首页> 外国专利> DERIVATIVES OF ARYL CARBOXYLIC ACIDS, METHODS FOR THEIR PREPARING, PHARMACEUTICAL COMPOSITION BASED ON THEREOF, METHODS FOR TREATMENT AND PROPHYLAXIS OF DIFFERENT DISEASES, INTERMEDIATE COMPOUNDS AND METHODS FOR THEIR PREPARING

DERIVATIVES OF ARYL CARBOXYLIC ACIDS, METHODS FOR THEIR PREPARING, PHARMACEUTICAL COMPOSITION BASED ON THEREOF, METHODS FOR TREATMENT AND PROPHYLAXIS OF DIFFERENT DISEASES, INTERMEDIATE COMPOUNDS AND METHODS FOR THEIR PREPARING

机译:芳基羧酸的衍生物,其制备方法,基于其的药物组合物,不同疾病的治疗和预防方法,中间化合物及其制备方法

摘要

FIELD: organic chemistry, chemical technology, medicine, pharmacy.;SUBSTANCE: invention relates to derivatives of aryl carboxylic acids and describes a compound of the formula (I):; , wherein groups R1, R2, R3, R4 and groups R5 and R6 when they are joined to carbon atom can be similar or different and mean hydrogen, halogen atom, hydroxy-group or optionally substituted group taken among alkyl, alkoxy-group, phenyl, carboxylic acid or sulfonic acid; one or both substitutes R5 and R6 can mean oxo-group also if they are joined to carbon atom; if R5 and R are joined to nitrogen atom then they mean hydrogen atom, hydroxy-group or optionally substituted alkyl or benzyl; X means heteroatom taken among oxygen and sulfur atom or NH; Ar means optionally substituted bivalent a single or condensed aromatic or heterocyclic group wherein aromatic ring represents phenyl, naphthyl and heterocyclic group represents furan; R7 means hydrogen, halogen atom, alkoxy-group, alkyl, or it forms a bond with the adjacent group R8; R8 means hydrogen atom, hydroxy-, alkoxy-group, alkyl or optionally substituted benzyl; or R8 forms a bond in common with R7; R9 means hydrogen atom or optionally substituted group taken among alkyl, phenyl or benzyl group; R10 means hydrogen atom or optionally substituted group taken among alkyl, phenyl or benzyl group; Y means oxygen atom or NR12 wherein R12 means hydrogen atom, alkyl or benzyl; R10 and R12 can form in common five- or six-membered cyclic structure comprising carbon atoms that involves optionally one or some heteroatoms taken among oxygen, sulfur or nitrogen atoms; a binding group represented by the formula: -(CH2)n-(O)m- can be joined through nitrogen atom or through carbon atom and wherein n means a whole number from 1 to 4; m means a whole number from 0 to 1 under condition that when a binding group is joined through carbon atom then R5 either R6 represents oxo-group; Y means oxygen atom; R9 doesn't mean hydrogen atom; or its derivatives, analogs, its tautomeric forms, its stereoisomers, its polymorphic forms, its pharmaceutically acceptable salts, its pharmaceutically acceptable solvates. Also, invention describes methods for preparing compounds of the general formula (I), intermediate compounds and methods for their preparing, a pharmaceutical composition eliciting activity with respect to hPPR, hPPR and inhibitory activity with respect to HMG-CoA-reductase and involving compound of the formula (I). Also, invention relates to methods for prophylaxis and treatment of different diseases caused by above said activity, a method for reducing the total cholesterol level and a method for reducing the glucose level. Invention provides preparing new compounds eliciting valuable biological properties.;EFFECT: improved preparing methods, valuable medicinal properties of compounds.;27 cl, 64 ex
机译:发明领域本发明涉及芳基羧酸的衍生物,并描述式(I)的化合物: 其中组R 1 ,R < Sup> 2 ,R 3 ,R 4 以及组R 5 和R 6 与碳原子连接的碳原子可以相同或不同,并且是指氢,卤素原子,羟基或烷基,烷氧基,苯基,羧酸或磺酸中的任选取代的基团;如果R 5 和R 6 中的一个或两个都与碳原子相连,也可以表示氧代基。如果R 5 和R与氮原子相连,则它们表示氢原子,羟基或任选取代的烷基或苄基; X表示氧原子,硫原子或NH中的杂原子。 Ar表示任选取代的二价的单或稠合的芳族或杂环基,其中芳环代表苯基,萘基且杂环基代表呋喃; R 7 是指氢,卤原子,烷氧基,烷基或与相邻的R 8 基团形成键; R 8 是指氢原子,羟基,烷氧基,烷基或任选取代的苄基;或R 8 与R 7 共同形成一个键; R 9 是指氢原子或烷基,苯基或苄基中的任选取代的基团; R 10 是指氢原子或烷基,苯基或苄基中的任选取代的基团; Y表示氧原子或NR 12 ,其中R 12 表示氢原子,烷基或苄基; R 10 和R 12 可以形成包含碳原子的常见的五元或六元环状结构,所述碳原子任选地涉及一个或多个选自氧,硫或氮原子的杂原子;由式-(CH 2 n -(O) m -表示的结合基团可以通过氮原子或碳原子连接原子,其中n是1-4的整数; m是在通过碳原子连接了结合基团的情况下,R 5 中的任一个R 6 表示氧代基的条件下的0〜1的整数。 Y表示氧原子; R 9 并不表示氢原子;或其衍生物,类似物,其互变异构形式,其立体异构体,其多晶型形式,其药学上可接受的盐,其药学上可接受的溶剂化物。另外,本发明还描述了通式(I)的化合物的制备方法,中间体化合物及其制备方法,引起对hPPR的活性,对hPPR的活性和对HMG-CoA-还原酶的抑制活性的药物组合物,并且涉及式(I)。本发明还涉及预防和治疗由上述活性引起的不同疾病的方法,降低总胆固醇水平的方法和降低葡萄糖水平的方法。发明提供了制备具有有价值生物学特性的新化合物。效果:改进的制备方法,化合物的有价值医学特性。27 cl,64 ex

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