Chinoin Gyogyszer Es Vegyeszeti Termekek Gyara Rt.

Lelle V Vasvari Nee Debreczy

Agnes Horvath

Istvan Hermecz

Zoltan Meszaros

Tibor Breining

Sandor Virag

Jozsef Kokosi

Jozsef Knoll

Judit Sipos

Gabor Kovacs

Laszlo Tardos

Peter Szentmiklosi

Klara Gyires

Agoston David

Gyula Sebestyen

Tamas Szuts

Istvan Bitter

Gyorgy Szasz

Maria Blaogh

Attila Mandi

Gabor Nagy

Maria Balogh

Peter Ritli

Aniko Pajor

Geza Kereszturi

Tamas Szucs

Katalin Marmarosi Nee Kellner

Gabor Horvath

Jozsef Lengyel

Jozse Knoll

Istvan Hurmecz

Ilona Erdelyi

Istvan Hermes

Geza Kerszturi

The present invention relates to novel 4-oxo-4H-pyrido[1,2-a]pyrimidine-3-carboxamide derivatives of the general formula (I) and the acid addition salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the general formula (I) ##STR1## R stands for a C.sub.1-12 alkyl group optionally substituted by a C.sub.1-4 alkoxycarbonyl group; a C.sub.3-9 cycloalkyl, adamantyl or optionally substituted phenyl group;

Pyridopyrimidine derivatives, pharmaceutical compositions containing

A method of using a compound of the Formula (V) ##STR1## or a pharmaceutically acceptable salt thereof is disclosed, wherein R.sup.1 and R.sup.2 are each C.sub.1 to C.sub.6 aliphatic acyloxy, unsubstituted or substituted by halogen, or are each C.sub.7 to C.sub.11 aromatic acyloxy, for preventing amination of the 6-position when a compound of the Formula (I) ##STR2## or a pharmaceutically acceptable salt thereof is to be formed, which comprises the steps of:

Process for the preparation of quinoline carboxyolic acids

The present invention relates to novel 4-oxo-4H-pyrido[1,2-a]pyrimidine -3-carbonamide derivatives of the general formula (I) and the acid addition salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the general formula (I) ##STR1## wherein: R stands for a C.sub.1-12 alkyl group optionally substituted by a C.sub.1-4 alkoxycarbonyl group; a C.sub.3-9 cycloalkyl, adamantyl or optionally substituted phenyl group;

Pyridopyrimidine derivatives useful in treatment of ulcers

The invention relates to a new process for the preparation of compounds of the Formula I ##STR1## (wherein R stands for hydrogen or methyl) and pharmaceutically acceptable salts thereof which comprises reacting a compound of the Formula V ##STR2## (wherein R.sup.1 and R.sup.2 stand for an aliphatic acyloxy group comprising 2-6 carbon atoms and optionally substituted by halogen; or for an aromatic acyloxy group comprising 7-11 carbon atoms) with an amine of the Formula VI ##STR3## (wherein R has the same meaning as stated above) or a salt thereof and subjecting the compound of the Formula VII ##STR4## thus obtained (wherein R, R.sup.1 and R.sup.2 are as stated above) to hydrolysis after or without isolation and if desired converting the compound of the Formula I thus obtained into a salt thereof or setting free the same from its salt. The compounds of the Formula I are known antibacterial agents. The advantage of the process of the present invention is that it makes the desired compounds of the Formula I available in a simple manner, with high yields and in a short reaction time.

Process for the preparation of quinoline carboxylic acids

N,N,N-trimethyl-2-hydroxyethyl-ammonium-[1-ethyl-6-fluoro-4-oxo-7-(1-pipera zinyl)-1,4-dihydro-quinolizine-3-carboxylate] of the formula I ##STR1## as a norfloxacin antimicrobial salt capable of enteral administration.

Medicinal norfloxacin salts

The invention relates to a process for the restoration and prevention of gastrointestinal injuries, which comprises treating a patient with an effective dose of racemic or optically active 1,6-dimethyl-4-oxo-1,6,7,8,9,9a-hexahydro-4H-pyrimido[1,2-a]pyrimidine-3-c arboxamide.

Treating process

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

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

New optionally racemic or optically active pyrimido(1,2a) heterocyclic compounds of the formula ##STR1## wherein m is 0, 1 or 2,

Antiphlogistic and anticoagulant condensed pyrimidine derivatives

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.

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Budapest, Hungary

Lelle V Vasvari Nee Debreczy