Naphthopyran derivatives and use thereof
    7.
    发明公开
    Naphthopyran derivatives and use thereof 失效
    萘并吡喃衍生物及其用途

    公开(公告)号:EP0337413A2

    公开(公告)日:1989-10-18

    申请号:EP89106450.3

    申请日:1989-04-12

    IPC分类号: C07D311/92 A61K31/35

    CPC分类号: C07D311/92

    摘要: The present invention relates to an aromatase inhibiting composition which contains a compound of the formula:
    wherein R is hydroxy, lower alkoxy or amino which may be substituted by lower alkyl; R¹ is hydrogen or lower alkyl; and A is hydrogen, a group of the formula
    in which R² is hydroxy, lower alkoxy or amino which may be substituted by lower alkyl and R³ is hydrogen or lower alkyl, or a group of the formula
    in which R⁴ and R⁵ are independently hydrogen or lower alkyl, or a salt thereof.
    The present composition is useful in the prevention and treatment of estrogen-dependent diseases, such as breast cancer.

    摘要翻译: 本发明涉及芳香酶抑制组合物,其含有下式化合物:其中R为羟基,低级烷氧基或可被低级烷基取代的氨基; R 1是氢或低级烷基; A为氢,下式基团其中R 2为羟基,低级烷氧基或可被低级烷基取代的氨基,R 3为氢或低级烷基,或下式基团其中R 4和R 5独立地为氢或 低级烷基或其盐。 本发明组合物可用于预防和治疗雌激素依赖性疾病,例如乳腺癌。

    Production of optically active compounds
    8.
    发明公开
    Production of optically active compounds 失效
    Herstellung optisch aktiver Verbindungen

    公开(公告)号:EP0710725A1

    公开(公告)日:1996-05-08

    申请号:EP95117120.6

    申请日:1995-10-31

    IPC分类号: C12P41/00

    摘要: A process for producing an optically active form of a compound of formula (I)

    wherein R₁ represents hydrogen or a hydrocarbon group that may be substituted; R₂ and R₃ independently represent hydrogen, a hydrocarbon group that may be substituted, or a heteroaromatic group that may be substituted; X' represents a substituent comprising an esterified carboxyl group or an acylated hydroxyl group; ring A represents a benzene ring that may be substituted or a heteroaromatic ring that may be substituted; ring J' represents a 7- or 8-membered heterocyclic ring containing at most 3 hetero-atoms as ring-constituent members, which may have a further substituent or substituents in addition to R₁, R₂, R₃ and X', and C* denotes a chiral carbon atom or a salt thereof, which comprises subjecting the racemic compound of the formula (I) or a salt thereof, or alternatively a racemic starting compound for synthesizing the compound of the formula (I) to enzymatically enantioselective hydrolysis to provide an optically active form thereof.

    摘要翻译: 一种制备光学活性形式的式(I)化合物的方法其中R 1表示氢或可被取代的烃基; R2和R3独立地表示氢,可被取代的烃基或可被取代的杂芳族基; X'表示包含酯化羧基或酰化羟基的取代基; 环A表示可被取代的苯环或可被取代的杂芳环; 环J'表示含有至多3个杂原子作为环构成成员的7或8元杂环,除R1,R2,R3和X'之外,还可以具有另外的取代基或取代基,C *表示 其包括使式(I)的外消旋化合物或其盐或外消旋起始化合物合成式(I)化合物进行酶对映选择性水解以提供光学 其活性形式。

    Physiologically active substance fa-4283, its derivatives and production thereof
    9.
    发明公开
    Physiologically active substance fa-4283, its derivatives and production thereof 失效
    Physiologisch aktive Substanz FA-4283,Derivate und ihre Herstellung。

    公开(公告)号:EP0259811A2

    公开(公告)日:1988-03-16

    申请号:EP87113012.6

    申请日:1987-09-05

    摘要: The present invention relates to a compound FA-4283 or its derivative of the formula:
    wherein R is hydrogen or lower alkyl, and 3,4-and 3',4'-double bonds may be saturated with hydrogens, and the method of production thereof.
    The compound (I) of the invention has an action of inhibiting fatty acid synthesis, thus being useful as an agent for prophylaxis.improvement of disorders of glucose and lipid methabolism.

    摘要翻译: 本发明涉及化合物FA-4283或其衍生物,其分子式为:CHEM,其中R为氢或低级烷基,3,4-和3',4'-双键可用氢饱和, 生产方法。 本发明的化合物(I)具有抑制脂肪酸合成的作用,因此可用作预防药物,改善葡萄糖和脂质代谢紊乱的病症。

    Physiologically active substance FA-5859, its derivative; their production and antidiabetic agents containing said compounds
    10.
    发明公开
    Physiologically active substance FA-5859, its derivative; their production and antidiabetic agents containing said compounds 失效
    生理活性化合物FA-5898,其衍生物,以及含有这些化合物的抗糖尿病剂的制备。

    公开(公告)号:EP0080695A1

    公开(公告)日:1983-06-08

    申请号:EP82110866.9

    申请日:1982-11-24

    摘要: Physiologically active substance FA-5859 and its deacetyl compound represented by the formula:
    wherein R, is a hydrogen atom or an acetyl group, are produced by a cultivation of a microorganism of the genus Emericelle or Aspergillus (compound wherein R, is an acetyl group) or by a method of chemical synthesis (compound wherein R, is a hydrogen atom or an acetyl group).
    Said compounds or a salt thereof have excellent fatty acid degradation inhibiting activity and is useful as an antidiabetic agent in mammalian animals or as a biochemical reagent for studies on fatty acid metabolism.

    摘要翻译: 生理活性物质FA-5859和由下式表示其脱乙酰基化合物: worin R1是氢原子或乙酰基,是由属的微生物的培养产生裸胞壳或曲霉属(化合物worin R1为乙酰 基团)或通过化学合成的方法(化合物worin R1是氢原子或乙酰基)。 所述化合物或其盐具有优异的脂肪酸抑制降解活性和可用作在哺乳动物抗糖尿病药或作为用于对脂肪酸代谢研究的生物化学试剂。