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Tetrahydroisoquinoline compounds substituted as XIA factor inhibitors
专利权人:
Bristol-Myers Squibb Company
发明人:
ORWAT, Michael J.,PINTO, Donald J.P.,SMITH II, Leon M.,SRIVASTAVA, Shefali
申请号:
ES12778913
公开号:
ES2625256T3
申请日:
2012.10.12
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A compound according to formula (I): ** Formula ** or a stereoisomer, a tautomer, a pharmaceutically acceptable salt or a solvate thereof, wherein: ring A is a C3-6 carbocycle; Ring B is a 4- to 7-membered heterocycle containing additional carbon atoms and 0-3 heteroatoms selected from the group consisting of N, NR6, O and S (O) p; optionally, ring B forms a condensed ring or a spiro ring with a 4- to 7-membered heterocycle containing carbon atoms and 1-3 heteroatoms selected from the group consisting of NR6, O and S (O) p; Ring B, including the condensed ring or the spiro ring, is substituted with 1-3 R5; L is selected from the group consisting of: -CHR10CHR10-, -CR10>; = CR10-, -CºC-, -CHR10NH-, -NHCHR10-, - SCH2-, -CH2S-, -SO2CH2-, -CH2SO2-, - NHCH2- and -CH2NH-; R1, at each occurrence, is selected from the group consisting of: H, halo, C1-6 alkyl, C1-4 alkoxy, C1-4 alkylthio, OH, SH, CHF2, CF3, OCF3, CN, NH2, CO- C1-4 alkyl, CO2 (C1-4 alkyl), -CH2CO2H, -CH2CO2 (C1-4 alkyl), - CH2NH2, -CONH2, -CONH (C1-4 alkyl), -NHCO (C1-4 alkyl), - NHCO2 (C1-4 alkyl), -NHSO2 (C1-4 alkyl) and - SO2NH2 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, CH2NH2 and a 5- to 7-membered heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, NRc, O and S (O) p, wherein said heterocycle is substituted with 0-2 R2a; R2a, at each occurrence, is selected from the group consisting of: H, halo, C1-4 alkyl, C1-4 alkoxy, OH, CF3, OCF3, CN, NH2, CO2H, CO2 (C1-4 alkyl), CO (C1-4 alkyl), -CONH2, -CH2OH, -CH2O-C1-4 alkyl, -CH2NH2-, CONH (C1-4 alkyl), -CON (C1-4 alkyl) 2, -SO2 (C1-4 alkyl ), -SO2NH2, -SO2NH (C1-4 alkyl) and -SO2N (C1-4 alkyl) 2; R3 is selected from the group consisting of: C1-6 alkyl substituted with 1-3 R3a, - (CH2) n-carbocycle C3-10 substituted with 0-3 R3a or - (CH2) 5-10 membered n-heterocycle containing carbon atoms and 1-4 heteroatoms
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