Orion-yhtyma Oy

Tapio J Korkolainen

Aino K Pippuri

Erkki A Nissinen

Erkki J Honkanen

Reijo J Backstrom

Inge-Britt Y Linden

Pentti Pohto

Reijo B Ackstr Om

A compound of formula I ##STR1## wherein R.sub.1 is nitro, halogeno or cyano group and R.sub.2 is a group selected from ##STR2## wherein Y and Z are independently oxygen, sulfur or NR, wherein R is hydrogen, straight or branched C.sub.1-8 alkyl, C.sub.5-7 cycloalkyl, phenylC.sub.1-8 alkyl or phenyl group and X.sub.1 and X.sub.2 are NR, where R is hydrogen, straight or branched C.sub.1-8 alkyl, C.sub.5-7 cycloalkyl, phenylC.sub.1-8 alkyl or phenyl group, or a pharmaceutically acceptable salt or ester thereof. Pharmaceutical compositions are also disclosed.

Pharmacologically active catechol derivatives

##STR1## Compounds of formula (I), wherein R.sub.1 is an electronegative substituent such as nitro, halogeno or cyano group and R.sub.2 is a group selected from (Ia) and (Ib), wherein R is hydrogen, or an alkyl, cycloalkyl, aralkyl or aryl group, wherein X.sub.1, X.sub.2, Y and Z are independently oxygen, sulfur of NR, wherein R may be as defined above and pharmaceutically acceptable esters and salts thereof are useful in the prevention or treatment of tissue damage induced by lipid peroxidation.

New catechol derivatives and pharmaceutically acceptable salts and esters thereof useful as pharmaceutical antioxidants are disclosed. Cellular damage by oxygen derived radicals is a significant factor in heart disease, rheumatoid arthritis, cancer, inflammatory disease, transplant rejection reactions and ischemia.

Known and new catechol derivates may be used as medicinal antioxidants in the prevention or treatment of tissue damage induced by lipid peroxidation. The conditions and diseases to be treated are for example heart disease, rheumatoid arthritis, cancer, inflammatory disease, a rejection reaction in organ transplants, ischemia, cancer and aging.

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Helsinki, Finland

Tapio J Korkolainen