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    • 4. 发明授权
    • Compound nanaomycin A and derivatives thereof and a process for
producing the same
    • 复方纳诺霉素A及其衍生物及其制备方法
    • US4324728A
    • 1982-04-13
    • US47451
    • 1979-06-11
    • Satoshi OmuraHaruo TanakaJuichi AwayaToju Hata
    • Satoshi OmuraHaruo TanakaJuichi AwayaToju Hata
    • C07D311/92A61K31/35A61K31/352A61P31/04C12P7/66C12P17/06
    • C12R1/465C12P17/06
    • The present invention relates to new compound nanaomycin A and derivatives thereof represented by general formula: ##STR1## in which (a) R is H and R' is OH (nanaomycin A),(b) R is H and R' is NH.sub.2 (nanaomycin C),(c) R is COCH.sub.3 and R' is OH (acetylnanaomycin A), and(d) R is H and R' is OCH.sub.3 (nanaomycin A methyl ester).Nanaomycin A is a new compound of quinone type and its acute toxicity (LD.sub.50, intra-penetrial injection) in mice is 28.2 mg/Kg. Nanaomycin A and derivatives thereof are active on Gram-positive bacteria, trichophyton and mycoplasma and are useful as a medicament for humans and animals. Nanaomycins A and C are produced by culturing a nanaomycin-producing strain belonging to the genus Streptomyces aerobically in a medium to accumulate nanaomycins A and C in the cultured broths. The derivatives acetylnanaomycin A and nanaomycin A methyl ester have similar properties to those of nanaomycin A.
    • 本发明涉及由以下通式表示的新化合物纳那霉素A及其衍生物:其中(a)R是H,R'是OH(纳那霉素A),(b)R是H和R' 是NH2(纳那霉素C),(c)R是COCH 3,R'是OH(乙酰氨基霉素A),和(d)R是H,R'是OCH 3(纳诺霉素A甲酯)。 Nanaomycin A是醌类的新化合物,其在小鼠中的急性毒性(LD50,内渗注射)为28.2mg / Kg。 纳诺霉素A及其衍生物对革兰氏阳性菌,毛毛虫和支原体具有活性,可用作人和动物的药物。 Nanaomycins A和C通过在培养基中培养产生链霉菌属的链霉菌属的纳米霉素生产菌株在培养基中培养以在培养的肉汤中积累纳米菌素A和C而产生。 乙酰纳他霉素A和纳那霉素A甲酯的衍生物具有与纳那霉素A相似的性质。
    • 5. 发明授权
    • Production of nanaomycin A and derivatives thereof
    • 生产纳诺霉素A及其衍生物
    • US4196266A
    • 1980-04-01
    • US858215
    • 1977-12-07
    • Satoshi OmuraHaruo TanakaJuichi AwayaToju Hata
    • Satoshi OmuraHaruo TanakaJuichi AwayaToju Hata
    • C12P17/06C12D9/14
    • C12R1/465C12P17/06Y10S435/886
    • The present invention relates to new compound nanaomycin A and derivatives thereof represented by general formula: ##STR1## in which (a) R is H and R' is OH (nanaomycin A),(b) R is H and R' is NH.sub.2 (nanaomycin C),(c) R is COCH.sub.3 and R' is CH (acetylnanaomycin A), and(d) R is H and R' is OCH.sub.3 (nanaomycin A methyl ester).Nanaomycin A is a new compound of quinone type and its acute toxicity (LD.sub.50, intra-penetrial injection) in mice is 28.2 mg/Kg. Nanaomycin A and derivatives thereof are active on Gram-positive bacteria, trichophyton and mycoplasma and are useful as a medicament for humans and animals. Nanaomycins A and C are produced by culturing a nanaomycin-producing strain belonging to the genus Streptomyces aerobically in a medium to accumulate nanaomycins A and C in the cultured broths. The derivatives acetylnanaomycin A and nanaomycin A methyl ester have similar properties to those of nanaomycin A.
    • 本发明涉及由以下通式表示的新化合物纳那霉素A及其衍生物:其中(a)R是H,R'是OH(纳那霉素A),(b)R是H和R' 是NH2(纳那霉素C),(c)R是COCH 3,R'是CH(乙酰氨基霉素A),和(d)R是H,R'是OCH 3(纳诺霉素A甲酯)。 Nanaomycin A是醌类的新化合物,其在小鼠中的急性毒性(LD50,内渗注射)为28.2mg / Kg。 纳诺霉素A及其衍生物对革兰氏阳性菌,毛毛虫和支原体具有活性,可用作人和动物的药物。 Nanaomycins A和C通过在培养基中培养产生链霉菌属的链霉菌属的纳米霉素生产菌株在培养基中培养以在培养的肉汤中积累纳米菌素A和C而产生。 乙酰纳他霉素A和纳那霉素A甲酯的衍生物具有与纳那霉素A相似的性质。
    • 6. 发明授权
    • Production of nanaomycin B
    • 生产纳诺霉素B
    • US4194064A
    • 1980-03-18
    • US858216
    • 1977-12-07
    • Satoshi OmuraHaruo TanakaJuichi AwayaToju Hata
    • Satoshi OmuraHaruo TanakaJuichi AwayaToju Hata
    • C12P17/06C12D9/14
    • C12R1/465C12P17/06Y10S435/886
    • The present invention relates to new compound designated as nanaomycin B represented by general formula: ##STR1## Nanaomycin B is a quinone type and is active on mycoplasma, Gram-positive bacteria and trycophyton. This compound is useful as a medicament for infectious diseases of humans and animals caused by a parasite of trichophyton or mycoplasma etc. The acute toxicity (LD.sub.50, intra-penetrial injection) in mice of this compound is 169 mg/kg. Nanaomycin B is produced by fermentation in which a nanaomycin-producing strain belonging to the genus Streptomyces is cultured in a medium under aerobic conditions and the accumulated nanaomycin B in the cultured broths is recovered therefrom.
    • 本发明涉及以通式表示的纳那霉素B的新化合物:< IMAGE> Nanaomycin B是醌类,对支原体,革兰氏阳性菌和真菌是有活性的。 该化合物可用作由毛癣菌或支原体寄生虫等引起的人类和动物感染性疾病的药物。该化合物小鼠的急性毒性(LD50,内渗注射)为169mg / kg。 纳豆霉素B通过发酵生产,其中在需氧条件下培养在属于链霉菌属的纳米霉素生产菌株,并从其中回收培养肉汤中积累的纳诺霉素B.
    • 8. 发明授权
    • Lactacystin derivatives
    • 乳酸衍生物
    • US5869675A
    • 1999-02-09
    • US979637
    • 1997-11-28
    • Satoshi OmuraToshiaki SunazukaHaruo Tanaka
    • Satoshi OmuraToshiaki SunazukaHaruo Tanaka
    • C07D207/12C07D207/28C07D401/12
    • C07D401/12C07D207/28
    • Novel lactacystin derivatives other than lactacystin per se, with superior activity for the genesis of neurites and highly selective toxicity and low cytotoxicity as compared with known lactacystin have been prepared, of the formula ##STR1## wherein R is lower alkoxy, --S--(CH.sub.2).sub.n R.sup.1 or --S--(CH.sub.2) .sub.n --CH(R.sup.2)-(R.sup.3), in which R.sup.1 is branched or straight-chain lower alkyl, hydroxy, carboxyl, lower alkoxycarbonyl, optionally substituted phenyl, substituted or unsubstituted amino or pyridyl, R.sup.2 is substituted or unsubstituted amino, lower alkyl or amino acid residue, R.sup.3 is carboxyl, lower alkoxycarbonyl, lower alkenyloxycarbonyl or amino acid residue, and n is 0-4, or a pharmacologically acceptable salt thereof.
    • 与已知的乳胞蛋白相比,已经制备了除了乳糖蛋白本身以外的新型乳胞素衍生物,具有优异的神经突发生活性和高选择性毒性和低细胞毒性,其中R为低级烷氧基,-S - (CH2)nR1或-S-(CH2)n-CH(R2) - (R3),其中R1是支链或直链低级烷基,羟基,羧基,低级烷氧基羰基,任选取代的苯基,取代或未取代的氨基 或吡啶基,R2为取代或未取代的氨基,低级烷基或氨基酸残基,R3为羧基,低级烷氧基羰基,低级链烯氧基羰基或氨基酸残基,n为0-4,或其药理学上可接受的盐。