The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Sep. 19, 2017

Filed:

Nov. 23, 2015
Applicant:

Aurinia Pharmaceuticals Inc., Victoria, CA;

Inventors:

Selvaraj A. Naicker, Edmonton, CA;

Randall W Yatscoff, Edmonton, CA;

Robert T Foster, Edmonton, CA;

Assignee:

Aurinia Pharmaceuticals Inc., Victoria, B.C., CA;

Attorneys:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
A61K 45/00 (2006.01); A61K 47/00 (2006.01); A61K 38/12 (2006.01); C07K 5/00 (2006.01); C07K 7/00 (2006.01); C07K 16/00 (2006.01); C07K 17/00 (2006.01); C07K 7/64 (2006.01); A61K 9/00 (2006.01); A61K 9/107 (2006.01); A61K 9/48 (2006.01); A61K 38/13 (2006.01); B82Y 5/00 (2011.01); A61K 38/00 (2006.01);
U.S. Cl.
CPC ...
C07K 7/645 (2013.01); A61K 9/0095 (2013.01); A61K 9/1075 (2013.01); A61K 9/4858 (2013.01); A61K 38/13 (2013.01); B82Y 5/00 (2013.01); C07K 7/64 (2013.01); A61K 38/00 (2013.01); Y10S 530/806 (2013.01);
Abstract

The invention is directed to isomeric mixtures of cyclosporine analogs 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 ISA247, and derivatives thereof. Mixtures of ISA247 isomers exhibit a combination of enhanced potency and reduced toxicity over the naturally occurring and presently known cyclosporins. ISA247 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 greater than about 80 percent by weight of the E-isomer and less than about 20 percent by weight of the Z-isomer, based on the total weight of the mixture.


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