Patent ID: 6489440
Filing Date: 2002-12-03
Classification: A61K,A61P,C07K

Abstract:
A compound of the formula whereinR1 is guanidino, tri-lower alkylammonio, â€”N(R10)â€”R11, â€”N(R15)â€”COâ€”R14, â€”N(R15)â€”COâ€”CH[N(R10)R11]â€”R13, â€”NHCOCH(R13)â€”NHCOCH(NH2)â€”R13, R10 and R11 are each independently selected from hydrogen; heteroaryl substituted with one or two amino; lower alkyl optionally substituted with one or more amino, amino-lower alkyl, cyano, guanidino, nitrogen containing heterocycle(s) or phenyl group(s) containing an amino, amidino or guanidino group; R13 is a residue derived from natural or unnatural amino acids; R14 is lower alkyl substituted with one or more amino, guanidino, nitrogen containing heterocycle(s) or phenyl group(s) containing an amino, amidino or guanidino group; R15 is hydrogen, lower alkyl optionally substituted with one or more amino, guanidino, nitrogen containing heterocycle(s) or phenyl group(s) containing an amino, amidino or guanidino group; R2 is hydrogen, hydroxysulfonyl, lower alkyl or lower alkenyl, wherein lower alkyl and lower alkenyl optionally substituted with acyl, carbamoyl, amino, mono-lower alkylamino or di-lower alkylamino; R3 is hydrogen, hydroxy, nitro, amino, acylamino, (lower alkylcarbamoyl)amino, carboxyl, lower alkoxy, lower alkoxycarbonyl, lower alkyl, lower alkenyl or lower alkynyl, wherein lower alkyl, lower alkenyl and lower alkynyl is optionally substituted with hydroxy, amino, mono-lower alkylamino, di-lower alkylamino, lower alkoxycarbonyl or carbamoyl; R4 is alkyl, alkenyl, alkoxy or alkenyloxy which is optionally substituted with lower alkyl, aryl, cycloalkyl or fluorine atom(s); R5 is â€”CONH2, â€”CN or â€”CH2NH2; X is a single bond, or an aryl, biphenyl or terphenyl group optionally containing one or more hetero atom(s) and/or being substituted with halogen atom(s) or lower alkyl; Y is a single bond, â€”CH2â€”, â€”CH(lower alkyl)-, â€”CONHâ€” or â€”CON(lower alkyl)-; Z is â€”Oâ€”, â€”NHâ€” or â€”N(lower alkyl)-; m is an integer of 0 to 4; and n is an integer of 2 to 5; with the proviso that when â€”Yâ€”(CH2)m-Xâ€”R4 is alkyl or aralkyl, then R1 is not amino, R2 and R3 are not hydrogen, R5 is not â€”CONH2, and Z is not â€”Oâ€” or â€”NHâ€” at the same time; or a pharmaceutically acceptable salt thereof.