首页> 外国专利> a-anilated pyrrole derivatives and their pharmacological uses (a-Annelated Pyrrole Derivatives and Pharmaceutical Use Thereof)

a-anilated pyrrole derivatives and their pharmacological uses (a-Annelated Pyrrole Derivatives and Pharmaceutical Use Thereof)

机译:[a]-苯胺基吡咯衍生物及其药理用途([a]-苯并吡咯衍生物及其药物用途)

摘要

The present invention relates to a heterocyclic compound represented by the following formula (I).;In this formula, the radicals R RTI ID = 0.0 One, R2And R32 is H, or is optionally halogen, pseudohalogen, CF3, NO2, OH, alkoxy, OCF3Alkyl, and aryloxy, or is an aryl radical having one or more oxygen, nitrogen and / or sulfur atoms, optionally condensed with a phenyl or naphthyl radical, optionally substituted with halogen, CF3, A 1 or 2 ring aromatic heterocyclic radical substituted by alkyl or alkoxy; Radical ROne, R2And R3The other is H, CHO, CO2H, COO alkyl, COS alkyl, COCO2H, COCO2Alkyl or A-Y, wherein A is COne-C8Alkylene or C2-C8Alkenylene, Y is CO2H, CO, OPO (OH)2, OP (OH)2, Acid type groups, COO alkyl, SO2O alkyl, CHO, OH, or CONR8R9; Wherein R8And R9May be the same or different and are H, alkyl, OH, acyl, SO2Alkyl, or SO2Phenyl, the alkyl radical of the sulfonyl group is optionally substituted with one or more halogen atoms, the aryl radical optionally substituted with one or more halogens, COne-C8Alkyl or COne-C8Alkoxy radical; R4, R5, R6And R7May be the same or different and represent H, alkyl, Y, or AY according to the definition above, and two of the adjacent radicals represent a chemical bond between the two ring atoms to which they are attached and the other two are as defined above , Or two of the superimposed radicals together with the carbon atoms to which they are attached represent a carbonyl group or a thio analog thereof; X is O, S, SO, SO2, CO, or NR10, Wherein R10/RTI is H, or optionally halogen, COne-C8Alkyl or COne-C8Alkyl substituted with alkoxy, A-Y according to the definition above, or aryl, and B is CR11R12(Wherein R11And R12May be the same or different). H, alkyl, Y, or A-Y according to the definition above, or R11And R12Or a carbonyl group or a thio group thereof, and a is 0, 1 or 2;;The compounds are useful for the treatment of diseases of the rheumatic group and for the prevention of allergic diseases.
机译:本发明涉及由下式(I)表示的杂环化合物:在该式中,基团R 1 One,R 2 S和R 3 2>为H,或可选为卤素,假卤素,CF 3 ,NO 2 ,OH,烷氧基,OCF 3 烷基和芳氧基,或者是具有一个或多个氧,氮和/或硫原子的芳基,可选地与苯基或萘基稠合,可选地被卤素,CF 3 取代,被烷基或烷氧基取代的1或2个环芳族杂环基;自由基R 一个,R 2 和R 3 另一个是H,CHO,CO 2 H,COO烷基,COS烷基,COCO 2 H,COCO 2 烷基或AY,其中A为C One -C 8 亚烷基或C 2 -C 8 亚烯基,Y为CO 2 H,CO,OPO(OH) 2 ,OP(OH) 2 ,酸型基团,COO烷基,SO 2 O烷基,CHO,OH或CONR 8 R 9 ;其中R 8 和R 9 可以相同或不同,并且为H,烷基,OH,酰基,SO 2 烷基或SO < Sub> 2 苯基,磺酰基的烷基任选被一个或多个卤素原子取代,芳基任选被一个或多个卤素,C One -C 8 烷基或C 一个 -C 8 烷氧基; R 4 ,R 5 ,R 6 和R 7 可以相同或不同,表示H,烷基,Y或AY根据上述定义,并且两个相邻的基团表示它们所连接的两个环原子之间的化学键,另外两个如上定义,或者两个重叠的基团与碳一起它们所连接的原子表示羰基或其硫代类似物; X是O,S,SO,SO 2 ,CO或NR 10 ,其中R 10 是H,或可选卤素,C One -C 8 烷基或C One -C 8 烷基被烷氧基取代的AY上面的定义或芳基,并且B是CR 11 R 12 (其中R 11 和R 12 可以相同或不同)。根据上述定义的H,烷基,Y或AY,或R 11 和R 12 或羰基或硫基,并且a为0、1或2;该化合物可用于治疗风湿病和预防过敏性疾病。

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