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1. 发明授权

US3867372A Benzodiazepine process 失效
标题翻译：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。

2. 发明授权

US3634402A Process for producing 1 4-benzodiazepine derivatives and their salts 失效
标题翻译：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,

3. 发明授权

US3641002A Benzodiazepine derivatives and salts thereof 失效
标题翻译：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.

4. 发明授权

US3555013A Procedure for preparing 1,4-benzodiazepine-2-one derivatives 失效
标题翻译：制备1,4-二苯并噻吩-2-酮衍生物的方法
公开(公告)号：US3555013A
公开(公告)日：1971-01-12
申请号：US3555013D
申请日：1969-04-14
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 , KOBAYSHI TSUYOSHI , IZUMI TAKAHIRO
IPC分类号： A61K31/55 , C07D243/24 , C07D243/36 , D04G3/02 , C07D53/06
CPC分类号： C07D243/24 , A61K31/55 , C07D243/36 , D04G3/02
摘要： 1,4-BENZODIAZEPINE-2-ONE DERIVATIVE RESPRESENTED BY THE FORMULA,

1-(R1-N(-R2)-CO-CNH2N-),5-(R4-PHENYL),R3-2,3-DIHYDRO-1H-

1,4-BENZODIAZEPIN-2-ONE

WHEREIN R1 AND R2 SIGNIFY RESPECTIVELY A HYDROGEN ATOM OR A LOWER ALKYL GROUP; R3 AND R4 SIGNIFY RESPECTIVELY A HYDROGEN ATOM, A HALOGEN ATOM, A NITRO GROUP, A LOWER ALKYL GROUP OR A HLAOGENATED LOWER ALKYL GROUP; AND N SIGNIFIES 1, 2 OR 3, AND BEING EFFECTIVE AS TRANQUILLIZERS, MUSCLE-RELAXANTS AND HYPNOTICS, ARE PRODUCED BY REACTING WITH AN OXIDIZING AGENT A 2-AMINOMETHYL INDOLE DERIVATIVE, OR A SALT THEREOF, REPRESENTED BY THE FORMULA

1-(R1-N(-R2)-CO-CNH2N-),2-(NH2-CH2-),3-(R4-PHENYL),R3-

INDOLE

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

5. 发明授权

US3910889A Novel benzodiazepine derivatives and preparation thereof 失效
标题翻译：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。

6. 发明授权

US3875142A Process for preparing 2,3-dihydro-1H-benzodiazepine derivatives and their salts 失效
标题翻译：制备2,3-二氢-1H-苯并二氮杂衍生物及其盐的方法
公开(公告)号：US3875142A
公开(公告)日：1975-04-01
申请号：US25214072
申请日：1972-05-10
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： A61K31/55 , C07D209/04 , C07D233/32 , C07D233/70 , C07D243/16 , C07D487/04 , G03D15/00 , C07D53/06
CPC分类号： C07D209/04 , A61K31/55 , C07D233/32 , C07D233/70 , C07D243/16 , C07D487/04 , G03D15/00
摘要： 2,3-Dihydro-1H-benzodiazepine derivatives, and their salts, represented by the formula,
WHEREIN X and Y are as defined in the formula (I), with an acid.

WHEREIN X and Y are as defined in the formula (I), and then contacting the resultant piperazino-benzophenone derivative represented by the formula,

D R A W I N G
WHEREIN X and Y are as defined in the formula (I) with basic hydrolyzing agent. The imidazolidino benzophenone derivative is prepared by oxidizing a piperazino-(1,2-a)-indole derivative represented by the formula,

WHEREIN X and Y signify respectively a hydrogen atom, a halogen atom or a trifluoromethyl group, which are useful as tranquillizers, muscle-relaxants and hypnotics, are produced by contacting imidazolidino benzophenone derivative represented by the formula,
摘要翻译： 2,3-二氢-1H-苯并二氮杂衍生物及其盐，由式WHEREIN X和Y分别表示可用作镇静剂，肌肉松弛剂和催眠药的氢原子，卤素原子或三氟甲基，通过将式（I）所示的咪唑烷基二苯甲酮衍生物与式（I）所定义的基本水解试剂接触。

7. 发明授权

US3860575A Purification of benzodiazepine derivatives 失效
标题翻译：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。

8. 发明授权

US3702323A Method for preparing benzodiazepine derivatives 失效
标题翻译：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.

9. 发明授权

US3535334A 1-piperonoyl-3-indolyl aliphatic acid derivatives 失效
标题翻译： 1-哌啶-3-基吲哚基酸衍生物
公开(公告)号：US3535334A
公开(公告)日：1970-10-20
申请号：US3535334D
申请日：1967-11-24
申请人： SUMITOMO CHEMICAL CO
发明人： YAMAMOTO HISAO , MISAKI ATSUKO , IZUMI TAKAHIRO
IPC分类号： C07D317/60 , C07D405/06 , C07D27/56
CPC分类号： C07D405/06 , C07D317/60

10. 发明授权

US3702321A Process for preparing benzodiazepine derivatives 失效
标题翻译：制备苯二酸衍生物的方法
公开(公告)号：US3702321A
公开(公告)日：1972-11-07
申请号：US3702321D
申请日：1969-02-07
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： C07D209/04 , C07D209/08 , C07D241/08 , C07D487/04 , C07D51/72 , C07D53/06 , C07D57/02
CPC分类号： C07D209/04 , C07D209/08 , C07D241/08 , C07D487/04
摘要： A 2,3-DIHYDRO-1H-1,4-BENZODIAZEPINE DERIVATIVE, WHICH IS USEFUL AS TRANQUILLIZER, HYPNOTIC, MUSCLE-RELAXANT AND ANTICONVULSANT, IS PRODUCED BY HYDROLYZING A 2-(DIOXOPIPERAZINO)-BENZOPHENONE DERIVATIVE. THE 2-(DIOXOPIPERAZINO)-BENZOPHENONE DERIVATIVE IS PREPARED BY TREATING A 3-PHENYL-INDOLE-2-CARBOXYLIC ACID ESTER DERIVATIVE WITH A REACTIVE ESTER OF CYANOMETHYLALCOHOL, AND REDUCING THE RESULTING 1-CYANOMETHYL COMPOUND, AND THEN CONTACTING THE RESULTING PIPERAZINO-INDOLE DERIVATIVE WITH A SUITABLE OXIDIZING AGENT.

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