发明名称 Remedy for diabetes
摘要 A method of screening a compound having a hypoglycemic effect (hereinafter referred to as “hypoglycemic compound”), a remedy for diabetes which contains a compound having a novel function mechanism, etc. More specifically speaking, a method of screening a hypoglycemic compound capable of binding to the β subunit of a trimeric GTP-binding protein, a remedy for diabetes comprising a hypoglycemic compound, which is characterized by being capable of binding to the β subunit of a trimeric GTP-binding protein, as the active ingredient, etc.
申请公布号 US8772281(B2) 申请公布日期 2014.07.08
申请号 US201213709798 申请日期 2012.12.10
申请人 Ajinomoto Co., Inc. 发明人 Fukuchi Naoyuki;Okamoto Satoru;Miyanaga Wataru;Takeshita Sen;Takayanagi Masaru;Fukuda Yumiko;Ikenoue Takao;Yamada Naoyuki;Arashida Naoko
分类号 A01N43/62;A61K31/55 主分类号 A01N43/62
代理机构 Oblon, Spivak, McClelland, Maier & Neustadt, L.L.P. 代理人 Oblon, Spivak, McClelland, Maier & Neustadt, L.L.P.
主权项 1. A compound represented by general formula (I) or a pharmaceutically acceptable salt thereof: wherein in the general formula (I), A and B may be the same or different and independently represent an optionally substituted aromatic ring, an optionally substituted heterocyclic ring, or an optionally substituted aliphatic ring; R1 represents a lower alkyl group, a lower alkenyl group, a lower alkynyl group, or a lower alkoxy group, the groups being optionally substituted by 1 to 3 substituents; —X— and —Y— may be the same or different and independently represent a hydrogen atom, —O—, —NR2—, —S—, —SO—, —SO2—, —CH2—, —CR3R4—, —COO—, —CONR2—, or —CO—, in which R2 represents a hydrogen atom, an optionally substituted lower alkyl group, an optionally substituted acyl group, an optionally substituted alkoxycarbonyl group, an optionally substituted carbamoyl group, or an optionally substituted sulfonyl group, and R3 and R4 may be the same or different and independently represent a hydrogen atom, a halogen atom, a hydroxyl group, an alkyl group, a mercapto group, an alkoxy group, an alkylthio group, an alkylsulfonyl group, an acyl group, an acyloxy group, an amino group, an alkylamino group, a carboxyl group, an alkoxycarbonyl group, a carbamoyl group, a nitro group, a cyano group, or a trifluoromethyl group; —W— represents an optionally substituted alkyl chain having 1 to 20 carbon atoms, and 1 to 10 carbon atoms in the alkyl chain may be replaced by —O—, —NR5—, —S—, —SO—, —SO2—, or —CO—, in which R5 represents a hydrogen atom, an optionally substituted lower alkyl group, an optionally substituted acyl group, an optionally substituted alkoxycarbonyl group, an optionally substituted carbamoyl group, or an optionally substituted sulfonyl group; Q represents a hydrogen atom, biotin, a fluorophore, a chromophore, a chemiluminescent functional group, an enzyme, a solid phase, a diazo group, or an azido group; one or more atoms in the formula may be (a) radioisotope(s); with the proviso that: i) in the optionally substituted groups, each substituent is selected from the group consisting of halogen atoms, a hydroxyl group, alkyl groups, mercapto groups, alkoxy groups, alkylthio groups, alkylsulfonyl groups, acyl groups, acyloxy groups, amino groups, alkylamino groups, a carboxyl group, alkoxycarbonyl groups, carbamoyl groups, a nitro group, a cyano group, a trifluoromethyl group, aryl groups, heteroaryl groups, diazo groups, and azido groups, and the substituent may be labeled with biotin, a fluorophore, a chromophore, a chemiluminescent moiety, or an enzyme; ii) when —X— is a hydrogen atom, —W—, —Y—, and Q do not exist; iii) when —Y— is a hydrogen atom, Q does not exist; and iv) the compound of the general formula (I) satisfies at least one of the following conditions a) to f): a) —X— and —Y— are other than a hydrogen atom, and Q is biotin, a fluorophore, a chromophore, a chemiluminescent functional group, or an enzyme;b) —X— and —Y— are other than a hydrogen atom, and Q is a diazo group or an azido group;c) —X— and —Y— are other than a hydrogen atom, and Q is a solid phase;d) labeled with at least one radioisotope atom;e) substituted with at least one substituent which is labeled with biotin, a fluorophore, a chromophore, a chemiluminescent moiety, or an enzyme; orf) substituted with at least one diazo group or azido group as a substituent.
地址 Tokyo JP