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    Bicyclic aryl azepinone selective factor Xa inhibitors for treating thrombosis related diseases
    33.
    发明专利
    Bicyclic aryl azepinone selective factor Xa inhibitors for treating thrombosis related diseases 未知

    公开(公告)号：NZ502877A

    公开(公告)日：2001-11-30

    申请号：NZ50287798

    申请日：1998-08-11

    Applicant: COR THERAPEUTICS INC

    Inventor： ZHU BING-YAN ,  SCARBOROUGH ROBERT M

    IPC: A61K38/55 ,  A61K38/00 ,  A61P7/02 ,  A61P9/10 ,  C07K5/062 ,  C07K5/078 ,  C07K5/06 ,  A61K38/05

    Abstract: 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; q is an integer from 0-2, 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-; Q is selected from the group consisting of H, or a formula of group (c); 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 (d); 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 (e). The compounds may be used in pharmaceutical compositions for preventing or treating a condition characterised by undesired thrombosis, angina, myocardial infarction, transient ischemic attack, thrombotic stroke, disseminated intravascular coagulation.

    Fused bicyclic lactam selective factor Xa inhibitors for treating thrombosis related diseases
    34.
    发明专利
    Fused bicyclic lactam selective factor Xa inhibitors for treating thrombosis related diseases 未知

    公开(公告)号：NZ502876A

    公开(公告)日：2001-11-30

    申请号：NZ50287698

    申请日：1998-08-11

    Applicant: COR THERAPEUTICS INC

    Inventor： ZHU BING-YAN ,  SCARBOROUGH ROBERT M

    IPC: A61K38/00 ,  A61P7/02 ,  C07K5/06 ,  C07K5/078 ,  A61K38/05

    Abstract: 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

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