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6 条记录 (耗时 0.018 秒)

    1,2,4-thiadiazines
    2.
    发明授权
    1,2,4-thiadiazines 失效
    1,2,4-噻二嗪

    公开(公告)号：US4654338A

    公开(公告)日：1987-03-31

    申请号：US716050

    申请日：1985-03-26

    申请人： Stuart D. Jones ,  Wilfred R. Tully ,  Peter D. Kennewell

    发明人： Stuart D. Jones ,  Wilfred R. Tully ,  Peter D. Kennewell

    IPC分类号： C07D233/61 ,  A61K31/415 ,  A61K31/54 ,  A61P25/20 ,  C07D285/18 ,  C07D413/04 ,  C07D417/04

    CPC分类号： C07D285/18

    摘要： Novel 1,2,4-thiadiazines of the formula ##STR1## wherein R.sub.3 is selected from the group consisting of hydrogen, --OH, --CF.sub.3, alkyl, alkoxy and alkylthio of 1 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms optionally substituted with alkyl of 1 to 6 carbon atoms and ##STR2## R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen and alkyl of 1 to 3 carbon atoms or taken together with the nitrogen to which they are attached form a saturated heterocycle of 4 to 8 carbon atoms optionally containing a heteroatom of the group consisting of --O--, --S-- and ##STR3## and R' is hydrogen or alkyl of 1 to 3 carbon atoms, R.sub.5 is ##STR4## R.sub.4 is selected from the group consisting of hydrogen, halogen and alkyl and alkoxy of 1 to 3 carbon atoms, R.sub.6 is selected from the group consisting of hydrogen, halogen and alkyl of 1 to 3 carbon atoms with the proviso that R.sub.6 may represent halogen only when R.sub.3 is hydrogen, --OH, alkyl and alkoxy of 1 to 6 carbon atoms or cycloalkyl of 3 to 6 carbon atoms optionally substituted with alkyl of 1 to 6 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having a remarkable anxiolytic activity and novel intermediates.

    摘要翻译： 式Ⅰ的新的1,2,4-噻二嗪其中R 3选自氢，-OH，-CF 3，烷基，烷氧基和1至6个碳原子的烷硫基，3至6个碳原子的环烷基 任选被1至6个碳原子的烷基取代的原子，且R 1和R 2分别选自氢和1至3个碳原子的烷基，或与它们所连接的氮一起形成饱和杂环 4至8个碳原子，任选地含有-O - ， - S-和＆lt; IMAGE＆gt;的杂原子，R'是氢或1至3个碳原子的烷基，R 5选自 由氢，卤素和1至3个碳原子的烷基和烷氧基组成的基团，R 6选自氢，卤素和1至3个碳原子的烷基，条件是R 6可以仅在R3是氢时表示卤素， -OH，1至6个碳原子的烷基和烷氧基或3至6个碳的环烷基 任选被1至6个碳原子的烷基取代的原子及其无毒的药学上可接受的具有显着抗焦虑活性的酸加成盐和新的中间体。

    7-cyclopropyl-imidazodiazepines
    5.
    发明授权
    7-cyclopropyl-imidazodiazepines 失效
    7-环丙基咪唑烷酮

    公开(公告)号：US5247079A

    公开(公告)日：1993-09-21

    申请号：US781755

    申请日：1991-10-23

    申请人： Charles J. R. Hedgecock ,  Stuart D. Jones

    发明人： Charles J. R. Hedgecock ,  Stuart D. Jones

    IPC分类号： A61K31/55 ,  A61P3/04 ,  A61P25/08 ,  A61P25/20 ,  A61P25/28 ,  C07D471/14 ,  C07D487/04 ,  C07D487/14

    CPC分类号： C07D487/04 ,  C07D487/14

    摘要： A compound selected from the group consisting of a compound of the formula ##STR1## wherein Y is a nitrogen atom or carbon atom bearing Z, Z is selected from the group consisting of hydrogen, halogen, --C.ident.N, --N.sub.3 and --C(Hal).sub.3, Hal is a halogen, X is cycloalkyl of 3 to 6 carbon atoms or hydrogen with the proviso that when X is hydrogen, Y must be nitrogen, R is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, phenyl and substituted phenyl and their non-toxic, pharmaceutically acceptable acid addition salts, a process and intermediate for preparing them, having tranquillizing properties.

    摘要翻译： 选自下列化合物的化合物其中Y是氮原子或带有Z的碳原子的化合物，其中Z选自氢，卤素，-C = N，-N 3和 - C（Hal）3，Hal是卤素，X是3至6个碳原子的环烷基或氢，条件是当X是氢时，Y必须是氮，R选自氢， 5个碳原子，苯基和取代的苯基及其无毒的药学上可接受的酸加成盐，制备它们的方法和中间体，具有镇静特性。

    Novel imidazobenzodiazepines
    6.
    发明授权
    Novel imidazobenzodiazepines 失效
    新型咪唑并二氮杂

    公开(公告)号：US5017574A

    公开(公告)日：1991-05-21

    申请号：US516194

    申请日：1990-04-26

    申请人： Charles J. R. Hedgecock ,  Stuart D. Jones ,  Elizabeth A. Kuo

    发明人： Charles J. R. Hedgecock ,  Stuart D. Jones ,  Elizabeth A. Kuo

    IPC分类号： A61K31/55 ,  A61P3/04 ,  A61P25/18 ,  A61P25/28 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： A compound selected from the group consisting of a compound of the formula ##STR1## wherein the R.sub.1 s are the same and are alkyl of 1 to 3 carbon atoms or together are alkylene of 2 to 5 carbon atoms, X, Y and W are individually --O-- or --S--, R.sub.2 is hydrogen or alkyl of 1 to 3 carbon atoms, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms and phenyl optionally substituted with at least one member of the group consisting of halogen, alkyl and alkoxy of 1 to 3 carbon atoms and --CF.sub.3, R.sub.4 and R.sub.5 are individually selected from the group consisting of hydrogen, halogen, --OH, alkyl and alkoxy of 1 to 3 carbon atoms and --CF.sub.3 with the proviso that when R.sub.1 and R.sub.2 are alkyl, X and Y are the same and their non-toxic, pharmaceutically acceptable acid addition salts having benzodiazepine inverse agonist properties.

    摘要翻译： 选自下式的化合物的化合物其中R 1相同并且是1至3个碳原子的烷基或一起是2至5个碳原子的亚烷基，X，Y和W分别是 -O-或-S-，R 2是氢或1至3个碳原子的烷基，R 3选自氢，1至5个碳原子的烷基和任选被至少一个成员组成的组的苯基， 的卤素，具有1至3个碳原子的烷基和烷氧基和-CF 3，R 4和R 5分别选自氢，卤素，-OH，具有1至3个碳原子的烷基和烷氧基和-CF 3，条件是 当R1和R2是烷基时，X和Y是相同的，它们是具有苯并二氮杂反向激动剂性质的无毒的药学上可接受的酸加成盐。