DERIVATIVES OF PYRROLOPYRIMIDINE, METHOD FOR PREPARING AND THEIR USING Russian patent published in 2005 - IPC

FIELD: organic chemistry, chemical technology, medicine.

SUBSTANCE: invention relates to new derivatives of pyrrolopyrimidine of the formula (1) and their pharmaceutically acceptable salts possessing properties of selective inhibitor of specific cyclic guanosine 3',5'-monophosphate phosphodiesterase (specific cGMP PDE) (PDE V). In the formula (1) R¹ represents hydrogen atom (H), (C₁-C₃)-alkyl substituted optionally with one or some fluorine atoms; R² represents H, halogen atom, (C₁-C₆)-alkyl substituted optionally with hydroxyl group (-OH), (C₁-C₃)-alkoxy-group, (C₃-C₆)-cycloalkyl or one or some fluorine atoms, (C₃-C₆)-cycloalkyl; R³ represents (C₁-C₆)-alkyl substituted optionally with (C₃-C₆)-cycloalkyl or one or some fluorine atoms; R⁴ represents (C₁-C₆)-alkyl substituted optionally with one or some fluorine atoms; R⁵ represents -SO₂NR⁶R, -NHSO₂R⁸ or heterocyclyl such as tetrazolyl; each R⁶ and R⁷ represents independently H or (C₁-C₆)-alkyl substituted optionally with -CO₂H or one or some fluorine atoms; or in common with nitrogen atom to which they are bound form monocylic ring, such as imidazole, pyrrolidine, piperidine, morpholine, piperazine and homopiperazine wherein indicated group is replaced optionally with R⁹ wherein R⁹ represents (C₁-C₆)-alkyl substituted optionally with one or some halogen atoms, hydroxyl group (OH), (C₁-C₃)-alkoxy-group that is replaced optionally with one or some fluorine atoms, -NR¹¹R¹², -C=NR¹³(NR¹⁴R¹⁵) or tetrazolyl group, 6-membered nitrogen-containing heteroaryl group; each R¹¹ and R¹² represents independently H or (C₁-C₄)-alkyl; R¹³represents H; each R¹⁴ and R¹⁵ represents independently H. Also, invention relates to intermediate compounds, methods for preparing compounds and pharmaceutical compositions. Proposed compounds can be used in treatment of impotency, sexual dysfunction in females, stable, nonstable and variant (Prinzmental) stenocardia and other diseases also.

EFFECT: improved preparing method, valuable medicinal properties of compounds.

15 cl, 1 tbl, 250 ex