Methods of making deuterated cyclosporin analogs
US7538189B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Oct 6, 2005 |
| Grant date | May 26, 2009 |
| Priority date | — |
| Expiry date | Mar 3, 2026 |
Classification
- Technology area (CPC Y)Emerging Cross-Sectional Technologies
- CPC primaryY10S530/807
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
Cyclosporine derivatives are disclosed which possess enhanced efficacy and reduced toxicity over naturally occurring and other presently known cyclosporins and cyclosporine derivatives. The cyclosporine derivatives of the present invention are produced by chemical and isotopic substitution of the cyclosporine A (CsA) molecule by: (1) Chemical substitution and optionally deuterium substitution of amino acid 1; and (2) deuterium substitution at key sites of metabolism of the cyclosporine A molecule such as amino acids 1, 4, 9. Also disclosed are methods of producing the cyclosporine derivatives and method of producing immunosuppression with reduced toxicity with the disclosed cyclosporine derivatives.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.