C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 5/083 (2006.01) A61K 38/05 (2006.01) A61K 38/06 (2006.01) C07K 5/06 (2006.01) C07K 5/062 (2006.01) A61K 38/00 (2006.01)
Patent
CA 2180006
The present invention relates to crystalline forms of the compound (S)-1-[(S)-2-(4- methoxybenzamido)-3-methylbutyryl]-N-[(S)-2-methyl- 1-(trifluoroacetyl)propyl]pyrrolidine-2-carboxamide (I) and crystalline solvates thereof 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 phrmaceutical compositions containing the crystalline forms and solvates, processes for preparing the crystalline forms and solvates and intermediates useful in the synthesis of the crystalline forms and solvates.
L'invention porte sur des formes cristallines du composé [(<u>S</u>)-1-[(<u>S</u>)-2-(4-méthoxybenzamido)-3-méthylbutyryl]-<u>N</u>-[(<u>S</u>)-2-méthyl-1-(trifluoroacétyl)propyl]pyrrolidine-2-carboxamide] et ses solvates cristallins inhibiteurs de l'élastase leucocytaire humaine (HLE), également dite élastase neutrophile humaine (HNE), utiles chaque fois qu'une telle inhibition est requise, par exemple comme outils de recherche en matière de pharmacologie, de diagnostic ou d'études associées et dans le traitement d'affections de mammifères où l'HLE intervient. L'invention porte également sur des compositions pharmaceutiques en contenant les formes cristallines et les solvates, leurs procédés de préparation, et sur les intermédiaires de synthèse de formes cristallines et de solvates.
Davies Elwyn Peter
Pegg Stephen John
Sependa George Joseph
Veale Chris Allan
Smart & Biggar
Zeneca Limited
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