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    • 8. 发明授权
    • Carboxylic acid compound having cyclopropane ring
    • 具有环丙烷环的羧酸化合物
    • US07468389B2
    • 2008-12-23
    • US10450816
    • 2001-12-18
    • Tomoyuki NishizakiAkito Tanaka
    • Tomoyuki NishizakiAkito Tanaka
    • A61K31/215C07C61/00C07C61/04
    • C07C61/04C07C53/134C07C57/26C07C61/12C07C61/28C07C61/35
    • A carboxylic acid compound having cyclopropane ring(s) of the formula (I): wherein R is alkyl or alkenyl optionally having one or more 1,2-cyclopropylene in a carbon chain and/or optionally having cyclopropyl at the end of a chain,X is a single bond or alkylene, wherein the total number of carbon less the number of cyclopropane ring is 10-25, and a pharmaceutically acceptable salt thereof are provided. The compound (I) shows an LTP-like potentiation of synaptic transmission, allows slow metabolism in the living body, show a stable LTP-like potentiation of synaptic transmission, and is useful as an agent for LTP-like potentiation of synaptic transmission, a cognition-enhancing drug or an agent for the prophylaxis and treatment of dementia, a learning and memory disorder and a neurotransmitter release disorder.
    • 具有式(I)的环丙烷环的羧酸化合物:其中R是在碳链中任选具有一个或多个1,2-亚丙基的烷基或链烯基和/或在链末端任选具有环丙基的羧酸化合物, X是单键或亚烷基,其中提供环丙烷环数少于10-25的碳总数及其药学上可接受的盐。 化合物(I)显示突触传递的LTP样增强,允许活体中的代谢缓慢,表现出稳定的LTP样增强突触传递,并且可用作LTP样增强突触传递的药剂,a 认知增强药物或预防和治疗痴呆,学习和记忆障碍和神经递质释放障碍的药剂。
    • 10. 发明授权
    • Process for producing trans-1,4-cyclohexanedicarboxylic acid
    • 反式-1,4-环己烷二羧酸的制备方法
    • US07420086B2
    • 2008-09-02
    • US10831156
    • 2004-04-26
    • Koetsu EndouHirofumi NakamuraShinichi Tanaka
    • Koetsu EndouHirofumi NakamuraShinichi Tanaka
    • C07C61/00
    • C07C51/353C07C51/363C07C2601/14C07C61/09
    • A subject for the invention is to obtain trans-1,4-cyclohexanedicarboxylic acid (t-CHDA) in a high concentration by efficiently isomerizing cis-1,4-cyclohexanedicarboxylic acid (c-CHDA) by a simple method. The invention provides: (1) a process for producing t-CHDA which comprises heating crude CHDA to 180° C. or higher in an inert atmosphere and causing the t-CHDA formed by isomerization to precipitate in the molten c-CHDA while holding the crude CHDA at a temperature in the range of not lower than 180° C. and less than the melting point of t-CHDA; (2) a process for producing t-CHDA, wherein crude CHDA which is powdery or granular is heat-treated at a temperature of not lower than the melting point of c-CHDA and lower than the melting point of t-CHDA to thereby isomerize the cis isomer to the trans isomer while maintaining the powdery or granular state; (3) a process for producing t-CHDA, wherein crude CHDA is held at a temperature of not lower than the melting point of c-CHDA and lower than the melting point of t-CHDA in an inert atmosphere while maintaining flowing to thereby obtain powdery or granular t-CHDA; and (4) a process for purifying crude CHDA in which crude CHDA obtained through the step of hydrogenating TPA or the like is heated in an atmosphere of an inert gas to volatilize and remove impurities.
    • 本发明的目的是通过简单的方法有效地使顺式-1,4-环己烷二羧酸(c-CHDA)异构化,以高浓度获得反式-1,4-环己烷二羧酸(t-CHDA)。 本发明提供:(1)一种生产t-CHDA的方法,其包括在惰性气氛中将粗CHDA加热至180℃或更高,并使通过异构化形成的t-CHDA在熔融的c-CHDA中沉淀,同时保持 原料CHDA在不低于180℃且小于t-CHDA的熔点的温度范围内; (2)生产t-CHDA的方法,其中将粉末状或粒状的粗CHDA在不低于c-CHDA的熔点并低于t-CHDA的熔点的温度下进行热处理,从而异构化 顺式异构体反式异构体,同时保持粉状或颗粒状态; (3)生产t-CHDA的方法,其中将粗CHDA保持在不低于c-CHDA的熔点并低于在惰性气氛中的t-CHDA的熔点的温度,同时保持流动,从而获得 粉状或颗粒状t-CHDA; (4)一种纯化粗制CHDA的方法,其中通过氢化TPA等步骤得到的粗CHDA在惰性气体气氛中加热,挥发除去杂质。