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Title:
NEW NK3 RECEPTOR AGONIST
Document Type and Number:
WIPO Patent Application WO/2015/083816
Kind Code:
A1
Abstract:
 Provided is a new NK3 receptor selective ligand which is expected to have high activity and high selectivity, and to act in a sustained manner in vivo. A compound expressed by formula (I) X1 - A2 - A3 - X4 - X5 - Met - NH2 [the symbols in the formula are as set forth in the description] or a pharmaceutically acceptable salt thereof has a highly active and highly selective NK3 receptor agonist activity, and is effective as a drug for the treatment of disorders associated with an excess or deficiency in the secretion of tachykinins, for example as a pharmaceutical for the treatment of pain or for the improvement of sexual dysfunction accompanying excess or deficiency in the secretion of sex hormones.

Inventors:
FUJII NOBUTAKA (JP)
OHNO HIROAKI (JP)
OISHI SHINYA (JP)
MISU RYOSUKE (JP)
YAMADA AI (JP)
YAMAMOTO KOKI (JP)
OKAMURA HIROAKI (JP)
YAMAMURA TAKASHI (JP)
Application Number:
PCT/JP2014/082217
Publication Date:
June 11, 2015
Filing Date:
December 05, 2014
Export Citation:
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Assignee:
UNIV KYOTO (JP)
NAT INST OF AGROBIO SCIENCES (JP)
International Classes:
C07K7/06; A61K38/00; A61P5/24; A61P15/00; A61P25/04; A61P29/02; A61P43/00; C07K5/107; C07K5/113
Domestic Patent References:
WO1994009031A11994-04-28
WO2014061772A12014-04-24
Other References:
ALMEIDA, T.A. ET AL.: "Tachykinins and tachykinin receptors: structure and activity relationships", CURRENT MEDICINAL CHEMISTRY, vol. 11, no. 15, August 2004 (2004-08-01), pages 2045 - 2081, XP002459773
MISU, R. ET AL.: "Structure-activity relationship study of tachykinin peptides for the development of novel neurokinin-3 receptor selective agonists", BIOORGANIC & MEDICINAL CHEMISTRY, vol. 21, no. 8, pages 2413 - 2417, XP028524303, DOI: doi:10.1016/j.bmc.2013.01.036
MISU, R. ET AL.: "Development of Novel Neurokinin 3 Receptor (NK3R) Selective Agonists with Resistance to Proteolytic Degradation", JOURNAL OF MEDICINAL CHEMISTRY, vol. 57, 23 September 2014 (2014-09-23), pages 8646 - 8651
Attorney, Agent or Firm:
TAKASHIMA, HAJIME (JP)
Takashima 1 (JP)
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