IP Library Granted Patent US 8,450,332
Granted Patent B2
US 8,450,332 · App. 13/486,122 · Granted May 28, 2013

LIMK2 inhibitors, compositions comprising them, and methods of their use

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Quick Facts
Patent No.
US 8,450,332
App. No.
13/486,122
Granted
May 28, 2013
Kind
B2
Abstract

Inhibitors of LIM kinase 2 are disclosed, along with pharmaceutical compositions comprising them and methods of their use. Particular compounds are of the formula:

Claims (11)

1. A method of lowering intraocular pressure in a patient, which comprises administering to a patient in need thereof a therapeutically or prophylactically effective amount of a compound of the formula:

or a pharmaceutically acceptable salt thereof, wherein:

R 3A is cyano, C(O)R 3C , CO 2 R 3C , CON(R 3C ) 2 , or optionally substituted alkyl, alkylaryl, alkylheterocycle, aryl, heteroalkyl, heteroalkylaryl, heteroalkylheterocycle, or heterocycle;

each R 3C is independently optionally substituted alkyl, aryl or heterocycle; and

each R 4A is independently hydrogen or optionally substituted alkyl or heteroalkyl.

2. The method of claim 1 , wherein R 3A is heteroalkyl.

3. The method of claim 2 , wherein R 3A is aminomethyl, (dimethylamino)methyl, or (dimethylamino)ethyl.

4. The method of claim 1 , wherein at least one R 4A is methyl.

5. The method of claim 1 , wherein the compound is 3-(4-(aminomethyl)-1-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamido)phenyl dimethylcarbamate.

6. The method of claim 1 , wherein the compound is administered in a pharmaceutical formulation comprising a liquid vehicle suitable for ophthalmic administration.

7. A method of lowering intraocular pressure in a patient, which comprises administering to a patient in need thereof a therapeutically effective amount of a pharmaceutical formulation comprising 3-(4-(aminomethyl)-1-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamido)phenyl dimethylcarbamate and a liquid vehicle suitable for ophthalmic administration.

Assignments (4)
RELEASE OF SECURITY INTEREST Recorded May 5, 2026
From: OXFORD FINANCE LLC
To: LEXICON PHARMACEUTICALS, INC.; LEXICON PHARMACEUTICALS
Reel/Frame 075545/0601 →
SECURITY INTEREST Recorded Mar 17, 2022
From: LEXICON PHARMACEUTICALS, INC.
To: OXFORD FINANCE LLC, AS COLLATERAL AGENT
Reel/Frame 059432/0709 →
RELEASE OF SECURITY INTEREST Recorded Sep 14, 2020
From: BIOPHARMA CREDIT PLC
To: LEXICON PHARMACEUTICALS, INC.
Reel/Frame 053767/0445 →
SECURITY INTEREST Recorded Dec 20, 2017
From: LEXICON PHARMACEUTICALS, INC.
To: BIOPHARMA CREDIT PLC
Reel/Frame 044958/0377 →