首页> 外国专利> 7- (Piperazin-1-ylmethyl) -1H-indole-2-carboxylic acid (phenyl) -amide derivatives and related compounds as MAP-QUINASA P38 inhibitors for the treatment of respiratory tract diseases.

7- (Piperazin-1-ylmethyl) -1H-indole-2-carboxylic acid (phenyl) -amide derivatives and related compounds as MAP-QUINASA P38 inhibitors for the treatment of respiratory tract diseases.

机译:7-(哌嗪-1-基甲基)-1H-吲哚-2-羧酸(苯基)-酰胺衍生物和相关化合物,作为MAP-QUINASA P38抑制剂,用于治疗呼吸道疾病。

摘要

Compounds of the general formula I ** Formula ** Ar means a substituent of the formula (II), (III) or (IV) wherein R3 means C1-6 alkyl, C3-6 cycloalkyl, C1-4 alkoxy, C1 perfluoroalkyl -2,3-methyl-oxetan-3-yl, - C1-2 perfluoroalkoxy, morpholinyl, wherein the cycloalkyl radical may eventually be substituted with C1-3 alkyl, wherein R4 means H, C1-4 alkyl, C1- alkoxy 4, wherein R5 means H, C1-5-sulfonyl-amino, C3-6-cycloalkyl-amino, (C1-5-sulfonyl) - (methyl) -amino, (C3-6-sulfonyl cycloalkyl) - (methyl) -amino, C1-5 alkylcarbonyl amino, C3-6-cycloalkyl amino, - (C1-5 alkylcarbonyl) - (methyl) -amino, (C3-6-carbonylcycloalkyl) - ( methyl) -amino, aminocarbonyl, C1-5-alkyl-carbonyl alkyl, C3-6 -cycloalkylcarbonyl, di- (C1-3alkyl) -aminocarbonyl, di- (C1-3alkyl) -amino-alkyl C1-2, di- (C1-3 alkyl) -amino-pyrrolidin-1-yl-C1-2 alkyl, 4-alkyl C1-5-piperazin-1-ylalkylC1-2, - 4-di- (C1-alkyl) 3) -amino-piperidin-1-yl-C1- alkyl 2,3-di- (C1-3 alkyl) -amino-piperidin-1-yl-C1-2 alkyl, C1-5 alkyl sulfinyl, C3-6 cycloalkyl sulfinyl, C1-5 alkyl sulfonyl, C3 cycloalkyl 6-sulfonyl, hydroxy-C1-2 alkyl, C1-5 alkyl sulfinyl methyl, C1-5 alkyl sulfonyl methyl, wherein R6 means C1-3 alkyl or phenyl, - wherein the radical C1-3 alkyl can be optionally substituted with hydroxy or di- (C1-3 alkyl) -amino and where the phenyl radical may eventually be substituted with fluorine or C1-3.alkyl where D or E means nitrogen, where G and E 'mean, of independently of one another, nitrogen or oxygen, - where R6 is only attached to E 'when E' means nitrogen, R1 means a C4-6 cycloalkyl system containing 1 to 2 nitrogen atoms that may eventually be mono- or disubstituted with R7, wherein R7 can be C1-3 alkyl, hydroxy, C1-3 alkoxy, amino, C1-3 alkyl, di- (C1-3 alkyl) -amino.- R2 means hydrogen, halogen or C1-alkyl 4; L means -C (H) or -N , M means -C (H) or -N , T means a C1-4 alkylene or bond, wherein the C1-4 alkylene radical may be substituted with C1-2 alkyl, - m means 0, 1, 2 or 3, n means 1, 2 or 3 , p means 0, 1, 2 or 3, where, as long as nothing else has been mentioned, the aforementioned alkyl groups may be straight or branched chain, - their tautomers, their stereoisomers, their mixtures and their salts, in especially its physiologically compatible salts.
机译:通式I **化合物** Ar表示式(II),(III)或(IV)的取代基,其中R3表示C1-6烷基,C3-6环烷基,C1-4烷氧基,C1全氟烷基- 2,3-甲基-氧杂环丁-3-基,-C1-2全氟烷氧基,吗啉基,其中环烷基可以最终被C1-3烷基取代,其中R4是指H,C1-4烷基,C1-烷氧基4,其中R 5表示H,C 1-5-磺酰基-氨基,C 3-6-环烷基-氨基,(C 1-5-磺酰基)-(甲基)-氨基,(C 3-6-磺酰基环烷基)-(甲基)-氨基,C 1 -5烷基羰基氨基,C3-6-环烷基氨基,-(C1-5烷基羰基)-(甲基)-氨基,(C3-6-羰基环烷基)-(甲基)-氨基,氨基羰基,C1-5-烷基-羰基烷基,C 3-6-环烷基羰基,二-(C 1-3烷基)-氨基羰基,二-(C 1-3烷基)-氨基-烷基C 1-2,二-(C 1-3烷基)-氨基-吡咯烷-1-基-C 1 -2烷基,4-烷基C1-5-哌嗪-1-基烷基C1-2,-4-二-(C1-烷基)3)-氨基-哌啶-1-基-C1-烷基2,3-二-( C 1-3烷基)-氨基-哌啶-1-基-C 1-2烷基,C 1-5烷基finyl,C3-6环烷基亚磺酰基,C1-5烷基磺酰基,C3环烷基6-磺酰基,羟基-C1-2烷基,C1-5烷基亚磺酰基甲基,C1-5烷基磺酰基甲基,其中R6表示C1-3烷基或苯基-,其中基团C1-3烷基可以任选地被羟基或二-(C1-3烷基)-氨基取代,并且其中苯基基团最终可以被氟或C1-3。烷基取代,其中D或E是氮,其中G和E'彼此独立地表示氮或氧,-其中R6仅连接到E',当E'表示氮时,R1表示包含1-2个氮原子的C4-6环烷基系统,最终可能是用R7单或二取代,其中R7可以是C1-3烷基,羟基,C1-3烷氧基,氨基,C1-3烷基,二-(C1-3烷基)-氨基。-R2是指氢,卤素或C1-烷基4; L表示-C(H)或-N,M表示-C(H)或-N,T表示C1-4亚烷基或键,其中C1-4亚烷基可以被C1-2烷基取代,-m表示0、1、2或3,n表示1、2或3,p表示0、1、2或3,其中,只要没有其他记载,上述烷基可以是直链或支链的,-它们的互变异构体,立体异构体,混合物和盐,特别是生理相容性盐。

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