December 10, 2012

CAS databases provide millions of journal article references from more than 10,000 major scientific journals worldwide, patent and patent family references from 63 patent authorities around the world, and other reputable web sources.  

The following patent record is from the CAplusSM database.


Patent Number: WO 2012130780
Title: Preparation of thiazolopyrimidine derivatives for use as SYK inhibitors
Inventor(s): Hermann, Johannes Cornelius; Lowrie, Lee Edwin, Jr.; Lucas, Matthew C.; Luk, Kin-Chun Thomas; Padilla, Fernando; Wanner, Jutta; Xie, Wenwei; Zhang, Xiaohu
Patent Assignee(s): F. Hoffmann-La Roche AG, Switz.
Source: PCT Int. Appl., 162pp. CODEN: PIXXD2
Language: English


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.

View the full-text patent here.

Note: 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.

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