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1. 发明授权

US3840529A 1-(1-(3-substituted-1-propenyl)-4-piperidyl)-2-oxobenzimidazolines 失效
标题翻译： 1-（1-（3-取代-1-丙烯基）-4-哌啶基）-2-氧代苯并咪唑
公开(公告)号：US3840529A
公开(公告)日：1974-10-08
申请号：US28302572
申请日：1972-08-23
申请人： SUMITOMO CHEMICAL CO
发明人： MARUYAMA I , NAKAO M , SASAJIMA K , YAMAMOTO H , YANAGIHARA I , INABA S
IPC分类号： C07D295/08 , A61K31/435 , A61P25/00 , A61P25/18 , C07D211/52 , C07D295/084 , C07D401/04 , C07D471/10 , C07D29/36
CPC分类号： C07D295/084 , C07D211/52
摘要： WHEREIN R1 IS A HYDROGEN ATOM, A HALOGEN ATOM, A LOWER ALKYL, LOWER ALKOXY, NITRO, LOWER ALKANOYLAMINE OR TRIFLUOROMETHYL GROUP; R2 IS A HYDROGEN OR HALOGEN ATOM; R3 IS A HYDROGEN ATOM OR A LOWER ALKANOYL GROUP; R4 IS A HYDROGEN ATOM, A HALOGEN ATOM OR A LOWER ALKYL GROUP; AND X IS AN OXYGEN ATOM, A SULFUR ATOM, A SULFINYL OR SULFONYL GROUP.

2-(O=),3-R3,R4-BENZIMIDAZOLINE

1-(1-((R1,R2-PHENYL)-X-CH2-CH=CH-)-PIPERIDIN-4-YL-),

1. A PROPENYLAMINE DERIVATIVE OF THE FORMULA

2. 发明授权

US3833648A Process for preparing acylphenoxyaliphatic acid derivatives 失效
标题翻译：制备乙酰氧基酸衍生物的方法
公开(公告)号：US3833648A
公开(公告)日：1974-09-03
申请号：US8487570
申请日：1970-10-28
申请人： SUMITOMO CHEMICAL CO
发明人： MORIYAMA H , YAMAMOTO H , INABA S , NAGATA H , TAMAKI T
IPC分类号： C07C59/125 , C07C49/84 , C07C51/00 , C07C59/90 , C07C67/00 , C07C65/14
CPC分类号： C07C59/90 , C07C49/84
摘要： A PROCESS FOR PRODUCING ACYLPHENOXY ALIPHATIC CARBOXYLIC ACID DERIVATIVES REPRESENTED BY THE GENERAL FORMULA,

((R-CO-),(X)M-PHENYL)-O-CNH2N-COOH

WHEREIN R IS A LOWER ALKYL, ALKENYL OR ALKYNYL GROUP, X IS THE SAME OR DIFFERENT HYDROGEN ATOM, HALOGEN ATOM, LOWER ALKYL GROUP, TRIFLUOROMETHYL GROUP OR LOWER ALKOXY GROUP, AND WHEN SUBSTITUTED ON ADJACENT CARBON ATOMS OF THE BENZENE RING, TWO X''S RADICALS MAY BE JOINED TOGETHER TO FORM A HYDROCARBYLENE CHAIN CONTAINING FOUR CARBON ATOMS BETWEEN ITS POINTS OF ATTACHMENT, FOR EXAMPLE, TETRAMETHYLENE, 1,3-BUTADIENYLENE, ETC., M IS AN INTEGER OF 1 TO 4 AND N IS AN INTEGER OF 1 TO 4, CHARACTERIZED BY REACTING AN W-NITROACYLPHENOXYALKYL HYDROCARBON DERIVATIVE REPRESENTED BY THE GENERAL FORMULA, ((R-CO-),(X)M-PHENYL)-O-CNH2N-CH2-NO2 WHEREIN R, X, M AND N ARE AS DEFINED ABOVE, WITH A STRONG ACID.

3. 发明授权

US3812135A Pyrroloindole and pyridoindole derivatives 失效
标题翻译：吡咯烷和吡啶衍生物
公开(公告)号：US3812135A
公开(公告)日：1974-05-21
申请号：US23003572
申请日：1972-02-28
申请人： SUMITOMO CHEMICAL CO
发明人： OKAMOTO T , INABA S , YAMAMOTO H , AKASE T , IZUMI T
IPC分类号： C07D471/04 , C07D487/04 , C07D27/36
CPC分类号： C07D471/04 , C07D487/04
摘要： NOVEL INDOLE DERIVATIVES OF THE FORMULA

1-(Y-PHENYL),2,3-(-NH-CH2-CNH2N-),3-R,X-INDOLINE

WHEREIN X AND Y ARE EACH HYDROGEN, HALOGEN, LOWER ALKYL OR LOWER ALKOXY; R IS HYDROGEN OR LOWER ALKYL; AND N IS 1 OR 2, OR SALTS THEREOF HAVING HIGH ANTI-INFLAMMATORY ACTIVITY. THE INDOLE DERIATIVES ARE PREPARED BY REDUCING A 2-OXYINDOLE DERIVATIVE OF THE FORMULA,

1-(Y-PHENYL),3-(NC-CNH2N-),3-R,X-INDOLIN-2-ONE

WHEREIN X, Y, R AND N ARE AS DEFINED ABOVE.

4. 发明授权

US3712892A Quinazolinone derivatives 失效
标题翻译：喹诺酮衍生物
公开(公告)号：US3712892A
公开(公告)日：1973-01-23
申请号：US3712892D
申请日：1970-07-29
申请人： SUMITOMO CHEMICAL CO
发明人： INABA S , MORI K , YAMAMOTO H , YAMAMOTO M , ISHIZUMI K
IPC分类号： A61K31/505 , B02C4/10 , C07D239/78 , C07D239/82 , C07D401/04 , C07D51/48
CPC分类号： C07D401/04 , A61K31/505 , C07C255/00 , C07D239/82
摘要： NOVEL QUINAZOLINE DERIVATIVES, WHICH ARE USEFUL AS MEDICINES, OF THE FORMULA,

1-(R4-CNH2N-),2-(W=),4-D,R1,R2-QUINAZOLINE

WHEREIN D IS A GROUP OF THE FOMULA

R3-PHENYL, OR PYRIDYL

N IS 0 OR AN INTEGER OF 1 TO 3; R1, R2 AND R3 EACH IS HYDROGEN, HALOGEN, C1-4 ALKYL, C1-4 ALKOXY, NITRO, TRIFLUOROMETHYL, ETC.; R4 IS C3-6 CYCLOALKYL; AND W IS OXYGEN OR SULFUR. THESE QUINAZOLINE DERIVATIVES ARE PRODUCED BY ANY OF REACTIONS AS SHOWN IN THE FOLLOWING REACTION SCHEMA; WHEREIN D, N, R1, R2, R4 AND W ARE THE SAME AS DEFINED BELOW, AND R5 IS C1-4 ALKOXY-CARBONYL, CARBOXY, CARBAMYL OR CYANO.

D R A W I N G

5. 发明授权

US3845057A N-substituted sulfinyl alkylene piperazines 失效
标题翻译： N-取代的亚苄基亚苄基哌嗪
公开(公告)号：US3845057A
公开(公告)日：1974-10-29
申请号：US14506571
申请日：1971-05-19
申请人： SUMITOMO CHEMICAL CO
发明人： MARUYAMA I , YAMAMOTO H , SASAJIMA K , KITAGAWA S , NAKAO M , SAKAI S , INABA S
IPC分类号： C07D295/092 , C07D51/70
CPC分类号： C07D295/088
摘要： 1. AN N-SUBSTITUTED HETEROCYCLIC COMPOUND REPRESENTED BY THE FORMULA,

R1-PHENYLENE-S(=O)-H2NCN-N
CH(-R2)-CH2-)

WHEREIN R1 IS C1-C7 ALKOXY OR A HALOGEN ATOM; R2 IS HYDROGEN ATOMS; R3 IS C1-C7 ALKOXY- OR HALOGEN-SUSUBSTITUTED PHENYL; M IS 0; N IS 3 OR 4; AND K IS 1, AND A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF.

6. 发明授权

US3828027A 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：US3828027A
公开(公告)日：1974-08-06
申请号：US76234168
申请日：1968-09-16
申请人： SUMITOMO CHEMICAL CO
发明人： YAMAMOTO H , HIROHASHI T , ISHIZUMI K , INABA S , OKAMOTO T , MORI K , KOBAYASHI T , YAMAMOTO M , MARUYAMA I
IPC分类号： A01N57/24 , A61K31/40 , C07C59/84 , C07D209/04 , C07D209/14 , C07D243/24 , C07D243/36 , C07D53/06
CPC分类号： C07D209/04 , A01N57/24 , C07C59/84 , C07C251/72 , C07D209/14 , C07D243/24
摘要： THE PROCESS FOR PRODUCING BENZODIAZEPINE DERIVATIVES USEFUL FOR TRANQUILIZER,

1-R1,5-(X-PHENYL),R2,1,2-DIHYDRO-3H-1,4-BENZODIAZEPIN-2-

ONE

WHEREIN R1 IS HYDROGEN, C1-C3 ALKYL GROUP OR C4-C7 CYCLOHEXYLMETHYL GROUP AND R2 IS HYDROGEN OR HALOGENS AND X IS HALOGENS. 2-AMINOO-METHYLINDOLE DERIVATIVES OR THEIR SALTS 1-R1,2-(H2N-CH2-),3-(X-PHENYL),R2-INDOLE WHEREIN R1, R2 AND X RESPECTIVELY HAVE THE SAME MEANINGS AS ABOVE IS ALLOWED TO REACT WITH AN APPROPRIATE OXIDIZING AGENT, SUCH AS FOR EXAMPLE, CHROMIUM TRIOXIDE.
摘要翻译：制备用于镇定剂的苯并二氮杂衍生物的方法，其中R1是氢，C1不同C3烷基或C4差氮C7环己基甲基，R2是氢或卤素，X是卤素。

7. 发明授权

US3817984A Process for producing benzodiazepine derivatives 失效
标题翻译：生产苯二酸衍生物的方法
公开(公告)号：US3817984A
公开(公告)日：1974-06-18
申请号：US23015772
申请日：1972-02-28
申请人： SUMITOMO CHEMICAL CO
发明人： MORIYAMA H , YAMAMOTO H , INABA S , NAGATA H
IPC分类号： C07D243/16 , C07D53/06
CPC分类号： C07D243/16
摘要： R1 - NH - CH2 - CH2 - NH2 wherein R1 is as defined above, preferably in the presence of a catalyst such as copper acetate and an acid binding agent such as anhydrous potassium carbonate, anhydrous sodium acetate, pyridine or N-ethylmorpholine.

WHEREIN R1 is a hydrogen atom, a lower alkyl group or a cycloalkylmethyl group; R2 is a hydrogen atom, a halogen atom, a nitro group, a lower alkoxy group or a trifluoromethyl group; and R3 is a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group or a trifluoromethyl group, are produced by reacting a diphenylmethyleneimine derivative of the formula,

Novel process for producing 2,3-dihydro-III-1,4-benzodiazepine derivatives. 2,3-Dihydro-1H-1,4-benzodiazepine derivatives of the formula,
摘要翻译：制备2,3-二氢-III-1,4-苯并二氮杂衍生物的新方法。下式的2,3-二氢-1H-1,4-苯并二氮杂衍生物，其中R 1是氢原子，低级烷基或环烷基甲基; R2是氢原子，卤素原子，硝基，低级烷氧基或三氟甲基; R3是氢原子，卤素原子，低级烷基，低级烷氧基或三氟甲基，通过使下式的二苯基亚甲基亚胺衍生物反应来制备，其中R2和R3如上定义; 和X是卤素原子，其中R1-NH-CH2-CH2-NH2的乙二胺衍生物，其中R 1如上定义，优选在催化剂如乙酸铜和酸结合剂如无水物碳酸钾，无水乙酸钠，吡啶或N-乙基吗啉。

8. 发明授权

US3752806A Benzodiazepines 失效
标题翻译： BENZODIAZEPINES
公开(公告)号：US3752806A
公开(公告)日：1973-08-14
申请号：US3752806D
申请日：1971-08-16
申请人： SUMITOMO CHEMICAL CO
发明人： YAMAMOTO H , INABA S , MORI K , IZUMI T , MARUYAMA I , KUME Y , ISHIZUMI K , AKATSU M , HIROHASHI T , YAMAMOTO M
IPC分类号： C07D405/06 , C07D243/24 , C07D243/26 , C07D53/06
CPC分类号： C07D243/24
摘要： NOVEL BENZODIAZEPINES REPRESENTED BY THE FORMULA,

1-(R4-(-O-)>CH-CNH2N-),2-(O=),3-R3,5-R2,R1-1,2-DIHYDRO-

3H-1,4-BENZODIAZEPINE

WHEREIN R1 REPRESENTS HYDROGEN, HALOGEN, NITRO, C1-4 ALKOXY, CYANO OR TRIFLUOROMETHYL; R2 REPRESENTS A GROUP OF THE FORMULA,

(PYRIDYL)-, OR (R5,R6-BENZENE)

(WHEREIN R5 AND R6 REPRESENT HYDROGEN, HALOGEN, TRIFLUOROMETHYL, CYANO OR C1-4 ALKY); R3 AND R4 REPRESENT HYDROGEN OR C1-4 ALKYL; AND N REPRESENTS AN INTEGER OF 1 TO 4 ARE PREPARED BY REACTING A 1-UNSUBSTITUTED BENZODIAZEPINE REPRESENTED BY THE FORMULA,

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

WHEREIN R1, R2 AND R3 ARE AS DEFINED ABOVE, WITH A REACTIVE ESTER OF ALCOHOL REPRESENTED BY THE FORMULA

HO-CNH2N-CH
WHEREIN R4 IS AS DEFINED ABOVE. RHE BENZODIAZEPINE DERIVATIVES OF THE FORMULA I HAVE VALUABLE PHARMACOLOGICAL PROPERTIES, IN PARTICULAR EXCELLENT TRANQUILIZING, SEDATIVE, MUSCLE RELAXANT, ANTICONVULSANT AND HEXOBARBITAL POTENTIATING ACTIVITIES.

9. 发明授权

US3723464A Process for manufacturing nitrobenzodiazepine derivatives 失效
标题翻译：制备硝基二苯并咪唑衍生物的方法
公开(公告)号：US3723464A
公开(公告)日：1973-03-27
申请号：US3723464D
申请日：1971-04-06
申请人： SUMITOMO CHEMICAL CO
发明人： MARUYAMA I , MORI K , ISHIZUMI K , YAMAMOTO M , OKAMOTO T , HIROHASHI T , YAMAMOTO H , INABA S , KOBAYASHI T
IPC分类号： C07D209/04 , C07D27/56
CPC分类号： C07D209/04
摘要： WHEREIN X has the same significance as mentioned above. The starting 2-aminomethylindole derivatives are prepared by reacting a nitrophenylhydrazine of the formula,

WHEREIN X signifies a hydrogen or halogen atom, are obtained by reacting with an oxidizing agent, such as chromic acid or the like, a novel 2-aminomethylindole derivative of the formula,

D R A W I N G
WHEREIN X has the same significance as mentioned above, converting the indole-2-carboxylic acid derivative to a corresponding amide derivative, dehydrating the amide to a corresponding nitrile derivative, and then reducing the formed nitrile derivatives.

WHEREIN X has the same significance as mentioned above, to give an indole 2-carboxylic acid derivative of the formula,

WITH A PHENYLPYRUVIC ACID DERIVATIVE OF THE FORMULA,

Benzodiazepine derivatives, which have been well known as excellent tranquillizers and which have the formula,

D R A W I N G
摘要翻译：通过与氧化剂如铬酸等反应得到苯并二氮杂衍生物，它们是众所周知的优良镇静剂，其具有下式：其中X表示氢或卤素原子，通过与氧化剂如铬酸等反应得到新的2-氨基甲基吲哚衍生物公式，WHEREIN X具有与上述相同的意义。

10. 发明授权

US3812102A Process for producing benzodiazepine derivatives 失效
公开(公告)号：US3812102A
公开(公告)日：1974-05-21
申请号：US17229971
申请日：1971-08-16
申请人： SUMITOMO CHEMICAL CO
发明人： ISHIZUMI K , MORI K , INABA S
IPC分类号： C07D209/04 , C07D209/48 , C07D243/32 , C07D243/36 , C07D53/06
CPC分类号： C07D209/04 , C07D209/48
摘要： A NOVEL PROCESS FOR PRODUCING BENZODIAZEPINE DERIVATIVES REPRESENTED BY THE FORMULA,

1-R1,3-R2,5-(X-PHENYL),NH2,Y-2,3-DIHYDRO-1H-1,4-

BENZODIAZEPIN-2-ONE

WHEREIN R1 IS A HYDROGEN ATOM, OR A LOWER ALKYL OR CYCLOALKYLMETHYL GROUP, R2 IS A HYDROGEN ATOM OR A LOWER ALKYL GROUP, X AND Y ARE INDIVIDUALLY HYDROGEN OR HALOGEN ATOMS OR LOWER ALKYL GROUP, OR ACID SALTS THEREOF, WHICH COMPRISES REACTING A DIPHTHALIMIDOBENZOPHENONE DERIVATIVE REPRESENTED BY THE FORMULA,

1-((1,3-DI(O=)ISOINDOLINO)-CH(-R2)-CO-N(-R1)-),2-((X-

PHENYL)-CO-),(1,3-DI(O=)ISOINDOLINO),Y-BENZENE

WHEREIN R1, R2, X AND Y ARE THE SAME AS DEFINED ABOVE, WITH A HYDRAZINE DERIVATIVE TO OBTAIN THE BENZODIAZEPINE DERIVATIVES OF THE FORMULA (I). THE BENZODIAZEPINE DERIVATIVES REPRESENTED BY FORMULA (i) HAVE EXCELLENT EFFECTS AS SEDATIVES, MUSCLE-RELAXANT, ANTI-SPASMODICS, AND HYPNOTICS.

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