Ferrer Internacional, S.a.

Ferrer International, S.a.

Albert Palomer

Antonio Guglietta

Luis Anglada

José Luís Falcó

José L Falcó

Marta Princep

Montserrat Cano

Josep Lluis Falco

José Falcó

José Luis Falcó

Luís Anglada

The invention provides novel halogenated pyrazolo[1,5-a]pyrimidines of formula (I) wherein R, R, X and Y have different meanings, and pharmaceutically acceptable salts thereof. Compounds of formula (I) are useful for treating or preventing anxiety, epilepsy and sleep disorders including insomnia, and for inducing sedation-hypnosis, anesthesia, sleep and muscle relaxation. The invention also provides synthetic procedures for preparing said compounds and certain intermediates, as well as intermediates themselves. 

Method of treating insomnia with halogenated pyrazolo[1,5-a]pyrimidines

The invention provides novel imidazo[1,2-b]pyridazines of formula (I) and pharmaceutically acceptable salts, polymorphs, hydrates, tautomers, solvates and stereoisomers thereof. Compounds of formula (I) are useful for treating or preventing diseases associated with GABAreceptors modulation, anxiety, epilepsy, sleep disorders including insomnia, and for inducing sedation-hypnosis, anesthesia, sleep and muscle relaxation. The invention also provides synthetic procedures for preparing said compounds and certain intermediates, as well as intermediates themselves. 

Imidazo[1,2-b]pyridazines, processes, uses, intermediates and compositions

Halogenated pyrazolo[1,5-A]pyrimidines, processes, uses, compositions and intermediates

There is provided a salt of 1-cyclopropyl-8-methyl-7-[5-methyl-6-(methylamino)-3-pyridinyl]-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid selected from the group consisting of citrate, hemi-fumarate, maleate, L-tartrate, mesylate, hydrochloride, potassium, and sodium salts.

1-cyclopropyl-8-methyl-7-[5-methyl-6-(methylamino)-3-pyridinyl]-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid salts

The present invention relates to an amorphous form of N-{2-Fluoro-5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methyl-acetamide, methods for its preparation, its use as a therapeutically active agent and pharmaceutical compositions comprising the novel form.

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The present invention relates to a method of treating anxiety, epilepsy, sleep disorders, and insomnia, for inducing sedation-hypnosis, anesthesia, and muscle relaxation, and for modulating the necessary time to induce sleep and its duration, which comprises administering a therapeutically effective amount of Polymorph B of N-{2-Fluoro-5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methyl-acetamide characterized by a powder X-Ray diffraction pattern containing specific peaks at 2&#x3b8;=7.1&#xb0; (&#xb1;0.1&#xb0;) and 21.4&#xb0; (&#xb1;0.1&#xb0;) to a patient in need thereof.

Polymorph B of N-{2-Fluoro-5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methyl-acetamide

The invention provides new compounds of formula (I) wherein R, R, R, R, and X have different meanings. Preparative processes, pharmaceutical compositions, and uses thereof in the treatment or prevention of conditions mediated by melatonin receptors are also provided. 

The invention provides novel pyrazolo[1,5-a]pyrimidines which are useful for treating or preventing anxiety, epilepsy and sleep disorders including insomnia, and for inducing sedation-hypnosis, anesthesia, sleep and muscle relaxation.

The present invention relates to a novel polymorph of N-{2-Fluoro-5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methyl-acetamide, processes for its preparation, its use as a medicament, its use in the manufacture of a medicament, and pharmaceutical compositions comprising the novel polymorph.

Polymorph B of N-{2-Fluoro-5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a] pyrimidin-7-yl]-phenyl}-N-methyl-acetamide

The present invention relates to a novel process for the industrial manufacture of polymorph B of N-{2-Fluoro-5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methyl-acetamide.

The present invention relates to compounds of Formula (I): wherein R, Rand Rare as defined in the claims. The compounds have specific affinity for the GABAreceptor and are therefore useful in the treatment and prevention of diseases modulated by the &#x3b1;- and &#x3b1;-GABAreceptors. 

N-[3-(3-substituted-pyrazolo[1,5-a]pyrimidin-7-yl)phenyl]-sulfonamides, and compositions, and methods related thereto

The invention provides novel imidazo[1,2-a]pyridin-3-yl-acetic acid hydrazides of formula (I) wherein R, Rand Rhave different meanings, and pharmaceutically acceptable salts, polymorphs, hydrates, tautomers, solvates and stereoisomers thereof. Compounds of formula (I) are useful for treating or preventing, in a human or non-human mammal, diseases associated with GABAreceptors modulation, anxiety, epilepsy, sleep disorders including insomnia, and for inducing sedation-hypnosis, anesthesia, sleep and muscle relaxation. The invention also provides synthetic processes for preparing said compounds. 

Imidazo[1,2-A]pyridin-3-yl-acetic acid hydrazides, processes, for their preparation and pharmaceutical uses thereof

The invention provides new oxazolidinone compounds of formula (I) wherein A is certain heterocycles optionally substituted; R, R, Rand Rare independently selected from &#x2014;H and halogen; X is selected from O, S, NRand CRR; Rand Rhaving different meanings; Y is selected from O, S, SO, SO, NO, NRand CRR; Rand Rhaving different meanings. It also provides different processes for the preparation of such compounds. Oxazolidinone compounds of formula (I) are active against Gram-positive and some Gram-negative human and veterinary pathogens with a weak monoamine oxidase (MAO) inhibitory activity. They are useful for the treatment of bacterial infections. 

Oxazolidinone compounds, and compositions and methods related thereto

The present invention relates to a novel process for the industrial manufacture of substituted 7-allyl-6-hydroxy-indanes of formula (I) wherein R is a straight or branched (C-C)alkyl group and X is a halogen and enantiomers thereof.

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Barcelona, Spain

Albert Palomer