Cyclohexanol derivatives, production and use thereof
    3.
    发明公开
    Cyclohexanol derivatives, production and use thereof 失效
    Cyclohexanolderivate,ihre Herstellung und ihre Verwendung。

    公开(公告)号:EP0415294A2

    公开(公告)日:1991-03-06

    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.

    摘要翻译: 本发明涉及下式化合物:其中A为卤素,N(O)m R 1 R 2,N(R)R 1 R 2 R 3, ,X(=),S(O)nR 1或S((+))(O)m R 1 R 2,X( - ))其中R 1,R 2 >和R 3各自是任选取代的烃或杂环基,X'( - )>是抗衡阴离子; m为0或1的整数; n为0〜2的整数, R 1和R 2可以形成含氮或含硫杂环,其可以与相邻的氮原子或硫原子进一步形成稠环,并且这些含氮或含硫杂环 环可以具有取代基,B是O或NR 4,其中R 4是氢或任选取代的低级烷基或芳基,D是2-甲基-1-丙烯基或异丁基,E是氢, 任选取代的烃或任选取代的酰基; 条件是当A是氯时,E是除二硝基苯甲酰基以外的任选取代的烃或酰基,其盐,其制备和用途。 本发明的新型环己醇衍生物具有血管生成抑制活性和抗肿瘤活性,并且它们用作抗风湿剂,牛皮癣治疗剂,糖尿病性视网膜病变的治疗剂和抗肿瘤剂。

    Imidazole derivatives as glutaminose inhibitors
    5.
    发明公开
    Imidazole derivatives as glutaminose inhibitors 失效
    咪唑啉酮谷氨酰胺酶。

    公开(公告)号:EP0656210A1

    公开(公告)日:1995-06-07

    申请号:EP94118069.7

    申请日:1994-11-16

    IPC分类号: A61K31/415 C07D233/88

    CPC分类号: C07D233/88 A61K31/415

    摘要: There is disclosed a pharmaceutical composition for inhibiting glutaminase which comprises a imidazole derivative or a salt thereof. This compound selectively inhibits the proliferation of tumor cells, and the composition is useful as an anti-cancer agent. There is also disclosed a novel imidazole derivative having glutaminase inhibitory activity.

    摘要翻译: 公开了一种抑制谷氨酰胺酶的药物组合物,其包含咪唑衍生物或其盐。 该化合物选择性地抑制肿瘤细胞的增殖,该组合物可用作抗癌剂。 还公开了具有谷氨酰胺酶抑制活性的新型咪唑衍生物。

    Cyclohexanol derivatives, production and use thereof
    7.
    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-Amino-6-desoxyfumagillols, production and use thereof
    8.
    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。