Roussel Uclaf

Roussel Ucaf

Fernando Barzaghi

Emilio Toja

Giulio Galliani

Carla Bonetti

Carlo Gorini

Mario Bianchi

Carlo Zirotti

Michel Fortin

Alina Butti

Yani Christidis

Robert Fournex

Italo Medici

Andre Farcilli

Guilio Galliani

Mario Bianchi, Deceased

Compounds useful in the treatment of patients suffering from senile dementia, Alzheimer's disease or memory defects, of the formula ##STR1## in which R' represents hydrogen, a linear, branched or cyclic alkyl, alkenyl or alkynyl, containing up to 8 carbon atoms, and R represents a linear, branched or cyclic alkyl, alkenyl, or alkynyl, containing up to 18 carbon atoms, possibly substituted, aryl containing up to 14 carbon atoms, possibly substituted, aralkyl containing up to 18 carbon atoms, possibly substituted, as well as their addition salts with organic or mineral acids, and to compounds of formula (I) in which R represents phenyl substituted in the 4 position by Br, F, CH.sub.3, NO.sub.2 or C(CH.sub.3).sub.2 C(CH.sub.3).sub.3 and R' represents CH.sub.3.

Derivatives of the oxime of 1,2,5,6-tetrahydropyridine 3-carboxaldehyde,

Compounds useful in the treatment of Alzheimer's disease, senile dementia, or memory disorders which have the formula ##STR1## in which R represents a hydrogen atom, a linear, branched or cyclic alkyl radical, saturated or unsaturated, containing up to 8 carbon atoms, possibly substituted by a free or esterified carboxy radical or R represents an aralkyl radical containing up to 10 carbon atoms and R' represents a linear or branched, saturated or unsaturated, alkyl radical, containing up to 8 carbon atoms, a radical --COalk.sub.1 or a radical --(CH.sub.2).sub.2 N(alk.sub.2).sub.2, alk.sub.1 and alk.sub.2 representing an alkyl radical containing up to 8 carbon atoms, as well as their addition salts with acids. Also compositions containing the same, method of preparation and method of treatment using the same.

Compounds of 1,2,5,6-tetrahydropyridin-3-carboxaldehyde oxime which are

Compounds useful in the treatment of Alzheimer's disease, senile dimentia and memory disorders of the formula ##STR1## in which R represents hydrogen, hydroxyl, a linear, branched or cyclic, saturated or unsaturated, alkyl, containing up to 8 carbon atoms, possibly substituted by free or esterified carboxy or R represents aralkyl containing up to 10 carbon atoms or --COOZ in which Z represents a linear, branched or cyclic saturated or unsaturated, alkyl containing up to 8 carbon atoms and R.sub.2 represents hydrogen or a linear or branched, saturated or unsaturated alkyl containing up to 8 carbon atoms, COalk.sub.1 radical or (CH.sub.2).sub.2 N(alk.sub.2).sub.2, alk.sub.1 and alk.sub.2 representing an alkyl containing up to 8 carbon atoms, as well as their addition salts with acids provided that if R represents an alkyl R.sub.2 does not represent hydrogen; also therapeutic compositions containing at least one said compound and method of treating patients with said compounds.

Compounds of 1,2,5,6-tetrahydropyridine which are useful as cholinergic

1-arylsulphonyl-2-pyrrolidone derivatives for treating spasmodic disorders in gastro-enterology, in gynaecology, in obstetrics, in urology; intermediates in the preparation of such products; methods for preparing such products and pharmaceutical preparations containing such products.

1-arylsulphonyl-2-pyrrolidone derivatives, their preparation process and

The subject of the invention is the compounds of formula (I): ##STR1## in which: R represents a hydrogen atom, a saturated or unsaturated, linear, branched or cyclic alkyl radical containing up to 8 carbon atoms,

Derivatives of 1,2,5,6-tetrahydropyridin-3-carboxaldehyde oxime

Compounds useful in the treatment of Alzheimer's disease, senile dementia or memory disorders of the aged of the formula ##STR1## in which n represents the number 1, 2 or 3,

1-azabicycloalkane derivatives, their preparation process and their use

Compounds of the formula ##STR1## which have a long-lasting cholinomimetic activity by oral route. Also disclosed are methods for preparing the compounds and pharmaceutical compositions containing the compounds.

Compounds useful for the treatment of patients suffering from muscle spasms of the formula (I) ##STR1## in which R represents the radical ##STR2## in which R.sub.1, in any position on the phenyl nucleus, represents a linear, branched or cyclic alkyl, alkenyl or alkynyl, containing up to 8 carbon atoms, or the radical ##STR3## in which R.sub.2 and R.sub.3, identical or different each represents a hydrogen atom, a linear alkyl, alkenyl or alkynyl, containing up to 8 carbon atoms, or form together with the nitrogen atom to which they are joined, a heterocyclic radical optionally containing another heteroatom, or NO.sub.2, or OR', R' representing hydrogen, a linear, branched or cyclic alkyl containing up to 8 carbon atoms, or aryl containing up to 14 carbon atoms, or an SR.sub.4 or S(O)R.sub.5 radical, R.sub.4 and R.sub.5 representing a linear, branched or cyclic alkyl, alkenyl or alkynyl, containing up to 8 carbon atoms, or R represents naphthyl, optionally substituted by an R.sub.1 radical, as defined above; also therapeutic compositions containing the same and method of use.

Derivatives of 1-arylsulphonyl-2-pyrolidinone

Compounds useful for the treatment of patients suffering from muscle spasms of the formula (I) ##STR1## in which R represents the radical ##STR2## in which R.sub.1, in any position on the phenyl nucleus, represents a linear, branched or cyclic alkyl, alkenyl or alkynyl, containing up to 8 carbon atoms, or the radical ##STR3## in which R.sub.2 and R.sub.3, identical or different each represents a hydrogen atom, a linear alkyl, alkenyl or alkynyl, containing up to 8 carbon atoms, or form together with the nitogen atom to which they are joined, a heterocyclic radical optionally containing another heteroatom, or NO.sub.2, or OR', R' representing hydrogen, a linear, branched or cyclic alkyl containing up to 8 carbon atoms, or aryl containing up to 14 carbon atoms, or an SR.sub.4 or S(O)R.sub.5 radical, R.sub.4 and R.sub.5 representing a linear, branched or cyclic alkyl, alkenyl or alkynyl, containing up to 8 carbon atoms, or R represents naphthyl, optionally substituted by an R.sub.1 radical, as defined above; also therapeutic compositions containing the same and method of use.

Derivatives of 1-arylsulphonyl-2-pyrrolidinone, their preparation

Compounds of formula (I) ##STR1## in which X represents oxygen or sulphur, R.sub.1 represents hydrogen, a linear, branched or cyclic alkyl containing up to 8 carbon atoms, an alkenyl or alkynyl containing up to 6 carbon atoms, hydroxyl, an OCOalk.sub.1 radical in which alk.sub.1 represents alkyl containing up to 6 carbon atoms, an OCONHalk.sub.2 radical in which alk.sub.2 represents alkyl containing up to 6 carbon atoms, a CO.sub.2 alk.sub.3 radical in which alk.sub.3 represents alkyl or alkenyl containing up to 6 carbon atoms, an Oalk.sub.4 radical in which alk.sub.4 represents alkyl containing up to 6 carbon atoms, an OCOAr.sub.1, OCONHAr.sub.2 or CO.sub.2 Ar.sub.3 radical in which Ar.sub.1, Ar.sub.2 or Ar.sub.3 represents aryl containing up to 14 carbon atoms, R.sub.2 represents hydrogen, a linear, branched or cyclic alkyl containing up to 6 carbon atoms, alkenyl or alkynyl containing up to 6 carbon atoms, an alkoxyalkyl alk'.sub.1 Oalk'.sub.2 radical in which alk'.sub.1 and alk'.sub.2 represent alkyl containing up to 6 carabon atoms, hydroxyalkyl in which the alkyl contains up to 6 carbon atoms or aryl containing up to 14 carbon atoms, as well as their addition salts with organic or mineral acids, which compounds are useful in the treatment of patients suffering from Alzheimer's disease, senile dementia or memory disorders of the aged; also, compositions containing the same, method of use, method of preparation, and intermediates therefor.

Derivatives of 1,2,5,6-tetrahydropyridine substituted by a thiazolyl or

The invention relates to the products of formula ##STR1## in which R represents the radical ##STR2## in which R.sub.1 at any position on the benzene ring represents linear, branched or cyclic alkyl, alkenyl or alkynyl containing up to 8 carbon atoms, or the radical ##STR3## in which R.sub.2 and R.sub.3, which may be identical or different, represents hydrogen or linear alkyl, alkenyl or alkynyl containing up to 8 carbon atoms or form, together with the nitrogen atom to which they are attached, a carbonaceous heterocyclic radical optionally containing another hetero atom, or the radical OR', R' representing hydrogen, a linear, branched or cyclic alkyl containing up to 8 carbon atoms or aryl containing up to 14 carbon atoms, or the radical SR.sub.4 or S(O)R.sub.5, R.sub.4 and R.sub.5 representing linear, branched or cyclic alkyl, alkenyl, or alkynyl containing up to 8 carbon atoms, or R represents naphthyl optionally substituted with the radical R'.sub.1, R'.sub.1 being as defined above for R.sub.1, to a process and intermediates for the preparation thereof, to their application as medicinal products and to compositions containing them.

1-arylsulphonyl-2-piperidinone derivatives, process and intermediates

The invention relates to the products of formula ##STR1## in which R represents the radical ##STR2## in which R.sub.1 at any position on the benzene ring represents a linear, branched or cyclic alkyl, alkenyl or alkynyl containing up to 8 carbon atoms, or the radical ##STR3## in which R.sub.2 and R.sub.3, which may be identical or different, represent a hydrogen atom or a linear alkyl, alkenyl or alkynyl containing up to 8 carbon atoms or form, together with the nitrogen atom to which they are attached, a carbonaceous heterocyclic radical optionally containing another hetero form, or the radical OR', R' representing hydrogen, a linear, branched or cyclic alkyl radical containing up to 8 carbon atoms or an aryl radical containing up to 14 carbon atoms, or the radical SR.sub.4 or S(O)R.sub.5, R.sub.4 and R.sub.5 representing a linear, branched or cyclic alkyl, alkenyl or alkynyl containing up to 8 carbon atoms, or R represents naphthyl optionally substituted with a radical R'.sub.1, R'.sub.1 having one of the definitions stated above for R.sub.1, and n represents the number 1 or number 2, to a process for the preparation thereof, to their application as medicinal products and to compositions containing them.

1-arylsulphonyl-2-pyrrolidinethione or

Compounds useful in the treatment of Alzheimers's disease, senile dementia or memory disorders of the aged of the formula ##STR1## in which n represents the number 1, 2 or 3,

Derivatives of 1-arylsulphonyl-2-pyrrolidinone and their use as

Compounds useful in the treatment of patients suffering from intellectual or nervous asthenias, memory failures, senescence or mental strain of the formula (I): ##STR1## in which R' represents hydrogen, linear, branched or cyclic alkyl containing up to 12 carbon atoms, alkenyl containing from 2 to 8 carbon atoms, acyl containing from 1 to 6 carbon atoms or aralkyl containing from 7 to 15 carbon atoms and R represents aryl containing up to 14 carbon atoms, optionally substituted, or a mono- or polycryclic heterocyclic aromatic radical, optionally substituted; also therapeutic compositions containing those compounds and method of use.

Growing community of inventors

Monza, Italy

Fernando Barzaghi