N-substituted butyramide derivatives useful for treatment of conditions
responsive to inhibition of enkephalinase
    72.
    发明授权
    N-substituted butyramide derivatives useful for treatment of conditions responsive to inhibition of enkephalinase 失效
    用于治疗对脑啡肽酶抑制作用的病症的N-取代丁酰胺衍生物

    公开(公告)号:US4939261A

    公开(公告)日:1990-07-03

    申请号:US98755

    申请日:1987-09-17

    申请人: Gary M. Ksander

    发明人: Gary M. Ksander

    摘要: Disclosed are compounds of the formula ##STR1## wherein X and Y independently represent hydroxymethyl; cyano; carboxy; functionally modified carboxy selected from esterified carboxy, carbamoyl, and N-substituted carbamoyl; 5-tetrazolyl; 2-oxazolyl, 4,5-dihydro-2-oxazolyl, 2-imidazolyl or 4,5-dihydro-2-imidazolyl or any said grouping substituted by lower alkyl; R and R.sub.0 independently represent hydrogen, lower alkyl, (C.sub.3 -C.sub.7)-cycloalkyl-lower alkyl, or aryl-lower alkyl in which aryl represents phenyl, pyridyl, thienyl, furyl, biphenyl or naphthyl, each unsubstituted or mono- or di-substituted by halogen, lower alkyl, hydroxy, acyloxy, lower alkoxy, trifluoromethyl or cyano; A represents straight chain (C.sub.2 -C.sub.5)-alkylene; or A represents straight chain (C.sub.2 -C.sub.5)-alkylene substituted by lower alkyl, by lower alkylthio-lower alkyl, by hydroxy-lower alkyl, by acyloxy-lower alkyl, by lower alkoxy-lower alkyl, by amino or acyl-amino, by amino-lower alkyl, by acylamino-lower alkyl, by (C.sub.3 -C.sub.7)-cycloalkyl, by (C.sub.3 -C.sub.7)-cycloalkyl-lower alkyl, by aryl or aryl-lower alkyl in which aryl represents phenyl or phenyl mono- or disubstituted by halogen, lower alkyl, lower alkoxy, hydroxy, acyloxy, trifluoromethyl or cyano; or A represents phenylene or cyclohexylene; pharmaceutically acceptable prodrug derivatives of any said compounds having a free carboxy group; pharmaceutically acceptable salts of any said compounds with a salt-forming group; methods for synthesis; pharmaceutical compositions thereof; and use thereof as enkephalinase inhibitors.

    摘要翻译: 公开了式(I)的化合物,其中X和Y独立地表示羟甲基; 氰基; 羧基; 选自酯化羧基,氨基甲酰基和N-取代的氨基甲酰基的官能改性羧基; 5-四唑基; 2-恶唑基,4,5-二氢-2-恶唑基,2-咪唑基或4,5-二氢-2-咪唑基或被低级烷基取代的任何所述基团; 吡啶基,噻吩基,呋喃基,联苯基或萘基,其中每个未取代或单 - 或二 - 取代的芳基 - 芳基 - 低级烷基, 被卤素,低级烷基,羟基,酰氧基,低级烷氧基,三氟甲基或氰基取代; A表示直链(C 2 -C 5) - 亚烷基; 或A表示被低级烷基,低级烷硫基 - 低级烷基,羟基 - 低级烷基,酰氧基 - 低级烷基,低级烷氧基 - 低级烷基,氨基或酰基 - 氨基取代的直链(C2-C5) - 亚烷基, 由(C 3 -C 7) - 环烷基,(C 3 -C 7) - 环烷基 - 低级烷基,被芳基或芳基 - 低级烷基取代,其中芳基或芳基 - 低级烷基,其中芳基表示苯基或苯基单 - 或 卤素,低级烷基,低级烷氧基,羟基,酰氧基,三氟甲基或氰基二取代; 或A表示亚苯基或亚环己基; 任何所述具有游离羧基的化合物的药学上可接受的前药衍生物; 任何所述化合物与成盐基团的药学上可接受的盐; 合成方法; 其药物组合物; 并将其用作脑啡肽酶抑制剂。

    Substituted 1,3-dioxolane compounds and their use as fungicides

    公开(公告)号:US4859687A

    公开(公告)日:1989-08-22

    申请号:US833503

    申请日:1986-02-20

    申请人: Peter Riebli

    发明人: Peter Riebli

    摘要: The described novel pyridine derivatives are those of the general formula I ##STR1## wherein R is hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.6 -cycloalkyl, phenyl, benzyl, phenyl substituted by C.sub.1 -C.sub.4 -alkyl, halogen, C.sub.1 -C.sub.4 -alkoxy, NO.sub.2 and/or CF.sub.3, or benzyl substituted by C.sub.1 -C.sub.4 -alkyl, halogen, C.sub.1 -C.sub.4 -alkoxy, NO.sub.2 and/or CF.sub.3,R.sub.1 and R.sub.2 independently of one another are each hydrogen, C.sub.1 -C.sub.4 -alkyl, halogen or C.sub.1 -C.sub.4 -alkoxy,R.sub.3, R.sub.4 and R.sub.5 independently of one another are each hydrogen, halogen, CF.sub.3, NO.sub.2, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, phenyl, or phenyl substituted by C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, halogen, NO.sub.2 and/or CF.sub.3,U and V independently of one another are each C.sub.1 -C.sub.6 -alkyl, or alkyl substituted by halogen or C.sub.1 -C.sub.4 -alkoxy, or together form one of the following alkylene bridges: ##STR2## R.sub.a is hydrogen, C.sub.1 -C.sub.12 -alkyl, C.sub.1 -C.sub.12 -alkyl which is mono- or polysubstituted by halogen, or is phenyl, phenyl which is mono- or polysubstituted by halogen and/or C.sub.1 -C.sub.4 -alkyl, or is the group --CH.sub.2 --Z--R.sub.h,R.sub.b is C.sub.1 -C.sub.12 -alkyl, C.sub.1 -C.sub.12 -alkyl which is mono- or polysubstituted by halogen, or is phenyl, phenyl which is mono- or polysubstituted by halogen and/or C.sub.1 -C.sub.4 -alkyl, or is the group --CH.sub.2 --Z--R.sub.h, whereinZ is oxygen or sulfur, andR.sub.h is hydrogen, C.sub.1 -C.sub.8 -alkyl, C.sub.1 -C.sub.8 -alkyl which is substituted by C.sub.1 -C.sub.4 -alkoxy, or is C.sub.3 -C.sub.4 -alkenyl, 2-propynyl, 3-halo-2-propynyl, phenyl, phenyl which is substituted by halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, NO.sub.2 and/or CF.sub.3, or is benzyl, or benzyl substituted by halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, NO.sub.2 and/or CF.sub.3,R.sub.c, R.sub.d and R.sub.f independently of one another are each hydrogen or C.sub.1 -C.sub.4 -alkyl, andR.sub.g is hydrogen or C.sub.1 -C.sub.4 -alkyl; including the acid addition salts thereof.There is also described the production of these substances, as well as agrochemical compositions containing these substances as active ingredients for controlling phytopathogenic microorganisms.

    Novel compositions prepared from alkyl substituted nitrogen-containing
aromatic heterocyclic compounds and dicarboxylic acid monoanhydrides
    80.
    发明授权
    Novel compositions prepared from alkyl substituted nitrogen-containing aromatic heterocyclic compounds and dicarboxylic acid monoanhydrides 失效
    由烷基取代的含氮芳族杂环化合物和二羧酸一酸酐制备的新型组合物

    公开(公告)号:US4725373A

    公开(公告)日:1988-02-16

    申请号:US831966

    申请日:1986-02-24

    IPC分类号: C07D213/50 C23F11/14

    摘要: New compositions of matter are disclosed which are the products resulting from reacting an alkyl substituted aromatic heterocyclic nitrogen-containing compound such as 2,4,6-trimethylpyridine or 2,3,5,6-tetramethylpyrazine with a dicarboxylic acid monoanhydride such as 2-dodecen-1-yl succinic anhydride. These compositions are useful in preventing corrosion of metallic articles in corrosive environments. They are particularly useful in down hole oil and gas well applications.

    摘要翻译: 公开了新的物质组合物,其是使烷基取代的芳族杂环含氮化合物如2,4,6-三甲基吡啶或2,3,5,6-四甲基吡嗪与二羧酸单酐如2- 十二碳烯-1-基琥珀酸酐。 这些组合物可用于防止金属制品在腐蚀性环境中的腐蚀。 它们在井下油气井应用中特别有用。