Retinoid-like compounds
    65.
    发明授权
    Retinoid-like compounds 失效
    类视黄醇样化合物

    公开(公告)号:US6008251A

    公开(公告)日:1999-12-28

    申请号:US49430

    申请日:1998-03-27

    摘要: The present invention relates to a compound of the formula ##STR1## wherein X is --CONH-- or --NHCO--, or a nontoxic pharmaceutically acceptable salt, physiologically hydrolyzable ester or solvate thereof.The compounds of the present invention exhibit retinoid-like properties and are thus useful as antiinflammatory agents for chronic skin inflammatory diseases such as psoriasis and atopic dermatitis, as agents for the treatment of rheumatic diseases such as rheumatoid arthritis, as antitumor agents for the treatment of various tumors, and as agents for the treatment of non-malignant proliferative skin conditions.

    摘要翻译: 本发明涉及下式的化合物,其中X是-CONH-或-NHCO-,或其无毒的药学上可接受的盐,生理上可水解的酯或其溶剂化物。 本发明的化合物表现出类视黄醇样的性质,因此可用作慢性皮肤炎症性疾病如牛皮癣和特应性皮炎的抗炎剂,作为治疗风湿性疾病如类风湿性关节炎的药物,作为用于治疗 各种肿瘤,以及用于治疗非恶性增殖性皮肤病症的药剂。

    Method for controlling resistant fungi
    66.
    发明授权
    Method for controlling resistant fungi 失效
    防治真菌的方法

    公开(公告)号:US5891918A

    公开(公告)日:1999-04-06

    申请号:US877946

    申请日:1997-06-18

    CPC分类号: A01N37/50 A01N37/20

    摘要: A method for controlling phytopathogenic fungi is disclosed. The method uses a fungicidal composition which has been found to be effective against strains of fungi which are resistant to benzimidazole fungicides. When combined with one or more of benzimidazole, thiophanate, or dicarboximide fungicides, and applied to a mixed population of sensitive and resistant fungi, the fungicidal compound of the present invention is more effective against the mixed population of fungi than either of the fungicidal compounds alone.

    摘要翻译: 公开了一种控制植物病原真菌的方法。 该方法使用已被发现对抗苯扎莫尔杀真菌剂的真菌菌株有效的杀真菌组合物。 当与一种或多种苯并咪唑,硫菌灵或二甲酰亚胺杀真菌剂组合并施用于敏感和抗性真菌的混合群体时,本发明的杀真菌化合物对于混合真菌群体比单独的杀真菌化合物更有效 。

    Process to chloroketones using oxazolines
    67.
    发明授权
    Process to chloroketones using oxazolines 失效
    使用恶唑啉的氯代酮的方法

    公开(公告)号:US5859254A

    公开(公告)日:1999-01-12

    申请号:US58832

    申请日:1998-04-13

    摘要: This invention relates to a process for the preparation of an .alpha.-chloroketone compound comprising the steps of(i) cyclizing an alkynyl amide to form a 5-methyleneoxazoline ##STR1## (ii) chlorinating the 5-methyleneoxazoline using trichloroisocyanuric acid to produce a chlorinated oxazoline intermediate ##STR2## and (iii) hydrolyzing the chlorinated oxazoline intermediate with an aqueous acid to produce the desired monochloroketone ##STR3## wherein Z is alkyl or substituted alkyl, aryl or substituted aryl, heteroaryl or substituted heteroaryl or phenylene,R is a hydrogen atom or alkyl, andR.sup.1 and R.sup.2 are each independently an alkyl or substituted alkyl group, or R.sup.1 and R.sup.2 together with the carbon atom to which they are attached form a cyclic structure.Additionally, when R is a hydrogen atom, a dichloroketone can be conveniently formed through adjustment of reaction conditions.

    摘要翻译: 本发明涉及一种制备α-氯代酮化合物的方法,包括以下步骤:(i)使炔基酰胺环化以形成5-亚甲基恶唑啉(ii)使用三氯异氰脲酸氯化5-亚甲基恶唑啉以产生氯代 恶唑啉中间体+图像>和(iii)用含水酸水解氯代恶唑啉中间体以产生所需的单氯代酮其中Z是烷基或取代的烷基,芳基或取代的芳基,杂芳基或取代的杂芳基或亚苯基 R为氢原子或烷基,R 1和R 2各自独立地为烷基或取代的烷基,或者R 1和R 2与它们所连接的碳原子一起形成环状结构。 此外,当R是氢原子时,可以通过调整反应条件方便地形成二氯酮。

    Mammalian DNA topoisomerase II inhibitor and method
    70.
    发明授权
    Mammalian DNA topoisomerase II inhibitor and method 失效
    哺乳动物DNA拓扑异构酶II抑制剂和方法

    公开(公告)号:US5426224A

    公开(公告)日:1995-06-20

    申请号:US32867

    申请日:1993-03-18

    摘要: A novel antiproliferative drug and methods are disclosed. The drug has the general structural formula: ##STR1## where R1=OR.sub.1 ', SR.sub.1 ', or N(R.sub.1 'R.sub.1 ").sub.2, where R.sub.1 ' and R.sub.1 " are H or lower alkyl groups, and R.sub.2 is an acylamino, or aroylamino group. The compound is useful for inhibiting cell proliferation in drug-resistant tumor cells. Also disclosed is a method of chemical converting a colchicine derivative to form an active inhibitor of DNA topisomerase II.

    摘要翻译: 公开了一种新型抗增生药物和方法。 该药物具有以下通式结构式:其中R1 = OR1',SR1'或N(R1'R1“)2,其中R1'和R1”为H或低级烷基,R2为 是酰氨基或芳酰氨基。 该化合物可用于抑制耐药肿瘤细胞中的细胞增殖。 还公开了将秋水仙碱衍生物化学转化以形成DNA拓扑异构酶II的活性抑制剂的方法。