IP Library › Granted Patent US 10,391,083
Granted Patent B2
US 10,391,083 · App. 15/919,460 · Granted Aug 27, 2019

Triazolone compounds as MPGES-1 inhibitors

Inventors: Laxmikant A. Gharat (Thane, IN); Nagarajan Muthukaman (Erode, IN); Neelima Khairatkar-Joshi (Thane, IN); Vidya G. Kattige (Thane, IN)
Assignee: GLENMARK PHARMACEUTICALS S.A
A61K31/4196A61K31/422A61K31/428A61K31/4245A61K31/433A61K31/4439A61K31/5377C07D249/12C07D401/04C07D401/10C07D403/04C07D403/10C07D403/12C07D405/12C07D409/14C07D413/10C07D413/12C07D417/10C07D417/12
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Quick Facts
Patent No.
US 10,391,083
App. No.
15/919,460
Granted
Aug 27, 2019
Kind
B2
Abstract

The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.

Claims (22)

1. A process for preparing a compound of formula

or a pharmaceutically acceptable salt thereof, the process comprising:

Step 1: reacting a compound of the formula

 with a compound of the formula

 to obtain a compound of the formula

Step 2: converting the compound of formula

 and

Step 3: converting the compound of formula

2. The process according to claim 1 , wherein Step 1 is carried out in the presence of a suitable solvent.

3. The process according to claim 1 , wherein Step 1 is carried out in the presence of dichloromethane.

4. The process according to claim 1 , wherein Step 1 is carried out in the presence of a suitable acid.

5. The process according to claim 1 , wherein Step 1 is carried out in the presence of trifluoroacetic acid.

6. The process according to claim 1 , wherein Step 2 is carried out in the presence of a suitable solvent.

7. The process according to claim 1 , wherein Step 2 is carried out in the presence of tetrahydrofuran.

8. The process according to claim 1 , wherein Step 2 is carried out in the presence of a suitable base.

9. The process according to claim 1 , wherein Step 2 is carried out in the presence of potassium hydroxide.

10. The process according to claim 1 , wherein in Step 3 the compound of formula

is reacted with pivaloyl chloride.

11. The process according to claim 1 , wherein Step 3 is carried out in the presence of suitable solvent.

12. The process according to claim 1 , wherein Step 3 is carried out in the presence of tetrahydrofuran.

13. The process according to claim 1 , wherein Step 3 is carried out in the presence of a suitable base.

14. The process according to claim 1 , wherein Step 3 is carried out in the presence of N,N-diisopropylethylamine.

Assignments (1)
CHANGE OF NAME Recorded Mar 26, 2020
From: GLENMARK PHARMACEUTICALS S.A.
To: ICHNOS SCIENCES SA
Reel/Frame 052232/0474 →
Priority Claims (3)
IN 1733/MUM/2012 · Jun 15, 2012 · national
IN 3319/MUM/2012 · Nov 19, 2012 · national
IN 387/MUM/2013 · Feb 8, 2013 · national
Continuity (7)
Continuation 15228681 · Aug 4, 2016
Continuation 14745204 · Jun 19, 2015
Continuation 14123409
Provisional Application 61792225 · Mar 15, 2013
Provisional Application 61735679 · Dec 11, 2012
Provisional Application 61668146 · Jul 5, 2012
Related Publication 20180200229A1 · Jul 19, 2018