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    • 2. 发明授权
    • Aryl (sulfide, sulfoxide and sulfone) derivatives and drugs containing the same as the active ingredient
    • 芳基(硫醚,亚砜和砜)衍生物和含有与活性成分相同的药物
    • US06300514B1
    • 2001-10-09
    • US09214116
    • 1999-01-15
    • Kanji TakahashiTsuneyuki Sugiura
    • Kanji TakahashiTsuneyuki Sugiura
    • C07C32100
    • C07K5/0812C07C317/44C07C317/46C07C317/50C07C323/52C07C323/59C07C323/60C07K5/06078
    • Pharmaceutical composition containing aryl (sulfide, sulfoxide, sulfone) derivatives of the formula (1) and the salts thereof as active ingredient (wherein R1 is H, alkyl; R2 is COOR7, CONHOR8; E is —CONR9—, —NR9CO—, —OCO—,—COO—, —CH2—O—, —(CH2)2—, vinylene, ethynylene; J is bond, alkylene; A is H, alkyl, Ar, alkyl-OH ; R3, R4 is H, alkyl, COOR19, hydroxy, —NR20R21, Ar1 etc.); R5, R6 is H, methyl) and the novel aryl (sulfide, sulfoxide, sulfone) derivatives of the formula (I). The compounds of the formula (I) have inhibitory activity against matrix metalloproteinases, therefore, the compounds of the formula (I) are useful for prevention and/or treatment of rheumatoid diseases, arthrosteitis, unusual bone resorption, osteoporosis, periodontitis, interstitial nephritis, arteriosclerosis, pulmonary emphysema, cirrhosis, cornea injury, autoimmune diseases, diseases caused by vascular emigration or infiltration of leukocytes, arterialization etc.
    • 含有式(1)的芳基(硫醚,亚砜,砜)衍生物及其盐作为活性成分(其中R 1为H,烷基; R 2为COOR 7,CONHOR 8; E为-CONR 9 - , - NR 9 CO-, - OCO - , - COO-, - CH 2 -O - , - (CH 2)2 - ,亚乙烯基,亚乙炔基; J是键,亚烷基; A是H,烷基,Ar,烷基-OH; R 3,R 4是H,烷基, COOR 19,羟基,-NR 20 R 21,Ar 1等); R5,R6是H,甲基)和式(Ⅰ)的新型芳基(硫醚,亚砜,砜)衍生物。式(I)化合物对基质金属蛋白酶具有抑制活性,因此式 I)可用于预防和/或治疗类风湿病,关节炎,异常骨吸收,骨质疏松症,牙周炎,间质性肾炎,动脉硬化,肺气肿,肝硬化,角膜损伤,自身免疫性疾病,血管迁移或白细胞浸润引起的疾病, 动脉化等