Patent ID: 6046169
Filing Date: 2000-04-04
Classification: A61K,C07K

Abstract:
A method for treating a condition in a mammal characterized by undesired thrombosis comprising administering to said mammal a therapeutically effective amount of a compound having the formula ##STR46## wherein: m is 0,1,2,3,4;n is 0,1,2,3,4;Y is CHO, COCF.sub.3, COCF.sub.2 CF.sub.3, COCO.sub.2 R.sub.7, COCONR.sub.8 R.sub.9, B(OR.sub.10).sub.2 ; where: R.sub.7, R.sub.8, R.sub.9, R.sub.10 are the same or different and =H, Cl -6alyI, C.sub.3-8 cycloalkyl, arylC.sub.1-3 alkyl, heteroarylC.sub.1-3 alkyl;A is piperidinyl, pyrrolidinyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl, C.sub.3-8 heteroaryl, or is absent;R.sub.1 is H or C.sub.1-3 alkyl;J is O or H.sub.2 ;R.sub.2 =H or C.sub.1-3 alkyl;D is N,CH, NCH.sub.2, NCH.sub.2 CH.sub.2, CHCH.sub.2 ;R.sub.3 is H or C.sub.1-3 alkyl;E is O or H.sub.2 ;R.sub.4 is H or CH.sub.3 ;Q is piperdinyl, pyrrolidinyl, C.sub.3-8 cycloalkyl, phenyl, substituted phenyl, naphthyl, or pyridyl, or is absent;G is N, CH, or is H;R.sub.5 is H or C.sub.1-3 alkyl, or is absent if G is H;R.sub.6 is H or CH.sub.3 ;W is H, arylacyl, heteroarylacyl, arylC.sub.1-3 alkylsulfonyl, arylsulfonyl, substituted arylsulfonyl, arylC.sub.1-4 alkenylsulfonyl, C.sub.1-8 alkylsulfonyl, heteroarylC.sub.1-3 alkylsulfonyl, heteroarylsulfonyl, aryloxycarbonyl, C.sub.1-6 alkyloxycarbonyl, arylC.sub.1-3 alkyloxycarbonyl, arylaminocarbonyl, C.sub.1-6 alkylaminocarbonyl, arylC.sub.1-3 alkylaminocarbonyl, or HOOC--C.sub.0-3 alkylcarbonyl, or is absent if G is H;X is NR'R"", NH--C(NR'R"").dbd.NH, NH--C(NHR').dbd.NR"", S--C(NR'R"").dbd.NH, S--C(NHR').dbd.NR"", C(NR'R"").dbd.NH, C(NHR')=NR"", or CR'.dbd.NR""; where: R',R"" are the same or different and =H, C.sub.1-6 alkyl, C.sub.1-3 arylalkyl, and aryl, or R' and R"" taken together represent (CH.sub.2).sub.p, where p is an integer from 2 to 5;Z is NR'R"", NH--C(NR'R"").dbd.NH, NH--C(NHR').dbd.NR', S--C(NR'R"").dbd.NH, S--C(NHR').dbd.NR"", C(NR'R).dbd.NH, C(NHR').dbd.NR"", or CR'.dbd.NR""; where: R',R"" are the same or different and =H, C.sub.1-6 alkyl, C.sub.1-3 arylalkyl, and aryl, or R' and R"" taken together represent (CH.sub.2).sub.p, where p is an integer from 2 to 5;with the proviso that when A and Q are both absent, X is NH--C(NH.sub.2).dbd.NH, Y is CHO, m is 1-4, and n is 3, then Z is not NH--C(NH.sub.2).dbd.NH or NH.sub.2 ;and all pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives thereof.