873191-25-4Relevant academic research and scientific papers
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
Synthesis and structure-activity relationships of 3H-quinazolin-4-ones and 3H-pyrido[2,3-d]pyrimidin-4-ones as CXCR3 receptor antagonists
Storelli, Stefania,Verzijl, Dennis,Al-Badie, Jawad,Elders, Niels,Bosch, Leontien,Timmerman, Henk,Smit, Martine J.,De Esch, Iwan J. P.,Leurs, Rob
, p. 281 - 291 (2008/02/10)
CXC chemokine receptor-3 (CXCR3) is a G-protein coupled receptor (GPCR) predominantly expressed on activated T lymphocytes that promote Th1 responses. Previously, we described the 3H-quinazolin-4-one containing VUF 5834 (decanoic acid {1-[3-(4-cyano-pheny
ARYL NITRILE COMPOUNDS AND COMPOSITIONS AND THEIR USES IN TREATING INFLAMMATORY AND RELATED DISORDERS
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Page/Page column 39-40, (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 46-47, (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.
