IP Library Granted Patent US 8,193,202
Granted Patent B2
US 8,193,202 · App. 12/426,661 · Granted Jun 5, 2012

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

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Quick Facts
Patent No.
US 8,193,202
App. No.
12/426,661
Granted
Jun 5, 2012
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 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 compound of claim 1 , wherein R 3A is heteroalkyl.

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

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

5. A compound, or a pharmaceutically acceptable salt thereof, which is 3-(4-(aminomethyl)-1-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamido)phenyl dimethylcarbamate.

6. A pharmaceutical formulation comprising a liquid vehicle suitable for ophthalmic administration and a compound of claim 1 .

7. A pharmaceutical formulation comprising a liquid vehicle suitable for ophthalmic administration and a compound of claim 5 .

Assignments (6)
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 May 4, 2026
From: LEXICON PHARMACEUTICALS, INC.; LEXICON PHARMACEUTICALS (NEW JERSEY), INC.; LION ACQUISITION CORPORATION
To: HERCULES CAPITAL, INC., AS AGENT
Reel/Frame 075498/0899 →
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 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 8, 2009
From: BURGOON, HUGH ALFRED; GOODWIN, NICOLE CATHLEEN; HARRISON, BRYCE ALDEN; HEALY, JASON PATRICK; LIU, YING; MABON, ROSS; MARINELLI, BRETT; RAWLINS, DAVID BRENT; RICE, DENNIS STEWART; WHITLOCK, NORRIS ANDREW
To: LEXICON PHARMACEUTICALS, INC.
Reel/Frame 022791/0339 →