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    4.
    发明专利
    未知

    公开(公告)号：NO134208C

    公开(公告)日：1976-09-01

    申请号：NO273971

    申请日：1971-07-16

    Applicant: HOFFMANN LA ROCHE

    Inventor： BERNAUER K ,  BORGULYA J ,  BOEHNI 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.

    NAPHTHOQUINONE DERIVATIVES
    5.
    发明专利
    NAPHTHOQUINONE DERIVATIVES 未知

    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.

    ANTIBACTERIAL COMPOSITIONS
    8.
    发明专利
    ANTIBACTERIAL COMPOSITIONS 未知

    公开(公告)号：ZA7605015B

    公开(公告)日：1977-08-31

    申请号：ZA7605015

    申请日：1976-08-20

    Applicant: HOFFMANN LA ROCHE

    Inventor： ZANETTI G ,  BOEHNI E

    IPC: C07D239/49 ,  A61K31/505 ,  A61P31/04 ,  A61K

    CPC classification number: A61K31/505 ,  Y02A50/473

    Abstract: 1510938 Antibacterial agent containing N'- (5 - methoxy - 2 - pyrimidinyl) - sulphonilamide F HOFFMAN LA ROCHE & CO AG 27 Aug 1976 [29 Aug 1975] 35744/76 Heading A5B An antibacterial agent contains N' - (5 - methoxy - 2 - pyrimidinyl) - sulphanilamide or a salt thereof with a strong base, and a sulphonamide potentiator of the formula:- wherein R 1 and R 2 each represent a methyl, ethyl, methoxy or ethoxy group and R 3 represents a methoxy or ethoxy group, or a physiologically acceptable acid addition salt thereof. The compositions may be made up in a form suitable for oral or parenteral use or in the form of a suppository.

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