51.
    发明专利
    未知

    公开(公告)号:SE377798B

    公开(公告)日:1975-07-28

    申请号:SE922771

    申请日:1971-07-16

    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
    54.
    发明专利

    公开(公告)号:ZA714392B

    公开(公告)日:1972-02-23

    申请号:ZA714392

    申请日:1971-07-05

    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.

    PHENETHYLAMINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS

    公开(公告)号:NZ209479A

    公开(公告)日:1988-04-29

    申请号:NZ20947984

    申请日:1984-09-07

    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.

    5-(P-AMINOPHENYL)-4-PHENYL-2,2-DI(METHYL OR TRIFLUOROMETHYL)OXAZOLINES

    公开(公告)号:NZ195830A

    公开(公告)日:1984-07-06

    申请号:NZ19583080

    申请日:1980-12-15

    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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