发明名称 FACTOR IXA INHIBITORS
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.
申请公布号 EP2934538(A1) 申请公布日期 2015.10.28
申请号 EP20130873301 申请日期 2013.12.16
申请人 MERCK SHARP & DOHME CORP.;MOCHIDA PHARMACEUTICAL CO., LTD. 发明人 SMITH, CAMERON, JAMES;TAN, JOHN, QIANG;ZHANG, TING;BALKOVEC, JAMES;GREENLEE, WILLIAM, JOHN;GUO, LIANGQIN;XU, JIAYI;CHEN, YI-HENG;CHEN, YILI;CHACKALAMANNIL, SAMUEL;HIRABAYASHI, TOMOKAZU;NAGASUE, HIROSHI;OGAWA, KOUKI
分类号 C07D413/12;A61K31/5377;A61P7/02 主分类号 C07D413/12
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