Spofa United Pharmaceutical Works

Spofa, Spojene Podniky Pro Zdravotnickou Vyrobu

Spofa, Pharmaceutical Works

Antonin Cerny

Miroslav Semonsky

Jiri Krepelka

Karel Rezabek

Miroslav Seda

Jaroslava Grimova

Marie Auskova

Bohumil Sevcik

Josef Kral

Rudolf Kotva

Oldrich Nemecek

Vaclav Trcka

Milan Pesak

Milan Melka

Vojtech Pujman

Josef Picha

Stanislava Pokorna

Milan Miko

Irena Kejhova

Ruzena Reichlova

Oskar Andrysek

Hana Vesela, Deceased

Maria Fruhaufova

Karel Rezabeck

Antonin Borovicka

Josef Stuchlik

Jana Strakova

Petr Bilek

Marie Krajcrova

Dagmar Picmausova

Marta Beitova

6-purinyl N-(2-chloroethyl) carbamate and thiocarbamate are disclosed of the general formula I, ##STR1## in which X stands for an oxygen or sulfur atom, and also a process for their preparation by reacting a purine derivative of the general formula II (hypoxanthine or 6-mercaptopurine, respectively) with 2-chloroethylisocyanate. The subject compounds of formula I show a remarkable antineoplastic effect in vitro and in vivo, and consequently have great potential for the treatment of malignant neoplastic diseases in mammals.

6-purinyl N-/2-chloroethyl/carbamate and thiocarbamate and process for

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

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

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

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Prague, Czechia

Antonin Cerny