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INHIBITOR FOR PROGRESS OF PTERYGIUM AND ITS POSTOPERATIVE RECURRENCE

机译:翼状PRO肉进展抑制剂及其术后复发

摘要

PROBLEM TO BE SOLVED: To obtain the subject inhibitor having effect inhibiting the propagation of pterygium tissue and capable of remarkably inhibiting both progress of pterygium and its postoperative recurrence by including a specific imidazolecarboxylic acid derivative (or its salt) as an active principle.;SOLUTION: This inhibitor for progress of pterygium and its postoperative recurrence is prepared by including an imidazolecarboxylic acid derivative of formula I [one of A and B is expressed by formula II (R1 is H, OH or the like; R2 and R3 are each H, a lower alkyl or the like) and the other is a mono- or di-hydroxy lower alkoxycarbonyl or the like; R4 can be a lower alkyl; R5 can be H or a lower alkyl; R4 and R5 can combine with each other into an alicyclic amino group] (or its salt) as an active principle. The compound of formula I is obtained by reacting a cinnamic acid derivative of formula III (R1a is H, a halogen or the like) (or its functionally reactive derivative such as an active ester) with an aminoimidazole derivative of formula IV (one of P and Q is amino and the other is a mono- or di-hydroxy lower alkoxycarbonyl having a protecting group or the like) in an inert solvent.;COPYRIGHT: (C)2000,JPO
机译:解决的问题:通过包含特定的咪唑羧酸衍生物(或其盐)作为活性成分,获得具有抑制翼状tissue肉组织增殖的效果并且能够显着抑制翼状progress肉的进展及其术后复发的本发明的抑制剂。 :该翼状progress肉的进展及其术后复发抑制剂是通过包括式I的咪唑羧酸衍生物制备的[A和B之一由式II表示(R1是H,OH等; R2和R3分别是H,低级烷基等),另一个是单或二羟基低级烷氧羰基等。 R4可以是低级烷基; R5可以是H或低级烷基; R 4和R 5可以彼此结合成脂环族氨基](或其盐)作为有效成分。通过使式III的肉桂酸衍生物(R 1a为H,卤素等)(或其功能性反应性衍生物如活性酯)与式IV的氨基咪唑衍生物(P中的一个为P Q是氨基,另一个是在惰性溶剂中的具有保护基等的单或二羟基低级烷氧羰基。)版权所有:(C)2000,JPO

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