Amino O-aryl macrolides having immunosuppressive activity
US5262533A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | May 6, 1992 |
| Grant date | Nov 16, 1993 |
| Priority date | — |
| Expiry date | May 6, 2012 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D498/18
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
Amino O-aryl macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by arylation 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; 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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.