- INHIBITORS OF ALPHA 2 BETA 1 INTEGRIN AND METHODS OF USE THEREOF
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Disclosed herein, inter alia, are inhibitors of alpha 2 beta 1 integrin and methods of using the same.
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Paragraph 0724; 1140-1142
(2021/11/06)
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- NOVEL PROCESS FOR THE PREPARATION OF LIFITEGRAST
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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).
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- A method for synthesizing intermediate advantage non-si te (by machine translation)
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The invention discloses a method of preparing intermediates of advantage non-si te, comprises the following steps: (1) heating compound 1, tetramethyl diethylamine and butyl lithium treatment, adding chloromethane acid benzyl ester, in - 70 °C following temperature reaction, to obtain compound 2; (2) taking compound 2 with the strong alkali solution reaction, after the reaction adjusting PH to 3 - 4, extraction, to obtain compound 3. The advantage non-si te intermediates prepared by the process of a high degree of selectivity, the controllability is strong, good stability, the total yield is high, suitable for commercial scale production. (by machine translation)
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Paragraph 0073-0074
(2018/04/21)
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- LFA-1 INHIBITOR AND POLYMORPH THEREOF
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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.
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Paragraph 00118; 00119
(2014/02/16)
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- Discovery of tetrahydroisoquinoline (THIQ) derivatives as potent and orally bioavailable LFA-1/ICAM-1 antagonists
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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.
- 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
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scheme or table
p. 5269 - 5273
(2010/10/18)
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- MODULATORS OF CELLULAR ADHESION
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The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1-R4, n, p, A, B, D, E, L and AR1 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of disorders mediated by the CD11/CD18 family of cellular adhesion molecules (e.g., LFA-1).
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Page/Page column 77-79
(2010/02/11)
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