Substituted phenylacetylenes, pharmaceutical compositions...

C - Chemistry – Metallurgy – 07 – C

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C07C 275/64 (2006.01) A61K 31/16 (2006.01) A61K 31/33 (2006.01) C07C 259/06 (2006.01) C07D 213/42 (2006.01) C07D 213/56 (2006.01) C07D 215/14 (2006.01) C07D 317/60 (2006.01) C07D 333/04 (2006.01) C07D 333/20 (2006.01) C07D 333/28 (2006.01) C07D 333/58 (2006.01) C07D 333/60 (2006.01)

Patent

CA 2043823

Abstract Substituted phenylacetylenes of the formula Image wherein one of the groups R1 is a hydrogen atom and the other repre- sents the group of the formula Image in which R3 is hydrogen, methyl or ethyl and R4 is a methyl or an amino group and wherein R2 represents mono- or binuclear aromatic or heterocyclic residues containing sulfur, nitrogen or oxygen as hetero atoms and optionally being substituted by 1 to 3 substituents as defined, which specifically inhibit 5-lipoxygenase and are useful in pharmaceutical compositions for prophylaxis and treatment of diseases due to the ac- tion of leukotrienes. The compounds may be prepared by reacting a compound of the formula Image II wherein R2 has the same meaning as above and one of the groups R7 is a hydrogen atom and the other represents the group of the formula -COR3, with hydroxylamine to form the oxime which then is reduced to the cor- responding hydroxylamine compound into which the group of the formula -COR4 is introduced. This and other processes for the preparation of compounds of formula I are described.

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