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13 条记录 (耗时 0.011 秒)

    Benzodiazepine derivatives and salts thereof
    1.
    发明授权
    Benzodiazepine derivatives and salts thereof 失效
    苯并咪唑衍生物及其盐

    公开(公告)号：US3641002A

    公开(公告)日：1972-02-08

    申请号：US3641002D

    申请日：1969-06-09

    申请人： SUMITOMO CHEMICAL CO

    发明人： IZUMI TAKAHIRO ,  YAMAMOTO HISAO ,  KITAGAWA SUMIO ,  INABA SHIGEHO ,  SAKAI SHIGERU ,  HIROHASHI TOSHIYUKI ,  MARUYAMA ISAMU ,  AKATSU MITSUHIROO

    IPC分类号： A61K31/55 ,  C07D401/04 ,  C07D53/06

    CPC分类号： C07D401/04 ,  A61K31/55

    摘要： NOVEL 1-SUBSTITUTED 1,4-BENZODIAZEPIN-2-ONE DERIVATIVES REPRESENTED BY THE FORMULA,

    1-(4-R-PIPERIDINYL),2-(O=),5-(Y-PHENYL),X-1,2-DIHYDRO-3H-

    1,4-BENZODIAZEPINE

    WHEREIN R SIGNIFIES A LOWER ALKYL GROUP, AND X AND Y SIGNIFY RESPECTIVELY A HYDROGEN ATOM, A HALOGEN ATOM, A NITRO GROUP OR A TRIFLUOROMETHYL GROUP, WHICH ARE EFFECTIVE AS TRANQUILIZERS, MUSCLE-RELAXANTS AND HYPNOTICS, ARE PRODUCED BY REACTING WITH A REACTIVE ESTER OF A PIPERIDNOL DERIVATIVE OF THE FORMULA,

    4-R,(HO-)PIPERIDINE

    WHEREIN R IS AS DEFINED ABORE, A 1,4-BENZODIAZEPIN-2-ONE DERIVATIVE REPRESENTED BY THE FORMULA,

    2-(O=),5-(Y-PHENYL),X-1,2-DIHYDRO-3H-1,4-BENZODIAZEPINE

    WHEREIN X AND Y ARE AS DEFINED ABOVE, OR CONTACTING, WITH AN OXIDIZING AGENT, A 2-AMINOMETHYL-INDOLE DERIVATIVE REPRESENTED BY THE FORMULA,

    1-(4-R-PIPERIDINYL),2-(H2N-CH2-),3-(Y-PHENYL),X-INDOLE

    WHEREIN R, X AND Y ARE AS DEFINED ABOVE.

    Benzodiazepine process
    3.
    发明授权
    Benzodiazepine process 失效
    苯二氮卓工艺

    公开(公告)号：US3867372A

    公开(公告)日：1975-02-18

    申请号：US11114171

    申请日：1971-01-29

    申请人： SUMITOMO CHEMICAL CO

    发明人： YAMAMOTO HISAO ,  INABA SHIGEHO ,  HIROHASHI TOSHIYUKI ,  YAMAMOTO MICHIHIRO ,  ISHIZUMI KIKUO ,  AKATSU MITSUHIRO ,  MARUYAMA ISAMU ,  MORI KAZUO ,  KUME YOSHIHARU ,  IZUMI TAKAHIRO

    IPC分类号： A61K31/55 ,  C07D243/24 ,  C07D243/30 ,  C07D401/04 ,  C07D53/06

    CPC分类号： C07D243/24 ,  A61K31/55 ,  C07D243/26 ,  C07D243/28 ,  C07D243/30 ,  C07D243/36 ,  C07D401/04

    摘要： (WHEREIN R5 and R6 represent individually a hydrogen atom, a halogen atom, a lower alkyl group or a trifluoromethyl group); R3 is a hydrogen atom or a lower alkyl group; R4 is a lower alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl group; m is 1 or 2; and n is an integer of 1 to 4, and a process for preparation thereof and pharmaceutical use of the same. The benzodiazepine derivatives are effective as tranquillizers, muscle-relaxants and hypnotics.
    Novel 1-substituted benzodiazepine derivatives and salt thereof having the formula,

    WHEREIN R1 is a hydrogen atom, a halogen atom, a nitro group, a cyano group, a lower alkoxy group or a trifluoromethyl group; R2 is a pyridyl group or a group of the formula

    摘要翻译： 具有下式的新的1-取代苯并二氮杂衍生物及其盐WHEREIN R1是氢原子，卤原子，硝基，氰基，低级烷氧基或三氟甲基; R2是吡啶基或式（WHEREIN R5和R6分别表示氢原子，卤素原子，低级烷基或三氟甲基）的基团; R3是氢原子或低级烷基; R4是低级烷基，环烷基，环烷基烷基，芳基或芳烷基; m为1或2; n为1〜4的整数，其制备方法和药物用途。

    Process for producing 1 4-benzodiazepine derivatives and their salts
    4.
    发明授权
    Process for producing 1 4-benzodiazepine derivatives and their salts 失效
    生产1种4-苯并二氮杂衍生物及其盐的方法

    公开(公告)号：US3634402A

    公开(公告)日：1972-01-11

    申请号：US3634402D

    申请日：1969-04-16

    申请人： SUMITOMO CHEMICAL CO

    发明人： YAMAMOTO HISAO ,  INABA SHIGEHO ,  HIROHASHI TOSHIYUKI ,  AKATSU MITSUHIRO ,  MARUYAMA ISAMU ,  IZUMI TAKAHIRO

    IPC分类号： A61K31/55 ,  C07D209/04 ,  C07D209/14 ,  C07D243/14 ,  C07D243/24 ,  C07D243/36 ,  C07D53/06

    CPC分类号： C07D209/04 ,  C07C251/72 ,  C07D243/24

    摘要： WHEREIN R1, R2 AND R3 ARE AS DEFINED ABOVE.

    1-R3,2-(H2N-CO-),3-R2,R1-INDOLE

    WHEREIN R1, R2 AND R3 ARE AS DEFINED ABOVE, AND R4 SIGNIFIES A HYDROGEN ATOM OR A LOWER ALKYL GROUP, AND REDUCING THE RESULTING INDOLE-2-CARBOXYLIC ACID DERIVATIVE OF THE FORMULA,

    1-R3,2-(R4-OOC-),3-R2,R1-INDOLE

    WHEREIN R1, R2 AND R3 ARE AS DEFINED ABOVE, WITH AN OXIDIZING AGENT SUCH AS OZONE, HYDROGEN PEROXIDE, A PERACID OR CHROMIC ACID. THE 2-AMINOMETHYL INDOLE DERIVATIVE IS PRODUCED, FOR EXAMPLE, BY AMIDATION OF AN INDOLE2-CARBOXYLIC ACID DERIVATIVE OF THE FORMULA,

    1-R3,2-(H2N-CH2-),3-R2,R1-INDOLE

    WHEREIN R1 SIGNIFIES A HYDROGEN ATOM, A HALOGEN ATOM, A LOWER ALKYL GROUP, A LOWER ALKOXY GROUP OR A TRIFLUOROMETHYL GROUP; R2 SIGNIFIES A LOWER ALKYL GROUP OR AN ARALKYL GROUP; AND R3 SIGNIFIES A HYDROGEN ATOM, A LOWER ALKYL GROUP, AN ARALKYL GROUP, CYCLOALYL GROUP OR AN UNSUBSTITUTED OR HALOGEN-SBUSTITUTED PHENYL GROUP, ARE PRODUCED BY CONTACTING A 2-AMINOMETHYL INDOLE DERIVATIVE OF THE FORMULA,

    1-R3,2-(O=),5-R2,R1-1,2-DIHYDRO-3H-1,4-BENZODIAZEPINE

    1,4-BENZODIAZEPINE DERIVATIVES, WHICH ARE USEFUL AS TRANQUILIZERS, MUSCLE-RELAXANTS, ANTI-SPASMODICS AND HYPNOTICS AND REPRESENTED BY THE FORMULA,

    Novel benzodiazepine derivatives and preparation thereof
    5.
    发明授权
    Novel benzodiazepine derivatives and preparation thereof 失效
    新型苯并二氮杂衍生物及其制备方法

    公开(公告)号：US3910889A

    公开(公告)日：1975-10-07

    申请号：US17370171

    申请日：1971-08-20

    申请人： SUMITOMO CHEMICAL CO

    发明人： AKATSU MITSUHIRO ,  KUME YOSHIHARU ,  HIROHASHI TOSHIYUKI ,  ISHIZUMI KIKUO ,  YAMAMOTO MICHIHIRO ,  MARUYAMA ISAMU ,  MORI KAZUO ,  IZUMI TAKAHIRO ,  INABA SHIGEHO ,  YAMAMOTO HISAO

    IPC分类号： C07D243/24 ,  C07D243/26 ,  C07D243/28 ,  C07D243/30 ,  C07D243/36

    CPC分类号： C07D243/24

    摘要： A novel benzodiazepine derivatives represented by the formula,

    and acid addition salts thereof, wherein R1 represents hydrogen, halogen, nitro, C1 4 alkoxy, cyano or trifluoromethyl; R2 represents a group of the formula,

    WHEREIN R5 and R6 represent hydrogen, halogen, C1 4 alkyl or trifluoromethyl; R3 represents hydrogen, C1 4 alkyl or aralkyl; R4 represents tetrahydropyranyloxy, tetrahydrofuranyloxy, aryloxy, aralkoxy or alkoxyalkoxy; N REPRESENTS AN INTEGER OF 1 TO 4; AND M REPRESENTS ZERO OR 1, WHICH IS PREPARED BY A. REACTING A 1-UNSUBSTITUTED BENZODIAZEPINE DERIVATIVE OF THE FORMULA,

    with a reactive ester of a compound of the formula,

    摘要翻译： R4代表氢原子，卤素，硝基，硝基，苯基，噻吩基，噻吩基，噻吩基， C 1-4烷氧基，氰基或三氟甲基; R 2表示下式的基团，其中R 5和R 6表示氢，卤素，C 1-4烷基或三氟甲基; R3代表氢，C1-4烷基或芳烷基; R4表示四氢吡喃氧基，四氢呋喃氧基，芳氧基，芳烷氧基或烷氧基烷氧基; N代表1到4的整数; 和M代表零或1，由A.制备的1-取代的苯并二氮吡啶衍生物，反应性酯（反应性酯），C = N ANGLE |（O）m R 2与反应性酯 的化合物，即HO-CnH2n-R4III。

    Purification of benzodiazepine derivatives
    7.
    发明授权
    Purification of benzodiazepine derivatives 失效
    苯二酚衍生物的纯化

    公开(公告)号：US3860575A

    公开(公告)日：1975-01-14

    申请号：US24080472

    申请日：1972-04-03

    申请人： SUMITOMO CHEMICAL CO

    发明人： ISHIZUMI KIKUO ,  MORI KAZUO ,  OKAMOTO TADASHI ,  AKASE TAKESHI ,  IZUMI TAKAHIRO ,  AKATSU MITSUHIRO ,  KUME YOSHIHARU ,  INABA SHIGEHO ,  YAMAMOTO HISAO

    IPC分类号： C07D243/16 ,  C07D53/06

    CPC分类号： C07D243/16

    摘要： WHEREIN R1 is a lower (C1 - C4) alkyl, cyclo (C3 - C6) alkyl-(C1 - C4) alkyl, (C1 - C4) alkoxy-(C1 - C4) alkyl, or (C1 - C3) acyloxy-(C1 - C4) alkyl; R2 is hydrogen or a lower (C1 - C4) alkyl; X is hydrogen or a halogen, nitro or trifluoromethyl; and Y and Z are individually hydrogen, a halogen, a lower (C1 - C4) alkyl or nitro, treating the crude product with an acylating agent to acylate an impurity contained in the crude product, and then extracting the reaction mixture with an acid to recover the objective 2,3-dihydro-1H-1,4-benzodiazepine derivative of formula (I).

    A process for purifying a crude 2,3-dihydro-1H-1,4benzodiazepine derivative having effects as tranquilizers, antispasmodics and muscle-relaxants, represented by the formula,

    摘要翻译： 纯化作为镇静剂，抗痉挛剂和肌肉松弛剂的粗制2,3-二氢-1H-1,4-苯并二氮杂衍生物的方法，由下式表示，其中R1为低级（C1-C4）烷基， 环（C 3 -C 6）烷基 - （C 1 -C 4）烷基，（C 1 -C 4）烷氧基 - （C 1 -C 4）烷基或（C 1 -C 3）酰氧基 - （C 1 -C 4） R2是氢或低级（C1-C4）烷基; X是氢或卤素，硝基或三氟甲基; 并且Y和Z分别为氢，卤素，低级（C 1 -C 4）烷基或硝基，用酰化剂处理粗产物以酰化粗产物中所含的杂质，然后用​​酸萃取反应混合物 回收式（I）的目标2,3-二氢-1H-1,4-苯并二氮杂衍生物。

    Method for preparing benzodiazepine derivatives
    8.
    发明授权
    Method for preparing benzodiazepine derivatives 失效
    制备苯二酸衍生物的方法

    公开(公告)号：US3702323A

    公开(公告)日：1972-11-07

    申请号：US3702323D

    申请日：1970-04-07

    申请人： SUMITOMO CHEMICAL CO

    发明人： YAMAMOTO HISAO ,  INABA SHIGEHO ,  OKAMOTO TADASHI ,  HIROHASHI TOSHIYUKI ,  ISHIZUMI KIKUO ,  YAMAMOTO MICHIHIRO ,  MARUYAMA ISAMU ,  MORI KAZUO ,  KOBAYASHI TSUYOSHI ,  IZUMI TAKAHIRO

    IPC分类号： C07D243/24 ,  C07D243/32 ,  C07D243/36 ,  C07D403/06 ,  C07D53/06

    CPC分类号： C07D243/24 ,  C07D243/32 ,  C07D243/36 ,  C07D403/06

    摘要： NOVEL AND IMPROVED METHOD FOR PREPARING BENZODIAZEPINE DERIVATIVES, WHICH HAVE PROMINENT EFFECTS AS TRANQUILIZERS, MUSCLE RELAXANTS, ANTISPASMODICS, ANTICONVULSANTS AND HYPNOTICS, REPRESENTED BY THE FORMULA,

    2-(O=),3-R3,5-(R2-PHENYL),R1-1,2-DIHYDRO-3H-1,4-

    BENZODIAZEPINE

    WHEREIN R1 IS HYDROGEN, HALOGEN, C1-4 ALKYL, NITRO OR TRIFLUOROMETHYL; R2 IS HYDROGEN OR HALOGEN; AND R3 IS HYDROGEN OR C1-4 ALKYL. THESE BENZODIAZEPINE DERIVATIVES ARE PREPARED BY REACTING A NOVEL 1-PHTHALIMIDOACYL-INDOLE DERIVATIVE REPRESENTED BY THE FORMULA,

    1-((1,3-DI(O=)ISOINDOLIN-2-YL)-CH(-R3)-CO-),2-R4,3-

    (R2-PHENYL),R1-INDOLE

    WHEREIN R1, R2 AND R3 ARE AS DEFINED ABOVE; AND R4 IS HYDROGEN OR C1-4 ALKYL, WITH OZONE AND THEN CONTACTING THE REACTION PRODUCT WITH A HYDRAZINE DERIVATIVE. THE 1-PHTHALIMIDOACYL-INDOLE DERIVATIVE IS PRODUCED BY PHTHALIMIDOACYLATION OF AN INDOLE DERIVATIVE REPRESENTED BY THE FORMULA,

    2-R4,3-(R2-PHENYL),R1-INDOLE

    OR FISCHER CYCLIZATION OF A PHTHALIMIDOACYL-PHENYLHYDRAZONE DERIVATIVE REPRESENTED BY THE FORMULA,

    1,3-DI(O=),2-((R2-PHENYL)-CH2-C(-R4)=N-N(-PHENYLENE-R1)-

    CO-CH(-R3)-)ISOINDOLE

    WHEREIN R1, R2, R3 AND R4 ARE AS DEFINED ABOVE.