The Three Cyclos Consist Of Two Carbocyclic Rings And A Five-membered Hetero Ring Which Includes A Ring Nitrogen (e.g., Ergolines, Etc.) Patents (Class 546/67)
Abstract: A number of pharmacologically active ergoline derivatives are disclosed, their preparation is described and examples of suitable pharmaceutical preparations are presented. Of quite particular interest among the rich series of compounds afforded by the present invention are D-2-bromo-1,6-dimethyl-8beta-(perhydroazepinylcarbonyloxymethyl)-ergoline and its salts (especially maleate and methanesulfonate) for the treatment of psychogenetic disorders, and D-2-bromo-6-methyl-8beta-(morpholinocarbonyloxymethyl)-ergoline and its salts (especially the maleate and the methanesulfonate for the treatment of asthma and allied ailments. Good tolerability, low toxicity and high effectiveness distinguish these compounds over those of the prior art.
Abstract: A method for preparing ergoline derivatives in which the ergoline structure is variously substituted by morpholino-piperazino- and other active radicals to obtain novel compounds useful in cardiology as alpha-blocking, vasodilating, antihypertensive active ingredients of pharmaceutical preparations.
Type:
Grant
Filed:
June 20, 1978
Date of Patent:
April 8, 1980
Assignee:
Simes Societa Italiana Medicinali e Sintetici
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: Novel sulfamoyl derivatives of 8.beta.-aminomethyl ergoline having the general formula: ##STR1## are disclosed, which have interesting pharmacological properties and are useful as anti-migrainic, anti-hypertensive and psychopharmaceutically active drugs. In the method for their preparation a compound having the formula: ##STR2## is reacted, in an aprotic solvent and at a temperature of between -20.degree. C. and +150.degree. C.
Type:
Grant
Filed:
November 3, 1977
Date of Patent:
November 27, 1979
Assignee:
SIMES Societa Italiana Medicinali e Sintetici S.p.A.
Abstract: Pyridazinyl-ergoline compounds having neuroleptic activity are obtained by reacting an 8.beta.-tosylmethyl ergoline with the sodium derivative of an amino-pyridazine or a mercaptopyridazine in a dipolar aprotic solvent.
Type:
Grant
Filed:
January 17, 1978
Date of Patent:
September 4, 1979
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Luigi Bernardi, Carlo Elli, Giovanni Falconi, Alberto Bonsignori
Abstract: 6-n-Propyl (ethyl or allyl)-8.beta.-methoxy-(methylsulfinyl, methylsulfonyl, or methylmercapto) methylergolines, 8-ergolenes or 9-ergolenes, useful as prolactin inhibitors and in the treatment of Parkinsonism.
Abstract: This invention provides new compounds of formula I, ##STR1## wherein X Y IS THE GROUP ##STR2## and R is hydrogen, cyano, a 5- or 6-membered unsaturated heterocyclic radical attached through a ring carbon atom and having 1, 2 or 3 hetero ring atoms, the first hetero atom being nitrogen, oxygen or sulphur, and the second and third hetero atoms, if present, being nitrogen, or 2- or 4-pyridyl monosubstituted by lower alkyl, lower alkoxy or halogen,Useful as anti-Parkinson agents.
Abstract: The present invention provides compounds of the formula, ##STR1## wherein R.sub.1 is alkyl (C.sub.1-5),R.sub.2 is alkyl (C.sub.1-5),R.sub.3 is hydrogen or halogen, and either each of R.sub.4 and R.sub.5 is hydrogen, orR.sub.4 and R.sub.5, together, are a bond,Which are useful as sleep-inducing and sleep-prolonging agents.
Abstract: 8,8-Disubstituted-6-methylergolines and 9-ergolenes, prepared by alkylation of lysergic, isolysergic or their 9,10-dihydro analogues, optionally followed by chemical modification of an 8-substituent.