公开(公告)号：US3862152A

公开(公告)日：1975-01-21

申请号：US26574072

申请日：1972-06-23

Applicant: TAKEDA CHEMICAL INDUSTRIES LTD

Inventor： KUWADA YUTAKA ,  MEGURO KANJI ,  MIYANO HIROSHI

IPC: C07D215/38 ,  C07D33/50

CPC classification number: C07D215/38 ,  Y10S514/925

Abstract: The present invention relates to novel quinoline derivatives, which have an antiulcer action, and also relates to a method for the production thereof. The present inventors studied quinoline derivatives and succeeded in synthesizing novel quinoline derivatives and further found out that these novel 3-carbamoylamino or thiocarbamoylamino phenylquinolines derivatives have an antiulcer action with low toxicity.

Abstract translation: 本发明涉及具有抗溃疡作用的新颖喹啉衍生物，还涉及其制备方法。

公开(公告)号：US3864356A

公开(公告)日：1975-02-04

申请号：US32941273

申请日：1973-02-05

Applicant: TAKEDA CHEMICAL INDUSTRIES LTD

Inventor： MEGURO KANJI ,  KUWADA YUTAKA

IPC: C07D243/20 ,  C07D57/02

CPC classification number: C07D243/20

Abstract: The compounds (III) and (IV) possess activity as central nervous system agents.


1-OXO- OR 1-THIOXO-S-TRIAZOLO (4,3-A)(1,4) BENZODIAZEPINE DERIVATIVES OR THE CORRESPONDING 5N-oxides or tautomers thereof are prepared as follows:
D R A W I N G

Abstract translation: 1-氧代 - 或1-硫代-S-三唑[4,3-A] [1,4]苯并恶嗪衍生物或其相应的5N氧化物或互变异构体如下制备：

公开(公告)号：US3887541A

公开(公告)日：1975-06-03

申请号：US28854472

申请日：1972-09-13

Applicant: TAKEDA CHEMICAL INDUSTRIES LTD

Inventor： TAWADA HIROYUKI ,  MEGURO KANJI ,  KUWADA YUTAKA

IPC: C07D243/20 ,  C07D53/06

CPC classification number: C07D243/20

Abstract: S-Triazolo (1,5-a)(1,4) benzodiazepine derivatives are produced by the following process:

Compounds (I), (IV) and (V), 4 or 5 N-oxides thereof and acid salts thereof are active central nervous system agents.

Abstract translation: S-三唑并[1,5-a] [1,4]苯并二氮杂衍生物通过以下方法制备：

公开(公告)号：US3927015A

公开(公告)日：1975-12-16

申请号：US48279874

申请日：1974-06-24

Applicant: TAKEDA CHEMICAL INDUSTRIES LTD

Inventor： KUWADA YUTAKA ,  MEGURO KANJI ,  TAWADA HIROYUKI

IPC: A61K20060101 ,  A61K31/55 ,  C07D20060101 ,  C07D239/92 ,  C07D243/00 ,  C07D249/00 ,  C07D249/08 ,  C07D487/04

CPC classification number: C07D239/92 ,  C07D249/08 ,  C07D487/04

Abstract: Compounds of the formula

WHERE R is hydrogen or lower alkyl and rings A and B may be substituted by halogen, nitro, trifluoromethyl, lower alkyl or lower alkoxy. These compounds are useful in preparing the corresponding compounds of the formula

BY SUBJECTING THE FORMER TO DEHYDRATION CONDITIONS TO EFFECT RING-CLOSURE. The latter compounds are useful as tranquilizers, sedatives and hyponotics.

D R A W I N G

Abstract translation: 式WHERE R为氢或低级烷基且环A和B的化合物可以被卤素，硝基，三氟甲基，低级烷基或低级烷氧基取代。 这些化合物可用于制备相应的式的化合物，其通过将前体引入脱盐条件来影响环封闭。 后一种化合物可用作镇定剂，镇静剂和hyponotics。

公开(公告)号：US3907820A

公开(公告)日：1975-09-23

申请号：US1697070

申请日：1970-03-05

Applicant: TAKEDA CHEMICAL INDUSTRIES LTD

Inventor： MEGURO KANJI ,  KUWADA YUTAKA

IPC: C07D243/20 ,  C07D487/04

CPC classification number: C07D487/04 ,  C07D243/20

Abstract: Benzodiazepine compounds of the formula

WHEREIN R1 is hydrogen or a hydrocarbon residue, R2 is hydrogen or a lower alkyl group, the rings A and B are unsubstituted or substituted by one or more of nitro, trifluoromethyl, halogen, alkyl and alkoxy groups are produced by reacting a compound of the formula
WITH A REACTIVE DERIVATIVE OF A CARBOXYLIC ACID TO PRODUCE A COMPOUND OF THE FORMULA

WHEREIN -OCOR3 is an acyloxy group convertible to a hydroxy or alkoxy group AND SUBJECTING COMPOUNDS II to hydrolysis or alcoholysis and optionally subjecting the compounds I wherein R2 is hydrogen to etherification. Compounds I and II are useful as anticonvulsants, sedatives and tranquilizing agents.

Abstract translation: 式WHEREIN R1的苯并二氮杂化合物是氢或烃残基，R 2是氢或低级烷基，环A和B是未被取代的或被硝基，三氟甲基，卤素，烷基和烷氧基中的一个或多个取代，由 使式的化合物与羧酸的反应性衍生物反应制备式IV的化合物，其中-OCOR 3是可转化为羟基或烷氧基的酰氧基，并且将化合物II进行水解或醇解并任选地使化合物I R2是氢至醚化。 化合物I和II可用作抗惊厥药，镇静剂和镇静剂。

公开(公告)号：US3876634A

公开(公告)日：1975-04-08

申请号：US40617273

申请日：1973-10-12

Applicant: TAKEDA CHEMICAL INDUSTRIES LTD

Inventor： MEGURO KANJI ,  TAWADA HIROYUKI ,  KUWADA YUTAKA

IPC: C07D249/08 ,  C07D55/06

CPC classification number: C07D249/08 ,  Y10S514/906 ,  Y10S514/923

Abstract: Where Z is halogen.

Where R is hydrogen or lower alkyl, X is O or NH, Y is unsubstituted or substituted ethylene or trimethylene and rings A and B may be substituted are useful as tranquilizers. Also provided are novel starting materials of the formula

Compounds of the formula

公开(公告)号：US3703525A

公开(公告)日：1972-11-21

申请号：US3703525D

申请日：1970-11-16

Applicant: TAKEDA CHEMICAL INDUSTRIES LTD

Inventor： TAWADA HIROYUKI ,  MEGURO KANJI ,  KUWADA YUTAKA

IPC: C07D243/16 ,  C07D243/18 ,  C07D243/20 ,  C07D487/04 ,  C07D53/06 ,  C07D57/02

CPC classification number: C07D243/20 ,  C07D487/04

Abstract: S-TRIAZOLO (1,5-A)(1,4) BENZODIAZEPINE DERIVATIVES ARE PRODUCED BY THE FOLLOWING PROCESS:

2-(H2N-),3-R'',5-PHENYL-3H-1,4-BENZODIAZEPINE (II)

R-C(-O-R1)3 III --STEP 1-->

2-(R1-O-C(-R)=N-),3-R'',5-PHENYL-3H-1,4-BENZODIAZEPINE (IV)

--STEP 2--> 2-(H2N-C(-R)=N-),3-R'',5-PHENYL-3H-1,4-BENZO

DIAZEPINE (V) --STEP 3-->

2-R,4-R'',6-PHENYL-4H-S-TRIAZOLO(2,3-A)(1,4)BENZODIAZEPINE

COMPOUNDS I, IV AND V, 4 OR 5 N-OXIDES THEREOF AND ACID SALTS THEREOF ARE ACTIVE CENTRAL NERVOUS SYSTEM AGENTS.

公开(公告)号：US3900490A

公开(公告)日：1975-08-19

申请号：US41484373

申请日：1973-11-12

Applicant: TAKEDA CHEMICAL INDUSTRIES LTD

Inventor： KUWADA YUTAKA ,  NATSUGARI HIDEAKI ,  MEGURO KANJI

IPC: A61K20060101 ,  A61K31/41 ,  C07D20060101 ,  C07D245/06 ,  C07D271/06 ,  C07D498/04

CPC classification number: Y10S514/96

Abstract: Compounds of the formula;

WHEREIN Y is O or S, R1 and R2 are hydrogen or lower alkyl, rings A and B

公开(公告)号：US3865811A

公开(公告)日：1975-02-11

申请号：US32941173

申请日：1973-02-05

Applicant: TAKEDA CHEMICAL INDUSTRIES LTD

Inventor： MEGURO KANJI ,  KUWADA YUTAKA

IPC: C07D243/20 ,  C07D53/06

CPC classification number: C07D243/20

Abstract: 1-OXO- OR 1-THIOXO-S-TRIAZOLO (4,3-A)(1,4) BENZODIAZEPINE DERIVATIVES OF THE CORRESPONDING 5N-oxides or tautomers thereof are prepared as follows:

The compounds (III) and (IV) possess activity as central nervous system agents.

Abstract translation: 相应的5N氧化物或互变异构体的1-氧代 - 或1-硫代-S-三唑[4,3-A] [1,4]苯并恶嗪衍生物如下制备：

公开(公告)号：US3692772A

公开(公告)日：1972-09-19

申请号：US3692772D

申请日：1969-09-03

Applicant: TAKEDA CHEMICAL INDUSTRIES LTD

Inventor： MEGURO KANJI ,  TAWADA HIROYUKI ,  KUWADA YUTAKA ,  MASUDA TORU

IPC: A61K31/55 ,  B05C11/11 ,  B26D3/18 ,  C07D243/24 ,  C07D243/26 ,  C07D243/28 ,  C07D53/06

CPC classification number: C07D243/24 ,  A61K31/55 ,  B05C11/11 ,  B26D3/18 ,  C07D243/26 ,  C07D243/28

Abstract: The process for preparing benzodiazepin-2-one derivatives of the formula

WHEREIN R1 is hydrogen or lower alkyl, and rings A and B are either unsubstituted or substituted by one or more groups of nitro, trifluoromethyl, halogen, alkyl and alkoxy groups, which comprises subjecting a 2-amino- Alpha phenylbenzylideneaminoacetal derivative to ring-closure, hydrolyzing the resultant product to obtain the 2hydroxybenzodiazepine derivative, and subjecting such derivative to oxidation to yield the benzodiazepin-2-one derivative. Also provided are novel 1-alkyl-2-hydroxybenzodiazepine derivatives of the formula

WHEREIN R''1 is lower alkyl and rings A and B may be either unsubstituted or substituted as defined above, such derivatives being useful as intermediates in the above process and also as tranquilizing agents.

Abstract translation: 制备式WHEREIN R1的苯并二氮杂-2-酮衍生物的方法是氢或低级烷基，环A和B是未取代的或被一个或多个硝基，三氟甲基，卤素，烷基和烷氧基基团取代，其包括 使2-氨基-α-苯基亚苄基氨基缩醛衍生物闭环，水解所得产物，得到2-羟基苯并二氮杂衍生物，并使该衍生物氧化得到苯并二氮杂-2-酮衍生物。 还提供了式WHEREIN R'1是低级烷基的新的1-烷基-2-羟基苯并二氮杂衍生物，A和B环可以是未取代的或如上所定义的取代基，这些衍生物可用作上述方法中的中间体，也可用作 镇静剂。