Heterocyclic thrombin inhibitors

Details Heterocyclic thrombin inhibitors Heterocyclic thrombin inhibitors

C - Chemistry, Metallurgy

07

K

C07K 5/00 (2006.01) A61K 31/445 (2006.01) A61K 31/55 (2006.01) A61K 38/04 (2006.01) C07D 211/60 (2006.01) C07D 223/06 (2006.01) C07D 401/12 (2006.01) C07D 413/12 (2006.01) C07K 5/06 (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) C07K 5/093 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2130793

Abstract HETEROCYCLIC THROMBIN INHIBITORS Heterocyclic thrombin inhibitors are provided which have the structure Image including all stereoisomers thereof wherein n is 0, 1 or 2; p is 0, 1 or 2; Q is a single bond or C=O; A is aryl or cycloalkyl, or an azacycloalkyl ring or an azaheteroalkyl ring; R5 is guanidine, amidine or aminomethyl, but when A is azacycloalkyl or azaheteroalkyl, R5 is amidine; R1 and R2 are independently hydrogen, lower alkyl, cycloalkyl, aryl, hydroxy, alkoxy, keto, thioketal, thioalkyl, thioaryl, amino or alkylamino; or R1 and R2 together with the carbons to which they are attached form a cycloalkyl, aryl, or heteroaryl ring; R4 is hydrogen, hydroxyalkyl, aminoalkyl, amidoalkyl, alkyl, cycloalkyl, aryl, arylalkyl, alkenyl, alkynyl, arylalkoxyalkyl, or an amino acid side chain, either protected or unprotected; and R3 is hydrogen, -?-R6, or -CO2R6 (wherein R6 is lower alkyl, aryl, arylalkyl or cyclohetero- alkyl): including pharmaceutically acceptable salts thereof.

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