IP Library Granted Patent US 10,821,100
Granted Patent B2
US 10,821,100 · App. 16/423,992 · Granted Nov 3, 2020

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: Ichnos Sciences SA
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 10,821,100
App. No.
16/423,992
Granted
Nov 3, 2020
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 (11)

1. A method of relieving a mPGES-1 mediated disease, disorder, syndrome or condition in a subject comprising administering an effective amount of a compound of formula

or a pharmaceutically acceptable salt thereof, wherein the mPGES-1 mediated disease, disorder, syndrome or condition is selected from the group consisting of inflammation, pain, inflammatory pain, chronic pain, acute pain, arthritis, osteoarthritis and cancer.

2. The method according to claim 1 , wherein the disease, disorder, syndrome or condition is pain.

3. The method according to claim 1 , wherein the disease, disorder, syndrome or condition is inflammation.

4. The method according to claim 1 , wherein the disease, disorder, syndrome or condition is rheumatoid arthritic pain, osteoarthritic pain, or neuropathic pain.

5. The method according to claim 1 , wherein the disease, disorder, syndrome or condition is rheumatoid arthritic pain.

6. The method according to claim 1 , wherein the disease, disorder, syndrome or condition is osteoarthritic pain.

7. The method according to claim 1 , wherein the disease, disorder, syndrome or condition is cancer.

8. A method of relieving a mPGES-1 mediated disease, disorder, syndrome or condition in a subject comprising administering an effective amount of a compound of formula

or a pharmaceutically acceptable salt thereof,

wherein the mPGES-1 mediated disease, disorder, syndrome or condition is selected from the group consisting of inflammation, a brain tumor, breast cancer, a gastrointestinal carcinoid tumor, kidney cancer, thyroid cancer, colon cancer, adrenocortical carcinoma, basal cell carcinoma, carcinoma of unknown primary, cardiac (heart) tumors, ductal carcinoma in situ, lobular carcinoma in situ, merkel cell carcinoma, midline tract carcinoma involving NUT gene, squamous cell carcinoma, thymoma and thymic carcinoma, and carcinoma of ureter and renal pelvis.

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 (8)
Continuation 15919460 · Mar 13, 2018
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 20190282548A1 · Sep 19, 2019