Acetohydroxamic compound and complexes pharmaceutical compositio

Details Acetohydroxamic compound and complexes pharmaceutical compositio Acetohydroxamic compound and complexes pharmaceutical compositio

1992-07-10

1993-10-12

Russell, Mark

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Carbohydrate doai

514438, 549 76, 536103, A61K 3170, A61K 3138, C07D 3370

Patent

active

052525627

ABSTRACT:
An acetohydroxamic acid compound of formula I ##STR1## as such or in form of a complex with .beta.-cyclodextrin or hydroxypropyl-.beta.-cyclodextrin specifically inhibits 5-lipoxygenase and is useful in pharmaceutical compositions for prophylaxis and treatment of diseases due to the action of leucotrienes. The acetohydroxamic acid compound may be prepared by reacting 3-thiophenecarboxaldehyde with hydroxylamine or a salt thereof to form the corresponding oxime, reducing the oxime with a boron-containing reducing agent to form N-(thien-3-yl)methyl-hydroxylamine, and introducing an acetyl group.

REFERENCES:
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patent: 5011854 (1991-04-01), Takahashi et al.
patent: 5026729 (1991-06-01), Brooks et al.
patent: 5036157 (1991-07-01), Kneen et al.
R. Morrison et al., "Organic Chemistry" 3rd ed., pp. 639-641, Allyn and Bacon, Inc., Boston (1973).
Summers et al., "Orally Active Hydroxamic Acid Inhibitors of Leukotriene Biosynthesis", J. Med. Chem., 31, 3-5 (1988).
Tateson et al., in Brit. J. Pharmacol., 94, 528 to 539 (1988).
J. B. Summers et al., J. Med. Chem., 31, 1960 (1988).
H. Konzett et al. Naunyn Schniedeberg's Arch. Exp. Path. Pharma., vol. 195, 71 to 74 (1940).

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