Farmitalia Carlo Erba

Societa' Farmaceutici Italia

Giuliana Arcari

Luigi Bernardi

Gianfederico Doria

Carlo Passarotti

Aldemio Temperilli

Germano Bosisio

Ugo Scarponi

Alfredo Glasser

Sergio Mantegani

Ada Buttinoni

Giovanni B Falconi

Anna M Caravaggi

Fulvio Luini

Patricia Salvati

Maurizio Foglio

Daniela Ruggieri

Giorgio Palamidessi

Pietro De Micheli

Innocenzio Sinatra

Pharmacologically active thiazolo[3,2-a]pyrimidines of the formula ##STR1## wherein A is a bond between the .alpha.- and .beta.-carbon atoms or (--CH.sub.2 --) group; R.sub.1 and R.sub.2 represent hydrogen, C.sub.1 -C.sub.4 alkyl, cyano, CF.sub.3, thienyl, pyridyl, biphenyl, naphtyl, phenyl optionally substituted, ##STR2## wherein R' and R' are hydrogen or alkyl; R.sub.3 represents hydrogen, halogen, alkyl, OH, formyloxy, alkanoyloxy, alkenyloxy; R.sub.4 represents substituted pyrrole, substituted phenyl or substituted thiazolyl. The compounds have antiinflammatory, antiulcerorgenic and antigastric secretory activity.

Substituted thiazolo[3,2-a]pyrimidines and process for their preparation

There are provided ergoline derivatives of formula ##STR1## wherein R.sub.1 .dbd.H, CH.sub.3 ; R.sub.2 .dbd.H or halogen atom, or CH.sub.3,CN, alkyl- or phenyl-thio; R.sub.3 .dbd.H, OCH.sub.3 ; R.sub.4 .dbd.C.sub.1 -C.sub.4 hydrocarbon group; X.dbd.O, S, NH; A.dbd.CO, SO.sub.2 ; B.dbd.C.sub.1 -C.sub.4 hydrocarbon group, aryl, aralkyl, heterocyclic ring group, alkoxy, aryloxy; n.dbd.0, 1, 2; and pharmaceutically acceptable salts thereof. A process for preparing said compounds is also provided. The compounds show anti-hypertensive activity and are active on the gastroenteric system.

Ergoline derivatives

Compounds of the formula (I) ##STR1## wherein R.sub.1 is:

Substituted ethenyl derivatives of 1H-pyrazolo-[1,5-a]pyrimidine having

Pharmacologically active thiazolo[3,2-a]pyrimidines of the formula ##STR1## wherein A is a bond between the .alpha. and .beta.-carbon atoms or (--CH.sub.2 --) group; R.sub.1 and R.sub.2 represent hydrogen or halogen, C.sub.1 -C.sub.4 alkyl, cyano, CF.sub.3, thienyl, pyridyl, biphenyl, naphtyl, phenyl optionally substituted, ##STR2## wherein R' and R' are hydrogen or alkyl; R.sub.3 represents hydrogen, halogen, alkyl, OH, formyloxy, alkanoyloxy, alkenyloxy; R.sub.4 represents pyridyl optionally substituted by alkyl. The compounds have antiinflammatory, antiulcerogenic and anti-gastric secretory activity.

Substituted Pyrrolo [2,1-b] and Pyrido [2, 1 b] Quinazolines are provided, together with pharmaceutical compositions, containing them. The compounds have pharmaceutical utility, and are particularly useful for the treatment of or prevention of the formation of gastrointestinal ulcers.

Substituted pyrrolo[2,1-b]quinazolines and pyrido[2,1-b]quinazolines

A compound is disclosed of the formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom, or a carboxy, alkoxycarbonyl, piperidinocarbonyl, 1-pyrrolidinylcarbonyl, morpholinocarbonyl, carbamoyl or benzylcarbamoyl group, or an alkylcarbamoyl or dialkylcarbamoyl group in which the, or each, alkyl group has from 1 to 4 carbon atoms;

Tetracyclic indole derivatives

Compounds and process for making same are disclosed, the compounds having the formula (I): ##STR1## wherein R.sub.1 represents a methyl, phenyl, piperidino, 1-pyrrolidinyl, morpholino or 4-methyl-1-piperazinyl group, an alkyl or alkoxy group having from 1 to 4 carbon atoms, an amino group, a substituted amino group of the formula NHR' (wherein R' represents an alkyl group having from 1 to 4 carbon atoms, a cycloalkyl group, a benzyl group, or a phenyl group) or a substituted amino group of the formula NR' R'' (wherein R' and R'' both represent alkyl groups having from 1 to 4 carbon atoms);

Ergot derivatives

Compounds are disclosed of the general formula (I): ##STR1## wherein R.sub.1 is a lower alkyl having from 1 to 4 carbon atoms; R.sub.2 is hydrogen or a lower alkyl having from 1 to 4 carbon atoms; and R.sub.3 is a saturated or unsaturated straight or branched alkyl having from 1 to 4 carbon atoms. A process for making such compounds is also disclosed. These compounds are useful as antiulcer agents and as inhibitors of gastric secretion.

4,5,6,7-Tetrahydroimidazo-[4,5-c]-pyridine derivatives

New 4,5,6,7-tetrahydroimidazo-[4,5-c]-pyridine derivatives are disclosed, and more particularly derivatives of Formula I ##STR1## where R.sub.1 is hydrogen or an alkyl having from 1 to 4 carbon atoms;

Pyrimidinoaminoethyl ergoline derivatives of the formula: ##STR1## wherein R is hydrogen or methyl; R.sub.1 and R.sub.2 are independently selected from the group consisting of hydrogen, alkyl having 1 to 3 carbon atoms, methoxy and phenyl; R.sub.3 is hydrogen, halogen, alkyl and alkoxy each having 1 to 3 carbon atoms, phenyl, nitro, amino, cyano, acylamino, carboxamido and carbalkoxy each having 1 to 3 carbon atoms, trifluoromethyl or --SO.sub.2 --Y wherein Y is hydroxyl, amino or methyl and R.sub.4 is hydrogen or methoxy are prepared by reacting an ergoline derivative of formula III and a 2-aminopyrimidine anion of formula II ##STR2##

Pyrimidinoaminoethyl ergoline derivatives

New derivatives of caffeine are disclosed having the formula: ##SPC1## Where R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are selected from the group consisting of hydrogen, chlorine, bromine, an alkyl or an alkoxy radical containing from 1 to 4 carbon atoms. They are made by transforming 8-.alpha. hydroxyethyl caffeine into the corresponding 8-.alpha.-chloroethyl caffeine by the action of a suitable chlorinating agent such as thionyl chloride, reacting the product so obtained in a suitable solvent such as anhydrous dimethylformamide at a temperature from 40.degree. to 110.degree. C and for a period of time from 1 to 5 hours with the sodium or potassium salt of a nicotinic acid of the formula: ##SPC2## Where R.sub.1, R.sub.2, R.sub.3 and R.sub.4 have the above-mentioned meanings, and crystallizing the resulting product from a suitable solvent, such as ethanol. These new compounds have broncholitic activity.

Caffeine derivatives

Ergoline derivatives are disclosed having the general formula ##SPC1## Wherein R is selected from the group consisting of a lower alkyl radical having from 1 to 4 carbon atoms; an --NH-lower alkyl radical having from 1 to 4 carbon atoms; a free or substituted phenyl- or 2-furanoyl radical; the --O--CH.sub.2 --C.sub.6 H.sub.5 radical; a (3)- or (4)-pyridine radical free or substituted by a methyl radical or a chlorine or bromine atom; a pyrrole radical of formula ##SPC2## Wherein

1,6-Dimethyl-8.beta.-[2' or 3'-pyrroyloxyethyl or substituted

Novel 8.beta.-pyrimidino-aminomethyl-10.alpha.-ergoline and 10.alpha.-methoxyergoline derivatives which possess a high and prolonged adrenolytic activity and a low toxicity, and some of which also possess hypotensive and analgesic activity are prepared by reacting a pyrimidine anion with an ergoline derivative in an aprotic solvent.

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Milan, Italy

Giuliana Arcari