Bifunctional agents possessing antioxidant and antiarrhythmic activity
AssigneeUni-Pharma Kleon Tsetis Pharmaceutical Laboratories S.A.
InventorsMaria Koufaki, Theodora Calogeropoulou, Alexandros Makriyannis
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Abstract
The present invention relates to novel bifunctional agents possessing antioxidant and antiarrhytmic activity, methods for the synthesis of the same and their applications in treating ischemia-reperfusion injury, as well as a variety of disorders related to free radicals and/or arrhythmias. These bifunctional drugs should preferentially segregate in the membrane and produce their antiarrhytmic effects while, at the same time, help in protecting the membrane lipids by scavenging free radicals. The present invention comprises compounds represented by Formula (I), wherein R1, R2, R3, R4, R5 are further defined
Claims7
A compound of Formula I
- wherein
- X=CH2,
- n=1,
- R1=H, alkyl, alkenyl, alkynyl, aryl all of which may be optionally substituted,
- R2=Alkyl, aryl, C(O)Y, C(O)R″′, CH2Y(CO)R″′, CH2YCH2R″′,
- R3=Alkyl, C(O)NH(CH2CH2)mNR′R″, NHC(O)CH2NR′R″, NHC(O)R″′,
- R4, R5=Lower alkyl,
- Y=HN(CH2CH2)mNH, HNCHR1NH, HN-cycloalkyl-NH, HN-aryl-NH, heterocyclic diamine, m=1–5
- R′, R″=Alkyl, and
- R″′=(methylsulfonyl)amino-N-aryl.
A process for the manufacture of a medicament for treating and/or reducing reperfusion arrhythmias, said process comprising including in said medicament a compound of Formula I
- wherein
- X=CH2, n=1,
- R1=alkyl, alkenyl, alkynyl, or aryl, all of which may be optionally substituted,
- R2=Alkyl, aryl, C(O)YC(O)R″′, CH2Y(CO)R″′, CH2YCH2R″′,
- R3=Alkyl, C(O)NH(CH2CH2)mNR′R″, NHC(O)CH2NR′R″, NHC(O)R″′,
- R4, R5=Lower alkyl,
- Y=HN(CH2CH2)mNH, HNCHR1NH, HN-cycloalkyl-NH, HN-aryl-NH, heterocyclic diamine, m=1–5,
- R′, R″=Alkyl, and
- R′″=(methylsulfonyl)amino-N-aryl.
A pharmaceutical formulation comprising at least one compound of Formula I and/or at least one pharmaceutically acceptable salt thereof
- wherein
- X=CH2, n=1,
- R1=H, alkyl, alkenyl, alkynyl, or aryl, all of which may be optionally substituted,
- R2=Alkyl, aryl, C(O)YC(O)R″′, CH2Y(CO)R″′, CH2YCH2R″′,
- R3=Alkyl, C(O)NH(CH2CH2)mNR′R″, NHC(O)CH2NR′R″, NHC(O)R″′,
- R4, R5=Lower alkyl,
- Y=HN(CH2CH2)mNH, HNCHR1NH, HN-cycloalkyl-NH, HN-aryl-NH, heterocyclic diamine, m=1–5,
- R′, R″=Alkyl, and
- R′″=(methylsulfonyl)amino-N-aryl.
Dependencies are inferred from the claim text.