IP Library Granted Patent US 9,682,982
Granted Patent B2
US 9,682,982 · App. 14/658,653 · Granted Jun 20, 2017

Inhibitors of adapter associated kinase 1, compositions comprising them, and methods of their use

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Quick Facts
Patent No.
US 9,682,982
App. No.
14/658,653
Granted
Jun 20, 2017
Kind
B2
Abstract

The adaptor associated kinase 1 (AAK1) inhibitor 3-methyloxetan-3-yl-4-(3-(2-methoxypyridin-3-yl)pyrazolo[1,5-a]pyrimidin-5-yl)piperazine-1-carboxylate: and pharmaceutically acceptable salts and solid forms thereof are disclosed. Compositions comprising the compound and methods of their use to treat, manage and/or prevent diseases and disorders mediated by mediated by AAK1 activity are also disclosed.

Claims (11)

1. A compound, which is 3-methyloxetan-3-yl-4-(3-(2-methoxypyridin-3-yl)pyrazolo[1,5-a]pyrimidin-5-yl)piperazine-1-carboxylate:

or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1 , which is crystalline.

3. The compound of claim 2 , which has a melting point of about 182.5° C.

4. The crystalline compound of claim 2 , which has an X-ray powder diffraction pattern with peaks at about 12.7, 14.8, 18.7, 19.0, 19.7 and/or 25.1 degrees 2θ.

5. A method of inhibiting adaptor associated kinase 1 (AAK1) activity, comprising contacting AAK1 with a compound of claim 1 .

6. A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable excipient or diluent.

7. A method of treating or managing a disease or disorder mediated by AAK1 activity, which comprises administering to a patient in need thereof a therapeutically effective amount of a compound of claim 1 , or a pharmaceutical composition of claim 6 .

8. The method of claim 7 , wherein the disease or disorder is Alzheimer's disease, bipolar disorder, pain, Parkinson's disease, or schizophrenia.

9. The method of claim 8 , wherein the pain is neuropathic pain.

10. The method of claim 9 , wherein the neuropathic pain is fibromyalgia or peripheral neuropathy.

Assignments (4)
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 May 11, 2015
From: BI, YINGZHI; KUMI, GODWIN
To: LEXICON PHARMACEUTICALS, INC.
Reel/Frame 035606/0634 →