JP2011522796A5 - - Google Patents
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- JP2011522796A5 JP2011522796A5 JP2011508615A JP2011508615A JP2011522796A5 JP 2011522796 A5 JP2011522796 A5 JP 2011522796A5 JP 2011508615 A JP2011508615 A JP 2011508615A JP 2011508615 A JP2011508615 A JP 2011508615A JP 2011522796 A5 JP2011522796 A5 JP 2011522796A5
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| US6239270B1 (en) | 1993-05-24 | 2001-05-29 | Rhone-Poulenc Rorer S.A. | Nucleic acids encoding human calcium sensor protein |
| AU6727798A (en) * | 1997-03-10 | 1998-09-29 | Roche Diagnostics Gmbh | Method for simultaneous detection of hiv antigens and hiv antibodies |
| US6790950B2 (en) | 1999-04-09 | 2004-09-14 | Pharmacia & Upjohn Company | Anti-bacterial vaccine compositions |
| CA2366520C (en) | 1999-04-09 | 2013-10-01 | Zoetis Services Llc | Anti-bacterial vaccine compositions |
| US7192713B1 (en) * | 1999-05-18 | 2007-03-20 | President And Fellows Of Harvard College | Stabilized compounds having secondary structure motifs |
| AUPQ776100A0 (en) | 2000-05-26 | 2000-06-15 | Australian National University, The | Synthetic molecules and uses therefor |
| US20020115606A1 (en) | 2000-10-17 | 2002-08-22 | Myriad Genetics, Inc. | Protein-protein interactions in neurodegenerative diseases |
| EP1997828B1 (en) * | 2003-11-05 | 2017-10-04 | Dana-Farber Cancer Institute, Inc. | Stabilized alpha helical peptides from BCL-2 and uses thereof |
| US20100159477A1 (en) | 2006-07-13 | 2010-06-24 | Peter Hornbeck | Reagents for the detection of protein phosphorylation in signaling pathways |
| US20100151483A1 (en) | 2006-07-13 | 2010-06-17 | Cell Signaling Technology, Inc. | Reagents for the detection of protein phosphorylation in signaling pathways |
| BRPI0715027A2 (pt) | 2006-09-11 | 2013-05-28 | Univ Illinois | modificaÇÕes dos peptÍdeos derivados da cupredoxina e seus mÉtodos de utilizaÇço |
| AU2007307254A1 (en) | 2006-10-05 | 2008-04-17 | New York Blood Center, Inc. | Stabilized therapeutic small helical antiviral peptides |
| US8937154B2 (en) | 2006-10-05 | 2015-01-20 | New York Blood Center, Inc. | Stabilized therapeutic small helical antiviral peptides |
| EP2952522B1 (en) | 2007-01-31 | 2019-10-30 | Dana-Farber Cancer Institute, Inc. | Stabilized p53 peptides and uses thereof |
| JP5078401B2 (ja) * | 2007-03-27 | 2012-11-21 | 株式会社Ａｄｅｋａ | 防水シート |
| JP5783721B2 (ja) * | 2007-09-26 | 2015-09-24 | ダナ ファーバー キャンサー インスティテュート インコーポレイテッド | Ｂｃｌ−２ファミリーポリペプチドを調節する方法及び組成物 |
| JP5788178B2 (ja) * | 2008-01-23 | 2015-09-30 | ダナ ファーバー キャンサー インスティテュート インコーポレイテッド | ウィルス感染症の治療のための組成物及び方法 |
| CA2725227A1 (en) * | 2008-05-06 | 2009-11-12 | Asim Kumar Debnath | Antiviral cell penetrating peptides |
| US20110218155A1 (en) * | 2008-10-10 | 2011-09-08 | Dana-Farber Cancer Institute, Inc. | Chemical modulators of pro-apoptotic bax and bcl-2 polypeptides |
-
2009
- 2009-05-05 CA CA2725227A patent/CA2725227A1/en not_active Abandoned
- 2009-05-05 WO PCT/US2009/042913 patent/WO2009137532A1/en not_active Ceased
- 2009-05-05 AU AU2009244400A patent/AU2009244400B2/en not_active Ceased
- 2009-05-05 US US12/436,080 patent/US8324153B2/en not_active Expired - Fee Related
- 2009-05-05 JP JP2011508615A patent/JP2011522796A/ja active Pending
- 2009-05-05 EP EP09743518A patent/EP2283033A1/en not_active Withdrawn
-
2012
- 2012-10-31 US US13/664,699 patent/US8933019B2/en active Active
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