Lg Chemical Ltd.

Lg Chem-investment Ltd.

Kwang-Yul Moon

Jong Sung Koh

Ho Il Choi

Sung Chun Kim

Chang-Yuil Kang

Heungsik Yoon

Sang Soo Kim

Nakyen Choy

Young Chan Son

Chang Sun Lee

Chi Hyo Park

Mi-Jeong Park

Tae-Hee Lee

Chung Ryeol Kim

Wonhee Jung

Hye-Kyung Chang

Tae-Kyo Park

Eunice Eun-Kyeong Kim

Chang-Hee Min

Young-Myeong Kim

Young-Leem Oh

Hyun-Ho Chung

The present invention provides to an isoxazoline derivative of formula (I), the pharmaceutically acceptable salts, esters and stereochemically isomeric forms thereof, and the use of the derivative in inhibiting the activity of caspases. The present invention also provides a pharmaceutical composition for preventing inflammation and apoptosis which comprise the isoxazoline derivative, pharmaceutically acceptable salts, esters and stereochemically isomeric forms thereof and the process for preparing the same. The derivative according to the present invention can be effectively used in treating diseases due to caspases, such as, for example the disease in which cells are abnormally died, dementia, cerebral stroke, AIDS, diabetes, gastric ulcer, hepatic injury by hepatitis, sepsis, organ transplantation rejection reaction and anti-inflammation.

Isoxazoline derivative and a process for the preparation thereof

Novel cis-epoxide compounds of formula (I) are useful for treating or preventing diseases caused by HIV infection: ##STR1## wherein A, B, R.sub.1 to R.sub.4 and n have the same meanings as defined in the specification. The novel HIV protease inhibitor of the formula (I) has a specific structure to form a stable bonding with the enzyme active site, which entails a highly enhanced irreversible inhibition against HIV protease.

Irreversible HIV protease inhibitors, intermediates, compositions and

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Daejeon, South Korea

Kwang-Yul Moon