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Page 1
Process Development of a Macrocyclic Peptide Inhibitor of PD-L1.
Mukherjee S, Rogers A, Creech G, Hang C, Ramirez A, Dummeldinger M, Brueggemeier S, Mapelli C, Zaretsky S, Huang M, Black R, Peddicord MB, Cuniere N, Kempson J, Pawluczyk J, Allen M, Parsons R, Sfouggatakis C. Mukherjee S, et al. Among authors: pawluczyk j. J Org Chem. 2024 May 17;89(10):6651-6663. doi: 10.1021/acs.joc.4c00430. Epub 2024 Apr 25. J Org Chem. 2024. PMID: 38663026
Challenges with the Synthesis of a Macrocyclic Thioether Peptide: From Milligram to Multigram Using Solid Phase Peptide Synthesis (SPPS).
Kempson J, Zhao R, Pawluczyk J, Wang B, Zhang H, Hou X, Allen MP, Wu DR, Li P, Yip S, Smith A, Traeger SC, Huang S, Cutrone J, Mukherjee S, Sfouggatakis C, Poss M, Scola PM, Meanwell NA, Carter PH, Mathur A. Kempson J, et al. Among authors: pawluczyk j. J Org Chem. 2024 May 17;89(10):6639-6650. doi: 10.1021/acs.joc.4c00429. Epub 2024 Apr 23. J Org Chem. 2024. PMID: 38651358
Discovery of (S)-1-((2',6-Bis(difluoromethyl)-[2,4'-bipyridin]-5-yl)oxy)-2,4-dimethylpentan-2-amine (BMS-986176/LX-9211): A Highly Selective, CNS Penetrable, and Orally Active Adaptor Protein-2 Associated Kinase 1 Inhibitor in Clinical Trials for the Treatment of Neuropathic Pain.
Luo G, Chen L, Kostich WA, Hamman B, Allen J, Easton A, Bourin C, Gulianello M, Lippy J, Nara S, Maishal TK, Thiyagarajan K, Jalagam P, Pattipati SN, Dandapani K, Dokania M, Vattikundala P, Sharma V, Elavazhagan S, Verma MK, Das ML, Wagh S, Balakrishnan A, Johnson BM, Santone KS, Thalody G, Denton R, Saminathan H, Holenarsipur VK, Kumar A, Rao A, Putlur SP, Sarvasiddhi SK, Shankar G, Louis JV, Ramarao M, Conway CM, Li YW, Pieschl R, Tian Y, Hong Y, Ditta J, Mathur A, Li J, Smith D, Pawluczyk J, Sun D, Yip S, Wu DR, Vetrichelvan M, Gupta A, Wilson A, Gopinathan S, Wason S, Bristow L, Albright CF, Bronson JJ, Macor JE, Dzierba CD. Luo G, et al. Among authors: pawluczyk j. J Med Chem. 2022 Mar 24;65(6):4457-4480. doi: 10.1021/acs.jmedchem.1c02131. Epub 2022 Mar 8. J Med Chem. 2022. PMID: 35257579
Long-Acting Tumor-Activated Prodrug of a TGFβR Inhibitor.
Zhang Y, Parrish KE, Tortolani DR, Poss MA, Huang A, Wan H, Purandare AV, Donnell AF, Kempson J, Hou X, Pawluczyk J, Yip S, Luk E, Raghavan N, Swanson J, Smalley J, Murtaza A, Yang Z, Augustine-Rauch K, Lombardo LJ, Borzilleri R. Zhang Y, et al. Among authors: pawluczyk j. J Med Chem. 2021 Nov 11;64(21):15787-15798. doi: 10.1021/acs.jmedchem.0c02043. Epub 2021 Oct 27. J Med Chem. 2021. PMID: 34704759
A Stereocontrolled Synthesis of a Phosphorothioate Cyclic Dinucleotide-Based STING Agonist.
Kempson J, Zhang H, Hou X, Cornelius L, Zhao R, Wang B, Hong Z, Oderinde MS, Pawluczyk J, Wu DR, Sun D, Li P, Yip S, Smith A, Caceres-Cortes J, Aulakh D, Sarjeant AA, Park PK, Harikrishnan LS, Qin LY, Dodd DS, Fink B, Vite G, Mathur A. Kempson J, et al. Among authors: pawluczyk j. J Org Chem. 2021 Jul 2;86(13):8851-8861. doi: 10.1021/acs.joc.1c00784. Epub 2021 Jun 14. J Org Chem. 2021. PMID: 34126006
Driving Potency with Rotationally Stable Atropisomers: Discovery of Pyridopyrimidinedione-Carbazole Inhibitors of BTK.
Srivastava AS, Ko S, Watterson SH, Pattoli MA, Skala S, Cheng L, Obermeier MT, Vickery R, Discenza LN, D'Arienzo CJ, Gillooly KM, Taylor TL, Pulicicchio C, McIntyre KW, Yip S, Li P, Sun D, Wu DR, Dai J, Wang C, Zhang Y, Wang B, Pawluczyk J, Kempson J, Zhao R, Hou X, Rampulla R, Mathur A, Galella MA, Salter-Cid L, Barrish JC, Carter PH, Fura A, Burke JR, Tino JA. Srivastava AS, et al. Among authors: pawluczyk j. ACS Med Chem Lett. 2020 Sep 16;11(11):2195-2203. doi: 10.1021/acsmedchemlett.0c00335. eCollection 2020 Nov 12. ACS Med Chem Lett. 2020. PMID: 33214829 Free PMC article.
Synthesis of 1-(tert-Butyl) 4-Methyl (1R,2S,4R)-2-Methylcyclohexane-1,4-dicarboxylate from Hagemann's tert-Butyl Ester for an Improved Synthesis of BMS-986251.
Cornelius LAM, Li J, Smith D, Krishnananthan S, Yip S, Wu DR, Pawluczyk J, Aulakh D, Sarjeant AA, Kempson J, Tino JA, Mathur A, Murali Dhar TG, Cherney RJ. Cornelius LAM, et al. Among authors: pawluczyk j. J Org Chem. 2020 Aug 21;85(16):10988-10993. doi: 10.1021/acs.joc.0c01169. Epub 2020 Aug 7. J Org Chem. 2020. PMID: 32687358
22 results