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    1-{8 {65 -O-Amino-p-halophenyl-oxy, thio or sulfinyl)-propyl{9 -4-(alkoxy or halo phenyl)piperazines
    1.
    发明授权
    1-{8 {65 -O-Amino-p-halophenyl-oxy, thio or sulfinyl)-propyl{9 -4-(alkoxy or halo phenyl)piperazines 失效
    1- {8- {6-（N-氨基 - 对卤代苯氧基，硫代或亚磺酰基） - 丙基{9-4（烷氧基或卤代苯基）哌嗪

    公开(公告)号：US3925387A

    公开(公告)日：1975-12-09

    申请号：US31210672

    申请日：1972-12-04

    申请人： SUMITOMO CHEMICAL CO

    发明人： MARUYAMA ISAMU ,  NAKAO MASARU ,  SASAJIMA KIKUO ,  ONO KEIICHI ,  TAKAYAMA MASAHARU ,  KATAYAMA SHIGENARI ,  TANAKA YOSHIHIRO ,  YANAGIHARA IZUMI ,  INABA SHIGEHO ,  YAMAMOTO HISAO

    IPC分类号： C07D295/08 ,  A61K31/415 ,  A61K31/435 ,  A61K31/495 ,  A61P9/12 ,  A61P25/04 ,  A61P25/08 ,  A61P25/18 ,  A61P25/20 ,  C07D211/52 ,  C07D295/092 ,  C07D401/04 ,  C07D471/10 ,  C07D295/12

    CPC分类号： C07D295/088 ,  C07D211/52

    摘要： WHEREIN Y is as defined above.

    WHEREIN R1, R2, R3, Z and m are as defined above and X is halogen atom, with a compound of the formula,

    (WHEREIN R4 is hydrogen or halogen atom or lower alkyl or lower alkoxy group; R5 is hydrogen atom or lower alkyl or lower alkanoyl group; R6 is hydrogen or halogen atom or lower alkyl or lower alkoxy group; R7 is hydroxy, lower alkoxy or lower alkanoyloxy group; R8 is hydrogen or halogen atom or lower alkyl, lower alkoxy or trifluoromethyl group; R9 is hydrogen atom or lower alkyl or lower alkanoyl group; R10 is hydrogen or halogen atom or lower alkyl or lower alkoxy group; and n is 0, 1 or 2); and m is an integer from 2 to 5, and pharmaceutically acceptable salts thereof, which have excellent anti-psychotonic, analgesic, anti-inflammatory and anti-hypertensive activities, are produced by reacting a compound of the formula,

    WHEREIN R1 and R2 are each hydrogen atom or lower alkyl, lower alkanoyl or aroyl group; R3 is hydrogen or halogen atom or lower alkyl or lower alkoxy group; Z is oxygen or sulfur atom or sulfinyl or sulfonyl group; Y is

    Novel alkylamine derivatives represented by the formula,

    摘要翻译： 由式WHEREIN R1和R2表示的新型烷基胺衍生物各自为氢原子或低级烷基，低级烷酰基或芳酰基; R3是氢或卤素原子或低级烷基或低级烷氧基; Z是氧或硫原子或亚磺酰基或磺酰基; Y为（其中R4为氢或卤素原子或低级烷基或低级烷氧基; R5为氢原子或低级烷基或低级烷酰基; R6为氢或卤素原子或低级烷基或低级烷氧基; R7为羟基，低级烷氧基 或低级烷酰氧基; R8为氢或卤素原子或低级烷基，低级烷氧基或三氟甲基; R9为氢原子或低级烷基或低级烷酰基; R10为氢或卤素原子或低级烷基或低级烷氧基; n为 0，1或2）; m为2〜5的整数，及其药学上可接受的盐，其具有优异的抗心理，镇痛，抗炎和抗高血压活性，是通过使下式的化合物，即WHEREIN R1，R2，R3 ，Z和m如上所定义，X是卤素原子，与下式的化合物，其中Y如上定义。

    Butyrophenone derivatives
    2.
    发明授权
    Butyrophenone derivatives 失效
    丁酰苯衍生物

    公开(公告)号：US3907812A

    公开(公告)日：1975-09-23

    申请号：US32913073

    申请日：1973-02-02

    申请人： SUMITOMO CHEMICAL CO

    发明人： YAMAMOTO HISAO ,  OKAMOTO TADASHI ,  SASAJIMA KIKUO ,  NAKAO MASARU ,  MARUYAMA ISAMU ,  KATAYAMA SHIGENARI

    IPC分类号： C07D211/52

    CPC分类号： C07D211/52 ,  Y10S514/96

    摘要： A novel process for preparing central nervous system active butyrophenone derivatives in which gamma piperidinobutyrophenone derivatives of the formula,

    wherein R1 is hydrogen, halogen, amino, acylamino, alkylamino or N-acylalkylamino; R2 is hydrogen or halogen; R3 is hydrogen or unsubstituted or alkyl-, alkoxy-, halogen- or trifluoromethylsubstituted phenyl; and R4 is hydrogen or hydroxyl, can be prepared by reacting an indole derivative of the formula,

    wherein R2, R3 and R4 are as defined above, and R5 and R6 are each independently hydrogen or alkyl, with an oxidizing agent to yield an o-acylamino- gamma -piperidinobutyrophenone derivative of the formula,

    wherein R2, R3, R4, R5 and R6 are as defined above, and further, if necessary, hydrolyzing the product to yield an o-amino- gamma -piperidinobutyrophenone derivative of the formula,

    wherein R2, R3, R4 and R5 are as defined above, and further diazotizing, if desired, in case R5 is hydrogen, the obtained oamino- gamma -piperidinobutyrophenone derivative and subsequently decomposing the resultant diazonium compound to replace the diazonium group by hydrogen or halogen. Among the butyrophenone derivatives thus obtained, those in which R1 is halogen, amino, acylamino, alkylamino or N-acylalkylamino are novel compounds.

    摘要翻译： 一种用于制备中枢神经系统活性丁酰苯衍生物的新方法，其中式为CO-CH 2 -CH 2 -CH 2 -YGLE R 1的γ-哌啶基丁酰苯衍生物，其中R 1为氢，卤素，氨基，酰氨基，烷基氨基或N-酰基烷基氨基; R2是氢或卤素; R3是氢或未取代的或烷基，烷氧基，卤素或三氟甲基取代的苯基; 并且R 4是氢或羟基，可以通过使下式的吲哚衍生物CH2-CH2-CH2-ANGLE R6 | R5（其中R2，R3和R4如上定义）与R5和R6各自独立地是氢或烷基 与氧化剂反应得到下式的邻酰基氨基-γ-哌啶基丁酰苯衍生物，其中R2，R3，R4，R5和R6的定义如上所定义，CO- 此外，如果需要，水解产物以产生下式的邻氨基-γ-哌啶基丁酰苯衍生物，其中R2，R3，R4和R5如上所定义，进一步重氮化， 如果需要，在R5为氢的情况下，得到的邻氨基-γ-哌啶基丁酰苯衍生物，随后分解所得重氮化合物以用氢或卤素代替重氮基团。 在由此获得的丁酰苯衍生物中，R 1为卤素，氨基，酰氨基，烷基氨基或N-酰基烷基氨基的那些是新化合物。

    2-({62 -Alkyl thioethyl)-6,7-benzomorphans
    3.
    发明授权
    2-({62 -Alkyl thioethyl)-6,7-benzomorphans 失效
    2 - （{62-烷基硫代乙基）-6,7-苯并吗啉

    公开(公告)号：US3903093A

    公开(公告)日：1975-09-02

    申请号：US41805273

    申请日：1973-11-21

    申请人： SUMITOMO CHEMICAL CO

    发明人： KOBAYASHI KENJI ,  FUKUMARU TOSHITSUGU ,  MIZOTE HIROYUKI ,  INABA SHIGEHO ,  YAMAMOTO HISAO

    IPC分类号： A61K31/395 ,  A61K31/435 ,  A61P25/04 ,  C07D221/26 ,  C07D39/00

    CPC分类号： A61K31/395 ,  C07D221/26 ,  Y10S514/849

    摘要： Novel 2-substituted 6,7-benzomorphan derivatives of the formula:

    AND ACID ADDITION SALTS THEREOF, WHICH ARE USEFUL AS NONADDICTING ANALGESICS, PAIN RELIEVING AGENTS AND ANTITUSSIVES AND CAN BE PREPARED BY REACTING 6,7-BENZOMORPHAN DERIVATIVES OF THE FORMULA:

    WITH THE REACTIVE DERIVATIVES OF ALCOHOLS OF THE FORMULA:

    wherein R is a hydrogen atom, a hydroxyl group, an alkoxy group or an alkanoyloxy group; R1 is a hydrogen atom, an alkyl group, an alkoxyalkyl group or a substituted or unsubstituted aryl group; R3 is a hydrogen atom or a hydroxyl group; R4 is a hydrogen atom, an alkyl group or a substituted or unsubstituted aryl group, or R3 and R4 may form an alkylidene group or a carbonyl group together with the carbon atom to which these substituents are bonded; R2, R5, R6, R7, R8, R9 and R10 are each a hydrogen atom or an alkyl group; A is an alkylene group; and m is an integer of 0 to 2.

    摘要翻译： 具有下式的新颖的2-取代的6,7-苯并吗啉衍生物：

    Quinazoline derivatives
    4.
    发明授权
    Quinazoline derivatives 失效
    喹诺酮衍生物

    公开(公告)号：US3859237A

    公开(公告)日：1975-01-07

    申请号：US30435772

    申请日：1972-11-07

    申请人： SUMITOMO CHEMICAL CO

    发明人： INABA SHIGEHO ,  YAMAMOTO MICHIHIRO ,  ISHIZUMI KIKUO ,  MORI KAZUO ,  KOSHIBA MASAO ,  YAMAMOTO HISAO

    IPC分类号： C07D239/80 ,  C07D239/82 ,  C07D401/04 ,  C07D409/04 ,  C07D51/48

    CPC分类号： C07D401/04 ,  C07D239/80 ,  C07D239/82 ,  C07D409/04

    摘要： Quinazoline derivatives represented by the formula WHEREIN R1 and R2 are individually a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a nitro group, a lower alkylthio group or a lower alkylsulfonyl group; R3 is a hydrogen atom, a lower alkyl group, a lower cycloalkyl group, a naphthyl group, a furyl group or a thienyl group; R4 is a lower cycloalkyl group or a trihalomethyl group; and n is an integer of 1 to 3, are novel compounds and have excellent pharmacological properties, particularly as anti-inflammatory and analgesic effects with low toxicity. They can be prepared by treating with ammonia a trihaloacetamidophenylketone derivative of the formula WHEREIN R1, R2 and R3 are as defined above: R is a hydrogen atom or a group of the formula -CnH2n-R4; and X is a halogen atom.

    Process for preparing benzodiazocines and benzodiazonines
    5.
    发明授权
    Process for preparing benzodiazocines and benzodiazonines 失效
    制备苯二酸和苯并二恶英的方法

    公开(公告)号：US3697508A

    公开(公告)日：1972-10-10

    申请号：US3697508D

    申请日：1968-12-09

    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

    IPC分类号： C07D245/06 ,  C07D53/00

    CPC分类号： C07D245/06

    摘要： Novel 2-oxo-6-phenyl-1,5-benzodiazocine and 2-oxo-7-phenyl-1,6benzodiazonine derivatives are prepared by such a manner that an indole-2-alkylamine derivative is formed by reducing an indole-2aliphatic acid amide or thioamide, or by other processes, and oxidizing the resulting indole-2-alkylamine derivative. These 2oxo-6-phenyl-1,5-benzodiazocine and 2-oxo-7-phenyl-1,6benzodiazonine derivatives are useful as tranquilizers, musclerelaxants and hypnotics.

    摘要翻译： 新的2-氧代-6-苯基-1,5-苯并二氮辛和2-氧代-7-苯基-1,6-苯并二氮杂衍生物通过使吲哚-2-烷基胺衍生物通过还原吲哚-2- 2-脂肪酸酰胺或硫代酰胺，或通过其它方法，氧化得到的吲哚-2-烷基胺衍生物。 这些2-氧代-6-苯基-1,5-苯并二氮辛和2-氧代-7-苯基-1,6-苯并二氮杂衍生物可用作镇定剂，肌肉松弛剂和催眠药。

    Benzodiazepine derivatives and salts thereof
    6.
    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.