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433 results

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Page 1
Discovery of BMS-753426: A Potent Orally Bioavailable Antagonist of CC Chemokine Receptor 2.
Yang MG, Xiao Z, Zhao R, Tebben AJ, Wang B, Cherney RJ, Batt DG, Brown GD, Cvijic ME, Duncia JV, Gallela MA, Gardner DS, Khandelwal P, Malley MF, Pang J, Rose AV, Santella JB 3rd, Sarjeant AA, Xu S, Mathur A, Mandlekar S, Vuppugalla R, Zhao Q, Carter PH. Yang MG, et al. Among authors: khandelwal p. ACS Med Chem Lett. 2021 May 25;12(6):969-975. doi: 10.1021/acsmedchemlett.1c00082. eCollection 2021 Jun 10. ACS Med Chem Lett. 2021. PMID: 34141082 Free PMC article.
Use of a Conformational-Switching Mechanism to Modulate Exposed Polarity: Discovery of CCR2 Antagonist BMS-741672.
Yang MG, Xiao Z, Cherney RJ, Tebben AJ, Batt DG, Brown GD, Chen J, Cvijic ME, Dabros M, Duncia JV, Galella M, Gardner DS, Khandelwal P, Ko SS, Malley MF, Mo R, Pang J, Rose AV, Santella JB 3rd, Shi H, Srivastava A, Traeger SC, Wang B, Xu S, Zhao R, Barrish JC, Mandlekar S, Zhao Q, Carter PH. Yang MG, et al. Among authors: khandelwal p. ACS Med Chem Lett. 2019 Jan 16;10(3):300-305. doi: 10.1021/acsmedchemlett.8b00439. eCollection 2019 Mar 14. ACS Med Chem Lett. 2019. PMID: 30891130 Free PMC article.
Rationally Designed, Conformationally Constrained Inverse Agonists of RORγt-Identification of a Potent, Selective Series with Biologic-Like in Vivo Efficacy.
Marcoux D, Duan JJ, Shi Q, Cherney RJ, Srivastava AS, Cornelius L, Batt DG, Liu Q, Beaudoin-Bertrand M, Weigelt CA, Khandelwal P, Vishwakrishnan S, Selvakumar K, Karmakar A, Gupta AK, Basha M, Ramlingam S, Manjunath N, Vanteru S, Karmakar S, Maddala N, Vetrichelvan M, Gupta A, Rampulla RA, Mathur A, Yip S, Li P, Wu DR, Khan J, Ruzanov M, Sack JS, Wang J, Yarde M, Cvijic ME, Li S, Shuster DJ, Borowski V, Xie JH, McIntyre KW, Obermeier MT, Fura A, Stefanski K, Cornelius G, Hynes J Jr, Tino JA, Macor JE, Salter-Cid L, Denton R, Zhao Q, Carter PH, Dhar TGM. Marcoux D, et al. Among authors: khandelwal p. J Med Chem. 2019 Nov 14;62(21):9931-9946. doi: 10.1021/acs.jmedchem.9b01369. Epub 2019 Oct 31. J Med Chem. 2019. PMID: 31638797
Discovery of BMS-986251: A Clinically Viable, Potent, and Selective RORγt Inverse Agonist.
Cherney RJ, Cornelius LAM, Srivastava A, Weigelt CA, Marcoux D, Duan JJ, Shi Q, Batt DG, Liu Q, Yip S, Wu DR, Ruzanov M, Sack J, Khan J, Wang J, Yarde M, Cvijic ME, Mathur A, Li S, Shuster D, Khandelwal P, Borowski V, Xie J, Obermeier M, Fura A, Stefanski K, Cornelius G, Tino JA, Macor JE, Salter-Cid L, Denton R, Zhao Q, Carter PH, Dhar TGM. Cherney RJ, et al. Among authors: khandelwal p. ACS Med Chem Lett. 2020 Mar 31;11(6):1221-1227. doi: 10.1021/acsmedchemlett.0c00063. eCollection 2020 Jun 11. ACS Med Chem Lett. 2020. PMID: 32551004 Free PMC article.
Tricyclic sulfones as potent, selective and efficacious RORγt inverse agonists - Exploring C6 and C8 SAR using late-stage functionalization.
Shi Q, Xiao Z, Yang MG, Marcoux D, Cherney RJ, Yip S, Li P, Wu DR, Weigelt CA, Sack J, Khan J, Ruzanov M, Wang J, Yarde M, Ellen Cvijic M, Li S, Shuster DJ, Xie J, Sherry T, Obermeier M, Fura A, Stefanski K, Cornelius G, Chacko S, Shu YZ, Khandelwal P, Hynes J Jr, Tino JA, Salter-Cid L, Denton R, Zhao Q, Dhar TGM. Shi Q, et al. Among authors: khandelwal p. Bioorg Med Chem Lett. 2020 Dec 1;30(23):127521. doi: 10.1016/j.bmcl.2020.127521. Epub 2020 Aug 31. Bioorg Med Chem Lett. 2020. PMID: 32882417
Novel Tricyclic Pyroglutamide Derivatives as Potent RORγt Inverse Agonists Identified using a Virtual Screening Approach.
Liu Q, Batt DG, Weigelt CA, Yip S, Wu DR, Ruzanov M, Sack JS, Wang J, Yarde M, Li S, Shuster DJ, Xie JH, Sherry T, Obermeier MT, Fura A, Stefanski K, Cornelius G, Khandelwal P, Tino JA, Macor JE, Salter-Cid L, Denton R, Zhao Q, Dhar TGM. Liu Q, et al. Among authors: khandelwal p. ACS Med Chem Lett. 2020 Nov 6;11(12):2510-2518. doi: 10.1021/acsmedchemlett.0c00496. eCollection 2020 Dec 10. ACS Med Chem Lett. 2020. PMID: 33335675 Free PMC article.
Tricyclic-Carbocyclic RORγt Inverse Agonists-Discovery of BMS-986313.
Yang MG, Beaudoin-Bertrand M, Xiao Z, Marcoux D, Weigelt CA, Yip S, Wu DR, Ruzanov M, Sack JS, Wang J, Yarde M, Li S, Shuster DJ, Xie JH, Sherry T, Obermeier MT, Fura A, Stefanski K, Cornelius G, Khandelwal P, Karmakar A, Basha M, Babu V, Gupta AK, Mathur A, Salter-Cid L, Denton R, Zhao Q, Dhar TGM. Yang MG, et al. Among authors: khandelwal p. J Med Chem. 2021 Mar 11;64(5):2714-2724. doi: 10.1021/acs.jmedchem.0c01992. Epub 2021 Feb 16. J Med Chem. 2021. PMID: 33591748
Azatricyclic Inverse Agonists of RORγt That Demonstrate Efficacy in Models of Rheumatoid Arthritis and Psoriasis.
Liu Q, Xiao HY, Batt DG, Xiao Z, Zhu Y, Yang MG, Li N, Yip S, Li P, Sun D, Wu DR, Ruzanov M, Sack JS, Weigelt CA, Wang J, Li S, Shuster DJ, Xie JH, Song Y, Sherry T, Obermeier MT, Fura A, Stefanski K, Cornelius G, Chacko S, Khandelwal P, Dudhgaonkar S, Rudra A, Nagar J, Murali V, Govindarajan A, Denton R, Zhao Q, Meanwell NA, Borzilleri R, Dhar TGM. Liu Q, et al. Among authors: khandelwal p. ACS Med Chem Lett. 2021 Apr 30;12(5):827-835. doi: 10.1021/acsmedchemlett.1c00112. eCollection 2021 May 13. ACS Med Chem Lett. 2021. PMID: 34055233 Free PMC article.
Optimization of physicochemical properties of pyrrolidine GPR40 AgoPAMs results in a differentiated profile with improved pharmacokinetics and reduced off-target activities.
Jurica EA, Wu X, Williams KN, Haque LE, Rampulla RA, Mathur A, Zhou M, Cao G, Cai H, Wang T, Liu H, Xu C, Kunselman LK, Antrilli TM, Hicks MB, Sun Q, Dierks EA, Apedo A, Moore DB, Foster KA, Cvijic ME, Panemangalore R, Khandelwal P, Wilkes JJ, Zinker BA, Robertson DG, Janovitz EB, Galella M, Li YX, Li J, Ramar T, Jalagam PR, Jayaram R, Whaley JM, Barrish JC, Robl JA, Ewing WR, Ellsworth BA. Jurica EA, et al. Among authors: khandelwal p. Bioorg Med Chem. 2023 May 1;85:117273. doi: 10.1016/j.bmc.2023.117273. Epub 2023 Apr 4. Bioorg Med Chem. 2023. PMID: 37030194
Discovery of novel pyridinones as MGAT2 inhibitors for the treatment of metabolic disorders.
Moore F, Wang W, Zhao G, Mignone J, Meng W, Chu CH, Ma Z, Azzara A, Cullen MJ, Pelleymounter MA, Appiah K, Cvijic ME, Dierks E, Chang S, Foster K, Kopcho L, O'Malley K, Li YX, Khandelwal P, Whaley JM, Mathur A, Hou X, Wu DR, Robl JA, Cheng D, Devasthale P. Moore F, et al. Among authors: khandelwal p. Bioorg Med Chem Lett. 2023 Jul 15;91:129362. doi: 10.1016/j.bmcl.2023.129362. Epub 2023 Jun 8. Bioorg Med Chem Lett. 2023. PMID: 37295614
433 results