C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
167/231, 167/233
C07D 491/052 (2006.01) A61K 31/40 (2006.01) A61K 31/44 (2006.01) C07D 311/92 (2006.01) C07D 311/94 (2006.01) C07D 491/04 (2006.01) C07D 493/04 (2006.01) C07D 495/04 (2006.01)
Patent
CA 1268460
ABSTRACT There are provided benzopyrans of formula I, Image I wherein an adjacent pair of R5, R6, R7 and R8 represent the chain -X-CR12R13-CR14R15-NR20- in which the chain is substituted by -A1E1, X represents CR10R11 or a single bond, and (a) R14 and R20 together form a single bond and optionally R10 and R12 together form a single bond, or (b) R12 and R14 together form a single bond, or (c) R10, R12 and R14 each represent hydrogen; and the remainder of R10, R11, R12, R13, R14, and R15, which may be the same or different, independently represent hydrogen, alkyl, NR21COR22. CN or CnHxF(2n+1-x); in addition, a geminal pair of R10, R11, R12, R13, R14, R15, R16, and R17 together with the carbon atom to which they are attached, may represent C=O or C=N-OR23; also a vicinal pair of R11, R13, and R15, may form the chain -CH=CH-CH=CH- which is substituted by A1E1, A and A1, which may be the same or different, represent a single bond, (CH2)m or arylene, n represents an integer from 1 to 10 inclusive, x represents 0 or an integer from 1 to 2n inclusive, m represents an integer from 1 to 10 inclusive, when R20 does not form a single bond with R14, R20 may represent hydrogen, alkyl, aryl or alkyl substituted by aryl, R21, R22, and R23, which may be the same or different, independently represent hydrogen, alkyl or aryl; the remainder of R5, R6, R7 and R8, which may be the same or different, each independently represent hydrogen, hydroxy, alkoxy, amino, halogen, nitro, cyano, alkyl, aryl or alkyl substituted by aryl, E and E1, which may be the same or different, independently represent -COOH, or 5H-tetrazolyl, provided that when the chain -X-CR12R13- CR14R15-NR20- i) represents a chain -CO-CR13=CR15-NR20-, in which one of R13 and R15 represents E1, then E1 represents hydrogen, and ii) represents a chain -CR=CR13-CR15=N-, then at least one of R11, R13 or R15, which may be the same or different, represents NR21COR22, CN or CnHxF(2n+1-x), and pharmaceutically acceptable derivatives thereof. There are also described processes to the compounds of formula I and pharmaceutical, e.g. anti-asthma, compositions containing them.
472848
Dicker Ian D.
Suschitzky John L.
Dicker Ian D.
Fisons Plc
Ridout & Maybee Llp
Suschitzky John L.
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