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    42.
    发明专利
    未知

    公开(公告)号：DK545980A

    公开(公告)日：1981-06-22

    申请号：DK545980

    申请日：1980-12-19

    Applicant: HOFFMANN LA ROCHE

    Inventor： BERNAUER K ,  PFOERTNER K

    IPC: C07D263/10 ,  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.

    PYRROLIDINE DERIVATIVES
    46.
    发明专利
    PYRROLIDINE DERIVATIVES 未知

    公开(公告)号：AU500184B2

    公开(公告)日：1979-05-10

    申请号：AU1062976

    申请日：1976-01-29

    Applicant: HOFFMANN LA ROCHE

    Inventor： BERNAUER K ,  PFOERTNER K ,  SCHNEIDER F ,  SCHMID H

    IPC: C07D213/50 ,  C07D401/04 ,  A61K31/44

    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.

    49.
    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.

    50.
    发明专利
    未知

    公开(公告)号：DK72876A

    公开(公告)日：1976-08-22

    申请号：DK72876

    申请日：1976-02-20

    Applicant: HOFFMANN LA ROCHE F

    Inventor： BERNAUER K ,  PFOERTNER K ,  SCHNEIDER F ,  SCHMID H

    IPC: C07D213/50 ,  C07D401/04

    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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