Pyrido (2,3-d) pyrimidine derivatives, pharmaceutical compositions containing them and processes for preparing the pyrido (2,3-d) pyrimidine derivatives
申请人:AMERICAN HOME PRODUCTS CORPORATION
公开号:EP0018139A2
公开(公告)日:1980-10-29
The pyrido[2,3-d]pyrimidines are of the formula
wherein 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.
吡啶并[2,3-d]
嘧啶的结构式为
其中 R2 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;R5 是羟基、烷基
氨基、2-羟乙基
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,但如果 R8 是烷基,R2 是
苯基,则不是
氨基,如果 R8 是烷基,R2 是烷
硫基,则 R5 不是 1-
吡咯烷基; R6是
氢、烷基、2-烷
氧基乙基、
烯丙基、
丙炔基、
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。这些化合物可用作抗分泌剂。有些化合物还具有抗过敏活性。本文介绍了制备这些化合物的工艺以及在这些工艺中有用的新型
中间体。