Other

Università Degli Studi Di Roma "La Sapienza"

Rottapharm Spa

Universitá Degli Studi Di Siena

Rottapharm Biotech S.r.l.

Universta' Degli Studi Di Siena

Mariangela Biava

Maurizio Botta

Fabrizio Manetti

Giulio Cesare Porretta

Raffaello Pompei

Lucio C Rovati

Antonio Giordani

Maurizio Anzini

Delia Deidda

Francesco Makovec

Gianfranco Caselli

Andrea Cappelli

Vincenzo Calderone

Alessandro De Logu

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 compounds having formula 3 as well as the synthesis, intermediates and methods of using the same.

Pyrrole compounds as inhibitors of mycobacteria, synthesis thereof and intermediates thereto

The present invention concerns pyrrole compounds, derivatives of 1-{[1,5-bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl]methyl}-4-methylpiperazine (BM212). The invention concerns the use of the described compounds as antitubercular agents having high activity and low toxicity and process to obtain intermediates and final compounds.

Derivatives of 1-{[1,5-bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl]methyl}-4-methylpiperazine, synthesis process and uses thereof

Derivatives of 1-{[1,5-bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl] methyl}-4-methylpiperazine, synthesis process and uses thereof

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

Growing community of inventors

Rome, Italy

Mariangela Biava