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公开(公告)号:SE377798B
公开(公告)日:1975-07-28
申请号:SE922771
申请日:1971-07-16
Applicant: HOFFMANN LA ROCHE
Inventor: BERNAUER K , BORGULYA J , BOHNI E
IPC: C07C211/00 , C07C35/29 , C07C49/433 , C07C49/657 , C07C225/30 , C07C97/22
Abstract: 1314118 2 - Aminonaphthaquinone derivatives F HOFFMANN-LA ROCHE & CO AG 16 July 1971 [17 July 1970] 33475/71 Heading C2C Novel compounds of Formula I: wherein R is H, halogen or C 1-4 alkoxy and R 1 is a group of Formula Ib: or Ia: wherein R 2 is H, C 1-7 alkyl, phenyl optionally substituted by halogen, nitro, amino or hydroxy or is phenyl-(C 1-4 )-alkyl or a salt thereof, are prepared either by oxidation of a compound of Formula IV: or by reaction of a compound of Formula II: wherein R 3 is acyloxy, alkoxy, aryloxy, aralkoxy, arylthio, aralkylthio, hydroxy or halogen with an amine R 1 -NH 2 , and optionally converting a compound wherein R is H or halogen other than chlorine into a compound where R is chlorine or any compound into an acid addition salt. 2 - (2 - Endo - bornylamino) - 3 - chloro - 1,4- dihydroxy-naphthalene is prepared by reduction of the corresponding naphthaquinone. Amines of formula R 1 -NH 2 are prepared either by reduction of the corresponding oxime R 1 =NOH optionally with separation of stereoisomers by crystallization of the acetates or by hydrolysis of the N-acetylamino compound and where R 2 is nitro-phenyl, by nitration of the compound where R 2 is phenyl prior to hydrolysis. The N-acetyl compounds R 1 -NACOCH 3 are prepared by reaction of the appropriate 2-R 2 -2-borneol with acetonitrile. 2-Heptyl-2-borneol is prepared by reduction of 2-heptynyl-2-borneol obtained by reaction of camphor 1-heptyne and ethylmagnesium bromide. N - (4 - Phenethyl - 2 - exobornyl) - acetamide is obtained by reaction of acetonitrile with 2-(1- phenethylidene)-camphane obtained by reaction of 2-phenethylborneol with acetic anhydride. Pharmaceutical compositions in conventional forms for oral, rectal or parenteral administration and having amoebicidal and bacteriostatic activity comprise an above novel compound and a carrier therefor.
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公开(公告)号:ZA734651B
公开(公告)日:1974-06-26
申请号:ZA734651
申请日:1973-07-10
Applicant: HOFFMANN LA ROCHE
Inventor: HOHENLOHE OEHRINGEN K , BERNAUER K , WEIS G , BRETSCHNEIDER H , BORGULYA J , MONTAVON M
IPC: C07C67/00 , C07C211/38 , C07C209/00 , C07C209/08 , C07C209/16 , C07C209/24 , C07C311/00 , C07C
Abstract: The present invention is concerned with norbornane derivatives and a process for the manufacture thereof.
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公开(公告)号:ZA7304651B
公开(公告)日:1974-06-26
申请号:ZA7304651
申请日:1973-07-10
Applicant: HOFFMANN LA ROCHE
Inventor: BERNAUER K , WEIS G , BRETSCHNEIDER H , HOHENLOHE OEHRINGEN K , BORGULYA J , MONTAVON M
IPC: C07C211/38 , C07C67/00 , C07C209/00 , C07C209/08 , C07C209/16 , C07C209/24 , C07C311/00 , C07C
CPC classification number: C07C311/00
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公开(公告)号:ZA714392B
公开(公告)日:1972-02-23
申请号:ZA714392
申请日:1971-07-05
Applicant: HOFFMANN LA ROCHE
Inventor: BERNAUER K , BORGULYA J , BOEHNI E
IPC: C07C211/00 , C07C35/29 , C07C49/433 , C07C49/657 , C07C225/30 , C07D
Abstract: 1314118 2 - Aminonaphthaquinone derivatives F HOFFMANN-LA ROCHE & CO AG 16 July 1971 [17 July 1970] 33475/71 Heading C2C Novel compounds of Formula I: wherein R is H, halogen or C 1-4 alkoxy and R 1 is a group of Formula Ib: or Ia: wherein R 2 is H, C 1-7 alkyl, phenyl optionally substituted by halogen, nitro, amino or hydroxy or is phenyl-(C 1-4 )-alkyl or a salt thereof, are prepared either by oxidation of a compound of Formula IV: or by reaction of a compound of Formula II: wherein R 3 is acyloxy, alkoxy, aryloxy, aralkoxy, arylthio, aralkylthio, hydroxy or halogen with an amine R 1 -NH 2 , and optionally converting a compound wherein R is H or halogen other than chlorine into a compound where R is chlorine or any compound into an acid addition salt. 2 - (2 - Endo - bornylamino) - 3 - chloro - 1,4- dihydroxy-naphthalene is prepared by reduction of the corresponding naphthaquinone. Amines of formula R 1 -NH 2 are prepared either by reduction of the corresponding oxime R 1 =NOH optionally with separation of stereoisomers by crystallization of the acetates or by hydrolysis of the N-acetylamino compound and where R 2 is nitro-phenyl, by nitration of the compound where R 2 is phenyl prior to hydrolysis. The N-acetyl compounds R 1 -NACOCH 3 are prepared by reaction of the appropriate 2-R 2 -2-borneol with acetonitrile. 2-Heptyl-2-borneol is prepared by reduction of 2-heptynyl-2-borneol obtained by reaction of camphor 1-heptyne and ethylmagnesium bromide. N - (4 - Phenethyl - 2 - exobornyl) - acetamide is obtained by reaction of acetonitrile with 2-(1- phenethylidene)-camphane obtained by reaction of 2-phenethylborneol with acetic anhydride. Pharmaceutical compositions in conventional forms for oral, rectal or parenteral administration and having amoebicidal and bacteriostatic activity comprise an above novel compound and a carrier therefor.
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公开(公告)号:NZ209479A
公开(公告)日:1988-04-29
申请号:NZ20947984
申请日:1984-09-07
Applicant: HOFFMANN LA ROCHE
Inventor: BERNAUER K , BRUDERER H
IPC: A61K31/135 , C07C205/26 , C07C205/57 , C07C91/30 , C07C91/23 , C07C93/14 , C07C97/10
Abstract: The novel phenethylamine derivatives of the general formula I wherein R1 and R2 each signify hydrogen, halogen, trifluoromethyl, lower alkoxy, lower alkyl, hydroxy or nitro, with the proviso that at least one of R1 and R2 is different from hydrogen, R3 and R4 each signify lower alkyl, n signifies the number 1, 2, 3 or 4 and B signifies the group -CO- or -CHOH-, and their pharmaceutically acceptable acid addition salts have interesting analgesic and antidepressant properties. These substances can be manufactured according to various methods which are known per se and can be used as medicaments in the form of pharmaceutical preparation.
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公开(公告)号:NZ195830A
公开(公告)日:1984-07-06
申请号:NZ19583080
申请日:1980-12-15
Applicant: HOFFMANN LA ROCHE
Inventor: BERNAUER K , PFOERTNER K
IPC: C07D263/10 , C07D263 , A61K31/42
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: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:YU35476A
公开(公告)日:1982-10-31
申请号:YU35476
申请日:1976-02-16
Applicant: HOFFMANN LA ROCHE
Inventor: BERNAUER K , PFOERTNER K , SCHNEIDER F , SCHMID H
IPC: C07D213/50 , C07D401/04 , C07D207/08 , A61K31/395
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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公开(公告)号:LU83017A1
公开(公告)日:1982-07-07
申请号:LU83017
申请日:1980-12-19
Applicant: HOFFMANN LA ROCHE
Inventor: BERNAUER K , PFOERTNER K
IPC: C07D263/10 , C07D , A61K
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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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