| 摘要 |
Sulfonamido heterocyclic thrombin inhibitors are provided which have the structure <CHEM> wherein G is <CHEM> including all stereoisomers thereof and salts thereof, wherein n is 0, l or 2 or 3; m is 0, l, 2 or 3; Y is NH or S; p is 0, l or 2, Q is a single bond or <CHEM> A is aryl, cycloalkyl, azacycloalkyl or azaheteroalkyl; R is hydrogen, hydroxyalkyl, aminoalkyl, alkyl, cycloalkyl, amidoalkyl, arylalkyl, alkenyl, aryl, alkynyl, arylalkoxyalkyl, or an amino acid side chain; R<1> and R<2> are independently hydrogen, lower alkyl, cycloalkyl, aryl, hydroxy, alkoxy, keto, thioketal, thioalkyl, thioaryl, amino or alkylamino; or R<1> and R<2> can be taken together with the carbons to which they are attached to form a cycloalkyl, aryl or heteroaryl ring; R<3> is lower alkyl, aryl, arylalkyl, heteroaryl, quinolinyl or tetrahydroquinolinyl; and R<4> can be guanidine, amidine or aminomethyl; where A includes a hetero atom, R<4> is amidino; otherwise it may be any of the R<4> moieties set out above. |
