公开(公告)号：NO901399D0

公开(公告)日：1990-03-27

申请号：NO901399

申请日：1990-03-27

Applicant: HOFFMANN LA ROCHE

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

IPC: A61K31/16 ,  A61K31/27 ,  A61K31/38 ,  A61K31/381 ,  A61K31/415 ,  A61K31/425 ,  A61K31/426 ,  A61K31/4427 ,  A61K31/445 ,  A61K38/00 ,  A61K38/55 ,  A61P9/00 ,  A61P9/12 ,  C07C237/06 ,  C07C271/16 ,  C07C271/18 ,  C07C271/20 ,  C07D231/12 ,  C07D233/54 ,  C07D233/64 ,  C07D277/20 ,  C07D277/30 ,  C07D333/24 ,  C07D401/12 ,  C07D403/12 ,  C07K5/02 ,  C07K5/065 ,  C07C ,  C07D

Abstract: The compounds of the formula … … in which A, R , R , R and R have the meaning stated in Claim 1,… in the form of optically pure diastereomers, mixtures of diastereomers, 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：FI901490A0

公开(公告)日：1990-03-26

申请号：FI901490

申请日：1990-03-26

Applicant: HOFFMANN LA ROCHE

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

IPC: A61K31/16 ,  A61K31/27 ,  A61K31/38 ,  A61K31/381 ,  A61K31/415 ,  A61K31/425 ,  A61K31/426 ,  A61K31/4427 ,  A61K31/445 ,  A61K38/00 ,  A61K38/55 ,  A61P9/00 ,  A61P9/12 ,  C07C237/06 ,  C07C271/16 ,  C07C271/18 ,  C07C271/20 ,  C07D231/12 ,  C07D233/54 ,  C07D233/64 ,  C07D277/20 ,  C07D277/30 ,  C07D333/24 ,  C07D401/12 ,  C07D403/12 ,  C07K5/02 ,  C07K5/065 ,  C07D

Abstract: The compounds of the formula … … in which A, R , R , R and R have the meaning stated in Claim 1,… in the form of optically pure diastereomers, mixtures of diastereomers, 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：NO901033D0

公开(公告)日：1990-03-05

申请号：NO901033

申请日：1990-03-05

Applicant: HOFFMANN LA ROCHE

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

IPC: A61K31/195 ,  A61K31/27 ,  A61K31/335 ,  A61K31/357 ,  A61K31/42 ,  A61K31/421 ,  A61K31/47 ,  A61K31/472 ,  A61K38/00 ,  A61P31/12 ,  C07C211/08 ,  C07C211/36 ,  C07C229/30 ,  C07C233/88 ,  C07C237/22 ,  C07C251/36 ,  C07C271/22 ,  C07D213/40 ,  C07D217/06 ,  C07D233/26 ,  C07D263/04 ,  C07D295/12 ,  C07D295/13 ,  C07D295/20 ,  C07D295/205 ,  C07D317/30 ,  C07D405/12 ,  C07D413/12 ,  C07F7/18 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07K

公开(公告)号：PT89899A

公开(公告)日：1989-11-10

申请号：PT8989989

申请日：1989-03-03

Applicant: HOFFMANN LA ROCHE

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

IPC: A61K31/16 ,  A61K31/41 ,  A61K31/425 ,  A61K31/426 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K38/00 ,  A61P9/04 ,  A61P9/12 ,  C07C215/26 ,  C07C231/02 ,  C07C237/00 ,  C07C237/22 ,  C07C317/44 ,  C07C323/60 ,  C07D231/12 ,  C07D233/54 ,  C07D233/64 ,  C07D263/04 ,  C07D263/06 ,  C07D263/24 ,  C07D277/20 ,  C07D277/30 ,  C07D307/52 ,  C07D333/24 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12 ,  C07D413/12 ,  C07D417/06 ,  C07D417/12 ,  C07F9/6506 ,  C07K5/06 ,  C07K14/81 ,  C07C101/00 ,  C07D233/00 ,  C07D277/00 ,  A61K31/195

Abstract: The compounds of the formula I wherein A, R1, R2, R3, R4, R5 and R6 are as set forth above, are described. The compounds of formula I have an inhibitory activity on the natural enzyme renin and can accordingly be used in the form of pharmaceutical preparations for the control or prevention of high blood pressure and cardiac insufficiency.

公开(公告)号：FI891006A0

公开(公告)日：1989-03-02

申请号：FI891006

申请日：1989-03-02

Applicant: HOFFMANN LA ROCHE

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

IPC: A61K31/16 ,  A61K31/41 ,  A61K31/425 ,  A61K31/426 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K38/00 ,  A61P9/04 ,  A61P9/12 ,  C07C215/26 ,  C07C231/02 ,  C07C237/00 ,  C07C237/22 ,  C07C317/44 ,  C07C323/60 ,  C07D231/12 ,  C07D233/54 ,  C07D233/64 ,  C07D263/04 ,  C07D263/06 ,  C07D263/24 ,  C07D277/20 ,  C07D277/30 ,  C07D307/52 ,  C07D333/24 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12 ,  C07D413/12 ,  C07D417/06 ,  C07D417/12 ,  C07F9/6506 ,  C07K5/06 ,  C07K14/81 ,  C07K

Abstract: The compounds of the formula I wherein A, R1, R2, R3, R4, R5 and R6 are as set forth above, are described. The compounds of formula I have an inhibitory activity on the natural enzyme renin and can accordingly be used in the form of pharmaceutical preparations for the control or prevention of high blood pressure and cardiac insufficiency.

公开(公告)号：NO157374C

公开(公告)日：1988-03-09

申请号：NO820125

申请日：1982-01-15

Applicant: HOFFMANN LA ROCHE

Inventor： ASCHWANDEN WERNER ,  PFISTER RUDOLF ,  BRANCA QUIRICO ,  KYBURZ EMILIO

IPC: C07D295/02 ,  A61K31/00 ,  A61P37/08 ,  C07C1/00 ,  C07C13/547 ,  C07C17/00 ,  C07C17/16 ,  C07C17/26 ,  C07C22/04 ,  C07C27/00 ,  C07C33/34 ,  C07C35/37 ,  C07C67/00 ,  C07C301/00 ,  C07C303/22 ,  C07C303/32 ,  C07C309/63 ,  C07D207/04 ,  C07D295/03 ,  C07D207/06

Abstract: 1-[2-(4,5,10,11-Tetrahydro-1H-dibenzo[a,d]cyclohepten-5-yl)ethyl]pyrro lidine of the formula I and its pharmaceutically acceptable acid addition salts, prepared through various intermediates, are described. The compounds have valuable histamine-H1 antagonistic properties and are suitable for the control or prevention of allergic reactions,such as, urticaria, hay fever, anaphylaxis and over-sensitivity to medicaments.

公开(公告)号：AU545357B2

公开(公告)日：1985-07-11

申请号：AU6681881

申请日：1981-02-02

Applicant: HOFFMANN LA ROCHE

Inventor： BRANCA QUIRICO ,  FISCHLI ALBERT EDUARD ,  SZENTE ANDRE

IPC: A61K31/55 ,  A61P1/16 ,  A61P9/04 ,  A61P9/12 ,  C07D243/24 ,  C07D487/04

Abstract: There are presented compounds of the formula I wherein R1 is a hydrogen atom or a lower alkyl group, R2 and R3 each are a hydrogen atom or a lower alkyl group, R4 is a halogen atom and either R5 is a hydrogen atom or a lower alkyl group and R6 is a lower alkyl or lower hydroxyalkyl group or R5 and R6 together with the nitrogen atom to which they are attached are a 3-membered to 7-membered heterocycle, and pharmaceutically acceptable acid addition salts thereof. The compounds and their salts are novel and possess valuable pharmacodynamic properties.

公开(公告)号：HU184981B

公开(公告)日：1984-11-28

申请号：HU7382

申请日：1982-01-12

Applicant: HOFFMANN LA ROCHE

Inventor： ASCHWANDER WERNER ,  BRANCA QUIRICO ,  KYBURZ EMILIO ,  PFISTER RUDOLF

IPC: C07D295/02 ,  A61K31/00 ,  A61P37/08 ,  C07C1/00 ,  C07C13/547 ,  C07C17/00 ,  C07C17/16 ,  C07C17/26 ,  C07C22/04 ,  C07C27/00 ,  C07C33/34 ,  C07C35/37 ,  C07C67/00 ,  C07C301/00 ,  C07C303/22 ,  C07C303/32 ,  C07C309/63 ,  C07D207/04 ,  C07D295/03

Abstract: 1-[2-(4,5,10,11-Tetrahydro-1H-dibenzo[a,d]cyclohepten-5-yl)ethyl]pyrro lidine of the formula I and its pharmaceutically acceptable acid addition salts, prepared through various intermediates, are described. The compounds have valuable histamine-H1 antagonistic properties and are suitable for the control or prevention of allergic reactions,such as, urticaria, hay fever, anaphylaxis and over-sensitivity to medicaments.

公开(公告)号：CA1152066A

公开(公告)日：1983-08-16

申请号：CA364874

申请日：1980-11-18

Applicant: HOFFMANN LA ROCHE

Inventor： BRANCA QUIRICO ,  FISCHLI ALBERT E ,  SZENTE ANDRE

IPC: A61K31/55 ,  A61P1/16 ,  A61P9/04 ,  A61P9/12 ,  C07D243/24 ,  C07D487/04

Abstract: RAN 4008/310 The novel compounds of the formula I wherein R1 represents a hydrogen atom or a lower alkyl group, R2 and R3 each represent a hydrogen atom or a lower alkyl group, R4 represents a halogen atom and either R5 represents a hydrogen atom or a lower alkyl group and R6 represents a lower alkyl or lower hydroxyalkyl group or R5 and R6 together with the nitrogen atom to which they are attached represent a 3-membered to 7-membered heterocycle, and their pharmaceutically acceptable acid addition salts have aldosterone-antagonistic properties and are therefore suitable for the control or prevention of heart failure, hepatic ascites, primary aldosteronism and idiopathic hypertension. They can be manufactured according to various methods starting from partially novel starting materials and can be brought into galenical administration forms.

公开(公告)号：ZA815112B

公开(公告)日：1982-08-25

申请号：ZA815112

申请日：1981-07-24

Applicant: HOFFMANN LA ROCHE

Inventor： BRANCA QUIRICO ,  FISCHLI ALBERT EDUARD ,  SZENTE ANDRE

IPC: A61K31/135 ,  A61K31/15 ,  A61K31/195 ,  A61P5/38 ,  C07C67/00 ,  C07C239/00 ,  C07C251/48 ,  C07D243/24 ,  C07C ,  A61K

Abstract: There is presented novel benzophenone derivatives of the formula I wherein R1 is hydrogen or lower alkyl, R2 is hydrogen or aminoacetyl, R3 is hydrogen or lower alkyl, R4 is hydrogen or halogen, R5 is hydrogen, amino, nitro or a group of the formula R3-ON=C(R6)-and R6 is lower alkyl, with the proviso that R5 is a group of the formula H-ON=C(R6)-when R2 and R3 are both hydrogen, and their pharmaceutically acceptable acid addition salts. The compounds exhibit aldosterone-antagonistic properties and are accordingly suitable for the control or prevention of heart failure, hepatic ascites, primary aldosteronism and idiopathic hypertension.