Granted Patent
B2
US 12,492,182 · App. 18/114,043 · Granted Dec 9, 2025
Hydroxytriazine compounds and pharmaceutical use thereof
Assignee:
Japan Tobacco Inc.
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Abstract
The present invention provides a compound having an mPGES-1 inhibitory activity and useful for the prophylaxis or treatment of pain, rheumatism, osteoarthritis, fever, Alzheimer's disease, multiple sclerosis, arteriosclerosis, glaucoma, ocular hypertension, ischemic retinal disease, systemic scleroderma and/or cancer including colorectal cancer. The present invention relates to a compound of formula [I-a], [I-b] or [I-c] or a pharmaceutically acceptable salt thereof: wherein each symbol is as defined in the specification.
Claims (47)
1 . A compound of the formula [I-c], or a pharmaceutically acceptable salt thereof:
wherein
R is
(1) the formula:
wherein
R 1a is C 1-4 alkyl,
R 1b is C 1-4 alkyl or trifluoromethyl, and
R 1c is
(a) C 1-4 alkyl,
(b) C 1-4 fluoroalkyl,
(c) C 1-4 alkoxy, or
(d) C 1-4 alkoxy C 1-4 alkyl, or
(2) the formula:
wherein
n is 1,2, 3, 4 or 5, and
R 1d is
(a) fluoro,
(b) C 1-4 alkyl,
(c) C 1-4 fluoroalkyl,
(d) C 1-4 alkoxy, or
(e) C 1-4 alkoxy C 1-4 alkyl,
R 2 is hydrogen, and
R 6 is 1-methylbutyl or n-hexyl.
2 . The compound or pharmaceutically acceptable salt according to claim 1 , wherein R 1 is the formula:
wherein
R 1a is C 1-4 alkyl,
R 1b is C 1-4 alkyl or trifluoromethyl, and
R 1c is
(b) difluoromethyl or trifluoromethyl, or
(c) methoxy.
3 . The compound or pharmaceutically acceptable salt according to claim 1 , wherein R 1 is the formula:
wherein
n is 3, 4 or 5, and
R 1d is
(a) fluoro,
(c) C 1-4 fluoroalkyl,
(d) methoxy, or
(e) methoxymethyl.
4 . The compound or pharmaceutically acceptable salt according to claim 3 , wherein
n is 3 or 4, and
R 1d is monofluoromethyl, difluoromethyl or trifluoromethyl.
5 . A compound selected from the following formulas:
or a pharmaceutically acceptable salt thereof.
6 . A pharmaceutical composition comprising the compound or pharmaceutically acceptable salt according to claim 1 , and a pharmaceutically acceptable carrier.
7 . A method of treating pain, rheumatism, fever, osteoarthritis, glaucoma, or ocular hypertension, which comprises administering a therapeutically effective amount of the compound or pharmaceutically acceptable salt according to claim 1 to a human in need thereof.
8 . A compound of the following formula or a pharmaceutically acceptable salt thereof:
9 . A compound of the following formula:
Assignments (2)
NUNC PRO TUNC ASSIGNMENT
Recorded Apr 8, 2026
From: JAPAN TOBACCO INC.
To: SHIONOGI & CO., LTD.
Reel/Frame 074312/0259 →
ASSIGNMENT OF ASSIGNOR'S INTEREST
Recorded May 4, 2023
From: MITANI, IKUO; HIRONO, YUTARO; YAMASHITA, MASAKI
To: JAPAN TOBACCO INC.
Reel/Frame 063538/0874 →
Priority Claims (1)
JP 2015-160284
· Aug 17, 2015
· national
Continuity (3)
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