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    Preparation of Monacolin K
    3.
    发明授权
    Preparation of Monacolin K 失效
    莫纳可林K的制备

    公开(公告)号：US4323648A

    公开(公告)日：1982-04-06

    申请号：US137821

    申请日：1980-04-04

    申请人： Kazuhiko Tanzawa ,  Seigo Iwado ,  Yoshio Tsujita ,  Masao Kuroda ,  Kouhei Furuya

    发明人： Kazuhiko Tanzawa ,  Seigo Iwado ,  Yoshio Tsujita ,  Masao Kuroda ,  Kouhei Furuya

    IPC分类号： A61K36/06 ,  A61K31/35 ,  A61P3/06 ,  C07D233/64 ,  C07D309/30 ,  C12P1/02 ,  C12P7/62 ,  C12P17/02 ,  C12P17/06 ,  C12R1/645

    CPC分类号： C12P17/06 ,  C07D309/30 ,  Y10S435/911

    摘要： Monacolin K, which is an antihypercholesteraemic agent of molecular formula C.sub.24 H.sub.36 O.sub.5, is prepared by cultivating one or more of the microorganisms Monascus anka SANK 10171 (IFO 6540), Monascus purpureus SANK 10271 (IFO 4513), Monascus ruber SANK 10671 (FERM 4958), Monascus vitreus SANK 10960 (FERM 4960), Monascus paxii SANK 11172 (IFO 8201), Monascus ruber SANK 13778 (FERM 4959), Monascus ruber SANK 15177 (FERM 4956) or Monascus ruber SANK 18174 (FERM 4957) in a suitable culture medium and then isolating the Monacolin K from the resulting culture broth.

    摘要翻译： 作为分子式C24H36O5的抗高胆固醇血症药的莫纳可林K是通过培养一种或多种微生物Monkaus又名SANK 10171（IFO 6540），红曲霉SANK 10271（IFO 4513），红曲霉SANK 10671（FERM 4958）， 红曲霉玻璃体SANK 10960（FERM 4960），红曲霉SANK 11172（IFO 8201），红曲霉SANK 13778（FERM 4959），红曲霉SANK 15177（FERM 4956）或红曲霉SANK 18174（FERM 4957）在合适的培养基中， 然后从所得培养液中分离出莫纳可林K。

    Macrolide compounds, their preparation and their use
    6.
    发明授权
    Macrolide compounds, their preparation and their use 失效
    大环内酯类化合物，其制备及其用途

    公开(公告)号：US5008191A

    公开(公告)日：1991-04-16

    申请号：US131413

    申请日：1987-12-10

    申请人： Takao Okazaki ,  Shuji Takahashi ,  Seigo Iwado ,  Keiji Tanaka ,  Toshiaki Yanai ,  Hisaki Kajino

    发明人： Takao Okazaki ,  Shuji Takahashi ,  Seigo Iwado ,  Keiji Tanaka ,  Toshiaki Yanai ,  Hisaki Kajino

    IPC分类号： C07D493/22 ,  A01N43/90 ,  A01N49/00 ,  A01P7/02 ,  A01P7/04 ,  C07D307/00 ,  C07D309/00 ,  C07H19/01 ,  C12P17/18 ,  C12P19/54

    CPC分类号： C07H19/01 ,  A01N49/00 ,  C12P17/181 ,  Y02P20/55 ,  Y10S435/898

    摘要： Compounds with acaricidal, insecticidal and anthelmintic activities have the formula: ##STR1## wherein: --X--Y-- is selected from the group consisting of --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CHOH--, --CH.dbd.CH--, and --CH.sub.2 --C(.dbd.O)--;R.sup.1 is selected from the group consisting of a methyl group, an ethyl group, an isopropyl group, a sec-butyl group and groups of formula --C(CH.sub.3).dbd.CHR.sup.5 in which R.sup.5 is selected from the group consisting of a methyl group, an ethyl group and an isopropyl group;R.sup.2 represents a group of formula --(CH.sub.2).sub.n --C(R.sup.6).dbd.C(R.sup.7)(R.sup.8) in which n is 0, 1 or 2, R.sup.6 and R.sup.7 each is selected from the group consisting of a hydrogen atom and a methyl group and R.sup.8 is selected from the group consisting of a hydrogen atom, a C.sub.1-4 alkyl group, a phenyl group and a phenyl group substituted with at least one substituent selected from the group consisting of halogen, methyl and nitro substitutents;R.sup.3 is selected from the group consisting of a hydrogen atom, a methyl group, a hydroxy-protecting group, an ester-forming carboxylic acid residue, and an ester-forming carbonic acid residue; andR.sup.4 is selected from the group consisting of a hydrogen atom and an .alpha.-L-oleandrosyl-.alpha.-L-oleandrosyloxy group, with the proviso that R.sup.4 represents a hydrogen atom when the group R.sup.1 is selected from the group consisting of a methyl group, an ethyl group, and groups of formula --C(CH.sub.3).dbd.CHR.sup.5 in which R.sup.5 is selected from the group consisting of a methyl group, an ethyl group and an isopropyl group.

    Macrolide compounds, their preparation and their use
    7.
    发明授权
    Macrolide compounds, their preparation and their use 失效
    大环内酯类化合物，其制备及其用途

    公开(公告)号：US5212322A

    公开(公告)日：1993-05-18

    申请号：US644100

    申请日：1991-01-22

    申请人： Takao Okazaki ,  Shuji Takahashi ,  Seigo Iwado ,  Keiji Tanaka ,  Toshiaki Yanai ,  Hisaki Kajino

    发明人： Takao Okazaki ,  Shuji Takahashi ,  Seigo Iwado ,  Keiji Tanaka ,  Toshiaki Yanai ,  Hisaki Kajino

    IPC分类号： A01N49/00 ,  C07H19/01 ,  C12P17/18

    CPC分类号： C07H19/01 ,  A01N49/00 ,  C12P17/181 ,  Y02P20/55 ,  Y10S424/08

    摘要： Compounds with acaricidal, insecticidal and anthelmintic activities have the formula: ##STR1## wherein: --X--Y-- is selected from the group consisting of --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CHOH--, --CH.dbd.CH--, and --CH.sub.2 --C(.dbd.O)--;R.sup.1 is selected from the group consisting of a methyl group, an ethyl group, an isopropyl group, a sec-butyl group and groups of formula --C(CH.sub.3).dbd.CHR.sup.5 in which R.sup.5 is selected from the group consisting of a methyl group, an ethyl group and an isopropyl group;R.sup.2 represents a group of formula --(CH.sub.2).sub.n --C(R.sup.6).dbd.C(R.sup.7)(R.sup.8) in which n is 0, 1 or 2, R.sup.6 and R.sup.7 each is selected from the group consisting of a hydrogen atom and a methyl group and R.sup.8 is selected from the group consisting of a hydrogen atom, a C.sub.1-4 alkyl group, a phenyl group and a phenyl group substituted with at least one substituent selected from the group consisting of halogen, methyl and nitro substituents;R.sup.3 is selected from the group consisting of a hydrogen atom, a methyl group, a hydroxy-protecting group, an ester-forming carboxylic acid residue, and an ester-forming carbonic acid residue; andR.sup.4 is selected from the group consisting of a hydrogen atom and an .alpha.-L-oleandrosyl-.alpha.-L-oleandrosyloxy group, with the proviso that R.sup.4 represents a hydrogen atom when the group R.sup.1 is selected from the group consisting of a methyl group, an ethyl group, and groups of formula --C(CH.sub.3).dbd.CHR.sup.5 in which R.sup.5 is selected from the group consisting of a methyl group, an ethyl group and an isopropyl group.

    摘要翻译： 具有杀螨，杀虫和驱虫活性的化合物具有下式：其中：-XY-选自-CH 2 -CH 2 - ， - CH 2 -CHOH - ， - CH = CH-和 - CH2-C（= O） - ; R 1选自甲基，乙基，异丙基，仲丁基和式-C（CH 3）= CHR 5的基团，其中R 5选自甲基， 乙基和异丙基; R 2表示式 - （CH 2）n C（R 6）= C（R 7）（R 8）的基团，其中n为0,1或2，R 6和R 7各自为氢原子和甲基 并且R 8选自氢原子，C 1-4烷基，苯基和被至少一个选自卤素，甲基和硝基取代基的取代基取代的苯基; R3选自氢原子，甲基，羟基保护基，成酯羧酸残基和形成酯的碳酸残基; 并且R 4选自氢原子和α-L-甘氨酰基-α-L-胆碱基氧基，条件是当R 1选自甲基时，R 4表示氢原子 ，乙基和式-C（CH 3）= CHR 5基团，其中R 5选自甲基，乙基和异丙基。