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33 条记录 (耗时 0.042 秒)

    Piperazine derivatives
    4.
    发明授权
    Piperazine derivatives 失效
    哌嗪衍生物

    公开(公告)号：US5369103A

    公开(公告)日：1994-11-29

    申请号：US861834

    申请日：1992-06-19

    申请人： Ian A. Cliffe ,  Alan C. White ,  Anderson D. Ifill

    发明人： Ian A. Cliffe ,  Alan C. White ,  Anderson D. Ifill

    IPC分类号： A61K31/495 ,  A61P9/12 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/26 ,  A61P43/00 ,  C07D213/56 ,  C07D295/14 ,  C07D295/18 ,  C07D295/185 ,  A61K31/395 ,  C07D403/06 ,  C07D403/14

    CPC分类号： C07D295/185 ,  C07D213/56

    摘要： ##STR1## where A is an alkylene chain of 1 or 2 carbon atoms optionally substituted by one or more lower alkyl groups, R is hydrogen or lower alkyl, R
    1 is a mono or bicyclic aryl or a heteroaryl radical, R
    2 is an aryl radical, a heteroaryl radical, or an aryl-or heteroaryl-lower alkyl radical, R
    3 is hydrogen, lower alkyl or aryl and R
    4 is hydrogen, lower alkyl, cycloalkyl, cycloalkyl(lower)alkyl, aryl, or aryl(lower)alkyl or R
    3 and R
    4 together with the nitrogen atom to which they are both attached represent a saturated heterocyclic ring which may contain a further hetero atom and the dotted line represents a single or double bond, the hydrogen atoms shown in brackets being present when the dotted line represents a single bond and their pharmaceutically acceptable acid addition salts are 5-HT
    1A binding agents which may be used, for example, for the treatment of CNS disorders such as anxiety.

    摘要翻译： （I）其中A是任选被一个或多个低级烷基取代的1或2个碳原子的亚烷基链，R是氢或低级烷基，R 1是单或双环芳基或杂芳基，R 2是 芳基，芳基或杂芳基 - 低级烷基，R3是氢，低级烷基或芳基，R4是氢，低级烷基，环烷基，环烷基（低级）烷基，芳基或芳基（低级）烷基 或者R 3和R 4与它们所连接的氮原子一起表示饱和杂环，其可以含有另外的杂原子，虚线表示单键或双键，当虚线表示时，括号中所示的氢原子存在 代表单键，并且其药学上可接受的酸加成盐是可用于例如治疗CNS病症如焦虑症的5-HT1A结合剂。

    N-(2,3-dihydro-1,4-benzodioxinyl)-N-substituted aminopyrido-fused cycloalkanes
    5.
    发明授权
    N-(2,3-dihydro-1,4-benzodioxinyl)-N-substituted aminopyrido-fused cycloalkanes 失效
    N-（2,3-二氢-1,4-苯并二恶英基）-N-取代的氨基吡啶并 - 稠合的环烷烃

    公开(公告)号：US5194439A

    公开(公告)日：1993-03-16

    申请号：US765282

    申请日：1991-09-25

    申请人： Ian A. Cliffe ,  Howard L. Mansell ,  Richard S. Todd ,  Alan C. White

    发明人： Ian A. Cliffe ,  Howard L. Mansell ,  Richard S. Todd ,  Alan C. White

    IPC分类号： C07D215/38 ,  C07D405/12

    CPC分类号： C07D405/12 ,  C07D215/38

    摘要： Pyridine derivatives of formula ##STR1## their heteroaromatic N-oxides and their pharmaceutically acceptable acid addition salts are disclosed. In the formula z is 0, 1 and 2; R is hydrogen, hydroxy, lower alkyl, lower alkoxy, halogen, trifluoromethyl, nitro, amino, (lower)alkylamino or di(lower)alkylamino; R.sup.1 is hydrogen or lower alkyl; R.sup.2 is --(CH.sub.2).sub.n --R.sup.3 or --CH.sub.2 --CH.dbd.CH--(CH.sub.2).sub.m --R.sup.3 or --CH.sub.2.C.tbd.C.(CH.sub.2).sub.m --R.sup.3 where n is 1 to 6, and m is 0 to 3; and R.sup.3 is a ring of formula ##STR2## The compounds exhibit activity as 5-HT.sub.1A agonists, antagonists or partial agonists and are used for the treatment of CNS disorders, e.g. anxiety, as antihypertensives and in treating anorexia.

    摘要翻译： 公开了式（I）的吡啶衍生物，它们的杂芳族N-氧化物及其药学上可接受的酸加成盐。 式中Z为0,1和2; R为氢，羟基，低级烷基，低级烷氧基，卤素，三氟甲基，硝基，氨基，（低级）烷基氨基或二（低级）烷基氨基; R1是氢或低级烷基; R 2是 - （CH 2）n -R 3或-CH 2 -CH = CH-（CH 2）m -R 3或-CH 2 C 3 OCH 3（CH 2）m -R 3，其中n为1至6，m为0至3 ; 并且R 3是式的环。化合物表现出作为5-HT 1A激动剂，拮抗剂或部分激动剂的活性，并且用于治疗CNS疾病，例如， 焦虑，作为抗高血压药物和治疗厌食症。

    Pyrimidoindoles useful as hypoglycaemics
    6.
    发明授权
    Pyrimidoindoles useful as hypoglycaemics 失效
    嘧啶二醇可用作低血糖症

    公开(公告)号：US4784996A

    公开(公告)日：1988-11-15

    申请号：US23337

    申请日：1987-03-09

    申请人： Alan C. White ,  Ian A. Cliffe ,  Richard S. Todd

    发明人： Alan C. White ,  Ian A. Cliffe ,  Richard S. Todd

    IPC分类号： C07D487/04 ,  A61K31/505

    CPC分类号： C07D487/04

    摘要： Compounds of formula ##STR1## wherein A represents a lower alkylene chain optionally containing one double or triple bond, RO represents (lower)alkoxy, aryl(lower)alkoxy, hydroxy or protected hydroxy, R.sup.1 and R.sup.2 which may be the same or different each represent hydrogen, hydroxyl, lower alkyl, lower alkoxy, halo(lower)alkyl, halogen, amino or mono- or di(lower)alkylamino and R.sup.3 and R.sup.4 each independently represent hydrogen or lower alkyl and their pharmaceutically acceptable acid addition salts are useful as hypoglycaemics or as intermediates for hypoglycaemics.

    摘要翻译： 式（I）的化合物其中A表示任选含有一个双键或三键的低级亚烷基链，RO表示（低级）烷氧基，芳基（低级）烷氧基，羟基或被保护的羟基，R 1和R 2可以相同 或各自代表氢，羟基，低级烷基，低级烷氧基，卤代（低级）烷基，卤素，氨基或单或二（低级）烷基氨基，并且R 3和R 4各自独立地表示氢或低级烷基及其药学上可接受的酸加成盐 作为低血糖症或低血糖症的中间体是有用的。