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Compuestos de tetrahidroisoquinolina sustituidos como inhibidores del factor XIa
专利权人:
Bristol-Myers Squibb Company
发明人:
ORWAT, Michael J.,PINTO, Donald J.P.,SMITH II, Leon M.,SRIVASTAVA, Shefali,CORTE, James R.
申请号:
ES12778912
公开号:
ES2572908T3
申请日:
2012.10.12
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
A compound according to Formula (I): Formula ** ** or a stereoisomer, a tautomer, a pharmaceutically acceptable salt thereof, wherein: ring A is C3-10 carbocycle L is selected from the group consisting of: a bond, -CHR10CHR10-, -CR10> = CR10- and -C≡C- Q is selected from the group consisting of: C, CH and N --- it is an optional bond provided that when Q is N, the optional bond is absent ring B is a 5- to 6-membered containing carbon atoms and 1-3 heteroatoms selected from the group consisting of N, NR6, O and S (O) p, wherein said heterocycle is substituted with 0-3 R5 optionally, ring B is fused with further phenyl ring substituted with 0-2 R5 or a 5- to 6-membered containing carbon atoms and 1-2 heteroatoms selected from the group consisting of N, NR6, O and S (O) p wherein he said heteroaryl is substituted with 0-2 R5 R1, in each instance, is selected from the group consisting of: H, halo, C1-2 alkyl, -O (C1-4 alkyl), CN, -CH2NH2 and -C (> = NH) NH2 R2 is selected from the group consisting of: H, halo, CN, OH, C1-6 alkyl, C1-4 alkoxy, C1-6 haloalkyl, C1-6 haloalkoxy, CO (C1-4 alkyl), CONH2, CO2H and a 5- to 7-membered comprising carbon atoms and 1-4 heteroatoms selected from N, NH, N (C1-4 alkyl), O and S (O) p, wherein said heterocycle is substituted with 1-2 R2a R2a, at each occurrence, is selected from the group consisting of: H, halo, C1-4alkyl, CO2H, -CO2 alkyl (C1-4alkyl), -CONH2, -CH2OH, -CH2O C1-4alkyl and -CH2NH2 R3 is selected from the group consisting of: C1-6 alkyl substituted with 1-3 R3a, C3-10 carbocycle substituted with 1-3 R3a and 5-10 membered heterocycle containing carbon atoms and 1-4 heteroatoms selected from the group consisting of N, NR7, O and S (O) p wherein said heterocycle is substituted with 1-3 R3a R3a, at each occurrence, is selected from the group consisting of: H,> = O, halo, C1-4alkyl, -OH, C1-4 alkoxy, -CN, -NH2, -NH alkyl (C1-4 alkyl) , -N (C1-4alkyl) 2, -CO2H, -CH2CO2H, -CO2 (C1-4 alkyl), -CO 2 C 1-4 alkylene or (C1-4 alkyl)
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