Chinoin Gyogyszer Es Vegyeszeti Termekek Gyara Rt.

Tibor Breining

Istvan Hermecz

Agnes Horvath

Zoltan Meszaros

Lelle V Vasvari Nee Debreczy

Jozsef Kokosi

Sandor Virag

Gyorgy Szasz

Gyula Sebestyen

Attila Mandi

Gabor Nagy

Tamas Szuts

Istvan Bitter

Tamas Szucs

Lelle Vasvari, Nee Debreczy

Lelle Vasuarl Nee Debreczy

Lelle Vasvari Nee Debreczi

Istvan Bitteer

The invention relates to new azepino[1,2-a]pyrimidine derivatives--of the general formula ##STR1## wherein p=1, 2 and acid addition salts thereof which can be prepared by

Bronchodilatory azepino(1,2-A)pyrimidine derivatives and acid addition

New 3-substituted-2-oxo-tetrahydro-pyrrolo[1,2-a]pyrimidines of the formula (II) ##STR1## or a pharmaceutically acceptable acid addition or quaternary ammonium salts thereof are disclosed, wherein

3-Substituted-2-oxo-tetrahydro-pyrrol[1,2-a]pyrimidines having

New Rutecarpine analogs are disclosed having Rutecarpine-like activity, especially diuretic activity. Also a novel process for the preparation of the Rutecarpine analogs is disclosed.

Indolo[2',3';3,4]pyrido[2,1-b]quinazoline-5-ones, a process for the

Compounds of the formula I ##STR1## or pharmaceutically acceptable salts, hydrates, stereoisomers, optically active isomers, geometrical isomers or tautomeric forms thereof are disclosed wherein

Nitrogen bridgehead compounds having anti-allergic effect

A process for the preparation of nitrogen bridgehead condensed pyrimidine compounds of the general formula ##STR1## [wherein R represents hydrogen or lower alkyl;

Process for the preparation of

A process is disclosed for the preparation of compounds of the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are each hydrogen or lower alkyl;

Process for the preparation of nitrogen-bridgehead condensed pyrimidine

3 Substituted hexahydro-pyrimido[1, 2 a]azepines and quaternary derivatives, useful as antianginals are prepared. Specifically tested are 3 carboxylates and carbo hydrazides. 3 Cyano Carbamonyl and alkyl compounds are also disclosed.

2-Oxo-2,6,7,8,9,10 hexahydro-pyrimido[1,2-a]azepines and antianginal

Intermediates useful in the preparation of Rutecarpine and Rutecarpine derivatives are disclosed as well as a process for the preparation of said intermediates having the following formula: ##STR1## wherein R, R.sup.1 and R.sup.2 are the same or different and stand for hydrogen, halogen, nitro, carboxy, nitrile, alkoxy containing 1 to 4 carbon atoms, alkoxycarbonyl containing 1 to 4 carbon atoms in the alkoxy group, alkyl containing 1 to 4 carbon atoms, amino or hydroxy or R and R.sup.1 together stand for methylenedioxy, R.sup.2 stands for hydrogen, R.sup.3 represents hydrogen or alkyl containing 1 to 4 carbon atoms, R.sup.4 stands for phenyl, phenyl substituted by 1 to 3 same or different substituents selected from the group of halogen(s), alkyl, and alkoxy containing 1 to 4 carbon atoms, phenyloxy, hydroxy, nitro, amino, cyano, carboxy, alkoxycarbonyl having 1 to 4 carbon atoms, alkanoyl having 1 to 4 carbon atoms, methylenedioxy, trifluoromethyl, phenyl and dialkylamino having 1 to 4 carbon atoms in the alkyl part or naphthyl and the dotted line indicated an optional double bond. Also pharmaceutically acceptable acid addition and quaternary ammonium salts are disclosed.

6-Hydrazono-pyrido[2,1-b] quinazoline-11 ones

Chemical compounds having an effect on the circulatory system have the formulas ##STR1## or a mixture thereof, or a pharmaceutically suitable acid-addition salt or quaternary salt thereof, wherein

3-Substituted-tetrahydro-pyrrolo[1,2-a]pyrimidines and pharmaceutical

Antiallergic and antiasthmatic compounds of the formula ##STR1## of which 9-phenylamino-6-methyl-4-oxo-6,7-dihydro-4H-pyrido(1,2-a)pyrimidine-3-carb oxylic acid and optically active antipodes and salts thereof are examples.

Antiallergic nitrogen bridge-head compounds

Antiallergic and particularly antiasthmatic compounds of the formula: ##STR1## of which 9-phenylhydrazono-6-methyl-4-oxo-6,7,8,9-tetrahydro-4H-pyrido(1,2-a)pyrimi dine-3-carboxylic acid is an especially significant example.

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Budapest, Hungary

Tibor Breining