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公开(公告)号:KR820002388B1
公开(公告)日:1982-12-29
申请号:KR820004632
申请日:1982-10-14
Applicant: HOFFMANN LA ROCHE
Inventor: BERNAUER K , LINK H , STOHLER H
IPC: C07D233/90
Abstract: The imidazolidines I(R=Cl, CF3; R1=H,F, Cl; R2=H, Cl; Z=O, NH) were prepd. for use as schistosomicides and antiandrogenic substances (test data tabulated). Thus, 3,4-(F3C)CLC6H3NCO reacted with Me2CH(NH2)CN at 100≦̸C to give I(R = CF5, R1 = Cl, R2 = H, Z = NH), which was hydrolyzed to give I(Z = O)
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公开(公告)号:KR820002387B1
公开(公告)日:1982-12-29
申请号:KR820004633
申请日:1982-10-14
Applicant: HOFFMANN LA ROCHE
Inventor: BERNAUER K , LINK H , STOHLER H
IPC: C07D233/72
Abstract: Title compds. (I; R=II, III, IV, V, VI), useful as an schistosomicide and antiandrogenic substance were prepd. by hydrolyzing Ia. Thus, 61 mg 1-(3-trifluoromethy1-4-chloro-pheny1)-5-imino-4, 4-dimethy1-2-imidazolidinone was dissolved in 4 ml 0.1N HCl, added 2ml H2O and filtrated after 20 hr to give 3-(3-trifluoromethy1-4-chloropheny1)-5,5-dimethylhydantoin(m.p. 156-157.5oC).
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公开(公告)号:KR820002386B1
公开(公告)日:1982-12-29
申请号:KR780003228
申请日:1978-10-27
Applicant: HOFFMANN LA ROCHE
Inventor: BERNAUER K , LINK H , STOHLER H
IPC: C07D233/72
Abstract: The imidazolidines I(R=Cl, CF3; R1=H,F, Cl; R2=H, Cl; Z=O, NH) were prepd. for use as schistosomicides and antiandrogenic substances. Thus, 3, 4-(F3C)ClC6H3NCO reacted with Me2CHCH(NH2)CN at 100≦̸ to give I(R=CF5, R1=Cl, R2=H, z= NH), which washydrolyzed to I(Z=O).
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公开(公告)号:ZA785929B
公开(公告)日:1980-05-28
申请号:ZA785929
申请日:1978-10-20
Applicant: HOFFMANN LA ROCHE
Inventor: BERNAUER K , STOHLER H , LINK H
IPC: A61K20060101 , C07D20060101 , A61K , C07D
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公开(公告)号:ZA7805929B
公开(公告)日:1980-05-28
申请号:ZA7805929
申请日:1978-10-20
Applicant: HOFFMANN LA ROCHE
Inventor: BERNAUER K , STOHLER H , LINK H
IPC: A61K20060101 , C07D20060101 , A61K , C07D
CPC classification number: Y02A50/423
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公开(公告)号:BR7807097A
公开(公告)日:1979-05-08
申请号:BR7807097
申请日:1978-10-27
Applicant: HOFFMANN LA ROCHE
Inventor: STOHLER H , BERNAUER K , LINK H
IPC: A61K31/415 , A61K31/4166 , A61P5/00 , A61P33/10 , C07D233/66 , C07D233/72 , C07D233/74 , C07D233/88 , C07D233/70
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:SE7811193A
公开(公告)日:1979-04-29
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 , A61K9/00
CPC classification number: C07D233/72 , A61K31/24 , C07D233/88 , Y02A50/423
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:YU70888A
公开(公告)日:1989-12-31
申请号:YU70888
申请日:1988-04-08
Applicant: HOFFMANN LA ROCHE
Inventor: FURLENMEIER A , GOETSCHI E , HEBEISEN P , HOFHEIZ W , LINK H
IPC: C07D519/06 , A61K31/545 , A61P31/04 , C07D501/36 , C07D501/46 , C07D519/00 , C07D501/00
Abstract: Acyl derivatives of the formula I in which R is an acyl group, excluding those acyl groups of the formula in which A is a group of the formulae -NHCO-, -NHCONHCO-, -NHCOCH=CH-, wherein R6 is hydrogen or lower alkyl; R1 and R2 are hydrogen or a protecting group, X is hydrogen, halogen, lower alkoxy, nitro or -OR2, n is 1 or 2, R4 and R5 are hydrogen or together represent an additional bond and Z is a direct bond or carbonyl (where R4 and R5 both represent hydrogen) or a group of the formula -O-B- (where R4 and R5 together represent an additional bond) in which B is a straight-chain, branched or cyclic lower alkylene; and wherein R3 is a substituted bicyclic group of the formulae 7 5 NR7NNN+RE wherein R7 and R8 are independently hydrogen, lower alkyl or trifluoromethyl or, in formulae (a), (b), (e) and (f) together represent alkylene with 3 or 4 carbon atoms, and R', R'' and R''' are independently hydrogen, lower alkyl or lower cycloalkyl; wherein compounds of formula I in which R4 and R5 together represent an additional bond are present in the syn-isomeric form or as a mixture with the anti-isomeric form in which the syn-isomeric form predominates, as well as readily hydrolyzable esters and salts of these compounds and hydrates of the compounds of formula I or of their esters and salts. These compounds are useful as antibiotics.
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公开(公告)号:ZA785930B
公开(公告)日:1979-09-26
申请号:ZA785930
申请日:1978-10-20
Applicant: HOFFMANN LA ROCHE
Inventor: STOHLER H , LINK H , BERNAUER K
IPC: A61K20060101 , C07D20060101 , C07D
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公开(公告)号:BR7807115A
公开(公告)日:1979-05-15
申请号:BR7807115
申请日:1978-10-27
Applicant: HOFFMANN LA ROCHE
Inventor: BERNAUER K , STOHLER H , LINK H
IPC: A61K31/215 , A61K31/22 , A61K31/24 , A61P5/00 , A61P33/00 , C07C67/00 , C07C239/00 , C07C275/42 , C07D233/66 , C07D233/72 , C07D233/88 , A61K31/17 , A61K31/415 , C07C127/15
Abstract: Imidazolidine derivatives, as well as processes for their preparation, which have antiandrogenic and schistosomicidal activity.
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