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    • 85. 发明专利
    • CH555366A
    • 1974-10-31
    • CH1449168
    • 1968-09-27
    • CIBA GEIGY AG
    • A61K31/155A23K1/16A45D42/00A45D42/04A61P25/00A61P25/02C07D223/32C07D487/08C07J73/00C07D101/00
    • 1,254,806. 3 - Aza - A - homo - steroids. CIBA-GEIGY A.G. 23 Sept., 1969 [27 Sept., 1968], No. 46831/69. Heading C2C. Novel title steroids of the formulµ (where R is free of ketalized oxo, or #-OH or an ether or ester thereof together with α-H or -C 1-5 aliphatic hydrocarbon, or α-H or -OH or an ether or ester thereof together with #-COCH 3 or -COCH 2 OH or their ketal or ester derivatives or α-OH together with #-1 1 ,- 51-dimethylhexyl; and R 1 is C 1-5 alkanoyl) are prepared by oxidation of steroids of the formula (where R is as above and R 1 is H or C 1-5 alkanoyl) and, when required, hydrolysis of an N-acylated product. The N-unsubstituted 19- als cyclize spontaneously to the hemi-acetals, which on acylation give the N-acyl-19-als. In the products, esterified or etherified OH groups or protected oxo groups may be liberated, free OH groups esterified or etherified or oxidized to oxo groups and/or an oxo group reduced toan OH group. The new 3-aza-A-homo-steroids act strongly on the central nervous system in a manner similar to that of the salamander alkaloids, and also have a strong local anaesthetic activity. They may be made up into pharmaceutical and veterinary compositions with suitable carriers. Specification 1,254,626 is referred to.
    • 87. 发明专利
    • BR6912780D0
    • 1973-02-08
    • BR21278069
    • 1969-09-26
    • CIBA GEIGY
    • JEGER OWEHRLI H
    • A61K31/155A23K1/16A45D42/00A45D42/04A61P25/00A61P25/02C07D223/32C07D487/08C07J73/00
    • 1,254,806. 3 - Aza - A - homo - steroids. CIBA-GEIGY A.G. 23 Sept., 1969 [27 Sept., 1968], No. 46831/69. Heading C2C. Novel title steroids of the formulµ (where R is free of ketalized oxo, or #-OH or an ether or ester thereof together with α-H or -C 1-5 aliphatic hydrocarbon, or α-H or -OH or an ether or ester thereof together with #-COCH 3 or -COCH 2 OH or their ketal or ester derivatives or α-OH together with #-1 1 ,- 51-dimethylhexyl; and R 1 is C 1-5 alkanoyl) are prepared by oxidation of steroids of the formula (where R is as above and R 1 is H or C 1-5 alkanoyl) and, when required, hydrolysis of an N-acylated product. The N-unsubstituted 19- als cyclize spontaneously to the hemi-acetals, which on acylation give the N-acyl-19-als. In the products, esterified or etherified OH groups or protected oxo groups may be liberated, free OH groups esterified or etherified or oxidized to oxo groups and/or an oxo group reduced toan OH group. The new 3-aza-A-homo-steroids act strongly on the central nervous system in a manner similar to that of the salamander alkaloids, and also have a strong local anaesthetic activity. They may be made up into pharmaceutical and veterinary compositions with suitable carriers. Specification 1,254,626 is referred to.