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37 条记录 (耗时 0.021 秒)

    Thieno[2,3-d]pyrimidine derivatives and salts thereof
    8.
    发明授权
    Thieno[2,3-d]pyrimidine derivatives and salts thereof 失效
    噻吩并[2,3-d]嘧啶衍生物及其盐

    公开(公告)号：US4695568A

    公开(公告)日：1987-09-22

    申请号：US685768

    申请日：1984-12-24

    申请人： Kunihiro Ninomiya ,  Issei Nitta ,  Akihiro Tobe ,  Mitsuo Egawa ,  Ryoji Kikumoto

    发明人： Kunihiro Ninomiya ,  Issei Nitta ,  Akihiro Tobe ,  Mitsuo Egawa ,  Ryoji Kikumoto

    IPC分类号： A61K31/505 ,  A61K31/55 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  C07D495/04 ,  A61K31/38 ,  C07D239/00

    CPC分类号： C07D495/04

    摘要： This invention relates novel thieno[2,3-d]pyrimidine derivatives represented by the following general formula (I): ##STR1## or salts thereof; wherein R.sup.1 and R.sup.2 independently represent hydrogen, halogen or alkyl group having 1 to 6 carbon atoms; or R.sup.1 and R.sup.2 may concatenate to form a cycloalkylene group having 5 or 6 ring carbon atoms; R.sup.3 and R.sup.4 independently represent hydrogen or alkyl group having 1 to 6 carbon atoms; R.sup.5 represents a member selected from(1) hydrogen or alkyl having 1 to 6 carbon atoms,(2) ##STR2## in which m is an integer of from 1 to 3 and X represents halogen, or (3) ##STR3## in which R.sup.6 represents alkyl group having 1 to 6 carbon atoms; Ar represents substituted or unsubstituted phenyl, or 2- or 3-thienyl group; and n is 2 or 3. The derivatives of the invention can be used in the treatment of the various depression disease or the higher dysfunction of the brain.

    摘要翻译： 本发明涉及由以下通式（I）表示的新颖的噻吩并[2,3-d]嘧啶衍生物或其盐; 其中R 1和R 2独立地表示氢，卤素或具有1至6个碳原子的烷基; 或者R1和R2可以连接形成具有5或6个环碳原子的亚环烷基; R3和R4独立地表示氢或具有1-6个碳原子的烷基; R5表示选自（1）氢或具有1至6个碳原子的烷基的成员，（2）其中m是1至3的整数，X表示卤素，或（3）其中 R6代表具有1-6个碳原子的烷基; Ar表示取代或未取代的苯基，或2-或3-噻吩基; 并且n为2或3.本发明的衍生物可用于治疗各种抑郁症或较高的脑功能障碍。

    Anxiolytic drug
    9.
    发明授权
    Anxiolytic drug 失效
    溶血药

    公开(公告)号：US5219855A

    公开(公告)日：1993-06-15

    申请号：US839737

    申请日：1992-02-19

    申请人： Ken-Ichi Saito ,  Akihiro Tobe ,  Heitaro Iwata ,  Akemichi Baba ,  Toshio Matsuda

    发明人： Ken-Ichi Saito ,  Akihiro Tobe ,  Heitaro Iwata ,  Akemichi Baba ,  Toshio Matsuda

    IPC分类号： A61K31/495 ,  A61K31/505 ,  C07D317/64 ,  C07D319/18 ,  C07D321/10 ,  C07D405/12

    CPC分类号： C07D405/12 ,  A61K31/495 ,  A61K31/505 ,  C07D317/64 ,  C07D319/18 ,  C07D321/10

    摘要： Disclosed herein are anxiolytic drugs containing as an active ingredient a piperazine derivative represented by the following general formula (I): ##STR1## wherein m represents an integer from 2 to 4,X represents ##STR2## Ar represents a pyridyl group, a pyrimidinyl group, or a phenyl group which may be substituted with halogen atom, trifluoromethyl group, alkoxy group or alkyl group, andR.sub.1, R.sub.2 and R.sub.3 which may be identical or different represent lower alkoxy groups, or R.sub.3 is a hydrogen atom and R.sub.1 when taken together with R.sub.2 forms ##STR3## (n=1, 2 or 3); and its acid addition salt.The anxiolytic drugs disclosed herein have the high binding capacities to 5-HT.sub.1A receptor which is one of the receptors for 5-hydroxytryptamine (5-HT), thereby exerting anxiolytic effects.

    摘要翻译： 本文公开了含有作为活性成分的由以下通式（I）表示的哌嗪衍生物的抗焦虑药物：其中m表示2至4的整数，X表示Ar表示 吡啶基，嘧啶基或可被卤素原子，三氟甲基，烷氧基或烷基取代的苯基，并且可以相同或不同的R 1，R 2和R 3表示低级烷氧基，或者R 3为氢 原子和R1与R2一起形成（n = 1,2或3）; 及其酸加成盐。 本文公开的抗焦虑药物具有对5-HT1A受体的高结合能力，其为5-羟色胺（5-HT）的受体之一，从而发挥抗焦虑作用。

    O-aminoalkylene (or aminoalkyleneoxy) phenylsulfone compounds having anti-ulcer effect
    10.
    发明授权
    O-aminoalkylene (or aminoalkyleneoxy) phenylsulfone compounds having anti-ulcer effect 失效
    具有抗溃疡作用的O-氨基亚烷基（或氨基亚烷氧基）苯基砜化合物

    公开(公告)号：US4734500A

    公开(公告)日：1988-03-29

    申请号：US838569

    申请日：1986-03-11

    申请人： Akihiro Tobe ,  Shinichiro Fujimori ,  Tomoshi Yamazaki ,  Mamoru Sugano ,  Ryoji Kikumoto ,  Issei Nitta

    发明人： Akihiro Tobe ,  Shinichiro Fujimori ,  Tomoshi Yamazaki ,  Mamoru Sugano ,  Ryoji Kikumoto ,  Issei Nitta

    IPC分类号： A61K31/135 ,  A61K31/19 ,  A61K31/195 ,  A61K31/215 ,  A61K31/22 ,  A61K31/275 ,  A61K31/495 ,  A61P1/04 ,  C07C47/11 ,  C07C67/00 ,  C07C313/00 ,  C07C317/22 ,  C07C317/32 ,  C07C317/44 ,  C07C317/46 ,  C07C317/48 ,  C07D295/08 ,  C07D295/092 ,  C07D295/096 ,  C07D333/76 ,  C07D333/50

    CPC分类号： C07D295/096 ,  C07D295/088 ,  C07D333/76

    摘要： A novel sulfone compound represented by the general formula (I) ##STR1## wherein R.sup.1 is cyclohexyl, phenyl; or a phenyl substituted with a group selected from nitro, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and halogen; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are respectively hydrogen, halogen, cyano or carbonyl, wherein R.sup.1 and R.sup.2 may form an o-phenylene or an o-phenylene substituted with at least one group selected from nitro C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and halogen; X is oxygen or methylene; Y is --(CH.sub.2).sub.n --, wherein n is an integer of 0, 5 or 6, or ##STR2## wherein m is an integer 1-3; R.sup.6 is hydrogen, C.sub.1 -C.sub.3 alkyl, .omega.-alkylaminoalkyl, wherein each alkyl has 1-3 carbon atoms, or .omega.-dialkylaminoalkyl, wherein each alkyl has 1-3 carbon atoms; R.sup.7 is hydrogen or C.sub.1 -C.sub.3 alkyl; and R.sup.6 and R.sup.7 may form a ring together with N, or ##STR3## wherein R.sup.8 is hydrogen, C.sub.1 -C.sub.3 hydroxyalkyl or phenyl; or a pharmaceutically acceptable salt thereof is disclosed. The compound has anti-ulcer effect.

    摘要翻译： 由通式（I）表示的新型砜化合物其中R 1是环己基，苯基; 或被选自硝基，C 1 -C 3烷基，C 1 -C 3烷氧基和卤素的基团取代的苯基; R2，R3，R4和R5分别是氢，卤素，氰基或羰基，其中R1和R2可以形成被至少一个选自硝基C1-C3烷基，C1-C3烷氧基的基团取代的邻亚苯基或邻亚苯基 和卤素; X是氧或亚甲基; Y是 - （CH 2）n - ，其中n是0或5或6的整数，或者其中m是整数1-3; R6是氢，C1-C3烷基，ω-烷基氨基烷基，其中每个烷基具有1-3个碳原子，或ω-二烷基氨基烷基，其中每个烷基具有1-3个碳原子; R7是氢或C1-C3烷基; 并且R 6和R 7可以与N或其中R 8是氢，C 1 -C 3羟基烷基或苯基形成环; 或其药学上可接受的盐。 该化合物具有抗溃疡作用。