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1. (WO2005035501) NOVEL OLEFIN DERIVATIVE
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2005/035501    International Application No.:    PCT/JP2004/015648
Publication Date: 21.04.2005 International Filing Date: 15.10.2004
IPC:
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
Title (EN) NOVEL OLEFIN DERIVATIVE
(FR) NOUVEAU DERIVE D'OLEFINE
(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)
(JA)本発明は、医薬として有用な新規オレフィン誘導体を創製し、その誘導体の新たな薬理作用を見出すことを目的とする。本発明化合物は一般式[I]で示され、優れたRhoキナーゼ阻害作用を有する。式中、Xはベンゼン環、シクロアルカン環又は単環式芳香族複素環を;Yはピリジン環又は1H−ピロロ[2,3−b]ピリジン環を;R1とR2はH又はアルキルを;R3とR4はハロゲン、H、OH、アルコキシ、アリールオキシ、アルキル、アリール、アミノ、アルキルアミノ又はアリールアミノを;R5とR6はハロゲン、H、OH、アルコキシ、アルケニルオキシ、アルキニルオキシ、シクロアルキルオキシ、シクロアルケニルオキシ、アリールオキシ、アルキル、アルケニル、アルキニル、シクロアルキル、シクロアルケニル、アリール、カルボキシ、ホルミル、アルキルカ等を示す。各基は置換基を有してもよい。           
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)