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BMS-986163, a Negative Allosteric Modulator of GluN2B with Potential Utility in Major Depressive Disorder.
Marcin LR, Warrier J, Thangathirupathy S, Shi J, Karageorge GN, Pearce BC, Ng A, Park H, Kempson J, Li J, Zhang H, Mathur A, Reddy AB, Nagaraju G, Tonukunuru G, Gupta GVRKM, Kamble M, Mannoori R, Cheruku S, Jogi S, Gulia J, Bastia T, Sanmathi C, Aher J, Kallem R, Srikumar BN, Vijaya KK, Naidu PS, Paschapur M, Kalidindi N, Vikramadithyan R, Ramarao M, Denton R, Molski T, Shields E, Subramanian M, Zhuo X, Nophsker M, Simmermacher J, Sinz M, Albright C, Bristow LJ, Islam I, Bronson JJ, Olson RE, King D, Thompson LA, Macor JE. Marcin LR, et al. Among authors: sinz m. ACS Med Chem Lett. 2018 Apr 13;9(5):472-477. doi: 10.1021/acsmedchemlett.8b00080. eCollection 2018 May 10. ACS Med Chem Lett. 2018. PMID: 29795762 Free PMC article.
Preclinical Characterization of (R)-3-((3S,4S)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl)-1-(4-methylbenzyl)pyrrolidin-2-one (BMS-986169), a Novel, Intravenous, Glutamate N-Methyl-d-Aspartate 2B Receptor Negative Allosteric Modulator with Potential in Major Depressive Disorder.
Bristow LJ, Gulia J, Weed MR, Srikumar BN, Li YW, Graef JD, Naidu PS, Sanmathi C, Aher J, Bastia T, Paschapur M, Kalidindi N, Kumar KV, Molski T, Pieschl R, Fernandes A, Brown JM, Sivarao DV, Newberry K, Bookbinder M, Polino J, Keavy D, Newton A, Shields E, Simmermacher J, Kempson J, Li J, Zhang H, Mathur A, Kallem RR, Sinha M, Ramarao M, Vikramadithyan RK, Thangathirupathy S, Warrier J, Islam I, Bronson JJ, Olson RE, Macor JE, Albright CF, King D, Thompson LA, Marcin LR, Sinz M. Bristow LJ, et al. Among authors: sinz m. J Pharmacol Exp Ther. 2017 Dec;363(3):377-393. doi: 10.1124/jpet.117.242784. Epub 2017 Sep 27. J Pharmacol Exp Ther. 2017. PMID: 28954811
Design and synthesis of 4-heteroaryl 1,2,3,4-tetrahydroisoquinolines as triple reuptake inhibitors.
Liu S, Zha C, Nacro K, Hu M, Cui W, Yang YL, Bhatt U, Sambandam A, Isherwood M, Yet L, Herr MT, Ebeltoft S, Hassler C, Fleming L, Pechulis AD, Payen-Fornicola A, Holman N, Milanowski D, Cotterill I, Mozhaev V, Khmelnitsky Y, Guzzo PR, Sargent BJ, Molino BF, Olson R, King D, Lelas S, Li YW, Johnson K, Molski T, Orie A, Ng A, Haskell R, Clarke W, Bertekap R, O'Connell J, Lodge N, Sinz M, Adams S, Zaczek R, Macor JE. Liu S, et al. Among authors: sinz m. ACS Med Chem Lett. 2014 May 13;5(7):760-5. doi: 10.1021/ml500053b. eCollection 2014 Jul 10. ACS Med Chem Lett. 2014. PMID: 25050161 Free PMC article.
Discovery of a Hepatitis C Virus NS5B Replicase Palm Site Allosteric Inhibitor (BMS-929075) Advanced to Phase 1 Clinical Studies.
Yeung KS, Beno BR, Parcella K, Bender JA, Grant-Young KA, Nickel A, Gunaga P, Anjanappa P, Bora RO, Selvakumar K, Rigat K, Wang YK, Liu M, Lemm J, Mosure K, Sheriff S, Wan C, Witmer M, Kish K, Hanumegowda U, Zhuo X, Shu YZ, Parker D, Haskell R, Ng A, Gao Q, Colston E, Raybon J, Grasela DM, Santone K, Gao M, Meanwell NA, Sinz M, Soars MG, Knipe JO, Roberts SB, Kadow JF. Yeung KS, et al. Among authors: sinz m. J Med Chem. 2017 May 25;60(10):4369-4385. doi: 10.1021/acs.jmedchem.7b00328. Epub 2017 May 4. J Med Chem. 2017. PMID: 28430437 Clinical Trial.
Discovery of a Potent Acyclic, Tripeptidic, Acyl Sulfonamide Inhibitor of Hepatitis C Virus NS3 Protease as a Back-up to Asunaprevir with the Potential for Once-Daily Dosing.
Sun LQ, Mull E, Zheng B, D'Andrea S, Zhao Q, Wang AX, Sin N, Venables BL, Sit SY, Chen Y, Chen J, Cocuzza A, Bilder DM, Mathur A, Rampulla R, Chen BC, Palani T, Ganesan S, Arunachalam PN, Falk P, Levine S, Chen C, Friborg J, Yu F, Hernandez D, Sheaffer AK, Knipe JO, Han YH, Schartman R, Donoso M, Mosure K, Sinz MW, Zvyaga T, Rajamani R, Kish K, Tredup J, Klei HE, Gao Q, Ng A, Mueller L, Grasela DM, Adams S, Loy J, Levesque PC, Sun H, Shi H, Sun L, Warner W, Li D, Zhu J, Wang YK, Fang H, Cockett MI, Meanwell NA, McPhee F, Scola PM. Sun LQ, et al. Among authors: sinz mw. J Med Chem. 2016 Sep 8;59(17):8042-60. doi: 10.1021/acs.jmedchem.6b00821. Epub 2016 Aug 26. J Med Chem. 2016. PMID: 27564532
Development of BET Inhibitors as Potential Treatments for Cancer: Optimization of Pharmacokinetic Properties.
Hill MD, Fang H, Norris D, Delucca GV, Huang H, DeBenedetto M, Quesnelle C, Schmitz WD, Tokarski JS, Sheriff S, Yan C, Fanslau C, Haarhoff Z, Huang C, Kramer M, Madari S, Menard K, Monereau L, Morrison J, Raghavan N, Shields EE, Simmermacher-Mayer J, Sinz M, Tye CK, Westhouse R, Xie C, Zhang H, Zhang L, Zvyaga T, Lee F, Gavai AV, Degnan AP. Hill MD, et al. Among authors: sinz m. ACS Med Chem Lett. 2022 Jul 5;13(7):1165-1171. doi: 10.1021/acsmedchemlett.2c00219. eCollection 2022 Jul 14. ACS Med Chem Lett. 2022. PMID: 35859878 Free PMC article.
89 results