Amino O-alkyl, O-alkenyl and O-alkynlmacrolides having immunosup

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514 63, 540452, 540456, A61K 31395, A61K 31695, C07D49816, C07F 701

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active

051623340

ABSTRACT:
Amino O-alkyl, O-alkenyl and O-alkynylmacrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by alkylation and amination at C-3"/C-4" of the cyclohexyl ring. These macrolide immunosuppressants 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.

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