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Page 1
Invention of VH-937, a Potent HIV-1 Maturation Inhibitor with the Potential for Infrequent Oral Dosing in Humans.
Sit SY, Chen Y, Chen J, Venables BL, Swidorski JJ, Xu L, Sin N, Hartz RA, Lin Z, Zhang S, Li Z, Wu DR, Li P, Kempson J, Hou X, Shanmugam Y, Parker D, Jenkins S, Simmermacher J, Falk P, McAuliffe B, Cockett M, Hanumegowda U, Dicker I, Krystal M, Meanwell NA, Regueiro-Ren A. Sit SY, et al. Among authors: falk p. ACS Med Chem Lett. 2024 Oct 17;15(11):1997-2004. doi: 10.1021/acsmedchemlett.4c00419. eCollection 2024 Nov 14. ACS Med Chem Lett. 2024. PMID: 39563829
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: falk p. 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
Discovery and Preclinical Profiling of GSK3839919, a Potent HIV-1 Allosteric Integrase Inhibitor.
Parcella K, Wang T, Eastman K, Zhang Z, Yin Z, Patel M, Tu Y, Zheng BZ, Walker MA, Saulnier MG, Frennesson D, Bowsher M, Gillis E, Peese K, Belema M, Cianci C, Dicker IB, McAuliffe B, Ding B, Falk P, Simmermacher J, Parker DD, Sivaprakasam P, Kish K, Lewis H, Hanumegowda U, Jenkins S, Kadow JF, Krystal M, Meanwell NA, Naidu BN. Parcella K, et al. Among authors: falk p. ACS Med Chem Lett. 2022 May 9;13(6):972-980. doi: 10.1021/acsmedchemlett.2c00115. eCollection 2022 Jun 9. ACS Med Chem Lett. 2022. PMID: 35707159 Free PMC article.
Preclinical Profile of the HIV-1 Maturation Inhibitor VH3739937.
McAuliffe B, Falk P, Chen J, Chen Y, Sit SY, Swidorski J, Hartz RA, Xu L, Venables B, Sin N, Meanwell NA, Regueiro-Ren A, Wensel D, Hanumegowda U, Krystal M. McAuliffe B, et al. Among authors: falk p. Viruses. 2024 Sep 24;16(10):1508. doi: 10.3390/v16101508. Viruses. 2024. PMID: 39459843 Free PMC article.
Discovery and early clinical evaluation of BMS-605339, a potent and orally efficacious tripeptidic acylsulfonamide NS3 protease inhibitor for the treatment of hepatitis C virus infection.
Scola PM, Wang AX, Good AC, Sun LQ, Combrink KD, Campbell JA, Chen J, Tu Y, Sin N, Venables BL, Sit SY, Chen Y, Cocuzza A, Bilder DM, D'Andrea S, Zheng B, Hewawasam P, Ding M, Thuring J, Li J, Hernandez D, Yu F, Falk P, Zhai G, Sheaffer AK, Chen C, Lee MS, Barry D, Knipe JO, Li W, Han YH, Jenkins S, Gesenberg C, Gao Q, Sinz MW, Santone KS, Zvyaga T, Rajamani R, Klei HE, Colonno RJ, Grasela DM, Hughes E, Chien C, Adams S, Levesque PC, Li D, Zhu J, Meanwell NA, McPhee F. Scola PM, et al. Among authors: falk p. J Med Chem. 2014 Mar 13;57(5):1708-29. doi: 10.1021/jm401840s. Epub 2014 Feb 20. J Med Chem. 2014. PMID: 24555570
The discovery of asunaprevir (BMS-650032), an orally efficacious NS3 protease inhibitor for the treatment of hepatitis C virus infection.
Scola PM, Sun LQ, Wang AX, Chen J, Sin N, Venables BL, Sit SY, Chen Y, Cocuzza A, Bilder DM, D'Andrea SV, Zheng B, Hewawasam P, Tu Y, Friborg J, Falk P, Hernandez D, Levine S, Chen C, Yu F, Sheaffer AK, Zhai G, Barry D, Knipe JO, Han YH, Schartman R, Donoso M, Mosure K, Sinz MW, Zvyaga T, Good AC, Rajamani R, Kish K, Tredup J, Klei HE, Gao Q, Mueller L, Colonno RJ, Grasela DM, Adams SP, Loy J, Levesque PC, Sun H, Shi H, Sun L, Warner W, Li D, Zhu J, Meanwell NA, McPhee F. Scola PM, et al. Among authors: falk p. J Med Chem. 2014 Mar 13;57(5):1730-52. doi: 10.1021/jm500297k. Epub 2014 Mar 5. J Med Chem. 2014. PMID: 24564672
P3-P4 ureas and reverse carbamates as potent HCV NS3 protease inhibitors: Effective transposition of the P4 hydrogen bond donor.
Venables BL, Sin N, Wang AX, Sun LQ, Tu Y, Hernandez D, Sheaffer A, Lee M, Dunaj C, Zhai G, Barry D, Friborg J, Yu F, Knipe J, Sandquist J, Falk P, Parker D, Good AC, Rajamani R, McPhee F, Meanwell NA, Scola PM. Venables BL, et al. Among authors: falk p. Bioorg Med Chem Lett. 2018 Jun 1;28(10):1853-1859. doi: 10.1016/j.bmcl.2018.04.009. Epub 2018 Apr 5. Bioorg Med Chem Lett. 2018. PMID: 29650290
Scaffold modifications to the 4-(4,4-dimethylpiperidinyl) 2,6-dimethylpyridinyl class of HIV-1 allosteric integrase inhibitors.
Parcella K, Patel M, Tu Y, Eastman K, Peese K, Gillis E, Belema M, Dicker IB, McAuliffe B, Ding B, Falk P, Simmermacher J, Parker DD, Sivaprakasam P, Khan JA, Kish K, Lewis H, Hanumegowda U, Jenkins S, Kadow JF, Krystal M, Meanwell NA, Naidu BN. Parcella K, et al. Among authors: falk p. Bioorg Med Chem. 2022 Aug 1;67:116833. doi: 10.1016/j.bmc.2022.116833. Epub 2022 May 19. Bioorg Med Chem. 2022. PMID: 35605346
Potent Inhibitors of Hepatitis C Virus NS3 Protease: Employment of a Difluoromethyl Group as a Hydrogen-Bond Donor.
Zheng B, D'Andrea SV, Sun LQ, Wang AX, Chen Y, Hrnciar P, Friborg J, Falk P, Hernandez D, Yu F, Sheaffer AK, Knipe JO, Mosure K, Rajamani R, Good AC, Kish K, Tredup J, Klei HE, Paruchuri M, Ng A, Gao Q, Rampulla RA, Mathur A, Meanwell NA, McPhee F, Scola PM. Zheng B, et al. Among authors: falk p. ACS Med Chem Lett. 2018 Jan 19;9(2):143-148. doi: 10.1021/acsmedchemlett.7b00503. eCollection 2018 Feb 8. ACS Med Chem Lett. 2018. PMID: 29456803 Free PMC article.
Discovery of BMS-986144, a Third-Generation, Pan-Genotype NS3/4A Protease Inhibitor for the Treatment of Hepatitis C Virus Infection.
Sun LQ, Mull E, D'Andrea S, Zheng B, Hiebert S, Gillis E, Bowsher M, Kandhasamy S, Baratam VR, Puttaswamy S, Pulicharla N, Vishwakrishnan S, Reddy S, Trivedi R, Sinha S, Sivaprasad S, Rao A, Desai S, Ghosh K, Anumula R, Kumar A, Rajamani R, Wang YK, Fang H, Mathur A, Rampulla R, Zvyaga TA, Mosure K, Jenkins S, Falk P, Tagore DM, Chen C, Rendunchintala K, Loy J, Meanwell NA, McPhee F, Scola PM. Sun LQ, et al. Among authors: falk p. J Med Chem. 2020 Dec 10;63(23):14740-14760. doi: 10.1021/acs.jmedchem.0c01296. Epub 2020 Nov 23. J Med Chem. 2020. PMID: 33226226
258 results