Rationally Designed, Conformationally Constrained Inverse Agonists of RORγt-Identification of a Potent, Selective Series with Biologic-Like in Vivo Efficacy.

Autor: Marcoux D; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Duan JJ; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Shi Q; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Cherney RJ; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Srivastava AS; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Cornelius L; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Batt DG; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Liu Q; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Beaudoin-Bertrand M; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Weigelt CA; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Khandelwal P; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Vishwakrishnan S; Department of Discovery Synthesis , Biocon Bristol-Myers Squibb Research Centre , Biocon Park, Bommasandra IV Phase, Jigani Link Road , Bengaluru 560099 , India., Selvakumar K; Department of Discovery Synthesis , Biocon Bristol-Myers Squibb Research Centre , Biocon Park, Bommasandra IV Phase, Jigani Link Road , Bengaluru 560099 , India., Karmakar A; Department of Discovery Synthesis , Biocon Bristol-Myers Squibb Research Centre , Biocon Park, Bommasandra IV Phase, Jigani Link Road , Bengaluru 560099 , India., Gupta AK; Department of Discovery Synthesis , Biocon Bristol-Myers Squibb Research Centre , Biocon Park, Bommasandra IV Phase, Jigani Link Road , Bengaluru 560099 , India., Basha M; Department of Discovery Synthesis , Biocon Bristol-Myers Squibb Research Centre , Biocon Park, Bommasandra IV Phase, Jigani Link Road , Bengaluru 560099 , India., Ramlingam S; Department of Discovery Synthesis , Biocon Bristol-Myers Squibb Research Centre , Biocon Park, Bommasandra IV Phase, Jigani Link Road , Bengaluru 560099 , India., Manjunath N; Department of Discovery Synthesis , Biocon Bristol-Myers Squibb Research Centre , Biocon Park, Bommasandra IV Phase, Jigani Link Road , Bengaluru 560099 , India., Vanteru S; Department of Discovery Synthesis , Biocon Bristol-Myers Squibb Research Centre , Biocon Park, Bommasandra IV Phase, Jigani Link Road , Bengaluru 560099 , India., Karmakar S; Department of Discovery Synthesis , Biocon Bristol-Myers Squibb Research Centre , Biocon Park, Bommasandra IV Phase, Jigani Link Road , Bengaluru 560099 , India., Maddala N; Department of Discovery Synthesis , Biocon Bristol-Myers Squibb Research Centre , Biocon Park, Bommasandra IV Phase, Jigani Link Road , Bengaluru 560099 , India., Vetrichelvan M; Department of Discovery Synthesis , Biocon Bristol-Myers Squibb Research Centre , Biocon Park, Bommasandra IV Phase, Jigani Link Road , Bengaluru 560099 , India., Gupta A; Department of Discovery Synthesis , Biocon Bristol-Myers Squibb Research Centre , Biocon Park, Bommasandra IV Phase, Jigani Link Road , Bengaluru 560099 , India., Rampulla RA; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Mathur A; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Yip S; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Li P; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Wu DR; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Khan J; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Ruzanov M; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Sack JS; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Wang J; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Yarde M; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Cvijic ME; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Li S; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Shuster DJ; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Borowski V; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Xie JH; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., McIntyre KW; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Obermeier MT; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Fura A; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Stefanski K; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Cornelius G; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Hynes J Jr; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Tino JA; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Macor JE; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Salter-Cid L; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Denton R; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Zhao Q; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Carter PH; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States., Dhar TGM; Research and Development , Bristol-Myers Squibb , 3551 Lawrenceville Rd , Princeton , New Jersey 08540 , United States.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2019 Nov 14; Vol. 62 (21), pp. 9931-9946. Date of Electronic Publication: 2019 Oct 31.

Structure-based Discovery of Phenyl (3-Phenylpyrrolidin-3-yl)sulfones as Selective, Orally Active RORγt Inverse Agonists.

Autor: Duan JJ; Research and Development, Bristol-Myers Squibb Company, Princeton, New Jersey 08543-4000, United States., Lu Z; Research and Development, Bristol-Myers Squibb Company, Princeton, New Jersey 08543-4000, United States., Jiang B; Research and Development, Bristol-Myers Squibb Company, Princeton, New Jersey 08543-4000, United States., Stachura S; Research and Development, Bristol-Myers Squibb Company, Princeton, New Jersey 08543-4000, United States., Weigelt CA; Research and Development, Bristol-Myers Squibb Company, Princeton, New Jersey 08543-4000, United States., Sack JS; Research and Development, Bristol-Myers Squibb Company, Princeton, New Jersey 08543-4000, United States., Khan J; Research and Development, Bristol-Myers Squibb Company, Princeton, New Jersey 08543-4000, United States., Ruzanov M; Research and Development, Bristol-Myers Squibb Company, Princeton, New Jersey 08543-4000, United States., Galella MA; Research and Development, Bristol-Myers Squibb Company, Princeton, New Jersey 08543-4000, United States., Wu DR; Research and Development, Bristol-Myers Squibb Company, Princeton, New Jersey 08543-4000, United States., Yarde M; Research and Development, Bristol-Myers Squibb Company, Princeton, New Jersey 08543-4000, United States., Shen DR; Research and Development, Bristol-Myers Squibb Company, Princeton, New Jersey 08543-4000, United States., Shuster DJ; Research and Development, Bristol-Myers Squibb Company, Princeton, New Jersey 08543-4000, United States., Borowski V; Research and Development, Bristol-Myers Squibb Company, Princeton, New Jersey 08543-4000, United States., Xie JH; Research and Development, Bristol-Myers Squibb Company, Princeton, New Jersey 08543-4000, United States., Zhang L; Research and Development, Bristol-Myers Squibb Company, Princeton, New Jersey 08543-4000, United States., Vanteru S; Bristol-Myers Squibb-Biocon Research Center, Bangalore 560099, India., Gupta AK; Bristol-Myers Squibb-Biocon Research Center, Bangalore 560099, India., Mathur A; Research and Development, Bristol-Myers Squibb Company, Princeton, New Jersey 08543-4000, United States., Zhao Q; Research and Development, Bristol-Myers Squibb Company, Princeton, New Jersey 08543-4000, United States., Foster W; Research and Development, Bristol-Myers Squibb Company, Princeton, New Jersey 08543-4000, United States., Salter-Cid LM; Research and Development, Bristol-Myers Squibb Company, Princeton, New Jersey 08543-4000, United States., Carter PH; Research and Development, Bristol-Myers Squibb Company, Princeton, New Jersey 08543-4000, United States., Dhar TGM; Research and Development, Bristol-Myers Squibb Company, Princeton, New Jersey 08543-4000, United States.

Publikováno v: ACS medicinal chemistry letters [ACS Med Chem Lett] 2019 Feb 26; Vol. 10 (3), pp. 367-373. Date of Electronic Publication: 2019 Feb 26 (Print Publication: 2019).

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One-Pot, Metal- and Azide-Free Synthesis of 1,2,3-Triazoles from α-Ketoacetals and Amines.

Autor: Zehnder, Luke R., Hawkins, Joel M., Sutton, Scott C.

Publikováno v: Synlett; 2020, Vol. 31 Issue 2, p175-178, 4p