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    • 4. 发明授权
      US4916142A N-heterocyclic-N-(4-piperidinyl)amides and pharmaceutical compositions and their use as analgesics 失效
    • N-heterocyclic-N-(4-piperidinyl)amides and pharmaceutical compositions and their use as analgesics
    • N-杂环-N-（4-哌啶基）酰胺和药物组合物及其作为止痛剂的用途
    • US4916142A
    • 1990-04-10
    • US362119
    • 1989-06-06
    • Jerome R. Bagley , H. Kenneth Spencer
    • Jerome R. Bagley , H. Kenneth Spencer
    • C07D211/58 , C07D211/72 , C07D401/12 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14 , A61K31/44 , C07D213/02 , C07D239/02
    • C07D401/12 , C07D211/58 , C07D211/72 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14
    • This invention pertains to novel substituted N-heterocyclic-N-(4-piperidinyl)amides useful as analgesics and antagonists of opiolds, wherein the compounds have the general formula: ##STR1## including optically active isomeric forms, and the pharmaceutically acceptable acid addition salts thereof, wherein:R is a substituted or unsubstituted unsaturated heterocyclic ring system having 5 to 6 cyclic member atoms containing at least one nitrogen atom, and is preferably selected from the group consisting of pyridinyl, pyrimidinyl, and pyrazinyl;R.sub.1 is selected from the group consisting of unsubstituted or substituted heterocyclic ring systems having 5 cyclic member atoms, lower cyclic alkyl ring systems, lower-alkyl and lower-alkoxy lower-alkyl, and is preferably selected from the group consisting of furanyl lower-alkyl, thienyl lower-alkyl, pyrrolyl lower-alkyl, lower-alkyl, lower-cycloalkyl, and lower-alkoxy lower-alkyl of 2 to 6 carbons;R.sub.2 is a cyclic ring system lower-alkyl having 5 to 6 cyclic member atoms, and is preferably selected from the group consisting of phenyl lower-alkyl, thienyl lower-alkyl, thienyl hydroxy lower-alkyl, pyrazoyl lower-alkyl, and (4,5-dihydro-5-oxo-1H-tetrazol-1-yl) lower-alkyl which may be substituted in the 4-position with a group selected from lower-alkyl; andR.sub.3 is selected from the group consisting of hydrogen and methyl.
    • 本发明涉及用作阿片类药物的止痛剂和拮抗剂的新型取代的N-杂环-N-（4-哌啶基）酰胺，其中化合物具有以下通式：包括旋光异构体形式的和其药学上可接受的酸加成盐 其中：R是具有5至6个含有至少一个氮原子的环状原子的取代或未取代的不饱和杂环系，优选选自吡啶基，嘧啶基和吡嗪基; R1选自具有5个环状成员原子的未取代或取代的杂环系，低级环烷基环系，低级烷基和低级烷氧基低级烷基，优选选自呋喃基低级烷基 2至6个碳原子的噻吩基低级烷基，吡咯基低级烷基，低级烷基，低级环烷基和低级烷氧基低级烷基; R2是具有5至6个环状原子的环状体系的低级烷基，优选选自苯基低级烷基，噻吩基低级烷基，噻吩基羟基低级烷基，吡唑基低级烷基和（4 可以在4-位上被选自低级烷基的基团取代的5-二氢-5-氧代-1H-四唑-1-基）低级烷基; 并且R 3选自氢和甲基。
    • 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
    • 5. 发明授权
      US4912109A N-heterocyclic-N-(4-piperidinyl) amides and pharmaceutical compositions and methods employing such compounds 失效
    • N-heterocyclic-N-(4-piperidinyl) amides and pharmaceutical compositions and methods employing such compounds
    • N-杂环-N-（4-哌啶基）酰胺和使用这些化合物的药物组合物和方法
    • US4912109A
    • 1990-03-27
    • US282092
    • 1988-12-09
    • Jerome R. Bagley , H. Kenneth Spencer
    • Jerome R. Bagley , H. Kenneth Spencer
    • C07D211/58 , C07D211/72 , C07D401/12 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14
    • C07D401/12 , C07D211/58 , C07D211/72 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14
    • This invention pertains to novel substituted N-heterocyclic-N-(4-piperidinyl)amides useful as analgesics and antagonists of opiods, wherein the compounds have the general formula: ##STR1## including optically active isomeric forms, and the pharmaceutically acceptable acid addition salts thereof, wherein:R is a substituted or unsubstituted unsaturated heterocyclic ring system having 5 to 6 cyclic member atoms containing at least one nitrogen atom, and is preferably selected from the group consisting of pyridinyl, pyrimidinyl, and pyrazinyl;R.sub.1 is selected from the group consisting of unsubstituted or substituted heterocyclic ring systems having 5 cyclic member atoms, lower cyclic alkyl ring systems, lower-alkyl and lower-alkoxy lower-alkyl, and is preferably selected from the group consisting of furanyl lower-alkyl, thienyl lower-alkyl, pyrrolyl lower-alkyl, lower-alkyl, lower-cycloalkyl, and lower-alkoxy lower-alkyl of 2 to 6 carbons;R.sub.2 is a cyclic ring system lower-alkyl having 5 to 6 cyclic member atoms, and is preferably selected from the group consisting of phenyl lower-alkyl, thienyl lower-alkyl, thienyl hydroxy lower-alkyl, pyrazoyl lower-alkyl, and (4,5-dihydro-5-oxo-1H-tetrazol-1-yl) lower-alkyl which may be substituted in the 4-position with a group selected from lower-alkyl; andR.sub.3 is selected from the group consisting of hydrogen and methyl.
    • 本发明涉及用作阿片类止痛剂和拮抗剂的新型取代的N-杂环-N-（4-哌啶基）酰胺，其中该化合物具有以下通式：包括旋光异构体形式的“IMAGE”和其药学上可接受的酸加成盐 其中：R是具有5至6个含有至少一个氮原子的环状原子的取代或未取代的不饱和杂环系，优选选自吡啶基，嘧啶基和吡嗪基; R1选自具有5个环状成员原子的未取代或取代的杂环系，低级环烷基环系，低级烷基和低级烷氧基低级烷基，优选选自呋喃基低级烷基 2至6个碳原子的噻吩基低级烷基，吡咯基低级烷基，低级烷基，低级环烷基和低级烷氧基低级烷基; R2是具有5至6个环状原子的环状体系的低级烷基，优选选自苯基低级烷基，噻吩基低级烷基，噻吩基羟基低级烷基，吡唑基低级烷基和（4 可以在4-位上被选自低级烷基的基团取代的5-二氢-5-氧代-1H-四唑-1-基）低级烷基; 并且R 3选自氢和甲基。
    • 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
    • 8. 发明授权
      US4954506A N-heterocyclic-N-(4-piperidinyl)amides and pharmaceutical compositions and methods employing such compounds 失效
    • N-heterocyclic-N-(4-piperidinyl)amides and pharmaceutical compositions and methods employing such compounds
    • N-杂环-N-（4-哌啶基）酰胺和使用这些化合物的药物组合物和方法
    • US4954506A
    • 1990-09-04
    • US468381
    • 1990-01-22
    • Jerome R. Bagley , H. Kenneth Spencer
    • Jerome R. Bagley , H. Kenneth Spencer
    • C07D211/58 , C07D211/72 , C07D401/12 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14
    • C07D401/12 , C07D211/58 , C07D211/72 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14
    • This invention pertains to novel substituted N-heterocyclic-N-(4-piperidinyl)amides useful as analgesics and antagonists of opioids, wherein the compounds have the general formula: ##STR1## including optically active isomeric forms, and the pharmaceutically acceptable acid addition salts thereof, wherein:R is a substituted or unsubstituted unsaturated heterocyclic ring system having 5 to 6 cyclic member atoms containing at least one nitrogen atom, and is preferably selected from the group consisting of pyridinyl, pyrimidinyl, and pyrazinyl;R.sub.1 is selected from the group consisting of unsubstituted or substituted heterocyclic ring systems having 5 cyclic member atoms, lower cyclic alkyl ring systems, lower-alkyl and lower-alkoxy lower-alkyl, and is preferably selected from the group consisting of furanyl lower-alkyl, thienyl lower-alkyl, pyrrolyl lower-alkyl, lower-alkyl, lower-cycloalkyl, and lower-alkoxy lower-alkyl of 2 to 6 carbons;R.sub.2 is a cyclic ring system lower-alkyl having 5 to 6 cyclic member atoms, and is preferably selected from the group consisting of phenyl lower-alkyl, thienyl lower-alkyl, thienyl hydroxy lower-alkyl, pyrazoyl lower-alkyl, and (4,5-dihydro-5-oxo-1H-tetrazol-1-yl) lower-alkyl which may be substituted in the 4-position with a group selected from lower-alkyl; andR.sub.3 is selected from the group consisting of hydrogen and methyl.
    • 本发明涉及用作阿片样物质的止痛剂和拮抗剂的新型取代的N-杂环-N-（4-哌啶基）酰胺，其中所述化合物具有以下通式：包括旋光异构体形式的和其药学上可接受的酸加成盐 其中：R是具有5至6个含有至少一个氮原子的环状原子的取代或未取代的不饱和杂环系，优选选自吡啶基，嘧啶基和吡嗪基; R1选自具有5个环状成员原子的未取代或取代的杂环系，低级环烷基环系，低级烷基和低级烷氧基低级烷基，优选选自呋喃基低级烷基 2至6个碳原子的噻吩基低级烷基，吡咯基低级烷基，低级烷基，低级环烷基和低级烷氧基低级烷基; R2是具有5至6个环状原子的环状体系的低级烷基，优选选自苯基低级烷基，噻吩基低级烷基，噻吩基羟基低级烷基，吡唑基低级烷基和（4 可以在4-位上被选自低级烷基的基团取代的5-二氢-5-氧代-1H-四唑-1-基）低级烷基; 并且R 3选自氢和甲基。
    • 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
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