Title:
NOVEL NK3-RECEPTOR AGONIST
Document Type and Number:
WIPO Patent Application WO/2017/073764
Kind Code:
A1
Abstract:
The present invention addresses the problem of providing a novel NK3-receptor selective ligand which is expected to have a highly-active/highly-selective and sustained effect in vivo. A compound represented by formula (I) X1-A2-A3-X4-X5-Met-NH2 [each symbol in the formula is as defined in the description] or a pharmaceutically acceptable salt thereof has highly-active and highly-selective NK3-receptor agonist activity, and is useful as a therapeutic agent for disorders associated with excessive or deficient secretion of tachykinins, such as a drug for amelioration of pain, or sexual dysfunction associated with excessive/deficient secretion of sex hormones, and the like.
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Inventors:
OISHI SHINYA (JP)
FUJII NOBUTAKA (JP)
OHNO HIROAKI (JP)
KUWAI SHINJI (JP)
WAKABAYASHI YOSHIHIRO (JP)
YAMAMURA TAKASHI (JP)
TANAKA TOMOMI (JP)
ENDO NATSUMI (JP)
FUJII NOBUTAKA (JP)
OHNO HIROAKI (JP)
KUWAI SHINJI (JP)
WAKABAYASHI YOSHIHIRO (JP)
YAMAMURA TAKASHI (JP)
TANAKA TOMOMI (JP)
ENDO NATSUMI (JP)
Application Number:
PCT/JP2016/082160
Publication Date:
May 04, 2017
Filing Date:
October 28, 2016
Export Citation:
Assignee:
UNIV KYOTO (JP)
International Classes:
C07K7/06; A61K38/00; A61P5/24; A61P15/08; A61P29/02; A61P43/00; C07K17/10
Domestic Patent References:
| WO2015083816A1 | 2015-06-11 |
Other References:
MISU R. ET AL.: "Development of novel neurokinin 3 receptor (NK3R) selective agonists with resistance to proteolytic degradation", J. MED. CHEM., vol. 57, no. 20, 23 October 2014 (2014-10-23), pages 8646 - 8651, XP055381711
MISU R. ET AL.: "Structure-activity relationship study on senktide for development of novel potent neurokinin-3 receptor selective agonists", MED. CHEM. COMMUN., vol. 6, no. 3, 5 January 2015 (2015-01-05), pages 469 - 476, XP055381713
ZALIPSKY S. ET AL.: "Functionalized poly (ethylene glycol) for preparation of biologically relevant conjugates", BIOCONJUGATE CHEM., vol. 6, no. 2, 1995, pages 150 - 165, XP002068523
VERONESE F. M. ET AL.: "PEGylation, successful approach to drug delivery", DRUG DISCOV. TODAY, vol. 10, no. 21, 1 November 2005 (2005-11-01), pages 1451 - 1458, XP027684962
PASUT G. ET AL.: "State of the art in PEGylation: The great versatility achieved after forty years of research", J. CONTROLLED RELEASE, vol. 161, no. 2, 20 July 2012 (2012-07-20), pages 461 - 472, XP028927182
ROBERTS M. J. ET AL.: "Chemistry for peptide and protein PEGylation", ADV. DRUG DELIV. REV., vol. 54, no. 4, 17 June 2002 (2002-06-17), pages 459 - 476, XP002293146
SHINJI KUWAI ET AL.: "PEG Shushoku ni yoru Chojikan Sayogata NK3 Juyotai Sadoyaku no Sosei", DAI 33 KAI SYMPOSIUM ON MEDICINAL CHEMISTRY, 1 November 2015 (2015-11-01), pages 92
MISU R. ET AL.: "Structure-activity relationship study on senktide for development of novel potent neurokinin-3 receptor selective agonists", MED. CHEM. COMMUN., vol. 6, no. 3, 5 January 2015 (2015-01-05), pages 469 - 476, XP055381713
ZALIPSKY S. ET AL.: "Functionalized poly (ethylene glycol) for preparation of biologically relevant conjugates", BIOCONJUGATE CHEM., vol. 6, no. 2, 1995, pages 150 - 165, XP002068523
VERONESE F. M. ET AL.: "PEGylation, successful approach to drug delivery", DRUG DISCOV. TODAY, vol. 10, no. 21, 1 November 2005 (2005-11-01), pages 1451 - 1458, XP027684962
PASUT G. ET AL.: "State of the art in PEGylation: The great versatility achieved after forty years of research", J. CONTROLLED RELEASE, vol. 161, no. 2, 20 July 2012 (2012-07-20), pages 461 - 472, XP028927182
ROBERTS M. J. ET AL.: "Chemistry for peptide and protein PEGylation", ADV. DRUG DELIV. REV., vol. 54, no. 4, 17 June 2002 (2002-06-17), pages 459 - 476, XP002293146
SHINJI KUWAI ET AL.: "PEG Shushoku ni yoru Chojikan Sayogata NK3 Juyotai Sadoyaku no Sosei", DAI 33 KAI SYMPOSIUM ON MEDICINAL CHEMISTRY, 1 November 2015 (2015-11-01), pages 92
Attorney, Agent or Firm:
TAKASHIMA, Hajime (JP)
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