April 8, 2013

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The following patent record is from the CAplusSM database.


Patent Number: WO 2013003298
Title: Preparation of substituted 2-(imidazo[1,2-a]pyridin-7-yl)-[1,2,4]triazolo[1,5-a]pyrazines as inhibitors of PDE10
Inventor(s): Schmitz, William D.; Debenedetto, Mikkel V.; Kimura, S. Roy
Patent Assignee(s): Bristol-Myers Squibb Company, USA
Source: PCT Int. Appl., 59pp. CODEN: PIXXD2
Language: English

The title compds. I [R = cycloalkyl or II (wherein Q = N or CR1; Q1 = N or CR4; R1-R5 = H, alkoxy, alkyl, etc.); R6 = H, alkyl; X = N, CR7; one of R7 and R8 = H, CN, halo, etc., and the other = (un)substituted III containing 2-4 N atoms (Y = N or CH; Z = N or C); with the proviso], useful as PDE10 inhibitors, were prepared and claimed. E.g., a multi-step synthesis of IV, starting from Me 2-aminoisonicotinate, was described. Exemplified compds. I were tested in the PDE10a inhibition assay (data given for representative compds. I). Compns. comprising compds. I and methods for using the compds. I to inhibit PDE10 are also disclosed.

Please note:  Abstracts and Titles for patent records in CAplus are routinely enhanced to better describe the claimed invention. The title of the PCT publication is Inhibitors of PDE10.

 View the full-text here.

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