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Title:
1-INDANE DERIVATIVE HAVING ANTI-PROTOZOAL ACTIVITY
Document Type and Number:
WIPO Patent Application WO/2014/076965
Kind Code:
A1
Abstract:
The present invention provides: an inhibitor of the proliferation of a human-infecting malaria-causing protozoa and a human-infecting protozoa of the genus trypanosome; and a therapeutic agent and a prophylactic agent. Specifically, a pharmaceutical composition having a prophylactic or therapeutic effect on infections caused by a malaria-causing protozoa and a protozoa of the genus trypanosome, said pharmaceutical composition comprising a compound represented by general formula (I) and a pharmacologically acceptable salt thereof as active ingredients. [In the formula, R1 to R4 independently represent a hydrogen atom, a C1-8 alkyl group, a C2-8 alkenyl group, a C6-10 aryl group, a C1-8 alkoxy group, a C1-8 alkylthio group, a hydroxy group, a halogen atom or an amino group (wherein a case in which each of R1 to R4 represents a hydroxy group is excluded); and R5 and R6 independently represent a hydroxy group or a group -SO3Na, or R5 and R6 together form an oxo group or a group =N-R7.]

Inventors:
OMURA SATOSHI (JP)
OTOGURO KAZUHIKO (JP)
IWATSUKI MASATO (JP)
ISHIYAMA AKI (JP)
OTAKI YOSHIHIRO (JP)
SHIBAHARA SEIJI (JP)
KONDO SHINICHI (JP)
Application Number:
PCT/JP2013/006722
Publication Date:
May 22, 2014
Filing Date:
November 15, 2013
Export Citation:
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Assignee:
KITASATO INST (JP)
BIOFRONTIER PARTNERS INC (JP)
International Classes:
A61K31/445; A61P33/02; A61P33/06; C07D211/24; C07D211/28
Domestic Patent References:
WO2010019560A12010-02-18
Foreign References:
US4895841A1990-01-23
Other References:
LIM, L. Y. ET AL.: "The anticholinesterase activity of mefloquine", CLINICAL AND EXPERIMENTAL PHARMACOLOGY AND PHYSIOLOGY, vol. 12, no. 5, 1985, pages 527 - 531, XP000900059
LENTA, B. N. ET AL.: "Anti-plasmodial and cholinesterase inhibiting activities of some constituents of Psorospermum glaberrimum", CHEMICAL & PHARMACEUTICAL BULLETIN, vol. 56, no. 2, 2008, pages 222 - 226
DEVKOTA, K. P. ET AL.: "Cholinesterase inhibiting and antiplasmodial steroidal alkaloids from Sarcococca hookeriana", CHEMICAL & PHARMACEUTICAL BULLETIN, vol. 59, no. 9, 2007, pages 1397 - 1401
MCARDLE, J. J. ET AL.: "Mefloquine inhibits cholinesterases at the mouse neuromuscular junction", NEUROPHARMACOLOGY, vol. 49, no. 8, 2005, pages 1132 - 1139, XP005160054, DOI: doi:10.1016/j.neuropharm.2005.06.011
DE ANDRASE, J. P . ET AL.: "Bioactive alkaloid extracts from Narcissus broussonetii: Mass spectral studies", JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, vol. 70, 12 May 2012 (2012-05-12), pages 13 - 25
Attorney, Agent or Firm:
HASEGAWA, Hiroshi et al. (JP)
Hiroshi Hasegawa (JP)
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