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    • 5. 发明专利
    • DE2315422A1
    • 1973-10-04
    • DE2315422
    • 1973-03-28
    • CHINOIN GYOGYSZER ES VEGYESZET
    • CEHMLNG ZOLTAN MESZAROS DRKNOLL HOZSEF DRHERMECZ ISTVANVASVARI GEB DEBRECZY LELLESZENTMIKLOSI PETER DRSIMON GEB PARKANYI PIROSKAHORVATH AGNESDAVID AGOSTON DRHORVATH GABOR DRDVORTSAK PETERKOVACS GEB MINDLER VERA DR
    • C07D471/04C07D57/20
    • 1428845 Substituted pyrido-pyrimidines and 2-pyridyl-1-pyrroles and their pharmaceutical compositions CHINOIN GYOGYSZER ES VEGYESZETI TERMEKEK GYARA RT 28 March 1973 [29 March 1972] 14960/73 Heading C2C The invention comprises (a) pyridopyrimidines of general Formula Ia wherein R 4 is a carboxyl, alkoxyearbonyl, carbhydrazide, carboxamide or nitrile group; R 1 and R 2 are each hydrogen or together represent the group attached to two adjacent carbon atoms of the ring A; the ring A is optionally substituted by one or two substituents selected from alkyl, nitro, hydroxy, alkoxy, amino, carboxyl, alkoxycarbonyl, carboximide, alkylamino, and carboxylic acylamino group and halogen atoms and p is 1 or 2 which may be prepared by cyclizing a compound of Formula II wherein R 1 , R 2 , ring A and p are as defined above and R 5 and R 6 are independently carboxyl or alkoxycarbonyl groups to form a compound of Formula Va wherein R 1 , R 2 , ring A, R 6 and p are as defined above and optionally modifying the group R 6 by known methods to obtain a compound of Formula Ia, (b) pyridyl-pyrroles of general Formula Ib wherein R 1 , R 2 , R 4 and ring A are as defined above and R 3 is hydrogen, halogen, hydroxyl, alkoxy, aralkoxy, aryloxy, nitro, or amino which may be prepared by cyclizing a compound of Formula II in which p is 1 to obtain a compound of Formula Vb wherein R 1 , R 2 , ring A and R 5 are as defined above and R 7 is hydrogen, halogen or hydroxyl optionally followed by modification of the group R 7 by known methods to obtain a compound of Formula Ib and (c) tautomers of compounds of Formula Ib in which R 7 is OH and acid addition and quaternary ammonium salts of the compounds of Formulµ Ia and Ib. Pharmaceutical compositions having analgesic, anti-inflammatory and antipyretic activity comprise a compound of Formula Ia and Ib or a pharmaceutically acceptable salt thereof together with a pharmaceutically acceptable carrier.