公开(公告)号：US3905994A

公开(公告)日：1975-09-16

申请号：US46703174

申请日：1974-05-06

Applicant: HOFFMANN LA ROCHE

Inventor： METLESICS WERNER ,  STERNBACH LEO HENRYK

IPC: A61K31/00 ,  C07C45/41 ,  C07C49/86 ,  C07C51/363 ,  C07D209/44 ,  C07D233/22 ,  C07D487/04 ,  C07D49/34

CPC classification number: C07D487/04 ,  A61K31/00 ,  C07C45/29 ,  C07C45/41 ,  C07C51/363 ,  C07D209/44 ,  C07D233/22 ,  Y10S514/916 ,  C07C49/86 ,  C07C65/34

Abstract: 2(2-(1,3-diazacycloalk-2-enyl))benzophenone compounds and 1,3diazacycloalkenyl(2,1-a)isoindole compounds having useful analgesic and psychostimulant properties are prepared inter alia by condensation of o-benzoylbenzaldehydes with aliphatic diamines.

Abstract translation: 具有有用的止痛和精神兴奋剂性质的2- [2-（1,3-二氮杂环烯-2-烯基）]二苯甲酮化合物和1,3-二氮杂环烯基[2,1-a]异吲哚化合物特别是通过邻苯甲酰基苯甲醛与 脂肪族二胺。

公开(公告)号：US3880840A

公开(公告)日：1975-04-29

申请号：US43881074

申请日：1974-02-01

Applicant: HOFFMANN LA ROCHE

Inventor： FIELD GEORGE FRANCIS ,  STERNBACH LEO HENRYK ,  WALSER ARMIN

IPC: C07D241/20 ,  C07D241/26 ,  C07D401/06 ,  C07D403/06 ,  C07D487/04 ,  C07D57/24

CPC classification number: C07D401/06 ,  C07D241/20 ,  C07D241/26 ,  C07D403/06 ,  C07D487/04 ,  Y10S514/906

Abstract: Novel pyrazino-1,4-diazepines are disclosed together with processes for their preparation and novel intermediates used in these processes. These novel diazepines are useful as sedatives, muscle-relaxants and anti-convulsants.

Abstract translation: 公开了新的吡嗪-1,4-二氮杂及其制备方法和用于这些方法的新型中间体。 这些新的二氮杂类药物可用作镇静剂，肌肉松弛剂和抗惊厥药。

公开(公告)号：US3875238A

公开(公告)日：1975-04-01

申请号：US46717674

申请日：1974-05-06

Applicant: HOFFMANN LA ROCHE

Inventor： METLESICS WERNER ,  STERNBACH LEO HENRYK

IPC: A61K31/00 ,  C07C45/41 ,  C07C49/86 ,  C07D209/44 ,  C07D233/22 ,  C07D487/04 ,  C07C49/44

CPC classification number: C07D487/04 ,  A61K31/00 ,  C07C45/29 ,  C07C45/41 ,  C07C49/86 ,  C07D209/44 ,  C07D233/22

Abstract: Novel 2(2-(1,3-diazacycloalk-2-enyl))benzophenone compounds and novel 1,3-diazacycloalkenyl(2,1-a)isoindole compounds having useful analgesic and psychostimulant properties are prepared inter alia by condensation of o-benzoylbenzaldehydes with aliphatic diamines.

Abstract translation: 新颖的2- [2-（1,3-二氮杂环烯-2-烯基）]二苯甲酮化合物和具有有用的止痛和精神兴奋剂性质的新的1,3-二氮杂环烯基[2,1-a]异吲哚化合物特别是通过o- 苯甲酰基苯甲醛与脂族二胺。

公开(公告)号：US3875181A

公开(公告)日：1975-04-01

申请号：US41956473

申请日：1973-11-28

Applicant: HOFFMANN LA ROCHE

Inventor： DERIEG MICHAEL EDWARD ,  FRYER RODNEY IAN ,  STERNBACH LEO HENRYK

IPC: C07D487/04 ,  C07D49/34

CPC classification number: C07D487/04

Abstract: Novel 1H-1,4-benzodiazepines bearing between the 1,2-positions an imidazo ring. These novel benzodiazepines are useful as muscle relaxant, anti-convulsant and sedative agents.

Abstract translation: 在1,2位上带有咪唑环的新型1H-1,4-苯并二氮杂。 这些新型苯二氮卓类可用作肌肉松弛剂，抗惊厥药和镇静剂。

公开(公告)号：US3686308A

公开(公告)日：1972-08-22

申请号：US3686308D

申请日：1970-04-15

Applicant: HOFFMANN LA ROCHE

Inventor： NING ROBERT YE-FONG ,  STERNBACH LEO HENRYK

IPC: C07C271/22 ,  C07D243/16 ,  C07D243/24 ,  C07D243/28 ,  C07C103/42

CPC classification number: C07C247/00 ,  C07C271/22 ,  Y10S514/906

Abstract: The present invention relates to processes for the preparation of 7-lower alkanoyl-1,4-benzodiazepin-2-ones. These compounds are known to be useful as muscle relaxants, sedatives and anticonvulsants.

Abstract translation: 本发明涉及制备7-低级烷酰基-1,4-苯并二氮杂-2-酮的方法。 已知这些化合物可用作肌肉松弛剂，镇静剂和抗惊厥药。

公开(公告)号：US3682892A

公开(公告)日：1972-08-08

申请号：US3682892D

申请日：1970-12-23

Applicant: HOFFMANN LA ROCHE

Inventor： NING ROBERT YE-FONG ,  STERNBACH LEO HENRYK

IPC: C07D243/26 ,  C07D53/06

CPC classification number: Y10S514/906

Abstract: THE PRESENT INVENTION RELATES TO 7-HYDROXY LOWER ALKYL BENZODIAZEPINES, COMPOUNDS OF BIOLOGICAL INTEREST AS MUSCLE RELAXANTS, SEDATIVES AND ANTI-CONVULSANTS.

公开(公告)号：US3657436A

公开(公告)日：1972-04-18

申请号：US3657436D

申请日：1970-02-09

Applicant: HOFFMANN LA ROCHE

Inventor： BERGER LEO ,  GRUNBERG EMANUEL ,  STERNBACH LEO HENRYK ,  STEMPEL ARTHUR

IPC: A61K31/19 ,  A61K31/535 ,  A61K27/00

CPC classification number: A61K31/19 ,  A61K31/535

Abstract: ANTHRANILIC ACID DERIVATIVES WHICH ARE USEFUL IN COMBATTING VIRAL INFECTIONS CAUSED BY COL-SK AND COMPOSITIONS CONTAINING THESE DERIVATIVES.

公开(公告)号：US3644335A

公开(公告)日：1972-02-22

申请号：US3644335D

申请日：1968-05-07

Applicant: HOFFMANN LA ROCHE

Inventor： EARLEY JAMES VALENTINE ,  FRYER RODNEY IAN ,  STERNBACH LEO HENRYK

IPC: C07D215/38 ,  C07D241/44 ,  C07D53/06

CPC classification number: C07D215/38 ,  C07D241/44

Abstract: AMIDES ARE CONVERTED TO THEIR CORRESPONDING AMIDINES BY REACTING THE AMIDES WITH AN AMINO COMPOUND IN THE PRESENCE OF A NON-AQUEOUS ACID REAGENT, E.G., P-TOULENESULFONIC ACID OR TITANIUM TETRACHLORIDE. THIS PROCEDURE IS APPLICABLE TO PRIMARY AND SECONDARY AMINES. IN A SPECIFIC EMBODIMENT 1,4-BENZODIAZEPIN-2-ONES ARE DIRECTLY CONVERTED INTO 2-AMINO-1,4-BENZODIAZEPINES.

公开(公告)号：US3631089A

公开(公告)日：1971-12-28

申请号：US3631089D

申请日：1970-02-03

Applicant: HOFFMANN LA ROCHE

Inventor： REEDER EARL ,  STERNBACH LEO HENRYK

IPC: A61K31/00 ,  C07C329/20 ,  C07C331/08 ,  C07D281/10 ,  C07D513/04 ,  C07C154/00

CPC classification number: C07D513/04 ,  A61K31/00 ,  C07C329/20 ,  C07C331/08 ,  C07D281/10 ,  Y02P20/55 ,  Y10S514/906

Abstract: 2-ACETYL OR AROYL XANTHIC ACID PHENYL ESTERS (A). (A) IS PREPARED BY REACTING CORRESPONDING 2-AMINOPHENYL KETONE WITH NITROUS ACID; TREATING RESULTING PRODUCT WITH SALT OF FLUOROBORIC ACID TO OBTAIN CORRESPONMDING DIAZONIUM COMPOUND. DIAZONIUM COMPOUND IS CONVERTED TO (A) WITH ALKALI OR ALKALINE EARTH XANTHATE. (A) IS CONVERTIBLE INTO 1,4-BENZOTHIAZEPINES, USEFUL AS MUSCLE RELAXANTS AND ANTICONVULSANTS.

公开(公告)号：US3627754A

公开(公告)日：1971-12-14

申请号：US3627754D

申请日：1970-05-13

Applicant: HOFFMANN LA ROCHE

Inventor： NING ROBERT YE-FONG ,  STERNBACH LEO HENRYK

IPC: C07C233/00 ,  C07C271/22 ,  C07D243/16 ,  C07D243/24 ,  C07D243/26 ,  C07D53/06

CPC classification number: C07D243/24 ,  C07C233/00 ,  C07C247/00 ,  C07C271/22

Abstract: The present invention relates to processes for the preparation of 7-lower alkanoyl-1,4-benzodiazepin-2-ones utilizing ceric salts. The 7-lower alkanoyl benzodiazepin-2-ones are known to be useful as muscle relaxants, sedatives and anticonvulsants.