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    • 1. 发明申请
    • ARYL (SULFIDE, SULFOXIDE AND SULFONE) DERIVATIVES AND DRUGS CONTAINING THE SAME AS THE ACTIVE INGREDIENT
    • ARYL(SULFIDE,SULFOXIDE AND SULFONE)衍生物和含有它们的药物作为活性成分
    • WO1997049679A1
    • 1997-12-31
    • PCT/JP1997002200
    • 1997-06-25
    • ONO PHARMACEUTICAL CO., LTD.TAKAHASHI, KanjiSUGIURA, Tsuneyuki
    • ONO PHARMACEUTICAL CO., LTD.
    • C07C317/44
    • C07D263/57C07C317/44C07C317/46C07C317/48C07C317/50C07C323/52C07C323/59C07C323/60C07D233/18C07D333/24C07D409/12C07D413/12
    • Novel aryl (sulfide, sulfoxide and sulfone) derivatives represented by general formula (I) or salts thereof; and drugs containing the same as the active ingredient wherein R represents H or alkyl; R represents COOR or CONHOR ; E represents -CONR -, -NR CO-, -OCO-, -COO-, -CH2-O-, -(CH2)2-, vinylene or ethynylene; J represents a single bond or alkylene; A represents H, alkyl, Ar or alkyl -OH; R and R represent each H, alkyl, COOR , hydroxy, -NR R , (a), Ar , etc.; and R and R represent each H or methyl. These compounds inhibit matrix metalloproteinases and are useful in preventing and/or treating various diseases such as rheumatism, osteoarthritis, pathologic bone resorption, osteoporosis, periodontal diseases, interstitial nephritis, arteriosclerosis, pulmonary emphysema, hepatic cirrhosis, corneal injury, autoimmune diseases, diseases caused by the liberation or infiltration of leukocytic cells into blood vessels, and neovascularization.
    • 由通式(I)表示的新型芳基(硫醚,亚砜和砜)衍生物或其盐; 和含有与活性成分相同的药物,其中R 1表示H或烷基; R 2表示COOR 7或CONHOR 8; E表示-CONR 9 - ,-NR 9 CO - , - OCO - , - COO - , - CH 2 -O - , - (CH 2)2 - ,亚乙烯基或亚乙炔基; J表示单键或亚烷基; A表示H,烷基,Ar或烷基-OH; R 3和R 4分别表示H,烷基,COOR 19,羟基,-NR 20 R 21,(a),Ar 1等。 R 5和R 6各自表示H或甲基。 这些化合物抑制基质金属蛋白酶,并且可用于预防和/或治疗各种疾病如风湿病,骨关节炎,病理性骨吸收,骨质疏松症,牙周病,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,引起的疾病 通过白血球细胞的释放或浸润进入血管和新血管形成。
    • 3. 发明申请
    • PHENYLSULFONAMIDE DERIVATIVES
    • 苯磺酰胺衍生物
    • WO1997045402A1
    • 1997-12-04
    • PCT/JP1997001735
    • 1997-05-23
    • ONO PHARMACEUTICAL CO., LTD.TAKAHASHI, KanjiSUGIURA, Tsuneyuki
    • ONO PHARMACEUTICAL CO., LTD.
    • C07C311/00
    • C07D213/42C07C311/19C07C311/29C07C311/53C07D207/16C07D209/20C07D213/52C07D231/12C07D233/56C07D249/08
    • Phenylsulfonylamide derivatives represented by general formula (I) and salts thereof, (wherein R is hydrogen or alkyl; R is COOR or CONHOR ; E is vinylene or ethylene; A is hydrogen, alkyl, carbocycle or heterocycle; J is single bond or alkylene; R and R are each hydrogen, (substituted) alkyl, COR , carbocycle, heterocycle, etc.; and R is hydrogen, (substituted) alkyl, etc.); processes for producing the same; a matrix metalloproteinase inhibitor containing the same; and medicines containing the same and serving as preventives and/or remedies for rheumatism, osteoarthritis, pathologic bone resorption, osteoporosis, periodontosis, interstitial nephritis, arteriosclerosis, pulmonary emphysema, hepatocirrhosis, corneal injury, diseases due to cancer cell metastasis, infiltration and proliferation, autoimmune diseases (such as Crohn's disease and Sjögren's disease), diseases due to leukocyte emigration or infiltration, and neovascularization.
    • 由通式(I)表示的苯磺酰胺衍生物及其盐(其中R 1是氢或烷基; R 2是COOR 3或CONHOR 4); E是亚乙烯基或亚乙基; A是氢,烷基 ,碳环或杂环; J是单键或亚烷基; R 9和R 10各自是氢,(取代的)烷基,COR 11,碳环,杂环等; R 20是氢, (取代的)烷基等); 制造方法; 含有它的基质金属蛋白酶抑制剂; 以及用于预防和/或治疗风湿病,骨关节炎,病理性骨吸收,骨质疏松症,牙周病,间质性肾炎,动脉硬化,肺气肿,肝硬化,角膜损伤,癌细胞转移,浸润和增殖的疾病的药物, 自身免疫性疾病(如克罗恩病和Siegren病),白细胞迁移或浸润引起的疾病以及新生血管形成。