98193-35-2Relevant articles and documents
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.
7-[3-(4-Acetyl-3-methoxy-2-propylphenoxy)propoxy]-3,4-dihydro-8-propyl- 2H-1-benzopyran-2-carboxylic acid: An orally active selective leukotriene B4 receptor antagonist
Djuric,Collins,Jones,Shone,Tsai,Fretland,Butchko,Villani-Price,Keith,Zemaitis,Metcalf,Bauer
, p. 1145 - 1147 (2007/10/02)
-
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.
