发明名称 |
Novel use of HIV protease inhibiting compounds |
摘要 |
<p>Use of ritonavir, saquinavir or their salts as proteasome modifying drugs is new. Use of at least one human immunodeficiency virus (HIV) protease inhibitor (I) selected from ritonavir, saquinavir and their salts, in combination with a pharmaceutical carrier, is claimed for the preparation of a medicament for modulating the proteasome. An independent claim is included for a method for screening for HIV protease inhibitors, involving testing the compounds for their ability to modulate proteasome activity. ACTIVITY : Antiinflammatory; immunoregulatory; antirheumatic; antiarthritic; antidiabetic; antipsoriatic; antiviral; cytostatic. Oral treatment with saquinavir at 4 mg per day for 7 days inhibited mouse paw edema, induced by injection of lymphocytic chorio-meningitis virus, by 73%. MECHANISM OF ACTION : HIV protease inhibitor; proteasome modulator. Proteasome is the central enzymatic protein degradation system, present in cytosol and cell nuclei and having multiple peptidase activity. (I) especially inhibit the chymotrypsin-like activity and increase the trypsin-like activity of proteasome; modify the presentation of antigens at the cell surface (in combination with the major histocompatibility complex class 1); and inhibit or modify the activation of cytotoxic CD8+> T lymphocytes.</p> |
申请公布号 |
EP1637139(A2) |
申请公布日期 |
2006.03.22 |
申请号 |
EP20050028334 |
申请日期 |
1999.06.11 |
申请人 |
INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM);BIOMERIEUX |
发明人 |
ANDRE, PATRICE;LOTTEAU, VINCENT;ZINKERNAGEL, ROLF;KLENERMAN, PAUL;GROETTRUP, MARCUS |
分类号 |
A61K31/426;A61K31/427;A61K31/4725;A61P3/10;A61P17/06;A61P19/02;A61P25/00;A61P29/00;A61P31/12;A61P31/18;A61P35/00;A61P37/02;A61P37/06;A61P43/00 |
主分类号 |
A61K31/426 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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