Cyclohexanol derivatives, production and use thereof
    4.
    发明公开
    Cyclohexanol derivatives, production and use thereof 失效
    环辛醇衍生物,生产和使用

    公开(公告)号:EP0415294A3

    公开(公告)日:1991-06-12

    申请号:EP90116309.7

    申请日:1990-08-25

    摘要: The present invention relates to a compound of the formula:
    wherein A is halogen, N(O)mR¹R², N ⊕ R¹R²R³·X ⊖ , S(O)nR¹ or S ⊕ (O)mR¹R²·X ⊖ where R¹,R² and R³ are each optionally substituted hydrocarbon or heterocyclic group, X ⊖ is a counter anion; m is an integer of 0 or 1; n is an integer of 0 to 2; R¹ and R² may form a nitrogen-­containing or a sulfur-containing heterocyclic ring, which may further form a condensed ring, with the adjacent nitrogen atom or sulfur atom, and these nitrogen-containing or sulfur-containing heterocyclic rings may have substituents, B is O or NR⁴ where R⁴ is hydrogen or an optionally substituted lower alkyl or aryl group, D is 2-methyl-1-propenyl group or isobutyl group, and E is hydrogen, an optionally substituted hydrocarbon or an optionally substituted acyl group; provided that, when A is chlorine, E is an optionally substituted hydrocarbon or acyl excepting dinitrobenzoyl, a salt thereof, production and use thereof. The novel cyclohexanol derivatives of the present invention have angiogenesis inhibiting activity and anti-tumor activity, and they are used as anti-­rheumatic agents, therapeutic agents of psoriasis, therapeutic agents of diabetic retinopathy and anti-­tumor agents.

    6-Epifumagillols, production and use thereof
    5.
    发明公开
    6-Epifumagillols, production and use thereof 失效
    6-Epifumagillole,ihre Herstellung und ihre Verwendung。

    公开(公告)号:EP0387650A1

    公开(公告)日:1990-09-19

    申请号:EP90104177.2

    申请日:1990-03-03

    CPC分类号: C07D303/22 C07D405/12

    摘要: The present invention relates to a compound of the formula:
    wherein R¹ is 2-methyl-1-propenyl group or isobutyl group; R² is hydrogen atom, an optionally substituted aliphatic hydrocarbon residue or an optionally substituted acyl group or a salt thereof.
    The compound (I) of the invention has, among others, angiogenesis inhibiting activity, cell-­proliferation inhibiting activity and immune reaction inhibiting activity, thus being useful as medicines, etc.

    摘要翻译: 本发明涉及下式的化合物:其中R 1为2-甲基-1-丙烯基或异丁基; R 2是氢原子,任选取代的脂族烃残基或任选取代的酰基或其盐。 本发明的化合物(I)具有血管生成抑制活性,细胞增殖抑制活性和免疫反应抑制活性,因此可用作药物等。

    6-Amino-6-desoxyfumagillols, production and use thereof
    6.
    发明公开
    6-Amino-6-desoxyfumagillols, production and use thereof 失效
    6-Amino-6-desoxyfumagillole,ihre Herstellung und ihre Verwendung。

    公开(公告)号:EP0386667A1

    公开(公告)日:1990-09-12

    申请号:EP90104176.4

    申请日:1990-03-03

    CPC分类号: C07D405/04 C07D303/36

    摘要: The present invention relates to a compound of the formula:
    wherein R¹ is 2-methyl-1-propenyl group or isobutyl group; R² and R³ are each hydrogen atom, an optionally substituted hydrocarbon residue or an optionally substituted acyl group or R² and R³ may form a ring together with the adjacent nitrogen atom; and the bonding mark ∼ means α-linkage or β-linkage, or a salt thereof.
    The compound (I) of the present invention has, among others, angiogenesis inhibiting activity, cell-­growth inhibiting activity and immune reaction inhibiting activity, thus being useful as medicines, etc.

    摘要翻译: 本发明涉及下式的化合物:其中R 1为2-甲基-1-丙烯基或异丁基; R 2和R 3各自为氢原子,任选取代的烃残基或任选取代的酰基,或R 2和R 3可以与相邻的氮原子一起形成环; 并且粘合标记是指α-链接或β-连接,或其盐。 本发明的化合物(I)具有血管生成抑制活性,细胞生长抑制活性和免疫反应抑制活性,作为药物等有用。

    A method for producing thiazolidinedione derivatives
    8.
    发明公开
    A method for producing thiazolidinedione derivatives 失效
    Verfahren zur Herstellung von Thiazolidinedion-Derivaten。

    公开(公告)号:EP0257781A1

    公开(公告)日:1988-03-02

    申请号:EP87306425.7

    申请日:1987-07-20

    CPC分类号: C07D213/30 C07D417/12

    摘要: A compound of the formula:
    (wherein R¹ is hydrogen or a lower alkyl) can be produced advantageously by (1) reacting a compound of the formula:
    (wherein R¹ has the meaning given above) with a halogenating agent or sulfonyl halide to give a compound of the formula:
    (wherein R¹ has the meaning given above and X is a halogen or an alkyl- or aryl-sulfonyloxy), (2) reacting the resulting compound with a compound of the formula:
    to give a compound of the formula:
    (wherein R¹ has the meaning given above), (3) reacting the resulting compound with a compound of the formula:
    to give a compound of the formula:
    (wherein R¹ has the meaning given above), and (4) subjecting the resulting compound to catalytic reduction.

    摘要翻译: 下式化合物:其中R 1为氢或低级烷基可有利地通过以下方式制备:(1)使下式化合物:其中R 1具有给定的含义 (其中R 1具有上面给出的含义,X是卤素或烷基 - 或芳基 - 磺酰氧基),(2)使式(III)化合物与式 所得化合物与下式化合物反应,得到下式化合物:其中R 1具有上述含义,(3)使所得化合物与式 :,得到下式的化合物:其中R 1具有上述含义。(4)使所得化合物进行催化还原。

    Thiazolidinedione derivatives, their production and use
    9.
    发明公开
    Thiazolidinedione derivatives, their production and use 失效
    Thiazolidindion-Derivate,deren Herstellung und Anwendung。

    公开(公告)号:EP0193256A1

    公开(公告)日:1986-09-03

    申请号:EP86300220.0

    申请日:1986-01-15

    CPC分类号: C07D213/30 C07D417/12

    摘要: Thiazolidinedione derivatives of the formula:
    or pharmacologically acceptable salts thereof are novel compounds, which exhibit in mammals blood sugar- and lipid- lowering activity, and are of value as a therapeutic agent for diabetes and therapeutic agent for hyperlipemia.

    摘要翻译: 下式的噻唑烷二酮衍生物或其药理学上可接受的盐是新兴化合物,其表现出哺乳动物的血糖和降脂活性,并且作为糖尿病治疗剂和高脂血症治疗剂具有价值。