C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 237/22 (2006.01) A61K 31/50 (2006.01) A61K 31/535 (2006.01) C07D 401/00 (2006.01) C07D 401/06 (2006.01) C07D 401/12 (2006.01) C07D 403/00 (2006.01) C07D 405/00 (2006.01) C07D 405/06 (2006.01) C07D 413/00 (2006.01)
Patent
CA 2074261
NOVEL 3(2H)-PYRIDAZINONES, PHARMACUTICAL COMPOSITIONS CON- TAINING THEM AND PROCESS FOR PREPARING SAME Abstract The invention relates to novel, racemic and optically active 3(2H)-pyridazinone derivatives of the general formula (I), Image (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 - 2 - 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 com- positions containing as active ingredient a compound of the general formula (I) as well as to a process for the prepara- tion 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.
Behr Agnes P.
Bodi Ilona
Czako Klara
Farkas Lajos
Jaszlits Laszlo
Behr Agnes P.
Bodi Ilona
Czako Klara
Farkas Lajos
G. Ronald Bell & Associates
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