Patent ID: 6833366
Filing Date: 2004-12-21
Classification: A61P,C07D

Abstract:
A compound of the Formula: or a pharmaceutically acceptable salt thereof, wherein is a phenyl ring, optionally substituted with one or more substituent selected from the group consisting of alkyl, haloalkyl, aryl, heteroaryl, halogen, alkoxyalkyl, aminoalkyl, hydroxy, nitro, alkoxy, hydroxyalkyl, thioalkyl, amino, alkylamino, arylamino, alkylsulfonamide, acyl, acylamino, sulfone, sulfonamide, allyl, alkenyl, methylenedioxy, ethylenedioxy, alkynyl, carboxamide, cyano, and â€”(CH2)n COR wherein n is 0-2 and R is selected from the group consisting of hydroxy, alkoxy, alkyl and amino; A1 is a 5-9 membered monocyclic or 7-14 membered polycyclic heterocycle containing at least one nitrogen atom and optionally 1 to 4 heteroatoms or groups selected from O, N, S, SO2 or CO; optionally saturated or unsaturated; optionally substituted by one or more Rk selected from the group consisting of hydroxy, alkyl, alkoxy, alkoxyalkyl, thioalkyl, haloalkyl, cyano, amino, alkylamino, halogen, acylamino, sulfonamide and â€”COR wherein R is selected from hydroxy, alkoxy, alkyl and amino; or or A1 is wherein Y1 is selected from the group consisting of Nâ€”R2, O, and S; R2 is selected from the group consisting of H; alkyl; aryl; hydroxy; alkoxy; cyano; alkenyl; alkynyl; amido; alkylcarbonyl; arylcarbonyl; alkoxycarbonyl; aryloxycarbonyl; haloalkylcarbonyl; haloalkoxycarbonyl; alkylthiocarbonyl; arylthiocarbonyl; acyloxymethoxycarbonyl; R2 taken together with R7 forms a 4-12 membered dinitrogen containing heterocycle optionally substituted with one or more substituent selected from the group consisting of lower alkyl, thioalkyl, alkylamino, hydroxy, keto, alkoxy, halo, phenyl, amino, carboxyl or carboxyl ester, and fused phenyl; R2 taken together with R7 forms a 5-9 membered heteroaromatic ring optionally substituted with one or more substituent selected from lower alkyl, phenyl, alkoxy and hydroxy; R2 taken together with R7 forms a 5 membered heteroaromatic ring fused with a aryl or heteroaryl ring; R7 (when not taken together with R2) and R8 are independently selected from the group consisting of H; alkyl; alkenyl; alkynyl; aralkyl; amino; alkylamino; hydroxy; alkoxy; arylamino; amido, alkylcarbonyl, arylcarbonyl; alkoxycarbonyl; aryloxy; aryloxycarbonyl; haloalkylcarbonyl; haloalkoxycarbonyl; alkylthiocarbonyl; arylthiocarbonyl; acyloxymethoxycarbonyl; cycloalkyl; bicycloalkyl; aryl; acyl; benzoyl; or NR7 and R8 taken together form a 4-12 membered mononitrogen containing monocyclic or bicyclic ring optionally substituted with one or more substituent selected from lower alkyl, carboxyl derivatives, aryl or hydroxy and wherein said ring optionally contains a heteroatom selected from the group consisting of O, N and S; R5 is selected from the group consisting of H and alkyl; or A1 is â€ƒwherein Y2 is selected from the group consisting of alkyl; cycloalkyl, bicycloalkyl; aryl; monocyclic heterocycles; wherein R5 and R7 are defined above; Z1 is selected from the group consisting of CH2, CH2O, O, NH, CO, S, SO, CH(OH) and SO2; Z2 is a 1-5 carbon linker optionally containing one or more heteroatom selected from the group consisting of O, S and N; wherein the carbon and nitrogen atoms of Z1-Z2 are optionally substituted by a moiety selected from the group consisting of alkyl, alkoxy, thioalkyl, alkylsulfone, aryl, alkoxyalkyl, alkylamino, heteroaryl, alkenyl, alkynyl, carboxyalkyl, halogen, haloalky and acylamino; n is an integer 0, 1 or 2; Rc is selected from the group consisting of hydrogen; alkyl; halogen, hydroxy, nitro, alkoxy, amino, haloalkyl, aryl, heteroaryl, alkoxyalkyl, aminoalkyl, hydroxyalkyl, thioalkyl, alkylamino, arylamino, alkylsulfonylamino, acyl, acylamino, sulfonyl, sulfonamide, allyl, alkenyl, methylenedioxy, ethylenedioxy, alkynyl, alkynylalkyl, carboxy, alkoxycarbonyl, carboxamido, cyano, and â€”(CH2)nCOR wherein n is 0-2 and R is selected from hydroxy, alkoxy, alkyl and amino; X is selected from the group consisting of â€”CHReâ€”, â€”NHRfâ€”, â€”Oâ€”, â€”Sâ€”, â€”SO2â€”, and CO wherein Re is selected from H, lower alkyl, alkoxy, cycloalkyl, alkoxyalkyl, hydroxy, alkynyl, alkenyl, haloalkyl, thioalkyl and aryl; wherein when Re is hydroxy the hydroxy optionally forms a lactone with the carboxylic acid function of the chain; wherein Rf is selected from the group consisting of H, alkyl, aryl, benzyl and haloalkyl; Y is selected from the group consisting of â€”CRgâ€” and â€”Ngâ€” wherein Rg is selected from the group consisting of H, alkyl, haloalkyl, alkoxyalkyl, alkynyl, aryl, heteroaryl, aralkyl, hydroxy, alkoxy, and carboxyalkyl; Rb is X2â€”Rh wherein X2 is selected from the group consisting of O, S and NRj wherein Rh and Rj are independently selected from the group consisting of H, alkyl, aryl, aralkyl, acyl and alkoxyalkyl; and Ra is selected from the group consisting of hydrogen, alkyl, alkenyl, alkoxyalkyl, hydroxyalkyl, alkynyl, alkynylalkyl, alkenylalkyl, haloalkyl, aryl, heteroaryl, aralkyl, heteroaralkyl, cycloalkyl, carboxyl, amino, alkylamine, alkoxycarbonyl, carboxamido, hydroxy, cyano, alkoxy, thioalkyl, acylamino, sulfonyl amino, alkylsulfonyl, and â€”(CH2)n CORb wherein n is 0-2 and Rb is as defined above.