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Last Updated: April 19, 2024

Claims for Patent: 7,906,489


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Summary for Patent: 7,906,489
Title:18-membered macrocycles and analogs thereof
Abstract: The present invention relates generally to the 18-membered macrocyclic antimicrobial agents called Tiacumicins, specifically, OPT-80 (which is composed almost entirely of the R-Tiacumicin B), pharmaceutical compositions comprising OPT-80, and methods using OPT-80. In particular, this compound is a potent drug for the treatment of bacterial infections, specifically C. difficile infections.
Inventor(s): Shue; Youe-Kong (Carlsbad, CA), Hwang; Chan-Kou (San Diego, CA), Chiu; Yu-Hung (San Diego, CA), Romero; Alex (San Diego, CA), Babakhani; Farah (San Diego, CA), Sears; Pamela (San Diego, CA), Okumu; Franklin (Oakland, CA)
Assignee: Optimer Pharmaceuticals, Inc. (San Diego, CA)
Application Number:11/882,219
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 7,906,489
Patent Claims: 1. A method of treating diarrhea caused by C. difficile gastrointestinal infection in a human patient in need thereof comprising orally administering to said patient a therapeutically effective amount of a compound having the formula (IV): ##STR00023## or a pharmaceutically acceptable salt combined with one or more pharmaceutically acceptable carriers, wherein the compound having formula (IV) is greater than 90% by weight stereomerically pure.

2. The method of claim 1, wherein the compound of formula (IV) is formulated as a tablet.

3. The method of claim 1, wherein the compound of formula (IV) is formulated as a capsule.

4. The method of claim 1, wherein the compound of formula (IV) is greater than 93% by weight stereomerically pure.

5. The method of claim 1, wherein the compound of formula (IV) is greater than 95% by weight stereomerically pure.

6. The method of claim 1, wherein the compound of formula (IV) is greater than 97% by weight stereomerically pure.

7. The method of claim 1, wherein the compound of formula (IV) is substantially free of other diastereomers of the compound.

8. The method of claim 1, wherein the method consists of administering to the human patient a therapeutically effective amount of the compound having formula (IV) or a pharmaceutically acceptable salt thereof combined with one or more pharmaceutically acceptable carriers.

9. A method of treating diarrhea caused by C. difficile gastrointestinal infection in a human patient in need thereof consisting of orally administering to said patient a therapeutically effective amount of a compound having the formula (IV): ##STR00024## or a pharmaceutically acceptable salt thereof combined with one or more pharmaceutically acceptable carriers, wherein the compound of the formula (IV) is greater than 93% by weight stereomerically pure.

10. The method of claim 9, wherein the compound of formula (IV) is formulated as a tablet.

11. The method of claim 9, wherein the compound is formulated as a capsule.

12. The method of claim 9, wherein the compound of formula (IV) is greater than 95% by weight stereomerically pure.

13. The method of claim 9, wherein the compound of formula (IV) is greater than 97% by weight stereomerically pure.

14. The method of claim 9, wherein the compound of formula (IV) is substantially free of other diastereomers of the compound.

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