Hydrogenated benzo(C)thiophene derivatives as immunomodulators

摘要

Disclosed is a hydrogenated benzo(C)thiophene derivative of Formula (I), or a stereoisomer, salt, solvate, or polymorph thereof, wherein A is -CONH-CH2-, -CO-CH=CH-, -CO-CH2CH2-, -CO-CH2-O-, -CO-CH2-NH-, or an oxadiazole, and wherein the other substituents are as defined in the specification. Also disclosed is the use of the compound for treating diseases and disorders associated with an activated immune system, such as rejection of transplanted organs selected from kidney, liver, heart and lung; graft-versus-host diseases brought about by stem cell transplantation; autoimmune syndromes selected from rheumatoid arthritis, multiple sclerosis, psoriasis, psoriatic arthritis, Crohn's disease, and Hashimoto's thyroiditis; and atopic dermatitis. Also disclosed is the intermediate compound of formula (II), or a stereoisomer, salt, solvate, or polymorph thereof, wherein R8 is hydroxyl, C1-5alkoxy, or methyl, and wherein the other substituents are as for Formula (I).