Recordati S.a. Chemical and Pharmaceutical Company

Recordati Ireland Limited

Recordati Industria Chimica E Farmaceutica S.p.a.

Recordati S.a.

Recordati Industria Chimica E Farmacentica S.p.a.

Recordati, S.a., Chemical and Pharmacueticals Company

Carlo Riva

Amedeo Leonardi

Gianni Motta

Rodolfo Testa

Davide Graziani

Elena Poggesi

Patrizia Angelico

Luciano Guarneri

Carlo De Toma

Sergio Menegon

Matteo Longhi

Giorgio Sironi

Katia Dimitrova Karamfilova

Valerio Tazzari

Fabio Frigerio

Elisa Callegari

Elena Poggessi

Matteo Marco Longhi

This invention relates to compounds of formula I; and their use as antagonists of P2Xand P2Xreceptor activity, pharmaceutical compositions comprising such compounds, and methods of treatment therewith. Compounds of the invention can be used for the treatment and/or prevention of pain and chronic pain and tolerance to analgesic, respiratory disorders and dysfunctions, and treatment of overactive bladder, bladder pain syndrome, dysuria and in general in genitourinary diseases, cardiovascular disorders and more in general for the potential treatment of visceral organ diseases and disorders characterized by the involvement of P2Xand P2Xreceptors.

P2Xreceptor antagonists

Disclosed are triazole, imidazole and pyrrole condensed piperazine derivatives and their use as allosteric modulators of mGlus receptor activity, pharmaceutical compositions comprising such compounds, and methods of treatment therewith. Compounds of the invention can be used for the treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline, dementia or cognitive impairment, or other pathologies that can be related either directly or indirectly to glutamate dysfunction, i.e., disorders treatable by positive allosteric modulation (PAM) or by negative allosteric modulation (NAM) of mGluR. 

Substituted [1,2,4]triazolo[4,3-a]pyrazines as modulators of mGlu5 receptors

This invention relates to compounds of formula (I) and their use as allosteric modulators of mGluR5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for the treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction, such as schizophrenia or cognitive decline, dementia or cognitive impairment, or other pathologies that can be related directly or indirectly to glutamate dysfunction. 

Heterocyclylmethylidene derivatives and their use as modulators of mGluR5 receptors

This invention relates to compounds of formula I, their use as allosteric modulators of mGluR5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for the treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction, such as schizophrenia or cognitive decline, dementia or cognitive impairment, or other pathologies that can be related directly or indirectly to glutamate dysfunction.

Heterocyclylalkyne derivatives and their use as modulators of mGluR5 receptors

The invention is directed to methods of using antagonists selective for the metabotropic mGlu5 receptor to treat conditions of neuromuscular dysfunction of the lower urinary tract in a mammal. Provided are methods of treating a mammal suffering from a condition of neuromuscular dysfunction of the lower urinary tract by administering a selective mGlu5 antagonist. The selective mGlu5 antagonist may be administered alone or in combination with one or more additional therapeutic agents for treating such a condition. Also provided are methods of identifying selective mGlu5 antagonists that are useful for treating neuromuscular dysfunction of the lower urinary tract in a mammal. Methods for treating migraine and gastroesophageal reflux disease (GERD) using selective mGlu5 antagonists are also disclosed.

Spiroheterocyclic compounds as mGlu5 antagonists

This invention relates to novel heterocyclic compounds having selective affinity for the mGlu5 subtype of metabotropic receptors, pharmaceutical compositions thereof and uses for such compounds and compositions in the treatment of lower urinary tract disorders, such as neuromuscular dysfunction of the lower urinary tract, and in the treatment of migraine and gastroesophagael reflux disease (GERD).

Heterocyclic derivatives as M-GLU5 antagonists

N,N-Disubstituted diazocycloalkanes of the formula I 

N,N-disubstituted diazocycloalkanes

Disclosed herein are novel compounds and methods for the treatment of disorders of the lower urinary tract. The novel compounds are diarylalkylpiperazine derivatives. The methods comprise the administration of the novel compounds of the invention, and other compounds that bind to 5HTreceptors, for treating disorders of the lower urinary tract.

Diarylalkylpiperazines active on the lower urinary tract

The invention relates to novel N-(substituted phenyl)-N&prime;-&lsqb;&ohgr;-(3-substituted phenyl-4-isoxazolecarbonylamino)alkyl&rsqb;piperazines, their N-oxides, and pharmaceutically acceptable salts thereof. The compounds are endowed with enhanced selectivity for alpha1-adrenergic receptors and a low activity in lowering blood pressure. The compounds are useful in the treatment of obstructive syndromes of the lower urinary tract, including benign prostatic hyperplasia (BPH), and in the treatment of lower urinary tract symptoms (LUTS) and neurogenic lower urinary tract dysfunction (NLUTD), and other conditions. The compounds may be administered alone or in combination with an anticholinergic compound.

Isoxazolecarboxamide derivatives

The invention relates to novel N-(substituted phenyl)-N&prime;-&lsqb;&ohgr;-(5-substituted-7-oxo-7H-thieno&lsqb;3,2-b&rsqb;pyran-3-carbonylamino)alkyl&rsqb;piperazines their N-oxides and pharmaceutically acceptable salts thereof. The compounds are endowed with enhanced selectivity for alpha1-adrenergic receptors and a low activity in lowering blood pressure. The compounds are useful in the treatment of obstructive syndromes of the lower urinary tract, including benign prostatic hyperplasia (BPH), and in the treatment of lower urinary tract symptoms (LUTS) and neutogenic lower urinary tract dysfunction (NLUTD), and other conditions. The compounds may be administered alone or in combination with an anticholinergic compound.

Thienopyranecarboxamide derivatives

The invention relates to novel benzopyran derivatives of formula I, their N-oxides and pharmaceutically acceptable salts thereof. The compounds are endowed with enhanced selectivity for alpha1-adrenergic receptors and a low activity in lowering blood pressure. The compounds are useful in the treatment of obstructive syndromes of the lower urinary tract, including benign prostatic hyperplasia (BPH), and in the treatment of lower urinary tract symptoms (LUTS), neurogenic lower urinary tract dysfunction (NLUTD), and other conditions.

Benzopyran derivatives

The present invention is directed to novel 1-(N-phenylaminoalkyl)piperazine derivatives substituted at the position 2 of the phenyl ring. Pharmaceutical compositions comprising the compounds of the invention also are contemplated. The compounds of the present invention also are contemplated for use in treating neuromuscular dysfunction of the lower urinary tract in a mammal.

1-(N-phenylaminoalkyl)piperazine derivatives substituted at position 2 of the phenyl ring

The invention relates to novel N-(substituted phenyl)-N&prime;-&lsqb;&ohgr;-(5-substituted-7-oxo-7H-thieno&lsqb;3,2-b&rsqb;pyran-3-carbonylamino)alkyl&rsqb;piperazines their N-oxides and pharmaceutically acceptable salts thereof. The compounds are endowed with enhanced selectivity for alpha -adrenergic receptors and a low activity in lowering blood pressure. The compounds are useful in the treatment of obstructive syndromes of the lower urinary tract, including benign prostatic hyperplasia (BPH), and in the treatment of lower urinary tract symptoms (LUTS) and neurogenic lower urinary tract dysfunction (NLUTD). The compounds are also useful in the treatment of excessive intraocular pressure, cardiac arrhythmia, erectile dysfunction, sexual dysfunction, and for inhibiting cholesterol synthesis or reducing sympathetically mediated pain.

The invention relates to novel N-(substituted phenyl)-N&prime;-&lsqb;&ohgr;-(3-substituted phenyl-4-isoxazolecarbonylamino)alkyl&rsqb;piperazines, their N-oxides, and pharmaceutically acceptable salts thereof. The compounds are endowed with enhanced selectivity for alpha1-adrenergic receptors and a low activity in lowering blood pressure. The compounds are useful in the treatment of obstructive syndromes of the lower urinary tract, including benign prostatic hyperplasia (BPH), and in the treatment of lower urinary tract symptoms (LUTS) and neurogenic lower urinary tract dysfunction (NLUTD), and other conditions.

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Varese, Italy

Carlo Riva