O-aryl, o-alkyl, o-alkenyl and o-alkynylmacrolides having...

Details O-aryl, o-alkyl, o-alkenyl and o-alkynylmacrolides having... O-aryl, o-alkyl, o-alkenyl and o-alkynylmacrolides having...

C - Chemistry, Metallurgy

07

H

C07H 19/01 (2006.01) C07D 498/18 (2006.01)

Patent

CA 2068561

TITLE OF THE INVENTION O-ARYL, O-ALKYL, O-ALKENYL AND O-ALKYNYLMACROLIDES HAVING IMMUNOSUPPRESSIVE ACTIVITY ABSTRACT OF THE DISCLOSURE O-Aryl, O-alkyl, O-alkenyl and O-alkynyl- macrolides of the general structural Formula I: Image have been prepared from suitable precursors by alkylation and/or arylation at C-3" and/or C-4" of the cyclohexyl ring. These macrolide immunosup- pressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. In addition, these macrolide immunosuppressants are useful in the topical treatment of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses. Also, these macrolides are useful in the treatment of reversible obstructive airways disease, particularly asthma; as hair revitalizing agents, especially in the treatment of male pattern alopecia or alopecia senilis; in the reversal of multidrug resistance of tumor cells; in treatment of inflammation of mucosa and blood vessels, gastric ulcers, vascular damage, ischemic bowel disease, inflammatory bowel disease, necrotizing enterocolitis, intestinal lesions associated with thermal burns; in the treatment of cytomegalovirus infection; and in the treatment of idiopathic thrombocytopenic purpura and Basedow's disease.

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