- Derivatives of hydroxyphenylsulfanylbenzoic and hydroxphenylsulfanylarylacetic acids
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Processes for the preparation of derivatives of hydroxyphenylsulfanylbenzoic and hydroxyphenylsulfanylarylacetic acids of Formula (I) and pharmaceutical compositions including these compounds are provided: wherein X is H, halogen or NO2group, n is 0 or 1, and m is 2 to 4 if Z is either 4-acetyl-3 -hydroxy-2-propylphenoxy of Formula (II): or a piperazinyl residue, or m is 1 if Z is quinolin-2-yl or 6-chloroquinoli-2-yl.
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- 2,4-dihydroxyacetophenone derivatives as antileukotrienics with a multiple activity mechanism
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A series of 2,4-dihydroxy-3-propylacetophenone derivatives containing alkylthiobenzoic or arylacetic acid moiety was prepared. The antileukotrienic activity of the substances was assessed in terms of inhibition of the biosynthesis of LTB4 and b
- Kuchar, Miroslav,Culikova, Katerina,Panajotovova, Vladimira,Brunova, Bohumila,Jandera, Antonin,Kmonicek, Vojtech
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p. 103 - 114
(2007/10/03)
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- Leukotriene LTD4 and LTB4 antagonists
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This invention encompasses compounds of Formula I STR1 and the pharmaceutically acceptable salts and geometrical and optical isomers thereof wherein: X, Y, and Z are each independently O or S with S optionally oxidized to S=O; Alk is straight or branched chain alkylene or hydroxyalkylene containing 1-6 carbon atoms; R1 is hydrogen or lower alkyl; n is 0 to 5; R2 is hydrogen, lower alkyl, cycloalkyl, --(CH2)n --CO2 R1, phenyl, phenyl substituted with halo, lower alkyl or lower alkoxy; and Ar is 5,6,7,8-tetrahydro-1-naphthalenyl, phenyl, or phenyl substituted with lower alkyl, hydroxy, lower alkoxy, or lower alkanoyl. This invention is in the field of pharmaceutical agents which act as leukotriene D4 (LTD4) antagonists and includes embodiments which act as leukotriene B4 (LTD4) antagonists.
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- Disubstituted tetrazole leukotriene antagonists and methods for their use thereas
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The instant invention provides disubstituted tetrazoles that antagonizes the effect of leukotrienes C4, D4 or E4 or any combination thereof in selected tissues. The disubstituted tetrazoles are used in pharmaceutical formulations and methods of treatment of conditions caused by excessive release or production of leukotrienes C4, D4 or E4 or any combination thereof. Such conditions include an immediate hypersensitivity reaction of the type represented by asthma, or by shock or other adverse cardiovascular effects.
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- Leukotriene LTD4 and LTB4 antagonists
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The invention encompasses compounds of Formula I STR1 and the pharmaceutically acceptable salts and geometrical and optical isomers thereof wherein: X, Y, and Z are each independently O or S with S optionally oxidized to S=O; Alk is alkylene or hydroxyalkylene containing 1-6 carbon atoms; R1 is hydrogen or lower alkyl; n is 0 to 5; R2 is hydrogen, lower alkyl, cycloalkyl, --(CH2)n --CO2 R1, phenyl, phenyl substituted with halo, lower alkyl or lower alkoxy; and Ar is 5,6,7,8-tetrahydro-1-naphthalenyl, phenyl, or phenyl substituted with lower alkyl, hydroxy, lower alkoxy, or lower alkanoyl. The compounds are useful as anti-allergy agents and anti-inflammatory agents.
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- Thiadiazole compounds as antagonists of SRS-A
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Novel heterocyclic compounds shown by the general formula STR1 or the pharmaceutically acceptable salts thereof useful as medicament in particular as antagonist of slow reacting substance of anaphylaxis (SRS-A).
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- Leukotriene receptor antagonists. 1. Synthesis and structure-activity relationships of alkoxyacetophenone derivatives
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A series of derivatives of 2,4-dihydroxy-3-propylacetophenone were prepared and examined for their ability to block leukotriene D4 (LTD4) induced contraction of guinea pig ileum. Straight-chain carboxylic acids where the carboxyl gro
- Marshall,Goodson,Cullinan,Swanson-Bean,Haisch,Rinkema,Fleisch
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p. 682 - 689
(2007/10/02)
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