50534-23-1Relevant articles and documents
CHEMOKING RECEPTOR ANTAGONISTS
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Page/Page column 111-112, (2013/03/26)
Disclosed herein are chemokine receptor antagonists of formula (I) wherein G1, X1, X2, and X3 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.
Route selection and process development of a multikilogram route to the inhaled A2a agonist UK-432,097
Ashcroft, Christopher P.,Dessi, Yann,Entwistle, David A.,Hesmondhalgh, Lynsey C.,Longstaff, Adrian,Smith, Julian D.
scheme or table, p. 470 - 483 (2012/08/08)
This article describes the selection, process development, and scale-up of a synthetic route to a complex nucleoside analogue, the A2a agonist UK-432,097 (1), that culminated in the manufacture of over 25 kg of the API. The key steps in the process were (1) a stereoselective glycosidation reaction; (2) a scalable bleach-TEMPO oxidation; and (3) an unusual elevated temperature crystallization process for the final API. The problems that were encountered with the scale-up of the route together with how they were overcome are also presented.
TRIAZOLYLPIPERIDINE DERIVATIVES AND USE THEREOF IN THERAPY
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Page/Page column 28, (2010/11/25)
The present invention provides compounds of formula (I) Wherein R1 , R2, R3 , R4 , Het and m are as defined in the description. The compounds of the present invention are modulators, especially antagonists, of the activity of chemokine CCR5 receptors.