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PYRIMIDINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF RESPIRATORY DISEASES SUCH AS COPD

机译:嘧啶衍生物及其在治疗COPD等呼吸系统疾病中的用途

摘要

The present invention is directed to compounds of formula (I)(see formula I)wherein A is C-R1; R1 and R2 are hydrogen; R4 is hydrogen; R3 istrifluoromethyl,3-chloro or 3-bromo; R6 is hydrogen; R6 is hydrogen or -COOR A, wherein R A is(C1-C6)alkyl; -X1-X2- is z -NR19-CO-; R19 is a radical of formula -[Y]m-[Alk1]p-[Q]r-[Alk2]q-Z, wherein m, p, t are 0; q is 1; Alk2 represents a C1-C6 alkylene radical;Q represents a divalent mono- or bicyclic carbocyclic or heterocyclic radicalhaving3-9 ring members; Z is (i) -N(R A)(R B) wherein R A and R B are independentlyhydrogen,or a C1-C6-alkyl; or (ii)-N+(R A)(R B)(R C) wherein R A, R B and R C areindependently aC1-C6-alkyl. The compounds and pharmaceutical compositions are inhibitors ofneutrophil elastase. These compounds are useful in the treatment of diseasesandconditions in which human neutrophil elastase plays a part.
机译:本发明涉及式(I)的化合物(参见公式I)其中A是C-R1; R1和R2是氢; R4是氢; R3是三氟甲基3-氯或3-溴; R6是氢; R6是氢或-COOR A,其中RA是(C1-C6)烷基; -X1-X2-为z -NR19-CO-; R19是式-[Y] m-的基团[Alk1] p- [Q] r- [Alk2] q-Z,其中m,p,t为0; q是1; Alk2表示碳数1〜6的亚烷基。Q代表二价单环或双环碳环或杂环基有3-9个环成员; Z为(i)-N(R A)(R B),其中R A和R B独立地为氢,或C 1 -C 6烷基;或或(ii)-N +(R A)(R B)(R C)其中R A,R B和R C为独立地C1-C6-烷基。该化合物和药物组合物是下列药物的抑制剂中性粒细胞弹性蛋白酶。这些化合物可用于治疗疾病和人类嗜中性粒细胞弹性蛋白酶发挥作用的条件。

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