发明申请
WO2017053216A2 4'-SUBSTITUTED NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS AND PREPARATIONS THEREOF
审中-公开
基本信息:
- 专利标题： 4'-SUBSTITUTED NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS AND PREPARATIONS THEREOF
- 专利标题（中）：4'-取代的核苷酸逆转录酶抑制剂及其制备
- 申请号：PCT/US2016/052409 申请日：2016-09-19
- 公开(公告)号：WO2017053216A2 公开(公告)日：2017-03-30
- 发明人： GIRIJAVALLABHAN, Vinay, M. , MCLAUGHLIN, Mark , CLEATOR, Edward , KONG, Jongrock , GIBSON, Andrew William , LIEBERMAN, David, R. , DIEGUEZ VAZQUEZ, Alejandro , KEEN, Stephen Philip , WILLIAMS, Michael, J. , MOORE, Jeffrey, C. , MILCZEK, Erika, M. , PENG, Feng , BELYK, Kevin, M. , SONG, Zhiguo Jake
- 申请人： MERCK SHARP & DOHME CORP. , MERCK SHARP & DOHME LIMITED , GIRIJAVALLABHAN, Vinay, M. , MCLAUGHLIN, Mark , CLEATOR, Edward , KONG, Jongrock , GIBSON, Andrew William , LIEBERMAN, David, R. , DIEGUEZ VAZQUEZ, Alejandro , KEEN, Stephen Philip , WILLIAMS, Michael, J. , MOORE, Jeffrey, C. , MILCZEK, Erika, M. , PENG, Feng , BELYK, Kevin, M. , SONG, Zhiguo Jake
- 申请人地址： 126 East Lincoln Avenue Rahway, New Jersey 07065-0907 US
- 专利权人： MERCK SHARP & DOHME CORP.,MERCK SHARP & DOHME LIMITED,GIRIJAVALLABHAN, Vinay, M.,MCLAUGHLIN, Mark,CLEATOR, Edward,KONG, Jongrock,GIBSON, Andrew William,LIEBERMAN, David, R.,DIEGUEZ VAZQUEZ, Alejandro,KEEN, Stephen Philip,WILLIAMS, Michael, J.,MOORE, Jeffrey, C.,MILCZEK, Erika, M.,PENG, Feng,BELYK, Kevin, M.,SONG, Zhiguo Jake
- 当前专利权人： MERCK SHARP & DOHME CORP.,MERCK SHARP & DOHME LIMITED,GIRIJAVALLABHAN, Vinay, M.,MCLAUGHLIN, Mark,CLEATOR, Edward,KONG, Jongrock,GIBSON, Andrew William,LIEBERMAN, David, R.,DIEGUEZ VAZQUEZ, Alejandro,KEEN, Stephen Philip,WILLIAMS, Michael, J.,MOORE, Jeffrey, C.,MILCZEK, Erika, M.,PENG, Feng,BELYK, Kevin, M.,SONG, Zhiguo Jake
- 当前专利权人地址： 126 East Lincoln Avenue Rahway, New Jersey 07065-0907 US
- 代理机构： MERCK SHARP & DOHME CORP.
- 优先权： US62/222,304 20150923; US62/302,452 20160302
- 主分类号： A61K31/7064
- IPC分类号： A61K31/7064 ; C07H19/14
摘要：
The present invention is directed to 4'-substituted nucleoside derivatives of Formula (I) and their use in the inhibition of HIV reverse transcriptase, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS and/or ARC. The present invention also provides processes for the preparation of 4'-substituted nucleoside derivatives of Formula (I) and derivatives thereof.
摘要（中）：
本发明涉及式（I）的4'-取代的核苷衍生物及其在抑制HIV逆转录酶中的用途，HIV的感染预防，HIV感染的治疗以及预防，治疗和延迟 在AIDS和/或ARC的发病或进展中。 本发明还提供制备式（I）的4'-取代的核苷衍生物及其衍生物的方法。
IPC结构图谱:
| A | 人类生活必需 |
| --A61 | 医学或兽医学；卫生学 |
| ----A61K | 医用、牙科用或梳妆用的配制品 |
| ------A61K31/00 | 含有机有效成分的医药配制品 |
| --------A61K31/70 | .碳水化合物；糖；其衍生物 |
| ----------A61K31/7028 | ..含有通过配糖键与非糖化合物连接的糖基的化合物 |
| ------------A61K31/7052 | ...含有氮作为环杂原子的，例如核苷、核苷酸 |
| --------------A61K31/706 | ....含有氮作为环杂原子的六元环的 |
| ----------------A61K31/7064 | .....含有稠合或非稠合的嘧啶的 |