Benzothiophenes and benzofurans having antiallergic activity.

摘要

There is disclosed a compound having the following general formula (I) <CHEM> or a pharmaceutically acceptable salt thereof, wherein: R<1>, R<4>, and R<5> are each, independently, H, an alkyl having from one to twelve carbon atoms, an alkoxy having from one to twelve carbon atoms, a hydroxy, an aryl, a nitro group, an amino group, a substituted amino group, a mercapto radical, an alkylthio radical having from one to four carbon atoms, an alkylsulphinyl radical having from one to four carbon atoms, an alkylsulphonyl radical having from one to four carbon atoms, an arylthio radical, an arylsulphinyl radical, an arylsulphony radical or a halogen, R<1> being further chosen from a methylenedioxy radical attached to adjacent carbon atoms of the benzene ring; R<2> is an alkoxy having from one to twelve carbon atoms, an arylmethoxy, an amino group, a substituted amino group., a mercapto group, an alkylthio having from one to four carbon atoms, an alkylsulphinyl having from one to four carbon atoms, an alkylsulphonyl having from one to four carbon atoms, an arylthio, an arylsulphinyl, or an arylsulphonyl; and R<3> is A or B <CHEM> X is oxygen or S(O)q wherein q is zero, one, or two. Also disclosed is a process for preparing the compounds, compositions comprising the compounds and pharmaceutical uses of the compounds. The novel benzothiophene and benzofuran derivatives have antiallergic activity. The disclosure describes the use of derivatives for prevention of the release of mediators including histamine and leukotrienes from basophils and mast cells, and prevent respiratory burst in neutrophils providing activity useful in cardiovascular disorders as well as in antiinflammatory, psoriasis, and antimigraine treatment.