Chinoin Gyogyszer Es Vegyeszeti Termekek Gyara Rt.

Gyogyszerkutato Intezet Kft.

Schering Aktiengesellschaft

Egis Gyogyszergyar

Other

Egis Gyogyszergyar Rt.

Ivax Drug Research Institute

Chinoin Gyogyszer Rt

Antal Simay

Imre Moravcsik

Kalman Takacs

Ferenc Andrasi

Katalin Horv&aacute;th

Gabor Kovacs

Eva Somfai

P&aacute;l Berzsenyi

Ilona Kiss Nee Ajzert

Sandor Virag

Tamas Hamori

Pal Berzsenyi

Istvan Tarnawa

Peter Matyus

Gizella &Aacute;brah&aacute;m

Istv&aacute;n Tarnawa

Ildik&oacute; Varga

Istv&aacute;n Ling

Ferenc Andr&aacute;si

Alice Druga

P&eacute;ter M&aacute;tyus

Jozsef Knoll

Gyula Sebestyen

Lajos Toldy

Istvan Stadler

Kalman Nagy

Endre Kasztreiner

Katalin Goldschmidt

Zoltan Zubovics

Gyula Papp

Gyorgy Lugosi

Istvan Ling

Laszlo Simandi

Sandor Solyom

Zoltan Torok

Gyorgy Krasznai

Karoly Mozsolits

Laszlo Sebestyen

Peter L Nagy

Eszter Szentkuti

Marta Szollosy

Istvan Sziraki

Peter Literati Nagy

Eva Szinnyei

Janos Bodnar

Zsuzsanna Fittler

Matyas Szentivanyi

Ferenc Szederkenyi

Katalin Eszter Horvath

Eva Gal

Lajos Farkas

Emese Csuzdi

Valeria Vitkoczi

Agnes Papp

Erzsebet Zara

Eszter Hodula

Klara Sutka

Lajos Toldi

N&aacute;ndor Makk

Ilona K Ajzert

Peter N Literati

Gy&ouml;rgy Rabloczky

M&aacute;rta Varga

Egon K&aacute;rp&aacute;ti

Istv&aacute;n Kir&aacute;ly

S&aacute;ndor S&oacute;lyom

Gy&ouml;rgy M&aacute;th&eacute;

L&aacute;szl&oacute; Sebesty&eacute;n

Istv&aacute;n Pallagi

Tam&aacute;s H&aacute;mori

Janos Bergmann

Gabor Feher

Eva Kovacs Nee Bozo

Marta Rusz

Ildiko Mathe

Gyorgyi Vereczkey Nee Donath

Ernese Csuzdi

Judit Kos&aacute;ry

Katalin Farago

L&aacute;szl&oacute; H&aacute;rsing

Gyula Horvath

Tibor Balogh

Jeno Korosi

Peter Botka

Laszlo Szekeres

Gabor Zolyomi

Giorgio Cignarella

Gyorgy Somogyi

Erno Orban

Istvan Pallagi

Sandor Boros

Istvan Turcsan

Istvan Jelinek

Melinda Gal

Agnes Papp Nee Behr

Sandor J Nagy

Tivadar Rettegi

Laszlo Gabor Harsing

Ildiko Varga

Tibor Hasko

Pyridazino(4,5-b)(1,5)oxazepinone, -thiazepinone and -diazepinone compounds

Compounds of formula I are described, their production and use in pharmaceutical agents.

Condensed 2,3-benzodiazepine derivatives and their use as AMPA-receptor inhibitors

2,3-benzodiazepine derivatives

The invention concerns compounds of formula (I), in which R,, R,, R,and R,mean hydrogen or different substituents; X means hydrogen or halogen; Y means C,alkoxy or X and Y together mean &mdash;O&mdash;(CH,),&mdash;O&mdash;; n means 1, 2 or 3; and A together with nitrogen forms a saturated or unsaturated five-member heterocycle which can contain between 1 and 3 nitrogen atoms and/or an oxygen atom and/or one or two carbonyl groups. Owing to their non-competitive inhibiting of the AMPA receptors, these compounds can be used as medicaments for treating diseases of the central nervous system.

The present invention relates to novel, antiarrhythmically active phenoxyalkylamine derivatives possessing a double point of attack. More particularly, the present invention relates to new phenoxyalkylamine derivatives of the formula (1)

Antiarrhythmic compounds

The invention relates to R-2-&lsqb;3-(&lsqb;1,4&rsqb;benzodioxan-2-ylmethylamino)-1-propyl&rsqb;-3(2H)-pyridazinone of formula (1), and to S-2-&lsqb;3-(&lsqb;1,4&rsqb;benzodioxan-2-ylmethylamino)-1-propyl&rsqb;-3(2H)-pyridazinone of formula (2), and to acid-addition salts thereof as well as pharmaceutical compositions containing these compounds. Furthermore, the invention relates to a process for the preparation of the above compounds. The new starting compounds of formulae (4) and (5) are also involved in the scope of the invention. The compounds according to the invention possess &agr;,- and &agr;,-adrenoceptor antagonistic effects and urogenital selectivity. Thus, they are useful for the treatment of the benign prostate hyperplasia.

N-(&lsqb;1,4&rsqb;benzodioxan-2-ylmethyl)-N-(3-chloro-1-propyl)-amine

2,3-benzodiazepine derivatives and their use as AMPA-receptor inhibitors

The invention relates to R-2-&lsqb;3-(&lsqb;1,4&rsqb;benzodioxan-2-ylmethylamino)-1-propyl&rsqb;-3(2H)-pyridazionone of formula (1)

3(2H)-pyridazinone derivatives and pharmaceutical compositions containing these compounds

An N-benzoylamino acid compound of the formula (I), ##STR1## wherein R.sup.3 is an NR.sup.4 R.sup.5 group where R.sup.4 and R.sup.5 which are the same or different are selected from the group consisting of hydrogen, a hydroxyl group, a C.sub.1-12 alkyl group, a C.sub.1-4 alkyl group substituted by a hydroxyl group and a C.sub.1-4 alkyl group substituted by an amino group;

N-benzoylamino acid derivatives, pharmaceutical compositions containing

3-substituted 3H-2, 3-benzodiazepine derivatives, the production and use

The invention relates to novel N-benzoylamino acid derivatives of the general formula (I), ##STR1## wherein R.sup.1 and R.sup.2, which are the same or different, stand for a hydroxyl group optionally bearing an acetyl group; or a C.sub.1-6 alkoxy group optionally substituted by a phenyl group;

N-benzoyl amino acid derivatives pharmaceutical compositions containing

The invention relates to a process for the preparation of 1-(3-chlorophenyl)-4-methyl-7,8-dimethoxy-5 H-2,3-benzodiazepine of formula (I) ##STR1## in high purity and in a quality suitable for pharmaceutical purposes. According to the invention the reaction of 1 mole of 2-acetonyl-3'-chloro-4,5-dimethoxybenzophenone of formula (II) ##STR2## with 3-7 moles of hydrazine hydrate in an organic solvent or in a mixture of organic solvents at a temperature between 15.degree. C. and 85.degree. C. is carried out in the absence of air oxygen, optionally in the presence of water. The crude product is then recrystallized from an aliphatic alcohol containing 1 to 5 carbon atom(s).

Process for the preparation of high-purity

The invention relates to an improved process for the preparation of 2,2-dimethyl-5-(2,5-dimethylphenoxy)-pentanoic acid of Formula (I) ##STR1## which comprises reacting an ester of the general Formula (X) ##STR2## wherein X represents halogen and Z stands for a straight or branched chain C.sub.1-8 alkylene group optionally substituted by one or two 2,2-dimethyl-5-halopentanoyloxy group(s), wherein halo represents chlorine or bromine, and in which alkylene group one or two methylene group(s) may be optionally replaced either by hetero atom(s) or by a bivalent heterocyclic group--with an alkali salt of 2,5-dimethylphenol of Formula (II) ##STR3## or with an ester of the latter formed with a lower alkanoic acid, and hydrolizing the aryloxy-substituted ester of the general Formula (XI) thus obtained. ##STR4## Furthermore the invention relates to intermediate compounds of the general Formula (X), wherein X and Z are as stated above, and to a process for the preparation thereof.

Process for the preparation of

The present invention relates to a pharmaceutical composition comprising as active ingredient a compound of the Formula I ##STR1## wherein R.sup.1 stands for straight or branched chain alkyl comprising 1 to 8 carbon atoms; phenyl alkyl having 7 to 10 carbon atoms; phenyl; or cycloalkyl comprising 3 to 8 carbon atoms;

Psychostimulant agent

The invention relates to an improved process for the preparation of 2,2-dimethyl-5-(2,5-dimethylphenoxy)-pentanoic acid of Formula (I) ##STR1## which comprises reacting an ester of the general Formula (X) ##STR2## wherein X represents halogen and Z stands for a straight or branched chain C.sub.1-8 alkylene group optionally substituted by one or two 2,2-dimethyl-5-halopentanoyloxy group(s), wherein halo represents chlorine or bromine, and in which alkylene group one or two methylene group(s) may be optionally replaced either by hetero atom(s) or by a bivalent heterocyclic group--with an alkali salt of 2,5-dimethylphenol of Formula (II) ##STR3## or with an ester of the latter formed with a lower alkanoic acid, and hydrolizing the aryloxy-substituted ester of the general Formula (XI) thus obtained. Furthermore the invention relates to intermediate compounds of the general Formula (X), wherein X and Z are as stated above, and to a process for the preparation thereof.

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Budapest, Hungary

Antal Simay