US2006100432A1PendingUtilityA1

Crystalline materials of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione

53
Individually held — no corporate assignee on recordPriority: Nov 9, 2004Filed: Nov 4, 2005Published: May 11, 2006
Est. expiryNov 9, 2024(expired)· nominal 20-yr term from priority
Inventors:John D. MatiskellaChenkou WeiQi GaoChong-Hui GuShan-Ming Kuang
C07D 471/04
53
PatentIndex Score
0
Cited by
0
References
0
Claims

Abstract

The instant invention provides crystalline materials of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione; processes for the production of such crystalline materials; pharmaceutical compositions comprising such crystalline materials; and methods of treating HIV or AIDS with such crystalline materials or such pharmaceutical compositions.

Claims

exact text as granted — not AI-modified
1 . Form P-1 of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione characterized by an X-ray powder diffraction pattern substantially in accordance with that shown in  FIG. 1 .  
   
   
       2 . Form P-1 of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione characterized by an X-ray powder diffraction pattern comprising two or more 20 values selected from the group consisting of: 8.90±0.10, 11.21±0.10, 16.91±0.10 and 21.00±0.10.  
   
   
       3 . Form P-1 according to  claim 1  or 2 wherein the 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione is substantially pure.  
   
   
       4 . Form P-1 according to  claim 3 , wherein substantially pure is greater than 90 percent pure.  
   
   
       5 . Form P-1 of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione characterized by a differential scanning calorimetry (DSC) thermogram substantially in accordance with that shown in  FIG. 2 .  
   
   
       6 . Form P-1 of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione characterized by a thermo gravimetric analysis (TGA) diagram substantially in accordance with that shown in  FIG. 3 .  
   
   
       7 . Form P-2 of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione characterized by an X-ray powder diffraction pattern substantially in accordance with that shown in  FIG. 4 .  
   
   
       8 . Form P-2 of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione characterized by an X-ray powder diffraction pattern comprising two or more 2θ values selected from the group consisting of: 5.28±0.10, 9.13±0.10, 10.57±0.10 and 21.31±0.10.  
   
   
       9 . Form P-2 according to  claim 7  or 8 wherein the 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione is substantially pure.  
   
   
       10 . Form P-2 according to  claim 9 , wherein substantially pure is greater than 90 percent pure.  
   
   
       11 . Form P-2 of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione characterized by a differential scanning calorimetry (DSC) thermogram substantially in accordance with that shown in  FIG. 5 .  
   
   
       12 . Form P-2 of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione characterized by a thermo gravimetric analysis (TGA) diagram substantially in accordance with that shown in  FIG. 6 .  
   
   
       13 . Form P-3 of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione characterized by an X-ray powder diffraction pattern substantially in accordance with that shown in  FIG. 7 .  
   
   
       14 . Form P-3 of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione characterized by an X-ray powder diffraction pattern comprising two or more 20 values selected from the group consisting of: 10.66±0.10, 12.16±0.10, 21.46±0.10 and 25.28±0.10.  
   
   
       15 . Form P-3 according to  claim 13  or 14 wherein the 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione is substantially pure.  
   
   
       16 . Form P-3 according to  claim 15 , wherein substantially pure is greater than 90 percent pure.  
   
   
       17 . Form P-3 of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione characterized by a differential scanning calorimetry (DSC) thermogram substantially in accordance with that shown in  FIG. 8 .  
   
   
       18 . Form P-3 of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione characterized by a thermo gravimetric analysis (TGA) diagram substantially in accordance with that shown in  FIG. 9 .  
   
   
       19 . Form P-4 of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione characterized by an X-ray powder diffraction pattern substantially in accordance with that shown in  FIG. 10 .  
   
   
       20 . Form P-4 of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione characterized by an X-ray powder diffraction pattern comprising two or more 20 values selected from the group consisting of 9.12±0.10, 10.64±0.10, 17.52±0.10 and 21.28±0.10.  
   
   
       21 . Form P-4 according to  claim 19  or 20 wherein the 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione is substantially pure.  
   
   
       22 . Form P-4 according to  claim 21 , wherein substantially pure is greater than 90 percent pure.  
   
   
       23 . Form P-4 of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione characterized by a differential scanning calorimetry (DSC) thermogram substantially in accordance with that shown in  FIG. 11 .  
   
   
       24 . Form P-4 of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione characterized by a thermo gravimetric analysis (TGA) diagram substantially in accordance with that shown in  FIG. 12 .  
   
   
       25 . Form P-1 of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione characterized by an X-ray powder diffraction pattern substantially in accordance with that shown in  FIG. 1 , a differential scanning calorimetry (DSC) thermogram substantially in accordance with that shown in  FIG. 2 , and a thermo gravimetric analysis (TGA) diagram substantially in accordance with that shown in  FIG. 3 .  
   
   
       26 . Form P-2 of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione characterized by an X-ray powder diffraction pattern substantially in accordance with that shown in  FIG. 4 , a differential scanning calorimetry (DSC) thermogram substantially in accordance with that shown in  FIG. 5 , and a thermo gravimetric analysis (TGA) diagram substantially in accordance with that shown in  FIG. 6 .  
   
   
       27 . Form P-3 of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione characterized by an X-ray powder diffraction pattern substantially in accordance with that shown in  FIG. 7 , a differential scanning calorimetry (DSC) thermogram substantially in accordance with that shown in  FIG. 8 , and a thermo gravimetric analysis (TGA) diagram substantially in accordance with that shown in  FIG. 9 .  
   
   
       28 . Form P-4 of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione characterized by an X-ray powder diffraction pattern substantially in accordance with that shown in  FIG. 10 , a differential scanning calorimetry (DSC) thermogram substantially in accordance with that shown in  FIG. 11 , and a thermo gravimetric analysis (TGA) diagram substantially in accordance with that shown in  FIG. 12 .

Join the waitlist — get patent alerts

Track US2006100432A1 — get alerts on status changes and closely related new filings.

We store only your email — no account needed. See our privacy policy.