Patent ID: 6492374
Filing Date: 2002-12-10
Classification: A61P,C07D

Abstract:
An isobenzofuran having the Formula I: wherein R1 is hydrogen, halogen, trifluoromethyl, trifluoromethylsulfonyloxy, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-8 cycloalkyl, C1-6 alkoxy, hydroxy, formyl, â€”COâ€”C1-6 alkyl, amino, C1-6 alkylamino, C2-12 dialkylamino, â€”NHâ€”COâ€”C1-6 alkyl, C1-6 alkoxycarbonylamino, aminocarbonylamino, C1-6 alkylaminocarbonylamino, C2-12 dialkylaminocarbonylamino, nitro, cyano, COOH, or COOâ€”C1-6 alkyl; R2 and R3 are each independently selected from hydrogen, trifluoromethyl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-8 cycloalkyl and C1-6 alkoxy; n is 1, 2, 3, 4 or 5; m is 0 or 1; A is selected from the following groups; wherein Z is O or S; s is 0 or 1; q is 0 or 1; R4 is hydrogen, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C1-6-alkyl-phenyl, or C1-6-alkyl-O-phenyl; D is a spacer group selected from branched or straight chain C1-6-alkylene, C2-6-alkenylene and C2-6-alkynylene; B is a selected from the group of formula (II), (III) and (IV) wherein R5, R6, R7, R8, R9 and R10 are each independently selected among the R1 substituents; or R8 and R9 together form a fused 5or 6-membered ring optionally containing further heteroatoms; and the resulting heterocycle is optionally substituted with substituents selected among the R1 substituents; or two of the groups of R5, R6 and R7 are linked together thereby forming a â€”Oâ€”(CH2)â€”Oâ€” bridge wherein p is 1 or 2; Ar is independently selected from the group consisting of phenyl, 2-thienyl, 3-thienyl, 2-furanyl, 3-furanyl, 2-pyrimidyl, 1-indolyl, 2-indolyl, 3-indolyl, 1-indol-2-onyl, 3-indol-2-onyl, 2- or 3-benzofuranyl, 2- or 3-benzothiophenyl, 1-napthyl or 2-naphthyl, each optionally substituted with halogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, hydroxy, C1-6 alkylsulfonyl, cyano, trifluoromethyl, trifluoromethylsulfonyloxy, C3-8 cycloalkyl, C3-8 cycloalkyl-C1-6 alkyl, nitro, amino, C1-6 alkylamino, C2-12 dialkylamino, acylamino or alkylenedioxy; its enantiomers, and pharmaceutically acceptable acid addition salt thereof.