Azolopyridin-3-one derivatives as inhibitors of endothelial lipaseThe present invention relates to azolopyridin-3-one derivatives of the general formula (I) with the meanings indicated in the description, their pharmaceutically usable salts and their use as medicinal substances. The compounds are inhibitors of endothelial lipase.The tautomeric form of formula I compound, this compounds and physiology thereof the tolerance salt,Implication wherein is:X is identical or differently=C (R)-or=N-, wherein at least one and maximum two X are=N-;Y is NR6 or O;R is hydrogen, halogen, (C identical or differently 1-C 6)-alkyl, (C 1-C 3)-haloalkyl, (C 1-C 3)-alkoxyl group-(C 1-C 3)-alkylidene group, aryl, heterocycle, hydroxyl, (C 1-C 6)-alkoxyl group, (C 1-C 3)-halogenated alkoxy, aryloxy, cyano group, nitro ,-S (O) p-(C 1-C 6)-alkyl, p=0,1 or 2 wherein, amino-sulfonyl, five fluorine sulfenyls, amino, (C 1-C 6)-alkylamino, two-(C 2-C 12)-alkylamino ,-CO-(C 1-C 6)-alkyl ,-COOR3 ,-CO-NR4R5 ,-O-CO-NR4R5 ,-O-CO-(C 1-C 6)-alkylidene group-CO-O-(C 1-C 6)-alkyl ,-O-CO-(C 1-C 6)-alkylidene group-CO-OH or-O-CO-(C 1-C 6)-alkylidene group-CO-NR4R5; R1 is (C 5-C 16)-alkyl, (C 1-C 4)-alkylidene group-aryl, (C 1-C 4)-alkylidenyl-heterocyclic, (C 1-C 4)-alkylidene group-(C 3-C 12)-cycloalkyl, (C 8-C 14)-two ring, wherein aryl, heterocycle, cycloalkyl or two rings can be by following preferred group lists or polysubstituted: halogen, (C 1-C 6)-alkyl, (C 1-C 3)-alkoxyl group, hydroxyl, (C 1-C 6)-alkyl thiol, amino, (C 1-C 6)-alkylamino, two-(C 2-C 12)-alkylamino, list-(C 1-C 6)-alkyl amino-carbonyl, two-(C 2-C 8)-alkyl amino-carbonyl, (C 1-C 6)-alkoxy carbonyl, (C 1-C 6)-alkyl-carbonyl, cyano group, nitro, trifluoromethyl, trifluoromethoxy, five fluorine sulfenyls, (C 1-C 6)-alkyl sulphonyl, amino-sulfonyl; R2 is a hydrogen;R3 is hydrogen, (C 1-C 6)-alkyl, benzyl; R4, R5 are hydrogen, (C identical or differently 1-C 6)-alkyl, aryl, (C 3-C 12)-cycloalkyl, (C 1-C 4)-alkylidene group-aryl, (C 1-C 4)-alkylidene group-(C 3-C 12)-cycloalkyl; R6 is hydrogen, (C 1-C 10)-alkyl, (C 1-C 4)-alkylidene group-CN, (C 1-C 4)-alkylidene group-aryl, (C 1-C 4)-alkylidenyl-heterocyclic, (C 1-C 4)-alkylidene group-(C 3-C 12)-cycloalkyl, (C 8-C 14)-two ring, wherein aryl, heterocycle, cycloalkyl or two rings can be by following preferred group lists or polysubstituted: halogen, (C 1-C 6)-alkyl, (C 1-C 6)-alkoxyl group, hydroxyl, (C 1-C 6)-alkyl thiol, amino, (C 1-C 6)-alkylamino, two-(C 2-C 12)-alkylamino, list-(C 1-C 6)-alkyl amino-carbonyl, two-(C 2-C 8)-alkyl amino-carbonyl, (C 1-C 6)-alkoxy carbonyl, (C 1-C 6)-alkyl-carbonyl, cyano group, trifluoromethyl, trifluoromethoxy, nitro (C 1-C 6)-alkyl sulphonyl, amino-sulfonyl.
내피 리파제의 억제제로서의 아졸로피리딘-3-온 유도체본 발명은 명세서에 기재된 바와 같은 화학식 I의 아졸로피리딘-3-온 유도체, 이들의 약제학적으로 유용한 염, 및 의약 물질로서의 이들의 용도에 관한 것이다. 화학식 I의 화합물, 이의 토터머 형태 및 이의 약리학적으로 허용되는 염. 화학식 I [이미지] 위의 화학식 I에서, X는 동일하거나 상이하게 =C(-R)- 또는 =N-이고, 이때 1개 이상 2개 이하의 X가 =N-이며, Y는 NR6 또는 O이고, R은 동일하거나 상이하게 수소, 할로겐, (C1-C6)-알킬, (C1-C3)-할로알킬, (C1-C3)-알킬옥시-(C1-C3)-알킬렌, 아릴, 헤테로사이클, 하이드록시, (C1-C6)-알킬옥시, (C1-C3)-할로알킬옥시, 아릴옥시, 시아노, 니트로, 또는 -S(O)p-(C1-C6)-알킬(여기서, p는 0, 1 또는 2이다), 아미노설포닐, 펜타플루오로설파닐, 아미노, (C1-C6)-알킬아미노, 디-(C2-C12)-알킬아미노, -CO-(C1-C6)-알킬, -COOR3, -CO-NR4R5, -O-CO-NR4R5, -O-CO-(C1-C6)-알킬렌-CO-O-(C1-C6)-알킬, -O-CO-(C1-C6)-알킬렌-CO-OH 또는 -O-CO-(C1-C6)-알킬렌-CO-NR4R5이고, R1은 (C5-C16)-알킬, (C1-C4)-알킬렌-아릴, (C1-C4)-알킬렌-헤테로사이클, (C1-C4)-알킬렌-(C3-C12)-사이클로알킬, (C8-C14)-바이사이클이고, 여기서 아릴, 헤테로사이클, 사이클로알킬 또는 바이사이클은 바람직하게는 할로겐, (C1-C6)-알킬, (C1-C3)-알킬옥시, 하이드록시, (C1-C6)-알킬머캅토, 아미노, (C1-C6)-알킬아미노, 디-(C2-C12)-알킬아미노, 모노-(C1-C6)-알킬아미노카보닐, 디-(C2-C8)-알킬아미노-카보닐, (C1-C6)-알콕시카보닐, (C1-C6)-알킬카보닐, 시아노, 니트로, 트리플루오로메틸, 트리플루오로메틸옥시, 펜타플루오로설파닐, (C1-C6)-알킬-설포닐 또는 아미노설포닐에 의해 1회 이상 치환될 수 있고, R2는 수소이고, R3은 수소, (C1-C6)-알킬 또는 벤질이고, R4 및 R5는 동일하거나 상이하게 수소, (C1-C6)-알킬, 아릴, (C3-C12)-사이클로알킬, (C1-C4)-알킬렌-아릴, 또는 (C1-C4)-알킬렌-(C3-C12)-사이클로알킬이고, R6은 수소, (C1-C10)-알킬, (C1-C4)-알킬렌-CN, (C1-C4)-알킬렌-아릴, (C1-C4)-알킬렌-헤테로사이클, (C1-C4)-알킬렌-(C3-C12)-사이클로알킬 또는 (C8-C14)-바이사이클이고, 여기서 아릴, 헤테로사이클, 사이클로알킬 또는 바이사이클은 바람직하게는 할로겐, (C1-C6)-알킬, (C1-C6)-알킬옥시, 하이드록시, (C1-C6)-알킬머캅토, 아미노, (C1-C6)-알킬아미노, 디-(C2-C12)-알킬아미노, 모노-(C1-C6)-알킬아미노카보닐, 디-(C2-C8)-알킬아미노-카보닐, (C1-C6)-알콕시카보닐, (C1-C6)-알킬카보닐, 시아노, 트리플루오로메틸, 트리플루오로메틸옥시, 니트로 (C1-C6)-알킬설포닐 또는 아미노설포닐에 의해 1회 이상 치환될 수 있다.