120072-79-9Relevant academic research and scientific papers
Alkoxy-substituted dihydrobenzopyran-2-carboxylate derivatives.
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, (2008/06/13)
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.
Di-and tetrahydronapthyl anti-allergy agents
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, (2008/06/13)
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.
Alkoxy-substituted dihydrobenzopyran-2-carboxylate derivatives
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, (2008/06/13)
This invention encompasses compounds of Formula 1 and the pharmaceutically acceptable salts thereof. STR1 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 (CH2)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; R4 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 CH2 ; B represents CH2, C=O or CH--OH; R5 represents hydrogen, alkyl having 1 to 6 carbon atoms, or R5 and R6 together optionally represent a carbon to carbon bond; or R5 represents alkanoyl having 2 to 4 carbon atoms, carboxy, alkoxycarbonyl, or (CH2)y--CO2 R8 wherein y is 0 to 4 and R8 is hydrogen or alkyl having 1 to 6 carbon atoms; and A represents --Z--CO2 R7 or --Z--COR9 R10 wherein R7 represents hydrogen or alkyl having 1 to 6 carbon atoms, R9, R10, represent hydrogen, alkyl having 1 to 6 carbon atoms, or cycloalkyl having 3 to 6 carbon atoms or NR9 R10 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 B4 (LTB4) with little or no antagonism of leukotriene D4 (LTD4) and are useful anti-inflammatory agents for treating inflammatory bowel disease, rheumatoid arthritis, gout and psoriasis.
