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Pub. No.:    WO/2009/125809    International Application No.:    PCT/JP2009/057245
Publication Date: 15.10.2009 International Filing Date: 09.04.2009
C07D 471/04 (2006.01), A61K 31/437 (2006.01), A61K 31/4745 (2006.01), A61K 31/4985 (2006.01), A61K 31/519 (2006.01), A61K 31/5383 (2006.01), A61P 31/04 (2006.01), C07D 498/04 (2006.01), C07D 498/14 (2006.01), C07D 519/00 (2006.01)
Applicants: DAIICHI SANKYO COMPANY, LIMITED [JP/JP]; 3-5-1, Nihonbashi Honcho, Chuo-ku, Tokyo, 1038426 (JP) (For All Designated States Except US).
INAGAKI, Hiroaki; (For US Only).
FUJISAWA, Tetsunori; (For US Only).
ITOH, Masao; (For US Only).
HAYAKAWA, Miho; (For US Only).
TSUDA, Toshifumi; (For US Only).
NAGAMOCHI, Masatoshi; (For US Only).
TAKAHASHI, Hisashi; (For US Only).
TAKEMURA, Makoto; (For US Only)
Inventors: INAGAKI, Hiroaki; .
FUJISAWA, Tetsunori; .
ITOH, Masao; .
TSUDA, Toshifumi; .
NAGAMOCHI, Masatoshi; .
TAKAHASHI, Hisashi; .
Agent: ISHIBASHI, Koki; c/o DAIICHI SANKYO COMPANY, LIMITED, 1-16-13, Kitakasai, Edogawa-ku, Tokyo 1340081 (JP)
Priority Data:
2008-103869 11.04.2008 JP
(JA) ピペリジン誘導体
Abstract: front page image
(EN)It is expected to develop a drug which exhibits potent antibacterial activity against a wide variety of bacteria including Gram-positive bacteria, Gram-negative bacteria, and resistant strains thereof and which has high safety. Under such circumstances, it has been found that compounds represented by general formula (I) or salts thereof exhibit potent antibacterial activity against a wide variety of bacteria including Gram-positive bacteria and Gram-negative bacteria and have high safety requisite to antibacterial drugs, or preventive or therapeutic drugs for infectious diseases. Namely, the invention relates to compounds represented by general formula (I), pharmacologically acceptable salts thereof, or hydrates of both.
(FR)L’invention concerne un médicament qui présente une activité antibactérienne puissante contre un large éventail de bactéries, y compris les bactéries à gram positif, les bactéries à gram négatif et leurs souches résistantes, et qui présente une grande sûreté. Il a été découvert que les composés représentés par la formule générale (I) ou leurs sels présentent une activité antibactérienne puissante contre un large éventail de bactéries, y compris les bactéries à gram positif et les bactéries à gram négatif, ainsi que la grande sûreté requise pour médicaments antibactériens, ou médicaments préventifs ou thérapeutiques pour maladies infectieuses. L’invention concerne donc les composés représentés par la formule générale (I), leurs sels pharmacologiquement acceptables, ou les hydrates des deux.
(JA)グラム陽性菌、グラム陰性菌、およびそれらの耐性菌に対して幅広く強力な抗菌活性を示し、かつ高い安全性を有する薬剤の開発が望まれている。 【解決手段】  このような状況下において、本発明者らは、鋭意検討を行った結果、下式(I)で表わされる化合物またはその塩が、グラム陽性菌およびグラム陰性菌に対して幅広く、かつ強力な抗菌活性を示し、しかも抗菌薬および感染症の予防・治療薬として高い安全性を兼ね備えていることを見出し、本発明を完成させた。  すなわち、本発明は、下式(I)で表わされる化合物、その塩、またはそれらの水和物を提供する。  すなわち、本発明は、 (1)式(I): 【化1】 で表される化合物、または、その薬理上許容される塩。
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)