Triazine compounds and pharmaceutical use thereof
AssigneeJapan Tobacco Inc.
InventorsHironobu Nagamori, Ikuo Mitani, Masaki Yamashita, Takahiro Hotta, Yuichi Nakagawa, Masatoshi Ueda
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Abstract
Provided is 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 cancer including colorectal cancer. A compound represented by the formula [I] or a pharmaceutically acceptable salt thereof: wherein each symbol is as defined in the SPECIFICATION.
Claims10
A compound represented by the formula [I] or a pharmaceutically acceptable salt thereof:
- wherein
- X is CH,
- ring Cy is
- the formula:
- wherein R1 is
- (1) halogen,
- (2) C1-6 alkyl,
- (3) cyano or
- (4) haloC1-4 alkyl,
- R3 is
- (1) halogen,
- (2) hydroxy,
- (3) C1-6 alkyl or
- (4) —ORc, wherein the Rc is C1-6 alkyl optionally substituted by 1, 2 or 3 substituents selected from the group consisting of the following (a) to (f);
- (a) halogen,
- (b) hydroxy,
- (c) C1-6 alkoxy,
- (d) —C(O)NRc1Rc2, wherein the Rc1 and the Rc2 are each independently hydrogen or C1-6 alkyl,
- (e) C6-10 aryl, wherein the C6-10 aryl is optionally substituted by 1, 2 or 3 substituents selected from the group consisting of
- (i) halogen,
- (ii) hydroxy,
- (iii) C1-6 alkyl,
- (iv) C1-6 alkoxy, and
- (v) haloC1-4 alkyl, and
- (f) 5- or 6-membered heteroaryl containing 1, 2 or 3 nitrogen atoms, oxygen atoms or sulfur atoms, wherein the heteroaryl is optionally substituted by 1, 2 or 3 substituents selected from the group consisting of
- (i) halogen,
- (ii) hydroxy,
- (iii) C1-6 alkyl,
- (iv) C1-6 alkoxy, and
- (v) haloC1-4 alkyl, and
- R4 is
- (1) hydrogen,
- (2) halogen,
- (3) C1-6 alkyl or
- (4) C1-6 alkoxy,
- R5 is
- (1) halogen,
- (2) hydroxy,
- (3) C1-6 alkylsulfanyl,
- (4) C1-6 alkyl, wherein the C1-6 alkyl is optionally substituted by 1, 2 or 3 substituents selected from the group consisting of halogen, C6-10 aryl and C1-6 alkoxy,
- (5) C3-7 cycloalkyl,
- (6) —ORd, wherein the Rd is
- (a) C2-6 alkynyl,
- (b) C3-7 cycloalkyl optionally substituted by 1, 2 or 3 C1-6 alkyls or
- (c) C1-8 alkyl, wherein the C1-8 alkyl is optionally substituted by 1, 2 or 3 substituents selected from the group consisting of the following (i) to (v);
- (i) halogen,
- (ii) C6-10 aryl,
- (iii) C1-6 alkoxy,
- (iv) C3-7 cycloalkyl, wherein the C3-7 cycloalkyl is optionally substituted by 1, 2 or 3 substituents selected from the group consisting of C1-6 alkyl and haloC1-4 alkyl, and
- (v) 4-, 5- or 6-membered saturated heterocyclyl containing 1, 2 or 3 nitrogen atoms, oxygen atoms or sulfur atoms, wherein the saturated heterocyclyl is optionally substituted by 1, 2 or 3 substituents selected from the group consisting of C1-6 alkyl and haloC1-4 alkyl or
- (7) the formula:
- wherein Re is
- (a) C1-6 alkyl,
- (b) C3-7 cycloalkyl,
- (c) 5- or 6-membered heteroaryl containing 1, 2 or 3 nitrogen atoms, oxygen atoms or sulfur atoms, or
- (d) C6-10 aryl, wherein the C6-10 aryl is optionally substituted by 1, 2 or 3 substituents selected from the group consisting of
- (i) halogen,
- (ii) C1-6 alkyl,
- (iii) haloC1-4 alkyl,
- (iv) C1-6 alkoxy, and
- (v) haloC1-4 alkoxy, and
- m1 is 0, 1, 2 or 3 and, when m1 is 2 or 3, each R5 is selected independently,
- excluding 4,6-bis-(2,5-dimethyl-phenyl)-1,3,5-triazin-2-ol.
A compound of the following formula or a pharmaceutically acceptable salt thereof:
A compound of the following formula:
Dependencies are inferred from the claim text.