Patent ID: 6668527
Filing Date: 2003-12-30
Classification: A61P,C07C,C07D

Abstract:
A compound of Formula (1.0.0) and pharmaceutically acceptable salts and other prodrug derivative thereof, wherein:A is (C1-C6) alkyl, cycloalkyl, aryl, heteroaryl or heterocyclyl as defined herein; where said alkyl, cycloalkyl, aryl, heteroaryl or heterocyclyl is optionally substituted with 0 to 3 R9; or is a member selected from the group consisiting of the following radicals: A1-NHC(&boxH;O)NH-A2-, A1-NHC(&boxH;O)O-A2-, A1-OC(&boxH;O)NH-A2-, A1-NHSO2NH-A2-, A1-NHC(&boxH;O)-A2-, A1-C(&boxH;O)NH-A2-, A1NHSO2-A2-, A1SO2NH-A2-, A1-(CH2)rO-A2-, A1-O(CH2)rA2-, A1-(CH2)rA2, where A1 is aryl and A2 is aryl or pyridyl: group is substituted with 0 to 3 R9; B is a member independently selected from the group consisting of the following: where the symbol â€œ*â€  indicates the point of attachment of the moiety represented by each partial Formula (1.1.0) through (1.1.4), (1.1.6) and (1.1.8) to the moiety â€œCR2R3â€  in Formula (1.0.0); and the symbol â€œâ†’â€  indicates the point of attachment of the moiety represented by each partial Formula (1.1.0) through (1.1.4), (1.1.6) and (1.1.8) to the moiety â€œEâ€  in Formula (1.0.0); each of Formula (1.1.0) through (1.1.4), (1.1.6) and (1.1.8), may be optionally substituted with R9; E is a single bond X is â€”Oâ€”; Y is â€”C(&boxH;O); k is an integer independently selected from 0, 1 and 2; m is an integer independently selected from 0 and 1; n is an integer independently selected from 0, 1 and 2; p is 1; q is an integer independently selected from 0,1 and 2; r is an integer independently selected from 0, 1 and 2; R2 and R3 are each independently selected from the group consisting of hydrogen and (C1-C6) alkyl substituted with 0 to 3 R13; R4 is hydrogen; or (C1-C6) alkyl optionally substituted with R13; R5 and R6 are independently hydrogen; (C1-C6) alkyl; (C2-C6) alkenyl; (C2-C6) alkynyl; CF3; aryl; cycloalkyl; heteroaryl; or heterocyclyl; R7 is (C1-C6) alkyl; (CH2)kOR5; (CH2)kNR6C(&boxH;O)R5; (CH2)kNR6C(&boxH;O)OR5; (CH2)kNR6SO2R5; (CH2)kNR6R5; F; CF3; OCF3; aryl, substituted with to 3 R9; heterocyclyl, substituted with 0 to 3 R9; heteroaryl, substituted with 0 to 3 R9; cycloalkyl, substituted with 0 to 3 R7; or may be taken together with R8 to for a cycloalkyl or heterocyclyl ring; or R7 may be taken together with R11 to form a cycloalkyl or heterocyclyl ring; R8 is hydrogen; F; (C1-C6) alkyl or (C1-C6) alkoxy; R9 is halogen; (C1-C6) alkyl; (C1-C6) alkoxy; (C3-C6) cycloalkyl; (C3-C6) cycloalkoxy; cyano; (CH2)kOH; C(&boxH;O)R5; (CH2)kC(O)NR5R6; (CH2)kNR5R6; (CH2)kNR5SO2R6; CF3; OCF3; SO2NR5R6; (CH2)mC(&boxH;O)OR5; when R9 is attached to a saturated carbon atom R9 may be &boxH;O or &boxH;S; when R9 is attached to a sulphur atom R9 ma be &boxH;O; R10 is hydrogen; C(&boxH;O)R5; C(&boxH;O)OR5; (C1-C6) alkyl; aryl; heterocyclyl; heteroaryl; cycloalkyl; or SO2R5; R11 and R12 are independently hydrogen; (C1-C6) alkyl; hydroxy; cyano; (C1-C6) alkoxy; NR6C(&boxH;O)R5; NR6SO2R5; NR6R5; CF3; F; aryl; heterocyclyl; heteroaryl; cycloalkyl; cycloalkoxy; or R11 may be taken together with R12 to for a cycloalkyl or heterocyclyl ring; and R13 is independently selected from the group consisting of halogen; CF3; (C1-C6) alkyl; aryl; heteroaryl; heterocyclyl; hydroxy; cyano; (C1-C6) alkoxy; (C3-C6) cycloalkyl; (C3-C6) cycloalkoxy; (C2-C6) alkynyl; (C2-C6) alkenyl; -NR6R5; â€”C(&boxH;O)NR5R6; SO2R5; C(&boxH;O)R5; NR5SO2R6; NR5C(&boxH;O)R6; C(&boxH;O)NR5SO2R6; NR5C(&boxH;O)OR6; and SO2NR6R5.