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Page 1
Discovery of (S)-N-[2-[1-(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl] acetamide (apremilast), a potent and orally active phosphodiesterase 4 and tumor necrosis factor-alpha inhibitor.
Man HW, Schafer P, Wong LM, Patterson RT, Corral LG, Raymon H, Blease K, Leisten J, Shirley MA, Tang Y, Babusis DM, Chen R, Stirling D, Muller GW. Man HW, et al. Among authors: raymon h. J Med Chem. 2009 Mar 26;52(6):1522-4. doi: 10.1021/jm900210d. J Med Chem. 2009. PMID: 19256507
Discovery of CC-930, an orally active anti-fibrotic JNK inhibitor.
Plantevin Krenitsky V, Nadolny L, Delgado M, Ayala L, Clareen SS, Hilgraf R, Albers R, Hegde S, D'Sidocky N, Sapienza J, Wright J, McCarrick M, Bahmanyar S, Chamberlain P, Delker SL, Muir J, Giegel D, Xu L, Celeridad M, Lachowitzer J, Bennett B, Moghaddam M, Khatsenko O, Katz J, Fan R, Bai A, Tang Y, Shirley MA, Benish B, Bodine T, Blease K, Raymon H, Cathers BE, Satoh Y. Plantevin Krenitsky V, et al. Among authors: raymon h. Bioorg Med Chem Lett. 2012 Feb 1;22(3):1433-8. doi: 10.1016/j.bmcl.2011.12.027. Epub 2011 Dec 10. Bioorg Med Chem Lett. 2012. PMID: 22244937
Aminopurine based JNK inhibitors for the prevention of ischemia reperfusion injury.
Krenitsky VP, Delgado M, Nadolny L, Sahasrabudhe K, Ayala L, Clareen SS, Hilgraf R, Albers R, Kois A, Hughes K, Wright J, Nowakowski J, Sudbeck E, Ghosh S, Bahmanyar S, Chamberlain P, Muir J, Cathers BE, Giegel D, Xu L, Celeridad M, Moghaddam M, Khatsenko O, Omholt P, Katz J, Pai S, Fan R, Tang Y, Shirley MA, Benish B, Blease K, Raymon H, Bhagwat S, Henderson I, Cole AG, Bennett B, Satoh Y. Krenitsky VP, et al. Among authors: raymon h. Bioorg Med Chem Lett. 2012 Feb 1;22(3):1427-32. doi: 10.1016/j.bmcl.2011.12.028. Epub 2011 Dec 11. Bioorg Med Chem Lett. 2012. PMID: 22226655
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.
Mortensen DS, Perrin-Ninkovic SM, Shevlin G, Zhao J, Packard G, Bahmanyar S, Correa M, Elsner J, Harris R, Lee BG, Papa P, Parnes JS, Riggs JR, Sapienza J, Tehrani L, Whitefield B, Apuy J, Bisonette RR, Gamez JC, Hickman M, Khambatta G, Leisten J, Peng SX, Richardson SJ, Cathers BE, Canan SS, Moghaddam MF, Raymon HK, Worland P, Narla RK, Fultz KE, Sankar S. Mortensen DS, et al. Among authors: raymon hk. J Med Chem. 2015 Jul 9;58(13):5323-33. doi: 10.1021/acs.jmedchem.5b00626. Epub 2015 Jun 26. J Med Chem. 2015. PMID: 26083478
Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115.
Mortensen DS, Perrin-Ninkovic SM, Shevlin G, Elsner J, Zhao J, Whitefield B, Tehrani L, Sapienza J, Riggs JR, Parnes JS, Papa P, Packard G, Lee BG, Harris R, Correa M, Bahmanyar S, Richardson SJ, Peng SX, Leisten J, Khambatta G, Hickman M, Gamez JC, Bisonette RR, Apuy J, Cathers BE, Canan SS, Moghaddam MF, Raymon HK, Worland P, Narla RK, Fultz KE, Sankar S. Mortensen DS, et al. Among authors: raymon hk. J Med Chem. 2015 Jul 23;58(14):5599-608. doi: 10.1021/acs.jmedchem.5b00627. Epub 2015 Jul 8. J Med Chem. 2015. PMID: 26102506
CC-223, a Potent and Selective Inhibitor of mTOR Kinase: In Vitro and In Vivo Characterization.
Mortensen DS, Fultz KE, Xu S, Xu W, Packard G, Khambatta G, Gamez JC, Leisten J, Zhao J, Apuy J, Ghoreishi K, Hickman M, Narla RK, Bissonette R, Richardson S, Peng SX, Perrin-Ninkovic S, Tran T, Shi T, Yang WQ, Tong Z, Cathers BE, Moghaddam MF, Canan SS, Worland P, Sankar S, Raymon HK. Mortensen DS, et al. Mol Cancer Ther. 2015 Jun;14(6):1295-305. doi: 10.1158/1535-7163.MCT-14-1052. Epub 2015 Apr 8. Mol Cancer Ther. 2015. PMID: 25855786
CC-122, a pleiotropic pathway modifier, mimics an interferon response and has antitumor activity in DLBCL.
Hagner PR, Man HW, Fontanillo C, Wang M, Couto S, Breider M, Bjorklund C, Havens CG, Lu G, Rychak E, Raymon H, Narla RK, Barnes L, Khambatta G, Chiu H, Kosek J, Kang J, Amantangelo MD, Waldman M, Lopez-Girona A, Cai T, Pourdehnad M, Trotter M, Daniel TO, Schafer PH, Klippel A, Thakurta A, Chopra R, Gandhi AK. Hagner PR, et al. Among authors: raymon h. Blood. 2015 Aug 6;126(6):779-89. doi: 10.1182/blood-2015-02-628669. Epub 2015 May 22. Blood. 2015. PMID: 26002965 Free PMC article. Clinical Trial.
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