Patent ID: 6635771
Filing Date: 2003-10-21
Classification: C07D

Abstract:
A compound of the formula whereinR is â€”(CH2)nâ€”A, â€”(CH2)nâ€”Sâ€”A, or â€”(CH2)nâ€”Oâ€”A, where A represents: â€ƒD represents C1-C6 alkyl, C1-C6 alkoxy, â€”CF3 or â€”C1-3alkylâ€”CF3, B and C are each independently selected from the group consisting of phenyl, pyridinyl, pyrimidinyl, furanyl, thiophenyl or pyrrolyl groups, each optionally substituted by from 1 to 3, substituents selected independently from the group consisting of H, halogen, â€”CN, â€”CHO, â€”CF3, â€”OCF3, â€”OH, â€”C1-C6 alkyl, C1-C6 alkoxy, â€”NH2 , â€”N(C1-C6)2, â€”NH(C1-C6), â€”Nâ€”C(O)â€”(C1-C6), â€”NO2, or by a 5- or 6-membered heterocyclic or heteroaromatic ring containing 1 or 2 heteroatoms selected from O, N or S; Râ€² is selected from the group consisting of â€”CH2â€”OH, â€”CH2â€”NHâ€”S(O)2â€”(CH2)n2-halo, â€”CH2â€”NHâ€”S(O)2â€”CH&boxH;CH, â€”CH2â€”NH2, or a protected form of â€”CH2â€”NH2; R7 and R8 are independently selected from H, halogen, â€”CN, â€”CHO, â€”CF3, â€”OCF3, â€”OH, â€”C1-C6 alkyl, C1-C6 alkoxy, C1-C6 thioalkyl, â€”NH2, â€”N(C1-C6)2, â€”NH(C1-C6), â€”Nâ€”C(O)â€”(C1-C6), or â€”NO2; R9 represents â€”(CH2)n4â€”CO2H, a C1-C8 alkyl ester of â€”CH2)n4â€”CO2H, or a pharmaceutically acceptable acid mimic or mimetic; R10 is selected from H, halogen, â€”CN, â€”CHO, â€”CF3, â€”OCF3, â€”OH, â€”C1-C6 alkyl, C1-C6 alkoxy, C1â€”C6 thioalkyl, â€”NH2, â€”N(C1-C6)2, â€”NH(C1-C6), â€”Nâ€”C(O)â€”(C1â€”C6), or â€”NO2; R11 is selected from H, halogen, â€”CN, â€”CHO, â€”CF3, â€”OCF3, â€”OH, â€”C1-C6 alkyl, C1-C6 alkoxy, C1-C6 thioalkyl, â€”NH2, â€”N(C1-C6)2, â€”NH(C1-C6), â€”Nâ€”C(O)â€”(C1-C6), â€”NO2, â€”Nâ€”C(O)â€”N(C1-C3 alkyl)2, â€”Nâ€”C(O)â€”NH(C1-C3 alkyl), â€”Nâ€”C(O)â€”Oâ€”(C1-C3 alkyl), â€”SO2â€”C1-C6 alkyl, â€”Sâ€”C3-C6 cycloalkyl, â€”Sâ€”CH2-C3-C6 cycloalkyl, â€”SO2-C3-C6 cycloalkyl, , â€”SO2â€”CH2â€”C3-C6 cycloalkyl, C3-C6 cycloalkyl, â€”CH2â€”C3-C6 cycloalkyl, â€”Oâ€”C3-C6 cycloalkyl, , â€”Oâ€”CH2â€”C3-C6 cycloalkyl, phenyl, benzyl, benzyloxy, morpholino, pyrrolidino, piperidine, piperizine, furan, thiophene, imidazole, tetrazole, pyrazine, pyrazolone, pyrazole, imidazole, oxazole or isoxazole, the rings of each of these groups each being optionally substituted by from 1 to 3 substituents selected from the group of H, halogen, â€”CN, â€”CHO, â€”CF3, â€”OH, â€”C1-C6 alkyl, C1-C6 alkoxy, â€”NH2, â€”N(C1-C6)2, â€”NH(C1-C6), â€”Nâ€”C(O)â€”(C1-C6), â€”NO2, â€”SO2(C1-C3 alkyl), â€”SO2NH(C1-C3 alkyl), â€”SO2N(C1-C3 alkyl)2, or OCF3; n is an integer from 0 to 3; n, is an integer from 0 to 3; n2 is an integer from 0 to 3 n3 is an integer from 0 to 3; n4 is an integer from 0 to 2; and, X is a linking group selected from the group consisting of of â€”Oâ€”, â€”CH2â€”, â€”SO2â€”, â€”NHâ€”, and â€”N(C1-C6-alkyl)â€”.