N-heteroaryl, N-alkylheteroaryl, N-alkenylheteroaryl and N-alkynylheteroarylmacrolides having immunosuppressive activity
US5208241A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Sep 9, 1991 |
| Grant date | May 4, 1993 |
| Priority date | — |
| Expiry date | Sep 9, 2011 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61P37/06
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.