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1. 发明申请

US20210309671A1 TRICYCLIC HETEROCYCLE COMPOUNDS USEFUL AS HIV INTEGRASE INHIBITORS 有权
公开(公告)号：US20210309671A1
公开(公告)日：2021-10-07
申请号：US17057875
申请日：2019-05-31
申请人： Tao Yu , Alan Whitehead , Yili Chen , Chunrui Sun , Zhiy-ong Hu , Kake Zhao , Ronald M. Kim , John A. McCauley , MERCK SHARP & DOHME CORP.
发明人： Tao YU , Alan WHITEHEAD , Yili CHEN , Chunrui SUN , Zhiyong HU , Kake ZHAO , Ronald M. KIM , John A. McCAULEY
IPC分类号： C07D498/22 , C07D471/16 , C07D491/22 , A61K45/06 , A61P31/18
摘要： The present invention relates to Tricyclic Heterocycle Compounds of Formula (I): (I) and pharmaceutically acceptable salts or prodrug thereof, where-in R1, R2, R3, R4, R5, R6 and n are as defined herein. The present invention also relates to compositions comprising at least one Tricyclic Heterocycle Compound, and methods of using the Tricyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.

2. 发明申请

US20180169072A1 SUBSTITUTED TRIAZOLO BICYCLIC COMPOUNDS AS PDE2 INHIBITORS 审中-公开
公开(公告)号：US20180169072A1
公开(公告)日：2018-06-21
申请号：US15579878
申请日：2016-06-27
申请人： Gregori J. MORRIELLO , Lehua CHANG , Ashley FORSTER , Yili CHEN , Michael P. DWYER , Zack Zhiqiang GUO , Ming WANG , Shimin XU , Yingjian BO , Jianmin FU , MERCK SHARP & DOHME CORP.
发明人： Gregori J. MORRIELLO , Lehua CHANG , Ashley FORSTER , Yili CHEN , Michael P. DWYER , Zack Zhiqiang GUO , Ming WANG , Shimin XU , Yingjian BO , Jianmin FU
IPC分类号： A61K31/4196 , A61K31/52 , A61P25/06 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/28
CPC分类号： A61K31/4196 , A61K31/52 , A61P25/06 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/28 , C07D471/04 , C07D487/04
摘要： The present invention is directed to substituted triazolo bicyclic compounds of formula I which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

3. 发明申请

US20150322056A1 Factor IXa Inhibitors 有权
标题翻译：因子IXa抑制剂
公开(公告)号：US20150322056A1
公开(公告)日：2015-11-12
申请号：US14652237
申请日：2013-12-16
申请人： MERCK SHARP & DOHME CORP. , MOCHIDA PHARMACEUTICAL CO., LTD.
发明人： Cameron James SMITH , John Qiang TAN , Ting ZHANG , James BALKOVEC , William John GREENLEE , Liangqin GUO , Yi-Heng CHEN , Yili CHEN , Jiayi XU , Samuel CHACKALAMANNIL , Tomokazu HIRABAYASHI , Hiroshi NAGASUE , Kouki OGAWA
IPC分类号： C07D413/14 , C07D471/04
CPC分类号： C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D498/04
摘要： The present invention provides a compound of Formula (I) wherein R1 is H or C1-6 alkyl, R2, is H or C1-6 alkyl or CH2OH, R3 is H or C1-6 alkyl, and R4 is H or C1-6 alkyl, provided that when R1, R2, and R3 are H, R4 is C1-6 alkyl, and when R1, R2, and R4 are H, then R3 is C1-6 alkyl, and when R1, R3, and R4 are H, R2 is C1-6 alkyl or —CH2OH, and when R2, R3, and R4 are H, then R1 is C1-6 alkyl; A is 1) a 9-10 membered bicyclic heterocycle having 1-3 heteroatoms independently selected from N, S and O, which 9-10 membered bicyclic heterocycle is unsubstituted or substituted with R5 and unsubstituted or substituted with R6 and unsubstituted or substituted with NH2, or 2) a 6-9 membered monocyclic or bicyclic carbocyclic ring system unsubstituted or substituted with R5, unsubstituted or substituted with R6, and unsubstituted or substituted with —CH2NH2; and B is 1) a 5- or 6-membered monocyclic heterocycle having 1 or 2 heteroatoms independently selected from N, S or O, which is unsubstituted or substituted on a carbon or nitrogen atom with R7, unsubstituted or substituted on a carbon or nitrogen atom with R8, and unsubstituted or substituted on a carbon or nitrogen atom with R9, or 2) an 8- or 9-membered fused bicyclic heterocycle having 1, 2 or 3 nitrogen atoms which is unsubstituted or substituted on a carbon or nitrogen atom with R7, and unsubstituted or substituted on a carbon or nitrogen atom with R8; and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses.
摘要翻译：本发明提供式（I）的化合物，其中R 1为H或C 1-6烷基，R 2为H或C 1-6烷基或CH 2 OH，R 3为H或C 1-6烷基，R 4为H或C 1-6 烷基，条件是当R 1，R 2和R 3为H时，R 4为C 1-6烷基，当R 1，R 2和R 4为H时，R 3为C 1-6烷基，并且当R 1，R 3和R 4为H R 2为C 1-6烷基或-CH 2 OH，当R 2，R 3和R 4为H时，R 1为C 1-6烷基; A是1）具有1-3个独立地选自N，S和O的杂原子的9-10元双环杂环，其中9-10元双环杂环是未取代的或被R5取代，未被取代或被R6取代或被未取代或被NH 2取代，或2）未被取代或被未取代或被R 6取代的R 5取代或未被取代或被-CH 2 NH 2取代的6-9元单环或双环碳环系统; 和B是1）具有1或2个独立地选自N，S或O的杂原子的5或6元单环杂环，其未被取代或在碳或氮原子上被取代或未取代或在碳或氮上取代的R7取代具有R 8的未被取代或取代的碳原子或氮原子上的取代基，或2）具有1,2或3个氮原子的8或9元稠合双环杂环，其在碳或氮原子上未被取代或取代， R7，并且在碳或氮原子上未被取代或取代为R8; 和包含一种或多种所述化合物的药物组合物，以及使用所述化合物治疗或预防血栓形成的方法。

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