Title:
CRYSTAL OF SALT OF NOVEL 3-AZABICYCLO[3.1.0]HEXANE DERIVATIVE AND PHARMACEUTICAL USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2016/186184
Kind Code:
A1
Abstract:
The objective of the present invention is to provide: a crystal having high purity and excellent properties (such as stability and solubility) of a highly safe compound with few side effects, said compound having μ-opioid receptor antagonist activity; and a method for producing this crystal. A crystal of a salt or hydrate thereof, said salt being composed of a compound represented by formula (I) and an acid selected from the group consisting of hydrochloric acid, hydrobromic acid and oxalic acid. (In the formula, R2 represents a hydrogen atom or a halogen atom; and R1 represents a group selected from the group consisting of formulae AA, BB, CC and DD.)
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Inventors:
IWAMURA RYO (JP)
TSUZAKI YASUNORI (JP)
SETOGUCHI HIROYUKI (JP)
AKAZA HIROTO (JP)
YAMAMOTO YASUHITO (JP)
TAKAMA AKIRA (JP)
KUNO YUKA (JP)
TSUZAKI YASUNORI (JP)
SETOGUCHI HIROYUKI (JP)
AKAZA HIROTO (JP)
YAMAMOTO YASUHITO (JP)
TAKAMA AKIRA (JP)
KUNO YUKA (JP)
Application Number:
PCT/JP2016/064942
Publication Date:
November 24, 2016
Filing Date:
May 19, 2016
Export Citation:
Assignee:
SANWA KAGAKU KENKYUSHO CO (JP)
UBE INDUSTRIES (JP)
UBE INDUSTRIES (JP)
International Classes:
C07D209/52; A61K31/403; A61P1/00; A61P1/10; A61P3/04; A61P17/04; A61P25/18; A61P25/24; A61P25/30; A61P25/36; A61P43/00
Domestic Patent References:
| WO2015076310A1 | 2015-05-28 |
Foreign References:
| JP2002533440A | 2002-10-08 | |||
| JP2005511545A | 2005-04-28 | |||
| JP2007508367A | 2007-04-05 |
Other References:
LUNN,G. ET AL.: "SAR and biological evaluation of 3-azabicyclo[3.1.0]hexane derivatives as mu opioid ligands", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 22, no. 6, 2012, pages 2200 - 2203, XP028402839
See also references of EP 3299357A4
See also references of EP 3299357A4
Attorney, Agent or Firm:
SAKAMOTO TOMOHIRO (JP)
坂本 智弘 (JP)
坂本 智弘 (JP)
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