首页> 外国专利> Pyrido (2,3-d) pyrimidine derivatives, their use, pharmaceutical compositions containing them, processes for preparing the pyrido (2,3-d) pyrimidine derivatives and intermediates useful in the processes

Pyrido (2,3-d) pyrimidine derivatives, their use, pharmaceutical compositions containing them, processes for preparing the pyrido (2,3-d) pyrimidine derivatives and intermediates useful in the processes

机译:吡啶基(2,3-d)嘧啶衍生物,它们的用途,包含它们的药物组合物,制备吡啶基(2,3-d)嘧啶衍生物的方法和可用于该方法的中间体

摘要

The pyrido[2,3-d]pyrimidines are of the formulawherein R2 is hydrogen, hydroxy, alkyl, alkylthio, phenyl, 4-methoxyphenyl, 4-chlorophenyl, 1-pyrrolidinyl or methylphenylamino; R5 is hydroxy, alkylamino, 2-hydroxyethylamino, 2-alkoxymethylamino, dialkylamino, 4-methyl-1-piperazinyl, 4-morpholinyl or 1-pyrrolidinyl or amino with the provisos that if R8 is alkyl and R2 is phenyl then is other than amino and if R8 is alkyl and R2 is alkylthio then R5 is other than 1-pyrrolidinyl; is alkoxy, amino, mono- ordialkylamino, 2-hydroxyethylamino, 2-alkoxymethylamino or 2-(dialkylamino)-ethylamino; and R6 is hydrogen, alkyl, 2-alkoxyethyl, allyl, propargyl, phenyl, 4-methoxyphenyl, 4-chlorophenyl, benzyl, 4-methoxybenzyl, 4-chlorobenzyl, 4-(4-morpholinyl)-phenyl or piperonyl. The compounds are useful as anti-secretory agents. Some also exhibit anti-allergy activity. Processes for preparing the compounds are described and also novel intermediates useful in the processes.
机译:吡啶并[2,3-d]嘧啶具有下式 <图像文件=“ IMGA0001.GIF” he =“ 28” imgContent =“ chem” imgFormat =“ GIF” inline =“ no” wi =“ 41” /> 其中R 2 是氢,羟基,烷基,烷硫基,苯基,4-甲氧基苯基,4-氯苯基,1-吡咯烷基或甲基苯基氨基; R 5 是羟基,烷基氨基,2-羟基乙基氨基,2-烷氧基甲基氨基,二烷基氨基,4-甲基-1-哌嗪基,4-吗啉基或1-吡咯烷基或氨基,前提是如果R 8 是烷基,R 2 是苯基,则 <图像文件=“ IMGA0002.GIF” he =“ 4” imgContent =“ math” imgFormat =“ GIF“ inline =” yes“ wi =” 4“ /> 不是氨基,如果R 8 是烷基,R 2 是烷硫基,则R < Sup> 5 不是1-吡咯烷基。 <图像文件=“ IMGA0003.GIF” he =“ 4” imgContent =“ math” imgFormat =“ GIF” inline =“ yes” wi =“ 4” /> 是烷氧基,氨基,单或二烷基氨基,2-羟基乙基氨基,2-烷氧基甲基氨基或2-(二烷基氨基)-乙基氨基;和R 6 是氢,烷基,2-烷氧基乙基,烯丙基,炔丙基,苯基,4-甲氧基苯基,4-氯苯基,苄基,4-甲氧基苄基,4-氯苄基,4-(4-吗啉基) -苯基或胡椒基。该化合物可用作抗分泌剂。有些还具有抗过敏活性。描述了制备化合物的方法,以及在该方法中有用的新型中间体。

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