Novel compoundsThis invention relates to heterocyclic compounds, which are pyrimidinone derivatives having human neutrophil elastase inhibitory properties, and their use in therapy.A kind of compound, it is selected from：1- (2- 5- cyano group -2- [(r) -6- methoxycarbonyl -7- methyl -3- oxo -8- (3- trifluoromethyl-phenyl) -2,3,5, 8- tetrahydrochysene-[1,2,4] triazol [4,3a] pyrimidine -5- base]-phenyl }-ethyl) -4- methoxv-pyridinebromide；1- (2- 5- cyano group -2- [(r) -6- methoxycarbonyl -7- methyl -3- oxo -8- (3- trifluoromethyl-phenyl) -2,3,5, 8- tetrahydrochysene-[1,2,4] triazol [4,3-a] pyrimidine -5- base]-phenyl }-ethyl) -3- hydroxy-pyridinebromide；1- (2- 5- cyano group -2- [(r) -6- methoxycarbonyl -7- methyl -3- oxo -8- (3- trifluoromethyl-phenyl) -2,3,5, 8- tetrahydrochysene-[1,2,4] triazol [4,3-a] pyrimidine -5- base]-phenyl }-ethyl) -2- methvl-pyridiniumbromide；1- (2- 5- cyano group -2- [(r) -6- methoxycarbonyl -7- methyl -3- oxo -8- (3- trifluoromethyl-phenyl) -2,3,5, 8- tetrahydrochysene-[1,2,4] triazol [4,3-a] pyrimidine -5- base]-phenyl }-ethyl) -4- hydroxymethyl-pyridinebromide；1- (2- 5- cyano group -2- [(r) -6- methoxycarbonyl -7- methyl -3- oxo -8- (3- trifluoromethyl-phenyl) -2,3,5, 8- tetrahydrochysene-[1,2,4] triazol [4,3-a] pyrimidine -5- base]-phenyl }-ethyl) -4- isopropyl-pyridinebromide；1- (2- 5- cyano group -2- [(r) -6- methoxycarbonyl -7- methyl -3- oxo -8- (3- trifluoromethyl-phenyl) -2,3,5, 8- tetrahydrochysene-[1,2,4] triazol [4,3-a] pyrimidine -5- base]-phenyl }-ethyl) -5- hydroxy-2-methyl-pyridinebromination thing；1- (2- 5- cyano group -2- [(r) -6- methoxycarbonyl -7- methyl -3- oxo -8- (3- trifluoromethyl-phenyl) -2,3,5, 8- tetrahydrochysene-[1,2,4] triazol [4,3-a] pyrimidine -5- base]-phenyl }-ethyl) -2,4- dimethyl-pyridinebromide；1- (2- 5- cyano group -2- [(r) -6- methoxycarbonyl -7- methyl -3- oxo -8- (3- trifluoromethyl-phenyl) -2,3,5, 8- tetrahydrochysene-[1,2,4] triazol [4,3-a] pyrimidine -5- base]-phenyl }-ethyl) -3,5- dimethyl-pyridinebromide；1- (2- 5- cyano group -2- [(r) -6- methoxycarbonyl -7- methyl -3- oxo -8- (3- trifluoromethyl-phenyl) -2,3,5, 8- tetrahydrochysene-[1,2,4] triazol [4,3-a] pyrimidine -5- base]-phenyl }-ethyl) -2- ethylpyridinebromide；1- (2- 5- cyano group -2- [(r) -6- methoxycarbonyl -7- methyl -3- oxo -8- (3- trifluoromethyl-phenyl) -2,3,5, 8- tetrahydrochysene-[1,2,4] triazol [4,3-a] pyrimidine -5- base]-phenyl }-ethyl) -2- (2- hydroxy-ethyl)-pyridinebromination thing；1- (2- 5- cyano group -2- [(r) -6- methoxycarbonyl -7- methyl -3- oxo -8- (3- trifluoromethyl-phenyl) -2,3,5, 8- tetrahydrochysene-[1,2,4] triazol [4,3-a] pyrimidine -5- base]-phenyl }-ethyl) -4- ethylpyridinebromide；pharmaceutically acceptable salt with them.
신규화합물본 발명은 인간 호중구 엘라스타제 억제 특성을 가지는 피리미디논 유도체인 헤테로사이클릭 화합물 및 치료에서의 이들의 용도에 관한 것이다.1-(2-{5-시아노-2-[(R)-6-메톡시카보닐-7-메틸-3-옥소-8-(3-트라이플루오로메틸-페닐)-2,3,5,8-테트라하이드로-[1,2,4]트라이아졸로[4,3a]피리미딘-5-일]-페닐}-에틸)-4-메톡시-피리디늄 브로마이드;1-(2-{5-시아노-2-[(R)-6-메톡시카보닐-7-메틸-3-옥소-8-(3-트라이플루오로메틸-페닐)-2,3,5,8-테트라하이드로-[1,2,4]트라이아졸로[4,3-a]피리미딘-5-일]-페닐}-에틸)-3-하이드록시-피리디늄 브로마이드;1-(2-{5-시아노-2-[(R)-6-메톡시카보닐-7-메틸-3-옥소-8-(3-트라이플루오로메틸-페닐)-2,3,5,8-테트라하이드로-[1,2,4]트라이아졸로[4,3-a]피리미딘-5-일]-페닐}-에틸)-2-메틸-피리디늄 브로마이드;1-(2-{5-시아노-2-[(R)-6-메톡시카보닐-7-메틸-3-옥소-8-(3-트라이플루오로메틸-페닐)-2,3,5,8-테트라하이드로-[1,2,4]트라이아졸로[4,3-a]피리미딘-5-일]-페닐}-에틸)-4-하이드록시메틸-피리디늄 브로마이드;1-(2-{5-시아노-2-[(R)-6-메톡시카보닐-7-메틸-3-옥소-8-(3-트라이플루오로메틸-페닐)-2,3,5,8-테트라하이드로-[1,2,4]트라이아졸로[4,3-a]피리미딘-5-일]-페닐}-에틸)-4-아이소프로필-피리디늄 브로마이드;1-(2-{5-시아노-2-[(R)-6-메톡시카보닐-7-메틸-3-옥소-8-(3-트라이플루오로메틸-페닐)-2,3,5,8-테트라하이드로-[1,2,4]트라이아졸로[4,3-a]피리미딘-5-일]-페닐}-에틸)-5-하이드록시-2-메틸-피리디늄 브로마이드;1-(2-{5-시아노-2-[(R)-6-메톡시카보닐-7-메틸-3-옥소-8-(3-트라이플루오로메틸-페닐)-2,3,5,8-테트라하이드로-[1,2,4]트라이아졸로[4,3-a]피리미딘-5-일]-페닐}-에틸)-2,4-다이메틸-피리디늄 브로마이드;1-(2-{5-시아노-2-[(R)-6-메톡시카보닐-7-메틸-3-옥소-8-(3-트라이플루오로메틸-페닐)-2,3,5,8-테트라하이드로-[1,2,4]트라이아졸로[4,3-a]피리미딘-5-일]-페닐}-에틸)-3,5- 다이메틸-피리디늄 브로마이드;1-(2-{5-시아노-2-[(R)-6-메톡시카보닐-7-메틸-3-옥소-8-(3-트라이플루오로메틸-페닐)-2,3,5,8-테트라하이드로-[1,2,4]트라이아졸로[4,3-a]피리미딘-5-일]-페닐}-에틸)-2-에틸-피리디늄 브로마이드;1-(2-{5-시아노-2-[(R)-6-메톡시카보닐-7-메틸-3-옥소-8-(3-트라이플루오로메틸-페닐)-2,3,5,8-테트라하이드로-[1,2,4]트라이아졸로[4,3-a]피리미딘-5-일]-페닐}-에틸)-2-(2-하이드록시-에틸)-피리디늄 브로마이드;1-(2-{5-시아노-2-[(R)-6-메톡시카보닐-7-메틸-3-옥소-8-(3-트라이플루오로메틸-페닐)-2,3,5,8-테트라하이드로-[1,2,4]트라이아졸로[4,3-a]피리미딘-5-일]-페닐}-에틸)-4-에틸-피리디늄 브로마이드;로 이루어진 군으로부터 선택되는 화합물 및 이들의 약제학적으로 허용가능한 염.