利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

19 条记录 (耗时 0.022 秒)

    3,5-Dihydroxypentanoic ester derivatives having antihyperlipaemic activity
    2.
    发明授权
    3,5-Dihydroxypentanoic ester derivatives having antihyperlipaemic activity 失效
    具有抗高血脂活性的3,5-二羟基戊酸酯衍生物

    公开(公告)号：US4248889A

    公开(公告)日：1981-02-03

    申请号：US088619

    申请日：1979-10-26

    申请人： Hidehiko Oka ,  Akira Terahara ,  Akira Endo

    发明人： Hidehiko Oka ,  Akira Terahara ,  Akira Endo

    IPC分类号： C07C69/712 ,  A61K31/215 ,  A61K31/22 ,  A61P3/06 ,  C07C67/30 ,  C07C69/73 ,  C07C69/732

    CPC分类号： C07C67/30

    摘要： 3,5-Dihydroxypentanoic ester derivatives of formula (I): ##STR1## wherein: A represents an alkylene group which is optionally substituted by one or more alkyl groups, or an alkenylene group;Z represents a substituted or unsubstituted aryl or aryloxy group; andR represents a C.sub.1 -C.sub.4 alkyl group) may be prepared by reacting a dianion of an acetoacetic ester with an aldehyde of formula Z-A-CHO (wherein A and Z are as defined above) and then reducing the resulting compound. These 3,5-dihydroxypentanoic ester derivatives have antihyperlipaemic activity and are thus valuable pharmaceuticals.

    摘要翻译： （I）的3,5-二羟基戊酸酯衍生物：其中：A表示任选被一个或多个烷基或亚烯基取代的亚烷基; Z表示取代或未取代的芳基或芳氧基; 和R表示C1-C4烷基）可以通过使乙酰乙酸酯的二价阴离子与式Z-A-CHO的醛（其中A和Z如上定义）反应然后还原所得化合物来制备。 这些3,5-二羟基戊酸酯衍生物具有抗高血脂活性，因此是有价值的药物。

    4-Hydroxy-2-pyrone derivatives having antihyperlipaemic activity
    4.
    发明授权
    4-Hydroxy-2-pyrone derivatives having antihyperlipaemic activity 失效
    具有抗高血脂活性的4-羟基-2-吡喃酮衍生物

    公开(公告)号：US4255444A

    公开(公告)日：1981-03-10

    申请号：US88621

    申请日：1979-10-26

    申请人： Hidehiko Oka ,  Akira Terahara ,  Akira Endo

    发明人： Hidehiko Oka ,  Akira Terahara ,  Akira Endo

    IPC分类号： C07D309/30 ,  A61K31/365

    CPC分类号： C07D309/30

    摘要： 4-Hydroxy-2-pyrone derivatives of formula (I): ##STR1## (wherein A represents an alkylene group which is optionally alkyl-substituted or an alkenylene group, and Z represents a substituted or unsubstituted aryl or aryloxy group) may be prepared by cyclizing an ester of formula (II): ##STR2## (wherein A and Z are as defined above and R represents an organic group) and have valuable antilipaemic activities.

    摘要翻译： （I）的4-羟基-2-吡喃酮衍生物：其中（A表示任选烷基取代或亚烯基的亚烷基，Z表示取代或未取代的芳基或芳氧基） 可以通过使式（II）的酯环化来制备：其中A和Z如上定义，R代表有机基团，并且具有有价值的抗血脂活性。

    ML-236B Derivatives
    7.
    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
    9.
    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
    10.
    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。