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    • 32. 发明授权
    • Epoxysuccinic acid derivatives
    • 环氧琥珀酸衍生物
    • US5843992A
    • 1998-12-01
    • US930509
    • 1997-09-29
    • Yutaka NomuraToshihiro TakahashiKaoru HaraYasushi YoshinoMitsuo Masaki
    • Yutaka NomuraToshihiro TakahashiKaoru HaraYasushi YoshinoMitsuo Masaki
    • C07D303/48A61K31/335
    • C07D303/48
    • An epoxysuccinic acid derivative having the following formula: ##STR1## �wherein R.sup.1 is hydrogen, alkyl, aryl, or aralkyl; each of R.sup.2 and R.sup.3 independently is aryl, aralkyl or alkyl; X is --O-- or --NR.sup.4 --; and R.sup.4 is hydrogen, alkyl, or aralkyl! is useful for prevention and treatment of bone diseases such as osteoporosis, malignant hypercalcemia and Paget's syndrome, and further useful for treatment of osteoarthritis and rheumatoid arthritis which are accompanied by abnormal enhancement of cathepsin L activity, and furthermore useful as a medicine for treating diseases in which cathepsin B and L participate, such as muscular dystrophy and muscular atrophy.
    • PCT No.PCT / JP96 / 00889 Sec。 371日期:1997年9月29日 102(e)日期1997年9月29日PCT提交1996年4月1日PCT公布。 出版物WO96 / 30354 日期:1996年10月3日具有下式的环氧琥珀酸衍生物:其中R 1是氢,烷基,芳基或芳烷基; R2和R3各自独立地为芳基,芳烷基或烷基; X是-O-或-NR4-; 和R4是氢,烷基或芳烷基]可用于预防和治疗骨质疏松症,恶性高钙血症和佩吉特综合征等骨疾病,并且还可用于治疗组织蛋白酶L活性异常增强的骨关节炎和类风湿性关节炎, 并且还可用作治疗组织蛋白酶B和L参与的疾病的药物,例如肌营养不良和肌肉萎缩。
    • 33. 发明授权
    • Imidazole derivatives
    • 咪唑衍生物
    • US5180836A
    • 1993-01-19
    • US786392
    • 1991-11-01
    • Susumu OkabeMitsuo MasakiTomio YamakawaHitoshi MatsukuraYutaka Nomura
    • Susumu OkabeMitsuo MasakiTomio YamakawaHitoshi MatsukuraYutaka Nomura
    • C07D233/84C07D235/28
    • C07D233/84C07D235/28
    • Disclosed are novel imidazole derivatives having the formula: ##STR1## wherein R.sup.1 and R.sup.2 are H, alkyl, cycloalkyl, aryl, aralkyl or halogen-substituted alkyl, or R.sup.1 and R.sup.2 are combined to form a heterocyclic ring; R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are H, halogen, alkoxy, aralkyloxy, alkyl, alkoxycarbonyl, nitro, amino, acyl, fluorine substituted-alkyl, or fluorine substituted-alkoxy, or R.sup.3 is combined with R.sup.2 to form a heterocyclic ring; R.sup.8 and R.sup.9 are H, halogen, alkoxy, alkyl, alkoxycarbonyl, nitro, amino, acyl, fluorine substituted-alkyl, fluorine substituted-alkoxy, or aryl group which may have a substituent, or R.sup.8 and R.sup.9 are combined to form an alicyclic ring; R.sup.7 is, where R.sup.8 and R.sup.9 are not combined, H, and, where R.sup.8 and R.sup.9 are combined, H, alkyl which may have a substituent, aryl which may have a substituent, arylcarbonyl which may have a substituent, or a sulfur-containing heterocyclic group; and n is 0 or 1. The new imidazole derivatives are effective particularly as anti-ulcer agents.
    • 公开了具有下式的新的咪唑衍生物:其中R 1和R 2是H,烷基,环烷基,芳基,芳烷基或卤素取代的烷基,或者R 1和R 2结合形成杂环; R3,R4,R5和R6是H,卤素,烷氧基,芳烷氧基,烷基,烷氧基羰基,硝基,氨基,酰基,氟取代的 - 烷基或氟取代的 - 烷氧基,或R3与R2结合形成杂环; R8和R9是可以具有取代基的H,卤素,烷氧基,烷基,烷氧基羰基,硝基,氨基,酰基,氟取代的 - 烷基,氟取代的 - 烷氧基或芳基,或R8和R9组合形成脂环 ; R 7是,其中R 8和R 9不组合,其中R 8和R 9结合,可以具有取代基的烷基,可以具有取代基的芳基,可以具有取代基的芳基或含硫 杂环基; 并且n为0或1.新的咪唑衍生物特别用作抗溃疡剂。