ZA200306887B - Pyrazolopyrimidines as therapeutic agents. - Google Patents
Pyrazolopyrimidines as therapeutic agents. Download PDFInfo
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- ZA200306887B ZA200306887B ZA200306887A ZA200306887A ZA200306887B ZA 200306887 B ZA200306887 B ZA 200306887B ZA 200306887 A ZA200306887 A ZA 200306887A ZA 200306887 A ZA200306887 A ZA 200306887A ZA 200306887 B ZA200306887 B ZA 200306887B
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- 2002-03-22 KR KR10-2003-7012350A patent/KR20030088114A/ko not_active Withdrawn
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- 2002-03-22 PE PE2002000222A patent/PE20030047A1/es not_active Application Discontinuation
- 2002-03-22 CZ CZ20032837A patent/CZ20032837A3/cs unknown
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- 2002-03-22 WO PCT/US2002/008996 patent/WO2002076986A1/en not_active Ceased
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| JP4319412B2 (ja) | 2009-08-26 |
| IL157640A0 (en) | 2004-03-28 |
| BR0205890A (pt) | 2004-06-29 |
| MXPA03008560A (es) | 2004-06-30 |
| BG108268A (en) | 2005-04-30 |
| EP1379528A4 (en) | 2005-12-07 |
| WO2002076986A1 (en) | 2002-10-03 |
| CA2440714C (en) | 2010-08-10 |
| UY27222A1 (es) | 2002-10-31 |
| JP2005501811A (ja) | 2005-01-20 |
| KR20030088114A (ko) | 2003-11-17 |
| PE20030047A1 (es) | 2003-02-07 |
| US20040006083A1 (en) | 2004-01-08 |
| NO20034177L (no) | 2003-11-21 |
| EP1379528A1 (en) | 2004-01-14 |
| CZ20032837A3 (cs) | 2004-01-14 |
| ECSP034773A (es) | 2003-12-24 |
| US7332497B2 (en) | 2008-02-19 |
| HUP0400267A2 (hu) | 2004-08-30 |
| CN101426792A (zh) | 2009-05-06 |
| CO5570669A2 (es) | 2005-10-31 |
| CA2440714A1 (en) | 2002-10-03 |
| NO20034177D0 (no) | 2003-09-19 |
| SK13122003A3 (sk) | 2004-04-06 |
| PL363946A1 (en) | 2004-11-29 |
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