Cyclosporine analogue mixtures and their use as immunomodulating agents
US7332472B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Apr 28, 2005 |
| Grant date | Feb 19, 2008 |
| Priority date | — |
| Expiry date | Apr 28, 2025 |
Classification
- Technology area (CPC Y)Emerging Cross-Sectional Technologies
- CPC primaryY10S530/806
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
The invention is directed to isomeric mixtures of cyclosporine analogues that are structurally similar to cyclosporine A. The mixtures possess enhanced efficacy and reduced toxicity over the individual isomers and over naturally occurring and other presently known cyclosporines and cyclosporine derivatives. Embodiments of the present invention are directed toward cis and trans-isomers of cyclosporin A analogs referred to as ISATX247, and derivatives thereof. Mixtures of ISATX247 isomers exhibit a combination of enhanced potency and reduced toxicity over the naturally occurring and presently known cyclosporins. ISATX247 isomers and alkylated, arylated, and deuterated derivatives are synthesized by stereoselective pathways where the particular conditions of a reaction determine the degree of stereoselectivity. The ratio of isomers in a mixture may range from about 10 to 90 percent by weight of the (E)-isomer to about 90 to 10 percent by weight of the (Z)-isomer, based on the total weight of the mixture.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.