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Last Updated: April 19, 2024

Details for Patent: 9,708,303


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Title:LFA-1 inhibitor and methods of preparation and polymorph thereof
Abstract: Methods of preparation and purification of a compound of Formula I, intermediates thereof, a polymorph thereof, and related compounds are disclosed. Formulations and uses thereof in the treatment of LFA-1 mediated diseases are also disclosed. ##STR00001##
Inventor(s): Zeller; James Robert (Scottsdale, AZ), Venkatraman; Sripathy (Slingerlands, NY), Brot; Elisabeth C. A. (Albany, NY), Iyer; Subashree (Guilderland, NY), Hall; Michael (Albany, NY)
Assignee: SARCODE BIOSCIENCE INC. (Brisbane, CA)
Filing Date:Jun 23, 2015
Application Number:14/747,745
Claims:1. A method of purifying a compound of Formula I: ##STR00029## or a salt thereof, comprising the steps: a) obtaining crude compound of Formula I or a salt thereof and recrystallizing said crude compound with aqueous acetone; and b) isolating said compound of Formula I or a salt thereof by removal of aqueous acetone.

2. The method of claim 1, wherein said aqueous acetone is used in an amount of about 7 volumes.

3. The method of claim 1, wherein said aqueous acetone is about 30% aqueous acetone.

4. The method of claim 1, further comprising addition of a pH modifier to produce a pH of less than about 5.

5. The method of claim 4, wherein said method produces a pH between about 1 and about 5.

6. The method of claim 4, wherein said pH modifier is selected from an organic or mineral acid.

7. The method of claim 4, wherein said pH modifier is hydrochloric acid.

8. The method of claim 1, wherein said removal of aqueous acetone is by filtration.

9. The method of claim 1, wherein said method is performed for a period of time ranging from about 1 hour to about 48 hours.

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