Isoxazoline derivative and a process for the preparation thereof

   
   

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.

A invenção atual fornece a um derivative do isoxazoline da fórmula (i), os sais pharmaceutically aceitáveis, os esters e formulários stereochemically isomeric disso, e o uso do derivative em inibir a atividade dos caspases. A invenção atual fornece também uma composição pharmaceutical impedindo o inflammation e o apoptosis que compreendem os sais derivative, pharmaceutically aceitáveis do isoxazoline, esters e formulários stereochemically isomeric disso e o processo para preparar o mesmo. O derivative de acordo com a invenção atual pode eficazmente ser usado nas doenças de tratamento devido aos caspases, como, para o exemplo a doença em que as pilhas são morridas anormalmente, dementia, curso cerebral, AIDS, diabetes, ulcer gastric, ferimento hepatic pelo hepatitis, sepsis, reação da rejeção do transplantation do órgão e anti-inflammation.

 
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