Rotta Research Laboratorium S.p.a.

Rottapharm Spa

Universitá Degli Studi Di Siena

Rottapharm Biotech S.r.l.

Maurizio Anzini

Lucio C Rovati

Andrea Cappelli

Francesco Makovec

Salvatore Vomero

Antonio Giordani

Gianfranco Caselli

Mariangela Biava

Vincenzo Calderone

Germano Giuliani

Lucio Claudio Rovati

1,5-diaryl-2-alkylpyrrole-3-substituted nitro esters, of Formula (I) are provided. Such compounds are potent and selective COX-2 inhibitors which are able to release NO in concentrations that make it possible to counteract the side effects due to selective COX-2 inhibition, without giving rise to hypotensive effects. Formula (I) includes compounds wherein the groups R' and R&#x2033; are: &#x2014;H, &#x2014;F, &#x2014;Cl, &#x2014;Br, &#x2014;CH, &#x2014;CF, &#x2014;OCH, &#x2014;SCH, R1 is methyl, ethyl, trifluoromethyl, hydroxymethyl, methoxymethyl and the substituent in position &#x2212;3 of the pyrrole ring is a chain, where the groups X, Y, Z, W and R2 are: X is a carbonyl or a group &#x2014;(CHR)&#x2014;, Y is an oxygen atom or the group &#x2014;NR&#x2014; and Z is a carbonyl or a group &#x2014;(CHR)&#x2014;, or a [&#x2014;CH(COOH)&#x2014;] group, or a group &#x2014;(NR)&#x2014;, W is an aliphatic chain substituted with one or two (&#x2014;O&#x2014;NO) groups, R2 is: &#x2014;H, &#x2014;OH, &#x2014;OCH, or &#x2014;NHR. Ris: &#x2014;H, &#x2014;CH, &#x2014;CHCH, [&#x2014;CH(CH)]. R&#x2032;&#x2033; is methylsulphonyl or sulphonamido. Pharmaceutical formulations and methods of making an using such formulations are also provided.

1,5-Diary1-2-alkylpyrrole-3-substituted nitro esters, selective COX-2 inhibitors and nitric oxide donors

The present invention relates to compound of formula I: and their use as chemiluminescent and/or bioluminescent reagents. 

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Amidine, thiourea and guanidine derivatives of appropriately substituted 2-aminobenzothiazoles, 2-amino-3,1-4H-benzothiazines and 3-amino-1,4-3H-benzothiazines, as understood from formula (I), the related pharmaceutically acceptable salts and solvates thereof: 

Amidine, thiourea and guanidine derivatives of 2-aminobenzothiazoles and aminobenzothiazines for their use as pharmacological agents for the treatment of neurodegenerative pathologies

This invention relates to 3-substituted-1,5-diaryl-2-alkyl-pyrroles of Formula I, pharmaceutical compositions containing them, and to their use for the pharmacological treatment of pain and COX-2 over-activation associated disorders. Compounds of this invention are new pyrrole derivatives bearing in position -3 of the pyrrole ring, several variously functionalized, not aliphatic, side chains which confer to the compounds a relevant COX-2 potency and selectivity along with a remarkable oral efficacy. Phenyl rings in position -1 and -5 are variously substituted, but compounds of particular interest are those substituted in position -5 with 4-methylsulphonyl-phenyl or with 4-aminosulphonyl-phenyl groups. 

3-substituted-1,5-diarly-2-alkyl-pyrroles highly selective and orally effective COX-2 inhibitors

Basic derivatives of benz&lsqb;e&rsqb; isoindol-1-ones and pyrrolo&lsqb;3,4-c&rsqb; quinolin-1-ones with 5-HT3-antagonistic activity, their preparation and their therapeutic use

Novel basic derivatives of benz&lsqb;e&rsqb;isoindol-1-ones and pyrrolo&lsqb;3,4-c&rsqb;quinolin-1-ones which can be represented by the general formula (I) indicated below are described:

Basic derivatives of benz&lsqb;E&rsqb;isoindol-1-ones and pyrrolo&lsqb;3,4-c&rsqb;quinolin-1-ones with 5-HT3-antagonistic activity, their preparation and their therapeutic use

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Pianella/Castelnuovo Berardenga, Italy

Maurizio Anzini