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CAPLUS COPYRIGHT 2012 ACS
||Preparation of thiazolopyrimidine derivatives for use as SYK inhibitors
||Hermann, Johannes Cornelius; Lowrie, Lee Edwin, Jr.; Lucas, Matthew C.; Luk, Kin-Chun Thomas; Padilla, Fernando; Wanner, Jutta; Xie, Wenwei; Zhang, Xiaohu
||F. Hoffmann-La Roche AG, Switz.
||PCT Int. Appl., 162pp. CODEN: PIXXD2
Title compds. I [B = Ph, pyridinyl, pyrrolidinyl, or piperidinyl; X = OH, alkyl, CONH2, etc.; R1 = (un)substituted Ph], and their pharmaceutically acceptable salts, are prepared and disclosed as SYK inhibitors. Thus, e.g., II was prepared by amination of 5,7-dichlorothiazolo[5,4-d]pyrimidine with 3,4-dimethoxyphenylamine followed by coupling with 3-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-benzoic acid Me ester, and hydrolysis. Select I were evaluated in spleen tyrosine kinase (H-SYK-GST-SF9-C inactive-dephosphorylated) inhibition assays, e.g., II demonstrated an IC50 value of 0.421 uM.
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: Titles and abstracts for patent records in CAplus are routinely enhanced to better describe the claimed invention. In this example, CAS enhanced both the abstract and title using additional information found in the patent. The original title of the PCT application is Thiazolopyrimidine compounds . For the CAplus record, this title was enhanced to read Preparation of thiazolopyrimidine derivatives for use as SYK inhibitors.