公开(公告)号：JPS63139171A

公开(公告)日：1988-06-10

申请号：JP28228787

申请日：1987-11-10

Applicant: HOFFMANN LA ROCHE

Inventor： BRANCA QUIRICO ,  JAUNIN ROLAND ,  MAERKI HANS P ,  MARTI FRAENZI ,  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

公开(公告)号：US3441595A

公开(公告)日：1969-04-29

申请号：US3441595D

申请日：1966-02-10

Applicant: HOFFMANN LA ROCHE

Inventor： JAUNIN ROLAND ,  ZELLER PAUL

IPC: A61K31/135 ,  A61K31/15 ,  C07C20060101 ,  C07C271/06 ,  C07C125/06 ,  A61K27/00 ,  C07C109/02

CPC classification number: C07C243/00

公开(公告)号：US3459799A

公开(公告)日：1969-08-05

申请号：US3459799D

申请日：1964-03-09

Applicant: HOFFMANN LA ROCHE

Inventor： GUTMANN HUGO ,  JAUNIN ROLAND ,  KAISER ADO ,  ZELLER PAUL

IPC: A61K31/15 ,  C07C233/00 ,  C07C109/04

CPC classification number: C07C243/00

公开(公告)号：US3441594A

公开(公告)日：1969-04-29

申请号：US3441594D

申请日：1966-02-10

Applicant: HOFFMANN LA ROCHE

Inventor： JAUNIN ROLAND ,  ZELLER PAUL

IPC: A61K31/15 ,  C07C20060101 ,  C07C127/16 ,  C07C109/02 ,  C07C125/06

CPC classification number: C07C243/00

公开(公告)号：BG60937B2

公开(公告)日：1996-06-28

申请号：BG9846994

申请日：1994-02-14

Applicant: HOFFMANN LA ROCHE

Inventor： BRANCA QUIRICO ,  JAUNIN ROLAND ,  MAERKI HANS P ,  MARTI FRAENZI ,  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

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：HK110494A

公开(公告)日：1994-10-21

申请号：HK110494

申请日：1994-10-12

Applicant: HOFFMANN LA ROCHE

Inventor： BRANCA QUIRICO ,  JAUNIN ROLAND ,  MAERKI HANS P ,  MARTI FRAENZI ,  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

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：AU8038491A

公开(公告)日：1992-01-23

申请号：AU8038491

申请日：1991-07-11

Applicant: HOFFMANN LA ROCHE

Inventor： JAUNIN ROLAND

IPC: A61K31/52 ,  A61K31/522 ,  A61P9/10 ,  A61P9/12 ,  A61P43/00 ,  C07D473/00 ,  C07D473/04 ,  C07D473/16 ,  C07D473/18 ,  C07D473/20 ,  C07D473/22 ,  C07D473/24 ,  C07D473/30 ,  C07D473/32 ,  C07D473/34 ,  C07D473/38

Abstract: The compounds of the formula in which R , R , R , R , R and R are as defined in Claim 1, inhibit the angiotensin-II receptors and can therefore be used in the form of pharmaceutical preparations in the control, or prevention, of hypertension and arteriosclerosis. They can be prepared by N-biphenylmethylation of corresponding unsubstituted purine derivatives by methods known per se.

公开(公告)号：CA2044806A1

公开(公告)日：1992-01-19

申请号：CA2044806

申请日：1991-06-17

Applicant: HOFFMANN LA ROCHE

Inventor： JAUNIN ROLAND

IPC: A61K31/52 ,  A61K31/522 ,  A61P9/10 ,  A61P9/12 ,  A61P43/00 ,  C07D473/00 ,  C07D473/04 ,  C07D473/16 ,  C07D473/18 ,  C07D473/20 ,  C07D473/22 ,  C07D473/24 ,  C07D473/30 ,  C07D473/32 ,  C07D473/34

Abstract: RAN 4019/1 12 Compounds of the formula wherein R1, R2, R3, R4, R5 and R6 have the significance given in claim 1, inhibit angiotensin II receptors and can accordingly be used in the form of pharmaceutical preparations for the control or prevention of high blood pressure and arteriosclerosis. They can be manufactured by N-biphenylmethylating corresponding unsubstituted purine derivatives according to methods 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：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.