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AssigneeAurinia Pharmaceuticals Inc.
InventorsSelvaraj A. Naicker, Randall W Yatscoff, Robert T Foster
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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 comprises from about 70 to about 80 percent by weight of the E-isomer and from about 20 to about 30 percent by weight of the Z-isomer, based on the total weight of the mixture.
A composition comprising an isomeric mixture of cyclosporine analogues modified at the 1-amino acid residue with a 1,3-diene substituent, wherein the isomeric mixture comprises from about 70% to about 80% of the E-isomer and from about 20% to about 30% of the Z-isomer, wherein the isomers are the E- and Z-isomers as specified below:
Dependencies are inferred from the claim text.