ala-INNYTSLIHSLIEESQNQQEKNEQELL ； (51) OApc-β Ala-INNYTSLIHSLIEESQNQQEKNEQELL ； (52) BApo-β Ala-INNYTSLIHSLIEESQNQQEKNEQELL ； (53) UApo-β Ala-INNYTSLIHSLIEESQNQQEKNEQELL ； (54) OApo-β Ala-INNYTSLIHSLIEESQNQQEKNEQELL ； (55) INNYTSLIHSLIEESQNQQEKNEQELL-K(PAla-BAc); (56) INNYTSLIHSLIEESQNQQEKNEQELL-K (PAla-UAc); (57) INNYTSLIHSLIEESQNQQEKNEQELL-K (PAla-OAc); (58 ) INNYTSLIHSLIEESQNQQEKNEQELL-K ( β Ala-BAo); (59 ) INNYTSLIHSLIEESQNQQEKNEQELL-K ( β Ala-UAo); (60) INNYTSLIHSLIEESQNQQEKNEQELL-K(PAla-OAo); (61) INNYTSLIHSLIEESQNQQEKNEQELL-K ( β Ala-BApc); (62) INNYTSLIHSLIEESQNQQEKNEQELL-K (PAla-UApc); (63) INNYTSLIHSLIEESQNQQEKNEQELL-K(PAla-OApc); (64) INNYTSLIHSLIEESQNQQEKNEQELL-K(PAla-BApo); (65) INNYTSLIHSLIEESQNQQEKNEQELL-K(PAla-UApo); (66) INNYTSLIHSLIEESQNQQEKNEQELL-K(PAla-OApo); (67) BAc-β Ala-INNYTSLIHSLIEESQNQQEKNEQELL-K(β Ala-BAc); (68) UAc-β Ala-INNYTSLIHSLIEESQNQQEKNEQELL-K(β Ala-UAc); (69) OAc-β Ala-INNYTSLIHSLIEESQNQQEKNEQELL-K(β Ala-OAc); (70 ) BAo-β Ala-INNYTSLIHSLIEESQNQQEKNEQELL-K ( β Ala-BAo); (71) UAo-βAla-INNYTSLIHSLIEESQNQQEKNEQELL-K(^Ala-UAo)； (72) OAo-β Ala-INNYTSLIHSLIEESQNQQEKNEQELL-K(β Ala-OAo); (73) BApc-β Ala-INNYTSLIHSLIEESQNQQEKNEQELL-K(β Ala-BApc); (74) UApc-βAla-INNYTSLIHSLIEESQNQQEKNEQELL-K(^Ala-UApc)； (75) OApc-β Ala-INNYTSLIHSLIEESQNQQEKNEQELL-K(β Ala-OApc); (76) BApo-β Ala-INNYTSLIHSLIEESQNQQEKNEQELL-K(β Ala-BApo); (77 ) UApo-β Ala-INNYTSLIHSLIEESQNQQEKNEQELL-K ( β Ala-UApo); (78 ) OApo-β Ala-INNYTSLIHSLIEESQNQQEKNEQELL-K ( β Ala-OApo); (79) BAc-β Ala-INNYTSLIHSLIEESQNQQEKNEQELL-K(β Ala-BApc); (80) UAc-β Ala-INNYTSLIHSLIEESQNQQEKNEQELL-K(β Ala-UApc); (81) OAc-β Ala-INNYTSLIHSLIEESQNQQEKNEQELL-K(β Ala-OApc); (82) BAo-β Ala-INNYTSLIHSLIEESQNQQEKNEQELL-K(β Ala-BApo); (83) UAo-β Ala-INNYTSLIHSLIEESQNQQEKNEQELL-K(β Ala-UApo); (84) ΟΑο-β Ala-INNYTSLIHSLIEESQNQQEKNEQELL-K ( ^Ala-Oapo)； 或者上述化合物的衍生物、立体异构体、或可药用盐。
7. -种药物组合物，其含有至少一种权利要求1至6中任一项所述的式I化合物、其衍 生物、其立体异构体、或其可药用盐，以及任选的药学上可接受的辅料。
8. -种HIV融合抑制剂，其含有至少一种权利要求1至6中任一项所述的式I化合物、 其衍生物、其立体异构体、或其可药用盐。
9. 权利要求1至6中任一项所述的式I化合物、其衍生物、其立体异构体、或其可药用 盐在制备HIV融合抑制剂，或者在制备用于治疗和/或预防和/辅助治疗HIV感染相关疾 病尤其是艾滋病的药物中的用途。
10. -种在体内或体外抑制HIV融合的方法，包括使用有效量的权利要求1至6中任一 项所述的式I化合物、其衍生物、其立体异构体、或其可药用盐的步骤。
【专利摘要】本发明属于生物医药领域，涉及一种三萜-多肽缀合物、其药物组合物及用途。具体地，本发明涉及式I所示的缀合物、其衍生物、其立体异构体、或其可药用盐。本发明还涉及含有上述的式I缀合物、其衍生物、其立体异构体、或其可药用盐的药物组合物，以及式I缀合物、其衍生物、其立体异构体、或其可药用盐在治疗或预防HIV感染所致相关疾病尤其是获得性免疫缺陷综合征（AIDS，即艾滋病）的用途。本发明的化合物具有抑制HIV细胞融合例如抑制HIV-1细胞融合的活性。XA1-L1–P–K(L2-XA2)式Ⅰ。
【IPC分类】A61K38-16, C07K14-00, A61P31-18
【公开号】CN104877015
【申请号】CN201410069520
【发明人】刘克良, 王潮, 娜荷芽, 姜喜凤, 许笑宇
【申请人】中国人民解放军军事医学科学院毒物药物研究所
【公开日】2015年9月2日
【申请日】2014年2月28日
【公告号】WO2015127862A1