Chinoin Gyogyszer Es Vegyeszeti Termekek Gyara Rt.

Sanofi-aventis

Maria Balogh

Istvan Hermecz

Agnes Horvath

Judit Sipos

Aniko Pajor

Peter Ritli

Geza Kereszturi

Gabor Kovacs

Zoltan Kapui

Lelle Vasvari

Sandor Batori

Peter Aranyi

Tamas Szuts

Katalin Urban-Szabo

Endre Mikus

Lajos T Nagy

Laszlo Balazs

Tibor Szabo

Lelle V Vasvari Nee Debreczy

Christophe Philippo

Geza Timari

Kinga Boer

Judit Vargane Szeredi

Katalin Gerber

Judit Bence

Erzsebet Walcz

Zsuzsanna Tomoskozi

Zoltan Meszaros, Deceased

Jozsef Knoll

Laszlo Tardos

Philippe Bovy

Olivier Venier

Katalin Marmarosi

Claudie Namane

Klara Gyires

Michel Finet

Michel Aletru

Katalin Urban Szabo

Geza Keresturi

Lelle V Debreczy

Ilona Papp

Lelle Vasvavi

The present invention relates to substituted pyrimidine compounds of formula I useful as orexin receptor antagonists. The invention also relates to pharmaceutical compositions containing said compounds. 

Pyrimidine derivatives as orexin receptor antagonists

This invention is directed to a compound of formula (I), wherein R, R, R, R, R, R, R, R, R, R, X, Z, m, n, o, p and r are as defined herein, its preparation, pharmaceutical composition and use as an adenosine Areceptor ligand preferably an antagonist.

Imidazoquinoline derivatives as adenosine A3 receptor ligands

The present invention relates to the orexin receptor antagonists compounds of the general formula (I) as well as to their isomers, salts and solvates, to the pharmaceutical compositions containing them and to the therapeutic application thereof.

Pyrazole derivatives and use thereof as orexin receptor antagonists

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

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 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.

1-Methylamino-quinoline-carboxylic acid derivatives

Boric anhydrides of

Norfloxacin intermediate

Growing community of inventors

Dunakeszi, Hungary

Maria Balogh