发明名称 Fused bicyclic lactam selective factor Xa inhibitors for treating thrombosis related diseases
摘要 Compounds of formula (I) wherein: R1 and R2 are independently selected from H, C1-6alkyl, C3-8cycloalkyl, C1-3alkylaryl, C1-3alkyl-C3-8cycloalkyl and aryl; R3 is H, C1-6alkyl, or R2 and R3 are taken together to form a carbocyclic ring; r and t are an integer from 0-4, s is an integer from 0-1; A is selected from R8, -NR8R9, or a formula from group (a); D is selected from a direct link, C3-8cycloalkyl, C1-6alkenyl, C1-6alkenylaryl, aryl and a five to ten membered heterocyclic ring system containing 1-4 heteroatoms selected from N, 0 and S; E is selected from a direct link, -CO-, -SO2-, -O-CO-, -NR14-SO2- and -NR14-CO-, where R14 is selected from H, -OH, C1-6alkyl, aryl and C1-4alkylaryl; G is selected from a direct link, C3-8cycloalkyl, aryl, and a five to ten membered heterocyclic ring system containing 1-4 heteroatoms selected from N, 0 and S; J is selected from the group consisting of R15, -NR15R16, or a formula from group (b); K', K", K"' and K"" are independently selected from -CH-, -CR4-, -CR5- and -N-; with the proviso that no more than one of K', K", K"' and K"" are -CR4- and no more than one of K', K", K"' and K"" are -CR5-; L is selected from -CH2-, -O-, -S-, -SO-, -SO2- and X-(CH2)d-Y-(CH2)e-Z-N-; where X is selected from R33, -NR33R34, or a formula from group (c); Q is selected from the group consisting of H, or a formula of group (d); where R21 and R22 are independently selected from H, C1-3alkyl and aryl; and T is selected from the group H, -COOR23, -CONR23R24, -CF3, -CF2CF3 and a group having the formula from group (e); where R23 and R24 are independently selected from H, C1-6alkyl, aryl and C1-4alkylaryl; U' and U" are independently selected from -O-, -S-, -N- and -NH-; with the proviso that at least one of U' or U" is -N- or -NH-; R25 is selected from H, C1-6alkyl, C2-6alkenyl, C0-6alkylaryl, C2-6alkenylaryl, C0-6alkylheterocyclo, C2-6alkenylheterocyclo, -CF3 and -CF2CF3; V is selected from -S-, -SO-, -SO2-, -O- and -NR26-, where R26 is selected from H, C1-6alkyl and benzyl; and W is selected from the formula (f). The compounds are suitable for treating conditions characterized by undesired thrombosis, unstable angina, refractory angina, myocardial infarction, transient ischemic attacks, thrombotic stroke, embolic stroke, disseminated intravascular coagulation, septic shock, deep venous thrombosis, pulmonary embolism, or reocclusion or restenosis of reperfused coronary arteries
申请公布号 NZ502876(A) 申请公布日期 2001.11.30
申请号 NZ19980502876 申请日期 1998.08.11
申请人 COR THERAPEUTICS, INC 发明人 ZHU, BING-YAN;SCARBOROUGH, ROBERT M
分类号 A61K38/00;A61P7/02;C07K5/06;C07K5/078;(IPC1-7):C07K5/06;A61K38/05 主分类号 A61K38/00
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