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    • 1. 发明授权
    • Aromatic amide compounds and their production and use
    • 芳香族酰胺化合物及其生产和使用
    • US5480907A
    • 1996-01-02
    • US882025
    • 1992-05-13
    • Kyozo HayashiMunekazu Iinuma
    • Kyozo HayashiMunekazu Iinuma
    • C07C235/38C07D311/12C07D311/14C07D311/20A61K31/35
    • C07D311/12C07C235/38C07D311/14C07D311/20
    • Aromatic amide compounds of the formula: ##STR1## wherein R.sub.1, R.sub.2, and R.sub.3 are independently hydrogen, a lower alkyl or lower alkoxy group; Ar is an optionally substituted aromatic group; the groupC - - - -Cis C.dbd.C or HC--CH; X is hydrogen, CH.sub.2 COOH or CH.sub.2 CONHAr; and Y is hydrogen or COOH; provided that when X is CH.sub.2 COOH or Y is COOH, the COOH may be taken together with the adjacent hydroxy group on the benzene ring to form a lactone ring by dehydration, a quinone form thereof or a pharmaceutically acceptable salt thereof have potent nerve growth factor (NGF) secretion inducing activity, and are thus useful as a drug for the treatment or prophylaxis of degenerative nervous system disorders such as senilic dementis, and Alzheimer's disease.
    • 下式的芳族酰胺化合物:其中R 1,R 2和R 3独立地是氢,低级烷基或低级烷氧基; Ar是任选取代的芳族基团; C - - - C为C = C或HC-CH; X是氢,CH 2 COOH或CH 2 CONHAr; Y为氢或COOH; 条件是当X是CH 2 COOH或Y是COOH时,COOH可以与苯环上的相邻羟基一起与脱水形成内酯环,其醌形式或其药学上可接受的盐具有有效的神经生长因子 NGF)分泌诱导活性,因此可用作治疗或预防退行性神经系统疾病如老年性痴呆和阿尔茨海默氏病的药物。
    • 7. 发明申请
    • AGENT HAVING NEUROTROPHIC FACTOR-LIKE ACTIVITY
    • 具有神经营养因子活性的药剂
    • US20100204498A1
    • 2010-08-12
    • US12678671
    • 2008-09-18
    • Munekazu IinumaShoei Furukawa
    • Munekazu IinumaShoei Furukawa
    • C07C59/185
    • A61K31/20A61K31/201A61K31/23A61K31/231
    • The present invention provides a pharmaceutical agent having high safety and a neurotrophic factor-like activity, which contains, as an active ingredient, any one compound included in fatty acids each having 8 carbon atoms (C8) or having 10 carbon atoms (C10) to 12 carbon atoms (C12) or fatty acid esters thereof, such as 3,7-dimethyloctanoic acid ethyl ester, geranic acid ethyl ester, and the like, each of which has 8 carbon atoms (C8), decanoic acid methyl ester, trans-2-decenoic acid, trans-2-decenoic acid methyl ester, trans-2-decenoic acid ethyl ester, trans-2-decenoic acid-2-decenyl ester, trans-2-decenoic acid cyclohexyl ester, trans-2-decenoic acid isopropyl ester, trans-3-decenoic acid methyl ester, trans-9-decenoic acid methyl ester, and the like, each of which has 10 carbon atoms (C10), trans-10-undecenoic acid methyl ester, trans-10-undecenoic acid ethyl ester, and the like, each of which has 11 carbon atoms (C11), and dodecanoic acid, and the like, each of which has 12 carbon atoms (C12), or salts thereof or prodrugs thereof.
    • 本发明提供一种具有高安全性和神经营养因子样活性的药剂,其含有作为活性成分的包含在各自具有8个碳原子(C8)或10个碳原子(C10)的脂肪酸中的任何一种化合物, 12个碳原子(C12)或其脂肪酸酯,例如3,7-二甲基辛酸乙酯,香叶酸乙酯等,它们各自具有8个碳原子(C8),癸酸甲酯, 2-癸烯酸,反式-2-癸烯酸甲酯,反式-2-癸烯酸乙酯,反式-2-癸烯-2-癸烯基酯,反式-2-癸烯酸环己酯,反式-2-癸烯酸 异丙酯,反式-3-癸烯酸甲酯,反式-9-癸烯酸甲酯等,各自具有10个碳原子(C10),反式-10-十一碳烯酸甲酯,反式-10-十一碳烯酸 酸性乙酯等,各自具有11个碳原子(C11)和十二烷酸等,其各自具有12个碳原子 原子(C12)或其盐或其前药。