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14 条记录 (耗时 0.01 秒)

    1,4-disubstituted piperazines
    2.
    发明授权
    1,4-disubstituted piperazines 失效
    1,4-取代的哌嗪

    公开(公告)号：US5177077A

    公开(公告)日：1993-01-05

    申请号：US728492

    申请日：1991-07-11

    申请人： Rolf Hohlweg ,  Erling Guddal ,  Erik Nielsen

    发明人： Rolf Hohlweg ,  Erling Guddal ,  Erik Nielsen

    IPC分类号： C07D333/16 ,  C07D409/12

    CPC分类号： C07D409/12 ,  C07D333/16

    摘要： A disubstituted piperazine compound having the formula I ##STR1## wherein R.sup.1 is thienyl or phenyl, which may be substituted with C.sub.1-6 -alkyl or halogen, and R.sup.2 is thienyl, which may be substituted with C.sub.1-6 -alkyl or halogen, and R.sup.3 is C.sub.1-8 -alkyl, C.sub.3-8 -alkenyl or C.sub.3-8 -cycloalkyl which all may be substituted with hydroxy, oximino or keto in any position giving a stable tertiary amine or R.sup.3 is C.sub.1-8 -alkyl or C.sub.3-8 -alkenyl which in any position may be substituted as above, but is terminally substituted with phenoxy, phenyl, thienyl, furyl, methoxy or --CN and pharmaceutically acceptable acid addition salts thereof.The compounds are useful in the treatment of mental disorders in which a dopaminergic deficit is implicated.

    摘要翻译： 具有式I的二取代哌嗪化合物（I）其中R 1是噻吩基或苯基，其可以被C 1-6 - 烷基或卤素取代，R 2是噻吩基，其可以被C 1-6 - 烷基或 卤素和R 3是C 1-8 - 烷基，C 3-8 - 烯基或C 3-8 - 环烷基，其全部可以被羟基，肟基或酮基取代，得到稳定的叔胺或R3是C1-8 - 烷基或 在任何位置可以如上所述被取代，但被苯氧基，苯基，噻吩基，呋喃基，甲氧基或-CN末端取代的C 3-8 - 烯基及其药学上可接受的酸加成盐。 这些化合物可用于治疗涉及多巴胺能缺乏症的精神障碍。

    p-Trimethylsilyloxyphenyl glycyloxy succinimide
    5.
    发明授权
    p-Trimethylsilyloxyphenyl glycyloxy succinimide 失效
    对三甲基甲硅烷氧基苯基甘氨酰氧基琥珀酰亚胺

    公开(公告)号：US4178294A

    公开(公告)日：1979-12-11

    申请号：US847855

    申请日：1977-11-02

    申请人： Erling Guddal

    发明人： Erling Guddal

    IPC分类号： C07F7/18

    CPC分类号： C07F7/1804

    摘要： p-Trimethylsilyloxy-D-(-)-phenylglycyloxysuccinimide or -phthalimide, process of preparing p-trimethylsilyloxy-D-(-)-phenylglycyloxysuccinimide or -phthalimide by reacting D-(-)-p-trimethylsilyloxyphenylglycin-N-carboxyanhydride with a N-hydroxyimide, and process for preparing 6-(p-hydroxyphenylglycylamido)-penam or 7-(p-hydroxyphenylglycylamido)-cephem compounds by reacting p-trimethylsilyloxy-D-(-)-phenylglycyloxysuccinimide or -phthalimide with a phosphite amide or an ester of 6-aminopenicillanic acid or of an ester of a 7-amino-3-cephem-4-carboxylic acid in the presence of the hydrochloride of a weak amine.

    摘要翻译： 对 - 三甲基甲硅烷氧基-D-（ - ） - 苯基甘氨酰氧基琥珀酰亚胺或邻苯二甲酰亚胺，通过使D - （ - ） - 对三甲基甲硅烷氧基苯基甘氨酸-N-羧酸酐与N（ - ） - - 对 - 羟基酰亚胺，以及通过使对三甲基甲硅烷氧基-D - （ - ） - 苯基甘氨酰氧基琥珀酰亚胺或邻苯二甲酰亚胺与亚磷酸酯酰胺或酯反应制备6-（对羟基苯基甘氨酰胺基） - 苯甲酸或7-（对羟基苯基甘氨酰胺基） 的6-氨基青霉烷酸或7-氨基-3-头孢烯-4-羧酸的酯在弱胺的盐酸盐存在下进行。

    1,4-disubstituted piperazines
    8.
    发明授权
    1,4-disubstituted piperazines 失效
    1,4-二取代的哌嗪

    公开(公告)号：US5276035A

    公开(公告)日：1994-01-04

    申请号：US879518

    申请日：1992-05-04

    申请人： Rolf Hohlweg ,  Erling Guddal ,  Erik B. Nielsen

    发明人： Rolf Hohlweg ,  Erling Guddal ,  Erik B. Nielsen

    IPC分类号： C07D261/08 ,  C07D263/10 ,  C07D271/06 ,  C07D295/084 ,  C07D295/088 ,  C07D295/15 ,  C07D333/20 ,  C07D333/22 ,  C07F9/6509 ,  A61K31/495 ,  A61K33/42 ,  C07D409/06

    CPC分类号： C07D263/10 ,  C07D261/08 ,  C07D271/06 ,  C07D295/084 ,  C07D295/088 ,  C07D295/15 ,  C07D333/20 ,  C07D333/22 ,  C07F9/650958

    摘要： A disubstituted piperazine compound having the formula ##STR1## wherein R.sup.1 is halogen, methoxy, C.sub.1-6 -alkyl or trifluoromethyl, and R.sup.2 is methyl or substituted C.sub.1-8 -alkyl, C.sub.3-8 -alkenyl or C.sub.3-8 -cycloalkyl, where substituents may be hydroxy-, keto- or oximino-groups in any position leading to a stable tertiary amine; or R.sup.2 is a straight or branched C.sub.1-8 -alkyl or C.sub.3-8 -alkenyl, which in any position may be substituted as above, but is terminally substituted with one of the following groups: cyano, optionally C.sub.1-4 -alkoxy-substituted C.sub.1-4 -alkoxy, dimethoxy, optiontionally substituted phenoxy, phosphonic acid, thienyl, furyl, oxazoline, isoxazole, oxadiazole, where the optional substitution is represented by C.sub.1-6 -alkyl or phenyl, provided that when cyano is the only substituent in R.sup.2, R.sup.2 must contain at least four carbon atoms, and pharmaceutically acceptable acid addition salts thereof.The compounds are useful in the treatment of mental disorders in which a dopaminergic deficit is implicated.

    摘要翻译： 具有式（I）的二取代哌嗪化合物，其中R 1是卤素，甲氧基，C 1-6 - 烷基或三氟甲基，R 2是甲基或取代的C 1-8 - 烷基，C 3-8 - 烯基或C 3-8 - 环烷基，其中取代基可以是导致稳定叔胺的任何位置的羟基，酮基或肟基; 或R 2是直链或支链C 1-8 - 烷基或C 3-8 - 烯基，其在任何位置可以如上所述被取代，但被下列基团之一末端取代：氰基，任选地C 1-4 - 烷氧基取代 C 1-4 - 烷氧基，二甲氧基，选择性取代的苯氧基，膦酸，噻吩基，呋喃基，恶唑啉，异恶唑，恶二唑，其中任选的取代由C 1-6 - 烷基或苯基表示，条件是当氰基是R 2中的唯一取代基 ，R2必须含有至少四个碳原子，及其药学上可接受的酸加成盐。 这些化合物可用于治疗涉及多巴胺能缺乏症的精神障碍。

    P-Trimethylsilyloxyphenyl glycyloxyphthalimide
    10.
    发明授权
    P-Trimethylsilyloxyphenyl glycyloxyphthalimide 失效
    对三甲苯磺酰基苯乙酰乙酰胆碱酯

    公开(公告)号：US4098796A

    公开(公告)日：1978-07-04

    申请号：US693516

    申请日：1976-06-07

    申请人： Erling Guddal

    发明人： Erling Guddal

    IPC分类号： C07D499/00 ,  C07F7/18 ,  C07D209/34

    CPC分类号： C07F7/1856 ,  C07D499/00

    摘要： P-Trimethylsilyloxy-D-(-)-phenylglycyloxysuccinimide or -phthalimide, process of preparing p-trimethylsilyloxy-D-(-)-phenylglycyloxysuccinimide or -phthalimide by reacting D-(-)-p-trimethylsilyloxyphenylglycin-N-carboxyanhydride with a N-hydroxyimide, and process for preparing 6-(p-hydroxyphenylglycylamido)-penam or 7-(p-hydroxyphenylglycylamido)-cephem compounds by reacting p-trimethylsilyloxy-D-(-)-phenylglycyloxysuccinimide or -phthalimide with a phosphite amide of an ester of 6-aminopenicillanic acid or of an ester of a 7-amino-3-cephem-4-carboxylic acid in the presence of the hydrochloride of a weak amine.