Dompe' Farmaceutici S.p.a.

Isf S.p.a.

Craf Sud

Dompe' Farmaceutica S.p.a.

Roberto P Giani

Giancarlo Tonon

Ettore Parini

Mario Pinza

Giampietro Broccali

Goffredo Bolis

Giorgio Pifferi

Salvatore Malandrino

Massimiliano Borsa

Piero Bellani

A process for the optical resolution of racemic dropropizine, carried out using L(+)tartaric acid as the optical resolution agent in aqueous medium, is described.

Process for the optical resolution of dropopizine

New alkylthiobenzimidazole derivatives are described which belong to the class of formula: ##STR1## wherein R.sub.1 and R.sub.2 each represent a 1-3 carbon atom alkyl radical or they may form with the adjacent nitrogen atom, an optionally substituted heterocyclic ring,

Pharmacologically active alkylthiobenzimidazole derivatives and process

New alkylol derivatives are described, which belong to the class having the structure formula ##STR1## where R represents a 5 or 6 membered heterocyclic ring selected among pyridine, pyrimidine, pyrazine, pyridazine, thiophene, furan, thiazole which optionally may be substituted with one or more groups selected among alkyl, alkoxy, halogen, amide, hydroxy, methylthio, trifluoromethyl, cyano, carboxy and the corresponding alkyl esters and salts with alkali metals

Pharmacologically active alkylol derivatives

The present invention refers to an improved method for the preparation of 6,11-dihydro-5H-pyrido[2,3-b][1,5]benzodiazepin-5-one in which the condensation between 2-chloronicotinic acid and o-phenylenediamine is carried out by refluxing in the presence of a solvent consisting of a cycloalkanol. The end product is in pure state and it may be utilized as such.

Process for the preparation of pyridobenzodiazepinone

Quaternary salts of 11-acyl derivatives of 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one, 6,11-dihydro-5H-pyrido[2,3-b][1,5]benzodiazepin-5-one and 5,10-dihydro-11H-dibenzo[b,e][1,4]diazepin-11-one are described. Said quaternary salts are endowed with antiulcer, antisecretory, spasmolytic and antimuscarinic activity.

Quaternary salts of dibenzo[1,4]diazepinones,

11-Acyl derivatives of 5,11-dihydro-6H-pyrido-[2,3-b][1,4]benzodiazepin-6-one, 6,11-dihydro-5H-pyrido[2,3-b][1,5]benzodiazepin-5-one and 5,11-dihydro-6H-benzo[2,3-b][1,4]benzodiazepin-6-one, their preparation and pharmaceutical compositions endowed with antisecretory, antiulcer, antimuscarinic, spasmolytic activities containing the same, are described.

Pyrido[1,5]benzodiazepinone derivatives and pharmacological activities

There is described a new class of ketohydroxyimino derivatives of cephalosporins of the formula ##STR1## wherein: R is an alkyl radical having from 2 to 4 carbon atoms, a phenyl, or a 5-membered heterocyclic radical which may be substituted, containing nitrogen, oxygen and/or sulphur;

Ketoiminocephalosporin derivatives

Formyl derivatives of hydrazinopenicillins of the formula ##STR1## wherein R is thienyl or phenyl, R' is hydrogen, formyl or alkyl containing from 1 to 3 carbon atoms and R' is hydrogen or formyl, provided that at least one of R' and R' is a formyl group, the carbon atom with the asterisk indicating a center of asymmetry of the molecule, and pharmaceutically acceptable salts and esters thereof, as mixture or as separated epimers. These compounds have antibacterial activity against Gram-negative and Gram-positive bacteria and are prepared by a process wherein the corresponding hydrazinopenicillin is reacted under anhydrous conditions with acetoformic anhydride to give the desired compounds.

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Roberto P Giani