Patent ID: 6387932
Filing Date: 2002-05-14
Classification: A61P,C07D

Abstract:
A compound represented by structural formula I: wherein:R1 is and is unsubstituted or substituted with a substitutent selected from: 1 to 3 of C1-C6 alkyl, 1 to 3 of halogen, 1 to 2 of â€”OR2, methylenedioxy, â€”S(O)mR2, 1 to 2 of â€”CF3, â€”OCF3, nitro, â€”N(R2)C(O)(R2), â€”C(O)OR2, â€”C(O)N(R2)(R2), -1H-tetrazol-5-yl, â€”SO2N(R2)(R2), â€”N(R2)SO2 phenyl, or â€”N(R2)SO2R2; R2 & R5 are selected from hydrogen, C1-C8 alkyl, (CH2)t aryl, and C3-C7 cycloalkyl, and where two C1-C6 alkyl groups are present on one atom, they optionally are joined to form a C3-C8 cyclic ring, optionally including oxygen, sulfur or NR3a, where R3a is hydrogen, or C1-C6 alkyl, optionally substituted by hydroxyl; aryl is defined within; Aryl is an aromatic ring selected from phenyl and naphthyl; Heteroaryl is a monocyclic aromatic hydrocarbon group having 5 or 6 ring atoms, or a bicyclic aromatic group having 8 to 10 atoms, containing at least one heteroatom selected from O, S or N, in which a carbon or nitrogen atom is the point of attachment, and in which one additional carbon atom is optionally replaced by a heteroatom selected from O or S, and in which from 1 to 3 additional carbon atoms are optionally replaced by nitrogen heteroatoms; R2a is selected from the group consisting of hydrogen and C1-C3 alkyl, said alkyl optionally substituted by hydroxyl; R3 is selected from the group consisting of H, C1-8 alkyl, (CH2)t aryl and (CH2)t heteroaryl; R4 is CH(CO2R2)(CH2)nN(R2)2, CH(R2)â€”(CH2)nN(R2)2, CH(CO2R2), CHCON(R2)2, CH(CO2R2)CH2W(CH2)nN(R2)2, CHR2(CH2)nW(CH2)nN(R2)2, or is selected from R6; R6 is: â€ƒwherein R6 is optionally substituted with 1 to 3 groups of R2, 1 to 3 of halogen, 1 to 2 of â€”OR2, methylenedioxy, â€”S(O)mR2, 1 to 2 of â€”CF3, â€”OCF3, â€”N(R2)C(O)(R2), â€”C(O)OR2, â€”C(O)N(R2)(R2), â€”SO2N(R2)(R2), â€”N(R2)SO2 phenyl, or â€”N(R2)SO2R2; or optionally, â€ƒrepresents one of the following: where W is selected from the group consisting of O, S, CH2, N(R2)C(O) and C(O)N(R2); Y is (H, H) or O; Z is CH; A is CO, SO2, â€ƒ(alkyl having 1-6 carbons), (CH2)xC3-8 cycloalkyl, C3-8 cycloalkyl, aryl, heteroaryl, (CH2)xaryl, (CH2)x heteroaryl, heterocyclyl, C1-C6 alkyl, wherein x is 1-6, wherein each aryl, heteroaryl, heterocyclyl, and cycloalkyl is optionally substituted with 1-6 substituents independently selected from halogen, methylenedioxy, alkyl having 1-6 carbon atoms, O-alkyl having from 1-6 carbon atoms, OH, CN, â€ƒhaving 1-6 carbon atoms, â€ƒhaving 1-6 carbon atoms, wherein each alkyl that is either A or is a substituent on A is optionally substituted with 1-6 halogen atoms and optionally 1-3 substituents selected from aryl, OH, NH2, cycloalkyl optionally having 1-4 C1-C3 alkyl groups, B is C1-C6 alkyl, C3-8cycloalkyl, NH, N(alkyl having 1-6 carbon atoms), O, or a single bond, wherein C3-8cycloalkyl is optionally substituted with 1-6 substituents independently selected from halogen, methylenedioxy, alkyl having 1-6 carbon atoms, O-alkyl having 1-6 carbon atoms, â€ƒhaving 1-6 carbon atoms, wherein each alkyl that is either B or is a substituent on B is optionally substituted with 1-6 halogen atoms and optionally 1-3 substituents selected from aryl, OH, NH2, C3-C8cycloalkyl optionally having 1-4 C1-C3 alkyl groups, andR88 is H, aryl, (CH2)x aryl, heteroaryl, (CH2)x heteroaryl, C3-C8 cycloalkyl, (CH2)x cycloalkyl having 3-8 carbons, C1-C6 alkyl, NH alkyl having 1-6 carbon atoms, N(alkyl)2, where each alkyl is independently a C1-C6 alkyl, â€ƒhaving 1-6 carbons, where x is 1-6 and each aryl, heteroaryl, and cycloalkyl is optionally substituted with 1-6 substituents independently selected from halogen, methylenedioxy, alkyl having 1-6 carbon atoms, O-alkyl having from 1-6 carbon atoms, OH, CN, â€ƒhaving 1-6 carbon atoms, â€ƒhaving 1-6 carbon atoms, wherein each alkyl that is either R88 or is a substituent on R88 is optionally substituted with 1-6 halogen atoms and optionally 1-3 substituents selected from aryl, OH, NH2, cycloalkyl optionally having 1-4 C1-C3 alkyl groups; m is an integer from 0 to 2; n is an integer from 0-5; q is 3; r is 0; and t is an integer from 0 to 3.