Amino-pyrimido-isoquinolinone derivs. - useful as hypotensives, bronchodilators and antiallergic agents

摘要

Pyrimido 6,1-a isoquinolinone derivs. of formula (I) and their acid-addn. and quat. ammonium salts are new: (R1-R3 are H, OH, 1-6C alkoxy or halogen, or adjacent R1-R3 gps. can form methyllenedioxy or ethylenedioxy; R4 is (i) H, (ii) 1-6C alkyl opt. substd. by 1-3C alkoxy, di(1-4C)alkylamino or di(1-4C)alkylphosphino(1-4C)alkyl, (iii) 3-6C cycloalkyl, (iv) =8C aralkyl opt. ring-substd. by halogen, NO2, 1-3C alkoxy and/or 1-3C alkyl, (v) heterocycloalkyl, (vi) aryl substd. by halogen, 1-3C alkyl, 1-3C alkoxy, 1-3C haloalkyl, NH2, OH and/or OM, or (vii) a lone pair if R5 is not a lone pair; M = alkali metal; R5 and R6 are (i) H, OH, 1-6C alkoxy, NH2, mono- or di-(1-3C alkyl)amino or arylamino, (ii) amino substd. by a 5- or 6-membered heterocyclic gp. contg. 1-3 heteroatoms selected from N, O and S, or (iii) 1-6C alkyl, 3-7C cycloalkyl, hydroxyl(1-6C)alkyl, alkoxy(1-6C)alkyl, dialkoxy-(1-6C)alkyl, 1-6C haloalkyl, dialkylaminoalkyl, 6-8C aralkyl, 1-6C acyl or opt. substd. =10C aryl; or R5 is a lone pair if R4 is not a lone pair; or NR5R6 is an opt. substd. heterocyclic gp. contg. another N or O heteroatom).