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Macrocycles with heterocyclic P2 ¿groups as inhibitors of factor XIa
专利权人:
Bristol-Myers Squibb Company
发明人:
CORTE, James R.,DE LUCCA, Indawati,FANG, Tianan,YANG, Wu,WANG, Yufeng,DILGER, Andrew K.,PABBISETTY, Kumar Balashanmuga,EWING, William R.,ZHU, Yeheng,WEXLER, Ruth R.,PINTO, Donald J. P.,ORWAT, Michael
申请号:
ES15705860
公开号:
ES2687498T3
申请日:
2015.01.30
申请国别(地区):
ES
年份:
2018
代理人:
摘要:
A compound of Formula (I): ** Formula ** or a stereoisomer, a tautomer, a pharmaceutically acceptable salt thereof, wherein: ring A is independently selected from a 6-membered aryl and a 5 to 5-heterocyclyl. 6 members, wherein said aryl and said heterocyclyl are optionally substituted with, where valence permits, one or more R4; Ring B is a 5-10 membered heterocyclyl optionally substituted with, where valence permits, one or more R3 or a 5-10 membered heterocyclyl comprising carbon atoms and 1-4 heteroatoms selected from N, NR3c , O, and S (O) py optionally substituted with, where valence permits, one or more R3; G1 is independently selected from C3-10 carbocyclyl and 5-10 membered heterocyclyl, wherein said carbocyclyl and said heterocyclyl are optionally substituted with, where valence permits, one or more R8; X is independently selected from C4-8 alkylene and C4-8 alkenylene, wherein said alkylene and said alkenylene are substituted with R1 and R2; alternatively one or more of the carbon atoms of said alkylene and said alkenylene can be substituted with O, C>; = O, S (>; = O) p, S (>; = O) pNH and NR15; Y is independently selected from -CR13NH-, -NHC (>; = O) -, -C (>; = O) NH-, -S (>; = O) pNH-, -NHS (>; = O) p- and alkylene C1-2; R1 and R2 are independently selected from H, D, halogen, haloalkyl, C1-6 alkyl (optionally substituted with R6), hydroxyl, and alkoxy optionally substituted with R6, and C3-6 cycloalkyl optionally substituted with R6; optionally, when R1 and R2 are attached to the same carbon atom, together they form a C3-6 oxo or cycloalkyl group; optionally, when R1 and R2 are attached to carbon atoms adjacent to each other, together they form a bond or a carbocyclyl; optionally, R1 and R15 or R2 and R15 taken together, form a ring; R3 is independently selected from H, NO2,>; = O, halogen, haloalkyl, C1-4 alkyl (optionally substituted with R6), C2-4 alkenyl (optionally substituted with R6), C2-4 alkynyl (optionally substituted with R6
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