IP Library Granted Patent US 9,394,308
Granted Patent B2
US 9,394,308 · App. 14/160,333 · Granted Jul 19, 2016

Inhibiting the transient receptor potential A1 ion channel

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Quick Facts
Patent No.
US 9,394,308
App. No.
14/160,333
Granted
Jul 19, 2016
Kind
B2
Abstract

This disclosure describes novel compounds and pharmaceutical compositions for inhibiting the TRPA1 ion channel and/or medical conditions related to TRPA1, such as pain and respiratory conditions.

Claims (26)

1. A compound of Formula (I), or a pharmaceutically acceptable salt thereof:

wherein,

R 1 is hydrogen or —CH 2 —R 1a , wherein R 1a is a phosphate moiety;

R 2 is CH 3 ;

R 3 is CH 3 ; and

A is N or CH.

2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein the compound of Formula (I) is a compound of Formula (Ia)

3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein A is CH.

4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein A is N.

5. A compound of Formula (I), or a pharmaceutically acceptable salt thereof:

wherein,

R 1 is hydrogen or —CH 2 —R 1a , wherein R 1a is a phosphate moiety;

R 2 is hydrogen;

R 3 is CH 3 ; and

A is N.

6. A compound selected from:

(S)-2-(1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)-N-(6-(2-(2,2-dimethylpyrrolidin-1-yl)pyrimidin-5-yl)pyrazin-2-yl)propanamide,

(S)-2-(1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)-N-(6-(2-((S)-2-methylpyrrolidin-1-yl)pyrimidin-5-yl)pyrazin-2-yl)propanamide,

or a pharmaceutically acceptable salt thereof.

7. A compound of Formula (I), or a pharmaceutically acceptable salt thereof:

wherein,

R 1 is hydrogen or —CH 2 —R 1a , wherein R 1a is a phosphate moiety;

R 2 is hydrogen;

R 3 is CH 3 ; and

A is CH.

8. The compound of claim 7 , or a pharmaceutically acceptable salt thereof, wherein R 1 is hydrogen.

Assignments (5)
MERGER Recorded Aug 8, 2022
From: MERCK SHARP & DOHME CORP.
To: MERCK SHARP & DOHME LLC
Reel/Frame 061102/0145 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 17, 2016
From: LIPPA, BLAISE S.; LI, QINGYI; CHENG, LILY; LIU, CHRISTOPHER M.; WRONA, IWONA E.; METCALF, CHESTER A., III; JACKSON, ANDREW J.
To: CUBIST PHARMACEUTICALS, INC.
Reel/Frame 037844/0747 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 9, 2015
From: CUBIST PHARMACEUTICALS LLC
To: MERCK SHARP & DOHME CORP.
Reel/Frame 036046/0602 →
CHANGE OF NAME Recorded Jul 9, 2015
From: CUBIST PHARMACEUTICALS, INC.
To: CUBIST PHARMACEUTICALS LLC
Reel/Frame 036084/0448 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 8, 2015
From: CHAPMAN, LAUREN M.
To: CUBIST PHARMACEUTICALS, INC.
Reel/Frame 036018/0883 →