Biolab Sanus Farmaceutica Ltda

Biolab Sanus Farmaceutical Ltda.

Sérgio Luiz Sacurai

Carlos Eduardo Da Costa Touzarim

Artur Franz Keppler

Marcio Henrique Zaim

Gilberto De Nucci

Fabiano Travanca Toledo

Bruno Artur De Sousa

Márcio Henrique Zaim

The present invention relates to novel derivatives of 6,7-dihydro-3H-oxazolo[3,4-a]pyrazine-5,8-dione represented by formula (I): and a mixture of these derivatives. The present invention also encompasses the pharmaceutical compositions comprising an effective amount of a said compounds, object of the present invention, as well as to the use of the compounds and/or derivatives as a phosphodiesterase enzyme inhibitor, and the use of the compounds and/or derivatives in the treatment of erectile dysfunction, disorders and/or conditions treatable with relaxation of tissues and disorders treatable with phosphodiesterase inhibitors, more particularly PDE-5 inhibitor. A further objective of the present invention is to provide a medication comprising a therapeutically effective amount of said compound and a method of treating using the said novel compounds.

Substituted oxazolo[3,4-a]pyrazines as pharmaceutcals

This invention describes new antifungal compounds that are aralkyl benzyl ethers of the formula (I): where Ar represents aryl, imidazolil, 1,2,4-triazolyl, benzimidazolil;R, R, Rand Rare independently hydrogen, halogen, Calkyl;Rrepresents halogen, Calkyl or O&#x2014;R' where R&#x2032; represents hydrogen or lower alkyl;Rrepresents aryl, substituted aryl, trifluoromethyl, trichloromethyl or O&#x2014;R&#x2032; where R&#x2032; represents hydrogen or lower alkyl; being the substituents of the aryl a halogen or a radical tetrazolyl;n and m represent independently an integer between 0 and 5;With the proviso that when Ar is imidazolil, Ris chlorine, Ris p-phenyl and R, R, Rand Rare hydrogen, n must be different from 2. When n and m are not 0 and 1, Ror Rcan be represented by substituents not necessarily equal.

Benzyl aralkyl ether compounds, method for preparing same, intermediate compounds, use of said compounds, method for treatment and/or prevention, pharmaceutical composition and medicament containing same

A series of derivatives of 6,7-dihydro-3H-oxazolo[3,4-a]pyrazine-5,8-dione, mixtures thereof, their pharmaceutically acceptable salts, which are inhibitors of PDE-5, possessing vasodilatator properties and relaxing effects. In particular, compounds of formula (I), where R, R, R, and Rare defined herein, processes for the preparation of said compounds, pharmaceutical compositions containing them, as well as uses as inhibitors of the enzyme phosphodiesterase type 5 (PDE-5) in the treatment of the erectile dysfunction and PDE-5 inhibitor treatable disorders. 

Derivatives of 6,7-dihydro-3H-oxazolo[3,4-a]pyrazine-5,9-dione as PDE-5 inhibitors

The present invention describes a series of derivatives of 2-(3-methylenedioxy)-benzoyl indol, their mixtures, their pharmaceutically acceptable salts, their enantiomers, pharmaceutical compositions comprising them, processes for preparing them, use in the prophylactic and/or curative treatment of sexual dysfunction. More specifically, the invention describes derivatives (R)-3-((2-(benzo[d][1,3]dioxol-5-carbonyl)-1H-indol-3-yl)methyl)-1-methylpiperazine-2,5-dione, and S)-3-((2-(benzo[d][1,3]dioxol-5-carbonyl)-1H-indol-3-yl)methyl)-1-methylpiperazine-2,5-dione.

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São Paulo, Brazil

Sérgio Luiz Sacurai