Butyne diol derivativesThe present invention relates to novel butyne diol derivatives ofgeneral formula (I) and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more compounds of the general formula (I) and especially their use as endothelin receptor antagonists.Chemical formula is the compound of general formula i. general formula i here:r 1represent phenyl; one five of forming of phenyl, halogen, hydroxyl, low-carbon alkyl, low alkenyl, low-carbon (lc) alkynyl, low-alkoxy, low alkene oxygen base, low alkynyloxy group, low alkylidene group or low alkenylene or low alkylene oxide group or low alkylene dioxo base and phenyl ring or six-ring, hydroxyl-low-carbon alkyl, hydroxyl hang down alkenyl, hydroxyl low-carbon (lc) alkynyl, low-alkoxy low-carbon alkyl, low-alkoxy-low-alkoxy, trifluoromethyl, trifluoromethoxy, cycloalkyl, hydroxyl-cycloalkyl is single, double or tri-substituted phenyl; heterocyclic radical; five yuan of hetero-aromatic rings that contain one or two n, s or o atom (may by halogen, low-carbon alkyl, low-alkoxy, hydroxyl-low-carbon alkyl, halogen, trifluoromethyl list or two replacement); the 2-pyridyl; the 2-pyridyl that 5-substituting group-usefulness low-carbon alkyl, low-alkoxy replace; phenyl; form one five or six-ring, hydroxyl-low-carbon alkyl, hydroxyl-hang down alkenyl, hydroxyl-low-carbon (lc) alkynyl, trifluoromethyl, trifluoromethoxy, cycloalkyl, hydroxyl-cycloalkyl, single, double or tri-substituted phenyl with phenyl, halogen, hydroxyl, low-carbon alkyl, low alkenyl, low alkynyl, low-alkoxy, low alkene oxygen base, low alkynyloxy group, low alkylidene group or low alkenylene or low alkylene oxide group or low alkylene dioxo base and phenyl ring; five yuan of hetero-aromatic rings that contain one or two n, s, o atom; aromatic base; heterocyclic aromatic base; r 2representation hydroxy; low-carbon alkyl; trifluoromethyl; one five of forming of phenyl, halogen, hydroxyl, low-carbon alkyl, low alkenyl, low-carbon (lc) alkynyl, low-alkoxy, low alkene oxygen base, low alkynyloxy group, low alkylidene group or low alkenylene or low alkylene oxide group or low alkylene dioxo base and phenyl ring or six-ring, hydroxyl-low-carbon alkyl, hydroxyl-hang down alkenyl, hydroxyl-low-carbon (lc) alkynyl, low-alkoxy-low-carbon alkyl, low-alkoxy-low-alkoxy, trifluoromethyl, trifluoromethoxy, cycloalkyl, hydroxyl-cycloalkyl is single, double or tri-substituted phenyl; heterocyclic radical; five yuan of hetero-aromatic rings that contain one or two n, s or o atom (may by halogen, low-carbon alkyl, low-alkoxy list or two replacement); phenyl; one five of forming of phenyl, halogen, hydroxyl, low-carbon alkyl, low alkenyl, low-carbon (lc) alkynyl, low-alkoxy, low alkene oxygen base, low alkynyloxy group, low alkylidene group or low alkenylene or low alkylene oxide group or low alkylene dioxo base and phenyl ring or six-ring, hydroxyl-low-carbon alkyl, hydroxyl-hang down alkenyl, hydroxyl-low-carbon (lc) alkynyl, trifluoromethyl, trifluoromethoxy, cycloalkyl, hydroxyl-cycloalkyl is single, double or tri-substituted phenyl; the 2-pyrimidyl; low-carbon alkyl, low-alkoxy, hydroxyl-low-carbon alkyl, halogen, trifluoromethyl, contain five yuan of fragrant heterocycles of one or two n, s, o atom; aromatic base; heteroaryl; heterocyclic radical; chemical formula is-c (a)-b-r afunctional group of gang here: a represents o or s;b represents nh or key;r arepresent low-carbon alkyl; cycloalkyl; trifluoromethyl; phenyl; one five of forming of phenyl, halogen, hydroxyl, low-carbon alkyl, low alkenyl, low-carbon (lc) alkynyl, low-alkoxy, low alkene oxygen base, low alkynyloxy group, low alkylidene group or low alkenylene or low alkylene oxide group or low alkylene dioxo base and phenyl ring or six-ring, hydroxyl-low-carbon alkyl, hydroxyl-hang down alkenyl, hydroxyl-low-carbon (lc) alkynyl, low-alkoxy-low-carbon alkyl, low-alkoxy-low-alkoxy, trifluoromethyl, trifluoromethoxy, cycloalkyl, hydroxyl-cycloalkyl is single, double or tri-substituted phenyl; heterocyclic radical; five yuan of hetero-aromatic rings that contain one or two n, s or o atom (may by halogen, low-carbon alkyl, low-alkoxy, trifluoromethyl, trifluoromethoxy list or two replacement); the hexa-member heterocycle that contains one or two n atom (may by halogen, low-carbon alkyl, low-alkoxy, trifluoromethyl, list or two replacement); ) r 3representation hydroxy, low-carbon alkyl, phenyl; low-carbon alkyl, low alkenyl, low-carbon (lc) alkynyl, low-alkoxy, amino, low alkylamino, amino-low-carbon alkyl, trifluoromethyl, trifluoromethoxy, halogen, sulfo-low-carbon alkyl, hydroxyl, hydroxyl-low-carbon alkyl, cyano group, carbonyl, lower alkanes acyl group, formyl radical is single, double or tri-substituted phenyl; the benzene furyl; heteroaryl; low-carbon alkyl, low alkenyl, low-carbon (lc) alkynyl, low-alkoxy, amino, low alkylamino, trifluoromethyl, halogen, hydroxyl, hydroxyl-low-carbon alkyl, cyano group, carbonyl list or two three substituted heteroaryls; r 4representation hydroxy, halogen, trifluoromethyl, low-carbon alkyl, low cycloalkyl, low-alkoxy, low cycloalkyloxy, sulfo-low-carbon alkyl, sulfo-low-carbon alkyl-low-carbon alkyl, hydroxyl-low-carbon alkyl, low-carbon alkyl-oxygen-low-carbon alkyl, h...
부틴 디올 유도체본 발명은 화학식 I의 신규한 부틴 디올 유도체 및 제약학적 조성물의 제조에서 활성 성분으로서 이들의 용도에 관한다. 또한, 본 발명은 상기 화합물의 제조 공정, 화학식 I의 한가지이상 화합물을 함유하는 제약학적 조성물 및 특히 엔도텔린 수용체 길항물질로서 이들의 용도를 비롯한 관련된 측면에 관한다. 화학식 I 의 화합물, 순수한 거울상이성질체, 거울상이성질성 측면에서 순수한 부분입체이성질체, 부분입체이성질체의 혼합물, 부분입체이성질성 라세미체, 부분입체이성질성 라세미체의 혼합물, 이들의 제약학적으로 수용가능한 염: 화학식 I [이미지] 여기서, R1은 페닐; 할로겐, 저가 알킬, 저가 알케닐, 저가 알키닐, 저가 알콕시, 하이드록시-저가 알킬, 하이드록시-저가 알케닐, 하이드록시-저가 알키닐, 트리플루오르메틸, 사이클로알킬, 하이드록시-사이클로알킬로 치환된 단일-, 이중- 혹은 삼중-치환된 페닐; 2-피리딜; 저가 알킬, 1개 혹은 2개의 질소, 황 또는 산소 원자를 보유하는 5각형 헤테로아릴 고리로 치환된 5-치환된 2-피리딜이다; R2는 수소; 저가 알킬; 페닐; 할로겐, 저가 알킬, 저가 알콕시, 저가 알콕시-저가 알킬, 트리플루오르메틸, 또는 할로겐, 저가 알킬, 저가 알콕시로 단일- 혹은 이중-치환시킬 수 있는 1개 혹은 2개의 질소, 황 또는 산소 원자를 보유하는 5각형 헤테로아릴 고리로 치환되는 단일-, 이중- 혹은 삼중-치환된 페닐; 벤질; 할로겐, 저가 알킬, 저가 알콕시, 트리플루오르메틸, 2-피리미딜로 치환된 단일- 혹은 이중-치환된 벤질; 저가 알킬, 저가 알콕시, 할로겐, 트리플루오르메틸, 또는 화학식 -C(A)-B-Ra 군(여기서, A는 O 또는 S이고; B는 NH이며; Ra는 저가 알킬; 사이클로알킬; 페닐; 할로겐 저가 알킬, 저가 알케닐, 저가 알콕시, 트리플루오르메틸, 또는 할로겐, 저가 알킬, 저가 알콕시로 단일- 혹은 이중-치환시킬 수 있는 1개 혹은 2개의 질소원자를 보유하는 6각형 헤테로아릴 고리다)으로 치환된 단일-, 이중- 혹은 삼중-치환된 페닐이다; R3은 저가 알킬, 저가 알케닐, 저가 알킬옥시, 트리플루오르메틸, 할로겐, 하이드록시로 치환된 단일-, 이중- 혹은 삼중-치환된 페닐이다; R4는 수소, 할로겐, 트리플루오르메틸, 저가 알킬, 저가 알킬옥시, 저가 알킬티오, 저가 알킬-옥시-저가 알킬; 페닐; 할로겐, 저가 알킬, 저가 알콕시, 페닐 고리와 5각형 혹은 6각형의 페닐 고리를 형성하는 저가 알킬렌이나 저가 알케닐렌 또는 저가 알킬렌옥시나 저가 알킬렌디옥시, 헤테로아릴로 치환된 단일- 혹은 이중-치환된 페닐; 헤테로사이클릴이다; X는 산소, 황 또는 원자의 손이다.