PHTHALAZINE DERIVATIVES AND THERAPEUTIC AGENTS IN ERECTILE DYSFUNCTION Russian patent published in 2004 - IPC

Abstract RU 2229476 C2

FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention relates to derivatives of phthalazine of the general formula (I) or their pharmaceutically acceptable salts or hydrates wherein R1 and R2 are similar or differ from one another and each represents halogen atom, (C1-C4)-alkyl group that can be substituted with halogen atom, hydroxyl group or (C1-C4)-alkoxy-group that can be substituted with halogen atom, or cyano-group; X represents cyano-group, halogen atom, hydroxyimino-group optionally O-substituted with (C1-C4)-alkyl group or heteroaryl group taken among thiazolyl, thienyl, pyrazolyl, triazolylyl and tetrazolyl groups that can be substituted with (C1-C4)-alkyl group; Y represents cyclic amino-groups i) - v) characterized in cl. 1 of the invention claim; vi) ethynyl or ethyl group substituted with (C1-C4)-alkyl group that, in turn, is substituted with series of substituents indicated in cl. 1 of invention claim; vii) optionally substituted phenyl group; viii) pyridyl or thiazolyl group. These compounds inhibit activity of cyclic phosphodiesterase type V and can be used as agents used in erectile dysfunction. Invention relates also to prophylactic and therapeutic agent used in erectile dysfunction that comprises above indicated compounds of invention as an active component. The object of invention is a therapeutic agent used in erectile dysfunction that comprises compound of the formula (VII) as an active component, its pharmacologically acceptable salt or hydrate wherein 1' represents a whole number from 1 to 3; R6 means halogen atom, (C1-C4)-alkyl group that can be substituted with halogen atom, or cyano-group; X1 represents cyano-group or halogen atom; Y1 represents groups i) - v) characterized in cl. 20 of the invention claim. Also, invention proposes method for preparing separate representatives of compounds of the general formula (I), pharmaceutical composition used for treatment of erectile dysfunction and method for treatment of erectile dysfunction, method for preparing compounds of the formula (VII), method for preparing intermediate compounds and method for preparing compounds of the formula (I). EFFECT: improved preparing method, valuable medicinal properties of compounds. 27 cl, 2 tbl, 168 ex

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RU 2 229 476 C2

Authors

Vatanabe Nobukhisa

Karibe Norio

Mijazaki Kazuki

Ozaki Fumikhiro

Kamada Atsusi

Mijazava Sukhei

Naoe Josimitsu

Kaneko Tosikhiko

Tsukada Itaru

Nagakura Tadasi

Isikhara Khiroki

Kodama Kokhtarou

Adati Khidejuki

Dates

2004-05-27Published

1999-02-17Filed