IP Library Granted Patent US 12,648,939
Granted Patent B2
US 12,648,939 · App. 18/133,926 · Granted Jun 9, 2026

Compounds and methods for treating spasticity

Inventors: Suma Gopinathan (The Woodlands, TX); Praveen Tyle (Spring, TX); Qi Melissa Yang (The Woodlands, TX)
Assignee: LEXICON PHARMACEUTICALS, INC.
A61K31/444A61P21/00A61P21/02A61P25/14
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Quick Facts
Patent No.
US 12,648,939
App. No.
18/133,926
Granted
Jun 9, 2026
Kind
B2
Abstract

Provided herein are methods of treating and preventing spasticity in a patient in need thereof. A particular method comprises administering an effective amount of an adaptor associated kinase 1 inhibitor of Formula (I):

Claims (28)

1 . A method of treating or preventing cerebral spasticity, which comprises administering a therapeutically or prophylactically effective amount of an adaptor associated kinase 1 (AAK1) inhibitor to a patient in need thereof, wherein the AAK1 inhibitor is a compound of Formula (I):

or a pharmaceutically acceptable salt thereof, wherein:

A is selected from

wherein “ ” denotes the point of attachment to B;

B is selected from

wherein “*” indicates the point of attachment to R 5 and “**” indicates the point of attachment to ring A;

R 1 is selected from hydrogen, amino, —CO 2 H, difluoromethyl, ethyl, halo, hydroxymethyl, methoxy, methyl, —NHC(O)CH 3 , —NHCO 2 CH 3 , trifluoromethoxy, and trifluoromethyl;

R 2 is selected from hydrogen, cyano, —CH 2 OH, halo, and methyl;

R 3 is selected from hydrogen, cyano, cyclopropyl, difluoromethyl, halo, hydroxymethyl, methoxy, methyl, methylsulfonyl, trifluoromethoxy, trifluoromethyl, —CH 2 N(CH 3 ) 2 , and a five-membered aromatic ring containing one, two, or three heteroatoms selected from nitrogen, oxygen, and sulfur;

R 4 is selected from hydrogen, halo, and methyl;

R 5 is selected from

R 6 is selected from hydrogen, ethyl, fluoromethyl, difluoromethyl, methyl, and trifluoromethyl; and

R 7 is methyl.

2 . The method of claim 1 , wherein the AAK1 inhibitor is a compound of Formula (II):

or a pharmaceutically acceptable salt thereof, wherein:

A is selected from

R 1 is selected from hydrogen, difluoromethyl, halo, methoxy, methyl, —NHC(O)CH 3 , —NHCO 2 CH 3 , and trifluoromethyl;

R 2 is selected from hydrogen, —CH 2 OH, and halo; and

R 3 is selected from hydrogen, cyano, cyclopropyl, difluoromethyl, halo, hydroxymethyl, methoxy, methyl, trifluoromethoxy, trifluoromethyl, and a five-membered aromatic ring containing one, two, or three heteroatoms selected from nitrogen, oxygen, and sulfur.

3 . The method of claim 2 , wherein A is

4 . The method of claim 2 , wherein B is

5 . The method of claim 1 , wherein the patient suffers from amyotrophic lateral sclerosis, cerebral palsy, multiple sclerosis, or stroke.

6 . A method of treating or preventing cerebral spasticity which comprises administering a therapeutically or prophylactically effective amount of an adaptor associated kinase 1 (AAK1) inhibitor to a patient in need thereof, wherein the AAK1 inhibitor is(S)-1-((2′,6-bis(difluoromethyl)-[2,4′-bipyridin]-5-yl)oxy)-2,4-dimethylpentan-2-amine:

or a pharmaceutically acceptable salt thereof.

7 . The method of claim 6 , wherein the AAK1 inhibitor is ((S)-1-((2′,6-bis(difluoromethyl)-[2,4′-bipyridin]-5-yl)oxy)-2,4-dimethylpentan-2-aminium dihydrogen phosphate.

8 . The method of claim 7 , wherein the AAK1 inhibitor has a melting point of 184±2° C.

9 . The method of claim 6 , wherein the patient suffers from amyotrophic lateral sclerosis, cerebral palsy, multiple sclerosis, or stroke.

10 . The method of claim 6 , wherein the AAK1 inhibitor is administered orally.

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 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 Aug 16, 2023
From: LEXICON PHARMACEUTICALS, INC.
To: OXFORD FINANCE LLC
Reel/Frame 064608/0846 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 29, 2023
From: GOPINATHAN, SUMA; TYLE, PRAVEEN; YANG, QI MELISSA
To: LEXICON PHARMACEUTICALS INC.
Reel/Frame 064111/0595 →
Continuity (2)
Provisional Application 63331547 · Apr 15, 2022
Related Publication 20230330074A1 · Oct 19, 2023
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