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Page 1
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 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 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
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
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
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 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.
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.
Carbamate and N-Pyrimidine Mitigate Amide Hydrolysis: Structure-Based Drug Design of Tetrahydroquinoline IDO1 Inhibitors.
Li D, Deng Y, Achab A, Bharathan I, Hopkins BA, Yu W, Zhang H, Sanyal S, Pu Q, Zhou H, Liu K, Lim J, Fradera X, Lesburg CA, Lammens A, Martinot TA, Cohen RD, Doty AC, Ferguson H, Nickbarg EB, Cheng M, Spacciapoli P, 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 KM, Vincent S, Sciammetta N, Pasternak A, Bennett DJ, Han Y. Li D, et al. Among authors: knemeyer i. ACS Med Chem Lett. 2021 Feb 26;12(3):389-396. doi: 10.1021/acsmedchemlett.0c00525. eCollection 2021 Mar 11. ACS Med Chem Lett. 2021. PMID: 33738066 Free PMC article.
25 results