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Tetrahidroisoquinolina substituted compounds as inhibitors of factor XIa
专利权人:
BRISTOL-MYERS SQUIBB COMPANY
发明人:
MICHAEL J. ORWAT,DONALD J. PINTO,LEON M. II SMITH,SHEFALI SRIVASTAVA
申请号:
ARP120103817
公开号:
AR088456A1
申请日:
2012.10.12
申请国别(地区):
AR
年份:
2014
代理人:
摘要:
Claim 1: a compound characterized by the formula (1) or one of its taut u00f3meros stereoisomers, pharmaceutically acceptable salts, where the ring is the Ring B is carbociclo c u2083 u208b u2086; heterocycle containing 4 to 7 carbon Atoms and hetero u00e1t 0 - 3 We further selected from the group consisting nr u2076, N, and S (or Optionally, u209a);The B ring is a Ring with a Spiro FUSED Ring or heterocycle containing 4 to 7 carbon Atoms and 1-3 hetero Atoms selected from the group consisting nr u2076 or s, and (OR) u209a; Ring B, including the Spiro FUSED Ring or ring is replaced with 1 - 3 r u2075; L Is selected from the group consisting chr u00b9 u2070chr u00b9 u2070: - - - - - cr u00b9 u2070 = cr u00b9 u2070, c u00bac chr u00b9 u2070nh - - - - - - - nhchr u00b9 u2070, sch u2082,Ch u2082s so u2082ch u2082 - - - - - - - - and ch u2082so u2082, nhch u2082 - ch u2082nh; r u00b9, in each appearance, is selected from the group consisting of H, alkyl, Halo, c u2081 u208b u2086 c u2081 u208b u2084 alkyl, alkoxy, c u2081 u208b u2084 - Man, Oh, sh, chf u2082, cf u2083, ocf u2083, CN, nh u2082, co alkyl (alkyl c u2081 u208b u2084 c u2081 u208b u2084, CO2), CH u2082co u2082h, ch u2082co u2082 - (alkyl c u2081 u208b u2084 ch u2082nh u2082 conh u2082), -, -, -, - (alkyl with c u2081 u208b u2084) nhco (c u2081 u208b u2084 alkyl (alkyl) - nhco u2082 c u2081 u208b u2084)- nhso u2082 (alkyl c u2081 u208b u2084) and so u2082nh u2082 - and - C (= NH) nh u2082; R u00b2 is selected from the group consisting of H, Oh, CN, Halo, c u2081 u208b u2086 c u2081 u208b u2084 alkyl, alkoxy, haloalquilo c u2081 u208b u2086, haloalcoxi c u2081 u208b u2086, CO (alkyl c u2081 u208b u2084), conh u2082, co u2082h, ch u2082nh u2082 heterocycle and a 5 7 members Comprising 1 to 4 carbon Atoms and nr u1d9c heteroatoms selected from N or s, and (OR) u209a where this heterocycle is replaced with 0 - 2 r u00b2 u1d43, r u00b2 u1d43;In every appearance, is selected from the group consisting of H, alkyl
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