Process for the conversion of echinocandin class of peptides to their c4-homotyrosine monodeoxy analogues
    2.
    发明授权
    Process for the conversion of echinocandin class of peptides to their c4-homotyrosine monodeoxy analogues 失效
    将棘白菌素类肽转化为其c4-同型酪氨酸单体氧化物类似物的方法

    公开(公告)号:US06809177B1

    公开(公告)日:2004-10-26

    申请号:US09673836

    申请日:2001-03-29

    IPC分类号: A61K3812

    摘要: The invention relates to a process for the conversion of echinocandin class of peptides to their C4-homotyrosine monodeoxy analogues, particularly mulundocandin to deoxymulundocandin, which consists of a single step selective reduction of C4-htyr (homotyrosine) hydroxyl group of echinocandins to their monodeoxy analogues under neutral conditions without prior protection/deprotection of the equally facile C5-Orn (ornithine) hydroxyl group and purification of the monodeoxy compound from the crude reaction mixture.

    摘要翻译: 本发明涉及将棘白菌素类的肽转化为其C4-同型酪氨酸单脱氧类似物,特别是将mulundocandin转化为脱氧木兰多糖,其由棘白菌素的C4-htyr(均一酪氨酸)羟基选择性还原为其单脱氧类似物 在没有预先保护/脱保护同样容易的C5-Orn(鸟氨酸)羟基)和从粗反应混合物中纯化单脱氧化合物的中性条件下进行。

    Antimicrobial histone H1 compositions, kits, and methods of use thereof
    3.
    发明授权
    Antimicrobial histone H1 compositions, kits, and methods of use thereof 有权
    抗微生物组蛋白H1组合物,试剂盒及其使用方法

    公开(公告)号:US06565854B2

    公开(公告)日:2003-05-20

    申请号:US09372500

    申请日:1999-08-11

    IPC分类号: A61K3602

    摘要: The invention includes antibiotic pharmaceutical compositions comprising eukaryotic histone H1 protein and methods of using eukaryotic histone H1 protein to kill or to inhibit the growth of microorganisms, including, but not limited to, human pathogenic bacteria. The invention further includes a eukaryotic histone H1-containing animal feed and methods of improving growth of an animal by supplying the feed to the animal. The invention still further includes a kit comprising a eukaryotic histone H1-containing antibiotic pharmaceutical composition and an instructional material which describes the use of the composition. In addition, the invention includes a vaccine comprising a eukaryotic histone H1 protein and a method of vaccinating an animal using the vaccine.

    摘要翻译: 本发明包括包含真核组蛋白H1蛋白的抗生素药物组合物和使用真核组蛋白H1蛋白来杀死或抑制微生物生长的方法,包括但不限于人类致病菌。 本发明还包括含有真核生物组蛋白H1的动物饲料和通过向动物供应饲料来改善动物生长的方法。 本发明还包括一种包含含有真核生物组蛋白H1的抗生素药物组合物的试剂盒和描述该组合物的用途的说明材料。 此外,本发明包括包含真核组蛋白H1蛋白的疫苗和使用疫苗接种动物的方法。

    Cationic oligopeptides having microbicidal activity
    7.
    发明授权
    Cationic oligopeptides having microbicidal activity 失效
    具有杀菌活性的阳离子寡肽

    公开(公告)号:US4659692A

    公开(公告)日:1987-04-21

    申请号:US609410

    申请日:1984-05-11

    摘要: Novel microbicidal compositions are provided which find use as preservatives, disinfectants, antigens and the like. Particularly, cationic oligopeptides of up to about thirty-five amino acids are provided having amino acid sequences substantially comparable to the amino acid sequences of cationic oligopeptides produced by macrophage. A conserved framework structure is provided.The invention described herein was in the course, or under a grant from the United States Public Health Service and the National Institutes of Health.

    摘要翻译: 提供新的杀微生物组合物,其用作防腐剂,消毒剂,抗原等。 特别地,提供高达约35个氨基酸的阳离子寡肽,其具有与由巨噬细胞产生的阳离子寡肽的氨基酸序列基本上相当的氨基酸序列。 提供了一种保守的框架结构。 本文描述的发明是在美国公共卫生局和美国国立卫生研究院的授课中。

    Antibiotics
    8.
    发明授权
    Antibiotics 失效
    抗生素

    公开(公告)号:US4604239A

    公开(公告)日:1986-08-05

    申请号:US743233

    申请日:1985-06-11

    摘要: Antibiotic A41030, a complex of 7 individual factors, is produced by submerged, aerobic fermentation of new Streptomyces virginiae NRRL 12525, and Streptomyces virginiae NRRL 15156. The antibiotic factors are separated and possess antibacterial activity against Staphylococcus and Streptococcus species which are penicillin resistant. In addition, the antibiotic factors have shown inhibition of Streptococcus pneumonia Park I. The complex and the individual factors enhance feed efficiency in ruminant animals, and are growth promoters in chickens and swine, and are especially valuable in milk production in dairy cattle.

    摘要翻译: 抗生素A41030是7种独立因子的复合物,通过新型牛链霉菌NRRL 12525和链霉菌NRRL 15156的浸没式好氧发酵产生。抗生素因子被分离并具有抗青霉素抗性的葡萄球菌和链球菌属的抗菌活性。 此外,抗生素因子已经显示出对肺炎链球菌Park I的抑制作用。复合物和个体因素提高了反刍动物的饲料效率,是鸡和猪的生长促进剂,在奶牛生产中特别有价值。

    Aminopropylaminobleomycin derivatives and process for preparation thereof
    9.
    发明授权
    Aminopropylaminobleomycin derivatives and process for preparation thereof 失效
    氨丙基氨基甜菜碱素衍生物及其制备方法

    公开(公告)号:US4568490A

    公开(公告)日:1986-02-04

    申请号:US743738

    申请日:1985-06-12

    摘要: An aminopropylaminobleomycin represented by the following formula or a salt thereof, which is minimized in side effects such as pulmonary toxicity:[BX]--NH--(CH.sub.2).sub.3 --A--)CH.sub.2).sub.3 --Bwherein[BX] represents the acyl group of bleomycinic acid whose formula differs from that of bleomycin acid by the removal of the hydroxyl group from the carboxyl group of said acid;A represents a group of the general formula ##STR1## wherein R.sub.1 is a lower alkyl or benzyl,R.sub.2 is a lower alkyl or benzyl,R is a lower alkylene, andn is 0 or 1; andB represents a group of the formula ##STR2## wherein (i) R.sub.3 is hydrogen and R.sub.4 is(a) benzyl substituted by one or more halogen atoms, provided that the benzyl is substituted by two halogen atoms when R.sub.1 is lower alkyl,(b) benzyl substituted by cyano, two or more alkoxy groups or two or more benzyloxy groups,(c) lower alkyl substituted by cycloalkyl or anthranyl,(d) phenylethyl substituted by one or more halogen atoms, or(e) diphenylethyl; or(ii) both R.sub.3 and R.sub.4 are benzyl which may be substituted by one or more(a) benzyloxy groups,(b) ring substituted benzyloxy groups in which the ring substituents may be one or more halogen atoms, lower alkoxy groups or benzyloxy groups, or(c) cycloalkylmethoxy groups;and a process for the preparation thereof.

    摘要翻译: 由下式表示的氨基丙基氨基伯合珠霉素或其盐,其在副作用如肺毒性中最小化:[BX] -NH-(CH2)3-A-)CH2)3-B其中[BX]表示酰基 通过从所述酸的羧基除去羟基,其公式不同于博来霉素酸的博来霉素酸; A表示通式为其中R 1为低级烷基或苄基的基团,R 2为低级烷基或苄基,R为低级亚烷基,n为0或1; 并且B代表下式的基团:其中(i)R3是氢,R4是(a)被一个或多个卤素原子取代的苄基,条件是当R 1是低级烷基时,苄基被两个卤原子取代,( (c)由氰基,两个或多个烷氧基或两个或更多个苄氧基取代的苄基,(c)被环烷基或蒽基取代的低级烷基,(d)被一个或多个卤素原子取代的苯基乙基,或(e)二苯基乙基; 或(ii)R 3和R 4均为可被一个或多个(a)苄氧基取代的苄基,(b)环取代的苄氧基,其中环取代基可以是一个或多个卤素原子,低级烷氧基或苄氧基 ,或(c)环烷基甲氧基; 及其制备方法。

    A41030 Antibiotics
    10.
    发明授权
    A41030 Antibiotics 失效
    A41030抗生素

    公开(公告)号:US4559323A

    公开(公告)日:1985-12-17

    申请号:US637096

    申请日:1984-08-02

    摘要: Antibiotic A41030, a complex of 7 individual factors, is produced by submerged, aerobic fermentation of new Streptomyces virginiae NRRL 12525, and Streptomyces virginiae NRRL 15156. The antibiotic factors are separated and possess antibacterial activity against Staphylococcus and Streptococcus species which are penicillin resistant. In addition, the antibiotic factors have shown inhibition of Streptococcus pneumonia Park I. The complex and the individual factors enhance feed efficiency in ruminant animals, and are growth promoters in chickens and swine, and are especially valuable in milk production in dairy cattle.

    摘要翻译: 抗生素A41030是7种独立因子的复合物,通过新型牛链霉菌NRRL 12525和链霉菌NRRL 15156的浸没式好氧发酵产生。抗生素因子被分离并具有抗青霉素抗性的葡萄球菌和链球菌属的抗菌活性。 此外,抗生素因子已经显示出对肺炎链球菌Park I的抑制作用。复合物和个体因素提高了反刍动物的饲料效率,是鸡和猪的生长促进剂,在奶牛生产中特别有价值。