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Patent Searching and Data

Document Type and Number:
WIPO Patent Application WO/2015/178265
Kind Code:
It was discovered that interposing a suitable aromatic amidation linker in making a prodrug to serve as a γ-glutamylation drug provides stability even in a close to physiological environment, recognition by GGT, and very rapid release of the pharmacologically active drug, and the invention was achieved. Specifically, a drug represented by general formula (1) to which a γ-glutamyl aromatic amide has been bonded releases the pharmacologically active drug rapidly in tissues expressing a high level of GGT and can become a drug having a high therapeutic effect.

YONETA Yasushi (31-12 Shimo 3-chome, Kita-k, Tokyo 88, 〒1158588, JP)
SEKINE Keiko (31-12 Shimo 3-chome, Kita-k, Tokyo 88, 〒1158588, JP)
NIITSUMA Setsuko (31-12 Shimo 3-chome, Kita-k, Tokyo 88, 〒1158588, JP)
Application Number:
Publication Date:
November 26, 2015
Filing Date:
May 13, 2015
Export Citation:
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NIPPON KAYAKU KABUSHIKI KAISHA (1-1 Marunouchi 2-chome, Chiyoda-ku Tokyo, 05, 〒1000005, JP)
International Classes:
C07D491/22; A61K31/4745; A61K31/704; A61K31/7068; A61P35/00; C07H15/252; C07H19/067
Foreign References:
Other References:
ZHANG,Q. ET AL.: "Development and Characterization of Glutamyl-Protected N- Hydroxyguanidines as Reno-Active Nitric Oxide Donor Drugs with Therapeutic Potential in Acute Renal Failure", JOURNAL OF MEDICINAL CHEMISTRY, vol. 56, no. 13, 2013, pages 5321 - 5334, XP055237991, ISSN: 0022-2623
ZHANG,Q. ET AL.: "A new class of NO -donor pro- drugs triggered by y-glutamyl transpeptidase with potential for reno-selective vasodilatation", CHEMICAL COMMUNICATIONS, vol. 49, no. 14, 2013, Cambridge, United Kingdom, pages 1389 - 1391
R KEREN ET AL.: "y-Glutamyl transpeptidase- dependent mutagenicity and cytotoxicity of y- glutamyl derivatives: A model for biochemical targeting of chemotherapeutic agents", ENVIRONMENTAL AND MOLECULAR MUTAGENESIS, vol. 32, no. 4, 1998, pages 377 - 386, XP055237992
Attorney, Agent or Firm:
KAWAGUTI & PARTNERS (Jochi Kioizaka Bldg, 7-1 Kioi-cho Chiyoda-k, Tokyo 94, 〒1020094, JP)
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