Reduced FK228 and use thereof
View Patent ↗The present invention relates to reduced FK228 of the formula (I) wherein R 1 and R 2 are the same or different and each is a hydrogen atom or a thiol-protecting group, or a salt thereof, and a histone deacetylase inhibitor containing this compound, an expression potentiator and a reactivation promoter of a transgene, and pharmaceutical agents containing them as active ingredients. The reduced FK228 or a salt thereof has a strong histone deacetylase inhibitory activity and this compound can be used for the prophylaxis or treatment of various diseases, in which histone deacetylation is involved, and for the gene therapy of such diseases.
1. A compound represented by the formula (I)
wherein R 1 and R 2 are the same or different and each is a hydrogen atom or a thiol-protecting group, or a salt thereof.
2. The compound of claim 1 , wherein R 1 and R 2 are each a hydrogen atom, or a salt thereof.
3. The compound of claim 2 , which is represented by the formula (II)
wherein R 1 and R 2 are each a hydrogen atom, or a salt thereof.
4. A method of producing a compound of claim 1 or a salt thereof, which comprises cleaving a disulfide bond in a compound represented by the formula (III)
5. The method of claim 4 , wherein the compound of the formula (III) is represented by the formula (IV)
6. A method for the treatment of tumor, inflammatory disorders, diabetes, diabetic complication, homozygous thalassemia, fibrosis, cirrhosis, acute promyelocytic leukemia (APL), organ transplant rejection or autoimmune disease, which comprises administering a pharmaceutically effective amount of a compound of claim 1 , or a salt thereof, to a patient in need thereof.