SULFONAMIDE INHIBITORS OF ASPARTYL PROTEASE

• Main Authors: MURCKO, MARK A, TUNG, ROGER D
• Format: Patent
• Language: English; Korean
• Published: 15.07.2000
• Edition: 7
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; COMPOUNDS OF UNKNOWN CONSTITUTION; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIRCHEMICAL OR PHYSICAL PROPERTIES; MEASURING; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PEPTIDES; PHYSICS; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS; TESTING

본 발명은 신규종의 아스파르틸 단백질 분해 효소 억제제인 하기 일반식(Ⅰ)의 설폰아미드에 관한 것이며, 일면 특이한 구조적 및 물리화학적 특성을 갖는 것을 특징으로 하는 신규종의 HIV 아스파르틸 단백질 분해 효소 억제제에 관한 것이다. 또한, 본 발명은 상기 화합물을 포함하는 약학적 조성물에 관한 것으로서, 본 발명에 의한 화합물 및 약학적 조성물은 특히 HIV-1 및 HIV-2 단백질 분해 효소의 활성을 억제하는데 매우 적합하며, 결과적으로 HIV-1 및 HIV-2 바이러스에 대한 항바이러스제로서 유리하게 사용될 수 있다. 또한, 본 발명은 본 발명의 화합물을 사용하여 HIV 아스파르틸 단백질 분해 효소의 활성을 억제하는 방법, 및 항-HIV 활성을 위해 화합물을 선별하는 방법에 관한 것이다: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors, of formula (I). In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as antiviral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.