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dr. - substituoituja fenyylijohdannaisia phosphodiesterase inhibiittoreina

机译:博士-取代的苯基衍生物作为磷酸二酯酶抑制剂

摘要

Compounds of general formula (1) are described wherein Y is a halogen atom or a group -OR1, where R1 is an optionally substituted alkyl group; X is -O-, -S- or -N(R8)-, where R8 is a hydrogen atom or an alkyl group; R2 is an optionally substituted alkyl, alkenyl, cycloalkyl or cycloalkenyl group; R3 is a hydrogen or halogen atom or an -OR9 group, where R9 is a hydrogen atom or an optionally substituted alkyl, alkenyl, alkoxyalkyl, or alkanoyl group, or a formyl, carboxamido or thiocarboxamido group; R4 and R5, which may be the same or different, is each a group (CH2)nAr, where Ar is a monocyclic or bicyclic aryl group optionally containing one ore more heteroatoms selected from oxygen, sulphur or nitrogen atoms and n is zero or an integer 1, 2 or 3; R6 is a hydrogen atom or an optionally substituted alkyl group; R7 is a hydrogen atom or an optionally substituted alkyl group; and the salts, solvates, hydrates and N-oxides thereof. Compounds according to the invention are potent, selective and orally active PDE IV inhibitors and are useful in the prophylaxis and treatment of asthma and other diseases. IMAGE
机译:描述了通式(1)的化合物,其中Y为卤原子或-OR 1基团,其中R 1为任选取代的烷基; X为-O-,-S-或-N(R 8)-,其中R 8为氢原子或烷基; R 2为任选取代的烷基,烯基,环烷基或环烯基; R 3是氢或卤素原子或-OR 9基团,其中R 9是氢原子或任选取代的烷基,烯基,烷氧基烷基或烷酰基,或甲酰基,羧酰胺基或硫代羧酰胺基; R 4和R 5可以相同或不同,各自为基团(CH 2)n Ar,其中Ar为单环或双环芳基,任选地包含一个或多个选自氧,硫或氮原子的杂原子n为零或整数1、2或3; R 6为氢原子或可具有取代基的烷基。 R 7为氢原子或可具有取代基的烷基。及其盐,溶剂化物,水合物和N-氧化物。根据本发明的化合物是有效的,选择性的和口服活性的PDE IV抑制剂,并且可用于预防和治疗哮喘和其他疾病。 <图像>

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