851784-76-4Relevant academic research and scientific papers
Compounds and methods of use
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Page/Page column 590-591, (2021/08/04)
Compounds are provided according to Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X1, X2, X3, X4, Y, A, L1, L2, R1, R2, R5, m and n are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.
NOVEL PROCESS FOR THE PREPARATION OF LIFITEGRAST
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Page/Page column 17, (2019/05/02)
The present invention relates to a novel process for the preparation of lifitegrast of Formula (I). The present invention further provides a novel process for the purification of lifitegrast of Formula (I).
LFA-1 INHIBITOR AND POLYMORPH THEREOF
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, (2014/02/16)
Methods of preparation and purification of a compound, intermediates thereof, a polymorph thereof, and related compounds are disclosed. Formulations and uses thereof in the treatment of LFA -1 mediated diseases are also disclosed.
Discovery of tetrahydroisoquinoline (THIQ) derivatives as potent and orally bioavailable LFA-1/ICAM-1 antagonists
Zhong, Min,Shen, Wang,Barr, Kenneth J.,Arbitrario, Jennifer P.,Arkin, Michelle R.,Bui, Minna,Chen, Teresa,Cunningham, Brian C.,Evanchik, Marc J.,Hanan, Emily J.,Hoch, Ute,Huen, Karen,Hyde, Jennifer,Kumer, Jeffery L.,Lac, Teresa,Lawrence, Chris E.,Martell, Jose R.,Oslob, Johan D.,Paulvannan, Kumar,Prabhu, Saileta,Silverman, Jeffrey A.,Wright, Jasmin,Yu, Chul H.,Zhu, Jiang,Flanagan, W. Mike
scheme or table, p. 5269 - 5273 (2010/10/18)
This letter describes the discovery of a novel series of tetrahydroisoquinoline (THIQ)-derived small molecules that potently inhibit both human T-cell migration and super-antigen induced T-cell activation through disruption of the binding of integrin LFA-1 to its receptor, ICAM-1. In addition to excellent in vitro potency, 6q shows good pharmacokinetic properties and its ethyl ester (6t) demonstrates good oral bioavailability in both mouse and rat. Either intravenous administration of 6q or oral administration of its ethyl ester (6t) produced a significant reduction of neutrophil migration in a thioglycollate-induced murine peritonitis model.
