, where R is selected from a group comprising hydrogen and C1-C10 alkyl, R1, R2, R3 and R4 are independently selected from a group comprising hydrogen, halogen, hydroxy, C1-C10 alkyl, substituted with 1-3 halogen atoms or C6-C14 acryl, C6-C14 aryl, -OR7, -SR7 and -SO2R7, where R7 is selected from a group comprising C1-C10 alkyl, C1-C10 alkyl substituted with C6-C14 aryl, C3-C10 cycloalkyl, C6-C14 aryl and C7-C8 heteroaryl containing 1-2 heteroatoms selected from a group comprising N, O and S, where C6-C14 aryl and C7-C8 heteroaryl are optionally substituted with 1-3 substitutes selected from a group comprising halogen, C1-C6 alkoxy, C1-C10 alkyl, C1-C6 dialkylamino and C4 heterocyclyl containing 2 heteroatoms selected from a group comprising nitrogen and oxygen, and R5 and R6 are independently selected from a group comprising hydrogen and C1-C3 alkyl, or pharmaceutically acceptable salts thereof. The invention also relates to novel cyanoquinoline derivatives of formula II , where R31, R32, R33 and R34 are independently selected from a group comprising hydrogen, hydroxy, halogen, C1-C10 alkyl substituted with 1-3 halogen atoms or with C6-C14 aryl, C6-C14 aryl, -OR37, -SR37 and -SO2R37, where R37 is selected from a group comprising C1-C10 alkyl, C1-C10 alkyl substituted with C6-C14aryl, C3-C10 aryl, C7-C8 heteroaryl containing 1-2 heteroatoms selected from a group comprising N, O and S, where C6-C14 aryl and C7-C8 heteroaryl are substituted with 1-3 substitutes selected from a group comprising halogen, C1-C6 alkoxy, C1-C10 alkyl, C1-C6 dialkylamino C4 heterocyclyl containing 2 heteroatoms selected from a group comprising nitrogen and oxygen, R35 denotes hydrogen or methyl, or pharmaceutically acceptable salts thereof. The invention also relates to specific cyanoisoquinoline compounds, a pharmaceutical composition based on the compound of formula I, a hypoxia-inducible factor (HIF) hydroxylase inhibiting method, a method of treating, preventing or slowing down development of a condition associated with hypoxia-inducible factor (HIF), a condition associated with erythropoietin (EPO), anaemia, based on use of the compound of formula I.;EFFECT: obtaining novel cyanoisoquinoline compounds having useful biological properties.;42 cl, 1 tbl, 54 ex"/> CYANOISOQUINOLINE COMPOUNDS (VERSIONS), PHARMACEUTICAL COMPOSITION BASED THEREON, HYPOXIA-INDUCIBLE FACTOR (HIF) HYDROXYLASE INHIBITING METHOD AND METHOD OF TREATING AND/OR PREVENTING HIF-ASSOCIATED CONDITION AND/OR ERYTHROPOIETIN-AND/OR ANAEMIA-ASSOCIATED CONDITION
首页> 外国专利> CYANOISOQUINOLINE COMPOUNDS (VERSIONS), PHARMACEUTICAL COMPOSITION BASED THEREON, HYPOXIA-INDUCIBLE FACTOR (HIF) HYDROXYLASE INHIBITING METHOD AND METHOD OF TREATING AND/OR PREVENTING HIF-ASSOCIATED CONDITION AND/OR ERYTHROPOIETIN-AND/OR ANAEMIA-ASSOCIATED CONDITION

CYANOISOQUINOLINE COMPOUNDS (VERSIONS), PHARMACEUTICAL COMPOSITION BASED THEREON, HYPOXIA-INDUCIBLE FACTOR (HIF) HYDROXYLASE INHIBITING METHOD AND METHOD OF TREATING AND/OR PREVENTING HIF-ASSOCIATED CONDITION AND/OR ERYTHROPOIETIN-AND/OR ANAEMIA-ASSOCIATED CONDITION

机译:氰基异喹啉化合物(版本),基于其的药物成分,低氧诱导因子(HIF)羟化酶抑制方法以及治疗和/或预防HIF伴随状况和/或红血球生成和/或氧化的方法

摘要

FIELD: chemistry.;SUBSTANCE: present invention relates to novel cyanoisoquinoline derivatives of formula I , where R is selected from a group comprising hydrogen and C1-C10 alkyl, R1, R2, R3 and R4 are independently selected from a group comprising hydrogen, halogen, hydroxy, C1-C10 alkyl, substituted with 1-3 halogen atoms or C6-C14 acryl, C6-C14 aryl, -OR7, -SR7 and -SO2R7, where R7 is selected from a group comprising C1-C10 alkyl, C1-C10 alkyl substituted with C6-C14 aryl, C3-C10 cycloalkyl, C6-C14 aryl and C7-C8 heteroaryl containing 1-2 heteroatoms selected from a group comprising N, O and S, where C6-C14 aryl and C7-C8 heteroaryl are optionally substituted with 1-3 substitutes selected from a group comprising halogen, C1-C6 alkoxy, C1-C10 alkyl, C1-C6 dialkylamino and C4 heterocyclyl containing 2 heteroatoms selected from a group comprising nitrogen and oxygen, and R5 and R6 are independently selected from a group comprising hydrogen and C1-C3 alkyl, or pharmaceutically acceptable salts thereof. The invention also relates to novel cyanoquinoline derivatives of formula II , where R31, R32, R33 and R34 are independently selected from a group comprising hydrogen, hydroxy, halogen, C1-C10 alkyl substituted with 1-3 halogen atoms or with C6-C14 aryl, C6-C14 aryl, -OR37, -SR37 and -SO2R37, where R37 is selected from a group comprising C1-C10 alkyl, C1-C10 alkyl substituted with C6-C14aryl, C3-C10 aryl, C7-C8 heteroaryl containing 1-2 heteroatoms selected from a group comprising N, O and S, where C6-C14 aryl and C7-C8 heteroaryl are substituted with 1-3 substitutes selected from a group comprising halogen, C1-C6 alkoxy, C1-C10 alkyl, C1-C6 dialkylamino C4 heterocyclyl containing 2 heteroatoms selected from a group comprising nitrogen and oxygen, R35 denotes hydrogen or methyl, or pharmaceutically acceptable salts thereof. The invention also relates to specific cyanoisoquinoline compounds, a pharmaceutical composition based on the compound of formula I, a hypoxia-inducible factor (HIF) hydroxylase inhibiting method, a method of treating, preventing or slowing down development of a condition associated with hypoxia-inducible factor (HIF), a condition associated with erythropoietin (EPO), anaemia, based on use of the compound of formula I.;EFFECT: obtaining novel cyanoisoquinoline compounds having useful biological properties.;42 cl, 1 tbl, 54 ex
机译:技术领域本发明涉及式I的新型氰基异喹啉衍生物。<图像文件=“ 00000176.GIF” he =“ 52” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 73” />,其中R选自氢和C 1 -C 10 烷基,R 1 ,R 2 , R 3 和R 4 独立地选自氢,卤素,羟基,C 1 -C 10 被1-3个卤原子或C 6 -C 14 丙烯酸,C 6 -C 14 取代的烷基>芳基,-OR 7 ,-SR 7 和-SO 2 R 7 ,其中R 7 选自C 1 -C 10 烷基,C 1 -C 10 被C 6 -C 14 芳基取代的烷基,C 3 -C 10 环烷基,C 含有1-2个选自N,O的杂原子的6 -C 14 芳基和C 7 -C 8 杂芳基和S,其中C 6 -C 14 芳基和C 7 -C 8 杂芳基任选被1取代-3个选自卤素,C 1 -C 6 烷氧基,C 1 -C 10 的取代基烷基,C 1 -C 6 二烷基氨基和C 4 杂环基,其中含有2个选自氮和氧的杂原子,以及R 5 和R 6 独立地选自氢和C 1 -C 3 烷基或其药学上可接受的盐。本发明还涉及式II的新型氰基喹啉衍生物。<图像文件=“ 00000177.GIF” he =“ 51” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 70” />,其中R 31 < / Sup>,R 32 ,R 33 和R 34 独立地选自氢,羟基,卤素,C 被1-3个卤原子或C 6 -C 14 芳基取代的1 -C 10 烷基,C 6 -C 14 芳基,-OR 37 ,-SR 37 和-SO 2 R 37 ,其中R 37 选自C 1 -C 10 烷基,C 被C 6 -C 14 芳基,C 3 -C取代的1 -C 10 烷基 10 芳基,C 7 -C 8 杂芳基,包含1-2个选自N,O和S的杂原子,其中C 6 -C 14 芳基和C 7 -C 8 杂芳基被1-3个选自co含卤素,C 1 -C 6 烷氧基,C 1 -C 10 烷基,C 1 -C 6 二烷基氨基C 4 杂环基,包含2个选自氮和氧的杂原子,R 35 表示氢或甲基或其药学上可接受的盐。本发明还涉及特定的氰基异喹啉化合物,基于式I化合物的药物组合物,低氧诱导因子(HIF)羟化酶抑制方法,治疗,预防或减慢与低氧诱导性疾病有关的疾病的发展的方法。因子(HIF),一种与促红细胞生成素(EPO)相关的疾病,贫血,基于使用式I化合物的影响;效果:获得具有有用生物学特性的新型氰基异喹啉化合物; 42 cl,1 tbl,54 ex

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