Cyclosporin analogs

Patent metadata

Field	Value
Publication number	US-9493511-B2
Application number	US-201414534677-A
Country	US
Kind code	B2
Filing date	Nov 6, 2014
Priority date	Oct 12, 2010
Publication date	Nov 15, 2016
Grant date	Nov 15, 2016

Abstract

Disclosed herein are novel analogs of cyclosporin, pharmaceutical compositions containing them, and methods for their use in the treatment of dry eye and other conditions.

First claim

We claim:

1. A compound selected from the group consisting of:
[(S)-2-diethylaminoethylthiomethyl-Sar] 3 cyclosporin A;
[(S)-2-(4-pyridyl)ethylthiomethyl-Sar] 3 cyclosporin A;
[(S)-2-aminoethylthiomethyl-Sar] 3 cyclosporin A;
[(S)-2-dimethylaminoethylthiomethyl-Sar] 3 cyclosporin A;
[(S)-(4-methylpiperidinyl)thiomethyl-Sar] 3 cyclosporin A;
[(S)-2-(morpholino)ethylthiomethyl-Sar] 3 cyclosporin A; and
[(S)-2-isopropylaminoethylthiomethyl-Sar] 3 cyclosporin A;
and pharmaceutically acceptable salts of the foregoing compounds.

2. The compound of claim 1 , which is [(S)-2-diethylaminoethylthiomethyl-Sar] 3 cyclosporin A, or a pharmaceutically acceptable salt thereof.

3. A pharmaceutical composition comprising a compound of claim 1 or 2 , the compound being present alone or in combination with one or more pharmaceutically acceptable excipients.

4. The pharmaceutical composition of claim 3 , wherein the concentration of the compound in the composition is about 0.01 to about 0.05 weight percent.

Assignees

• Allergan Inc

Inventors

• Frydrych Catherine Simone Victoire
• Carling William Robert
• Garst Michael E
• Stern Michael E
• Schaumburg Christopher S

Classifications

• A61P37/08

  Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14) · CPC title

• A61P31/22

  for herpes viruses · CPC title

• A61P37/06

  Immunosuppressants, e.g. drugs for graft rejection · CPC title

• A61P27/02

  Ophthalmic agents · CPC title

• C07K7/645 Primary

  Cyclosporins; Related peptides · CPC title