发明申请
WO2015157483A1 TRITERPENOIDS WITH HIV MATURATION INHIBITORY ACTIVITY, SUBSTITUTED IN POSITION 3 BY A NON-AROMATIC RING CARRYING A HALOALKYL SUBSTITUENT
审中-公开
基本信息:
- 专利标题： TRITERPENOIDS WITH HIV MATURATION INHIBITORY ACTIVITY, SUBSTITUTED IN POSITION 3 BY A NON-AROMATIC RING CARRYING A HALOALKYL SUBSTITUENT
- 专利标题（中）：具有HIV成熟活性的TRITERPENOIDS，通过携带HALOALKYL替代物的非芳香环取代位置3
- 申请号：PCT/US2015/025029 申请日：2015-04-09
- 公开(公告)号：WO2015157483A1 公开(公告)日：2015-10-15
- 发明人： SIT, Sing-Yuen , CHEN, Yan , CHEN, Jie , SWIDORSKI, Jacob , VENABLES, Brian Lee , SIN, Ny , MEANWELL, Nicholas A. , REGUEIRO-REN, Alicia , HARTZ, Richard A. , XU, Li , LIU, Zheng
- 申请人： BRISTOL-MYERS SQUIBB COMPANY
- 申请人地址： Route 206 and Province Line Road Princeton, New Jersey 08543 US
- 专利权人： BRISTOL-MYERS SQUIBB COMPANY
- 当前专利权人： BRISTOL-MYERS SQUIBB COMPANY
- 当前专利权人地址： Route 206 and Province Line Road Princeton, New Jersey 08543 US
- 代理机构： LEVIS, John F. et al.
- 优先权： US61/978,306 20140411
- 主分类号： C07J63/00
- IPC分类号： C07J63/00 ; A61K31/58 ; A61K31/56 ; A61P31/18 ; C07F5/02 ; C07C309/65
摘要：
Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formula I: with X selected from C 4-8 cycloalkyl, C 4-8 cycloalkenyl, C 4-9 spirocycloalkyl, C 4-9 spirocycloalkenyl, C 4-8 oxacycloalkyl, C 4-8 dioxacycloalkyl, C 6-8 oxacycloalkenyl, C 6-8 dioxacycloalkenyl, C 6 cyclodialkenyl, C 6 oxacyclodialkenyl, C 6-9 oxaspirocycloalkyl and C 6-9 oxaspirocycloalkenyl ring, such that X is substituted with A, wherein A is -C 1-6 alkyl- halo. These compounds are useful for the treatment of HIV and AIDS.
摘要（中）：
阐述了具有药物和生物影响特性的化合物，其药物组合物和使用方法。 特别地，具有独特抗病毒活性的三萜类化合物作为HIV成熟抑制剂提供，如式I化合物所示：X选自C 4-8环烷基，C 4-8环烯基，C 4-9螺环烷基，C 4-9螺环烯基，C 4 - 8个氧杂环烷基，C4-8二氧杂环烷基，C6-8氧杂环烯基，C6-8二氧杂环烯基，C6环二烯基，C6氧杂环辛烯基，C6-9氧杂螺环烷基和C6-9氧杂环烯烯基环，使得X被A取代，其中A是-C1-6 烷基卤。 这些化合物可用于治疗艾滋病毒和艾滋病。