IP Library Granted Patent US 9,334,265
Granted Patent B2
US 9,334,265 · App. 14/639,241 · Granted May 10, 2016

3-amino-pyrazole derivatives useful against tuberculosis

Inventors: Julia Castro Pichel (Madrid, ES); Raquel Fernandez Menendez (Madrid, ES); Esther Pilar Fernandez Velando (Madrid, ES); Silvia Gonzalez Del Valle (Madrid, ES)
Assignee: Glaxo Group Limited
C07D417/14C07D471/04
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 9,334,265
App. No.
14/639,241
Granted
May 10, 2016
Kind
B2
Abstract

A compound of Formula (I) or a pharmaceutically acceptable salt thereof: Wherein: Het is a 5 to 10-membered heteroaromatic ring; Either X is N and Y is CR 5 ; or X is C and Y is S; Z is selected from N and CH; R 1 is selected from H and C 1-2 alkyl; R 2 is selected from H, C 1-2 alkyl, OH, —CH 2 OH and C 1-2 alkoxy; Each R 3 is independently selected from OH, C 1-3 alkyl, F, Cl, Br, NH 2 , and C 1-3 alkoxy; R 4 is selected from C 1-3 alkyl and haloC 1-3 alkyl; R 5 is selected from H, C 1-3 alkyl and haloC 1-3 alkyl; R 6 and R 7 are either i) each independently selected from H, C 1-3 alkyl and C 1-3 alkoxy; or ii) R 6 and R 7 together with the ring to which they are attached form a 9-membered bicyclic ring; p is 0-3; and R A is selected from H and C 1-3 alkyl, compositions containing them, their use in therapy, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided.

Claims (7)

1. The compound (1S)-1-[5-({1-[(3-fluoro-2-pyridinyl)methyl]-1H-pyrazol-3-yl}amino)-1,3,4-thiadiazol-2-yl]-1-(4-methyl-1,3-thiazol-2-yl)ethanol, or a pharmaceutically acceptable salt thereof.

2. The compound: (1S)-1-[5-({1-[(3-fluoro-2-pyridinyl)methyl]-1H-pyrazol-3-yl}amino)-1,3,4-thiadiazol-2-yl]-1-(4-methyl-1,3-thiazol-2-yl)ethanol.

3. A compound according to claim 1 , for use in therapy.

4. A compound according to claim 1 , for use in the treatment of tuberculosis.

5. A method of treatment of tuberculosis in mammal, which method comprises the administration to a mammal in need of such treatment an effective amount of a compound or a pharmaceutically acceptable salt thereof according to claim 1 .

6. A pharmaceutical composition comprising a compound according to claim 1 , and one or more pharmaceutically acceptable carriers, excipients or diluents.

7. The method of claim 5 wherein said mammal is human.

Assignments (2)
CHANGE OF ADDRESS Recorded Apr 16, 2025
From: GLAXO GROUP LIMITED
To: GLAXO GROUP LIMITED
Reel/Frame 071044/0904 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 23, 2015
From: CASTRO PICHEL, JULIA; FERNANDEZ MENENDEZ, RAQUEL; FERNANDEZ VELANDO, ESTHER PILAR; GONZALEZ DEL VALLE, SILVIA; MALLO-RUBIO, ARACELI
To: GLAXO GROUP LIMITED
Reel/Frame 035226/0869 →
Priority Claims (1)
EP 10382266 · Oct 13, 2010 · regional
Continuity (3)
Continuation 14295589 · Jun 4, 2014
Continuation 13878889
Related Publication 20150307485A1 · Oct 29, 2015