US2014371249A1PendingUtilityA1

Crystal of a free tricyclic pyrazolopyrimidine derivative

Assignee: DAIICHI SANKYO CO LTDPriority: Aug 23, 2010Filed: Aug 29, 2014Published: Dec 18, 2014
Est. expiryAug 23, 2030(~4.1 yrs left)· nominal 20-yr term from priority
A61P 35/00C07D 495/16A61K 31/55C07D 417/06A61K 31/519
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Claims

Abstract

To provide a crystal of a tricyclic pyrazolopyrimidine compound inhibiting the effect of HSP90. The present invention provides a crystal of 2-{4-amino-2-[(3-chloro-4-methoxy-5-methylpyridin-2-yl)methyl]-2,7-dihydro-6-thia-1,2,3,5-tetraazabenzo[cd]azulen-8-yl}-N-methylacetamide which inhibits the ATPase activity of HSP90 and which has antitumor activity, a medicament comprising the same, an anticancer agent comprising the same, and the like.

Claims

exact text as granted — not AI-modified
1 . A crystal of 2-{4-amino-2-[(3-chloro-4-methoxy-5-methylpyridin-2-yl)methyl]-2,7-dihydro-6-thia-1,2,3,5-tetraazabenzo[cd]azulen-8-yl}-N-methylacetamide represented by the following formula (1): 
       
         
           
           
               
               
           
         
         wherein the crystal has the X-ray diffraction pattern shown in  FIG. 2 , in an X-ray powder diffraction pattern obtained by irradiation with copper Kα radiation (wavelength λ=1.54 angstroms). 
       
     
     
         2 . The crystal of  claim 1  which shows principal peaks at angles of diffraction 2θ of 5.04, 6.78, 7.72, 10.14, 11.16, 13.24, 13.66, 15.32, 18.50, 20.40, 22.36, 22.90, 25.16, 26.66, 27.92, 30.92 and 31.78, in an X-ray powder diffraction pattern obtained by irradiation with copper Kα radiation (wavelength λ=1.54 angstroms). 
     
     
         3 . A pharmaceutical composition comprising a crystal according to  claim 1  and a pharmaceutically acceptable carrier.

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