IP Library Granted Patent US 10,946,031
Granted Patent B2
US 10,946,031 · App. 16/593,171 · Granted Mar 16, 2021

PDE4 inhibitor (R)-4-(5-(4-methoxy-3-propoxyphenyl)pyridin-3-yl)-1,2-oxaborolan-2-ol

Inventors: Joseph Walter Strohbach (Wentzville, MO); David Clive Blakemore (East Lyme, CT); Peter Jones (Sharon, MA); Matthew Alexander Perry (Uncasville, CT)
Assignee: Pfizer Inc.
A61K31/69A61K31/519C07F5/025C07B2200/13
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Quick Facts
Patent No.
US 10,946,031
App. No.
16/593,171
Granted
Mar 16, 2021
Kind
B2
Abstract

The present invention relates to PDE4 inhibitor (R)-4-(5-(4-methoxy-3-propoxyphenyl)pyridin-3-yl)-1,2-oxaborolan-2-ol including the crystalline monohydrate thereof.

Claims (12)

1. A compound of the structure

or a pharmaceutically acceptable salt thereof.

2. A compound of the structure

3. A compound of the structure

wherein the compound is characterized by a powder X-ray diffraction pattern comprising diffraction peaks at angles (2θ) of 11.0° 0 0.2°, 22.9°±0.2°, and 25.1°±0.2°.

4. The compound of claim 3 , wherein the compound is further characterized by a powder X-ray diffraction pattern comprising additional diffraction peaks at angles (2θ) of 11.4°±0.2°, 18.8°±0.2°, and 26.4°±0.2°.

5. The compound of claim 3 , wherein the compound is further characterized by a powder X-ray diffraction pattern comprising additional diffraction peaks at angles (2θ) of 11.4±0.2°, 13.2°±0.2°, 18.8°±0.2, 19.7°±0.2°, 21.3±0.2°, 2 and 26.4±0.2°.

6. The compound of claim 3 , wherein the compound is further characterized by a powder X-ray diffraction pattern comprising additional diffraction peaks at angles (2θ) of 11.4°±0.2, 13.2°±0.2°, 14.5°±0.2°, 15.1°±0.2°, 15.6°±0.2°, 18.8°±0.2°, 19.7°±0.2°, 21.3°±0.2°, and 26.4°±0.2°.

7. The compound of claim 3 , wherein the compound is further characterized by a powder X-ray diffraction pattern comprising additional diffraction peaks at angles (2θ) of 11.4°±0.2, 13.2°±0.2°, 14.5°±0.2°, 15.1°±0.2°, 15.6°±0.2°, 18.8°±0.2°, 19.4°±0.2°, 19.7°±0.2°, 21.3°±0.2°, 25.9°±0.2°, 26.4°±0.2°, and 27.5°±0.2°.

8. The compound of claim 3 , wherein the compound is further characterized by a powder X-ray diffraction pattern comprising additional diffraction peaks at angles (2θ) of 11.4°±0.2, 13.2°±0.2°, 14.5°±0.2°, 15.1°±0.2°, 15.6°±0.2°, 15.9°±0.2°, 17.7°±0.2°, 18.8°±0.2°, 19.4°±0.2°, 19.7°±0.2°, 20.5°±0.2°, 21.3°±0.2°, 25.9°±0.2°, 26.4°±0.2°, and 27.5°±0.2°.

9. The compound of claim 3 , wherein the compound is further characterized by a powder X-ray diffraction pattern comprising additional diffraction peaks at angles (2θ) of 11.4°±0.2°, 13.2°±0.2°, 14.5°±0.2°, 15.1°±0.2°, 15.6°±0.2°, 15.9°±0.2°, 17.7°±0.2°, 18.8°±0.2°, 19.4°±0.2°, 19.7°±0.2°, 20.5°±0.2°, 21.3°±0.2°, 22.0°±0.2°, 24.5°±0.2°, 25.9°±0.2°, 26.4°±0.2°, 27.5°±0.2°, and 28.4°±0.2°.

10. The compound of claim 3 , wherein the compound is further characterized by a powder X-ray diffraction pattern comprising additional diffraction peaks at angles (2θ) of 11.4°±0.2°, 13.2°±0.2°, 14.5°±0.2°, 15.1°±0.2°, 15.6°±0.2°, 15.9°±0.2°, 17.7°±0.2°, 18.8°±0.2°, 19.4°±0.2°, 19.7°±0.2°, 2.5°±0.2°, 21.3°±0.2°, 22.0°±0.2°, 23.8°±0.2°, 24.5°±0.2°, 25.6°±0.2°, 25.9°±0.2°, 26.4°±0.2°, 27.5°±0.2°, 28.4°±0.2°, 28.8°±0.2°, and 30.4°±0.2°.

Assignments (1)
ASSIGNEE ADDRESS CORRECTION Recorded Mar 20, 2023
From: PFIZER INC.
To: PFIZER INC.
Reel/Frame 063119/0087 →