C - Chemistry – Metallurgy – 07 – H
Patent
C - Chemistry, Metallurgy
07
H
C07H 19/01 (2006.01) A61K 31/71 (1990.01)
Patent
CA 2077638
155/JET78 157/JET79 163/JET84 168/JET86 18514 TITLE OF THE INVENTION N-HETEROARYL, N-ALKYLHETEROARYL, N-ALKENYLHETEROARYL AND N-ALKYNYLHETEROARYLMACROLIDES HAVING IMMUNOSUPPRESSIVE ACTIVITY ABSTRACT OF THE DISCLOSURE N-Heteroaryl, N-alkylheteroaryl, N-alkenyl- heteroaryl and N-alkynylheteroaryl macrolides of the general structural Formula I: Image I 155/JET78 -ii- 18514 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 hyperpro- liferative 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.
Goulet Joung
Ok Hyun O.
Sinclair Peter J.
Goulet Joung
Merck & Co. Inc.
Ok Hyun O.
Sinclair Peter J.
Swabey Ogilvy Renault
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