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公开(公告)号:SE7811194L
公开(公告)日:1979-04-29
申请号:SE7811194
申请日:1978-10-27
Applicant: HOFFMANN LA ROCHE
Inventor: BERNAUER K , LINK H , STOHLER H
IPC: A61K31/415 , A61K31/4166 , A61P5/00 , A61P33/10 , C07D233/66 , C07D233/72 , C07D233/74 , C07D233/88
Abstract: Imidazolidine derivatives of the formula I wherein X is oxygen or imino and R is one of the groups their preparation, use as antiandrogenically or schistosomicidally active agents, and corresponding pharmaceutical preparations, are described.
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公开(公告)号:NZ206317A
公开(公告)日:1987-06-30
申请号:NZ20631783
申请日:1983-11-18
Applicant: HOFFMANN LA ROCHE
Inventor: BROMBACHER U , LINK H , MONTAVON M
IPC: A61K31/00 , A61K31/435 , A61P33/10 , C07D219/06 , C07D219/10 , C07D417/12 , C07D417/14 , C07D219/00 , C07D277/00 , C07D417/00 , A61K31/645
Abstract: For the Contracting States BE CH DE FR GB IT LI LU NL SE 1. Acridanone derivatives of the general formula see diagramm : EP0110298,P20,F1 wherein the dotted line signifies an optional bond, R**1 signifies hydrogen, halogen or nitro, R**2 signifies hydrogen or lower alkyl, one of the symbols R**3 and R**4 signifies hydrogen or lower alkyl and the other together with R signifies an additional bond, A signifies lower alkylene, R**5 signifies a 5-membered, nitrogen-containig, optionally lower alkyl-substituted aromatic heterocycle, amino or a group see diagramm : EP0110298,P20,F2 or see diagramm : EP0110298,P20,F3 the symbol see diagramm : EP0110298,P20,F4 signifies a 5- or 6-membered, optionally lower-alkyl substituted saturated heterocycle which can contain as a ring member an oxygen or sulphur atom or the group >NH ou >N(B)n -A**1-R**6, B signifies the group -CO-, -COO- or -SO2 -, n signifies the number 0 or 1, A**1 signifies lower alkylene, R**6 signifies hydrogen, amino, lower alkylamino or di(lower alkyl)amino and R**7 signifies hydrogen or lower alkyl, and the residues denoted as lower contain 1 to 7 carbon atoms, and pharmaceutically acceptable acid addition salts thereof. For the Contracting State AT 1. A process for the manufacture of acridanone derivatives of the general formula see diagramm : EP0110298,P22,F1 wherein the dotted line signifies an optional bond, R**1 signifies hydrogen, halogen or nitro, R**2 signifies hydrogen or lower alkyl, one of the symbols R**3 and R**4 signifies hydrogen or lower alkyl and the other together with R signifies an additional bond, A signifies lower alkylene, R**5 signifies a 5-membered, nitrogen-containing, optionally lower alkyl-substituted aromatic heterocycle, amino or a group see diagramm : EP0110298,P23,F2 or see diagramm : EP0110298,P23,F3 the symbol see diagramm : EP0110298,P23,F4 signifies a 5- or 6-membered, optionally lower-alkyl substituted saturated heterocycle which can contain as a ring member an oxygen or sulphur atom or the group >NH ou >N(B)n -A**1-R**6, B signifies the group -CO-, -COO- or -SO2 -, n signifies the number 0 or 1, A**1 signifies lower alkylene, R**6 signifies hydrogen, amino, lower alkylamino or di(lower alkyl)amino and R**7 signifies hydrogen or lower alkyl, and the residues denoted as lower contains 1 to 7 carbon atoms, and pharmaceutically acceptable acid addition salts thereof, characterized by a) cyclizing a compound of the general formula see diagramm : EP0110298,P23,F5 wherein one of the symbols R**31 and R**41 signifies hydrogen or lower alkyl and the other signifies hydrogen, R**42 signifies hydrogen or lower alkyl, R**51 signifies a residue R**5, but does not contain a primary or secondary basic amino group, and X' signifies a leaving group, and R**1, R**2 and R**5 have the above significance, b) reacting a compound of the general formula see diagramm : EP0110298,P23,F6 wherein A, R**1, R**42 and R**51 have the above significance, with a compound of the general formula see diagramm : EP0110298,P23,F7 wherein X" signifies a leaving group and the dotted line and R**2 have the above significance, or c) reacting a compound of the general formula see diagramm : EP0110298,P23,F8 wherein Y(anion) signifies an anion and X signifies a leaving group, and A, R**1 and R**51 have the above significance, with a compound of the general formula see diagramm : EP0110298,P23,F9 wherein the dotted line, R, R**2, R**3 and R**4 have the above significance, or d) cleaving off the N-protecting group in a compound of the general formula see diagramm : EP0110298,P24,F10 wherein R**8 signifies a residue R**5 which contains a primary or secondary basic amino group blocked by a N-protecting group and the dotted line, R, R**1, R**2, R**3 and R**4 have the above significance, and e) if desired, converting a compound of formula I obtained into a pharmaceutically acceptable acid addition salt.
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公开(公告)号:NZ188720A
公开(公告)日:1984-12-14
申请号:NZ18872078
申请日:1978-10-24
Applicant: HOFFMANN LA ROCHE
Inventor: BERNAUER K , LINK H , STOHLER H
IPC: A61K31/215 , A61K31/22 , A61K31/24 , A61P5/00 , A61P33/00 , C07C67/00 , C07C239/00 , C07C275/42 , C07D233/66 , C07D233/72 , C07D233/88 , C07C127/00 , C07D233/00 , A61K31/17
Abstract: Imidazolidine derivatives, as well as processes for their preparation, which have antiandrogenic and schistosomicidal activity.
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公开(公告)号:NZ188721A
公开(公告)日:1984-11-09
申请号:NZ18872178
申请日:1978-10-24
Applicant: HOFFMANN LA ROCHE
Inventor: BERNAUER K , LINK H , STOHLER H
IPC: A61K31/415 , A61K31/4166 , A61P5/00 , A61P33/10 , C07D233/66 , C07D233/72 , C07D233/74 , C07D233/88 , C07D233/00
Abstract: Imidazolidine derivatives of the formula I wherein X is oxygen or imino and R is one of the groups their preparation, use as antiandrogenically or schistosomicidally active agents, and corresponding pharmaceutical preparations, are described.
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公开(公告)号:PH13569A
公开(公告)日:1980-06-26
申请号:PH21743
申请日:1978-10-30
Applicant: HOFFMANN LA ROCHE
Inventor: LINK H , BERNAUER K , STOHLER H
IPC: A61K31/415 , A61K31/4166 , A61P5/00 , A61P33/10 , C07D233/66 , C07D233/72 , C07D233/74 , C07D233/88 , C07D235/00
Abstract: Imidazolidine derivatives of the formula I wherein X is oxygen or imino and R is one of the groups their preparation, use as antiandrogenically or schistosomicidally active agents, and corresponding pharmaceutical preparations, are described.
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公开(公告)号:ZA7805930B
公开(公告)日:1979-09-26
申请号:ZA7805930
申请日:1978-10-20
Applicant: HOFFMANN LA ROCHE
Inventor: STOHLER H , LINK H , BERNAUER K
IPC: A61K20060101 , C07D20060101 , C07D
CPC classification number: Y02A50/423
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公开(公告)号:SE7811194A
公开(公告)日:1979-04-29
申请号:SE7811194
申请日:1978-10-27
Applicant: HOFFMANN LA ROCHE
Inventor: BERNAUER K , LINK H , STOHLER H
IPC: A61K31/415 , A61K31/4166 , A61P5/00 , A61P33/10 , C07D233/66 , C07D233/72 , C07D233/74 , C07D233/88
CPC classification number: C07D233/88 , C07D233/72
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公开(公告)号:SE433304B
公开(公告)日:1984-05-21
申请号:SE7811193
申请日:1978-10-27
Applicant: HOFFMANN LA ROCHE
Inventor: BERNAUER K , LINK H , STOHLER H
IPC: A61K31/215 , A61K31/22 , A61K31/24 , A61P5/00 , A61P33/00 , C07C67/00 , C07C239/00 , C07C275/42 , C07D233/66 , C07D233/72 , C07D233/88 , A61K9/20 , A61K9/48
Abstract: Imidazolidine derivatives, as well as processes for their preparation, which have antiandrogenic and schistosomicidal activity.
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公开(公告)号:SE8202106L
公开(公告)日:1982-04-01
申请号:SE8202106
申请日:1982-04-01
Applicant: HOFFMANN LA ROCHE
Inventor: BERNAUER K , LINK H , STOHLER H
IPC: A61K31/215 , A61K31/22 , A61K31/24 , A61P5/00 , A61P33/00 , C07C67/00 , C07C239/00 , C07C275/42 , C07D233/66 , C07D233/72 , C07D233/88 , C07C127/19 , C07D233/28
Abstract: Imidazolidine derivatives, as well as processes for their preparation, which have antiandrogenic and schistosomicidal activity.
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公开(公告)号:DK174480A
公开(公告)日:1980-10-25
申请号:DK174480
申请日:1980-04-23
Applicant: HOFFMANN LA ROCHE
Inventor: LINK H
IPC: C07D233/88 , A61K31/415 , A61K31/4166 , A61P33/02 , C07C275/30 , C07D233/72 , C07D233/80 , C07D
Abstract: 1. Process for the manufacture of imidazolidine derivatives of the general formula see diagramm : EP0017976,P9,F1 wherein X represents imino or oxygen and R represents one of the groups see diagramm : EP0017976,P9,F2 characterized by reacting a compound of the general formula R-NH-R**4 with a compound of the general formula see diagramm : EP0017976,P9,F3 whereby in formulae II and III the one R**4 signifies hydrogen and the other R**4 signifies a COOR**5 group, wherein R**5 represents optionally substituted phenyl, and R signifies the same as above, to a compound of the general formula see diagramm : EP0017976,P9,F4 wherein R signifies the same as above, and, if desired, hydrolyzing the latter compound to a hydantoin compound of the general formula see diagramm : EP0017976,P9,F5 wherein R signifies the same as above.
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