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Page 1
The Discovery of ( S)-1-(6-(3-((4-(1-(Cyclopropanecarbonyl)piperidin-4-yl)-2-methylphenyl)amino)-2,3-dihydro-1 H-inden-4-yl)pyridin-2-yl)-5-methyl-1 H-pyrazole-4-carboxylic Acid, a Soluble Guanylate Cyclase Activator Specifically Designed for Topical Ocular Delivery as a Therapy for Glaucoma.
Ehara T, Adams CM, Bevan D, Ji N, Meredith EL, Belanger DB, Powers J, Kato M, Solovay C, Liu D, Capparelli M, Bolduc P, Grob JE, Daniels MH, Ferrara L, Yang L, Li B, Towler CS, Stacy RC, Prasanna G, Mogi M. Ehara T, et al. J Med Chem. 2018 Mar 22;61(6):2552-2570. doi: 10.1021/acs.jmedchem.8b00007. Epub 2018 Mar 2. J Med Chem. 2018. PMID: 29498522
Discovery of 4-((2S,4S)-4-Ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoic Acid (LNP023), a Factor B Inhibitor Specifically Designed To Be Applicable to Treating a Diverse Array of Complement Mediated Diseases.
Mainolfi N, Ehara T, Karki RG, Anderson K, Mac Sweeney A, Liao SM, Argikar UA, Jendza K, Zhang C, Powers J, Klosowski DW, Crowley M, Kawanami T, Ding J, April M, Forster C, Serrano-Wu M, Capparelli M, Ramqaj R, Solovay C, Cumin F, Smith TM, Ferrara L, Lee W, Long D, Prentiss M, De Erkenez A, Yang L, Liu F, Sellner H, Sirockin F, Valeur E, Erbel P, Ostermeier D, Ramage P, Gerhartz B, Schubart A, Flohr S, Gradoux N, Feifel R, Vogg B, Wiesmann C, Maibaum J, Eder J, Sedrani R, Harrison RA, Mogi M, Jaffee BD, Adams CM. Mainolfi N, et al. Among authors: ehara t. J Med Chem. 2020 Jun 11;63(11):5697-5722. doi: 10.1021/acs.jmedchem.9b01870. Epub 2020 Feb 19. J Med Chem. 2020. PMID: 32073845
A Novel Selective Soluble Guanylate Cyclase Activator, MGV354, Lowers Intraocular Pressure in Preclinical Models, Following Topical Ocular Dosing.
Prasanna G, Ferrara L, Adams C, Ehara T, Li B, Yang L, Xiang C, Ng CTH, Kim S, Towler C, Topley T, McAllister C, Ghosh M, Newton R, Stacy R, Rice DS, Mogi M. Prasanna G, et al. Among authors: ehara t. Invest Ophthalmol Vis Sci. 2018 Apr 1;59(5):1704-1716. doi: 10.1167/iovs.18-23772. Invest Ophthalmol Vis Sci. 2018. PMID: 29610853
Small-molecule factor B inhibitor for the treatment of complement-mediated diseases.
Schubart A, Anderson K, Mainolfi N, Sellner H, Ehara T, Adams CM, Mac Sweeney A, Liao SM, Crowley M, Littlewood-Evans A, Sarret S, Wieczorek G, Perrot L, Dubost V, Flandre T, Zhang Y, Smith RJH, Risitano AM, Karki RG, Zhang C, Valeur E, Sirockin F, Gerhartz B, Erbel P, Hughes N, Smith TM, Cumin F, Argikar UA, Haraldsson B, Mogi M, Sedrani R, Wiesmann C, Jaffee B, Maibaum J, Flohr S, Harrison R, Eder J. Schubart A, et al. Among authors: ehara t. Proc Natl Acad Sci U S A. 2019 Apr 16;116(16):7926-7931. doi: 10.1073/pnas.1820892116. Epub 2019 Mar 29. Proc Natl Acad Sci U S A. 2019. PMID: 30926668 Free PMC article.
Discovery of orally bioavailable cathepsin S inhibitors for the reversal of neuropathic pain.
Irie O, Kosaka T, Ehara T, Yokokawa F, Kanazawa T, Hirao H, Iwasaki A, Sakaki J, Teno N, Hitomi Y, Iwasaki G, Fukaya H, Nonomura K, Tanabe K, Koizumi S, Uchiyama N, Bevan SJ, Malcangio M, Gentry C, Fox AJ, Yaqoob M, Culshaw AJ, Allan Hallett. Irie O, et al. Among authors: ehara t. J Med Chem. 2008 Sep 25;51(18):5502-5. doi: 10.1021/jm800839j. J Med Chem. 2008. PMID: 18754655
Overcoming hERG issues for brain-penetrating cathepsin S inhibitors: 2-cyanopyrimidines. Part 2.
Irie O, Kosaka T, Kishida M, Sakaki J, Masuya K, Konishi K, Yokokawa F, Ehara T, Iwasaki A, Iwaki Y, Hitomi Y, Toyao A, Gunji H, Teno N, Iwasaki G, Hirao H, Kanazawa T, Tanabe K, Hiestand PC, Malcangio M, Fox AJ, Bevan SJ, Yaqoob M, Culshaw AJ, Hart TW, Hallett A. Irie O, et al. Among authors: ehara t. Bioorg Med Chem Lett. 2008 Oct 1;18(19):5280-4. doi: 10.1016/j.bmcl.2008.08.067. Epub 2008 Aug 22. Bioorg Med Chem Lett. 2008. PMID: 18783943
4-Amino-2-cyanopyrimidines: novel scaffold for nonpeptidic cathepsin S inhibitors.
Irie O, Yokokawa F, Ehara T, Iwasaki A, Iwaki Y, Hitomi Y, Konishi K, Kishida M, Toyao A, Masuya K, Gunji H, Sakaki J, Iwasaki G, Hirao H, Kanazawa T, Tanabe K, Kosaka T, Hart TW, Hallett A. Irie O, et al. Among authors: ehara t. Bioorg Med Chem Lett. 2008 Aug 15;18(16):4642-6. doi: 10.1016/j.bmcl.2008.07.011. Epub 2008 Jul 10. Bioorg Med Chem Lett. 2008. PMID: 18662880
Effect of cathepsin K inhibitors on bone resorption.
Teno N, Masuya K, Ehara T, Kosaka T, Miyake T, Irie O, Hitomi Y, Matsuura N, Umemura I, Iwasaki G, Fukaya H, Toriyama K, Uchiyama N, Nonomura K, Sugiyama I, Kometani M. Teno N, et al. Among authors: ehara t. J Med Chem. 2008 Sep 11;51(17):5459-62. doi: 10.1021/jm800626a. Epub 2008 Aug 16. J Med Chem. 2008. PMID: 18707091
Discovery of selective and nonpeptidic cathepsin S inhibitors.
Irie O, Ehara T, Iwasaki A, Yokokawa F, Sakaki J, Hirao H, Kanazawa T, Teno N, Horiuchi M, Umemura I, Gunji H, Masuya K, Hitomi Y, Iwasaki G, Nonomura K, Tanabe K, Fukaya H, Kosaka T, Snell CR, Hallett A. Irie O, et al. Among authors: ehara t. Bioorg Med Chem Lett. 2008 Jul 15;18(14):3959-62. doi: 10.1016/j.bmcl.2008.06.009. Epub 2008 Jun 10. Bioorg Med Chem Lett. 2008. PMID: 18572405
238 results