N-heteroaryl, N-alkylheteroaryl, N-alkenylheteroaryl and N-alkyn

Details N-heteroaryl, N-alkylheteroaryl, N-alkenylheteroaryl and N-alkyn N-heteroaryl, N-alkylheteroaryl, N-alkenylheteroaryl and N-alkyn

1991-09-09

1993-05-04

Bond, Robert T.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514183, 514411, 540456, C07D52100, A61K 31395

Patent

active

052082415

ABSTRACT:
N-Heteroaryl, N-alkylheteroaryl, N-alkenylheteroaryl and N-alkynylheteroaryl macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by amination, alkylation and/or arylation at C-3" and/or 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. Furthermore, these macrolides are useful as hair revitalizing agents, especially in the treatment of male pattern alopecia or alopecia senilis.

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