Metalloproteinase inhibitors
    1.
    发明授权
    Metalloproteinase inhibitors 失效
    金属蛋白酶抑制剂

    公开(公告)号:US06310084B1

    公开(公告)日:2001-10-30

    申请号:US09424290

    申请日:2000-02-11

    IPC分类号: C07C22904

    摘要: The present invention relates to therapeutically active hydroxamic acid, N-formyl-N-hydroxyamino and carboxylic acid derivatives, their preparation, and pharmaceutical compositions containing them. These compounds are useful in the inhibition of metalloproteases, such as stromelysin, gelatinase, matrilysin, and collagenase. These compounds are useful in the treatment of mammals having disease-states alleviated by the inhibition of such matrix metalloproteases.

    摘要翻译: 本发明涉及治疗活性的异羟肟酸,N-甲酰基-N-羟基氨基和羧酸衍生物,其制备方法和含有它们的药物组合物。 这些化合物可用于抑制金属蛋白酶,例如溶基质溶解素,明胶酶,基质溶素和胶原酶。 这些化合物可用于治疗通过抑制这种基质金属蛋白酶减轻疾病的哺乳动物。

    Method for producing long-chain glycine-N,N-diacetic acid derivatives
    3.
    发明授权
    Method for producing long-chain glycine-N,N-diacetic acid derivatives 失效
    制备长链甘氨酸-N,N-二乙酸衍生物的方法

    公开(公告)号:US06420593B2

    公开(公告)日:2002-07-16

    申请号:US09875995

    申请日:2001-06-08

    IPC分类号: C07C22904

    摘要: A process for preparing compounds of the formula IIb  where R is C6-C30-alkyl or C6-C30-alkenyl, which may additionally have upto 5 hydroxyl groups, formyl groups, C1-C4-alkoxy groups, phenoxy groups or C1-C4-alkoxycarbonyl groups as substituents and may be interrupted by upto 5 nonadjacent oxygen atoms, or alkoxylate groups of the formula —(CH2)k—O—(A1O)m—(A2O)n—Y where A1 and A2 are, independently of one another, 1,2-alkylene groups having 2 to 4 carbon atoms, Y is hydrogen, C1-C12-alkyl, phenyl or C1-C4-alkoxycarbonyl, and k is 1, 2 or 3, and m and n are each numbers from 0 to 50, and the total of m+n must be at least 4, by reacting iminodiacetonitrile with aldehydes of the formula R—CHO and HCN or alkali metal cyanides, the process being carried out a) in the absence of an organic solvent and in the presence of a Lewis or Brönsted acid, or b) in the presence or absence of an organic solvent and in the presence of an emulsifier, or c) in the presence or absence of an organic solvent and under a pressure in the range from 1 to 40 bar.

    摘要翻译: 制备式IIb化合物的方法,其中R是C 6 -C 30 - 烷基或C 6 -C 30烯基,其可另外具有多达5个羟基,甲酰基,C 1 -C 4 - 烷氧基,苯氧基或C 1 -C 4 - 烷氧基羰基作为取代基,并且可以被至多5个不相邻的氧原子间隔或式 - (CH2)kO-(A1O)m-(A2O)nY的烷氧基化物,其中A1和A2彼此独立地为1,2 具有2至4个碳原子的亚烷基,Y是氢,C 1 -C 12 - 烷基,苯基或C 1 -C 4 - 烷氧基羰基,k是1,2或3,m和n各自为0至50, 通过使亚氨基二乙腈与式R-CHO和HCN或碱金属氰化物的醛反应,所述m + n的总和必须至少为4,该方法在不存在有机溶剂的情况下进行,并且在Lewis的存在下 或布朗斯台德酸,环)在存在或不存在有机溶剂的情况下和在乳化剂orc的存在下)在存在或不存在有机溶剂的情况下 在1至40巴的压力范围内。