COMPOUNDS DERIVED FROM 6, 7-DIHYDRO-3H-OXAZOLO [3,4-A] PYRAZINE-5, 8-DIONE

摘要

The present invention relates to novel derivatives of 6,7-dihydro-3H-oxazolo[3,4-a]pyrazine-5,8-dione, 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.

主权项

1. A compound derived from 6,7-dihydro-3H-oxazolo[3,4-a]pyrazine-5,8-dione, wherein it has the formula (I) where: R1 is an aromatic group, an aromatic group containing one or more heteroatoms, phenyl groups, phenol, 3-methoxy-4-phenol, methylene-3,4-dioxyphenyl, 2-methoxyphenyl, 3-methoxyphenyl, 4-methoxyphenyl, 3,4-dimethoxyphenyl, 2-halo-phenyl, 3-halo-phenyl, 4-halo-phenyl, furyl; pyridine, aromatic bicyclic, aromatic bicyclic containing one or more heteroatoms; R2 is aryl, heteroaryl, bicyclic aryl, CH2(CH2)nR3, CH2(CH2)nNR4R6, CHR6CH2OH, CH2CH(OH)R7, CH2(CH2)OR8, CH2(CH2)nSR9, carboxylate salts, sulfonate salts or quaternary ammonium salts; R3 is OH, NH2, NH3+, S(O)Me, SO3H, CO2H, Cl, carboxylate salts, sulfonate salts or quaternary ammonium salts; R4 is hydrogen, methyl, ethyl, propyl, i-propyl, butyl, sec-butyl, tert-butyl, phenyl, benzyl or quaternary ammonium salts; R5 is hydrogen, methyl, ethyl, propyl, i-propyl, butyl, sec-butyl, tert-butyl, phenyl, benzyl or quaternary ammonium salts; R6 is (R)-Me, (R)-Et, (R)-i-prop, (R)-i-But, (R)-phenyl, (R)—CH2SH, (R)—CH2CH2SCH3, (R)-benzyl, (R)-sec-But, (S)-Me, (S)-Et, (S)-i-prop, (S)-i-But, (S)-phenyl, (S)—CH2SH, (S)—CH2CH2SCH3, (S)-benzyl, (S)-sec-But or CH2OH; R7 is (R)-Me, (R)-Et; (R)-prop, (R)-i-prop, (R)-phenyl, (R)-benzyl, (S)-Me, (S)-Et; (S)-prop, (S)-i-prop (S)-phenyl or (S)-benzyl; R8 is C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, phenyl or benzyl; R9 is C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, phenyl or benzyl; N is a number between 0 and 4;the mixture of these derivatives, their salts, solvates, hydrates, prodrugs and pharmaceutically acceptable esters; and their enantiomers and/or diastereoisomers separated in their individual forms and/or in the forms of racemic or non-racemic mixtures with enantiomeric excess in any proportion.