Identification of 2-amino-5-(thioaryl)thiazoles as inhibitors of nerve growth factor receptor TrkA

Autor: Mark E. Salvati, Jonathan Lippy, Brian E. Fink, Linda K. Stadnick, Robert V. Moquin, Soong-Hoon Kim, John S. Tokarski, Matthew V. Lorenzi, Gregory G. Vite, Ping Chen, Dan You, Kenneth J. Leavitt, Mary T. Obermeier, George L. Trainor

Publikováno v: Bioorganicmedicinal chemistry letters. 18(2)

2-Amino-5-(thioaryl)thiazoles are potent inhibitors of TrkA (e.g., 20h , TrkA IC 50 = 0.6 nM) that show anti-proliferative effect in cellular assays. A proposed inhibitor binding mode to TrkA active site is consistent with key SAR observations.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b15c4b91bfbccc3c0fa591d817fc342e
https://pubmed.ncbi.nlm.nih.gov/18055203

Discovery of Novel TLR7 Agonists as Systemic Agent for Combination With aPD1 for Use in Immuno-oncology.

Autor: Poudel YB; Bristol-Myers Squibb Research & Development, 700 Bay Road, Redwood City, California 94063, United States., He L; Bristol-Myers Squibb Research & Development, 700 Bay Road, Redwood City, California 94063, United States., Cox M; Bristol-Myers Squibb Research & Development, 700 Bay Road, Redwood City, California 94063, United States., Zhang Q; Bristol-Myers Squibb Research & Development, 700 Bay Road, Redwood City, California 94063, United States., Johnson WL; Bristol-Myers Squibb Research & Development, 700 Bay Road, Redwood City, California 94063, United States., Cong Q; Bristol-Myers Squibb Research & Development, 700 Bay Road, Redwood City, California 94063, United States., Cheng H; Bristol-Myers Squibb Research & Development, 700 Bay Road, Redwood City, California 94063, United States., Chowdari NS; Bristol-Myers Squibb Research & Development, 700 Bay Road, Redwood City, California 94063, United States., Tarby C; Bristol-Myers Squibb Research & Development, Princeton, New Jersey 08543, United States., Donnell AF; Bristol-Myers Squibb Research & Development, Princeton, New Jersey 08543, United States., Broekema M; Bristol-Myers Squibb Research & Development, Princeton, New Jersey 08543, United States., O'Malley DP; Bristol-Myers Squibb Research & Development, Princeton, New Jersey 08543, United States., Zhang Y; Bristol-Myers Squibb Research & Development, Princeton, New Jersey 08543, United States., A M Subbaiah M; The Biocon Bristol Myers Squibb Research Center (BBRC), Bangalore 560099, India., Kumar BV; The Biocon Bristol Myers Squibb Research Center (BBRC), Bangalore 560099, India., Subramani L; The Biocon Bristol Myers Squibb Research Center (BBRC), Bangalore 560099, India., Wang B; Bristol-Myers Squibb Research & Development, Princeton, New Jersey 08543, United States., Li YX; Bristol-Myers Squibb Research & Development, 700 Bay Road, Redwood City, California 94063, United States., Sivaprakasam P; Bristol-Myers Squibb Research & Development, Princeton, New Jersey 08543, United States., Critton D; Bristol-Myers Squibb Research & Development, Princeton, New Jersey 08543, United States., Mulligan D; Bristol-Myers Squibb Research & Development, Princeton, New Jersey 08543, United States., Sandhu B; Bristol-Myers Squibb Research & Development, Princeton, New Jersey 08543, United States., Xie C; Bristol-Myers Squibb Research & Development, Princeton, New Jersey 08543, United States., Ramakrishnan R; Bristol-Myers Squibb Research & Development, Princeton, New Jersey 08543, United States., Nagar J; The Biocon Bristol Myers Squibb Research Center (BBRC), Bangalore 560099, India., Dudhgaonkar S; The Biocon Bristol Myers Squibb Research Center (BBRC), Bangalore 560099, India., Oderinde MS; Bristol-Myers Squibb Research & Development, Princeton, New Jersey 08543, United States., Murtaza A; Bristol-Myers Squibb Research & Development, Princeton, New Jersey 08543, United States., Schieven GL; Bristol-Myers Squibb Research & Development, Princeton, New Jersey 08543, United States., Mathur A; Bristol-Myers Squibb Research & Development, Princeton, New Jersey 08543, United States., Gavai AV; Bristol-Myers Squibb Research & Development, Princeton, New Jersey 08543, United States., Vite G; Bristol-Myers Squibb Research & Development, Princeton, New Jersey 08543, United States., Gangwar S; Bristol-Myers Squibb Research & Development, 700 Bay Road, Redwood City, California 94063, United States.

Publikováno v: ACS medicinal chemistry letters [ACS Med Chem Lett] 2024 Jan 08; Vol. 15 (2), pp. 181-188. Date of Electronic Publication: 2024 Jan 08 (Print Publication: 2024).

Discovery and Preclinical Pharmacology of an Oral Bromodomain and Extra-Terminal (BET) Inhibitor Using Scaffold-Hopping and Structure-Guided Drug Design.

Autor: Gavai AV; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Norris D; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Delucca G; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Tortolani D; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Tokarski JS; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Dodd D; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., O'Malley D; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Zhao Y; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Quesnelle C; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Gill P; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Vaccaro W; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Huynh T; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Ahuja V; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Han WC; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Mussari C; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Harikrishnan L; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Kamau M; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Poss M; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Sheriff S; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Yan C; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Marsilio F; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Menard K; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Wen ML; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Rampulla R; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Wu DR; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Li J; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Zhang H; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Li P; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Sun D; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Yip H; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Traeger SC; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Zhang Y; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Mathur A; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Zhang H; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Huang C; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Yang Z; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Ranasinghe A; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Everlof G; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Raghavan N; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Tye CK; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Wee S; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Hunt JT; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Vite G; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Westhouse R; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States., Lee FY; Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2021 Oct 14; Vol. 64 (19), pp. 14247-14265. Date of Electronic Publication: 2021 Sep 20.

Conformational-Analysis-Guided Discovery of 2,3-Disubstituted Pyridine IDO1 Inhibitors.

Autor: Cherney EC; Bristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States., Zhang L; Bristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States., Guo W; Bristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States., Huang A; Bristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States., Williams D; Bristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States., Seitz S; Bristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States., Shan W; Bristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States., Zhu X; Bristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States., Gullo-Brown J; Bristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States., Maley D; Bristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States., Lin TA; Bristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States., Hunt JT; Bristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States., Huang C; Bristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States., Yang Z; Bristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States., D'Arienzo CJ; Bristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States., Discenza LN; Bristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States., Ranasinghe A; Bristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States., Grubb MF; Bristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States., Traeger SC; Bristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States., Li X; Bristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States., Johnston KA; Bristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States., Kopcho L; Bristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States., Fereshteh M; Bristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States., Foster KA; Bristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States., Stefanski K; Bristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States., Delpy D; Bristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States., Dhar G; Department of Discovery Synthesis, Biocon Bristol Myers Squibb R&D Centre, Syngene International Ltd., Biocon Park, Plot No. 2 & 3, Bommasandra-Jigani Road, Bangalore 560099, India., Anandam A; Department of Discovery Synthesis, Biocon Bristol Myers Squibb R&D Centre, Syngene International Ltd., Biocon Park, Plot No. 2 & 3, Bommasandra-Jigani Road, Bangalore 560099, India., Mahankali S; Department of Discovery Synthesis, Biocon Bristol Myers Squibb R&D Centre, Syngene International Ltd., Biocon Park, Plot No. 2 & 3, Bommasandra-Jigani Road, Bangalore 560099, India., Padmanabhan S; Department of Discovery Synthesis, Biocon Bristol Myers Squibb R&D Centre, Syngene International Ltd., Biocon Park, Plot No. 2 & 3, Bommasandra-Jigani Road, Bangalore 560099, India., Rajanna P; Department of Discovery Synthesis, Biocon Bristol Myers Squibb R&D Centre, Syngene International Ltd., Biocon Park, Plot No. 2 & 3, Bommasandra-Jigani Road, Bangalore 560099, India., Murali V; Department of Discovery Synthesis, Biocon Bristol Myers Squibb R&D Centre, Syngene International Ltd., Biocon Park, Plot No. 2 & 3, Bommasandra-Jigani Road, Bangalore 560099, India., Mariappan TT; Department of Discovery Synthesis, Biocon Bristol Myers Squibb R&D Centre, Syngene International Ltd., Biocon Park, Plot No. 2 & 3, Bommasandra-Jigani Road, Bangalore 560099, India., Pattasseri S; Department of Discovery Synthesis, Biocon Bristol Myers Squibb R&D Centre, Syngene International Ltd., Biocon Park, Plot No. 2 & 3, Bommasandra-Jigani Road, Bangalore 560099, India., Nimje RY; Department of Discovery Synthesis, Biocon Bristol Myers Squibb R&D Centre, Syngene International Ltd., Biocon Park, Plot No. 2 & 3, Bommasandra-Jigani Road, Bangalore 560099, India., Hong Z; Bristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States., Kempson J; Bristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States., Rampulla R; Bristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States., Mathur A; Bristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States., Gupta A; Department of Discovery Synthesis, Biocon Bristol Myers Squibb R&D Centre, Syngene International Ltd., Biocon Park, Plot No. 2 & 3, Bommasandra-Jigani Road, Bangalore 560099, India., Borzilleri R; Bristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States., Vite G; Bristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States., Balog A; Bristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States.

Publikováno v: ACS medicinal chemistry letters [ACS Med Chem Lett] 2021 Jun 16; Vol. 12 (7), pp. 1143-1150. Date of Electronic Publication: 2021 Jun 16 (Print Publication: 2021).

DNA-Model-Based Design and Execution of Some Fused Benzodiazepine Hybrid Payloads for Antibody-Drug Conjugate Modality.

Autor: Sivaprakasam P; Computer-Aided Drug Design, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States., McDonald I; Discovery Chemistry, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States., Iwuagwu C; Discovery Chemistry, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States., Chowdari NS; Discovery Chemistry, Bristol-Myers Squibb Research & Development, 700 Bay Road, Redwood City, California 94063, United States., Peese KM; Discovery Chemistry, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States., Langley DR; Computer-Aided Drug Design, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States., Cheng H; Discovery Chemistry, Bristol-Myers Squibb Research & Development, 700 Bay Road, Redwood City, California 94063, United States., Luzung MR; Chemical and Synthetic Development, Bristol-Myers Squibb, 1 Squibb Drive, New Brunswick, New Jersey 08903, United States., Schmidt MA; Chemical and Synthetic Development, Bristol-Myers Squibb, 1 Squibb Drive, New Brunswick, New Jersey 08903, United States., Zheng B; Chemical and Synthetic Development, Bristol-Myers Squibb, 1 Squibb Drive, New Brunswick, New Jersey 08903, United States., Tan Y; Chemical and Synthetic Development, Bristol-Myers Squibb, 1 Squibb Drive, New Brunswick, New Jersey 08903, United States., Cho P; Chemical and Synthetic Development, Bristol-Myers Squibb, 1 Squibb Drive, New Brunswick, New Jersey 08903, United States., Rakshit S; Chemical Development and API Supply, Biocon Bristol-Myers Squibb Research and Development Center, Biocon Park, Jigani Link Road, Bommasandra IV, Bangalore 560099, India., Lakshminarasimhan T; Chemical Development and API Supply, Biocon Bristol-Myers Squibb Research and Development Center, Biocon Park, Jigani Link Road, Bommasandra IV, Bangalore 560099, India., Guturi S; Chemical Development and API Supply, Biocon Bristol-Myers Squibb Research and Development Center, Biocon Park, Jigani Link Road, Bommasandra IV, Bangalore 560099, India., Kanagavel K; Chemical Development and API Supply, Biocon Bristol-Myers Squibb Research and Development Center, Biocon Park, Jigani Link Road, Bommasandra IV, Bangalore 560099, India., Kanusu U; Chemical Development and API Supply, Biocon Bristol-Myers Squibb Research and Development Center, Biocon Park, Jigani Link Road, Bommasandra IV, Bangalore 560099, India., Niyogi AG; Chemical Development and API Supply, Biocon Bristol-Myers Squibb Research and Development Center, Biocon Park, Jigani Link Road, Bommasandra IV, Bangalore 560099, India., Sidhar S; Chemical Development and API Supply, Biocon Bristol-Myers Squibb Research and Development Center, Biocon Park, Jigani Link Road, Bommasandra IV, Bangalore 560099, India., Vaidyanathan R; Chemical Development and API Supply, Biocon Bristol-Myers Squibb Research and Development Center, Biocon Park, Jigani Link Road, Bommasandra IV, Bangalore 560099, India., Eastgate MD; Chemical and Synthetic Development, Bristol-Myers Squibb, 1 Squibb Drive, New Brunswick, New Jersey 08903, United States., Kotapati S; Discovery Biotherapeutics, Bristol-Myers Squibb Research & Development, 700 Bay Road, Redwood City, California 94063, United States., Deshpande M; Discovery Biotherapeutics, Bristol-Myers Squibb Research & Development, 700 Bay Road, Redwood City, California 94063, United States., Pan C; Cell Biology and Pharmacology, Bristol-Myers Squibb Research & Development, 700 Bay Road, Redwood City, California 94063, United States., Cardarelli PM; Cell Biology and Pharmacology, Bristol-Myers Squibb Research & Development, 700 Bay Road, Redwood City, California 94063, United States., Xie C; Lead Discovery and Optimization, Bristol-Myers Squibb Research and Development, P.O. Box 4000, Princeton, New Jersey 08543, United States., Rao C; Discovery Biotherapeutics, Bristol-Myers Squibb Research & Development, 700 Bay Road, Redwood City, California 94063, United States., Holder P; Discovery Biotherapeutics, Bristol-Myers Squibb Research & Development, 700 Bay Road, Redwood City, California 94063, United States., Sarma G; Discovery Biotherapeutics, Bristol-Myers Squibb Research & Development, 700 Bay Road, Redwood City, California 94063, United States., Vite G; Discovery Chemistry, Bristol-Myers Squibb Research and Development, P.O. Box 4000, Princeton, New Jersey 08543, United States., Gangwar S; Discovery Chemistry, Bristol-Myers Squibb Research & Development, 700 Bay Road, Redwood City, California 94063, United States.

Publikováno v: ACS medicinal chemistry letters [ACS Med Chem Lett] 2021 Feb 10; Vol. 12 (3), pp. 404-412. Date of Electronic Publication: 2021 Feb 10 (Print Publication: 2021).