HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS

HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS

Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein each variable in Formula 1 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of i...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Hauptverfasser: Saionz, Kurt W, Hunter, Rachael C, Shao, Yuefei, Smith, Elizabeth M, Sun, Zhong-Yue, Tadesse, Dawit, Wu, Yusheng, Zhu, Zhaoning, Voigt, Johannes H, Strickland, Corey, Le, Thuy X.H, Qian, Gang, Gu, Huizhong, Lai, Gaifa, Mazzola, Robert D, Pan, Jianping, Guo, Tao, Duo, Jingqi, Iserloh, Ulrich, McKittrick, Brian, Liu, Xiaoxiang, Li, Guoqing, Ye, Yuanzan C, Huang, Ying, Misiaszek, Jeffrey A, Caldwell, John, Cumming, Jared N, Morris, Michelle L, Qu, Chuanxing, Stamford, Andrew, Greenlee, William J, Babu, Suresh D, Wang, Lingyan
Format: Patent
Sprache:hrv ; eng
Schlagworte:
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Beschreibung
Zusammenfassung:Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein each variable in Formula 1 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.