Proline derivatives
AssigneeZeneca Limited
InventorsChris Allan Veale, Peter Robert Bernstein, Elwyn Peter Davies
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Abstract
The present invention relates to particular forms of a novel 1-substituted-N-2-methyl-1-(trifluoroacetyl)propyl!pyrrolidine-2-carboxam ide 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.
Claims15
A compound of formula I
- or a solvated form thereof, as a mixture of diastereomeric forms of said compound wherein said mixture is comprised of 50% or more of the diastereoisomer of formula Ia ##STR4## or a solvated form thereof.
The compound (S)-1-(S)-2-(methoxycarbonylamino)-3-methylbutyryl!-N-2-methyl- 1-(trifluoroacetyl)propyl!-pyrrolidine-2-carboxamide, or a solvate thereof, in the form of a diastereomeric mixture of (S)-1-(S)-2-(methoxycarbonylamino)-3-methylbutyryl-N-(S)-2-methyl-1-(tri fluoroacetyl)propyl!pyrrolidine-2-carboxamide or a solvate thereof, and (S)-1-(S)-2-(methoxycarbonylamino)-3-methylbutyryl!-N-(R)-2-methyl- 1-(trifluoroacetyl)-propyl!pyrrolidine-2-carboxamide or a solvate thereof, or in the form of the substantially or essentially pure diastereoisomer (S)-1-(S)-2-(methoxycarbonylamino)-3-methylbutyryl!-N-(S)-2-methyl- 1-(trifluoroacetyl)propyl!pyrrolidine-2-carboxamide or a solvate thereof.
A compound of formula Ib ##STR6## or a hydrated form thereof, or a pharmaceutically-acceptable salt thereof.
Dependencies are inferred from the claim text.