Spofa United Pharmaceutical Works

Spofa, Spojene Podniky Pro Zdravotnickou Vyrobu

Spofa, United Pharmeceutical Works

Karel Rezabek

Miroslav Semonsky

Miroslav Seda

Jiri Krepelka

Antonin Cerny

Marie Auskova

Jaroslava Grimova

Oldrich Nemecek

Vaclav Trcka

Milan Melka

Milan Pesak

Bohumil Sevcik

Josef Picha

Rudolf Kotva

Josef Kral

Stanislava Pokorna

Ruzena Reichlova

Vojtech Pujman

Milos Beran

Maria Fruhaufova

Antonin Borovicka

Josef Stuchlik

Jana Strakova

Petr Bilek

Dagmar Picmausova

Iva Vancurova

Slavjanka Cernochova

Viktor Zikan

This invention relates to a method for the treatment of endometritis (chronic and/or acute puerperal inflammations) in mammalian females comprising the administration of 1-(8-alpha-ergolinyl)-3,3-diethylurea derivatives of Formula I ##STR1## in which R.sup.1 represents an alkyl group containing 1 to 3 carbon atoms, R.sup.2 represents a hydrogen atom or an alkyl group containing 1 to 3 carbon atoms, and X represents a hydrogen atom or a double bond between the carbon atoms at positions 9 and 10. The compound according to Formula I, or a pharmaceutically acceptable acid addition salt thereof, is the physiologically active component of the therapeutic composition and method. The compound may be combined with a pharmaceutically acceptable diluent, vehicle, excipient, auxiliary, or carrier. The invention is particularly advantageous in veterinary medicine, when applied to the treatment of farm animals, such a cows.

Method for treatment of endometritis in mammalian females

Basic ethers of 7-oxo-7H-benzo(c) fluorene have been shown to evidence a pronounced antineoplastic and immunosuppressive effect in mammals suffering from leukemia. The technique for preparing the described ethers and the addition salts thereof with pharmaceutically acceptable organic and inorganic acids involves the aminoalkylation of 5-hydroxy-7-oxo-7H-benzo(c) fluorene and its corresponding nuclear substituted derivatives on the hydroxylic oxygen atom.

Basic ethers of 7-oxo-7H-benzo(c) fluorene and a process for their

A procedure is described for the preparation of a novel group of alkyl cyanomethyl ergoline-I derivatives and pharmaceutically acceptable salts thereof. The compounds are D-6-alkyl-8-cyanomethylergoline-I derivatives of the formula ##STR1## wherein R is an alkyl group of 2-4 carbon atoms.

Alkyl cyanomethyl ergoline-I derivatives and salts thereof, and methods

A process is described for the preparation of novel 6 substituted derivatives of D-8-ergolin-I-ylacetamide and the pharmaceutically acceptable addition salts thereof. The described composition evidences superior antilactation and antinidation characteristics as compared with prior art compounds.

D-6-allyl-8-ergol-I-ylacetamide

8-(.beta.-AMINOETHYL)ERGOLINES-I of the general formula ##STR1## wherein R.sup.1 is a hydrogen atom or an acyl group of the general formula R.sup.3 --CO, R.sup.3 being a hydrogen atom, an alkyl group having from 1-5 carbon atoms, a phenyl group, a phenylalkyl group or a pyridyl group or substituents thereof, and R.sup.2 is a hydrogen atom or a methyl group. Acid addition salts of the described ergolines evidence pharmacological activity in the anti-inflammation and hypotensive fields.

8-(.beta.-AMINOETHYL)ERGOLINES-I

.alpha.-D-6-methylergolinyl-8-acetamides of the formula: ##SPC1## Are readily prepared from .alpha.-D-6-methylergolinyl-8-acetic acid azide hydrochloride and amines of the formula R.sub.1 -NH-R.sub.2 and may be converted to their salts with inorganic and organic acids by neutralization. In these formulas, R.sub.1 may be hydrogen or lower alkyl, R.sub.2 may be hydrogen, lower alkyl, cycloalkyl having 5 or 6 carbon atoms, hydroxyalkyl having 3 or 4 carbon atoms, or lower alkoxycarbonylmethyl or R.sub.1 and R.sub.2 jointly may be divalent alkylene having 4 or 5 C atoms. The salts of most of these bases with physiologically tolerated acids are nontoxic in doses which suppress lactatical and prevent pregnancy in rats when applied orally after copulation. The others, equally non-toxic, extend the effective period of thiopental.

Composition for preventing lactation or pregnancy in mammals and the

A new compound, N-(D-6-methyl-8-isoergoline-I-yl)-N', N'-diethylurea, processes for preparation and purification thereof, and therapeutic uses therefor in mammals.

N-(D-6-methyl-8-isoergoline-I-yl)-N',N'-diethylurea

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Prague, Czechia

Karel Rezabek