Discovery of the CCR1 Antagonist, BMS-817399, for the Treatment of Rheumatoid Arthritis

Joseph B. Santella; Daniel S. Gardner; John V. Duncia; Hong Wu; Murali Dhar; Cullen Cavallaro; Andrew J. Tebben; Percy H. Carter; Joel C. Barrish; Melissa Yarde; Stephanie W. Briceno; Mary Ellen Cvijic; R. Robert Grafstrom; Richard Liu; Sima R. Patel; Andrew J. Watson; Guchen Yang; Anne V. Rose; Rodney D. Vickery; Janet Caceres-Cortes; Christian Caporuscio; Daniel M. Camac; Javed A. Khan; Yongmi An; William R. Foster

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Discovery of the CCR1 Antagonist, BMS-817399, for the Treatment of Rheumatoid Arthritis

机译：发现用于治疗类风湿性关节炎的CCR1拮抗剂BMS-817399

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High-affinity, functionally potent, urea-based antagonists of CCR1 have been discovered. Modulation of PXR transactivation has revealed the selective and orally bioavailable CCR1 antagonist BMS-817399 (29), which entered clinical trials for the treatment of rheumatoid arthritis.

机译：已经发现了高亲和力，功能强大，基于尿素的CCR1拮抗剂。 PXR反式激活的调制揭示了选择性和口服生物利用的CCR1拮抗剂BMS-817399（29），该药物已进入治疗类风湿性关节炎的临床试验。

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《Journal of Medicinal Chemistry 》 |2014年第18期| 共15页
作者
Joseph B. Santella; Daniel S. Gardner; John V. Duncia; Hong Wu; Murali Dhar; Cullen Cavallaro; Andrew J. Tebben; Percy H. Carter; Joel C. Barrish; Melissa Yarde; Stephanie W. Briceno; Mary Ellen Cvijic; R. Robert Grafstrom; Richard Liu; Sima R. Patel; Andrew J. Watson; Guchen Yang; Anne V. Rose; Rodney D. Vickery; Janet Caceres-Cortes; Christian Caporuscio; Daniel M. Camac; Javed A. Khan; Yongmi An; William R. Foster;
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正文语种 eng
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Discovery; Antagonist; BMS-817399;

机译：发现者;拮抗剂;BMS-817399;

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专利

1. Discovery of the CCR1 Antagonist, BMS-817399, for the Treatment of Rheumatoid Arthritis [J] . Joseph B. Santella, Daniel S. Gardner, John V. Duncia, Journal of Medicinal Chemistry . 2014 ,第18期

机译：发现用于治疗类风湿性关节炎的CCR1拮抗剂BMS-817399
2. Chemokine receptor CCR1 antagonist CCX354-C treatment for rheumatoid arthritis: CARAT-2, a randomised, placebo controlled clinical trial [J] . TakP.P., BalanescuA., TseluykoV., Annals of the Rheumatic Diseases: A Journal of Clinical Rheumatology and Connective Tissue Research . 2013 ,第3期

机译：趋化因子受体CCR1拮抗剂CCX354-C治疗类风湿关节炎：CARAT-2，一项随机，安慰剂对照的临床试验
3. Balancing hERG affinity and absorption in the discovery of AZD5672, an orally active CCR5 antagonist for the treatment of rheumatoid arthritis [J] . CummingJ.G., TuckerH., OldfieldJ., Bioorganic and Medicinal Chemistry Letters . 2012 ,第4期

机译：在发现用于治疗类风湿性关节炎的口服活性CCR5拮抗剂AZD5672中平衡hERG亲和力和吸收
4. Application of High Sensitivity LC-MS/MS for Autoimmune Antigen Discovery in Antibiotic-refractory Lyme Arthritis or Rheumatoid Arthritis [C] . Qi Wang, Elise E. Drouin, Chunxiang Yao, ASMS Conference on Mass Spectrometry and Allied Topics . 2015

机译：高灵敏度LC-MS / MS在抗生素 - 难治性百婚关节炎或类风湿性关节炎中的自身免疫抗原发现的应用
5. Comparison of the Therapeutic Efficacy of Rheumatoid Arthritis Treatments [D] . Davis, Kacy. 2021

机译：类风湿性关节炎治疗治疗疗效的比较
6. Why CCR2 and CCR5 Blockade Failed and Why CCR1 Blockade Might Still Be Effective in the Treatment of Rheumatoid Arthritis [O] . Maria C. Lebre, Clarissa E. Vergunst, Ivy Y. K. Choi, 2011

机译：为什么CCR2和CCR5封锁失败以及为什么CCR1封锁在类风湿关节炎治疗中仍然有效
7. MLN3897 plus methotrexate in patients with rheumatoid arthritis: Safety, efficacy, pharmacokinetics, and pharmacodynamics of an oral CCR1 antagonist in a phase IIa, double-blind, placebo-controlled, randomized, proof-of-concept study [O] . Vergunst, Clarissa E., Gerlag, Danielle M., von Moltke, Lisa, 2009

机译：MLN3897加甲氨蝶呤治疗类风湿关节炎：IIa期，双盲，安慰剂对照，随机，概念验证性研究的口服CCR1拮抗剂的安全性，疗效，药代动力学和药效学

Discovery of the CCR1 Antagonist, BMS-817399, for the Treatment of Rheumatoid Arthritis

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