Spofa United Pharmaceutical Works

Spofa, United Pharmeceutical Works

Spofa, Pharmaceutical Works

Miroslav Semonsky

Miroslav Seda

Karel Rezabek

Antonin Cerny

Marie Auskova

Jiri Krepelka

Rudolf Kotva

Jaroslava Grimova

Oldrich Nemecek

Vaclav Trcka

Bohumil Sevcik

Josef Kral

Vojtech Pujman

Karel Rezabeck

Milos Beran

Viktor Zikan

Marie Krajcrova

Oskar Andrysek

Hana Vesela, Deceased

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

5-Carboxyalkyl-2-iminobarbituric and 5-carboxyalkyl-2-thioxobarbituric acids and derivatives thereof are prepared either by condensation of a triester of a tricarboxylic acid with a thio or imino diamide to yield an ester which is saponified, the desired compound being obtained by liberation with a mineral acid from an ammoniacal medium containing the saponified ester. Alternatively, free tricarboxylic acids may be substituted for the triesters. The compounds described herein have evidenced a therapeutic effect in animals having transplanted tumors, and have inhibited tumor growth and lengthened the life of animals and humans.

Derivatives of carboxyalkyl imino- and thioxo-barbituric acids

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

Novel N.beta.-substituted 8-.beta.-aminoethylergolin-I derivatives and the acid addition salts thereof are disclosed. The described compositions are prepared by either reductive alkylation or selective reduction of corresponding derivatives containing carbonyl groups.

N.beta.-substituted 8-.beta.-aminoethylergolin-I derivatives and their

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

Miroslav Semonsky