Chinoin Gyogyszer Es Vegyeszeti Termekek Gyara Rt.

Chinoin Gyogyszer Es Vegyeszeti

Eszakmagyarorszagi Vegyimuvek

Chinoin Pharmaceutical and Chemical Works Ltd.

Alkaloida Vegyeszeti Gyar Rt.

Alkaloida Vegyeszeti Gyar Tiszavasvari

Sandor Makleit

Jozsef Knoll

Rezso Bognar

Zoltan Meszaros

Agoston David

Gyula Valovics

Zsuzsanna Furst

Istvan Hermecz

Attila Mandi

Gabor Nagy

Peter Szentmiklosi

Laszlo Litkei

Istvan Gyoker

Sandor J Nagy

Geza Kiss

Sandor Berenyi

Gyorgy Toth

Attila Zoltai

Sandor Elek

Terez Mile

Istvan Toth

Karoly Balogh

Ferenc Mogyorodi

Tibor Bodi

Sandor Hosztafi

Eniko Koppany

Kalmany Zsupan

Zoltan Dinya

Laszlo Szlavik

Laszlo Szilagyi

Laszlo Szavik

Reszo Bognar

Gyorgy Litkei

Miklos Rakosi

The present invention relates to novel morphinane-skeletoned compounds of the formula (I) ##STR1## wherein Y in-NH phenyl or --NH dintro phenyl, Z is --CH.sub.2 -- CH.sub.2, R.sub.2 is hydroxyl and R.sub.3 is H or methyl, the steric isomers and the pharmaceutically acceptable salts thereof, a novel process for producing the same and pharmaceutical compositions comprising the same as active ingredients. The novel compounds can be used in the therapy as analgetic or morphine-antagonistic agents.

Morphinane-skeletoned hydrazone derivatives

The invention relates to a novel process for preparing chloroacetanilides of the formula ##STR1## wherein: R.sub.1 and R.sub.2 represent independently from each other a hydrogen atom or a C.sub.1-8 alkyl or C.sub.1-8 alkoxy group; and

Process for the preparation of substituted chloroacetanilides

Azidoethylmorphine, a new 7,8-dihydroisomorphine derivative, has excellent antitussive effects without respiration depression.

7,8-Dihydroisomorphine derivative, namely azidoethylmorphine

A process for the preparation of pharmaceutically acceptable 3-protected derivatives of 6-deoxy-6-azido-14-hydroxy-7, 8-dihydroisomorphine, selected from the group which consists of 3-O-acetyl-6-deoxy-6-azido-14-hydroxy-7, 8-dihydroisomorphine, 3-O-tetrahydropyranyl-6-deoxy-6-azido-14-hydroxy-7, 8-dihydroisomorphine and 3-O-methylenemethoxy-6-deoxy-6-azido-14-hydroxy-7, 8-dihydroisomorphine, and the salts of these compounds which comprise the following steps:

6-Deoxy-6-azido-14-hydroxy-7,8-dihydroisomorphine or a pharmaceutically

A pharmaceutical composition with synergistic analgesic effect which comprises an effective amount of 6-desoxy-6-azido-14-hydroxy-7,8-dihydro morphine or codeine or an analgesically effective salt thereof and an effective amount of a compound ##STR1## wherein R.sup.1 and R.sup.2 are lower alkyl and R.sup.3 is hydrogen or lower alkyl, and the dotted lines represent hydrogenated or unsaturated bonds or an analgesically effective salt or quaternary compound thereof.

Pharmaceutical composition having synergistic analgesic activity and

Pharmaceutical compositions of synergistic analgesic activity are provided which comprise an azido compound of the following formula: ##STR1## or a salt thereof wherein R is hydrogen, methyl, ethyl, acetyl or morpholino-methyl and a compound of the formula: ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 are hydrogen or lower alkyl and the dotted lines represent hydrogenated bonds or olefinic bonds and pharmaceutically acceptable salts and quaternary salts thereof, in admixture with suitable inert solid or liquid carriers or dilutents.

Pharmaceutical composition having synergistic analgesic activity

A pharmaceutical composition having synergistic analgesic effect which includes an azido compound of the formula: ##SPC1## namely an azido morphine or an azido codeine, and at least one compound of the formula: ##SPC2## The synergistic composition has been found to have less narcotic side effects than morphine and equal or better analgesic properties.

An analgesic substitute for morphine comprising the synergistic combination of azidomorphine or azidocodeine with a pyrimidazolium.

Growing community of inventors

Debrecen, Hungary

Sandor Makleit