发明名称 Heterocycle derivatives which inhibit factor Xa attributed to strong anticoagulant and antithrombotic effect of compounds
摘要 The compounds of the general Formula (I) are useful as inhibitors of blood coagulation in an ex-vivo situation such as, for example, the storage of whole blood or other biological samples suspected to contain Factor Xa and in which coagulation is detrimental. Wherein; A is a 5- or 6-membered monocyclic aromatic ring containing 1, 2 or 3 ring heteroatoms selected from nitrogen; B is an optionally substituted phenylene ring; T1 is CH or N; T2 is CH or N; with the proviso that at least one of T1 and T2 is N; X1 is SO, SO2, C(R4)2 or CO when T1 is CH or N; or in addition X1 is O or S when T1 is CH; and wherein each R4 is independently hydrogen or C1-4alkyl; L 1 is C1-4alkylene or C1-3alkylenecarbonyl; R2 is hydrogen or C1-4alkyl; R3 is hydrogen or C1-4alkyl; or R2 and R3 are joined to form a C1-4alkylene or -CH2CO- group; with the proviso that when T1 and T2 are both N, L1 is not methylene and R2 and R3 together are not methylene; X2 is S(O)y wherein y is one or two, C(R5)2 or CO; and each R5 is hydrogen or C1-4alkyl; Q is phenyl, naphthyl, phenylC1-4alkyl, phenylC2-4alkenyl. phenylC2-4alkynyl or a heterocyclic moiety containing up to 4 heteroatoms selected from nitrogen, oxygen and sulphur and Q is optionally substituted; and pharmaceutically acceptable salts thereof. Further structures illustrated as Formula (II), (III) and (IV) are examples of the disclosed application.
申请公布号 NZ334710(A) 申请公布日期 2000.11.24
申请号 NZ19970334710 申请日期 1997.11.04
申请人 ZENECA LIMITED 发明人 STOCKER, ANDREW;PRESTON, JOHN;RAYNER, JOHN WALL;SMITHERS, MICHAEL JAMES;TURNER, PAUL
分类号 A61K31/44;A61K31/444;A61K31/496;A61K31/501;A61K31/505;A61K31/506;A61P7/02;C07D213/00;C07D213/56;C07D213/61;C07D213/73;C07D213/84;C07D213/89;C07D237/08;C07D239/26;C07D241/00;C07D307/77;C07D401/10;C07D405/12;(IPC1-7):C07D239/26;C07D403/10 主分类号 A61K31/44
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