The present invention is concerned with the therapeutic composition comprising as an active ingredient a compound of the formula: and salts thereof; wherein Ar and Ar.sub.1 are independently phenyl, naphthyl or a nitrogen, oxygen, or sulfur heterocyclic ring; Z is an alkylene chain containing from 1 to 5 carbon atoms in the principal chain and up to a total of 10 carbon atoms; M is oxygen, sulfur, or NR.sub.5 ; R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each independently H, lower alkyl, lower alkoxy, hydroxy, halo, trihalomethyl, hydroxy lower alkyl, carboxy, formyl, aryl, aryloxy, benzyloxy, lower alkanoyl, carboxy lower alkoxy, nitro, amino, lower alkylamino, dilower alkylamino, cyano, lower alkanoyloxy, carbamoyl, lower alkoxy-alkoxy, carbo-lower-alkoxy-alkoxy, or tetrahydropyranylmethyl; and R.sub.5 is hydrogen or lower alkyl.
There are disclosed compounds having the formula ##STR1## wherein X is CR or N when n=1; or X is O, S, NR or CR when n=0; R is hydrogen or lower alkyl; Y is --CH.sub.2 --, --S--, --O-- or ##STR2## and A is ##STR3## Z is CH or N; R.sup.1 is halo or trifluoromethyl; R.sup.2 is hydrogen or halo; R.sup.3 is hydrogen or halo; with the proviso that when A is naphthyl, Y is --O-- and n=0, X is other than S; and their use in the treatment of inflammatory conditions and in the treatment of leukotriene-medicated naso-bronchial obstructive passageway conditions.
The invention relates to new nitrogen-arylmethoxy-thiophene derivatives of the formula I ##STR1## wherein the R--CH.sub.2 --O-group is in position 4 or 5 of the thiophene ring, R denotes a 2-pyridinyl- or 2-quinolinyl group and R.sub.1 denotes a --COO-lower alkyl-, --CO--(CH.sub.2)n--CH.sub.3 or --CH(OH)--(CH.sub.2).sub.n --CH.sub.3 group, wherein n represents an integer from 2 to 6, and their hydrates and/or their pharmaceutically acceptable acid addition salts, a process for their preparation and pharmaceutical products containing these compounds. The new compounds and their salts have useful pharmacological properties. They can be used as active compounds for medicaments for the treatment and prevention of diseases, caused by a disturbance in arachidonic acid metabolism.
This invention relates to new lipoxygenase inhibitors possessing anti-inflammatory and anti-allergic properties. The present new compounds are of the formula: ##STR1## and salts thereof; wherein Ar is phenyl, naphthyl or sulfur, oxygen or nitrogen heterocyclic; X is O, S, NR.sub.5, or a chemical bond; R is H, lower alkoxy, aryloxy, hydroxy, lower alkyl, aryl or lower aralkyl; R.sub.1 and R.sub.2 are independently hydrogen, hydroxy, lower alkoxy, lower alkyl, aryl, aryloxy, lower aralkyl, lower aralkoxy, formyl, lower alkanoyl, benzoyl, and lower aralkanoyl; R.sub.3 and R.sub.4 are independently hydrogen, halogen, hydroxy, lower alkoxy, aryloxy, lower aralkoxy, trifluoromethyl, lower carbalkoxy, carboxy, cyano, nitro, lower alkyl, lower alkenyl, lower alkynyl, aryl or lower aralkyl; R.sub.5 is H, lower alkyl, lower aralkyl or aryl; R.sub.6 is hydroxy or hydroxy-substituted lower alkyl; n and m are independently 0, 1, 2 or 3.
This invention comprises novel carbocyclic compounds of formula I (wherein A, Z, R.sup.11 and R.sup.12 are defined in the specification) derived from acylsulfonamide derivatives of .alpha.-carbocyclyltoluic acids wherein said compounds of formula I antagonize the actions of one or more of the arachidonic acid metabolites known as leukotrienes. The invention also provides pharmaceutically acceptable salts of the formula I compounds; pharmaceutical compositions containing the formula I compound, or their salts, for use in the treatment of, for example, allergic or inflammatory diseases, or endotoxic or traumatic shock conditions; and processes for the manufacture of the formula I compounds, as well as intermediates for use in such manufacture.
This invention relates to a class of novel aliphatic amino bis-aryl compounds containing at least four carbon atoms and an amino group either substituted thereon or incorporated therein and is further linked or bridged to two mono- and/or bicyclic rings. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.