Cyclosporine analogue mixtures and their use as immunomodulating agents
USRE48226E1 · kind E1 · reissue
Assignee
Inventors
Key dates
| Filing date | Jun 30, 2014 |
| Grant date | Sep 29, 2020 |
| Priority date | — |
| Expiry date | Jun 30, 2034 |
Classification
- Technology area (CPC —)General
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.