Patent ID: 6020382
Filing Date: 2000-02-01
Classification: A61K

Abstract:
A pharmaceutical composition which comprises a pharmaceutically acceptable carrier in combination with a compound of formula XI or XII: ##STR16## and ##STR17## or a pharmaceutically acceptable salt or acid addition salt thereof, wherein:each R is independently H, OH, alkyl of 1 to 6 carbon atoms which may be straight chain or branched; alkenyl of 2 to 6 carbon atoms which may be straight chain or branched; trifluoromethyl; alkoxy of 1 to 6 carbon atoms which may be straight chain or branched; SH; thioalkyl of 1 to 6 carbon atoms which may be straight chain or branched; phenyl; phenyl substituted by alkyl of 1 to 3 carbon atoms or by halogen; benzyl; phenethyl; halogen, amino; N(R.sub.4).sub.2 ; COOR.sub.4 ; CH.sub.2 OR.sub.4 ; formyl; CN; trifluoromethylthio; or nitro;R.sub.4 is H or alky of 1 to 6 caron atoms which may be straight or branched;each R' is independently R.sub.4 ; OR.sub.4 ; COOR.sub.4 ; N(R.sub.4).sub.2 ; SR.sub.4 ; CH.sub.2 OR.sub.4; CHO; or together R' and R' are O; CH.sub.2 ; or ##STR18## Y' is sulfur; sulfoxide; sulfone; ##STR19## NR.sub.12 ; ##STR20## N--CN; CH.sub.2 ; or C.dbd.O; R.sub.11 is H, alkyl of 1-4 carbon atoms which may be straight or branched, alkanoyl of 1-4 carbon atoms which may be straight or branched, phenylsuffonyl or tosyl;R.sub.12 is H or alkyl of 1-4 carbon atoms which may be straight or branched;R.sub.13 is alkyl of 1-4 carbon atoms which may be straight or branched, or alkoxy of 1-4 carbon atoms which may be straight or branched;Y is Y' and oxygen;each R.sub.1 is independently hydrogen or alkyl of 1-3 carbon atoms;each m is independently an integer from 0-6;R.sub.2 is ##STR21## each R.sub.6 is independently H or alkyl of 1-4 carbons; each R.sub.7 is independently H, OH, or alkyl of 1-4 carbons;each R.sub.8 is independently H, or alkyl of 1-4 carbons, and is absent when a triple bond is present;R.sub.5 is COOR.sub.4 ; CH.sub.2 OH; CHO; tetrazole; NHSO.sub.2 R.sub.14 ; hydroxymethylketone; CN; CON(R.sub.7).sub.2 ; a monocyclic or bicyclic heterocyclic ring containing an acidic hydroxyl group; or COOR.sub.15 where R.sub.15 is ##STR22## wherein each s is independently 0-3; R.sub.16 isA) a monocyclic or bicyclic heterocyclic radical containing from 3 to 12 nuclear carbon atoms and 1 or 2 nuclear heteroatoms selected from N and S with at least one being N, and with each ring in the heterocyclic radical being formed of 5 or 6 atoms, orB) the radical W-R.sub.17 wherein W is O, S or NH and R.sub.17 contains up to 21 carbon atoms and is (1) a hydrocarbon radical or (2) an acyl radical of an organic acyclic or monocyclic carboxylic acid containing not more than 1 heteroatom in the ring;R14 is OH, alkyl, or alkoxy of 1 to 6 carbon atoms, phenyl or phenyl substituted by alkyl or alkoxy groups of 1 to 3 carbon atoms, halogen, hydroxy, haloalkyl, COOH, CN, formyl, acyl of 1 to 6 carbon atoms or perfluoroalkyl of 1 to 4 carbon atoms;r and q are each independently 0-20 provided that the total of r and q does not exceed 20;p is 0 or 1;R.sub.3 is alkyl of 1 to 6 carbon atoms which may be straight or branched; or alkenyl of 3 to 6 carbon atoms which may be straight or branched;R.sub.9 is alkyl of 1 to 6 carbon atoms which may be straight or branched; alkoxy of 1 to 6 carbon atoms which may be straight or branched; or (CH.sub.2).sub.r R.sub.5 ; andR.sub.10 is H: alkyl of 1 to 6 carbon atoms which may be straight or branched; ##STR23## or R.sub.4 CH.sub.2 --.