Pierrel Spa

Edmond Pharma, S.r.l.

Boehringer Ingelheim Italia S.p.a.

Istituto De Angeli S.p.a.

B.i. Italia

Boehringer Ingelheim Italia

Istituto De Angeli

Massimo Nicola

Arturo Donetti

Marco Turconi

Rosamaria Micheletti

Cesare Casagrande

Antonio Giachetti

Ernesto Montagna

Annamaria Uberti

Franco De Marchi

Silvia Z Tricerri

Enzo Cereda

Guido Vandoni

Giovanni Battista Schiavi

Giancarlo B Fregnan

Pier Andrea Gatti

Matteo Zacche′

Marco Inglesi

The present invention provides novel crystalline polymorphs of enantiopure Erdosteine, referred to as Form I and Form II, and processes for the preparation thereof.

Polymorphs of enantiopure erdosteine

A method for treating a human host suffering from psychosis, which method comprises administering to such host a therapeutically effective amount of a compound of the formula I ##STR1## wherein the radicals are defined in claim 1.

Benzimidazoline-2-oxo-1-carboxylic acid derivatives useful as 5-ht

Salts of a glutathione alkylester and anaminoacids

Pharmacologically active benzimidazoline-2-oxo-1-carboxylic acid compounds which are useful for treating a human host suffering from anxiety.

Benzimidazoline-2-oxo-1-carboxylic acid derivatives useful as 5-HT

New pharmacologically active amidino and guanidino derivatives which are 5-HT.sub.3 receptor antagonists useful as antiemetic, gastric prokinetic and antimigrainic agents of the following general formula (I) ##STR1## wherein the substituents are defined hereinbelow in the specification, which compounds are 5-HT.sub.3 receptor antagonists useful as antiemetic gastric prokinetic and antimigraine agents, inter alia.

Amidino and guanidino derivatives

New pharmacologically active benzimidazoline-2-oxo-1-carboxylic acid derivatives which are 5-HT receptor antagonists useful as antiemetic agents and as gastric prokinetic agents of the following formula: ##STR1## wherein R is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl; R.sub.1 is hydrogen; R.sub.2 is hydrogen, halogen or C.sub.1-6 alkoxy; Y is oxygen or N--R.sub.3 in which R.sub.3 is hydrogen; A is a group selected from: ##STR2## wherein p is 1; r is 0, 2 or 3: R.sub.4 is hydrogen; R.sub.5 is hydrogen, C.sub.1-6 alkyl, or R.sub.5 is a group of the formula --CR.sub.6 =N--R.sub.7 wherein R.sub.6 is hydrogen, C.sub.1-4 alkyl or amino and R.sub.7 is hydrogen or C.sub.1-6 alkyl; or a pharmaceutically acceptable acid addition salt thereof. The processes for the preparation of the compounds of formula (I) as well as pharmaceutical compositions contained in them are also described.

Benzimidazoline-2-oxo-1-carboxylic acid compounds useful as 5-HT

New pharmacologically active amidino and guanidino derivatives which are 5-HT.sub.3 receptor antagonists useful as antiemetic, gastric prokinetic and antimigrainic agents of the following general formula (I) ##STR1## , wherein the substituents are defined hereinbelow, which compounds are 5-HT.sub.3 receptor antagonists useful as antiemetic gastric prokinetic and antimigraine agents, inter alia.

Indolyl derivatives and their use as 5-HT.sub.3, receptor antagonists

New pharmacologically active heterocyclic derivatives as muscarinic receptor blocking agents, useful for the treatment of gastrointestinal disorders, of the following formula ##STR1## wherein the substituents are defined hereinbelow.

1,3-diazocycloalkenes as muscarinic receptor blocking agents

Basic esters of 1,4-dihydropyridine-3,5-dicarboxylic acid of formula (I) ##STR1## are described, in which R.sup.1 is a linear or branched alkyl radical containing 1-5 carbon atoms which is unsubstituted or substituted by an alkoxy group; R.sup.2 is phenyl or a nitro phenyl radical; R.sup.3 is phenyl, phenyl substituted by one to three radicals selected from (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, fluoro, chloro, bromo, nitro, cyano, COOR in which R is alkyl of 1 to 4, trifluo carbon atoms, romethyl, hydroxy, amino, mono- or di-alkylamino, mono- or di-acylamino, mercapto, S(O).sub.n -alkyl with n=0, 1 or 2, (C.sub.1-5)acyl, carbamoyl, ureido or R.sup.3 is a 5 or 6 membered heteroaryl monocyclic radical which contains one or more heteroatoms which are N, O or S such as unsubstituted pyridyl, pyrazinyl, pyrimidyl, furyl, imidazolyl, thienyl, thiazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl or mono-, di- or tri-substituted with alkyl, alkoxy, halogen or trifluoromethyl; X is a linear or branched alkylen radical containing between 2 and 5 carbon atoms which is unsubstituted or substituted by an alkoxy group and their racemates, enantiomers and diastereoisomers and addition salts thereof with a pharmaceutically acceptable acid. The novel compounds exhibit calcium antagonistic activity.

Basic esters exhibiting an antagonistic activity to calcium, process for

Compounds having general formula I ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, lower alkoxy, alkyl enoxy, halogen, cyano, carboxyamido or ureido group optionally separated from the phenyl ring by a methylene or ethylene bridge;

Aryloxypropanolamine derivatives, pharmaceutical compositions and

Compounds of formula I: ##STR1## are described in which R.sup.1 is a linear or branched alkyl radical containing between 1 and 5 carbon atoms, the alkyl radical being unsubstituted or substituted by an alkoxy group; R.sup.2 is an unsubstituted phenyl of phenyl substituted by a nitro group; R.sup.3 is hydrogen or a linear or branched alkyl residue containing between 1 and 4 carbon atoms, the alkyl radical being unsubstituted or substituted by at least one alkoxy or fluorine atom or both alkoxy and fluorine atoms; R.sup.4 is hydrogen or a linear or branched alkyl containing between 1 and 4 carbon atoms, the alkyl radical being unsubstituted or substituted by alkoxy, carbalkoxy, dialkylamino, 1-aryl or 1-heteroarylpiperazinyl, aryl or a monocyclic 5 or 6 membered heterocycle in which at least one of the heteroatoms is N,O,S such as 1-piperidinyl, 4-morpholinyl or R.sub.4 is alkenyl or cyclo(C.sub.3 -C.sub.6)alkyl; and enantiomers, racemates, diastereoisomers and isomers (E) and (Z) and their salts with pharmaceutically acceptable acids. The novel compounds exhibit calcium-antagonistic activity.

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Pavia, Italy

Massimo Nicola