873191-26-5Relevant academic research and scientific papers
Discovery of potent and specific CXCR3 antagonists
Chen, Xiaoqi,Mihalic, Jeff,Deignan, Jeff,Gustin, Darin J.,Duquette, Jason,Du, Xiaohui,Chan, Johann,Fu, Zice,Johnson, Michael,Li, An-Rong,Henne, Kirk,Sullivan, Tim,Lemon, Bryan,Ma, Ji,Miao, Shichang,Tonn, George,Collins, Tassie,Medina, Julio C.
, p. 357 - 362 (2012/03/11)
The optimization of a series of 8-aza-quinazolinone analogs for antagonist activity against the CXCR3 receptor is reported. Compounds were optimized to avoid the formation of active metabolites and time-dependent-inhibitors of CYP3A4. In addition, antagon
Optimization of a series of quinazolinone-derived antagonists of CXCR3
Liu, Jiwen,Fu, Zice,Li, An-Rong,Johnson, Michael,Zhu, Liusheng,Marcus, Andrew,Danao, Jay,Sullivan, Tim,Tonn, George,Collins, Tassie,Medina, Julio
scheme or table, p. 5114 - 5118 (2010/03/31)
The evaluation of the CXCR3 antagonist AMG 487 in clinic trials was complicated due to the formation of an active metabolite. In this Letter, we will discuss the further optimization of the quinazolinone series that led to the discovery of compounds devoi
ARYL NITRILE COMPOUNDS AND COMPOSITIONS AND THEIR USES IN TREATING INFLAMMATORY AND RELATED DISORDERS
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Page/Page column 41, (2010/11/25)
Compounds, compositions and methods that are useful in the treatment of inflammatory and immune conditions and diseases are provided herein. In particular, the invention provides aryl nitrile compounds which modulate the expression and/or function of a ch
FUSED PYRIMIDINE DERIVATIVES AND COMPOSITIONS THEREOF AS CXCR3 RECEPTOR MODULATORS, USEFUL IN PREVENTION AND TREATMENT OF INFLAMMATORY AND IMMUNOREGULATORY DISORDERS AND DISEASES
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Page/Page column 47, (2010/02/15)
Compounds are provided having the formula: wherein variables Ra, R1, R2, R3, R4, A1, A4, L, Q, X and subscript n as described herein. The subject compounds are useful for treatment of inflammatory and immune conditions and diseases. Compositions and methods of treatment using the subject compounds are also provided. For example, the subject methods are useful for treatment of inflammatory and immune disorders and disease such as multiple sclerosis, rheumatoid arthritis, psoriasis, and inflammatory bowel disease.
