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    • 5. 发明授权
      US08003693B2 Modulation of anxiety through blockade of anandamide hydrolysis 有权
    • Modulation of anxiety through blockade of anandamide hydrolysis
    • 通过封闭anandamide水解调节焦虑
    • US08003693B2
    • 2011-08-23
    • US11496051
    • 2006-07-28
    • Daniele Piomelli , Andrea Duranti , Andrea Tontini , Marco Mor , Giorgio Tarzia
    • Daniele Piomelli , Andrea Duranti , Andrea Tontini , Marco Mor , Giorgio Tarzia
    • A61K31/27
    • C07C311/29 , C07C271/56 , C07C275/54 , C07C2601/14 , C07D209/08 , C07D211/06 , C07D215/06 , C07D307/79 , C07D487/04
    • Fatty acid amide hydrolase inhibitors of the Formula: are provided wherein X is NH, CH2, O, or S; Q is O or S; Z is O or N; R is an aromatic moiety selected from the group consisting of substituted or unsubstituted aryl; substituted or unsubstituted biphenylyl, substituted or unsubstituted naphthyl, and substituted or unsubstituted phenyl; substituted or unsubstituted terphenylyl; substituted or unsubstituted cycloalkyl, heteroaryl, or alkyl; and R1 and R2 are independently selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, and substituted or unsubstituted phenyl, substituted or unsubstituted biphenylyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; with the proviso that if Z is O, one of R1 and R2 is absent, and that if Z is N, optionally R1 and R2 may optionally be taken together to form a substituted or unsubstituted N-heterocycle or substituted or unsubstituted heteroaryl with the N atom to which they are each attached. Pharmaceutical compositions comprising the compounds of Formula I and methods of using them to inhibit FAAH and/or treat appetite disorders, glaucoma, pain, insomnia, and neurological and psychological disorders including anxiety disorders, epilepsy, and depression are provided.
    • 提供了下式的脂肪酸酰胺水解酶抑制剂：其中X是NH，CH 2，O或S; Q是O或S; Z是O或N; R是选自取代或未取代的芳基的芳族部分; 取代或未取代的联苯基，取代或未取代的萘基和取代或未取代的苯基; 取代或未取代的三联苯基; 取代或未取代的环烷基，杂芳基或烷基; 并且R 1和R 2独立地选自H，取代或未取代的烷基，取代或未取代的杂烷基和取代或未取代的苯基，取代或未取代的联苯基，取代或未取代的芳基和取代或未取代的杂芳基; 条件是如果Z是O，则不存在R 1和R 2之一，并且如果Z是N，则任选地R 1和R 2可以任选地一起形成取代或未取代的N-杂环或具有取代或未取代的杂芳基，其中N 它们各自附着的原子。 提供了包含式I化合物的药物组合物及其用于抑制FAAH和/或治疗食欲障碍，青光眼，疼痛，失眠以及包括焦虑障碍，癫痫和抑郁症在内的神经和心理障碍的方法。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 8. 发明授权
      US4211709A Aminopyrrole derivatives 失效
    • Aminopyrrole derivatives
    • 氨基吡咯衍生物
    • US4211709A
    • 1980-07-08
    • US960386
    • 1978-11-13
    • Giorgio Tarzia , Gianbattista Panzone
    • Giorgio Tarzia , Gianbattista Panzone
    • C07D207/34 , C07D207/36 , C07D209/40 , C07D207/44
    • C07D209/40 , C07D207/34 , C07D207/36
    • Pharmacologically-active aminopyrrole derivatives of the formula ##STR1## wherein: R is selected from hydrogen, (C.sub.1-4)alkyl, benzyl and chlorobenzyl;R.sub.1 is selected from hydrogen, (C.sub.1-4)alkyl, phenyl and phenyl substituted by a radical selected from methyl, ethyl, methoxy, ethoxy, benzyloxy, fluoro, chloro and bromo;R.sub.2 and R.sub.3 individually represent hydrogen or (C.sub.1-4)alkyl or, taken together, represent an isopropylidene, a benzylidene or a chlorobenzylidene radical;R.sub.4 is selected from (C.sub.2-4)alkanoyl; carbo(C.sub.1-3)alkoxy; benzoyl, benzoyl substituted by a radical selected from chloro, methoxy or ethoxy; carbamoyl, methylcarbamoyl and phenyl carbamoyl;R.sub.5 is selected from hydrogen, (C.sub.1-4)alkyl, carbo(C.sub.1-3)alkoxy, carbomethoxymethyl, carbethoxymethyl, trifluoromethyl and carbamoyl, with the proviso that when R is hydrogen, R.sub.1 and R.sub.5 are methyl and R.sub.4 is carbethoxy, and R.sub.2 and R.sub.3 cannot simultaneously represent hydrogen;and a salt thereof with a pharmaceutically-acceptable acid.The compounds have anti-inflammatory and CNS-depressant utility. They are also useful as analgesics and antipyretics and display a very low degree of anti-ulcerogenic activity.
    • 式（Ia）的药理学活性氨基吡咯衍生物，其中：R选自氢，（C 1-4）烷基，苄基和氯苄基; R 1选自氢，（C 1-4）烷基，苯基和被选自甲基，乙基，甲氧基，乙氧基，苄氧基，氟，氯和溴的基团取代的苯基; R2和R3分别表示氢或（C1-4）烷基，或者一起表示异亚丙基，亚苄基或氯亚苄基; R4选自（C2-4）烷酰基; 碳（C 1-3）烷氧基; 苯甲酰基，被选自氯，甲氧基或乙氧基的基团取代的苯甲酰基; 氨基甲酰基，甲基氨基甲酰基和苯基氨基甲酰基; R 5选自氢，（C 1-4）烷基，碳（C 1-3）烷氧基，甲酯基甲基，乙氧羰基甲基，三氟甲基和氨基甲酰基，条件是当R为氢时，R 1和R 5为甲基，R 4为乙氧羰基， 而R3不能同时代表氢; 及其与药学上可接受的酸的盐。 该化合物具有抗炎和CNS抑制作用。 它们也可用作镇痛药和解热药，并显示非常低程度的抗溃疡活性。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 9. 发明授权
      US4072689A Monoamino 2,4,5-trisubstituted oxazoles 失效
    • Monoamino 2,4,5-trisubstituted oxazoles
    • 单氨基2,4,5-三取代的恶唑
    • US4072689A
    • 1978-02-07
    • US641410
    • 1975-12-17
    • Giorgio Tarzia
    • Giorgio Tarzia
    • C07D263/34
    • C07D263/34
    • Pharmacologically active 2,4,5-trisubstituted oxazoles of the general formula ##STR1## wherein A is cyclohexyl, thienyl or a group of the formula ##STR2## in which R represents one to three substituents each independently selected from the group consisting of hydrogen, lower alkyl, halo, halo-lower alkyl, lower alkoxy, nitro, cyano, amino, carbamoyl, acetamino or carboxy; one of the R.sub.1 and R.sub.2 groups is a lower alkyl group and the other is an amido group, ##STR3## wherein R.sub.3 is selected from the group consisting of hydrogen, lower alkyl, lower alkenyl, cycloalkyl, phenyl, substituted phenyl, phenyl-lower alkyl, hydroxy-lower alkyl, lower acyloxy-lower alkyl, hydroxy, amino, lower alkylideneamino, cycloalkylideneamino, benzylideneamino and R.sub.4 is selected from hydrogen, lower alkyl, lower alkenyl, cycloalkyl, phenyl, substituted phenyl, phenyl-lower alkyl, hydroxy-lower alkyl, lower acyloxy-lower alkyl, or R.sub.3 and R.sub.4 taken together with the nitrogen atom may also form a 5- to 7-membered hetero ring which may contain one other hetero atom selected from N, O and S. The compounds have antiinflammatory activity.
    • 其中A是环己基，噻吩基或式“IMAGE”的基团，其中R表示一至三个独立地选自以下的取代基的药学活性的2,4,5-三取代的恶唑： 氢，低级烷基，卤素，卤代低级烷基，低级烷氧基，硝基，氰基，氨基，氨基甲酰基，乙酰氨基或羧基; R1和R2之一是低级烷基，另一个是酰胺基，其中R 3选自氢，低级烷基，低级烯基，环烷基，苯基，取代的苯基，苯基 - 低级 烷基，羟基 - 低级烷基，低级酰氧基 - 低级烷基，羟基，氨基，低级亚烷基氨基，亚环烷基氨基，亚苄基氨基和R4选自氢，低级烷基，低级烯基，环烷基，苯基，取代的苯基，苯基 - 低级烷基， 低级烷基，低级酰氧基 - 低级烷基或R3和R4与氮原子一起也可以形成5-7元杂环，其可以含有选自N，O和S的另一个杂原子。该化合物具有抗炎作用 活动。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
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