公开(公告)号：US3575983A

公开(公告)日：1971-04-20

申请号：US3575983D

申请日：1967-08-30

Applicant: HOFFMANN LA ROCHE

Inventor： LEIMGRUBER WILLY ,  SCHENKER FAUSTO EUGENIO

IPC: C07D217/02 ,  C07D217/04 ,  C07D217/10 ,  C07D35/28

CPC classification number: C07D217/04 ,  C07D217/02 ,  C07D217/10

Abstract: NOVEL PHARMACOLOGICALLY ACTIVE 1,2,3,4-TETRAHYDRO-8ISOQUINOLINOL, 1- AND/OR 2-(LOWER ALKYL)-1,2,3,4-TETRAHYDRO-8-ISOQUINOLINOLS AND INTERMEDIATES THEREFOR, ARE PREPARED UTILIZING, FOR EXAMPLE, 8-ISOQUINOLINOL AS A STARTING MATERIAL. THE PHARMACOLOGICALLY ACTIVE COMPOUNDS OF THE INVENTION ARE USEFUL AS HYPOTENSIVE AGENTS.

公开(公告)号：US3562280A

公开(公告)日：1971-02-09

申请号：US3562280D

申请日：1967-08-30

Applicant: HOFFMANN LA ROCHE

Inventor： LEIMGRUBER WILLY ,  SCHENKER FAUSTO EUGENIO

IPC: A61K31/00 ,  C07D217/02 ,  C07D217/04 ,  C07D217/06 ,  C07D217/10 ,  C07D35/10

CPC classification number: A61K31/00 ,  C07D217/02 ,  C07D217/04 ,  C07D217/06 ,  C07D217/10 ,  Y02P20/55

Abstract: NOVEL PHARMACOLOGICALLY ACTIVE 8-(LOWER ALKOXY)-1,23,4-TETRAHYDROISOQUINOLINES, 8-(LOWER ALKOXY)-1 AND/OR 2(LOWER ALKYL)-1,2,3,4-TETRAHYDROISOQUINOLINES AND INTERMEDIATES THEREFOR, ARE PREPARED UTILIZING, FOR EXAMPLE, 8ISOQUINOLINOL AS A STARTING MATERIAL. THE PHARMACOLOGICALLY ACTIVE COMPOUNDS OF THE INVENTION ARE USEFUL AS HYPOTENSIVE AGENTS.

公开(公告)号：US3501478A

公开(公告)日：1970-03-17

申请号：US3501478D

申请日：1967-03-29

Applicant: HOFFMANN LA ROCHE

Inventor： GRETHE GUENTER ,  SCHENKER FAUSTO EUGENIO

IPC: C07D217/04 ,  C07D217/10 ,  A61K27/00 ,  C07D5/10

CPC classification number: C07D217/04 ,  C07D217/10

公开(公告)号：US3903133A

公开(公告)日：1975-09-02

申请号：US41832873

申请日：1973-11-23

Applicant: HOFFMANN LA ROCHE

Inventor： BERGER LEO ,  LEIMGRUBER WILLY ,  SCHENKER FAUSTO EUGENIO

IPC: C07D333/50 ,  C07C69/74

CPC classification number: C07D333/50

Abstract: Tricyclic compounds of the formula

WHEREIN R1 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkylthio, trifluoromethyl, cyano, carbamoyl, carboxy, lower alkoxy carbonyl, nitro, amino, mono-lower alkylamino, dilower alkylamino, acyl, acylamido, sulfamoyl, di-lower alkylsulfamoyl, or difluoromethylsulfonyl; R2 is hydrogen, lower alkyl, amino-lower alkyl, mono-lower alkyl-amino-lower alkyl, or di-lower alkylamino-lower alkyl; n and r are independently 1 or 2; and X is oxygen or sulfur, prepared, inter alia, from the correspondingly substituted phenol or thiophenol and haloketocyclohexane or pentane carboxylic acid ester, are described. The end products are useful as anti-inflammatory and anti-rheumatic agents.

Abstract translation: 下式的三环化合物，其中R 1为氢，卤素，低级烷基，低级烷氧基，低级烷硫基，三氟甲基，氰基，氨基甲酰基，羧基，低级烷氧基羰基，硝基，氨基，单低级烷基氨基，二低级烷基氨基，酰基，酰基酰氨基 ，氨磺酰基，二低级烷基氨磺酰基或二氟甲基磺酰基; R2是氢，低级烷基，氨基 - 低级烷基，单低级烷基 - 氨基 - 低级烷基或二 - 低级烷基氨基 - 低级烷基; n和r独立地为1或2; 并且X是氧或硫，特别是由相应取代的苯酚或苯硫酚和卤代环己烷或戊烷羧酸酯制备。 最终产品可用作抗炎和抗风湿剂。

公开(公告)号：US3661913A

公开(公告)日：1972-05-09

申请号：US3661913D

申请日：1970-09-09

Applicant: HOFFMANN LA ROCHE

Inventor： LEIMGRUBER WILLY ,  SCHENKER FAUSTO EUGENIO

IPC: A61K31/00 ,  C07D217/02 ,  C07D217/04 ,  C07D217/06 ,  C07D217/10 ,  C07D35/10

CPC classification number: A61K31/00 ,  C07D217/02 ,  C07D217/04 ,  C07D217/06 ,  C07D217/10

Abstract: NOVEL PHARMACOLOGICALLY ACTIVE 8-(LOWER ALKOXY)-1,2, 3,4-TETRAHYDROISOQUINOLINES, 8-(LOWER ALKOXY)-1 AND/OR 2-(LOWER ALKYL)-1,2,3,4-TETRAHYDROISOQUINOLINES AND INTERMEDIATES THEREFOR, ARE PREPARED UTILIZING, FOR EXAMPLE, 8ISOQUINOLINOL AS A STARTING MATERIAL. THE PHARMACOLOGICALLY ACTIVE COMPOUNDS OF THE INVENTION ARE USEFUL AS HYPOTENSIVE AGENTS.

公开(公告)号：US3523941A

公开(公告)日：1970-08-11

申请号：US3523941D

申请日：1967-03-06

Applicant: HOFFMANN LA ROCHE

Inventor： LEIMGRUBER WILLY ,  SCHENKER FAUSTO EUGENIO

IPC: C07D487/04 ,  C07D27/30

CPC classification number: C07D487/04 ,  Y10S514/87 ,  Y10S514/96