公开(公告)号：US3886174A

公开(公告)日：1975-05-27

申请号：US32345373

申请日：1973-01-15

Applicant: UPJOHN CO

Inventor： HESTER JR JACKSON B

IPC: C07D57/02

Abstract: 6-Phenyl-4H-s-triazolo(4,3-a)(1,4)benzodiazepines of the formula (III):

wherein R is selected from the group consisting of cyano, nitro, alkylthio in which the alkyl groups are of 1 to 3 carbon atoms, inclusive, and -COOR'''' in which R'''' is an alkyl group defined as above; wherein R1 is selected from the group consisting of hydrogen and alkyl, defined as above, and wherein R2, R3, R4, and R5 are selected from the group consisting of hydrogen, alkyl defined as above, halogen, nitro, cyano, trifluoromethyl, and alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, and alkanoylamino, in which the carbon chain moieties are of 1 to 3 carbon atoms, inclusive, and dialkylamino in which alkyl is defined as above, are produced by condensing a 1,3-dihydro-5phenyl-2H-1,4-benzodiazepine-2-thione of the formula (I):

wherein R1, R2, R3, R4, and R5 are defined as above, with an organic acid hydrazide of the formula (II):

wherein R'' is selected from the groups consisting of cyano, nitro, and alkylthio in which the alkyl groups are defined as above, or by hydrolyzing a compound in which R'' is -CN, with an alcohol, water and hydrogen chloride to obtain a product III wherein R is -COOR'''', and R'''' is alkyl, defined as above. The new products of formula III including their pharmacologically acceptable acid addition salts are useful as sedatives, tranquilizers and muscle relaxants in mammals and birds.

Abstract translation: 式（III）的6-苯基-4H-三唑并[4,3-a] [1,4]苯并二氮杂：

公开(公告)号：US3880855A

公开(公告)日：1975-04-29

申请号：US44538274

申请日：1974-02-25

Applicant: BRISTOL MYERS CO

Inventor： JUBY PETER FREDERICK ,  HUDYMA THOMAS WILLIAM

IPC: A23K1/16 ,  C07D239/42 ,  C07D239/46 ,  C07D239/48 ,  C07D265/26 ,  C07D487/04 ,  C07D57/02

CPC classification number: C07D239/42 ,  C07D239/47 ,  C07D239/48 ,  C07D265/26 ,  C07D487/04 ,  Y10S514/916

Abstract: Appropriately substituted 11H-pyrimido(4,5-b)(1,4)benzodiazepines have shown biological activity, e.g., antihypoxic, hypothermic, antipyretic and anti-inflammatory. An example of a potent anti-hypoxic agent is 5,6-dihydro-11-methyl11H-pyrimido(4,5-b)(1,4)-benzodiazepine.

Abstract translation: 适当取代的11H-嘧啶并[4,5-b] - [1,4]苯并二氮杂卓具有生物活性，例如抗低氧，低温，解热和抗炎。 有效的抗缺氧剂的实例是5,6-二氢-11-甲基-11H-嘧啶并[4,5-b] [1,4] - 苯并二氮杂。

公开(公告)号：US3852300A

公开(公告)日：1974-12-03

申请号：US20617671

申请日：1971-12-08

Applicant: CIBA GEIGY CORP

Inventor： GAGNEUX A ,  HECKENDORN R ,  MEIER R

IPC: C07D249/10 ,  C07D487/04 ,  C07D57/02

CPC classification number: C07D487/04 ,  C07D249/10

Abstract: A new process for the production of compounds of the class of 6phenyl-4H-s-triazolo(1,5-a)(1,4)benzodiazepines and 2-lower alkyl-4H-s-triazolo(1,5-a)(1,4)benzodiazepines, their 5-oxides and their acid addition salts is provided. Compounds of the class of 6-phenyl-4H-s-triazolo(1,5-a)(1,4)benzodiazepines, their 5oxides and their pharmaceutically acceptable acid addition salts are also obtained by a second process and have valuable central depressant properties, in particular anticonvulsant action, and inhibit somatic reflexes. They are active ingredients for pharmaceutical compositions. Specific embodiments are 6-phenyl-8chloro-4H-s-triazolo-(1,5-a)(1,4)benzodiazepine and 6-(ochlorophenyl)-8-chloro-4H-s-triazolo(1,5-a)(1,4)benzodiazepine.

Abstract translation: 用于生产6-苯基-4H-s-三唑并[1,5-a] [1,4]苯并二氮杂类和2-低级烷基4H-三唑并[1,5- a] [1,4]苯并二氮杂，其5-氧化物及其酸加成盐。 6-苯基-4H-s-三唑并[1,5-a] [1,4]苯并二氮杂类的化合物，其5-氧化物及其药学上可接受的酸加成盐也通过第二种方法获得，并且具有有价值的中心 抑制性质，特别是抗惊厥作用，并抑制体细胞反射。 它们是药物组合物的活性成分。 具体实施方案是6-苯基-8-氯-4H-三唑并 - [1,5-a] [1,4]苯并二氮杂和6-（邻氯苯基）-8-氯-4H-三唑并[1 ，5-a] [1,4]苯并二氮杂。

公开(公告)号：US3773783A

公开(公告)日：1973-11-20

申请号：US3773783D

申请日：1972-07-24

Applicant: SANDOZ AG

Inventor： HOULIHAN W

IPC: C07D487/04 ,  C07D57/02

CPC classification number: C07D487/04

Abstract: BENZYL SUBSTITUTED-5-ARYL-IMIDAZO(2,1-A)ISOINDOLES, E.G., 5-BENZYL - 5 - (P-CHLOROPHENY)-5H-IMIDAZO(2,1-A)ISOINDOLES ARE PREPARED BY TREATING ALKALI METAL SALTS OF 5-ARYLIMIDAZO(2,1-A)ISOINDOLES WITH BENZYL HALIDES AND ARE USEFUL AS ANTI-MICROBIALS.

公开(公告)号：US3763178A

公开(公告)日：1973-10-02

申请号：US3763178D

申请日：1968-09-05

Applicant: AMERICAN HOME PROD

Inventor： SULKOWSKI T

IPC: C07D209/46 ,  C07D209/48 ,  C07D487/04 ,  C07D49/34 ,  C07D57/02

CPC classification number: C07D209/48 ,  C07D209/46 ,  C07D487/04

Abstract: THIS INVENTION IS CONCERNED WITH TETRAHYDROPYIMIDINYL PHENYL CARBOYL ACID ADDITION SALTS, IMIDAZOLINYL PHENYL CARBONYL ACID ADDITION SALTS, DIHYDROMIDAZOISOINDOLOLS, TETRAHYDROPYRIMIDOISOMDOLOLS, AND TETRAHYDROPYRIMIDOISOINDOLOL ACID ADDITION SALTS WHICH ARE ALL PHARMACOLOGICALLY EFFICACIOUS AS ANTI-DEPRESSANTS. THE TETRAHYDROPYRIMIDINYL PHENYL CARBONYL ACID ADDITION SALTS, THE TETRAHYDROPYRIMIDOISOIMDOLOLS AND THE TETRAHYDROPYRIMIDOISOINDOLOL ACID ADDITION SALTS ARE ALSO EFFICACIOUS AS DILURETICS WHILE THE IMIDAZOLINYL PHENYL CARBONYL ACID ADDITION SALTS AND THE DIHYDROMIDAZOISOINDOLOLS ARE EFFICACIOUS AS ANOREXIANTS. THIS INVENTION IS ALSO CONCERNED WITH SEVERAL PROCESSES FOR THE PREPARATION OF THESE COMPOUNDS.

公开(公告)号：US3759943A

公开(公告)日：1973-09-18

申请号：US3759943D

申请日：1971-04-28

Applicant: UPJOHN CO

Inventor： HESTER J

IPC: C07D487/04 ,  C07D57/02 ,  C07D99/02

CPC classification number: C07D487/04

Abstract: WHEREIN R1, R2, R3, R4, and R5 are defined as above and R is alkyl of one to three carbon atoms, inclusive.

WHEREIN R'' and R'''' are hydrogen, alkyl of one to three carbon atoms, inclusive, or together

Compounds of the formula:

Abstract translation: 下式的化合物：

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：US3655647A

公开(公告)日：1972-04-11

申请号：US3655647D

申请日：1970-03-16

Applicant: UPJOHN CO

Inventor： HESTER JACKSON B JR

IPC: C07D487/04 ,  C07D57/02

CPC classification number: C07D487/04

Abstract: A 3,4,5,10-TETRAHYDROAZEPINO(2,3-B)INDOL-1(2H)ONE REPRESENTED BY THE FORMULA

R-3,4,5,10-TETRAHYDROAZEPINO(2,3-B)INDOL-2(1H)-ONE

WHEREIN R IS A MEMBER OF THE GROUP CONSISTING OF HYDROGEN, ALKYL, ALKOXY, AND HALO RADICALS, WHEREIN THE ALKYL AND ALKOXY RADICALS CONTAIN FORM 1 TO 3 CARBON ATOMS, INCLUSIVE. USEFUL INTERMEDIATE FOR PREPARATION OF PHARMACOLOGICALLY ACTIVE COMPOUNDS.

公开(公告)号：US3642779A

公开(公告)日：1972-02-15

申请号：US3642779D

申请日：1969-10-22

Applicant: ROBINS CO INC A H

Inventor： DUNCAN ROBERT LOUIS JR ,  HELSLEY GROVER CLEVELAND

IPC: C07D209/14 ,  C07D487/04 ,  C07D57/02

CPC classification number: C07D487/04 ,  C07D209/14 ,  Y10S514/96 ,  Y10S514/962

Abstract: NOVEL INDOLO(1,2-D)(1,4)BENZDIAZEPIN-6-ONES HAVING PHARMACODYNAMIC ACTIVITY AS ANTIDEPRESSANTS AND ANTICONVULSANTS ARE DISCLOSE. THE COMPOUNDS ARE PREPARED BY ACYLATION OF 2-(2-AMINOPHENYL)INDOLES WITH HALOACETYLHALIDES FOLLOWED BY CYCLIZATION UNDER BASIC CONDITIONS. COMPOUNDS SUBSTITUTED IN THE 5-POSITION ARE PREPARED BY REACTION WITH COMPOUNDS HAVING DISPLACEABLE HALOGENS AND WITH ISOCYANATES.

公开(公告)号：US3637708A

公开(公告)日：1972-01-25

申请号：US3637708D

申请日：1967-11-20

Applicant: CIBA LTD

Inventor： PETER RICHARD ,  GALLACCHI ENRICO

IPC: D06P3/54 ,  C09B57/00 ,  C07D57/02

CPC classification number: C09B57/00 ,  Y10S8/922

Abstract: WATER-INSOLUBLE PERINONES CARRYING AT ONE OF THE PERIPOSITIONS OF THE NAPHTHALENE NUCLEUS A HETEROCYCLIC SUBSTITUENT BOUND VIA A SULFUR, NITROGEN OR OXYGEN ATOM.