Benzopyranols

A compound of formula (I):

• ##STR40## or, where appropriate, a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, in the form of a microfine powder wherein:
• one of A.sub.1 or A.sub.2 represents hydrogen and the other represents a group CF.sub.3 --Y-- wherein Y represents --CF.sub.2 --;
• Y.sub.1 represents --O--, R.sub.1 and R.sub.2 independently represent hydrogen or C.sub.1-12 alkyl;
• or R.sub.1 and R.sub.2 together represent a C.sub.2-7 polymethylene moiety;
• R.sub.3 represents hydrogen, hydroxy, C.sub.1-12 alkoxy or C.sub.1-12 alkylcarbonyloxy and R.sub.4 is hydrogen, or R.sub.3 and R.sub.4 together represent a bond;
• R.sub.5 represents either a moiety of formula (a):
• ##STR41## wherein A represents >C.dbd.X wherein X is O, S or NR.sub.8 wherein R.sub.8 represents CN, NO.sub.2, COR.sub.9 wherein R.sub.9 is C.sub.1-12 alkyl, amino, mono-C.sub.1-12 alkylamino, fluoro C.sub.1-12 alkyl comprising one or more fluorine atoms, phenyl or phenyl optionally substituted with up to five substituents selected from the group consisting of halogen, C.sub.1-12 alkyl, phenyl, C.sub.1-12 alkoxy, halo-C.sub.1-12 -alkyl, hydroxy, amino, nitro, carboxy, C.sub.1-12 alkoxycarbonyl, C.sub.1-12 alkoxycarbonylalkyl, C.sub.1-12 alkylcarbonyloxyl and C.sub.1-12 alkylcarbonyl or R.sub.8 is SO.sub.2 R.sub.9 wherein R.sub.9 is as defined above, or A represents a bond;
• when A represents >C.dbd.X wherein X is O or S, then R.sub.6 is hydrogen;
• C.sub.1-12 alkyl optionally substituted by one or more groups or atoms selected from halogen, hydroxy, C.sub.1-12 alkoxy, C.sub.1-12 alkoxycarbonyl, carboxy or an ester or amide thereof, amino, mono-C.sub.1-12 alkylamino, and di-C.sub.1-12 alkylamino;
• C.sub.2-12 alkenyl;
• amino optionally substituted by a C.sub.1-12 alkyl or C.sub.2-12 alkenyl group or by a C.sub.1-12 alkanoyl group optionally substituted by up to three halo atoms, by a phenyl group optionally substituted by C.sub.1-12 alkyl, C.sub.1-12 alkoxy or halogen;
• phenyl or naphthyl optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of C.sub.1-12 alkyl, C.sub.1-12 alkoxy, hydroxy, halogen, fluoro C.sub.1-12 alkyl comprising one or more fluorine atoms, nitro, cyano, carboxy or an ester thereof, C.sub.1-12 alkyl carbonyloxy, amino, mono-C.sub.1-12 alkylamino, and di-C.sub.1-12 alkylamino;
• aminocarbonyl, mono-C.sub.1-12 alkylaminocarbonyl, or di-C.sub.1-12 alkylaminocarbonyl;
• or 5- or 6-membered monocyclic heteroaryl moieties selected from the group consisting of furyl, thienyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl and thiadiazolyl, and pyridyl, pyridazyl, pyrimidyl, pyrrazyl and triazyl or 9- or 10-membered bicyclic heteroaryl groups selected from the group consisting of benzofuryl, benzothienyl, indolyl and indazolyl, quinolinyl and isoquinolinyl and quinazolinyl, optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of C.sub.1-12 alkyl, C.sub.1-12 alkoxy, hydroxy, halogen, fluoro C.sub.1-12 alkyl comprising one or more fluorine atoms, nitro, cyano, carboxy or an ester thereof, C.sub.1-12 alkylcarbonyloxy, amino, mono-C.sub.1-12 alkylamino, di-C.sub.1-12 alkylamino, aminocarbonyl, mono-C.sub.1-12 alkylaminocarbonyl and di-C.sub.1-12 alkylaminocarbonyl;
• and R.sub.7 represents hydrogen or C.sub.1-12 alkyl;
• or R.sub.6 and R.sub.7 together represent a linking chain of formula --A.sub.3 --A.sub.4 --, A.sub.3 being attached to the nitrogen atom of the moiety --N--A-- and A.sub.4 being attached to the group A on the said moiety, and wherein A.sub.3 represents a C.sub.1-12 alkyl- substituted or unsubstituted methylene group, A.sub.4 represents 2 or 3 linking members, one of the linking members optionally representing O, S or NR and the other linking members each independently representing a C.sub.1-12 alkyl- substituted or unsubstituted methylene group;
• R represents hydrogen, C.sub.1-12 alkyl, C.sub.1-12 alkanoyl, phenyl C.sub.1-4 alkyl, phenylcarbonyl or naphthylcarbonyl optionally substituted with up to five substituents selected from the group consisting of halogen, C.sub.1-12 alkyl, phenyl, C.sub.1-12 alkoxy, halo-C.sub.1-12 -alkyl hydroxy, amino, nitro, carboxy, C.sub.1-12 alkoxycarbonyl, C.sub.1-12 alkoxycarbonylalkyl, C.sub.1-12 alkylcarbonyloxy and C.sub.1-12 alkylcarbonyl;
• or R is furylcarbonyl, thienylcarbonyl or indolylcarbonyl;
• when A represents >C.dbd.X wherein X represents NR.sub.8, then R.sub.6 represents --NH.R.sub.10 wherein R.sub.10 is hydrogen, C.sub.1-12 alkyl C.sub.3-6 cycloalkyl, C.sub.2-12 alkenyl or C.sub.2-12 alkynyl and R.sub.7 is hydrogen or C.sub.1-12 alkyl;
• or R.sub.7 and R.sub.10 together represent C.sub.2-4 polymethylene;
• when A represents a bond, then R.sub.6 and R.sub.7 together with the nitrogen atom to which they are attached, form an unsaturated heterocyclic ring having 5 to 7 ring atoms, selected from the group consisting of unsubstituted pyridonyl, pyridonyl substituted with C.sub.1-12 -alkyl, hydroxyl, halogen, alkoxy, alkanoyloxy, nitro, amino, C.sub.1-12 alkylcarbonyl amino, carboxy or alkoxy carbonyl, unsubstituted thiopyridonyl, or thiopyridonyl substituted with C.sub.1-12 -alkyl, hydroxyl, halogen, alkoxy, alkanoyloxy, nitro, amino, C.sub.1-12 alkylcarbonyl amino, carboxy or alkoxy carbonyl, or R.sub.5 represents a moiety of formula (c):
• ##STR42## wherein L.sub.1 represents O or NR.sub.11 wherein R.sub.11 represents hydrogen, C.sub.1-12 alkyl, formyl, acetyl or hydroxymethyl, L.sub.2 represents N or CL.sub.4 wherein L.sub.4 is hydrogen, halogen, formyl or hydroxymethyl, L.sub.3 represents CH.sub.2, O, S, >CHL.sub.5 wherein L.sub.5 is halogen or NL.sub.6 wherein L.sub.6 is hydrogen or C.sub.1-12 alkyl and R.sub.12 and R.sub.13 each independently represent hydrogen or C.sub.1-12 alkyl or R.sub.12 together with R.sub.13 represents oxo or thioxo;
• and p represents 1, 2 or 3.