| 摘要 |
N,N-di(aryl) cyclic urea derivatives, such as the compounds of the following formula: <IMAGE> (III) wherein R1 is -C(NH)NH2, -C(NH)N(H)OR11, -C(NH)N(H)C(O)R9, or -C(NH)N(H)C(O)OR11; R2 and R3 are independently hydrogen, halo, lower alkyl, lower haloalkyl, aryl, -OR11, -C(O)OR11, -C(O)N(R11)R12, -N(R11)R12, -N(H)C(O)R11, or -N(H)S(O)2R11; R4 is halo, lower haloalkyl, imidazolyl, -C(NH)NH2, -C(NH)NHOR11, -C(NH)N(H)C(O)R9, -C(NH)N(H)C(O)OR11, -OR11, -C(O)R13, -(CH2)nC(O)OR11 (where n is 0 to 6), -C(O)N(R11)R12, or -N(11)R12; R7 and R8 are independently hydrogen, lower alkyl, lower haloalkyl, 4-pyridinyl, -C(O)OR11, -C(O)N(R11)R12, or aryl (optionally substituted by one or more substituents selected from the group consisting of halo, hydroxy, lower alkyl, lower haloalkyl, lower alkoxy and -N(R11)R12); R11 and R12 are independently hydrogen, lower alkyl, aryl or lower aralkyl; or R13 is pyrrolidinyl, 4-morpholinyl, piperazinyl, N-methylpiperazinyl, or piperidinyl; or a pharmaceutically acceptable salt thereof, are disclosed herein as being inhibitors of factor Xa and thereby being useful as anticoagulants.
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