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19 条记录 (耗时 0.018 秒)

    ML-236B Derivatives
    2.
    发明授权
    ML-236B Derivatives 失效
    ML-236B衍生物

    公开(公告)号：US4447626A

    公开(公告)日：1984-05-08

    申请号：US395968

    申请日：1982-07-07

    申请人： Akira Terahara ,  Minoru Tanaka

    发明人： Akira Terahara ,  Minoru Tanaka

    IPC分类号： A61K31/215 ,  A61K31/22 ,  A61K31/35 ,  A61K31/351 ,  A61K31/365 ,  A61P3/06 ,  C07C69/33 ,  C07C69/732 ,  C07D309/30 ,  C12P7/62 ,  C12P17/06 ,  C12R1/645 ,  C12R1/65

    CPC分类号： C12R1/645 ,  C07D309/30 ,  C12P17/06

    摘要： A compound of formula (I): ##STR1## (called 6-methoxy-IsoML-236B lactone) and its corresponding free hydroxy-carboxylic acid and salts and esters of said acid may be prepared by the enzymatic alkoxylation of an ML-236B compound, preferably using a microorganism of the genus Syncephalastrum, Absidia or Cunninghamella, e.g. Absidia coerulea, or a cell-free enzyme-containing extract from said microorganism. If desired, the lactone or carboxylic acid may be converted by conventional salification or esterification techniques to the desired salt or ester. These compounds have the ability to inhibit the biosynthesis of cholesterol and are thus of value in the treatment of hypercholesteraemia, for which purpose they may be formulated as compositions in admixture with conventional pharmaceutical carriers or diluents.

    摘要翻译： 式（I）化合物：可以通过ML-236B化合物的酶促烷氧基化来制备所述酸的“IMAGE”（称为6-甲氧基-IlyML-236B内酯）及其相应的游离羟基羧酸及其盐和酯 ，优选使用Syncephalastrum，Absidia或Cunninghamella属的微生物，例如， 或者来自所述微生物的无细胞的含酶提取物。 如果需要，内酯或羧酸可以通过常规的成盐或酯化技术转化成所需的盐或酯。 这些化合物具有抑制胆固醇生物合成的能力，因此在治疗高胆固醇血症方面具有价值，为此，它们可以配制成与常规药物载体或稀释剂混合的组合物。

    MB-530B derivatives containing them
    4.
    发明授权
    MB-530B derivatives containing them 失效
    含有它们的MB-530B衍生物

    公开(公告)号：US4820865A

    公开(公告)日：1989-04-11

    申请号：US908969

    申请日：1986-09-17

    申请人： Akira Terahara ,  Minoru Tanaka

    发明人： Akira Terahara ,  Minoru Tanaka

    IPC分类号： C12P17/06 ,  A61K31/35 ,  A61K31/351 ,  A61P3/06 ,  C07C51/00 ,  C07C59/60 ,  C07C67/00 ,  C07C69/734 ,  C07D309/30 ,  C12P7/40 ,  C12P7/42 ,  C12P7/62 ,  C12R1/785 ,  C07C67/02

    CPC分类号： C07D309/30

    摘要： Compounds of formula (I): ##STR1## wherein R.sup.1 represents a group of formula ##STR2## or a group of formula ##STR3## (wherein R.sup.2 represents a C.sub.1 --C.sub.10 alkyl group) and their corresponding free hydroxy-carboxylic acids and salts and esters of said acids may be prepared by the enzymatic hydroxylation of an MB-530B compound (which may be the lactone, the carboxylic acid or a salt or ester of MB-530B or a corresponding compound in which the 2-methylbutyryloxy group at the 1-position of these compounds has been replaced by another C.sub.2 --C.sub.11 acyloxy group), preferably using a microorganism of the genus Syncephalastrum, Mucor, Rhizopus, Zygorinchus, Circinella, Actinomucor, Gongronella, Phycomyces, Streptomyces, Absidia, Cunninghamella, Mortierella, Pycnoporus or Rhizoctonia, or a cell-free enzyme-containing extract from the microorganism. If desired, the lactone or carboxylic acid may be converted by conventional salification or esterification techniques to the desired salt or ester and the salt or ester may be converted to the parent lactone or acid. These compounds have the ability to inhibit the biosynthesis of cholesterol and are thus of value in the treatment of hypercholesteraemia, for which purpose they may be formulated as compositions in admixture with conventional pharmaceutical carriers or diluents.

    M-4 And IsoM-4 derivatives and compositions containing them
    5.
    发明授权
    M-4 And IsoM-4 derivatives and compositions containing them 失效
    M-4和含有它们的IsoM-4衍生物和组合物

    公开(公告)号：US4451481A

    公开(公告)日：1984-05-29

    申请号：US375333

    申请日：1982-05-05

    申请人： Akira Terahara ,  Minoru Tanaka

    发明人： Akira Terahara ,  Minoru Tanaka

    IPC分类号： A61K31/22 ,  A61K31/35 ,  A61K31/351 ,  A61K31/365 ,  A61P3/06 ,  C07C69/28 ,  C07D309/30

    CPC分类号： C07D309/30

    摘要： Dihydro-M-4 and dihydro-IsoM-4 are new compounds which may be prepared by the catalytic hydrogenation of M-4 or IsoM-4 respectively. They, and their salts and esters (which may be prepared by conventional salification or esterification reactions with the parent dihydro-M-4 or dihydro-IsoM-4), are capable of inhibiting cholesterol biosynthesis in the liver and may be formulated, for therapeutic use, with conventional pharmaceutical carriers or diluents.

    摘要翻译： 二氢-M-4和二氢-MlyM-4是可以分别通过M-4或IsoM-4的催化氢化制备的新化合物。 它们及其盐和酯（其可以通过与亲本二氢M-4或二氢-MlyM-4的常规盐化或酯化反应制备）能够抑制肝脏中的胆固醇生物合成并且可以配制用于治疗 与常规药物载体或稀释剂一起使用。

    ML-236B Derivatives
    7.
    发明授权
    ML-236B Derivatives 失效
    ML-236B衍生物

    公开(公告)号：US4448979A

    公开(公告)日：1984-05-15

    申请号：US351975

    申请日：1982-02-24

    申请人： Akira Terahara ,  Minoru Tanaka

    发明人： Akira Terahara ,  Minoru Tanaka

    IPC分类号： C07C69/03 ,  C07D309/30 ,  C12P7/62 ,  C12P17/06

    CPC分类号： C12R1/465 ,  C07D309/30 ,  C12P17/06 ,  C12P7/62 ,  C12R1/645 ,  C12R1/65 ,  C12R1/785 ,  C12R1/845 ,  Y10S435/886

    摘要： Compounds of formula (I): ##STR1## (wherein R represents a group of formula ##STR2## and the corresponding ring-closed lactones, salts (especially alkali metal salts) and esters (especially C.sub.1 -C.sub.5 alkyl esters) thereof may be prepared by subjecting ML-236B, or ML-236B carboxylic acid or a salt or ester thereof to enzymatic hydroxylation, which may be effected by means of microorganisms of the genera Mucor, Rhizopus, Zygorynchus, Circinella, Actinomucor, Gongronella, Phycomyces, Martierella, Pycnoporus, Rhizoctonia, Absidia, Cunninghamella, Syncephalastrum and Streptomyces, or cell-free, enzyme-containing extracts from said microorganisms. The compounds are capable of inhibiting biosynthesis of cholesterol and are thus useful in the treatment of hypercholesteraemia.

    摘要翻译： 式（I）的化合物：其中R表示式（Ⅰ）的基团或相应的闭环内酯，盐（特别是碱金属盐）和酯（特别是C 1 -C 5） 烷基酯）可以通过使ML-236B或ML-236B羧酸或其盐或酯进行酶羟基化来制备，其可以通过毛霉属，根霉属，丝状芽孢杆菌属，圆弧菌属，放线菌属， Gongronella，Phycomyces，Martierella，Pycnoporus，Rhizoctonia，Absidia，Cunninghamella，Syncephalastrum和Streptomyces，或来自所述微生物的无细胞的含酶提取物，这些化合物能够抑制胆固醇的生物合成，因此可用于治疗高胆固醇血症。

    ML-236B Derivatives and their preparation
    8.
    发明授权
    ML-236B Derivatives and their preparation 失效
    ML-236B衍生物及其制备方法

    公开(公告)号：US4346227A

    公开(公告)日：1982-08-24

    申请号：US270846

    申请日：1981-06-05

    申请人： Akira Terahara ,  Minoru Tanaka

    发明人： Akira Terahara ,  Minoru Tanaka

    IPC分类号： C07C69/03 ,  C07D309/30 ,  C12P7/62 ,  C12P17/06 ,  C07C69/013

    CPC分类号： C12R1/465 ,  C07D309/30 ,  C12P17/06 ,  C12P7/62 ,  C12R1/645 ,  C12R1/65 ,  C12R1/785 ,  C12R1/845 ,  Y10S435/886

    摘要： Compounds of formula (I): ##STR1## (wherein R represents a group of formula ##STR2## and the corresponding ring-closed lactones, salts (especially alkali metal salts) and esters (especially C.sub.1 -C.sub.5 alkyl esters) thereof may be prepared by subjecting ML-236B, or ML-236B carboxylic acid or a salt or ester thereof to enzymatic hydroxylation, which may be effected by means of microorganisms of the genera Mucor, Rhizopus, Zygorynchus, Circinella, Actinomucor, Gongronella, Phycomyces, Martierella, Pycnoporus, Rhizoctonia, Absidia, Cunninghamella, Syncephalastrum and Streptomyces, or cell-free, enzyme-containing extracts from said microorganisms. The compounds are capable of inhibiting biosynthesis of cholesterol and are thus useful in the treatment of hypercholesteraemia.

    摘要翻译： 式（I）的化合物：其中R表示式（Ⅰ）的基团和相应的闭环内酯，盐（特别是碱金属盐）和酯（特别是C 1 -C 5烷基 酯）可以通过使ML-236B或ML-236B羧酸或其盐或酯进行酶羟基化来制备，其可以通过毛霉属，根霉属，Zygorynchus，Circinella，Actinomucor，Gongronella ，Phycomyces，Martierella，Pycnoporus，Rhizoctonia，Absidia，Cunninghamella，Syncephalastrum和Streptomyces，或来自所述微生物的无细胞的含酶提取物，这些化合物能够抑制胆固醇的生物合成，因此可用于治疗高胆固醇血症。