Thiophene amino acid derivatives, process for preparing them and pharmaceutical compositions containing them

   
   

The invention provides compounds of Formula (I), 1 stereoisomers thereof, or pharmaceutically acceptable salts of said compounds or stereoisomers, wherein R.sub.1, R.sub.2, m, p, q, R.sub.7 and R.sub.8 are as defined below, as well as compositions comprising the same, processes for making the same, and methods of using the same to treat a variety of diseases, including, those requiring interaction with metalloproteases, and more specifically with macrophage metalloelastase (MMP-12), and for the prevention and treatment of respiratory pathologies such as chronic obstructive bronchopneumopathy (COPD), emphysema, chronic bronchitis, chronic pulmonary inflammation, asthma, cystic fibrosis, acute respiratory distress syndrome (ARDS), respiratory allergies including allergic rhinitis, and also diseases associated with the production of TNF.alpha. including severe fibrotic pulmonary disease, pulmonary sarcoidosis and silicosis. The compounds of the present invention also show inhibitory activity on metalloprotease-13 (MMP-13), making them useful for the treatment of pathologies involving this enzyme, such as cancer, osteoporosis, osteoarthritis, arthritis, rheumatoid arthritis, atherosclerosis, multiple sclerosis and cardiac insufficiency.

A invenção fornece compostos da fórmula (i), stereoisomers 1 disso, ou pharmaceutically sais aceitáveis de compostos ou de stereoisomers ditos, wherein R.sub.1, R.sub.2, m, p, q, R.sub.7 e R.sub.8 são como definidos abaixo, as.well.as as composições que compreendem o mesmo, processos para fazer o mesmo, e métodos de usar o mesmo tratar uma variedade das doenças, incluindo, daquelas que requerem a interação com os metalloproteases, e mais especificamente com o metalloelastase do macrophage (MMP-12), e para a prevenção e o tratamento de pathologies respiratory tais como bronchopneumopathy obstructive crônico (COPD), emphysema, bronchitis crônico, inflammation pulmonary crônico, asthma, o fibrosis cystic, o syndrome respiratory agudo da aflição (ARDS), os allergies respiratory including o rhinitis allergic, e também as doenças associaram com a produção de TNF.alpha. including a doença pulmonary fibrotic severa, o sarcoidosis pulmonary e o silicosis. Os compostos da invenção atual mostram também a atividade inhibitory em metalloprotease-13 (MMP-13), fazendo o útil para o tratamento dos pathologies que envolvem este enzyme, tal como o cancer, o osteoporosis, a osteodistrofia, o arthritis, o arthritis rheumatoid, o atherosclerosis, o sclerosis múltiplo e o insufficiency cardiac.

 
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