Highly selective Janus kinase 3 inhibitors based on a pyrrolo[2,3-d] pyrimidine scaffold: Evaluation of WO2013085802

Expert Opinion on Therapeutic Patents

Volumn 24, Issue 1, 2014, Pages 121-125

  Norman, Peter ^a  

^a NORMAN CONSULTING   (United Kingdom)

Author keywords

Asthma; Autoimmune disease; JAK3 inhibitor; Rheumatoid arthritis

Indexed keywords

ADELATINIB; ASP 015K; BARICITINIB; GLPG 0634; GSK 2586184; JANUS KINASE 3 INHIBITOR; PYRROLO[2,3 D]PYRIMIDINE NUCLEOSIDE; RUXOLITINIB; TOFACITINIB; UNCLASSIFIED DRUG;

ALLERGIC ASTHMA; ARTICLE; AUTOIMMUNE DISEASE; CHRONIC OBSTRUCTIVE LUNG DISEASE; COMPETITIVE INHIBITION; COVALENT BOND; DRUG POTENCY; DRUG SELECTIVITY; ENZYME ACTIVE SITE; HEMATOPOIETIC CELL; HUMAN; IC 50; LUPUS VULGARIS; MYELOPROLIFERATIVE DISORDER; NEOPLASM; PHASE 2 CLINICAL TRIAL (TOPIC); PHASE 3 CLINICAL TRIAL (TOPIC); PROTEIN EXPRESSION; PSORIASIS; RHEUMATOID ARTHRITIS; SUZUKI REACTION;

ANIMALS; DRUG DESIGN; HUMANS; JANUS KINASE 3; LEGISLATION, DRUG; MOLECULAR STRUCTURE; MOLECULAR TARGETED THERAPY; PATENTS AS TOPIC; PROTEIN KINASE INHIBITORS; PYRIMIDINES; PYRROLES; SIGNAL TRANSDUCTION; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84890348401     PISSN: 13543776     EISSN: 17447674     Source Type: Journal    
DOI: 10.1517/13543776.2014.851670     Document Type: Article

References (24)

1. Ihle JN. The Janus kinase family and signaling through members of the cytokine receptor superfamily. Proc Soc Exp Biol Med 1994;206(3):268-72
2. O'Shea JJ, Kontzias A, Yamaoka K, et al. Janus kinase inhibitors in autoimmune diseases. Ann Rheum Dis 2013;72(Suppl 2):ii111-5
3. Hoock T, Hogan J, Mahajan S, et al. VX-509, An orally available janus kinase 3 (JAK3) specific inhibitor, showed robust activity in pre-clinical models of aberrant immune/inflammatory function. Arthritis Rheum 2011;63(Suppl 10):1136
4. Fleischmann R, Spencer-Green GT, Fan F, et al. Dose ranging study of VX-509, an oral selective JAK3 inhibitor, as monotherapy in patients with active rheumatoid arthritis (RA). Arthritis Rheum 2011;63:4042
5. Thoma G, Nuninger F, Falchetto R, et al. Identification of a potent Janus kinase 3 inhibitor with high selectivity within the Janus kinase family. J Med Chem 2011;54(1):284-8
6. Soth M, Hermann JC, Yee C, et al. 3-Amido pyrrolopyrazine JAK kinase inhibitors: Development of a JAK3 vs JAK1 selective inhibitor and evaluation in cellular and in vivo models. J Med Chem 2013;56(1):345-56
7. Jaime-Figueroa S, De Vicente J, Hermann J, et al. Discovery of a series of novel 5H-pyrrolo[2,3-b]pyrazine-2- phenyl ethers, as potent JAK3 kinase inhibitors. Bioorg Med Chem Lett 2013;23(9):2522-6
8. Lynch SM, DeVicente J, Hermann JC, et al. Strategic use of conformational bias and structure based design to identify potent JAK3 inhibitors with improved selectivity against the JAK family and the kinome. Bioorg Med Chem Lett 2013;23(9):2793-800
9. Wilson LJ. Recent patents in the discovery of small molecule inhibitors of JAK3. Expert Opin Ther Pat 2010;20(5):609-23
10. Dymock BW, See CS. Inhibitors of JAK2 and JAK3: An update on the patent literature 2010 - 2012. Expert Opin Ther Pat 2013;23(4):449-501
11. Merck Sharp & Dohme Corp. Inhibitors of Janus kinases. WO2010014453; 2010
12. Merck Sharp & Dohme Corp. Inhibitors of Janus kinases. WO2010011375; 2010
13. Merck Sharp & Dohme Corp. Azaindoles as Janus kinase inhibitors. WO2011137022; 2011
14. Merck Sharp & Dohme Corp. Cyanomethylpyrazole carboxamides as Janus kinase inhibitors. WO-2013043962; 2013
15. Merck Sharp & Dohme Corp. Cycloalkylnitrile pyrazole carboxamides as Janus kinase inhibitors. WO-2013040863; 2013
16. Merck Sharp & Dohme Corp. Pyrazole carboxamides as Janus kinase inhibitors. WO-2013041042; 2013
17. Norman P. Selective JAK1 inhibitors based on a 3-Aminopyrazole-4- carboxamide scaffold. Expert Opin Ther Pat 2013;In press
18. Merck Sharp & Dohme Corp. Bicyclic diamines as Janus kinase inhibitors. WO2012054364; 2012
19. Merck Sharp & Dohme Corp. Pyrrolopyrimidines as Janus kinase inhibitors. WO-2013085802; 2013
20. Yamazaki S, Inami M, Ito M, et al. ASP015K: A Novel JAK inhibitor demonstrated potent efficacy in adjuvant-induced arthritis model in rats. Arthritis Rheum 2012;64(Suppl 10):2084
21. Vertex Pharmaceuticals, Inc. Tricyclic heteroaryl compounds useful as inhibitors of janus kinase. EP-2079740B1; 2007
22. Malaviya R, Laskin DL, Malaviya R. Janus kinase-3 dependent inflammatory responses in allergic asthma. Int Immunopharmacol 2010;10(8):829-36
23. Guntur VP, Reinero CR. The potential use of tyrosine kinase inhibitors in severe asthma. Curr Opin Allergy Clin Immunol 2012;12(1):68-75
24. Ghoreschi K, Laurence A, O'Shea JJ. Janus kinases in immune cell signaling. Immunol Rev 2009;228:273-87