Patent ID: 6420397
Filing Date: 2002-07-16
Classification: A61P,C07D

Abstract:
A compound having the Formula I: or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein:R1 is C6-10ar(C1-4)alkyl, C6-10aryl, C4-7cycloalkyl(C1-4)alkyl, heterocycle or heterocyclo(C1-4)alkyl, any of which is optionally substituted; and wherein the heterocycle of said heterocycle or said heterocyclo(C1-4)alkyl is a 5- to 7-membered mono-cyclic or a 9- to 10-membered bi-cyclic heterocyclic ring that is saturated or unsaturated, and contains 1 to 3 heteratoms selected from N, O and S; Z is â€”SO2â€”, â€”OCOâ€”, â€”COâ€”, â€”NR2COâ€” or a covalent bond, where R2 is hydrogen, alkyl, aralkyl, aryl, hydroxy(C2-10)alkyl, amino(C2-10)alkyl, monoalkylamino(C2-10)alkyl, dialkylamino(C2-10)alkyl or carboxyalkyl; Het is selected from the group consisting of â€ƒwhere R3, R4 and R5 are independently hydrogen, C1-4alkyl, C3-7cycloalkyl, C6-14aryl, C6-10ar(C1-4)alkyl, trifluoromethyl, halogen, hydroxyalkyl, cyano, nitro, carboxamide, carboxy, alkoxycarbonyl, carboxymethyl, alkoxycarbonylmethyl or cycloalkoxycarbonyl; R7 is hydrogen, C1-4alkyl, or C2-4alkenyl; R8 is hydrogen, C1-6alkyl, C2-6alkenyl, C6-10ar(C1-6)alkyl, C6-10aryl, hydroxyalkyl, aminoalkyl, monoalkylamino(C2-10)alkyl, dialkylamino(C2-10)alkyl or carboxyalkyl; R12 and R13 are independently hydrogen, C1-4alkyl, C6-10ar(C1-6)alkyl, C6-10aryl, hydroxyalkyl, aminoalkyl, monoalkylamino(C2-10)alkyl, dialkylamino(C2-10)alkyl or carboxyalkyl; or R12 and R13 are taken together to form â€”(CH2)yâ€”, where y is 2 to 7; X is oxygen or NR9, where R9 is hydrogen, alkyl, cycloalkyl or aryl, wherein said alkyl, cycloalkyl or aryl can be optionally substituted with amino, monoalkylamino, dialkylamino, alkoxy, hydroxy, carboxy, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, aryl, heteroaryl, acylamino, cyano or trifluoromethyl; Ra, Rb and Rc are independently hydrogen, alkyl, hydroxy, alkoxy, aryloxy, aralkoxy, alkoxycarbonyloxy, cyano or â€”CO2Rw, where Rw is alkyl, cycloalkyl, phenyl, benzyl, where Rd and Re are independently hydrogen, C1-6alkyl, C2-6alkenyl or phenyl, R1 is hydrogen, C1-6alkyl, C2-6alkenyl or phenyl, Rg is hydrogen, C1-6alkyl, C2-6alkenyl or phenyl, and Rh is aralkyl or C1-6alkyl; A is selected from the group consisting of: and â€”N(CH3)â€”Oâ€”CH3, where R14 is hydrogen, C1-6alkyl, carboxy(C1-6)alkyl, carboxy, C6-20aralkyl, C3-7cycloalkyl, C1-16alkoxycarbonyl, C1-16alkoxycarbonyl (C1-16)alkyl, or (C6-10)aryl; R15 is hydrogen, C3-7cycloalkyl, or C1-4alkyl; and the dashed line indicates point of attachment; n is from zero to 8; and m is from zero to 6.