Proline derivatives useful as inhibitors of human leukocyte...

C - Chemistry – Metallurgy – 07 – K

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C07K 5/083 (2006.01) A61K 38/06 (2006.01) C07C 213/08 (2006.01) C07C 215/08 (2006.01) C07K 5/06 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2209675

The present invention relates to particular forms of a novel 1-substituted-N- [2-methyl-1-(trifluoroacetyl)propyl]pyrrolidine-2-carboxamide of formula (I) which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes pharmaceutical compositions containing such forms, processes for preparing the forms and intermediates useful in the synthesis of the forms.

La présente invention concerne des formes particulières d'un nouveau N-[2-méthyl-1-(trifluoroacétyl)propyl]pyrrolidine-2-carboxamide substitué en 1 correspondant à la formule (I), lesquelles formes sont des inhibiteurs de l'élastase de leucocytes chez l'homme, également connue sous le nom d'élastase neutrophile chez l'homme. Ces formes sont utiles lorsqu'une telle inhibition est jugée nécessaire, comme pour des outils de recherche dans les domaines de la pharmacologie, des diagnostics ou dans d'autres domaines apparentés, ou encore dans le traitement, chez les mammifères, de maladies dues à l'élastase de leucocytes chez l'homme. Cette invention concerne également des compositions pharmaceutiques contenant de telles formes, des procédés de préparation de ces formes, ainsi que des produits intermédiaires utiles dans la synthèse desdites formes.

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