MEK inhibitors: a patent review 2008 – 2010

Bibliography

• Wallace E. Blake JF. Discovery of allosteric MEK inhibitors. In: Li R, Stafford JA, editors, Kinase Inhibitor Drugs. John Wiley and Sons, New York; 2009. p. 229-52
   Google Scholar
• Sebolt-Leopold JS, Bridges AJ. Road to PD0325901 and beyond: the MEK inhibitor quest. In: Li R, Stafford JA, editors, Kinase Inhibitor Drugs. John Wiley and Sons, New York; 2009. p. 205-27
   Google Scholar
• McCubrey JA, Steelman LS, Abrams SL, Emerging MEK inhibitors. Expert Opin Emerg Drugs 2010;15(2):203-23
   Google Scholar
• Wong KK. Recent developments in anti-cancer agents targeting the Ras/Raf/ MEK /ERK pathway. Recent Patents Anti-Cancer Drug Discov 2009;4(1):28-35
   PubMed Web of Science ®Google Scholar
• Price S. Putative allosteric MEK1 and MEK2 inhibitors. Expert Opin Ther Patents 2008;18(6):603-27
   Google Scholar
• Wang J, Wilcoxen KM, Nomoto K, Recent advances of MEK inhibitors and their clinical progress. Curr Top Med Chem 2007;7(14):1364-78
   PubMed Web of Science ®Google Scholar
• Wallace EM, Lyssikatos JP, Yeh T, Progress towards therapeutic small molecule MEK inhibitors for use in cancer therapy. Curr Top Med Chem 2005;5(2):215-29
   Google Scholar
• Lorusso PM, Adjei AA, Varterasian M, Phase I and pharmacodynamic study of the oral MEK inhibitor CI-1040 in patients with advanced malignancies. J Clin Oncol 2005;23:5281-93
   PubMed Web of Science ®Google Scholar
• Rinheart J, Adjei AA, Lorusso PM, Multicenter phase II study of the oral MEK inhibitor, CI-1040, in patients with advanced NSCL, breast, colon, and pancreatic cancer. J Clin Oncol 2004;22:4456-62
   Google Scholar
• Lorusso P, Krishnamurthi S, Rinheart JR, A phase 1-2 clinical study of a second generation oral MEK inhibitor, PD 0325901, in patients with advanced cancer. J Clin Oncol 2005;23:3011
   Web of Science ®Google Scholar
• Menon SS, Whitfield LR, Sadis S, PK and PD of PD-0325901, a second generation MEK inhibitor after multiple doses of PD-0325901 to advanced cancer patients. J Clin Oncol 2005;23:3066
   Web of Science ®Google Scholar
• Haura EB, Ricart AD, Larson TG, A Phase II study of PD-0325901, an oral MEK inhibitor, in previously treated patients with advanced non-small cell lung cancer. Clin Cancer Res 2010;16(8):2450-7
   PubMed Web of Science ®Google Scholar
• Barrett SD, Bridges AJ, Dudley DT, The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901. Bioorg Med Chem Lett 2008;18(24):6501-4
   PubMed Web of Science ®Google Scholar
• Warmus JS, Flamme C, Zhang LY, 2-Alkylamino- and alkoxy-substituted 2-amino-1,3,4-oxadiazoles-O-Alkyl benzohydroxamate esters replacements retain the desired inhibition and selectivity against MEK (MAP ERK kinase). Bioorg Med Chem Lett 2008;18(23):6171-4
   Google Scholar
• Lee L, Niu HF, Rueger R, The safety, tolerability, pharmacokinetics, and pharmacodynamics of single oral doses of CH4987655 in healthy volunteers: target suppression using a biomarker. Clin Cancer Res 2009;15(23):7368-74
   Google Scholar
• Lee L, Niu H, Goelzer P, The safety, tolerability, pharmacokinetics, and pharmacodynamics of single oral doses of RO5068760, an MEK inhibitor, in healthy volunteers: assessment of target suppression. J Clin Pharmacol 2010;50(12);1397-405
   Google Scholar
• Isshiki Y, Kohchi Y, Iikura H, Design and synthesis of novel allosteric MEK inhibitor CH4987655 as an orally available anticancer agent. Bioorg Med Chem Lett 2010; 21:179501801
   Google Scholar
• Daouti S, Higgins B, Kolinsky K, Preclinical in vivo evaluation of efficacy, pharmacokinetics, and pharmacodynamics of a novel MEK1/2 kinase inhibitor RO5068760 in multiple tumor models. Mol Cancer Ther 2010;9(1):134-44
   Google Scholar
• Abe H, Kikuchi S, Hayakawa K, Discovery of a highly potent and selective MEK inhibitor: GSK1120212. ACS Med Chem Lett 2011;2(4):320-4
   Google Scholar
• Gilmartin AG, Bleam MR, Groy A, GSK1120212 (JTP-74057) is an inhibitor of MEK activity and activation with favorable pharmacokinetic properties for sustained In vivo pathway inhibition. Clin Cancer Res 2011;17(5):989-1000
   Google Scholar
• Kim K, Kong S, Fulciniti M, Blockade of the MEK/ERK signaling cascade by AS703026, a novel selective MEK1/2 inhibitor, induces pleiotropic anti-myeloma activity in vitro and in vivo. Br J Haematol 2010;149(4):537-49
   Google Scholar
• Yoon J, Koo K, Choi K, MEK1/2 Inhibitors AS703026 and AZD6244 may be potential therapies for KRAS mutated colorectal cancer that is resistant to EGFR monoclonal antibody therapy. Cancer Res 2011;71(2):445-53
   Google Scholar
• Dong Q, Dougan DR, Gong X, Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer. Bioorg Med Chem Lett 2011;21:1315-19
   PubMed Web of Science ®Google Scholar
• Kay J, Morales R, Bellatin L, Treatment of rheumatoid arthritis with a MEK inhibitor: results of a 12-week, randomized, placebo-controlled phase 2 study in patients with active rheumatoid arthritis on a background of methotrexate. Annual European Congress of Rheumatology, June 17, 2010
   Google Scholar
• Yeh TC, Marsh V, Bernat BA, Biological characterization of ARRY-142886 (AZD6244 ), a potent, highly selective mitogen-activated protein kinase kinase 1/2 inhibitor. Clin Cancer Res 2007;13(5):1576-83
   PubMed Web of Science ®Google Scholar
• Adjei AA, Cohen RB, Franklin W, Phase I pharmacokinetic and pharmacodynamic study of the oral, small-molecule mitogen-activated protein kinase kinase 1/2 inhibitor AZD6244 (ARRY-142886) in patients with advanced cancers. J Clin Oncol 2008;26(13):2139-46
   PubMed Web of Science ®Google Scholar
• Board RE, Ellison G, Orr MCM, Detection of BRAF mutations in the tumor and serum of patients enrolled in the AZD6244 (ARRY-142886) advanced melanoma phase II study. Br J Cancer 2009;101(10):1724-30
   Google Scholar
• Banerji U, Camidge DR, Verheul HMW, The First-in-Human Study of the Hydrogen Sulfate (Hyd-Sulfate) Capsule of the MEK1/2 Inhibitor AZD6244 (ARRY-142886): a Phase I open-label multicenter trial in patients with advanced cancer. Clin Cancer Res 2010;16(5):1613-23
   PubMed Web of Science ®Google Scholar
• Desar IME, Bovenschen HJ, Timmer-Bonte AJNH, Case studies showing clinical signs and management of cutaneous toxicity of the MEK1/2 inhibitor AZD6244 (ARRY-142886) in patients with solid tumors. Acta Oncol 2010; 49(1):110-13
   Google Scholar
• Board RE, Ellison G, Orr MCM, Detection of BRAF mutations in the tumor and serum of patients enrolled in the AZD6244 (ARRY-142886) advanced melanoma phase II study. Br J Cancer 2009;101(10):1724-30
   Google Scholar
• Hainsworth JD, Cebotaru CL, Kanarev V, A phase II, open-label, randomized study to assess the efficacy and safety of AZD6244 (ARRY-142886) versus pemetrexed in patients with non-small cell lung cancer who have failed one or two prior chemotherapeutic regimens. J Thorac Oncol 2010;5(10):1630-6
   Google Scholar
• AstraZeneca. Antitumor combination comprising a MEK inhibitor and an Aurora kinase inhibitor 188. WO2009074827; 2009
   Google Scholar
• AstraZeneca. Combination therapy comprising AZD2171 and AZD6244 or MEK - Inhibitor II. WO2008125820; 2008
   Google Scholar
• AstraZeneca. Combination of a MEK inhibitor and a b-Raf inhibitor for the treatment of cancer WO2008120004; 2008
   Google Scholar
• AstraZeneca. Combination of an MEK inhibitor and the Src kinase inhibitor AZD0530 for use in the treatment of cancer. WO2008078086; 2008
   Google Scholar
• Merck Sharp & Dohme. Therapeutic combination of MK-2206 and AZD-6244 for treating cancer. WO 2010138377; 2010
   Google Scholar
• Ucb Pharma. Thienopyridine derivatives as MEK inhibitors and their preparation, pharmaceutical compositions and use in the treatment of diseases WO2009153554; 2009
   Google Scholar
• Ucb Pharma. Preparation of fused thiophene derivatives as MEK inhibitors. WO2009093013; 2009
   Google Scholar
• Ucb Pharma. Thieno-pyridine derivatives as MEK inhibitors. WO2009093008; 2009
   Google Scholar
• Ucb Pharma. Fused tricyclic thiophene derivatives and their pharmaceutical compositions as inhibitors of MEK enzymes useful in the treatment of diseases and preparation thereof. WO2009093009; 2009
   Google Scholar
• Ucb Pharma. Preparation of thieno-pyridine derivatives as MEK inhibitors. WO2009013462; 2009
   Google Scholar
• Ucb Pharma. Fused thiophene derivatives as MEK inhibitors and their preparation, pharmaceutical compositions and use in the treatment of inflammatory, autoimmune, cardiovascular, proliferative and nociceptive conditions. WO2008020206; 2008
   Google Scholar
• Ardea Biosciences. Preparation of dihydropyridyl sulfonamides and dihydropyridyl sulfamides as MEK inhibitors. WO2010108652; 2010
   Google Scholar
• Ardea Biosciences. Pharmaceutical combinations comprising RDEA119/Bay 869766 for the treatment of specific cancers. WO2010105110; 2010
   Google Scholar
• Ardea Biosciences. Use of (S)-N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide or a pharmaceutically acceptable salt thereof for treatment of pancreatic cancer. WO2010105082; 2010
   Google Scholar
• Ardea Biosciences. Preparation of phenylaminophenylsulfonamides for treatment of cancer and inflammatory disease. WO2009129246; 2009
   Google Scholar
• Ardea Biosciences. Combinations of MEK inhibitors and Raf kinase inhibitors and uses thereof. WO2009018238; 2009
   Google Scholar
• Ardea Biosciences. Preparation of N-[2-(arylamino)aryl] sulfonamide compounds as MEK kinase inhibitors. WO2009018233; 2009
   Google Scholar
• Ardea Biosciences. N-Heteroarylsulfonamide derivatives as MEK inhibitors and their preparation, pharmaceutical compositions and use in the treatment of hyperproliferative diseases. WO2008089459; 2008
   Google Scholar
• Ardea Biosciences. Inhibitors of MEK. US20080255133A1; 2008
   Google Scholar
• Ardea Biosciences. Preparation of N-(arylamino)-sulfonamide inhibitors of MEK. US20080058340; 2008
   Google Scholar
• Iverson C, Larson G, Lai C, RDEA119/ BAY869766 : A potent, selective, allosteric inhibitor of MEK1/2 for the treatment of cancer. Cancer Res 2009;69(17):6839-47
   PubMed Web of Science ®Google Scholar
• Chang Q, Chapman MS, Miner JN, Antitumour activity of a potent MEK inhibitor RDEA119/BAY 869766 combined with rapamycin in human orthotopic primary pancreatic cancer xenografts. BMC Cancer 2010;10:515
   PubMed Web of Science ®Google Scholar
• Exelixis Pharmaceuticals. Preparation of N-acylazetidine MEK inhibitors and 4-aryl-2-aminopyrimidine or 4-aryl-2-aminoalkylpyrimidine JAK-2 inhibitors and their combinations useful for treating neoplasm. WO2008124085; 2008
   Google Scholar
• Exelixis Pharmaceuticals. N-Acylazetidine derivatives as MEK inhibitors and their preparation, pharmaceutical compositions and use in the treatment of cancer. WO2008076415; 2008
   Google Scholar
• Exelixis Pharmaceuticals. Preparation of azetidine MEK kinase inhibitors and pyridopyrimidine and quinoxaline and analog PI3K inhibitors and methods of using MEK inhibitors in combination with PI3K inhibitors for the treatment of proliferative diseases, especially cancer. WO2008021389; 2008
   Google Scholar
• Bayer Schering. Preparation of substituted amido phenoxybenzamides for treating hyperproliferative and/or angiogenesis disorders. WO2010051935; 2010
   Google Scholar
• Bayer Schering. Preparation of substituted sulfonamido phenoxybenzamides for treating hyperproliferative and/or angiogenesis disorders. WO2010051933; 2010
   Google Scholar
• Bayer Schering. Preparation of substituted phenoxybenzamides as MEK inhibitors. WO2009129938; 2009
   Google Scholar
• Hoffmann-La Roche. Preparation of substituted hydantoins as MEK inhibitors. WO2009021887; 2009
   Google Scholar
• Hoffmann-La Roche. Combination of erlotinib and MEK inhibitors for inhibiting proliferation of tumor cells. WO2008101840; 2008
   Google Scholar
• Novartis. Preparation of phenylaminotetrahydroindolizine derivatives and analogs for use as MEK inhibitors. US20090275606; 2009
   Google Scholar
• Takeda Pharmaceuticals. Preparation of naphthyridinediones as MAPK/ERK kinase inhibitors and methods of use thereof. US20090246198; 2009
   Google Scholar
• Takeda Pharmaceuticals. Preparation of pyrroles and imidazoles as MAPK/ERK kinase inhibitors. WO2008055236; 2008
   Google Scholar
• Genentech, Inc. Preparation of indazole and benzo[d]isothiazole derivatives as MEK kinase inhibitors. WO2010003025; 2010
   Google Scholar
• Genentech, Inc. Preparation of isoindolone derivatives as MEK kinase inhibitors. WO2010003022; 2010
   Google Scholar
• Genentech, Inc. Preparation of aminoazaindolecarboxamides as MEK kinase inhibitors. WO2008067481; 2008
   Google Scholar
• Genentech, Inc. Azabenzothiophene derivatives as MEK kinase inhibitors and their preparation, pharmaceutical compositions and use in the treatment of cancer and inflammation. WO2008024724; 2008
   Google Scholar
• Genentech, Inc. Preparation of azabenzofuranyl compounds as MEK kinase inhibitors. WO2008024725; 2008
   Google Scholar
• Chemizon (Beijing), Ltd. Novel 6-arylamino pyridone sulfonamides and 6-arylamino pyrazinone sulfonamides as Mek inhibitors. WO2010145197; 2010
   Google Scholar