(I). In formula (I), the ring P is selected from a five-membered heteroaryl having from one to two heteroatoms selected from the group consisting of N, O and S as a ring atom, and a five-membered heterocyclyl having one N heteroatom as a ring atom; the ring Q is selected from phenyl and pyridyl; A, B or Y are selected from -CH- and N; R1 is selected from alkyl containing from 1 to 6 carbon atoms, and cycloalkyl containing from 3 to 6 carbon atoms, where said alkyl, which contains from 1 to 6 carbon atoms, or cycloalkyl, which contains from 3 to 6 carbon atoms, are optionally further substituted with one or more groups selected from the group consisting of alkyl containing from 1 to 6 carbon atoms, halogen and haloalkyl containing from 1 to 6 carbon atoms; R2 is selected from halogen and haloalkyl containing from 1 to 6 carbon atoms; R3 are the same or different and are each independently selected from hydrogen, alkyl containing from 1 to 6 carbon atoms, cycloalkyl containing from 3 to 6 carbon atoms, five or six membered heterocyclyl having one O hetero atom as a ring atom, and oxo, where the specified alkyl containing from 1 to 6 carbon atoms is optionally additionally substituted by one or more than one group selected from the group consisting of halogen, hydroxyl, alkoxy containing from 1 to 6 carbon atoms, and hydroxyalkyl containing from 1 to 6 carbon atoms; R4 is selected from phenyl and pyridyl, where each of said phenyl and pyridyl is optionally further substituted by one or more groups selected from the group consisting of halogen and haloalkyl containing from 1 to 6 carbon atoms, where the specified halogenated containing from 1 to 6 carbon atoms preferably represents trifluoromethyl; s is an integer from 0 to 3; t is 0 or 1. Also provided are a method for preparing a compound of formula (I), intermediate compounds of formula (IA), (IB), a pharmaceutical composition, and the use of the compound of formula (I).;EFFECT: proposed compounds of formula (I) have the ability to inhibit microsomal prostaglandin E-synthase-1 and can be used to obtain the drug.;17 cl, 4 tbl, 63 ex"/> AMIDE DERIVATIVES AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, PREPARATION METHOD THEREFOR AND MEDICINAL APPLICATION THEREOF
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AMIDE DERIVATIVES AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, PREPARATION METHOD THEREFOR AND MEDICINAL APPLICATION THEREOF

机译:酰胺衍生物及其药学上可接受的盐,制备方法及其在医学上的应用

摘要

FIELD: chemistry.;SUBSTANCE: present invention relates to a compound of general formula (I), or its enantiomer, or mixtures thereof, or its pharmaceutically acceptable salts:; (I). In formula (I), the ring P is selected from a five-membered heteroaryl having from one to two heteroatoms selected from the group consisting of N, O and S as a ring atom, and a five-membered heterocyclyl having one N heteroatom as a ring atom; the ring Q is selected from phenyl and pyridyl; A, B or Y are selected from -CH- and N; R1 is selected from alkyl containing from 1 to 6 carbon atoms, and cycloalkyl containing from 3 to 6 carbon atoms, where said alkyl, which contains from 1 to 6 carbon atoms, or cycloalkyl, which contains from 3 to 6 carbon atoms, are optionally further substituted with one or more groups selected from the group consisting of alkyl containing from 1 to 6 carbon atoms, halogen and haloalkyl containing from 1 to 6 carbon atoms; R2 is selected from halogen and haloalkyl containing from 1 to 6 carbon atoms; R3 are the same or different and are each independently selected from hydrogen, alkyl containing from 1 to 6 carbon atoms, cycloalkyl containing from 3 to 6 carbon atoms, five or six membered heterocyclyl having one O hetero atom as a ring atom, and oxo, where the specified alkyl containing from 1 to 6 carbon atoms is optionally additionally substituted by one or more than one group selected from the group consisting of halogen, hydroxyl, alkoxy containing from 1 to 6 carbon atoms, and hydroxyalkyl containing from 1 to 6 carbon atoms; R4 is selected from phenyl and pyridyl, where each of said phenyl and pyridyl is optionally further substituted by one or more groups selected from the group consisting of halogen and haloalkyl containing from 1 to 6 carbon atoms, where the specified halogenated containing from 1 to 6 carbon atoms preferably represents trifluoromethyl; s is an integer from 0 to 3; t is 0 or 1. Also provided are a method for preparing a compound of formula (I), intermediate compounds of formula (IA), (IB), a pharmaceutical composition, and the use of the compound of formula (I).;EFFECT: proposed compounds of formula (I) have the ability to inhibit microsomal prostaglandin E-synthase-1 and can be used to obtain the drug.;17 cl, 4 tbl, 63 ex
机译:通式(I)的化合物或其对映异构体或它们的混合物或其药学上可接受的盐: (I)。在式(I)中,环P选自具有1至2个选自N,O和S作为环原子的杂原子的五元杂芳基和具有一个N杂原子作为基团的五元杂环基。环原子;环Q选自苯基和吡啶基; A,B或Y选自-CH-和N; R 1 选自含1至6个碳原子的烷基和含3至6个碳原子的环烷基,其中所述含1至6个碳原子的烷基或含C 1至C 6的环烷基。 3至6个碳原子,任选地进一步被一个或多个选自含1至6个碳原子的烷基,卤素和含1至6个碳原子的卤代烷基的基团取代; R 2 选自卤素和含1-6个碳原子的卤代烷基; R 3 相同或不同,各自独立地选自氢,含1至6个碳原子的烷基,含3至6个碳原子的环烷基,具有一个O杂原子的五或六元杂环基含1至6个碳原子的指定烷基任选被一个或多个选自卤素,羟基,含1至6个碳原子的烷氧基和氧的取代基取代;含有1至6个碳原子的羟烷基; R 4 选自苯基和吡啶基,其中所述苯基和吡啶基中的每一个任选地进一步被一个或多个选自卤素和含1-6个碳原子的卤代烷基的基团取代,其中含有1至6个碳原子的指定卤代基优选代表三氟甲基; s是0到3的整数; t为0或1。还提供了制备式(I)的化合物,式(IA),(IB)的中间体化合物,药物组合物的用途以及式(I)的化合物的用途。效果:拟议的式(I)化合物具有抑制微粒体前列腺素E-合酶-1的能力,可用于获得药物。; 17 cl,4 tbl,63 ex

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