公开(公告)号：ZA906856B

公开(公告)日：1991-06-26

申请号：ZA906856

申请日：1990-08-28

Applicant: HOFFMANN LA ROCHE

Inventor： BRANCA QUIRICO ,  QUIRICO BRANCA ,  NEIDHART WERNER ,  WERNER NEIDHART ,  RAMUZ HENRI ,  HENRI RAMUZ ,  STADLER HEINZ ,  HEINZ STADLER ,  WOSTL WOLFGANG ,  WOLFGANG WOSTL

IPC: A61K20060101 ,  C07C20060101 ,  C07D20060101 ,  C07F20060101 ,  C07K20060101 ,  C07C ,  A61K ,  C07D ,  C07F ,  C07K

公开(公告)号：AU6136090A

公开(公告)日：1991-03-07

申请号：AU6136090

申请日：1990-08-27

Applicant: HOFFMANN LA ROCHE

Inventor： BRANCA QUIRICO ,  NEIDHART WERNER ,  RAMUZ HENRI ,  STADLER HEINZ ,  WOSTL WOLFGANG

IPC: C12N9/99 ,  A61K31/195 ,  A61K31/38 ,  A61K31/381 ,  A61K31/415 ,  A61K31/425 ,  A61K31/426 ,  A61K31/428 ,  A61K31/435 ,  A61K31/54 ,  A61K38/00 ,  A61K38/55 ,  A61P9/00 ,  A61P9/12 ,  A61P43/00 ,  C07C237/06 ,  C07C237/08 ,  C07C237/10 ,  C07D207/34 ,  C07D231/12 ,  C07D233/64 ,  C07D233/68 ,  C07D233/90 ,  C07D277/20 ,  C07D277/30 ,  C07D277/68 ,  C07D333/24 ,  C07D401/04 ,  C07D403/04 ,  C07D413/04 ,  C07D417/04 ,  C07D453/02 ,  C07F9/6512 ,  C07K1/113 ,  C07K5/06 ,  C07K5/065 ,  C07K14/81 ,  C07C323/60 ,  C07D409/12 ,  C07D403/12 ,  C07D417/12 ,  C07D401/12 ,  C07D405/12 ,  A61K31/535 ,  A61K31/47 ,  A61K31/445

Abstract: The compounds of the formula in which A, R , R , R , R , R , R , R and R have the meaning given in Claim 1, in the form of optically pure diastereomers, diastereomer mixtures, diastereomeric racemates or mixtures of diastereomeric racemates and pharmaceutically utilisable salts thereof inhibit the action of the natural enzyme rennin and can therefore be used in the form of pharmaceutical preparations in the control or prevention of high blood pressure and cardiac insufficiency. They can be prepared by various processes which are known per se.

公开(公告)号：ZA901498B

公开(公告)日：1990-11-28

申请号：ZA901498

申请日：1990-02-27

Applicant: HOFFMANN LA ROCHE

Inventor： BRANCA QUIRICO ,  QUIRICO BRANCA ,  EDENHOFER ALBRECHT ,  ALBRECHT EDENHOFER ,  MERRETT JOHN HERBERT ,  JOHN HERBERT MERRETT ,  MARTIN JOSEPH ARMSTRONG ,  JOSEPH ARMSTRONG MARTIN ,  NEIDHART WERNER ,  WERNER NEIDHART

IPC: A61K20060101 ,  A61K31/16 ,  C07C20060101 ,  C07C237/22 ,  C07C271/22 ,  C07D213/40 ,  C07D217/06 ,  C07D233/24 ,  C07D263/04 ,  C07D295/20 ,  C07D317/20 ,  C07F7/18 ,  C07K5/02 ,  A61K ,  C07C

公开(公告)号：ZA9001498B

公开(公告)日：1990-11-28

申请号：ZA9001498

申请日：1990-02-27

Applicant: HOFFMANN LA ROCHE

Inventor： BRANCA QUIRICO ,  QUIRICO BRANCA ,  EDENHOFER ALBRECHT ,  ALBRECHT EDENHOFER ,  MERRETT JOHN HERBERT ,  JOHN HERBERT MERRETT ,  MARTIN JOSEPH ARMSTRONG ,  JOSEPH ARMSTRONG MARTIN ,  NEIDHART WERNER ,  WERNER NEIDHART

IPC: A61K20060101 ,  A61K31/16 ,  C07C20060101 ,  C07C237/22 ,  C07C271/22 ,  C07D213/40 ,  C07D217/06 ,  C07D233/24 ,  C07D263/04 ,  C07D295/20 ,  C07D317/20 ,  C07F7/18 ,  C07K5/02 ,  A61K ,  C07C

公开(公告)号：HUT53598A

公开(公告)日：1990-11-28

申请号：HU203790

申请日：1990-04-02

Applicant: HOFFMANN LA ROCHE

Inventor： BRANCA QUIRICO ,  MARKI HANS PETER ,  NEIDHART WERNER ,  RAMUZ HENRI ,  WOSTL WOLFGANG

IPC: A61K38/00 ,  A61P9/04 ,  A61P9/12 ,  C07C237/06 ,  C07C271/20 ,  C07C279/12 ,  C07D231/12 ,  C07D233/54 ,  C07D233/58 ,  C07D233/64 ,  A61K31/16 ,  C07D277/22 ,  C07D333/10 ,  C07D401/12 ,  C07K5/02 ,  C07K5/065 ,  C07K5/097 ,  C07C237/08 ,  C07C323/57 ,  C07D213/00 ,  C07D263/00 ,  C07D307/00 ,  C07K5/00 ,  A61K31/095 ,  A61K31/33 ,  A61K37/02

Abstract: The compounds of the formula I wherein A, R1, R2, R3 and R4 have the significance given in claim 1, in the form of optically pure diastereomers, mixtures of diastereomers, diastereomeric racemates or mixtures of diastereomeric racemates as well as pharmaceutically usable salts thereof inhibit the activity of the natural enzyme renin and can accordingly be used in the form of pharmaceutical preparations in the control or prevention of high blood pressure and cardiac insufficiency.

公开(公告)号：PT93648A

公开(公告)日：1990-11-20

申请号：PT9364890

申请日：1990-04-03

Applicant: HOFFMANN LA ROCHE

Inventor： BRANCA QUIRICO ,  NEIDHART WERNER ,  RAMUZ HENRI ,  WOSTL WOLFGANG ,  MARKI HANS PETER ,  EDENHOFER ALBRECHT

IPC: C07D263/08 ,  A61K38/00 ,  A61K38/55 ,  A61P9/00 ,  A61P9/12 ,  C07C237/04 ,  C07C237/08 ,  C07D233/54 ,  C07D233/64 ,  C07K1/06 ,  C07K1/113 ,  C07K5/06 ,  C07K5/065 ,  C07K5/08 ,  C07K5/097 ,  C07K14/81 ,  C07C229/00 ,  C07D233/00 ,  A61K31/195

Abstract: The compounds of the formula in which A, R , R , R , R , R and n have the meaning stated in Claim 1, in the form of optically pure diastereomers, diastereomer mixtures, diastereomeric racemates or mixtures of diastereomeric racemates, and pharmaceutically utilisable salts thereof inhibit the action of the natural enzyme renin and can accordingly be used in the form of pharmaceutical products for controlling or preventing high blood pressure and heart failure. They can be prepared by various processes known per se.

公开(公告)号：PT86130B

公开(公告)日：1990-11-20

申请号：PT8613087

申请日：1987-11-13

Applicant: HOFFMANN LA ROCHE

Inventor： BRANCA QUIRICO ,  RAMUZ HENRI ,  MARKI HANS PETER ,  JAUNIN ROLAND ,  MARTI FRANZI

IPC: A61K31/415 ,  A61K31/4184 ,  A61K31/425 ,  A61K31/428 ,  A61K31/44 ,  A61K31/55 ,  A61K31/551 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  C07D233/54 ,  C07D233/64 ,  C07D235/14 ,  C07D235/26 ,  C07D243/14 ,  C07D277/62 ,  C07D277/64 ,  C07D401/06 ,  C07D471/04 ,  C07D487/04 ,  C07D521/00

Abstract: Compounds of the formula I wherein R is lower-alkyl, R1 is halogen, R2 is C1-C12-alkyl, R3 is hydroxy, lower-alkoxy, lower-alkyl-carbonyloxy, lower-alkoxy-lower-alkylcarbonoyloxy, lower-alkylaminocarbonyloxy, arylaminocarbonyloxy or aryl-lower alkylaminocarbonyloxy, X is C1-C18-alkylene which optionally can be interrupted by 1,4-phenylene or interrupted or lengthened by 1,4-cyclohexylene, A is di- or tri-substituted 2-imidazolyl attached via an ethylene group or a substituted or unsubstituted heterocycle selected from the group consisting of benzimidazolyl, benzimidazolonyl, imidazo[4,5-c]pyridinyl, imidazo[4,5-c]pyridinonyl, benzthiazolyl, benzodiazepine-2,5-dion-1-yl and pyrrolo[2,1-c]-[1,4]benzodiazepine-5,11-dion-10-yl and n is the number 0 or 1, in the form of racemates and optical antipodes, as well as N-oxides and pharmaceutically usable acid addition salts thereof. The compounds of formual I have a pronounced calcium-antagonistic and anti-arrhythmic activity and can accordingly be used as medicaments, especially for the control or prevention of angina pectoris, ischaemia, arrhythmias, high blood pressure and cardiac insufficiency.

公开(公告)号：FI904360A0

公开(公告)日：1990-09-04

申请号：FI904360

申请日：1990-09-04

Applicant: HOFFMANN LA ROCHE

Inventor： BRANCA QUIRICO ,  NEIDHART WERNER ,  RAMUZ HENRI ,  STADLER HEINZ ,  WOSTL WOLFGANG

IPC: C12N9/99 ,  A61K31/195 ,  A61K31/38 ,  A61K31/381 ,  A61K31/415 ,  A61K31/425 ,  A61K31/426 ,  A61K31/428 ,  A61K31/435 ,  A61K31/54 ,  A61K38/00 ,  A61K38/55 ,  A61P9/00 ,  A61P9/12 ,  A61P43/00 ,  C07C237/06 ,  C07C237/08 ,  C07C237/10 ,  C07D207/34 ,  C07D231/12 ,  C07D233/64 ,  C07D233/68 ,  C07D233/90 ,  C07D277/20 ,  C07D277/30 ,  C07D277/68 ,  C07D333/24 ,  C07D401/04 ,  C07D403/04 ,  C07D413/04 ,  C07D417/04 ,  C07D453/02 ,  C07F9/6512 ,  C07K1/113 ,  C07K5/06 ,  C07K5/065 ,  C07K14/81 ,  C07D

Abstract: The compounds of the formula in which A, R , R , R , R , R , R , R and R have the meaning given in Claim 1, in the form of optically pure diastereomers, diastereomer mixtures, diastereomeric racemates or mixtures of diastereomeric racemates and pharmaceutically utilisable salts thereof inhibit the action of the natural enzyme rennin and can therefore be used in the form of pharmaceutical preparations in the control or prevention of high blood pressure and cardiac insufficiency. They can be prepared by various processes which are known per se.

公开(公告)号：AU600769B2

公开(公告)日：1990-08-23

申请号：AU8090987

申请日：1987-11-09

Applicant: HOFFMANN LA ROCHE

Inventor： BRANCA QUIRICO ,  JAUNIN ROLAND ,  MARKI HANS PETER ,  MARTI FRANZI ,  RAMUZ HENRI

IPC: A61K31/415 ,  A61K31/4184 ,  A61K31/425 ,  A61K31/428 ,  A61K31/44 ,  A61K31/55 ,  A61K31/551 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  C07D233/54 ,  C07D233/64 ,  C07D235/14 ,  C07D235/26 ,  C07D243/14 ,  C07D277/62 ,  C07D277/64 ,  C07D401/06 ,  C07D471/04 ,  C07D487/04 ,  C07D521/00 ,  C07D233/61

Abstract: Compounds of the formula I wherein R is lower-alkyl, R1 is halogen, R2 is C1-C12-alkyl, R3 is hydroxy, lower-alkoxy, lower-alkyl-carbonyloxy, lower-alkoxy-lower-alkylcarbonoyloxy, lower-alkylaminocarbonyloxy, arylaminocarbonyloxy or aryl-lower alkylaminocarbonyloxy, X is C1-C18-alkylene which optionally can be interrupted by 1,4-phenylene or interrupted or lengthened by 1,4-cyclohexylene, A is di- or tri-substituted 2-imidazolyl attached via an ethylene group or a substituted or unsubstituted heterocycle selected from the group consisting of benzimidazolyl, benzimidazolonyl, imidazo[4,5-c]pyridinyl, imidazo[4,5-c]pyridinonyl, benzthiazolyl, benzodiazepine-2,5-dion-1-yl and pyrrolo[2,1-c]-[1,4]benzodiazepine-5,11-dion-10-yl and n is the number 0 or 1, in the form of racemates and optical antipodes, as well as N-oxides and pharmaceutically usable acid addition salts thereof. The compounds of formual I have a pronounced calcium-antagonistic and anti-arrhythmic activity and can accordingly be used as medicaments, especially for the control or prevention of angina pectoris, ischaemia, arrhythmias, high blood pressure and cardiac insufficiency.

公开(公告)号：NO901533D0

公开(公告)日：1990-04-04

申请号：NO901533

申请日：1990-04-04

Applicant: HOFFMANN LA ROCHE

Inventor： BRANCA QUIRICO ,  MAERKI HANS PETER ,  NEIDHART WERNER ,  RAMUZ HENRI ,  WOSTL WOLFGANG

IPC: A61K38/00 ,  A61P9/04 ,  A61K31/16 ,  A61P9/12 ,  C07C237/06 ,  C07C271/20 ,  C07C279/12 ,  C07D231/12 ,  C07D233/54 ,  C07D233/58 ,  C07D233/64 ,  C07D277/22 ,  C07D333/10 ,  C07D401/12 ,  C07K5/02 ,  C07K5/065 ,  C07K5/097 ,  C07K5/08 ,  C07K5/06

Abstract: The compounds of the formula I wherein A, R1, R2, R3 and R4 have the significance given in claim 1, in the form of optically pure diastereomers, mixtures of diastereomers, diastereomeric racemates or mixtures of diastereomeric racemates as well as pharmaceutically usable salts thereof inhibit the activity of the natural enzyme renin and can accordingly be used in the form of pharmaceutical preparations in the control or prevention of high blood pressure and cardiac insufficiency.