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    N-aryl-N-(1-substituted-3-alkoxy-4-piperidinyl)amides and pharmaceutical compositions and methods employing such compounds
    4.
    发明授权
    N-aryl-N-(1-substituted-3-alkoxy-4-piperidinyl)amides and pharmaceutical compositions and methods employing such compounds 失效
    N-芳基-N-（1-取代-3-烷氧基-4-哌啶基）酰胺和使用这些化合物的药物组合物和方法

    公开(公告)号：US4994471A

    公开(公告)日：1991-02-19

    申请号：US351360

    申请日：1989-05-12

    申请人： Nhora L. Lalinde ,  John Moliterni ,  H. Kenneth Spencer

    发明人： Nhora L. Lalinde ,  John Moliterni ,  H. Kenneth Spencer

    IPC分类号： C07D211/58 ,  C07D401/06 ,  C07D409/06

    CPC分类号： C07D401/06 ,  C07D211/58 ,  C07D409/06

    摘要： This invention pertains to novel N-aryl-N-[N-substituted 3-alkoxy-4-piperidinyl]amides useful as analgesics, and methods of administering analgesia, which comprises the systemic administration to mammals of such compounds, and pharmaceutical compositions containing such compounds, wherein the novel compounds have the general formula: ##STR1## including optically active isomeric forms, cis/trans isomeric forms and the pharmaceutically acceptable acid addition salts therof, wherein:R is an aryl group selected from the group consisting of phenyl and substituted phenyl, wherein the substituents on the phenyl group are independently selected from the group consisting of halogen, lower-alkyl, lower-alkoxy, and combinations thereof;R.sub.1 is an alkyl group selected from the group consisting of lower-alkyl, lower-alkenyl, and lower-alkoxy lower-alkyl, each alkyl group having from 1 to 6 carbon atoms;R.sub.2 is a member selected from the group consisting of phenyl lower-alkyl, thienyl lower-alkyl, pyrazolyl lower-alkyl, tetrazolyl lower-alkyl, 4,5-dihydro-5-oxo-1H-tetrazolyl lower-alkyl, 1,3-dihydro-1,3-dioxo-2H-isoindolyl lower-alkyl, and 2,3-dihydro-2-oxo-1H-benzimidazolyl lower-alkyl; andR.sub.3 is a member selected from the group consisting of hydrogen, lower-alkyl and lower-alkyl aryl.

    摘要翻译： 本发明涉及可用作止痛剂的新型N-芳基-N- [N-取代的3-烷氧基-4-哌啶基]酰胺和施用镇痛的方法，其包括向这些化合物的哺乳动物全身施用，以及含有这些化合物的药物组合物 化合物，其中新化合物具有以下通式：包括旋光异构体形式的顺式/反式异构体形式和其药学上可接受的酸加成盐，其中：R是选自以下的芳基： 苯基和取代的苯基，其中苯基上的取代基独立地选自卤素，低级烷基，低级烷氧基及其组合; R1是选自低级烷基，低级烯基和低级烷氧基低级烷基，每个烷基具有1至6个碳原子的烷基; R2是选自苯基低级烷基，噻吩基低级烷基，吡唑基低级烷基，四唑基低级烷基，4,5-二氢-5-氧代-1H-四唑基低级烷基，1,3 二氢-1,3-二氧代-2H-异吲哚基低级烷基和2,3-二氢-2-氧代-1H-苯并咪唑基低级烷基; 并且R 3是选自氢，低级 - 烷基和低级 - 烷基芳基的成员。

    N-aryl-n-(1-substituted-3-alkoxy-4-piperidinyl)amides and pharmaceutical compositions and methods employing such compounds
    6.
    发明授权
    N-aryl-n-(1-substituted-3-alkoxy-4-piperidinyl)amides and pharmaceutical compositions and methods employing such compounds 失效
    N-芳基 - 正（1-取代-3-烷氧基-4-哌啶基）酰胺和使用这些化合物的药物组合物和方法

    公开(公告)号：US5100903A

    公开(公告)日：1992-03-31

    申请号：US617122

    申请日：1990-11-21

    申请人： Nhora L. Lalinde ,  John Moliterni ,  H. Kenneth Spencer

    发明人： Nhora L. Lalinde ,  John Moliterni ,  H. Kenneth Spencer

    IPC分类号： C07D211/58 ,  C07D401/06 ,  C07D409/06

    CPC分类号： C07D401/06 ,  C07D211/58 ,  C07D409/06

    摘要： This invention pertains to novel N-aryl-N-[N-substituted 3-alkoxy-4-piperidinyl]amides useful as analgesics, and methods of administering analgesia, which comprises the systemic administration to mammals of such compounds, and pharmaceutical compositions containing such compounds, wherein the novel compounds have the general formula: ##STR1## including optically active isomeric forms, cis/trans isomeric forms and the pharmaceutically acceptable acid addition salts thereof, wherein:R is an aryl group selected from the group consisting of phenyl and substituted phenyl, wherein the substituents on the phenyl group are independently selected from the group consisting of halogen, lower-alkyl, lower-alkoxy, and combinations thereof;R.sub.1 is an alkyl group selected from the group consisting of lower-alkyl, lower-alkenyl, and lower-alkoxy lower-alkyl, each alkyl group having from 1 to 6 carbon atoms;R.sub.2 is a member selected from the group consisting of phenyl lower-alkyl, thienyl lower-alkyl, pyrazolyl lower-alkyl, tetrazolyl lower-alkyl, 4,5-dihydro-5-oxo-1H-tetrazolyl lower-alkyl, 1,3-dihydro-1,3-dioxo-2H-isoindolyl lower-alkyl, and 2,3-dihydro-2-oxo-1H-benzimidazolyl lower-alkyl; andR.sub.3 is a member selected from the group consisting of hydrogen, lower-alkyl and lower-alkyl aryl.

    摘要翻译： 本发明涉及可用作止痛剂的新型N-芳基-N- [N-取代的3-烷氧基-4-哌啶基]酰胺和施用镇痛的方法，其包括向这些化合物的哺乳动物全身施用，以及含有这些化合物的药物组合物 化合物，其中新化合物具有以下通式：包括旋光异构体形式的顺式/反式异构体形式及其药学上可接受的酸加成盐，其中：R是选自以下的芳基： 苯基和取代的苯基，其中苯基上的取代基独立地选自卤素，低级烷基，低级烷氧基及其组合; R1是选自低级烷基，低级烯基和低级烷氧基低级烷基，每个烷基具有1至6个碳原子的烷基; R2是选自苯基低级烷基，噻吩基低级烷基，吡唑基低级烷基，四唑基低级烷基，4,5-二氢-5-氧代-1H-四唑基低级烷基，1,3 二氢-1,3-二氧代-2H-异吲哚基低级烷基和2,3-二氢-2-氧代-1H-苯并咪唑基低级烷基; 并且R 3是选自氢，低级 - 烷基和低级 - 烷基芳基的成员。

    Analgesic N-aryl-N-[1-substituted-3,5-dimethyl-4-piperidinyl]amides
    7.
    发明授权
    Analgesic N-aryl-N-[1-substituted-3,5-dimethyl-4-piperidinyl]amides 失效
    止痛N-芳基-N- [1-取代-3,5-二甲基-4-哌啶基]酰胺

    公开(公告)号：US4939161A

    公开(公告)日：1990-07-03

    申请号：US351677

    申请日：1989-05-12

    申请人： Nhora L. Lalinde ,  John Moliterni ,  H. Kenneth Spencer

    发明人： Nhora L. Lalinde ,  John Moliterni ,  H. Kenneth Spencer

    IPC分类号： C07D211/58 ,  C07D401/06

    CPC分类号： C07D401/06 ,  C07D211/58

    摘要： This invention pertains to novel substituted N-aryl-N-[1-substituted 3,5-dimethyl-4-piperidinyl]amides useful as analgesics, and methods of administering analgesia, which comprises the systemic administration to mammals of such compounds, and pharmaceutical compositions containing such compounds, wherein the novel compounds have the general formula: ##STR1## including optically active isomeric forms, cis/trans isomeric forms and the pharmaceutically acceptable acid addition salts thereof, wherein:R.sub.1 is an alkyl group selected from the group consisting of lower-alkyl, and lower-alkoxy lower-alkyl, each alkyl group having from 1 to 6 carbon atoms; andR.sub.2 is a member selected from the group consisting of phenyl lower-alkyl, pyridinyl, lower-alkyl, thienyl lower-alkyl, pyrazolyl lower-alkyl, tetrazolyl lower-alkyl, 4,5-dihydro-5-oxo-1H-tetrazolyl lower-alkyl, 1,3-dihydro-1,3-dioxo-2H-isoindolyl (N-phthalimidyl) lower-alkyl, and 2,3-dihydro-2-oxo-1H-benzimidazolyl lower-alkyl.

    摘要翻译： 本发明涉及可用作止痛剂的新型取代的N-芳基-N- [1-取代的3,5-二甲基-4-哌啶基]酰胺，以及施用镇痛的方法，其包括向这些化合物的哺乳动物全身给药，以及药物 含有这些化合物的组合物，其中新化合物具有以下通式：包括旋光异构体形式的顺式/反式异构体形式及其药学上可接受的酸加成盐，其中：R 1是选自 由低级烷基和低级烷氧基低级烷基组成的基团，每个烷基具有1至6个碳原子; 并且R 2是选自苯基低级烷基，吡啶基，低级烷基，噻吩基低级烷基，吡唑基低级烷基，四唑基低级烷基，4,5-二氢-5-氧代-1H-四唑基 低级烷基，1,3-二氢-1,3-二氧代-2H-异吲哚基（N-苯二酰亚氨基）低级烷基和2,3-二氢-2-氧代-1H-苯并咪唑基低级烷基。