IP Library Granted Patent US 9,890,141
Granted Patent B2
US 9,890,141 · App. 15/144,892 · Granted Feb 13, 2018

Crystalline pharmaceutical and methods of preparation and use thereof

Inventor: John Burnier (Pacifica, CA)
Assignee: SARCODE BIOSCIENCE INC.
C07D405/06C07D405/10
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Quick Facts
Patent No.
US 9,890,141
App. No.
15/144,892
Granted
Feb 13, 2018
Kind
B2
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 (9)

1. A composition comprising an isolated compound of Formula I:

wherein said compound is synthesized according to a method comprising the steps:

performing hydrolysis of Formula AA with a base:

wherein R is a carbon containing moiety; and

isolating the compound of Formula I,

wherein the hydrolysis is performed in a solution comprising acetone, the composition is essentially free of a chemical catalyst, and the compound of Formula I is isolated by way of recrystallization from a solution comprising acetone.

2. The composition of claim 1 , wherein R is a substituted or unsubstituted group selected from lower alkyl, lower alkenyl, lower alkynyl, cyclo(lower)alkyl, cyclo(lower)alkenyl, aryl, aralkyl, heterocyclyl, and heteroaryl groups.

3. The composition of claim 1 , wherein R is benzyl.

4. The composition of claim 1 , wherein the base is sodium hydroxide.

Assignments (8)
INTELLECTUAL PROPERTY SECURITY AGREEMENT Recorded Dec 23, 2025
From: BAUSCH + LOMB IRELAND LIMITED
To: JPMORGAN CHASE BANK, N.A., AS COLLATERAL AGENT
Reel/Frame 074050/0573 →
INTELLECTUAL PROPERTY SECURITY AGREEMENT Recorded Dec 23, 2025
From: BAUSCH + LOMB IRELAND LIMITED
To: CITIBANK, N.A., AS NOTES COLLATERAL AGENT
Reel/Frame 074050/0709 →
INTELLECTUAL PROPERTY SECURITY AGREEMENT Recorded Dec 23, 2025
From: BAUSCH + LOMB IRELAND LIMITED
To: CITIBANK, N.A., AS NOTES COLLATERAL AGENT
Reel/Frame 074050/0682 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 6, 2023
From: NOVARTIS PHARMACEUTICALS CORPORATION
To: BAUSCH + LOMB IRELAND LIMITED
Reel/Frame 065789/0853 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 22, 2020
From: NOVARTIS AG
To: NOVARTIS PHARMACEUTICALS CORPORATION
Reel/Frame 054134/0708 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 31, 2019
From: SARCODE BIOSCIENCE INC.
To: NOVARTIS AG
Reel/Frame 050900/0268 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 2, 2017
From: BURNIER, JOHN
To: SARCODE CORPORATION
Reel/Frame 042208/0520 →
CHANGE OF NAME Recorded May 2, 2017
From: SARCODE CORPORATION
To: SARCODE BIOSCIENCE INC.
Reel/Frame 042385/0046 →
Continuity (5)
Continuation 14556715 · Dec 1, 2014
Continuation 13713238 · Dec 13, 2012
Continuation 12909241 · Oct 21, 2010
Provisional Application 61253828 · Oct 21, 2009
Related Publication 20170029410A1 · Feb 2, 2017