210244-51-2Relevant articles and documents
CN128: A New Orally Active Hydroxypyridinone Iron Chelator
Chen, Wenteng,Yuan, Xin,Li, Zhi,Lu, Zidong,Kong, Sisi,Jiang, Huidi,Du, Houbing,Pan, Xiuhong,Nandi, Manasi,Kong, Xiaole,Brown, Kathryn,Liu, Zudong,Zhang, Guolin,Hider, Robert C.,Yu, Yongping
, p. 4215 - 4226 (2020)
Deferoxamine, deferiprone, and deferasirox are used for the treatment of systemic iron overload, although they possess limitations due to lack of oral activity, lower efficacy, and side effects. These limitations led to a search for an orally active iron chelator with an improved therapeutic index. The lower efficacy of deferiprone is due to rapid glucuronidation, leading to the formation of a nonchelating metabolite. Here, we demonstrate that the influence of metabolism can be reduced by introducing a sacrificial site for glucuronidation. A log P-guided investigation of 20 hydroxpyridinones led to the identification of CN128. The Fe(III) affinity and metal selectivity of CN128 are similar to those of deferiprone, the log P value is more lipophilic, and its iron scavenging ability is superior. Overall, CN128 was demonstrated to be safe in a range of toxicity assessments and is now in clinical trials for the treatment of β-thalassemia after regular blood transfusion.
5-aminolevulinic acid/3-hydroxyl pyridone conjugate, preparation method therefor and use of 5-aminolevulinic acid/3-hydroxyl pyridone conjugate
-
Paragraph 0048; 0049, (2017/08/28)
The invention discloses conjugates of 5-aminolevulinic acid and 3-hydroxyl pyrid-4-one. The conjugates are conjugates of 5-aminolevulinic acid and an iron chelating agent, i.e., 3-hydroxyl pyrid-4-one and are ALA-HPO conjugates 1 to 4 separately. The invention further simultaneously discloses a preparation method for the conjugates of 5-aminolevulinic acid and 3-hydroxyl pyrid-4-one and use of the conjugates of 5-aminolevulinic acid and 3-hydroxyl pyrid-4-one. The conjugates can be used for preparing photodynamic therapy drugs and can also be used for preparing drugs for treating skin cancer, lung cancer or verruca acuminata.
PYRIDINONE COMPOUNDS FOR USE IN PHOTODYNAMIC THERAPY
-
Page/Page column 17, (2014/03/25)
A compound which is a compound of formula (I) or any salt thereof: wherein R1 is a Ci-C6 alkyl group, R2 is H or a Ci-C6 alkyl group, R3 is H or a Ci-C6 alkyl group, and n is an integer from 0 to 5.