Orally effective ion chelators

Abstract

Abstract Compounds are described of the general formula: ##STR1## wherein: R 1 is acyl of the formula --C(═O)--R 5 ; R 2 , R 3 , and R 4 are each selected from the group consisting of hydrogen and acyl of the formula: --C(═O)--R.sub.5 wherein R 5 is selected from the group consisting of alkyls, substituted alkyls, alkenyls, substituted alkenyls, cycloalkyls, substituted cycloalkyls, arylalkylenes, substituted arylalkylenes, alkylenecycloalkyls, alkylene substituted cycloalkyls, alkynyls, substituted alkynyls, aryls and substituted aryls, wherein R 2 , R 3 and R 4 are selected such that at least one of R 2 , R 3 and R 4 is an acyl. When R 2 , R 3 and R 4 include one or more acyls that are not identical to the acyl of R 1 , these compounds of formula I are novel compounds. The invention also includes processes to produce the compounds of formula I. Compounds of formula I complex and/or chelate tissue tri-valent ions, especially iron (Fe +++ ), when administered to a human being, and are therefore useful in therapy in the treatment of diseases in which tissue ion levels in the body have increased or toxic levels. These diseases include, for example, thalassemia major, sideroachrestic anemic, Blackfan-Diamond anemia, aplastic anemia, sickle cell anemia, nemolytic anemias and nemosiderosis brought about by multiple blood transfusions including treatment for the anemia accompanying conditions requiring kidney dialysis.

Inventors

• 👤 Donald E. Green

Bibliographic Details