BMS-582949: Crystalline form of a p38α inhibitor? WO2008079857

Expert Opinion on Therapeutic Patents

Volumn 19, Issue 8, 2009, Pages 1165-1168

  Norman, Peter ^a  

^a NORMAN CONSULTING   (United Kingdom)

Author keywords

BMS 582949; BMS 640994; IL 1; Inflammation; MAP kinase; p38; Rheumatoid arthritis; TNF

Indexed keywords

4 (4 FLUOROPHENYL) 2 (4 METHYLSULFINYLPHENYL) 5 (4 PYRIDYL)IMIDAZOLE; 5 (2,6 DICHLOROPHENYL) 2 (2,4 DIFLUOROPHENYLTHIO)PYRIMIDO[1,6 B]PYRIDAZIN 6 ONE; AM 102; AMIDE; ARRY 797; BMS 582949; BMS 640994; CRYSTALLIN; K 832; KC 706; MITOGEN ACTIVATED PROTEIN KINASE P38 INHIBITOR; N [5 (CYCLOPROPYLCARBAMOYL) 2 METHYLPHENYL] 5 METHYL 1 [3 (TRIFLUOROMETHYL)PYRIDIN 2 YL] 1H PYRAZOLE 4 CARBOXAMIDE; PH 797804; SEMAPIMOD; TALMAPIMOD; UNCLASSIFIED DRUG; VX 702; WO 2008079857;

ANTIINFLAMMATORY ACTIVITY; BIOASSAY; CLINICAL TRIAL; CORONARY ARTERY ATHEROSCLEROSIS; CROHN DISEASE; DRUG STRUCTURE; HUMAN; IN VITRO STUDY; IN VIVO STUDY; INFLAMMATORY DISEASE; NONHUMAN; PAIN; PATENT; PSORIASIS; REVIEW; RHEUMATOID ARTHRITIS;

ANIMALS; CLINICAL TRIALS, PHASE II AS TOPIC; HUMANS; P38 MITOGEN-ACTIVATED PROTEIN KINASES; PATENTS AS TOPIC; PROTEIN KINASE INHIBITORS; PYRAZOLES; PYRIDINES;

EID: 68249095929     PISSN: 13543776     EISSN: None     Source Type: Journal    
DOI: 10.1517/13543770902816160     Document Type: Review

References (16)

1. Lee JC, Kumar S, Griswold DE, et al. Inhibition of p38 MAP kinase as a therapeutic strategy. Immunopharmacology 2000;47:185-201 ••Excellent review of the older literature from what used to be the leading group.
2. Herlaar E, Brown Z. p38 MAPK signalling cascades in inflammatory disease. Mol Med Today 1999;5:439-448 ••Good, well-illustrated, review. (Pubitemid 29455026)
3. Dodeller F, Schulze-Koops H. The p38 mitogen-activated protein kinase signaling cascade in CD4 T cells. Arthritis Res Ther 2006:205
4. Lee MR, Dominguez C. MAP kinase p38 inhibitors: clinical results and an intimate look at their interactions with p38alpha protein. Curr Med Chem 2005;12(25):2979-2994 (Pubitemid 41672487)
5. Dominguez C, Powers DA, Tamayo N. p38 MAP kinase inhibitors: many are made, but few are chosen. Curr Opin Drug Discov Dev 2005;8(4):421-430 (Pubitemid 40921741)
6. Dambach DM. Potential adverse effects associated with inhibition of p38alpha/beta MAP kinases. Curr Top Med Chem 2005;5(10):929-939 •Rare review on the documented side effects of p38 inhibitors.
7. Norman P. Kinase therapeutic pipelines: an assessment of targets and agents in development CHI Insight reports december 2007. p. 71-76
8. Karaman MW, Herrgard S, Treiber DK, et al. A quantitative analysis of kinase inhibitor selectivity. Nat Biotechnol 2008;26:127-132 ••Comprehensive profiling of several kinase inhibitors.
9. Murali Dhar TG, Wrobleski ST, Lin S, et al. Synthesis and SAR of p38alpha MAP kinase inhibitors based on heterobicyclic scaffolds. Bioorg Med Chem Lett 2007;17(18):5019-5024 (Pubitemid 47259677)
10. Hynes J Jr, Dyckman AJ, Lin S, et al. Design, synthesis, and anti-inflammatory properties of orally active 4-(phenylamino) -pyrrolo[2,1-f ][1,2,4]triazine p38alpha mitogen-activated protein kinase inhibitors. J Med Chem 2008;51(1):4-16
11. Liu C, Lin J, Pitt S, et al. Benzothiazole based inhibitors of p38alpha MAP kinase. Bioorg Med Chem Lett 2008;18(6):1874-1879
12. Sack JS, Kish KF, Pokross M, et al. Structural basis for the high-affinity binding of pyrrolotriazine inhibitors of p38 MAP kinase. Acta Crystallogr D Biol Crystallogr 2008;D64(Pt 7):705-710 (Pubitemid 351872050)
13. Hynes J Jr, WU H, Pitt S, et al. The discovery of (R)-2-(sec-butylamino)- N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38alpha MAP kinase inhibitor. Bioorg Med Chem Lett 2008;18(6):1762-1767
14. Bristol-Myers Squibb Co. Process for preparing salts of 4-[[5-[(cyclopropylamino)carbonyl]-2-methylphenyl]amino]-5-methyln- propylpyrrolo[2,1-f ][1,2,4] triazine-6-carboxamide and novel stable forms produced therein. WO2006113682; 2006
15. Bristol-Myers Squibb Co. New pyrazole-amide compounds are p38 kinase inhibitors - useful for the treatment of inflammatory disorders. WO2004098518; 2004
16. Bristol-Myers Squibb Co. Pyrrolo-triazine aniline compounds useful as kinase inhibitors. WO03090912; 2003