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26 results

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Page 1
Discovery of MK-1454: A Potent Cyclic Dinucleotide Stimulator of Interferon Genes Agonist for the Treatment of Cancer.
Chang W, Altman MD, Lesburg CA, Perera SA, Piesvaux JA, Schroeder GK, Wyss DF, Cemerski S, Chen Y, DiNunzio E, Haidle AM, Ho T, Kariv I, Knemeyer I, Kopinja JE, Lacey BM, Laskey J, Lim J, Long BJ, Ma Y, Maddess ML, Pan BS, Presland JP, Spooner E, Steinhuebel D, Truong Q, Zhang Z, Fu J, Addona GH, Northrup AB, Parmee E, Tata JR, Bennett DJ, Cumming JN, Siu T, Trotter BW. Chang W, et al. Among authors: knemeyer i. J Med Chem. 2022 Apr 14;65(7):5675-5689. doi: 10.1021/acs.jmedchem.1c02197. Epub 2022 Mar 25. J Med Chem. 2022. PMID: 35332774
Definitive Metabolite Identification Coupled with Automated Ligand Identification System (ALIS) Technology: A Novel Approach to Uncover Structure-Activity Relationships and Guide Drug Design in a Factor IXa Inhibitor Program.
Zhang T, Liu Y, Yang X, Martin GE, Yao H, Shang J, Bugianesi RM, Ellsworth KP, Sonatore LM, Nizner P, Sherer EC, Hill SE, Knemeyer IW, Geissler WM, Dandliker PJ, Helmy R, Wood HB. Zhang T, et al. J Med Chem. 2016 Mar 10;59(5):1818-29. doi: 10.1021/acs.jmedchem.5b01293. Epub 2016 Feb 22. J Med Chem. 2016. PMID: 26871940
Discovery of 8-Amino-imidazo[1,5-a]pyrazines as Reversible BTK Inhibitors for the Treatment of Rheumatoid Arthritis.
Liu J, Guiadeen D, Krikorian A, Gao X, Wang J, Boga SB, Alhassan AB, Yu Y, Vaccaro H, Liu S, Yang C, Wu H, Cooper A, de Man J, Kaptein A, Maloney K, Hornak V, Gao YD, Fischmann TO, Raaijmakers H, Vu-Pham D, Presland J, Mansueto M, Xu Z, Leccese E, Zhang-Hoover J, Knemeyer I, Garlisi CG, Bays N, Stivers P, Brandish PE, Hicks A, Kim R, Kozlowski JA. Liu J, et al. Among authors: knemeyer i. ACS Med Chem Lett. 2015 Dec 19;7(2):198-203. doi: 10.1021/acsmedchemlett.5b00463. eCollection 2016 Feb 11. ACS Med Chem Lett. 2015. PMID: 26985298 Free PMC article.
Discovery of Spirocyclic Aldosterone Synthase Inhibitors as Potential Treatments for Resistant Hypertension.
Petrilli WL, Hoyt SB, London C, McMasters D, Verras A, Struthers M, Cully D, Wisniewski T, Ren N, Bopp C, Sok A, Chen Q, Li Y, Tung E, Tang W, Salituro G, Knemeyer I, Karanam B, Clemas J, Zhou G, Gibson J, Shipley CA, MacNeil DJ, Duffy R, Tata JR, Ujjainwalla F, Ali A, Xiong Y. Petrilli WL, et al. Among authors: knemeyer i. ACS Med Chem Lett. 2016 Nov 22;8(1):128-132. doi: 10.1021/acsmedchemlett.6b00455. eCollection 2017 Jan 12. ACS Med Chem Lett. 2016. PMID: 28105288 Free PMC article.
Discovery of novel BTK inhibitors with carboxylic acids.
Gao X, Wang J, Liu J, Guiadeen D, Krikorian A, Boga SB, Alhassan AB, Selyutin O, Yu W, Yu Y, Anand R, Liu S, Yang C, Wu H, Cai J, Cooper A, Zhu H, Maloney K, Gao YD, Fischmann TO, Presland J, Mansueto M, Xu Z, Leccese E, Zhang-Hoover J, Knemeyer I, Garlisi CG, Bays N, Stivers P, Brandish PE, Hicks A, Kim R, Kozlowski JA. Gao X, et al. Among authors: knemeyer i. Bioorg Med Chem Lett. 2017 Mar 15;27(6):1471-1477. doi: 10.1016/j.bmcl.2016.11.079. Epub 2016 Nov 25. Bioorg Med Chem Lett. 2017. PMID: 28254166
Discovery of 3-morpholino-imidazole[1,5-a]pyrazine BTK inhibitors for rheumatoid arthritis.
Boga SB, Alhassan AB, Liu J, Guiadeen D, Krikorian A, Gao X, Wang J, Yu Y, Anand R, Liu S, Yang C, Wu H, Cai J, Zhu H, Desai J, Maloney K, Gao YD, Fischmann TO, Presland J, Mansueto M, Xu Z, Leccese E, Knemeyer I, Garlisi CG, Bays N, Stivers P, Brandish PE, Hicks A, Cooper A, Kim RM, Kozlowski JA. Boga SB, et al. Among authors: knemeyer i. Bioorg Med Chem Lett. 2017 Aug 15;27(16):3939-3943. doi: 10.1016/j.bmcl.2017.03.040. Epub 2017 Mar 18. Bioorg Med Chem Lett. 2017. PMID: 28720503
Discovery of Amino-cyclobutarene-derived Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitors for Cancer Immunotherapy.
Zhang H, Liu K, Pu Q, Achab A, Ardolino MJ, Cheng M, Deng Y, Doty AC, Ferguson H, Fradera X, Knemeyer I, Kurukulasuriya R, Lam YH, Lesburg CA, Martinot TA, McGowan MA, Miller JR, Otte K, Biju PJ, Sciammetta N, Solban N, Yu W, Zhou H, Wang X, Bennett DJ, Han Y. Zhang H, et al. Among authors: knemeyer i. ACS Med Chem Lett. 2019 Sep 18;10(11):1530-1536. doi: 10.1021/acsmedchemlett.9b00344. eCollection 2019 Nov 14. ACS Med Chem Lett. 2019. PMID: 31749906 Free PMC article.
Strategic Incorporation of Polarity in Heme-Displacing Inhibitors of Indoleamine-2,3-dioxygenase-1 (IDO1).
White C, McGowan MA, Zhou H, Sciammetta N, Fradera X, Lim J, Joshi EM, Andrews C, Nickbarg EB, Cowley P, Trewick S, Augustin M, von Köenig K, Lesburg CA, Otte K, Knemeyer I, Woo H, Yu W, Cheng M, Spacciapoli P, Geda P, Song X, Smotrov N, Curran P, Heo MR, Abeywickrema P, Miller JR, Bennett DJ, Han Y. White C, et al. Among authors: knemeyer i. ACS Med Chem Lett. 2020 Mar 10;11(4):550-557. doi: 10.1021/acsmedchemlett.0c00010. eCollection 2020 Apr 9. ACS Med Chem Lett. 2020. PMID: 32292563 Free PMC article.
Potent, non-covalent reversible BTK inhibitors with 8-amino-imidazo[1,5-a]pyrazine core featuring 3-position bicyclic ring substitutes.
Liu J, Guiadeen D, Krikorian A, Gao X, Wang J, Babu Boga S, Alhassan AB, Yu W, Selyutin O, Yu Y, Anand R, Xu J, Kelly J, Duffy JL, Liu S, Yang C, Wu H, Cai J, Bennett C, Maloney KM, Tyagarajan S, Gao YD, Fischmann TO, Presland J, Mansueto M, Xu Z, Leccese E, Zhang-Hoover J, Knemeyer I, Garlisi CG, Stivers P, Brandish PE, Hicks A, Kim R, Kozlowski JA. Liu J, et al. Among authors: knemeyer i. Bioorg Med Chem Lett. 2020 Sep 1;30(17):127390. doi: 10.1016/j.bmcl.2020.127390. Epub 2020 Jul 11. Bioorg Med Chem Lett. 2020. PMID: 32738973
An orally available non-nucleotide STING agonist with antitumor activity.
Pan BS, Perera SA, Piesvaux JA, Presland JP, Schroeder GK, Cumming JN, Trotter BW, Altman MD, Buevich AV, Cash B, Cemerski S, Chang W, Chen Y, Dandliker PJ, Feng G, Haidle A, Henderson T, Jewell J, Kariv I, Knemeyer I, Kopinja J, Lacey BM, Laskey J, Lesburg CA, Liang R, Long BJ, Lu M, Ma Y, Minnihan EC, O'Donnell G, Otte R, Price L, Rakhilina L, Sauvagnat B, Sharma S, Tyagarajan S, Woo H, Wyss DF, Xu S, Bennett DJ, Addona GH. Pan BS, et al. Among authors: knemeyer i. Science. 2020 Aug 21;369(6506):eaba6098. doi: 10.1126/science.aba6098. Science. 2020. PMID: 32820094
26 results