Guanidinyl- or amidinyl-substituted methylamino heterocyclic...

Details Guanidinyl- or amidinyl-substituted methylamino heterocyclic... Guanidinyl- or amidinyl-substituted methylamino heterocyclic...

C - Chemistry, Metallurgy

07

D

C07D 401/12 (2006.01) A61K 31/40 (2006.01) A61K 31/445 (2006.01) A61K 31/495 (2006.01) C07D 207/08 (2006.01) C07D 207/09 (2006.01) C07D 211/60 (2006.01) C07D 403/12 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01) C07D 413/12 (2006.01) C07D 417/12 (2006.01) C07D 471/04 (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) A61K 38/00 (2006.01)

Patent

CA 2122646

Abstract METHYLAMINO HETEROCYCLIC THROMBIN INHIBITORS Guanidinyl- or amidinyl-substituted heterocyclic thrombin inhibitors are provided which have the structure Image wherein n is 0, 1 or 2; R1 is -A-R2, -CO-A-R2 or -SO2-A-R2; wherein R2 is guanidine, amidine or amino, and A is an alkyl, alkenyl or alkynyl chain of 2 to 6 carbons; or R1 is -(CH2)p-A'-R2 or -(CH2)p-CO-A'R2' where p is 0, 1 or 2, R2' is amidine and A' is an azacycloalkyl or azaheteroalkyl ring of 4 to 8 atoms, optionally substituted by alkyl, CO or halo; R1 is -(CH2)p-A"-R2", -(CH2)p-CO-A"-R2", or -(CH2)p-SO2-A" -R2", wherein R2"is guanidine, amidine or aminomethyl, and A" is aryl or cycloalkyl; and R3, R4, R5 and R6 are as defined herein.

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