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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; R5 is hydrogen;R3 is trifluoromethyl, 3-chloro or 3-bromo; R6 is -CO2R11; -X1X2- is -NR19-CO-;R11 represents a radical of formula -[Alk1]p-[Q]r-[Alk2]q-Z wherein p, q areindependently 0 or 1, t is 0; Alk1 and Alk2 each independently represent aC1-C6 alkylene radical; Z is (i) -N(R A)(R B) wherein R A and R B areindependentlyhydrogen, or a C1-C6-alkyl; or (ii)-N+(R A)(R B)(R C) wherein R A, R B and R Careindependently a C1-C6-alkyl; R19 is hydrogen or (C1-C6)alkyl. These compoundsareinhibitors of neutrophil elastase. The compounds of the invention andpharmaceutical compositions prepared therefrom are useful in the treatment ofdiseases and conditions 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; R5是氢;R3是三氟甲基,3-氯或3-溴; R6为-CO2R11; -X1X2-是-NR19-CO-;R11代表式-[Alk1] p- [Q] r- [Alk2] q-Z的基团,其中p,q是独立地为0或1,t为0; Alk1和Alk2各自独立代表C1-C6亚烷基; Z为(i)-N(R A)(R B),其中R A和R B为独立地氢或C 1 -C 6烷基;或(ii)-N +(R A)(R B)(R C)其中R A,R B和R C是独立地为C1-C6-烷基; R 19是氢或(C 1 -C 6)烷基。这些化合物是中性粒细胞弹性蛋白酶的抑制剂。本发明的化合物和由此制备的药物组合物可用于治疗人类嗜中性粒细胞弹性蛋白酶发挥作用的疾病和状况。

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