首页> 外国专利> Pyrazolo3,4-bpyridin forbindelser, farmasoytisk preparat omfattende slike forbindelser samt anvendelse av disse for fremstilling av medikamenter for behandling av sykdom

Pyrazolo3,4-bpyridin forbindelser, farmasoytisk preparat omfattende slike forbindelser samt anvendelse av disse for fremstilling av medikamenter for behandling av sykdom

机译:吡唑并[3,4-b]吡啶化合物,包含此类化合物的药物组合物及其在制备用于治疗疾病的药物中的用途

摘要

The invention relates to a compound of formula (I) or a salt thereof: wherein: R1 is C1-4alkyl, C1-3fluoroalkyl or -(CH2)2OH; R2 is a hydrogen atom (H), methyl or C1fluoroalkyl; R3a is a hydrogen atom (H) or C1-3alkyl; R3 is optionally substituted branched C3-6alkyl, optionally substituted C3-8cycloalkyl, optionally substituted mono-unsaturated-C5-7cycloalkenyl, optionally substituted phenyl, or an optionally substituted heterocyclic group of sub-formula (aa), (bb) or (cc): in which n1 and n2 independently are 1 or 2; and Y is O, S, SO2, or NR4; and wherein Het is of sub-formula (i), (ii), (iii), (iv) or (v): The compounds are phosphodiesterase (PDE) inhibitors, in particular PDE4 inhibitors. Also provided is the use of a compound of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for the treatment and/or prophylaxis of an inflammatory and/or allergic disease in a mammal such as a human, for example chronic obstructive pulmonary disease (COPD), asthma, or allergic rhinitis.
机译:本发明涉及式(I)的化合物或其盐:其中:R 1为C 1-4烷基,C 1-3氟烷基或-(CH 2)2 OH; R 2是氢原子(H),甲基或C 1氟烷基; R3a是氢原子(H)或C1-3烷基; R 3是任选取代的支链C 3-6烷基,任选取代的C 3-8环烷基,任选取代的单不饱和C 5-7环烯基,任选取代的苯基或子式(aa),(bb)或(cc)的任选取代的杂环基:其中n1和n2分别为1或2; Y为O,S,SO 2或NR 4;其中Het是式(i),(ii),(iii),(iv)或(v)的化合物:化合物是磷酸二酯酶(PDE)抑制剂,特别是PDE4抑制剂。还提供了式(I)化合物或其药学上可接受的盐在制备用于治疗和/或预防哺乳动物(例如人)的炎症和/或过敏性疾病的药物中的用途,例如慢性阻塞性肺疾病(COPD),哮喘或过敏性鼻炎。

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