Chinoin Gyogyszer Es Vegyeszeti Termekek Gyara Rt.

Chinoin Gyogyszer Es Vegyeszeti

Judit Sipos

Istvan Hermecz

Agnes Horvath

Peter Ritli

Aniko Pajor

Maria Balogh

Geza Kereszturi

Lelle Vasvari

Gabor Kovacs

Lelle V Vasvari Nee Debreczy

Jozsef Knoll

Laszlo Tardos

Tamas Szuts

Klara Gyires

Katalin Marmarosi

Maria Blaogh

Zoltan Meszaros, Deceased

Zoltan Kapui

Istv&aacute;n Hermecz

Gergely H&eacute;ja

Judit Bence

Gy&ouml;rgyn&eacute; Szvoboda

Lelle V Debreczy

P&eacute;ter Moln&aacute;r

Ilona Papp

K&aacute;roly K&aacute;nai

S&aacute;ndor B&aacute;tori

Lelle Vasvavi

Geza Keresturi

Viktor Lakics

S&aacute;ndor Erd&ouml;

Maria Halogh

Andrea Szappanos

Mari&aacute; Balogh

&Aacute;gnes Horv&aacute;th

Bodor Veronika B&aacute;rt&aacute;ne

Zsolt P&aacute;rk&aacute;nyi

Marie Balogh

The present invention relates to new prolylendopeptidase inhibitors of general formula (I).

Prolylendopeptidase inhibitors

3-(substituted tetrazolyl)-4-oxo-4H-pyrido-[1,2-a]pyrimidines, salts

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

The invention relates to a new process for the preparation of antibacterial compounds of the Formula I ##STR1## wherein R.sup.1 stands for phenyl substituted by 1 or 2 halogen atoms;

Process for the preparation of quinoline carboxylic acid derivatives

The invention relates to a new process for the preparation of compounds of the general Formula I ##STR1## wherein R stands for piperazinyl, 4-methyl-piperazinyl or 4-ethyl-piperazinyl group and pharmaceutically acceptable salts thereof which comprises reacting a compound of the general Formula II ##STR2## wherein R.sup.1 and R.sup.2 stand for halogen, for an aliphatic acyloxy group containing 2 to 6 carbon atoms and optionally substituted by halogen, or for an aromatic acyloxy group containing 7 to 11 carbon atoms with a piperazine derivative of the general Formula III ##STR3## wherein R.sup.3 stands for hydrogen, methyl or ethyl or a salt thereof and subjecting the compound of the general Formula IV ##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 general Formula I thus obtained into a salt thereof or setting free the same from its salt. The compounds of the general Formula I are known antibacterial agents.

Process for the preparation of quinoline carboxylic acids

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.

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

Baron chelates of quinoline carboxylic acids

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.

Quinoline carboxylic acid boric acid anhydrides

1-Methylamino-quinoline-carboxylic acid derivatives

Boric anhydrides of

Norfloxacin intermediate

Growing community of inventors

Budapest, Hungary

Judit Sipos