Abstract: 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.
Type:
Grant
Filed:
December 13, 1976
Date of Patent:
March 23, 1982
Assignee:
SPOFA, United Pharmaceutical Works
Inventors:
Antonin Cerny, Miroslav Semonsky, Rudolf Kotva, Karel Rezabek, Marie Auskova, Miroslav Seda
Abstract: Polysubstituted derivatives of 10-piperazinodibenzo (b,f) thiepine and processes for the preparation thereof are described. The compositions evidence psychotropic and antimicrobial characteristics and are of low toxicity. The described compounds are of the general formula ##STR1## wherein R.sup.2, R.sup.3, R.sup.7 and R.sup.8 are selected from among hydrogen, fluorine and chlorine atoms, a fluoromethyl group, a methoxy group and a hydroxyl group, at least three of R.sup.2, R.sup.3, R.sup.7 and R.sup.8 being other than hydrogen, R being selected from among hydrogen, alkyl or alkylhydroxy groups having from 1-3 carbon atoms, an acyloxyalkyl group having from 8-10 carbon atoms in the acyl moiety and from 2-3 carbon atoms in the alkyl moiety and an ethoxycarbonyl group, m and n representing integers from 0-1 and the bond between the 10 and 11 carbon atoms being either a single or double bond.
Type:
Grant
Filed:
January 6, 1976
Date of Patent:
December 9, 1980
Assignee:
SPOFA, United Pharmaceutical Works
Inventors:
Miroslav Protiva, Karel Sindelar, Irena Cervena, Jirina Metysova
Abstract: 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.
Type:
Grant
Filed:
April 20, 1978
Date of Patent:
December 2, 1980
Assignee:
SPOFA, United Pharmaceutical Works
Inventors:
Miroslav Semonsky, Rudolf Kotva, Antonin Cerny, Jiri Krepelka, Vojtech Pujman, Oskar Andrysek, Hana Vesela, deceased
Abstract: Antiinflammatory substituted phenylacetic acids of low toxicity are prepared by reaction of a salt of an alkyl 3 chloro-4-hydroxyphenylacetate with a substituted benzyl halide in the presence of an inert organic solvent at elevated temperatures.
Type:
Grant
Filed:
April 24, 1979
Date of Patent:
September 9, 1980
Assignee:
SPOFA, United Pharmaceutical Works
Inventors:
Jaroslava Grimova, Oldrich Nemecek, Miroslav Kuchar, Bohumila Brunova
Abstract: 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.
Type:
Grant
Filed:
December 6, 1977
Date of Patent:
January 8, 1980
Assignee:
Spofa, United Pharmaceutical Works
Inventors:
Milos Beran, Jiri Krepelka, Miroslav Semonsky, Karel Rezabek, Miroslav Seda, Marie Auskova
Abstract: A technique is described for the preparation of a novel anti-inflammatory agent comprising 2-phenyl-2-carboxyethyl 1-(p-chlorobenzoyl)-5-methoxy-2-methyl-3-indolylacetate. The preparative technique involves reacting indomethacin with tropic acid.
Abstract: 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.
Type:
Grant
Filed:
March 19, 1975
Date of Patent:
January 25, 1977
Assignee:
Spofa United Pharmaceutical Works
Inventors:
Miroslav Semonsky, Antonin Cerny, Oldrich Nemecek, Karel Rezabek, Miroslav Seda, Vaclav Trcka, Jaroslava Grimova
Abstract: .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.
Type:
Grant
Filed:
December 18, 1972
Date of Patent:
June 29, 1976
Assignee:
Spofa United Pharmaceutical Works
Inventors:
Miroslav Semonsky, Karel Rezabek, Miroslav Seda