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Title:
CYCLIC PEPTIDE COMPOUND HAVING HIGH MEMBRANE PERMEABILITY, AND LIBRARY CONTAINING SAME
Document Type and Number:
WIPO Patent Application WO/2018/225864
Kind Code:
A1
Abstract:
The present inventors found that, in screening a cyclic peptide compound capable of specifically binding to a target molecule, the hitting rate of a cyclic peptide compound capable of specifically binding to the target molecule can be improved by using a library which contains cyclic peptide compounds having a long side chain in the cyclic moiety. Meanwhile, the present inventors found that indole skeletons, which are employed in conventional low molecular drugs for oral use, and tryptophan and tyrosine residues, which are amino acid residues having a hydroxyphenyl group, are unsuitable for a peptide aiming at a high membrane permeability.

Inventors:
MURAOKA, Terushige (135 Komakado 1-chome, Gotemba-sh, Shizuoka 13, 〒4128513, JP)
IIDA, Takeo (200 Kajiwara, Kamakura-sh, Kanagawa 30, 〒2478530, JP)
MATSUO, Atsushi (135 Komakado 1-chome, Gotemba-sh, Shizuoka 13, 〒4128513, JP)
TAKEYAMA, Ryuichi (135 Komakado 1-chome, Gotemba-sh, Shizuoka 13, 〒4128513, JP)
TANADA, Mikimasa (135 Komakado 1-chome, Gotemba-sh, Shizuoka 13, 〒4128513, JP)
TANAKA, Shota (200 Kajiwara, Kamakura-sh, Kanagawa 30, 〒2478530, JP)
HAYASHI, Ryuji (135 Komakado 1-chome, Gotemba-sh, Shizuoka 13, 〒4128513, JP)
FUJINO, Machiko (200 Kajiwara, Kamakura-sh, Kanagawa 30, 〒2478530, JP)
IIKURA, Hitoshi (135 Komakado 1-chome, Gotemba-sh, Shizuoka 13, 〒4128513, JP)
Application Number:
JP2018/022097
Publication Date:
December 13, 2018
Filing Date:
June 08, 2018
Export Citation:
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Assignee:
CHUGAI SEIYAKU KABUSHIKI KAISHA (5-1 Ukima 5-chome, Kita-ku Tokyo, 43, 〒1158543, JP)
International Classes:
C40B40/10; C07K1/13; C07K2/00; C12P21/02; C40B30/04; G01N33/566; C07K7/64; C12N15/09
Domestic Patent References:
WO2013100132A12013-07-04
WO2017136708A12017-08-10
Foreign References:
JP2017043615A2017-03-02
Other References:
LOW, K. E. ET AL.: "Rational design of calpain inhibitors based on calpastatin peptidomimetics", JOURNAL OF MEDICINAL CHEMISTRY, vol. 59, no. 11, 9 June 2016 (2016-06-09), pages 5403 - 5415, XP055452019
OVADIA, 0. ET AL.: "The effect of multiple N- methylation on intestinal permeability of cyclic hexapeptides", MOLECULAR PHARMACEUTICS, vol. 8, no. 2, 4 April 2011 (2011-04-04), pages 479 - 487, XP055564613
TAKAHASHI, T. ET AL.: "Solid phase library synthesis of cyclic depsipeptides: aurilide and aurilide analogues", JOURNAL OF COMBINATORIAL CHEMISTRY, vol. 5, no. 4, July 2003 (2003-07-01), pages 414 - 428, XP055564620
Attorney, Agent or Firm:
HARUNA, Masao et al. (Kantetsu Tsukuba Bldg. 6F, 1-1-1 Oroshi-machi, Tsuchiura-sh, Ibaraki 47, 〒3000847, JP)
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