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    Lincomycin analogs
    11.
    再颁专利
    Lincomycin analogs 失效
    林可霉素类似物

    公开(公告)号：USRE29558E

    公开(公告)日：1978-02-28

    申请号：US730835

    申请日：1976-10-08

    申请人： Brian Bannister

    发明人： Brian Bannister

    IPC分类号： C07H5/02 ,  C07D327/04 ,  C07D327/06 ,  C07H3/02 ,  C07H5/08 ,  C07H15/16

    CPC分类号： C07H15/16 ,  C07D327/04 ,  C07D327/06 ,  Y02P20/55

    摘要： Compounds of the formula: ##STR1## are disclosed, wherein R.sub.1 taken independently is hydrogen; R.sub.2 taken independently is the moiety ##STR2## wherein Ac is carboxacyl or an acyl group of formula: ##STR3## wherein Z is hydrogen, lower alkyl or a protective group removable by hydrogenolysis; R.sub.5 is lower alkyl; R.sub.1 and R.sub.2 when together are the divalent group; ##STR4## wherein Z and R.sub.5 are as defined above; R.sub.3 is hydrogen when R.sub.1 and R.sub.2 are taken together and is a monovalent thio group of formula: ##STR5## located in the 7(S)-position when R.sub.1 and R.sub.2 are taken independently, A represents hydrogen or hydroxyl, B represents hydrogen or hydroxyalkyl, n is the integer 0 when B is hydroxyalkyl and n is an integer of 0 to 1, inclusive, when B is hydrogen, X is oxygen .[.or sulfur.]., D is the acyl radical of a lower hydrocarbon carboxylic acid; R.sub.4 is lower alkyl and Y is carboxacyl or hydrogen.Disclosed also are methods of making and using the novel compounds of the invention, which are useful intermediates in the chemical synthesis of useful antibacterial lincomycin analogs. Certain of the compounds of the invention are also active as antibacterial agents.

    Lincomycin analogs
    12.
    发明授权
    Lincomycin analogs 失效
    林可霉素类似物

    公开(公告)号：US3870699A

    公开(公告)日：1975-03-11

    申请号：US33845973

    申请日：1973-03-06

    申请人： UPJOHN CO

    发明人： BANNISTER BRIAN

    IPC分类号： C07H5/02 ,  C07D327/04 ,  C07D327/06 ,  C07H3/02 ,  C07H5/08 ,  C07H15/16 ,  C07C47/18

    CPC分类号： C07H15/16 ,  C07D327/04 ,  C07D327/06 ,  Y02P20/55

    摘要： LOCATED IN THE 7(S)-position when R1 and R2 are taken independently, A represents hydrogen or hydroxyl, B represents hydrogen or hydroxyalkyl, n is the integer 0 when B is hydroxyalkyl and n is an integer of 0 to 1, inclusive, when B is hydrogen, X is oxygen or sulfur, D is the acyl radical of a lower hydrocarbon carboxylic acid; R4 is lower alkyl and Y is carboxacyl or hydrogen. Disclosed also are methods of making and using the novel compounds of the invention, which are useful intermediates in the chemical synthesis of useful antibacterial lincomycin analogs. Certain of the compounds of the invention are also active as antibacterial agents.

    WHEREIN Z and R5 are as defined above; R3 is hydrogen when R1 and R2 are taken together and is a monovalent thio group of formula:

    WHEREIN Z is hydrogen, lower alkyl or a protective group removable by hydrogenolysis; R5 is lower alkyl; R1 and R2 when together are the divalent group;

    WHEREIN Ac is carboxacyl or an acyl group of formula:

    ARE DISCLOSED, WHEREIN R1 taken independently is hydrogen; R2 taken independently is the moiety

    Compounds of the formula:

    摘要翻译： 下式的化合物：

    1-Substituted glycopyranosides
    18.
    发明授权
    1-Substituted glycopyranosides 失效
    1-取代的吡喃糖苷

    公开(公告)号：US4228274A

    公开(公告)日：1980-10-14

    申请号：US922897

    申请日：1978-07-10

    申请人： Mitree M. Ponpipom ,  Robert L. Bugianesi ,  Philippe L. Durette ,  Howard M. Katzen ,  Tsung-Ying Shen

    发明人： Mitree M. Ponpipom ,  Robert L. Bugianesi ,  Philippe L. Durette ,  Howard M. Katzen ,  Tsung-Ying Shen

    IPC分类号： C07H13/04 ,  C07H15/04 ,  C07H15/14 ,  C07H5/06 ,  C07H5/08

    CPC分类号： C07H13/04 ,  C07H15/04 ,  C07H15/14

    摘要： The invention disclosed herein relates to novel 1-deoxy-glycopyranosides, preferably 1-deoxy-D-mannopyranosides, having in the 1-position of the pyranoside ring an .omega.-aminoalkylthio, .omega.-aminoalkyloxy or .omega.-aminoalkanoylamino substituent; and to novel processes for preparing these 1-substituted-1-deoxy-glycopyranosides starting with the corresponding tetra-O-acetyl-glycopyranosyl bromide or amine. These .omega.-amino(alkylthio, alkyloxy or alkanoylamino)-1-deoxy-glycopyranosides, and in particular 1-[(6'-aminohexyl)thio or oxy]-1-deoxy-D-mannopyranosides, possess insulin-like activity.

    摘要翻译： 本文公开的本发明涉及在吡喃糖苷环的1位具有ω-氨基烷硫基，ω-氨基烷氧基或ω-氨基烷酰基氨基取代基的1-脱氧-D-甘露吡喃糖苷类的新型1-脱氧-D-吡喃甘露糖苷， 以及由相应的四-O-乙酰基 - 吡喃葡糖基溴或胺开始制备这些1-取代-1-脱氧 - 糖吡喃糖苷的新方法。 这些ω-氨基（烷硫基，烷氧基或烷酰氨基）-1-脱氧 - 糖吡喃糖苷，特别是1 - [（6'-氨基己基）硫代或氧基] -1-脱氧-D-甘露吡喃糖苷类，具有胰岛素样活性。