Laboratorios Del Dr. Esteve S.a.

Laboratories Del Dr. Esteve S.a.

Laboratories Del Sr. Esteve, S.a.

Ramon Merce-Vidal

Jordi Frigola-Constansa

Carmen Almansa-Rosales

Joerg Holenz

Marina Virgili-Bernado

Carlos Alegret-Molina

Juan Pares-Corominas

Blas Andaluz-Mataro

Maria De Las Ermitas Alcalde-Pais

Maria De Les Neus Mesquida-Estevez

Lajos Novak

Monica Alonso-Xalma

Sara Lopez-Perez

Jose Luis Diaz-Fernandez

Blas Andaluz-Matar&oacute;

Josep Mas-Pri&oacute;

Maria De Las Ermitas Alcalde Pais

Maria De Les Neus Mesquida Estevez

Sara Lopez Perez

The present invention makes reference to new indene derivatives with general formula (I), as well as to their preparation procedures, their application as medicament and the pharmaceutical compositions containing them. The new compounds of formula (I) show affinity for 5-HTreceptors and are, therefore, effective for treating diseases mediated by these receptors. 

Indene derivatives, their preparation and use as medicaments

The present invention refers to new indanyl sulphonamide compounds with general formula (I), as well as to their preparation procedure, their application as medicine and the pharmaceuticals composition which they are made up of.  The new compounds of formula I show affinity for 5-HTreceptors and are, therefore, effective for treating diseases mediated by these receptors.

Substituted indanyl sulfonamide compounds, their preparation and use as medicaments

The present invention refers to substituted tetrahydro-quinoline-sulfonamide compounds of general formula (I): a method for their preparation, a medicament comprising these compounds and the use of substituted tetrahydro-quinoline-sulfonamide compounds for the preparation of medicaments for 5-HTreceptor regulation as well as for the treatment of disorders related thereto.

Substituted tetrahydro-quinoline-sulfonamide compounds, their preparation and use as medicaments

The thienylazolylalkoxyethanamines (I) where R1 is a hydrogen atom, a halogen atom or a lower alkyl radical; R2, R3 and R4 represent, independently, a hydrogen atom or a lower alkyl radical; and Az represents a five-member nitrogenated hetercyclic aromatic group, N-methyl-substituted, that contains from one to three nitrogen atoms. They have analgesic activity in mammals, including humans. The compounds (I) can be obtained, for example, by reaction of a derivative of hydroxy-thienylazol (IV) with a derivative of a suitable N-(ethyl)amine. The compounds (IV) are useful intermediates in the synthesis of the compounds (I). The compounds (I) have an application in human and/or veterinary medicine.

Thienylazolylalkoxyethanamines, their preparation and their application as medicaments

Derivatives of tetrahydropyridines (or 4-hydroxypiperidines)-butylazols of formula (I), wherein R, Rand R, which are similar or different, represent each of them hydrogen, halogen, alkyl C-C, trifluoromethyl, hydroxyl, alkoxyl, or two adjacent radicals can form a ring; A is a C atom and the dotted line represents an additional bond, or A is a C atom joined to a hydroxyl group and the dotted line represents absence of additional bond; Zis N or CR4; Zis N or CR; Zis N or CR; and R, R, Rand R, which different, represent hydrogen, halogen, alkyl C-C, aryl or substituted aryl, or two adjacent radicals can form part of another ring. These derivatives are useful for the treatment of acute pain, neuropathic pain or nociceptive pain in mammals, including human beings.

Utilization of derivatives of tetrahydropyridines(or 4-hydroxypiperidines)-butylazols in the preparation of a medicament for the treatment of pain

Thienylazolylalcoxyethanamines, their preparation and their application as medicaments

Derivatives of tetrahydropyridines (or 4-hydroxypiperidines)-butylazols of formula (I), wherein R , R and R , which are similar or different, represent each of them hydrogen, halogen, alkyl C -C , trifluoromethyl, hydroxyl, alkoxyl, or two adjacent radicals can form a ring; A is a C atom and the dotted line represents an additional bond, or A is a C atom joined to a hydroxyl group and the dotted line represents absence of additional bond; Z is N or CR4; Z is N or CR ; Z is N or CR ; and R , R , R and R , which different, represent hydrogen, halogen, alkyl C -C , aryl or substituted aryl, or two adjacent radicals can form part of another ring. These derivatives are useful for the treatment of acute pain, neuropathic pain or nociceptive pain in mammals, including human beings.

Utilization of derivatives of tetrahydropyridines (or 4-hydroxypiperidines)-butylazols in the preparation of a medicament for the treatment of pain

Antipsychotic compound 4-(4-chlorophenyl)-1,2,3,6-tetrahydro-1-&lsqb;4-(1H-1,2,4-triazol-1-yl) butyl&rsqb;pyridine, or one of its physiologically acceptable salts, pharmaceutical compositions containing those compounds and a method of treating a disease selected from psychosis and dementias in which a deficit of cognition predominates comprising administering to a patient in need of such treatment a therapeutically effective amount of the antipsychotic compound.

4-(4-Chlorophenyl)-1236-tetrahydro-1(1H-124-triazol-1-yl)butty)pyrideine and salts thereof; pharmaceutical compositions and method of treating psychoses utilizing same

Methods for preparing 2-(4-(4-(4,5-dichloro-2-methylimidazol-1yl)butyl)-1-piperazinyl)-5-fluoropyrimidine and its physiologically acceptable salts are disclosed.

Methods for preparation of 2-(4-(4-(4,5-dichloro-2-methylimidazol-1-yl)butyl)-1-piperazinyl)-5-fluoropyrimidine and salts thereof

2-&lcub;4-&lsqb;4-(4,5-dichloro-2-methylimidazol-1-yl)butyl&rsqb;-1-piperazinyl&rcub;-5-fluoropyrimidine, and its physiologically acceptable salts; pharmaceutical compositions containing these compounds, and a method of treating vertigo, travel sickness, nausea, depression, anxiety, gastric acid secretion, obsessive/compulsive disorders, panic attacks or sleep apnea using these compounds are disclosed.

2-&lcub;4-&lsqb;4-(4,5-dichloro-2-methylimidazol-1-yl)butyl&rsqb;-1-piperazinyl&rcub;-5-fluoropyrimidine, its preparation and its therapeutic use

The present invention relates to the compounds of general formula

Tetrahydropyridine-(or 4-hydroxypiperidine) alkylazoles

The present invention relates to the compounds of general formula ##STR1## used as medicaments possessing therapeutic activity for the treatment of anxiety, psychosis, epilepsy, convulsion, motoricity problems, amnesia, cerebrovascular diseases or senile dementia.

The present invention relates to a process for the preparation of 2-{4-[4-(4-chloro-1-pyrazolyl)buty1]-1-piperazinyl}pyrimidine (Lesopitron) of formula I: ##STR1## characterized in that the reaction between 2-(1-piperazinyl)pyrimidine, 4-chloropyrazole and the carbon chain of formula (III) ##STR2## in which X and Y, which may be identical or different, represent a suitable leaving group, is carried out in a single step in a suitable solvent.

Process for the preparation of

The present invention relates to the use of 1-{4-[4-aryl(or heteroaryl)-1-piperazinyl]butyl}-1H-azole derivatives and of their physiologically acceptable salts for the manufacture of medicaments intended for the treatment of disorders associated with gastric secretion.

Use of 1-[4-[4-aryl (or heteroaryl)-1-piperazinyl]-butyl)-1H-azole

2-[4-(4-azolylbutyl)-1-piperazinyl]-pyrimidine derivatives characterized in that they correspond to the general formula I ##STR1## in which X.sub.2 represents a nitrogen atom or a C-R.sub.2 group, X.sub.4 represents a nitrogen atom or a C-R.sub.4 group, X.sub.5 represents a nitrogen atom or a C-R.sub.5 group, the process for preparing them, their application as medicinal product, and the pharmaceutical compositions containing them.

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Barcelona, Spain

Ramon Merce-Vidal