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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: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:KR780000174B1
公开(公告)日:1978-05-13
申请号:KR730001305
申请日:1973-08-10
Applicant: HOFFMANN LA ROCHE
Inventor: BRETSCHNEIDEN H , JONES BORGULYA , HOHENLOHE-OEHRINGEN K , BERNAUER K , MONTAVON M
IPC: C07C211/38 , C07C67/00 , C07C209/00 , C07C209/08 , C07C209/16 , C07C209/24 , C07C311/00
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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:KR800001279B1
公开(公告)日:1980-10-26
申请号:KR760000422
申请日:1976-02-20
Applicant: HOFFMANN LA ROCHE
Inventor: BERNAUER K , SCHNEIDER F , PFOERTNER K
IPC: C07D207/10
Abstract: Analgesic pyrrolidine derivs. (I; R1 = pyridy1; R2 = H, lower alky1; R3 = H, lower alky1, benzy1; R4 = halogen, lower alcohol, lower alkoxy, nitro, and amino-substituted pheny1) were prepd. by the redn. of pyrrolines II. Thus, 4-methy1-4-nitro-3-(4-pytidy1)-valerophenon was reduced by Zn in CH3COOH followed by treating with 1n-HC1 and crystallizing with EtOH/(CH3)2CO gave trans-4-(2,2-dimethy1-5-pheny1-pyrolidy1)-pyridine dihydrochloride. I are useful as non-addictive analgesic agent, 3.0g., racemic 4-(cis-2,2-dimethy1-5-pheny1-3-pyrrolidiny1)-pyridine dihydrochloride had ED50 47mg/kg.
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公开(公告)号:KR800001143B1
公开(公告)日:1980-10-14
申请号:KR770001711
申请日:1977-07-25
Applicant: HOFFMANN LA ROCHE
Inventor: BERNAUER K , SCHNEIDER F , WERTNER K , SCHMITT H
IPC: C07D207/09
Abstract: Title compds. (I; R1 = 2-thienyl or phenyl substuted with lower t-amino group, R2 and R3 are independently, H or lower alkyl; R4 = halogen, lower alkyl, lower alkoxy, nitro, phenyl), useful as anaesthetics, were prepd. by reduction of compd. II in the presence of catalyst. Thus, 17 g 2-(P-methoxy-phenyl)-5, 5-dimethyl-4-(2-thienyl)-1-pyrroline and 10 g sodium borohydride were reacted in 250 ml anhydrous ethanol gor 6 hr with N2 gas to give cis-5-(p-methoxyphenyl)-2, 2-dimethyl-3-(2-thienyl)-pyrrolidine hydrochloric acid salt (m.p. 180oC).
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公开(公告)号:US3729492A
公开(公告)日:1973-04-24
申请号:US3729492D
申请日:1971-07-09
Applicant: HOFFMANN LA ROCHE
Inventor: BERNAUER K , BORGULYA J , BOEHNI E
IPC: C07C211/00 , C07C35/29 , C07C49/433 , C07C49/657 , C07C225/30 , C07C87/02 , C07C87/64 , C07C91/00 , C07C93/00
CPC classification number: C07C225/30 , C07B2200/07 , C07C2602/10 , C07C2602/42
Abstract: NOVEL ANPHTHOQUINONE COMPOUNDS REPRESENTED BY THE FORMULA
2-(R1-NH-),3-R-1,4-NAPHTHOQUINONE
WHEREIN R IS HYDROGEN, HALLOGEN, OR LOWER ALKOXY, R1 IS A RESIDUE OF THE FORMULA
NORBORNAN-2-YL, OR 1-CH3,4-R2-TRICYCLO(2.2.0.0(2,6))-
HEX-6-YL
WHEREIN R2 IS HYDROGEN, LOWER ALKYL, OPTIONALLY SUBSTITUTED PHENYL OR PHENYL LOWER ALKYL, AND APROCESS FOR THEIR PREPARATION ARE DESCRIBED.-
公开(公告)号:MC1366A1
公开(公告)日:1981-10-23
申请号:MC1490
申请日:1980-12-18
Applicant: HOFFMANN LA ROCHE
Inventor: PFOERTNER K , BERNAUER K
IPC: C07D263/10 , C07D , A61K
Abstract: Compounds of the formula I wherein R1 and R2, independently, are hydrogen, halogen or lower alkyl; R3, R4, R5, R6 and R7, independently, are hydrogen or lower alkyl; R8 is hydrogen, lower alkyl or formyl; R9 and R10, independently, are methyl or trifluoromethyl; and n is 0 (zero) or, when both R7 and R8 are lower alkyl, n is 0 (zero) or 1, prepared, inter alia, from p-aminobenzaldehydes which may be N-alkyl substituted, are described. The compounds of formula I are orally active antidiabetic agents.
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公开(公告)号:ZW28780A1
公开(公告)日:1981-07-15
申请号:ZW28780
申请日:1980-11-26
Applicant: HOFFMANN LA ROCHE
Inventor: BERNAUER K , PFOERTNER K
IPC: C07D263/10 , A61K , C07D
Abstract: Compounds of the formula I wherein R1 and R2, independently, are hydrogen, halogen or lower alkyl; R3, R4, R5, R6 and R7, independently, are hydrogen or lower alkyl; R8 is hydrogen, lower alkyl or formyl; R9 and R10, independently, are methyl or trifluoromethyl; and n is 0 (zero) or, when both R7 and R8 are lower alkyl, n is 0 (zero) or 1, prepared, inter alia, from p-aminobenzaldehydes which may be N-alkyl substituted, are described. The compounds of formula I are orally active antidiabetic agents.
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公开(公告)号:PH13135A
公开(公告)日:1979-12-12
申请号:PH18108
申请日:1976-02-16
Applicant: HOFFMANN LA ROCHE
Inventor: BERNAUER K , PFOERTNER K , SCHMID H , SCHNEIDER F
IPC: C07D213/50 , C07D401/04 , C07D207/00 , C07D211/00
Abstract: Compounds represented by the formula +q,10 WHEREIN R1 is a pyridyl, R2 is hydrogen or lower alkyl, R3 is hydrogen, lower alkyl or benzyl and R4 is phenyl or phenyl substituted at one or more carbon atoms with one or more of halogen, lower alkyl, lower alkoxy, nitro or amino AND PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF, HAVING ANALGESIC ACTIVITY ARE DISCLOSED.
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