发明名称 |
3(2H)-PYRIDAZINONES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESS FOR PREPARING SAME |
摘要 |
NOVEL 3(2H)-PYRIDAZINONES, PHARMACUTICAL COMPOSITIONS CON TAINING THEM AND PROCESS FOR PREPARING SAME The invention relates to novel, racemic and optically active 3(2H)-pyridazinone derivatives of the general formula (I), (I) wherein R1 means hydrogen; a C1-4alkyl group optionally substituted by an R5R6N- group where R5 and R6, being the same or different, stand for a C1-4alkyl group or R5R6N- together represents a 6-membered heterocyclic group optionally containing an oxygen or an R7N- moiety where R7 is a C1-4alkyl optionally substituted by a phenyoxy group or a C3-5alkenyl optionally substituted by a phenyl grup; or a C1-4alkyl group substituted by a mono- or polysubstituted phenyl, phenoxy or benzyloxy group; or a C3-5alkenyl or C3-5alkynyl optionally substituted by an unsubstituted or optionally substituted phenyl group; or a phenyl group; R2 means hydrogen; or a C1-4alkyl optionally substituted by a morpholino, pyridyl, 1,4-benzodioxanyl or an optionally substituted phenyl group; R3 means hydrogen or an optionally substituted phenyl group; R4 means hydrogen; or R8CO- group where R8 is a C1-4alkyl, phenyl or pyridyl group or an amino group substituted by a C1-4alkyl group; or an -SO3M moiety where M is hydrogen or an organic or inorganic cation; X means halogen; and n is 1, 2 or 3, with the proviso that R1 is different from a C1-4alkyl, alkenyl, aralkyl and phenyl group when n is 1, as well as their tautomers and the acid addition salts of these compounds. The invention further relates to pharmaceutical compositions containing as active ingredient a compound of the general formula (I) as well as to a process for the preparation of compounds of the general formula (I). The compounds of the invention possess a significant calmodulin-antagonizing effect, decrease the coronary resistance and are less toxic. Thus, these compounds are useful for treating cardiovascular diseases, particularly angina pectoris.
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申请公布号 |
CA2074261(A1) |
申请公布日期 |
1992.06.28 |
申请号 |
CA19912074261 |
申请日期 |
1991.12.20 |
申请人 |
RICHTER GEDEON VEGYESZETI GYAR RT |
发明人 |
MATYUS, PETER;JASZLITS, LASZLO;KURTHY, MARIA;ZARA, DENESNE;KOVACS, ANIKO;FARKAS, LAJOS;VARGA, ILDIKO;MAGO, ISTVANNE;RABLOCZKY, GYORGY;KOSARY, JUDIT;BEHR, AGNES P.;KARPATI, EGON;SEBESTYEN, LASZLO;CZAKO, KLARA;SANDOR, ELEK;MATHE, GYORGY;SZEDERKENYI, FERENC;BODI, ILONA;JEDNAKOVITS, ANDREA;PODANYI, BENJAMIN |
分类号 |
A61K31/50;A61P9/08;A61P9/10;C07D237/22;C07D237/24;C07D401/06;C07D401/12;C07D405/06;(IPC1-7):C07D237/22;C07D401/00;C07D403/00;C07D405/00;C07D413/00;A61K31/535 |
主分类号 |
A61K31/50 |
代理机构 |
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