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PROPHYLACTIC AND/OR THERAPEUTIC AGENT FOR DISEASES ASSOCIATED WITH AMPA RECEPTORS

Foreign code F180009537
File No. (S2017-0260-N0)
Posted date Nov 2, 2018
Country WIPO
International application number 2018JP000531
International publication number WO 2018131662
Date of international filing Jan 11, 2018
Date of international publication Jul 19, 2018
Priority data
  • P2017-002962 (Jan 11, 2017) JP
Title PROPHYLACTIC AND/OR THERAPEUTIC AGENT FOR DISEASES ASSOCIATED WITH AMPA RECEPTORS
Abstract This prophylactic and/or therapeutic agent for diseases associated with AMPA receptors contains a compound represented by formula (I), or a pharmaceutically acceptable salt or solvate thereof. (In the formula, A and Z independently represent CO, SO or SO2; X and Y are independently S or O; R1-R4 are independently hydrogen, an alkyl group, an alkenyl group, an alkynyl group or a halo group; R5 is, independently for each occurrence, an alkyl group, an alkenyl group, an alkynyl group or a halo group; and n is an integer of 0-4).
Outline of related art and contending technology BACKGROUND ART
AMPA receptor molecule is a synaptic function, play an important role in the spirit of the neural activity.The inventors of the present invention in vivo (glutamate receptor) AMPA receptor synaptic transfer, including memory and learning various higher order brain functions in molecular and cellular mechanisms of plastic phenomenon has been revealed that the (non-patent document 1-8).In addition, in recent years mainly AMPA receptors in postmortem brain research depression, schizophrenia, drug abuse, autism, epilepsy disease, ALS the spirit and many others, can be associated with a neurological disease have been reported.AMPA receptor agonist of the target disease such as a preclinical, clinical development has been actively performed.AMPA receptor drug target (AMPA receptor agonist) are roughly classified into the receptor antagonist (2) receptor function in the presence of active agents (1).With respect to the former, with respect to the disease epilepsy AMPA receptor antagonists in the March 2016 (ficompa; Inc. eisai co., ltd.) and marketed in Japan.On the other hand, AMPA receptor function activators are still not available on the market.The onset of the disease mechanism and the heteroatom, AMPA receptor agonist is effective in all considered to be not much higher possibility.Therefore, the activation action of the AMPA receptor function in the development of a pharmaceutical composition containing a compound has been required.
Scope of claims (In Japanese)請求の範囲
[請求項1]
 式(I)の化合物、又はその医薬として許容し得る塩若しくは溶媒和物:
[化1]
(式中、
A及びZは、それぞれ独立に、CO、SO又はSO 2であり;
X及びYは、それぞれ独立に、S又はOであり;
 R 1~R 4は、それぞれ独立に、水素、アルキル、アルケニル、アルキニル又はハロであり;
 R 5は、出現ごとにそれぞれ独立に、アルキル、アルケニル、アルキニル又はハロであり;
R5は、出現ごとにそれぞれ独立に、アルキル、アルケニル、アルキニル又はハロであり;
nは0~4の整数である。)
を含有する、AMPA受容体に関連する疾患の予防及び/又は治療剤。
[請求項2]
 R 1~R 4の全てが、水素となることはない、請求項1記載の予防及び/又は治療剤。
[請求項3]
 A及びZは、それぞれ独立に、CO又はSO 2である、請求項1又は2記載の予防及び/又は治療剤。
[請求項4]
 AがSO 2であり、かつZがCOである、請求項1~3のいずれか一項記載の予防及び/又は治療剤。
[請求項5]
 XがSであり、かつYがOである、請求項1~4のいずれか一項記載の予防及び/又は治療剤。
[請求項6]
 R 2がアルキル、アルケニル、又はアルキニルである、請求項1~5のいずれか一項記載の予防及び/又は治療剤。
[請求項7]
 R 2がアルキルである、請求項6記載の予防及び/又は治療剤。
[請求項8]
 R 1がアルキル又はハロである、請求項1~7のいずれか一項記載の予防及び/又は治療剤。
[請求項9]
 R 3及びR 4のうちの一方が水素であり、他方がアルキルである、請求項1~8のいずれか一項記載の予防及び/又は治療剤。
[請求項10]
 R 5がハロである、請求項1~9のいずれか一項記載の予防及び/又は治療剤。
[請求項11]
 前記ハロがフルオロである、請求項10記載の予防及び/又は治療剤。
[請求項12]
 nが2である、請求項1~11のいずれか一項記載の予防及び/又は治療剤。
[請求項13]
 下記からなる群から選択される、請求項1記載の予防及び/又は治療剤:
[化2]
[請求項14]
 AMPA受容体機能活性化剤である、請求項1~13記載の予防及び/又は治療剤。
[請求項15]
 AMAP受容体に関連する疾患が、精神疾患又は神経疾患である、請求項1~13いずれか1項に記載の予防及び/又は治療剤。
[請求項16]
 精神疾患がうつ病である、請求項15に記載の予防及び/又は治療剤。
  • Applicant
  • ※All designated countries except for US in the data before July 2012
  • PUBLIC UNIVERSITY CORPORATION YOKOHAMA CITY UNIVERSITY
  • Inventor
  • TAKAHASHI Takuya
  • MIYAZAKI Tomoyuki
  • NAKAJIMA Waki
IPC(International Patent Classification)
Specified countries National States: AE AG AL AM AO AT AU AZ BA BB BG BH BN BR BW BY BZ CA CH CL CN CO CR CU CZ DE DJ DK DM DO DZ EC EE EG ES FI GB GD GE GH GM GT HN HR HU ID IL IN IR IS JO JP KE KG KH KN KP KR KW KZ LA LC LK LR LS LU LY MA MD ME MG MK MN MW MX MY MZ NA NG NI NO NZ OM PA PE PG PH PL PT QA RO RS RU RW SA SC SD SE SG SK SL SM ST SV SY TH TJ TM TN TR TT TZ UA UG US UZ VC VN ZA ZM ZW
ARIPO: BW GH GM KE LR LS MW MZ NA RW SD SL SZ TZ UG ZM ZW
EAPO: AM AZ BY KG KZ RU TJ TM
EPO: AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
OAPI: BF BJ CF CG CI CM GA GN GQ GW KM ML MR NE SN ST TD TG
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