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1. (WO2019044868) PYRIMIDINE DERIVATIVE
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Pub. No.: WO/2019/044868 International Application No.: PCT/JP2018/031859
Publication Date: 07.03.2019 International Filing Date: 29.08.2018
IPC:
C07D 401/04 (2006.01) ,A61K 31/506 (2006.01) ,A61P 43/00 (2006.01) ,C07D 403/04 (2006.01) ,C07D 417/04 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
506
not condensed and containing further heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43
Drugs for specific purposes, not provided for in groups A61P1/-A61P41/108
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
403
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
Applicants:
あすか製薬株式会社 ASKA PHARMACEUTICAL CO., LTD. [JP/JP]; 東京都港区芝浦二丁目5番1号 5-1, Shibaura 2-chome, Minato-ku, Tokyo 1088532, JP
Inventors:
岡田 亮 OKADA Makoto; JP
中野 洋一 NAKANO Youichi; JP
能勢 卓 NOSE Takashi; JP
西本 恭博 NISHIMOTO Takahiro; JP
前田 智史 MAEDA Satoshi; JP
渡邊 友章 WATANABE Tomoaki; JP
Agent:
特許業務法人特許事務所サイクス SIKS & CO.; 東京都中央区京橋一丁目8番7号 京橋日殖ビル8階 8th Floor, Kyobashi-Nisshoku Bldg., 8-7, Kyobashi 1-chome, Chuo-ku, Tokyo 1040031, JP
Priority Data:
2017-16504930.08.2017JP
Title (EN) PYRIMIDINE DERIVATIVE
(FR) DÉRIVÉ PYRIMIDINE
(JA) ピリミジン誘導体
Abstract:
(EN) A compound which has mPGES-1 inhibitory activity and is useful as an active ingredient of a pharmaceutical product for the treatment of inflammation, pain or diseases such as rheumatism. (In the formula, X represents a carbonyl group or a sulfonyl group; R1 represents a hydrogen atom, a halogen atom, an alkyl group, an alkanoyl group, a cyano group or a carboxyl group; R2 represents an alkyl group, a carbocyclic group or a heterocyclic group; R3 represents a hydrogen atom or one to three substituents; each of R4 and R5 represents a hydrogen atom, a halogen atom or an alkyl group; R6 represents an alkyl group or an alkoxy group; and ring A represents a heterocyclic diyl group.)
(FR) La présente invention concerne un composé ayant une activité inhibitrice de mPGES-1 et qui est utile en tant que principe actif d'un produit pharmaceutique pour le traitement d'une inflammation, d'une douleur ou de maladies telles que le rhumatisme. (Dans la formule, X représente un groupe carbonyle ou un groupe sulfonyle ; R1 représente un atome d'hydrogène, un atome d'halogène, un groupe alkyle, un groupe alcanoyle, un groupe cyano ou un groupe carboxyle ; R2 représente un groupe alkyle, un groupe carbocyclique ou un groupe hétérocyclique ; R3 représente un atome d'hydrogène ou un à trois substituants ; chacun de R4 et R5 représente un atome d'hydrogène, un atome d'halogène ou un groupe alkyle ; R6 représente un groupe alkyle ou un groupe alcoxy ; et l'anneau A représente un groupe diyle hétérocyclique.)
(JA) mPGES-1阻害作用を有し、炎症、疼痛、又はリウマチなどの疾患の治療のための医薬の有効成分として有用な化合物(Xはカルボニル基又はスルホニル基;Rは水素原子、ハロゲン原子、アルキル基、アルカノイル基、シアノ基、又はカルボキシル基;R2はアルキル基、炭素環基、又は複素環基;R3は水素原子又は1ないし3個の置換基;R4及びR5は水素原子、ハロゲン原子、又はアルキル基;R6はアルキル基、又はアルコキシ基;環Aは複素環ジイル基を示す)。
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: Japanese (JA)
Filing Language: Japanese (JA)