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    Process for the production of lower alkyl 2-chloro-2-hydroxyiminoacetates
    3.
    发明授权
    Process for the production of lower alkyl 2-chloro-2-hydroxyiminoacetates 失效
    制备2-氯-2-羟基亚氨基乙酸低级烷基酯的方法

    公开(公告)号：US4190728A

    公开(公告)日：1980-02-26

    申请号：US895476

    申请日：1978-04-11

    申请人： Ikuo Adachi ,  Teruo Yamamori ,  Yoshiharu Hiramatsu

    发明人： Ikuo Adachi ,  Teruo Yamamori ,  Yoshiharu Hiramatsu

    IPC分类号： C07B61/00 ,  B01J21/00 ,  B01J27/00 ,  C07C67/00 ,  C07C239/00 ,  C07C251/34 ,  C07C259/02 ,  C07C259/06 ,  C07D261/14 ,  C07C131/00

    CPC分类号： C07C259/02 ,  C07D261/14

    摘要： Lower alkyl 2-chloro-2-hydroxyiminoacetates are produced by (A) reacting chloral with a lower alkanol and a hydroxylamine salt in the presence of a Lewis acid or a metal oxide which is convertible into said Lewis acid during the course of the reaction to give a lower alkyl 2-hydroxyiminoacetate and then chlorinating the resulting product or (B) reacting chloral oxime with a lower alkanol in the presence of a base to give a lower alkyl 2-hydroxyiminoacetate and finally chlorinating the thus formed product.

    摘要翻译： （A）在路易斯酸或金属氧化物存在下，通过（A）将低聚链烷醇和羟胺盐与低级链烷醇和羟胺盐反应来制备，所述路易斯酸或金属氧化物在反应过程中可转化成所述路易斯酸， 得到2-羟基亚氨基乙酸低级烷基酯，然后氯化所得产物或（B）在碱的存在下使肟与低级烷醇反应，得到2-羟基亚氨基乙酸低级烷基酯，最后氯化所形成的产物。

    Process for preparing benzothiazepine derivatives
    5.
    发明授权
    Process for preparing benzothiazepine derivatives 失效
    制备苯并硫氮杂衍生物的方法

    公开(公告)号：US5473066A

    公开(公告)日：1995-12-05

    申请号：US182828

    申请日：1994-01-19

    申请人： Teruo Yamamori ,  Hiroshi Harada ,  Eiichi Oosugi ,  Katsunori Sakai

    发明人： Teruo Yamamori ,  Hiroshi Harada ,  Eiichi Oosugi ,  Katsunori Sakai

    IPC分类号： B01J23/745 ,  B01J23/74 ,  C07B53/00 ,  C07B61/00 ,  C07C319/14 ,  C07C323/56 ,  C07D281/10 ,  C07D295/13 ,  C07B45/00 ,  C07D295/14

    CPC分类号： C07D295/13 ,  C07C319/14 ,  C07C323/56 ,  C07D281/10

    摘要： Process for stereoselectivity preparing a cis-form of 5-(aminoalkylamino)-1,5-benzothiazepine derivative represented by formula (VI): ##STR1## is provided, said process comprising carrying out a stereoselective addition reaction of an o-(aminoalkylamino) thiophenyl derivative with a trans-substituted glycidic ester at an elevated temperature in a nonpolar solvent in the presence of a divalent or trivalent iron ion to prepare a threo-form intermediate, hydrolyzing the ester group of said intermediate, acetylating the hydroxyl group of said hydrolyzed compound, and subjecting said acetylated compound to a ring closure reaction to obtain the objective compound (VI).

    摘要翻译： （VI）表示的5-（氨基烷基氨基）-1,5-苯并硫氮杂衍生物的顺式形式的立体选择性方法：所述方法包括进行邻位反应的立体选择性加成反应， （氨基烷基氨基）噻吩基衍生物与反式取代的缩水甘油酯在升高的温度下在非极性溶剂中在二价或三价铁离子存在下反应以制备苏式中间体，水解所述中间体的酯基，乙酰化羟基 的所述水解化合物，并使所述乙酰化合物进行闭环反应以获得目标化合物（VI）。

    Utilities of amide compounds
    6.
    发明授权
    Utilities of amide compounds 有权
    酰胺化合物的实用性

    公开(公告)号：US08106051B2

    公开(公告)日：2012-01-31

    申请号：US12081662

    申请日：2008-04-18

    申请人： Teruo Yamamori ,  Kiyoshi Nagata ,  Natsuki Ishizuka ,  Katsunori Sakai

    发明人： Teruo Yamamori ,  Kiyoshi Nagata ,  Natsuki Ishizuka ,  Katsunori Sakai

    IPC分类号： A01N43/58 ,  A01N43/60 ,  A61K31/50 ,  A61K31/495

    CPC分类号： C07D213/75 ,  A61K31/165 ,  A61K31/47 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12

    摘要： Compounds having an activity to enhance the expression of apoAI are provided, which are used as medicaments.Compounds of formula (I): in which ring A and Ar1 are independently a monocyclic or bicyclic aromatic carbocyclic group or aromatic heterocyclic group, each of which may be optionally substituted, or the like; R is a hydrogen or the like; Z is oxygen or the like; Y1 and Y2 are a hydrogen, a lower alkyl, or the like; n is an integer of 0 to 2; the broken line is the presence or absence of a bond; and the wavy line represents a cis- or trans-geometrical isomerism with respect to the double bond; are disclosed.

    摘要翻译： 提供具有增强载脂蛋白A表达活性的化合物，其用作药物。 式（I）的化合物：其中环A和Ar 1独立地是单环或双环芳族碳环基或芳族杂环基，其各自可以被任选取代;等等; R为氢等; Z是氧等; Y1和Y2是氢，低级烷基等; n为0〜2的整数， 虚线是存在或不存在债券; 并且波浪线表示相对于双键的顺式或反式几何异构体; 被披露。

    Benzothiazepine derivatives
    7.
    发明授权
    Benzothiazepine derivatives 失效
    苯并硫氮杂衍生物

    公开(公告)号：US5378698A

    公开(公告)日：1995-01-03

    申请号：US960851

    申请日：1992-10-14

    申请人： Teruo Yamamori ,  Hiroshi Harada ,  Katsunori Sakai ,  Kazumi Iwaki ,  Kazuki Matsunaga

    发明人： Teruo Yamamori ,  Hiroshi Harada ,  Katsunori Sakai ,  Kazumi Iwaki ,  Kazuki Matsunaga

    IPC分类号： A61K31/55 ,  A61K31/554 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  C07D281/10 ,  C07D417/12 ,  C07D417/06

    CPC分类号： C07D417/12 ,  C07D281/10

    摘要： A compound of the formula: ##STR1## wherein X is .dbd.N--A--R.sup.1 or .dbd.C(R.sup.1)R.sup.2 ; A is a single bond, polymethylene or --CO--; R.sup.1 and R.sup.2 are each hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, unsubstituted or substituted phenyl, optionally substituted benzhydryl, or optionally substituted 5 to 6 membered heterocyclic group; Y is hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.6 alkoxy, optionally substituted phenoxy, optionally substituted benzyloxy, or optionally substituted benzyl; Z is hydrogen or acyl; n is an integer of from 2 to 6, and pharmaceutically acceptable salt thereof. A pharmaceutical composition containing the compound, which is useful for treating hypertension and cardiac diseases, is also provided.

    摘要翻译： 下式的化合物：其中X为= N-A-R 1或= C（R 1）R 2; A是单键，聚亚甲基或-CO-; R 1和R 2各自为氢，C 1 -C 6烷基，C 3 -C 7环烷基，未取代或取代的苯基，任选取代的二苯甲基或任选取代的5至6元杂环基; Y是氢，卤素，C 1 -C 6烷基，C 3 -C 7环烷基，C 1 -C 6烷氧基，任选取代的苯氧基，任选取代的苄氧基或任选取代的苄基; Z是氢或酰基; n为2〜6的整数，及其药学上可接受的盐。 还提供含有该化合物的药物组合物，其可用于治疗高血压和心脏病。