Recent developments on JAK2 inhibitors: a patent review.
BACKGROUND
JAK2 is one of the most promising targets against neoplastic growth. A somatic mutation (V617F) resulting in enhanced JAK2 kinase activity can be frequently found in patients with serious myeloproliferative neoplasms such as polycythemia vera, essential thrombocythemia and primary myelofibrosis. Preclinical results strongly support that JAK2 inhibitors could be effectively used in these indications. Pharmaceutical companies and academic groups have developed a number of potent JAK2 inhibitors during the last decade. Tolerability and effectiveness of the most promising compounds are currently being investigated in clinical trials.


METHODS
In this paper, we aim to give a comprehensive review of the currently available patent literature of JAK2 inhibitors.


RESULTS
We tried to collect the published core structures possessing JAK2 inhibitory potency including compounds developed by academic and industrial research groups. We review the currently available patent literature as well as the key papers containing additional information about the described JAK2 inhibitors. Clinical status data were collected by searching the Prous Integrity and Pharmaprojects databases.


CONCLUSIONS
The significant number of JAK2 inhibitors published and numerous clinical trials involving these compounds suggest that some of them might be approved in the next few years and can serve as novel drugs for the treatment of JAK2-dependent pathologies.
Kiss
Róbert
R
Heriot-Watt University, Edinburgh, UK.
Sayeski
Peter P
PP
Keserũ
György M
GM
D000818:Animals; D000970:Antineoplastic Agents / Q000009:adverse effects / Q000494:pharmacology* / Q000627:therapeutic use; D002986:Clinical Trials as Topic; D016503:Drug Delivery Systems; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D006801:Humans; D053614:Janus Kinase 2 / Q000037:antagonists & inhibitors*; D009369:Neoplasms / Q000188:drug therapy* / Q000201:enzymology / Q000235:genetics; D010330:Patents as Topic; D047428:Protein Kinase Inhibitors / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use
D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; C507924:JAK2 protein, human; D053614:Janus Kinase 2