98193-35-2Relevant academic research and scientific papers
Alkoxy-substituted dihydrobenzopyran-2-carboxylate derivatives.
-
, (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.
Alkoxy-substituted dihydrobenzopyran-2-carboxylate derivatives
-
, (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.
Substituted dihydrobenzopyrans useful as leukotriene D4 inhibitors
-
, (2008/06/13)
The invention relates to compounds of the formula: STR1 which are useful as leukotriene D4 (LTD4) inhibitors and therefore useful in the treatment of allergies and inflammatory conditions.
Substituted dihydrobenzopyran-2-carboxylates
-
, (2008/06/13)
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.
