Patent ID: 6369063
Filing Date: 2002-04-09
Classification: A61K,A61P,C07K

Abstract:
A compound having the formula: wherein:R1 is selected from the group consisting of H, C1-6alkyl, C3-8cycloalkyl, C1-3alkylaryl, C1-3alkyl-C3-8cycloalkyl and aryl and R2 is H, or R1 and R2 are taken together to form a carbocyclic ring; m is an integer from 0-2; n is an integer from 0-6; k is 0; p is 0; q is 1; r is an integer from 0-4; s is an integer from 0-1; t is an integer from 0-4; A is selected from the group consisting of R3, â€”NR3R4, whereR3, R4, R5 and R6 are independently selected from the group consisting of H, â€”OH, C1-6alkyl, aryl and C1-4alkylaryl; R7 is selected from the group consisting of H, C1-6alkyl, aryl and C1-4alkylaryl, or can be taken together with R5 or R6 to form a 5-6 membered ring; and R8 is selected from the group consisting of H, C1-6alkyl, aryl and C1-4alkylaryl, or can be taken together with R6 to form a 5-6 membered ring; Q is selected from the group consisting of a direct link, â€”Sâ€”, â€”SOâ€”, â€”SO2â€”, â€”Oâ€”, â€”SO2NHâ€”, â€”NHSO2â€”, â€”COOâ€”, â€”CONHâ€”, C1-6alkyl, C3-8cycloalkyl, C2-6alkenyl, C2-6alkenylaryl, aryl a to ten membered heterocyclic ring system containing 1-4 heteroatoms selected from the group consisting of N, O and S; D is selected from the group consisting of a direct link, â€”COâ€”, â€”SO2â€”, â€”Oâ€”COâ€”, â€”NR9â€”SO2â€” and â€”NR9â€”COâ€”, where R9 is H, â€”OH, C1-6alkyl, aryl or C1-4alkylaryl; E is selected from the group consisting of a direct link, C3-8cycloalkyl, aryl, and a five to ten membered heterocyclic ring system containing 1-4 heteroatoms selected from the group consisting of N, O and S; G is selected from the group consisting of R10, â€”NR10OR11, whereR10, R11, R12 and R13 are independently selected from the group consisting of H, â€”OH, C1-6alkyl, aryl and C1-4alkylaryl; R14 is selected from the group consisting of H, C1-6alkyl, aryl and C1-4alkylaryl, or can be taken together with R12 or R13 to form a 5-6 membered ring; and R15 is selected from the group consisting of H, C1-6alkyl, aryl and C1-4alkylaryl, or can be taken together with R13 to form a 5-6 membered ring; with the proviso that when G is R10, then E must contain at least one N atom; K is selected from the group consisting of a direct link, C3-8cycloalkyl, C2-6alkenyl, C2-6alkenylaryl, aryl and a five to ten membered heterocyclic ring system containing 1-4 heteroatoms selected from the group consisting of N, O and S; T is selected from the group consisting of R28, â€”NR28R29, whereR28, R29, R30 and R31 are independently selected from the group consisting of H, â€”OH, C1-6alkyl, aryl and C1-4alkylaryl; R32 is selected from the group consisting of H, C1-6alkyl, aryl and C1-4alkylaryl, or can be taken together with R30 or R31 to form a 5-6 membered ring; and R33 is selected from the group consisting of H, C1-6alkyl, aryl and C1-4alkylaryl, or can be taken together with R31 to form a 5-6 membered ring; X and Y are independently selected from the group consisting of O and H2, with the proviso that at least one of X and Y is O; W is selected from the group consisting of H, whereR16 and R17 are independently selected from the group consisting of H, C1-3alkyl and aryl; and Z is selected from the group consisting of H, â€”COOR18, â€”CONR18R19, â€”CF3, â€”CF2CF3 and a group having the formula: where:R18 and R19 are independently selected from the group consisting of H, C1-6alkyl, aryl and C1-4alkylaryl; U is selected from the group consisting of â€”Oâ€”, â€”Sâ€”, â€”Nâ€” and â€”NHâ€”; and V is selected from the group consisting of â€”Oâ€”, â€”Sâ€”, â€”Nâ€” and â€”NHâ€”; with the proviso that at least one of U or V is â€”Nâ€” or â€”NHâ€”; R20 is selected from the group consisting of H, C1-6alkyl, C2-6alkenyl, C0-6alkylaryl, C2-6alkenylaryl, C0-6alkylheterocyclo, C2-6alkenylheterocyclo, â€”CF3 and â€”CF2CF3; J is selected from the group consisting of â€”Sâ€”, â€”SOâ€”, â€”SO2â€”, â€”Oâ€” and â€”NR21â€”, where R21 is selected from the group consisting of H, C1-6alkyl and benzyl; and L is selected from the group consisting of: â€ƒa C6-10 heterocyclic ring system substituted by R24 and R25 and containing 1-4 heteroatoms selected from N, S and O; where d is an integer from 0-2; R22 and R23 are independently selected from the group consisting of H, C1-6alkyl, aryl, C1-6alkylaryl, â€”COOR26, â€”CONR26R27, â€”CN and â€”CF3; R24 and R25 are independently selected from the group consisting of H, C1-6alkyl, aryl, C16alkylaryl, C1-4alkyloxy, halogen, â€”NO2, â€”NR26R27, â€”NR26COR27, â€”OR26, â€”OCOR26, â€”COOR26, â€”CONR26R27, â€”CN, â€”CF3, â€”SO2NR26R27 and C1-6alkyl-OR26; and R26 and R27 are independently selected from the group consisting of H, C1-6alkyl, C1-3alkylaryl and aryl, and all pharmaceutically acceptable salts and optical isomers thereof.