Crystalline pharmaceutical and methods of preparation and use thereof

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Quick Facts

Patent No.: US 8,871,935
App. No.: 13/710,651
Granted: Oct 28, 2014
Kind: B2

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Abstract

Novel crystalline polymorphic forms, Forms A, B, C, D, and E of a compound of Formula I, which has been found to be a potent inhibitor of LFA-1, are disclosed. Methods of preparation and uses thereof in the treatment of LFA-1 mediated diseases are also disclosed in this invention.

Claims (6)

1. A method of synthesizing a compound of Formula I:

comprising the steps:

a) hydrogenolyzing an ester of Formula A with a palladium catalyst and a source of protons; and

b) isolating a compound of Formula I.

2. The method of claim 1 , wherein the palladium catalyst is 10% palladium on carbon.

3. The method of claim 1 , wherein the proton source is formic acid.

Assignments (8)

INTELLECTUAL PROPERTY SECURITY AGREEMENT Recorded Dec 23, 2025

From: BAUSCH + LOMB IRELAND LIMITED

To: CITIBANK, N.A., AS NOTES COLLATERAL AGENT

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