IP Library Granted Patent US 9,000,181
Granted Patent B2
US 9,000,181 · App. 14/295,589 · Granted Apr 7, 2015

3-amino-pyrazole derivatives useful against tuberculosis

Inventors: Raquel Fernandez Menendez (Madrid, ES); Silvia Gonzalez Del Valle (Madrid, ES)
Assignee: Glaxo Group Limited
C07D471/04C07D417/14
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Quick Facts
Patent No.
US 9,000,181
App. No.
14/295,589
Granted
Apr 7, 2015
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 bicylic 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 (8)

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

2. The compound 1-(4-ethylthiazol-2-yl)-1-[5-({1-[(2-methylthiazol-4-yl)methyl]-1H-pyrazol-3yl}amino)-1,3,4-thiadiazol-2-yl]ethanol.

3. The compound

4. A compound or a pharmaceutically acceptable salt thereof according to claim 1 , for use in therapy.

5. A compound or a pharmaceutically acceptable salt thereof according to claim 1 , for use in the treatment of tuberculosis.

6. A method of treatment of tuberculosis in a 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 .

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

8. The method of claim 6 wherein said mammal is a 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 Sep 2, 2014
From: CASTRO PICHEL, JULIA; FERNANDEZ MENENDEZ, RAQUEL; FERNANDEZ VELANDO, ESTHER PILAR; GONZALEZ DEL VALLE, SILVIA; MALLO-RUBIO, ARACELI
To: GLAXO GROUP LIMITED
Reel/Frame 033648/0976 →
Priority Claims (1)
EP 10382266 · Oct 13, 2010 · regional
Continuity (2)
Continuation 13878889
Related Publication 20140288133A1 · Sep 25, 2014