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Title:
MORPHINAN DERIVATIVE
Document Type and Number:
WIPO Patent Application WO/2019/045006
Kind Code:
A1
Abstract:
A morphinan derivative represented by general formula (I) (in the formula, R1 represents a hydrogen atom, an optionally substituted C1-6 alkyl group, or the like, R2 and R3 are the same or different and represent a hydrogen atom, a hydroxy group, or the like, R4 represents a hydrogen atom, a halogen atom, a hydroxy group, or the like, R5 represents a hydrogen atom, hydroxy group, or the like, R6 represents a hydrogen atom, a C1-6 alkyl group, or the like, R7 and R8 are the same or different and represent a hydrogen atom, a C1-6 alkyl group, or the like, R9 represents a hydrogen atom, a C1-6 alkyl group, an optionally substituted C6-10 aryl group, or the like, X represents a nitrogen atom or the like, Y represents an oxygen atom or the like, and n represents an integer of 0-3), a tautomer, a stereoisomer, a deuterium substitution product, or a pharmaceutically acceptable salt of the compound or a solvate of these, and a medicine, an analgesic, and an antipruritic having these as an active ingredient.

Inventors:
NAGASE HIROSHI (JP)
YAMAMOTO NAOSHI (JP)
WATANABE YOSHIKAZU (JP)
MOGI YUZO (JP)
Application Number:
PCT/JP2018/032221
Publication Date:
March 07, 2019
Filing Date:
August 30, 2018
Export Citation:
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Assignee:
NIPPON CHEMIPHAR CO (JP)
UNIV TSUKUBA (JP)
International Classes:
C07D489/12; A61K31/485; A61K31/497; A61K31/501; A61K31/506; A61K31/5377; A61P17/04; A61P25/04; A61P43/00
Domestic Patent References:
WO1998043978A11998-10-08
Foreign References:
JP2018127432A2018-08-16
JP2009196933A2009-09-03
Other References:
YATA, MASAHIRO ET AL.: "Separation of anxiolytic activity by means of fixed active conformation of nalfurafine", LECTURE ABSTRACTS OF THE 34TH MEDICINAL CHEMISTRY SYMPOSIUM, 11 November 2016 (2016-11-11), pages 87, ISSN: 0919-214X
WATANABE, Y. ET AL.: "Design, synthesis, and structure-activity relationship of novel opioid K receptor selective agonists: a-Iminoamide derivatives with an azabicyclo [2.2.2] octene skeleton", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 24, no. 21, 29 September 2014 (2014-09-29), pages 4980 - 4983, XP029077487, ISSN: 0960-894X, DOI: doi:10.1016/j.bmcl.2014.09.029
Attorney, Agent or Firm:
CHIGUSA, Shinichi et al. (JP)
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