| 摘要 |
PURPOSE: To obtain an agent for suppressing the release, activation and synthesis of TGF-βin a cell originated from liver or lung. CONSTITUTION: This agent contains a compound of formula I (A is single bond or NH; E is OCO or COO; R<1> is Z-COOR<2> or group of formula II; Z is single bond, methylene, ethylene or vinylene; R<2> is H, an alkyl or CH2 CONR<3> R<4> ; R<3> and R<4> are each H or an alkyl; R<5> and R<6> are each H or an alkyl; R<7> is an alkenyl; R<8> is (CH2 )n -COOR<9> ; (n) is 0-4; R<9> is H or an alkyl) or its salt as an active component. The compound of formula I is useful for the treatment and prevention of diseases caused by excessive TGF-βinduction, e.g. organ fibrosis such as hepatic fibrosis, hepatic cirrhosis, myelofibrosis and systemic sclerosis, hepatic regeneration failure such as hepatic cirrhosis, subacute hepatitis and fulminant hepatitis, glomerular nephritis, nephrosclerosis, arthrorheumatism and intraocular proliferating disease. The dose for adult is 1-1,000mg per dose and one to several doses per day by oral or parenteral administration.
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