Heterocyclic compounds, intermediates thereof and elastase...

C - Chemistry – Metallurgy – 07 – K

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C07K 5/103 (2006.01) A61K 38/55 (2006.01) A61P 11/00 (2006.01) A61P 43/00 (2006.01) C07D 233/34 (2006.01) C07D 239/54 (2006.01) C07D 403/12 (2006.01) C07K 5/02 (2006.01) C07K 5/083 (2006.01) C07K 5/097 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2362911

Heterocyclic compounds represented by general formula (I-a), its esters or salts thereof; and human neutrophilic elastase inhibitors, etc. containing the same as the active ingredient wherein A and B are the same of different and each represents lower alkylene optionally substituted by oxo; D represents a monocyclic or dicyclic heterocyclic group optionally substituted by oxo; R1 and R2 are the same or different and each represents lower alkyl; R3 and R4 are different from each other and each represents hydrogen or hydroxy, or R3 and R4 form together oxo; and R5 represents 2-benzoxasolyl, trifluoromethyl, benzylaminocarbonyle, etc.

La présente invention concerne des composés hétérocycliques représentés par la formule générale (I-a) et certains de leurs esters et sels. L'invention concerne également des inhibiteurs humains de l'élastase neutrophile et dont le principe actif est un tel composé (I-a). En l'occurrence, A et B, qui sont identiques ou différents, sont chacun alkylène inférieur éventuellement substitué par oxo; D est un groupe hétérocyclique monocyclique ou bicyclique éventuellement substitué par oxo; R?1¿ et R?2¿, qui sont identiques ou différents, sont chacun alkyle inférieur; R?3¿ et R?4¿, qui sont identiques ou différents, sont chacun hydrogène ou hydroxy, mais R?3¿ et R?4¿ peuvent également former ensemble un oxo; enfin, R?5¿ est notamment 2-benzoxazolyle, trifluorométhyle, benzylaminocarbonyle.

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