Guanidinyl-substituted heterocyclic thrombin inhibitors

Details Guanidinyl-substituted heterocyclic thrombin inhibitors Guanidinyl-substituted heterocyclic thrombin inhibitors

C - Chemistry, Metallurgy

07

K

C07K 5/06 (2006.01) A61K 31/395 (2006.01) A61K 38/05 (2006.01) C07D 207/16 (2006.01) C07D 211/60 (2006.01) C07D 217/26 (2006.01) C07D 223/06 (2006.01) C07D 401/00 (2006.01) C07D 413/00 (2006.01) C07D 417/00 (2006.01) C07D 473/04 (2006.01) C07D 487/04 (2006.01) C07K 5/062 (2006.01) C07K 5/065 (2006.01) C07K 5/068 (2006.01) C07K 5/072 (2006.01) C07K 5/078 (2006.01) C07K 5/083 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2110464

Abstract SULFONAMIDO HETEROCYCLIC THROMBIN INGIBITORS Sulfonamido heterocyclic thrombin inhibitors are provided which have the structure Image wherein G is Image or Image including all stereoisomers thereof and salts thereof, wherein n is 0, 1 or 2 or 3; m is 0, 1, 2 or 3; Y is NH or S; p is 0, 1 or 2, Q is a single bond or Image 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; R1 and R2 are independently hydrogen, lower alkyl, cycloalkyl, aryl, hydroxy, alkoxy, keto, thioketal, thioalkyl, thioaryl, amino or alkylamino; or R1 and R2 can be taken together with the carbons to which they are attached to form a cycloalkyl, aryl or heteroaryl ring; R3 is lower alkyl, aryl, arylalkyl, hetero- aryl, quinolinyl or tetrahydroquinolinyl; and R4 can be guanidine, amidine or aminomethyl; where A includes a hetero atom, R4 is amidino; otherwise it may be any of the R4 moieties set out above.

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