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Page 1
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 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 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
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
SAR towards indoline and 3-azaindoline classes of IDO1 inhibitors.
Yu W, Deng Y, Hopkins B, Huang X, Sloman D, Zhang H, Li D, McGowan MA, White C, Pu Q, Liu K, Fradera X, Lesburg CA, Martinot T, Doty A, Ferguson H, Nickbarg EB, Cheng M, Geda P, Song X, Smotrov N, Abeywickrema P, Andrews C, Chamberlin C, Mabrouk O, Curran P, Richards M, Saradjian P, Miller JR, Knemeyer I, Otte K, Vincent S, Sciammetta N, Bennett DJ, Han Y. Yu W, et al. Among authors: knemeyer i. Bioorg Med Chem Lett. 2021 Sep 1;47:128214. doi: 10.1016/j.bmcl.2021.128214. Epub 2021 Jun 21. Bioorg Med Chem Lett. 2021. PMID: 34166782
Discovery of IDO1 inhibitors containing a decahydroquinoline, decahydro-1,6-naphthyridine, or octahydro-1H-pyrrolo[3,2-c]pyridine scaffold.
Yu W, Deng Y, Sloman D, Li D, Liu K, Fradera X, Lesburg CA, Martinot T, Doty A, Ferguson H, Richard Miller J, Knemeyer I, Otte K, Vincent S, Sciammetta N, Jonathan Bennett D, Han Y. Yu W, et al. Among authors: knemeyer i. Bioorg Med Chem Lett. 2021 Oct 1;49:128314. doi: 10.1016/j.bmcl.2021.128314. Epub 2021 Aug 13. Bioorg Med Chem Lett. 2021. PMID: 34391891
Oxetane Promise Delivered: Discovery of Long-Acting IDO1 Inhibitors Suitable for Q3W Oral or Parenteral Dosing.
Li D, Sloman DL, Achab A, Zhou H, McGowan MA, White C, Gibeau C, Zhang H, Pu Q, Bharathan I, Hopkins B, Liu K, Ferguson H, Fradera X, Lesburg CA, Martinot TA, Qi J, Song ZJ, Yin J, Zhang H, Song L, Wan B, DAddio S, Solban N, Miller JR, Zamlynny B, Bass A, Freeland E, Ykoruk B, Hilliard C, Ferraro J, Zhai J, Knemeyer I, Otte KM, Vincent S, Sciammetta N, Pasternak A, Bennett DJ, Han Y. Li D, et al. Among authors: knemeyer i. J Med Chem. 2022 Apr 28;65(8):6001-6016. doi: 10.1021/acs.jmedchem.1c01670. Epub 2022 Mar 3. J Med Chem. 2022. PMID: 35239336
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 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
25 results