Patent ID: 6426413
Filing Date: 2002-07-30
Classification: A61P,C07D

Abstract:
A compound represented by formula (I): wherein:Y is: m is 0 or 1; W is â€”CH2â€”, â€”C(O)â€”; X is â€”C(H)â€”, â€”C(R8)â€”; Z is â€”CH2â€”; each R1 is independently â€”H, â€”C(O)R8, â€”S(O)2R8, â€”S(O)R8, â€”R21, -alkyl-R21, -alkenyl-R21, -alkynyl-R21, -alkyl; R2 is â€”C(O)R8, â€”C(O)C(O)R8, â€”S(O)2R8, â€”S(O)R8, â€”C(O)OR8, â€”C(O)N(H)R8, â€”S(O)2N(H)-R8, â€”S(O)N(H)-R8, â€”C(O)C(O)N(H)R8, â€”C(O)CH&boxH;CHR8, â€”C(O)CH2OR8, â€”C(O)CH2N(H)R8, â€”C(O)N(R8)2, â€”S(O)2N(R8)2, â€”S(O)N(R8)2, â€”C(O)C(O)N(R8)2, â€”C(O)CH2N(R8)2, â€”CH2â€”R8, â€”CH2-alkenyl-R8, or â€”CH2-alkynyl-R8; R3 is â€”H, â€”R21, -alkyl-R21, -alkenyl-R21, -alkynyl-R21, alkyl, or an amino acid side chain; each R4 is independently â€”OH, â€”F, â€”Cl, â€”Br, â€”I, â€”NO2, â€”CN, â€”NH2, â€”CO2H, â€”C(O)NH2, â€”N(H)C(O)H, â€”N(H)C(O)NH2, -alkyl, -cycloalkyl, -perfluoroalkyl, â€”O-alkyl, â€”(H)alkyl, â€”N(alkyl)2, â€”C(O)N(H)alkyl, â€”C(O)N(alkyl)2, â€”N(H)C(O)alkyl, â€”N(H)C(O)N(H)alkyl, â€”N(H)C(O)N(alkyl)2, â€”S-alkyl, â€”S(O)2alkyl, â€”S(O)alkyl, â€”C(O)alkyl, â€”CH2NH2, â€”CH2N(H)alkyl, â€”CH2N(alkyl)2, or â€”N(H)C(O)Oalkyl; R5 is â€”OH, â€”OR8, â€”N(H)OH, or â€”N(H)SO2R8; R6 is â€”H, â€”CH2OR9, â€”CH2SR10, â€”CH2N(H)R9, â€”CH2N(R9)R11, â€”CHN2, â€”CH2F, â€”CH2Cl , â€”CH2Br, â€”CH2I, â€”C(O)N(R11)2, â€”R13, or â€”R14; each R8 is independently -alkyl, -cycloalkyl, -aryl, -heteroaryl, -heterocyclyl, -alkylcycloalkyl -alkylaryl, -alkylheteroaryl, or -alkylheterocyclyl; R9 is â€”H, â€”C(O)aryl, â€”C(O)heteroaryl, â€”C(O)alkylaryl, â€”C(O)alkylheteroaryl, -alkylaryl, -alkylheteroaryl, -aryl, -heteroaryl, or â€”P(O)(R15)2; R10 is -alkylaryl or -alkylheteroaryl; each R11 is independently â€”H, -alkyl, -aryl, -heteroaryl, -cycloalkyl, -alkylaryl, or -alkylheteroaryl; R13 is -alkylaryl or -alkylheteroaryl; wherein Q is â€”Oâ€” or â€”Sâ€”, any hydrogen atom in (i) is optionally replaced with â€”R17, and any hydrogen atom in (ii), (iii), and (iv) is optionally replaced with â€”R17, â€”R18 or -alkyl-R18; each R15 is independently â€”H, â€”OH, -alkyl, -aryl, -heteroaryl, -cycloalkyl, -alkylaryl, -alkylheteroaryl, â€”O-alkyl, â€”O-aryl, â€”O-heteroaryl, â€”O-alkylaryl, or â€”O-alkylheteroaryl; each R17 is independently â€”OH, â€”F, â€”Cl, â€”Br, â€”I, â€”NO2, â€”CN, â€”NH2, â€”CO2H, â€”C(O)NH2, â€”N(H)C(O)H, â€”N(H)C(O)NH2, â€”SO2NH2, â€”C(O)H, -alkyl, -cycloalkyl, -perfluoroalkyl, â€”O-alkyl, â€”N(H)alkyl, â€”N(alkyl)2, â€”CO2alkyl, â€”C(O)N(H)alkyl, â€”C(O)N(alkyl)2, â€”N(H)C(O)alkyl, â€”N(H)C(O)N(H)alkyl, â€”N(H)C(O)N(alkyl)2, â€”S(O)2N(H)alkyl, â€”S(O)N(H)alkyl, â€”S(O)2N(alkyl)2, â€”S(O)N(alkyl)2, â€”S-alkyl, â€”S(O)2alkyl, â€”S(O)alkyl, or â€”C(O)alkyl; each R18 is independently -aryl, -heteroaryl, -alkylaryl, -alkylheteroaryl, â€”O-aryl, â€”O-heteroaryl, â€”O-alkylaryl, â€”O-alkylheteroaryl, â€”N(H)aryl, â€”N(aryl)2, â€”N(H)heteroaryl, â€”N(heteroaryl)2, â€”N(H)alkylaryl, â€”N(alkylaryl)2, â€”N(H)alkylheteroaryl, â€”N(alkylheteroaryl)2, â€”S-aryl, â€”S-heteroaryl, â€”S-alkylaryl, â€”S-alkylheteroaryl, â€”C(O)aryl, â€”C(O)heteroaryl, â€”C(O)alkylaryl, â€”C(O)alkylheteroaryl, â€”CO2aryl, â€”CO2heteroaryl, â€”CO2alkylaryl, â€”CO2alkylheteroaryl, â€”C(O)N(H)aryl, â€”C(O)N(aryl)2, â€”C(O)N(H)heteroaryl, â€”C(O)N(heteroaryl)2, â€”C(O)N(H)alkylaryl), â€”C(O)N(alkylaryl)2, â€”C(O)N(H)alkylheteroaryl, â€”C(O)N(alkylheteroaryl)2, â€”S(O)2-aryl, â€”S(O)-aryl, â€”S(O)2-heteroaryl, â€”S(O)-heteroaryl, â€”S(O)2-alkylaryl, â€”S(O)-alkylaryl, â€”S(O)2-alkylheteroaryl, â€”S(O)-alkylheteroaryl, â€”S(O)2N(H)-aryl, â€”S(O)N(H)-aryl, â€”S(O)2NH-heteroaryl, â€”S(O)NH-heteroaryl, â€”S(O)2N(H)-alkylaryl, â€”S(O)N(H)-alkylaryl, â€”S(O)2N(H)-alkylheteroaryl, â€”S(O)N(H)-alkylheteroaryl, â€”S(O)2N(aryl)2, â€”S(O)N(aryl)2, â€”S(O)2N(heteroaryl)2, â€”S(O)N(heteroaryl)2, â€”S(O)2N(alkylaryl)2, â€”S(O)N(alkylaryl)2, â€”S(O)2N(alkylheteroaryl)2, â€”S(O)N(alkylheteroaryl)2, â€”N(H)C(O)N(H)aryl, â€”N(H)C(O)N(H)heteroaryl, â€”N(H)C(O)N(H)alkylaryl, â€”N(H)C(O)N(H)alkylheteroaryl, â€”N(H)C(O)N(aryl)2, â€”N(H)C(O)N(heteroaryl)2, â€”N(H)C(O)N(alkylaryl)2, or â€”N(H)C(O)N(alkylheteroaryl)2; each R21 is independently -aryl, -heteroaryl, cycloalkyl, or -heterocyclyl, wherein a hydrogen atom bound to any carbon atom is optionally replaced by R4 and a hydrogen atom bound to any nitrogen atom is optionally replaced by R2; each heterocyclyl is a mono-or polycyclic ring system which contains 1 to 15 carbon atoms and 1 to 4 heteroatoms selected from S, N, or O, in which the mono- or polycyclic ring system may optionally contain unsaturated bonds but is not aromatic; each cycloalkyl is a mono- or polycyclic, non-aromatic, hydrocarbon ring system which may optionally contain unsaturated bonds in the ring system; each heteroaryl is a mono- or polycyclic ring system which contains 1 to 15 carbon atoms and 1 to 4 heteroatoms selected from S, N, or O, and in which at least one ring of the ring system is aromatic; and each amino acid side chain is the substituent bound to the &agr;-carbon of a natural or non-natural &agr;-amino acid.