首页> 外国专利> 7 - piperazin acid amides of carboxylic acid - 2 - 1H indole inhibitors of p38 MAP Kinases, medicines containing them and Use thereof for the treatment of respiratory diseases.

7 - piperazin acid amides of carboxylic acid - 2 - 1H indole inhibitors of p38 MAP Kinases, medicines containing them and Use thereof for the treatment of respiratory diseases.

机译:7-羧酸的哌嗪酰胺-p38 MAP激酶的2-1-1H吲哚抑制剂,包含它们的药物及其在治疗呼吸系统疾病中的用途。

摘要

That is proposed for the treatment of Diseases of the Airways in Asthma and COPD.Claim 1, characterized in that: compounds have the General formula (1) wherein R is a Substituent of the formula (2), (3) or (4), where R3 is C1 - C3 6 alkyl, cycloalkyl - 6, c1-4 alkoxy, Perfluoroalkyl C1 - 2, 3 - methyl - oxetan - 3 - ILO, perfluoroalcoxi c1-2, morfolinilo, where ra Dical cycloalkyl can be eventually replaced with c1-3 alkyl, wherein R4 is H,C1-4 alkyl, c1-4 alkoxy, wherein R5 C1 is H, alkyl sulfonyl amino - 5, - 6 cicloalquil C3 (alkyl sulfonyl Amine, 5 - C1 - (Methyl sulfonyl) amino) -, (cicloalquil C3 - 6 - - - (Methyl sulfonyl) amino) c1-5 alkyl carbonyl amino -, cicloalquil C3 - 6carbonil (C1 - amino - 5 - alkyl carbonyl) - (methyl) amino -, (C cicloalquil 3 - 6 - carbonyl) - (methyl) - amino alkyl aminocarbonilo, C1 - 5 - amino carbonylCicloalquil C3 - 6 - amino carbonyl, di - (c1-3 alkyl) - amino carbonyl, di - (c1-3 alkyl) amino - 2 - alkyl - C1, D - (c1-3 alkyl amino) - alkyl pyrrolidin-1-yl C1 - 2, 4 - C1 alkyl 5 - (piperazin-1-yl alkyl C1 - 2, 4 - Di - (c1-3 alkyl) amino - piperidin-1-yl alkyl C1 - 2, 3 - Di - (c1-3 alkyl) amino - piperidin-1-yl - alqui The c1-2, sulfinilo C15 alkyl -, 6 - sulfinilo cicloalquil C3, C1 - 5 - alkyl sulfonyl,Cicloalquil C3 - 6 - hydroxy alkyl sulfonyl, c1-2 alkyl, C1 - 5 - Methyl sulfinyl, c1-5 alkyl sulfonyl Methyl, wherein R6 is c1-3 alkyl or phenyl, alkyl radical where the C1 - 3 can be eventually replaced with Hydroxy alkyl - or di - (C1 3) - Amine and phenyl radical where the event can be Ualmente replaced with Fluorine or c1-3 alkyl, where D and e are Nitrogen, where G and E 'areIndependently of each other, nitrogen or Oxygen, wherein R6 is only attached to e when e is Nitrogen, R1 is a system containing cycloalkyl C4 - 6 1 2 nitrogen Atoms which may eventually be mono - or alkylated with R7, where R7 can be c1-3 alkyl, Hydroxy ALCO, XI c1-3 alkyl, amino, C1 - Di - (3 - amino, c1-3 alkyl) amino -, R2 is Hydrogen,C1-4 alkyl or Halogen; L - C or - N (H) , M - C or - N (H) , t is a link or alquileno c1-4, where radical alquileno c1-4 alkyl can be substituted with c1-2, M is 0, 1, 2, or 3, N is 1, 2 or 3, p is 0, 1, 2 or 3, where, if not mentioned otherwise, alqui groups The previously mentioned may be linear or branched chain, its tautomeros,Their stereoisomers, their mixtures and their salts, in particular their physiologically compatible Salts.
机译:提出用于治疗哮喘和COPD中的气道疾病的方法。权利要求1,其特征在于:具有通式(1)的化合物,其中R是通式(2),(3)或(4)的取代基,其中R3是C1-C3 6烷基,环烷基-6,c1-4烷氧基,全氟烷基C1-2,3-甲基-氧杂环丁烷-3-ILO,全氟代醇c1-2,morfolinilo,其中ra Dical环烷基最终可以被取代c1-3烷基,其中R4是H,C1-4烷基,c1-4烷氧基,其中R5 C1是H,烷基磺酰基氨基-5,-6环氯基C3(烷基磺酰基胺,5-C1-(甲基磺酰基)氨基)-,(cicloalquil C3-6---(甲基磺酰基)氨基)c1-5烷基羰基氨基-,cicloalquil C3-6羰基(C1-氨基-5-烷基羰基)-(甲基)氨基-,(C cicloalquil 3 -6-羰基)-(甲基)-氨基烷基氨基羰基,C1-5-氨基羰基环烷基C3-6-氨基羰基,二-(c1-3烷基)-氨基羰基,二-(c1-3烷基)氨基-2 -烷基-C1,D-(c1-3烷基氨基)-烷基py rrolidin-1-yl C1-2,4-C1烷基5-(哌嗪-1-基烷基C1-2,4-二-(c1-3烷基)氨基-哌啶-1-基烷基C1-2,3-二-(c1-3烷基)氨基-哌啶-1-基-烷基c1-2,亚磺酰基C15烷基-,6-亚磺酰基环氯C3,C1-5-烷基磺酰基,环烷基C3-6-羟基烷基磺酰基,c1 -2烷基,C1-5-甲基亚磺酰基,c1-5烷基磺酰基甲基,其中R6是c1-3烷基或苯基,C1-3可最终被羟基烷基-或二-(C1 3)取代的烷基-胺和苯基自由基,其中该事件可以被氟或c1-3烷基取代,而D和e为氮,其中G和E'彼此独立地为氮或氧,其中R6仅在e时与e相连是氮,R1是一个包含环烷基C4-6 1 2氮的系统,该原子最终可能被R7单或烷基化,其中R7可以是c1-3烷基,羟基ALCO,XI c1-3烷基,氨基,C1-Di -(3-氨基,c1-3烷基)氨基-,R2是氢,C1-4烷基yl或卤素; L-C或-N(H),M-C或-N(H),t是链环或alquileno c1-4,其中alquileno c1-4烷基可以被c1-2,M取代是0、1、2或3,N是1、2或3,p是0、1、2或3,其中,如果没有另外说明,alqui基团前面提到的可能是直链或支链,其互变异构体,它们的立体异构体,它们的混合物和它们的盐,特别是它们的生理相容性盐。

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