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1. (WO2009139361) GLUCOCORTICOID RECEPTOR AGONIST COMPOSED OF 2,2,4-TRIMETHYL-6-PHENYL-1,2-DIHYDROQUINOLINE DERIVATIVE HAVING SUBSTITUTED OXY GROUP
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2009/139361    International Application No.:    PCT/JP2009/058801
Publication Date: 19.11.2009 International Filing Date: 12.05.2009
IPC:
C07D 215/14 (2006.01), A61K 31/47 (2006.01), A61K 31/4709 (2006.01), A61K 31/506 (2006.01), A61K 31/5377 (2006.01), A61P 1/02 (2006.01), A61P 1/04 (2006.01), A61P 1/16 (2006.01), A61P 3/08 (2006.01), A61P 5/14 (2006.01), A61P 5/16 (2006.01), A61P 5/38 (2006.01), A61P 5/44 (2006.01), A61P 7/00 (2006.01), A61P 7/04 (2006.01), A61P 7/06 (2006.01), A61P 9/00 (2006.01), A61P 11/00 (2006.01), A61P 11/02 (2006.01), A61P 11/06 (2006.01), A61P 13/12 (2006.01), A61P 15/00 (2006.01), A61P 17/00 (2006.01), A61P 17/02 (2006.01), A61P 17/04 (2006.01), A61P 17/06 (2006.01), A61P 17/14 (2006.01), A61P 21/00 (2006.01), A61P 21/02 (2006.01), A61P 21/04 (2006.01), A61P 25/00 (2006.01), A61P 25/02 (2006.01), A61P 25/28 (2006.01), A61P 27/02 (2006.01), A61P 27/16 (2006.01), A61P 29/00 (2006.01), A61P 31/00 (2006.01), A61P 31/04 (2006.01), A61P 31/06 (2006.01), A61P 31/22 (2006.01), A61P 35/00 (2006.01), A61P 35/02 (2006.01), A61P 37/02 (2006.01), A61P 37/08 (2006.01), A61P 39/02 (2006.01), A61P 43/00 (2006.01), C07D 401/12 (2006.01), C07D 405/12 (2006.01), C07D 409/12 (2006.01), C07D 409/14 (2006.01), C07D 413/12 (2006.01), C07D 417/12 (2006.01), C07D 417/14 (2006.01)
Applicants: SANTEN PHARMACEUTICAL CO., LTD. [JP/JP]; 9-19, Shimoshinjo 3-chome, Higashiyodogawa-ku, Osaka-shi, Osaka 5338651 (JP) (For All Designated States Except US).
KATO, Masatomo [JP/JP]; (JP) (For US Only).
TAKAI, Miwa [JP/JP]; (JP) (For US Only).
MATSUYAMA, Takahiro [JP/JP]; (JP) (For US Only).
KUROSE, Tatsuji [JP/JP]; (JP) (For US Only).
HAGIWARA, Yumi [JP/JP]; (JP) (For US Only).
MATSUDA, Mamoru [JP/JP]; (JP) (For US Only).
MORI, Toshiyuki [JP/JP]; (JP) (For US Only).
IMOTO, Kenji [JP/JP]; (JP) (For US Only).
DOTA, Atsuyoshi [JP/JP]; (JP) (For US Only)
Inventors: KATO, Masatomo; (JP).
TAKAI, Miwa; (JP).
MATSUYAMA, Takahiro; (JP).
KUROSE, Tatsuji; (JP).
HAGIWARA, Yumi; (JP).
MATSUDA, Mamoru; (JP).
MORI, Toshiyuki; (JP).
IMOTO, Kenji; (JP).
DOTA, Atsuyoshi; (JP)
Agent: HIBI, Norihiko; (JP)
Priority Data:
2008-124714 12.05.2008 JP
Title (EN) GLUCOCORTICOID RECEPTOR AGONIST COMPOSED OF 2,2,4-TRIMETHYL-6-PHENYL-1,2-DIHYDROQUINOLINE DERIVATIVE HAVING SUBSTITUTED OXY GROUP
(FR) AGONISTE DES RÉCEPTEURS DE GLUCOCORTICOÏDES COMPOSÉ DE DÉRIVÉ DE 2,2,4-TRIMÉTHYL-6-PHÉNYL-1,2-DIHYDROQUINOLÉINE AYANT UN GROUPE OXY SUBSTITUÉ
(JA) 置換オキシ基を有する2,2,4-トリメチル-6-フェニル-1,2-ジヒドロキノリン誘導体からなるグルココルチコイド受容体アゴニスト
Abstract: front page image
(EN)Disclosed is a glucocorticoid receptor agonist composed of a compound represented by formula (1) or a salt thereof, which is a 2,2,4-trimethyl-6-phenyl-1,2-dihydroquinoline derivative having a substituted oxy group.  A novel pharmacological action of the agonist is also disclosed.  In the formula, R1 represents a group represented by formula (2a), (3a), (4a) or (5a); R2 represents -(CO)-R8, -(CO)O-R9 or the like; R2-O- is substituted at the 4-position or the 5-position of the benzene ring A; R3 represents a lower alkyl group; R4, R5, R6 or R7 represents a halogen atom, an optionally substituted lower alkyl group or the like; m, n, p or q represents 0, 1 or the like; and R8, R9 or the like represents an optionally substituted lower alkyl group, a lower alkenyl group or the like.
(FR)L'invention porte sur un agoniste des récepteurs de glucocorticoïdes composé d'un composé représenté par la formule (1) ou d'un sel de celui-ci, qui est un dérivé de 2,2,4-triméthyl-6-phényl-1,2-dihydroquinoléine ayant un groupe oxy substitué. L'invention porte également sur un nouvel effet pharmacologique de l'agoniste. Dans la formule, R1 représente un groupe représenté par la formule (2a), (3a), (4a) ou (5a) ; R2 représente -(CO)-R8, -(CO)O-R9 ou similaire ; R2-O- est substitué au niveau de la position 4 ou de la position 5 du noyau benzénique A ; R3 représente un groupe alkyle inférieur ; R4, R5, R6 ou R7 représentent un atome d'halogène, un groupe alkyle inférieur facultativement substitué ou similaire ; m, n, p ou q représentent 0, 1 ou similaire ; et R8, R9 ou similaire représentent un groupe alkyle inférieur facultativement substitué, un groupe alcényle inférieur ou similaire.
(JA) 本発明は、置換オキシ基を有する2,2,4-トリメチル-6-フェニル-1,2-ジヒドロキノリン誘導体からなる、式(1)で表される化合物又はその塩からなるグルココルチコイド受容体アゴニスト及びそのアゴニストの新たな薬理作用に関する。式中、R1は式(2a)、(3a)、(4a)又は(5a)を、R2は-(CO)-R8、-(CO)O-R9等を、R2-O-はベンゼン環Aの4又は5位に置換し、R3は低級アルキル基を、R4、R5、R6又はR7はハロゲン原子、置換基を有してもよい低級アルキル基等を、m、n、p又はqは、0、1等を、R8、R9等は置換基を有してもよい低級アルキル基、低級アルケニル基等を示す。  
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW.
African Regional Intellectual Property Organization (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (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, SE, SI, SK, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG).
Publication Language: Japanese (JA)
Filing Language: Japanese (JA)