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Pub. No.:    WO/2005/035501    International Application No.:    PCT/JP2004/015648
Publication Date: 21.04.2005 International Filing Date: 15.10.2004
A61K 31/437 (2006.01), A61K 31/44 (2006.01), A61K 31/4409 (2006.01), C07F 7/18 (2006.01)
Applicants: UBE INDUSTRIES, LTD. [JP/JP]; 1978-96, Oaza Kogushi Ube-shi Yamaguchi 7808633 (JP) (For All Designated States Except US).
SANTEN PHARMACEUTICAL CO., LTD. [JP/JP]; 9-19, Shimoshinjo 3-chome, Higashiyodogawa-ku Osaka-shi Osaka 5338651 (JP) (For All Designated States Except US).
HAGIHARA, Masahiko [JP/JP]; (JP) (For US Only).
IZUMI, Naoyuki [JP/JP]; (JP) (For US Only).
TSUZAKI, Yasunori [JP/JP]; (JP) (For US Only).
MATSUGI, Takeshi [JP/JP]; (JP) (For US Only).
NAKAJIMA, Tadashi [JP/JP]; (JP) (For US Only).
HATANO, Masakazu [JP/JP]; (JP) (For US Only).
HARA, Hideaki [JP/JP]; (JP) (For US Only)
Inventors: HAGIHARA, Masahiko; (JP).
IZUMI, Naoyuki; (JP).
TSUZAKI, Yasunori; (JP).
MATSUGI, Takeshi; (JP).
NAKAJIMA, Tadashi; (JP).
HATANO, Masakazu; (JP).
HARA, Hideaki; (JP)
Agent: HIBI, Norihiko; c/o KISHIMOTO & CO. 3rd Floor, Inaba Building, 13-18, Nishishinsaibashi 1-chome, Chuo-ku Osaka-shi Yamaguchi 5420086 (JP)
Priority Data:
2003-354946 15.10.2003 JP
(JA) 新規オレフィン誘導体
Abstract: front page image
(EN)To prepare a novel olefin derivative useful as a medicine and to find out a new pharmacological activity of the derivative. The compound is represented by the general formula [I] and has excellent Rho-kinase inhibitory activity. In the formula, X is a benzene ring, cycloalkane ring, or monocyclic aromatic heterocycle; Y is a pyridine ring or 1H-pyrrolo[2,3-b]pyridine ring; R1 and R2 each is hydrogen or alkyl; R3 and R4 each is halogeno, hydrogen, OH, alkoxy, aryloxy, alkyl, aryl, amino, alkylamino, or arylamino; and R5 and R6 each is halogeno, hydrogen, OH, alkoxy, alkenyloxy, alkynyloxy, cycloalkyloxy, cycloalkenyloxy, aryloxy, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, carboxy, formyl, alkylcarbonyl, etc. These groups may be substituted.
(FR)Aux fins de préparer un nouveau dérivé d'oléfines qui convient comme médicament et de découvrir une nouvelle activité pharmacologique de ce dérivé. Ce composé est représenté par la formule générale (II) et possède une excellente activité inhibitrice de rho-kinase. Dans cette formule, X est un cycle benzène, un cycle cycloalkane ou un hétérocycle aromatique monocyclique, Y est un cycle pyridine ou un cycle 1h-pyrrolo(2,3-b)pyridine, R1 et R4 sont chacun halogéno, hydrogène, OH, alcoxy, aryloxy, alkyle, aryle, amino. Alkylamino ou arylamino et, R5 et R6sont chacun halogéno, hydrogène, OH, alcoxy, alkényloxy, alkynyloxy, cycloalkyloxy, cycloalkényloxy, aryloxy, alkyle, alkényle, alkynyle, cycloalkyle, cycloalkényle, aryle, carboxy, formyle, alkylcarbonyle, etc.. ces groupes peuvent être substitués. (I)
Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, 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, HU, IE, IT, LU, MC, NL, 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)