- Alkoxy-substituted dihydrobenzopyran-2-carboxylate derivatives.
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This invention encompasses compounds of Formula 1 and the pharmaceutically acceptable salts thereof. wherein R1 represents alkyl having 2-6 carbon atoms; R2 represents methyl or ethyl; R3 represents alkyl having 1 to 5 carbon atoms; W represents (CH?)x where x is 2 to 7, alkylene having 2 to 7 carbon atoms, alkenylene having 3 to 7 carbon atoms, alkynylene having 3 to 7 carbon atoms, or cyclopentyl; R? represents hydrogen, alkyl having 2-5 carbon atoms, alkenyl having 2 to 5 carbon atoms, or alkynyl having 2 to 5 carbon atoms; Q represents oxygen or CH?; B represents CH?, C=O or CH-OH; R? represents hydrogen, alkyl having 1 to 6 carbon atoms, or R? and R? together optionally represent a carbon to carbon bond; or R? represents alkanoyl having 2 to 4 carbon atoms, carboxy, alkoxycarbonyl, or (CH?)y-CO?R? wherein y is 0 to 4 and R? is hydrogen or alkyl having 1 to 6 carbon atoms; and A represents-Z-CO?R? or-Z-COR?R1? wherein R? represents hydrogen or alkyl having 1 to 6 carbon atoms, R?, R1?, represent hydrogen, alkyl having 1 to 6 carbon atoms, or cycloalkyl having 3 to 6 carbon atoms or NR?R1? form a heterocyclic ring, and wherein Z is absent or represents straight or branched chain alkylene or alkenylene having up to 6 carbon atoms.These compounds are selective antagonists of leukotriene B?(LTB?) with little or no antagonism of leukotriene D? (LTD?) and are useful anti-inflammatory agents for treating inflammatory bowel disease, rheumatoid arthritis, gout and psoriasis.
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- Di-and tetrahydronapthyl anti-allergy agents
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This invention relates to compounds of the formula: and the pharmaceutically acceptable salts thereof:, wherein R1 represents straight or branched chain alkyl having 2-4 carbon atoms;, wherein R2 represents hydrogen or straight or branched chain alkyl having 1-6 carbon atoms;, wherein R3 represents hydrogen or straight or branched chain alkyl having 1-3 carbon atoms;, wherein R4 and R10 are different and represent H or n-propyl;, wherein X represents an interger from 2 to 5;, wherein R5 is hydrogen, or acts with R7 to produce an additional carbon--carbon bond between C1 and C2;, wherein R6 represents hydrogen or -Z-COOR9, wherein Z is either absent or represents straight or branched chain alkyl or alkenyl having 1-5 carbon atoms; and R9 represents hydrogen, pharmaceutically acceptable cations, or straight or branched chain alkyl having 1-6 carbon atoms;, wherein R7 is hydrogen, or acts together with R5 to form an additional carbon-carbon bond between C1 and C2, or acts together with R8 to form when R8 is oxygen;, wherein R8 is hydrogen, -O-R11, or oxygen, such that when R8 is oxygen, R8 acts together with R7 to form and, wherein R11 is straight or branched chain alkyl having 1-4 carbon atoms. The di- and tetrahydronaphthyl compounds of this invention are pharmacologically active as leukotriene D4 (LTD4) antagonists and are useful as anti--inflammatory and anti-allergy agents.
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- Benzoic acid derivatives and their production
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A benzoic acid derivative of the formula: STR1 wherein R1 stands for a lower alkyl group, R2 stands for an optionally protected carboxyl group and X stands for a halogen or a salt thereof, has excellent antiasthmatic and antiinflamma
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- Substituted dihydrobenzopyran-2-carboxylates
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The invention relates to substituted dihydrobenzopyrans carboxylates of the formula: STR1 wherein A is a methylene chain having 1-10 carbon atoms, inclusive, optionally substituted by hydroxy; wherein V is: (a) hydrogen; (b) hydroxy; (c) =O; or (d) R6 CH2 O--; wherein R1 is: (a) --COCH3 ; (b) --CHOHCH3 ; (c) --C2 H5 ; (d) -hydrogen; or (e) --COOC2 H5 wherein R2 is: (a) -hydrogen; (b) -hydroxy; or (c) R12 CH2 CO2 --; wherein R3, R4, R6, R7, R8, R9, R10, R11 and R12 each of which may be the same or different, are: (a) hydrogen; (b) lower-alkyl having 1-6 carbon atoms inclusive; or (c) allyl; wherein R5 is: (a) hydrogen; or (b) R7 CH2 C(O)--; wherein R13 is hydrogen, hydroxy, alkoxy of 1 to 6 carbon atoms inclusive, or --OM wherein M is an alkali metal, alkyl of 1 to 6 carbon atoms, inclusive, or NR8≈ R9 R10 R11, or HNR8≈ R9 R10, or the pharmacologically acceptable addition salts thereof, which are useful as leukotriene D4 (LTD4) inhibitors and therefore useful in the treatment of allergies and inflammatory conditions.
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- Chemical compounds
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There are provided compounds of formula I, STR1 wherein R1, R2, R3, R4, R5 and R7 may be the same or different, and are hydrogen, hydroxy, alkoxy, alkoxy substituted by phenyl, acyl, amino, acylamino, alkenyl, halogen, or alkyl, provided that at least one of R1, R2, R3 and R7 are other than hydrogen and hydroxy, Or an adjacent pair of R1, R2, R3 and R7 represent a chain --COCH=CH--O--, X is a hydrocarbon chain containing from 2 to 10 carbon atoms and optionally substituted by a hydroxy group, and E is a carboxy group or a tetrazole group, And pharmaceutically acceptable derivatives thereof. The compounds are indicated for use as antagonists of SRS-A.
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- Pharmaceutical compositions containing 4-carboxy-flavones
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There are provided processes for preparing compounds of the formula: STR1 (wherein R1, R2, R3 and R4, which may be the same or different, each represent hydrogen, hydroxy, alkenyl, alkanoyl or alkyl, and X repre
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- 4'-Carboxy-flavone
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There are provided compounds of the formula: SPC1 (wherein R1, R2, R3 and R4, which may be the same or different, each represent hydrogen, hydroxy, alkenyl, alkanoyl or alkyl, and X represents a hydrocarbon chai
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