Compounds which inhibit beta-secretase activity and methods of use thereof

• Main Authors: LOY JEFFREY A, TURNER ROBERT T, KOELSCH GERALD E, BILCER GEOFFREY, TANG JORDAN J. N, HONG LIN, DEVASUMADRAM THIPPESWAMY, GHOSH ARUN K, CHANG WANPIN
• Format: Patent
• Language: English
• Published: 24.06.2004
• Edition: 7
• Subjects: BEER; BIOCHEMISTRY; CHEMISTRY; COMPOSITIONS OR TEST PAPERS THEREFOR; COMPOSITIONS THEREOF; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL ORENZYMOLOGICAL PROCESSES; CULTURE MEDIA; ENZYMOLOGY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIRCHEMICAL OR PHYSICAL PROPERTIES; MEASURING; MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEICACIDS OR MICROORGANISMS; MEDICAL OR VETERINARY SCIENCE; METALLURGY; MICROBIOLOGY; MICROORGANISMS OR ENZYMES; MUTATION OR GENETIC ENGINEERING; ORGANIC CHEMISTRY; PEPTIDES; PHYSICS; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; PROCESSES OF PREPARING SUCH COMPOSITIONS; PROPAGATING, PRESERVING OR MAINTAINING MICROORGANISMS; SPIRITS; TESTING; VINEGAR; WINE

Compounds inhibit memapsin 2 beta-secretase activity and selectively inhibit memapsin 2 beta-secretase activity relative to memapsin 1 beta-secretase activity. The compounds are employed in methods to inhibit memapsin 2 beta-secretase activity, in the treatment of Alzheimer's disease, in the inhibition of hydrolysis of a beta-secretase site of a betaamyloid precursor protein and to decrease beta-amyloid protein in in vitro samples and in mammals. Proteins of memapsin 2 associated with compounds of the invention are crystallized.