1-pyrimidinylacetamide human leukocyte elastate inhibitors

Details 1-pyrimidinylacetamide human leukocyte elastate inhibitors 1-pyrimidinylacetamide human leukocyte elastate inhibitors

1993-04-08

1995-08-15

Gupta, Yogendra N.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

5142358, 544123, 544243, 544295, 544296, 544319, 544322, 544333, A61K 31505, C07D23922

Patent

active

054419603

ABSTRACT:
The present invention relates to certain novel substituted ketones which are 1-pyrimidinylacetamide derivatives of formula I, ##STR1## set out herein, 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 intermediates ##STR2## useful in the synthesis of these substituted ketones processes for preparing the substituted ketones pharmaceutical compositions containing such substituted ketones and methods for their use.

REFERENCES:
patent: 4923890 (1990-05-01), Trainor et al.
Rees et al., "Asymmetric Reduction of Dihydrofolate Using Dihydrofolate Reductase and Chiral Boron-containing Compounds," Tetrahedron, vol. 42, No. 1, pp. 117-136, 1986.
Frick et al., "C-NMR.-Spektren von 7,8-Dihydro-- und 5,6,7,8-Tetrahydrofolsaure," Helvetica Chimica Acta, vol. 57, Fasc. 8, No. 293, 1974.,

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