Patent ReferencesHeteroaromatic and thioheteroaromatic substituted sulfonamide thrombin inhibitors Patent #: 5332822 InventorsAssigneeApplicationNo. 458598 filed on 06/02/1995US Classes:514/392, Divalent chalcogen or acyclic nitrogen double bonded at 2-position, or tautomeric equivalent548/322.5, Having -C(=X)-, wherein X is chalcogen, bonded directly to the diazole ring548/323.1, Acyclic nitrogen bonded directly to the -C(=X)- group548/323.5, Chalcogen attached indirectly to the diazole ring by acyclic nonionic bonding548/324.1, The chalcogen, X, is in a -C(=X)- group548/324.5Nitrogen attached indirectly to the diazole ring by acyclic nonionic bondingExaminersPrimary: Morris, Patricia L.Attorney, Agent or FirmForeign Patent References
International ClassesA61K 031/415C07D 233/32 AbstractN,N-di(aryl) cyclic urea derivatives, such as the compounds of the following formula: ##STR1## 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)2 R11 ;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)n C(O)OR11 (where n is 0 to 6), --C(O)N(R11)R12, or --N(R11)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; orR13 is pyrrolidinyl, 4-morpholinyl, piperazinyl, N-methylpiperazinyl, or piperidinyl; or apharmaceutically acceptable salt thereof, are disclosed herein as being inhibitors of factor Xa and thereby being useful as anticoagulants.Other References
Field of SearchHaving -C(=X)-, wherein X is chalcogen, bonded directly to the diazole ringAcyclic nitrogen bonded directly to the -C(=X)- group Chalcogen attached indirectly to the diazole ring by acyclic nonionic bonding The chalcogen, X, is in a -C(=X)- group Nitrogen attached indirectly to the diazole ring by acyclic nonionic bonding Divalent chalcogen or acyclic nitrogen double bonded at 2-position, or tautomeric equivalent |
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