Abstract: Benzenesulfonamides with a substituted-alkyl-S(O).sub.n -substituent are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.

Abstract: Aromatic sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.

Abstract: Selective .alpha..sub.2 -adrenergic receptor antagonists are effective in modifying gastrointestinal motility in a manner useful in the treatment of colonic spasm, irritable bowel syndrome and constipation.

Abstract: Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) or (II): ##STR1## wherein: n is 1 to 5;R is hydrogen or ##STR2## R.sup.1 is hydrogen or methyl; R.sup.2 is hydrogen or methyl; andR.sup.3 is hydrogen, C.sub.1-5 alkyl or C.sub.1-5 alkyl substituted with a member of the group consisting of phenyl, dimethylamino, or acetylamino; andthe dotted lines at a, b and c represent optional double bonds and pharmaceutically acceptable salts of the compounds (II) in which R.sup.3 is hydrogen are disclosed.

Abstract: Novel 2-sulfamoylbenzo[b]thiophenes and derivatives thereof are shown to be useful for the treatment of elevated intraocular pressure in compositions including ophthalmic drops and inserts.

Abstract: Thiophene-2-sulfonamides with a 5-alkyl-substituent are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.

Abstract: Hydroxyalkyl-phenoxy-propan-2-olamines and novel esters thereof are oculoselective .beta.-blockers useful in the treatment of elevated intraocular pressure with little or no effect on the pulmonary or cardiovascular system.

Abstract: Angiotensin converting enzyme inhibitors are useful in the treatment of senile macular degeneration.

Abstract: Novel tertiary aminohydroxypropoxy substituted aryl compounds exhibit .alpha..sub.1 -adrenoceptor and serotonin antagonism and are also useful as antihypertensive agents.

Abstract: Pharmaceutical compositions comprising 4-(dibenzo[a,d]cycloalkenyl)piperazine compounds and the use of said piperazine compounds for treatment of certain cardiovascular disorders are disclosed.

Abstract: This invention relates to a novel process for the preparation of 3-hydroxy-3-methylglutarylcoenzyme A (HMG-CoA) reductase inhibitors which contain a 4-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-one moiety, such as compactin and mevinolin, by utilizing an alkyl 4-cyano-3(R)-hydroxybutanoate as a chiral synthon for the stereospecific introduction of the 4-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-one moiety.

Abstract: A novel process for intermediates in the synthesis and hypercholesterolemic compounds of the HMG-CoA reductase type of the following general formula (1): ##STR1## involving an enantioselective aldol condensation is disclosed.

Abstract: The novel compounds of this invention and their pharmaceutically acceptable salts exhibit cardioselective .beta.-adrenergic blocking activity, with a direct relaxing effect on the .beta..sub.2 -adrenergic receptors and are useful as antihypertensive, cardioprotective, antiarrhythmic and, antianginal agents.

Abstract: 1-Aryloxy-3-(substituted aminoalkylamino)-2-propanols and pharmaceutically acceptable salts thereof have .beta.-adrenergic blocking activity with some cardioselectivity and hence are useful as antihypertensive, antianginal, antiarrhythmic and cardioprotective agents and in the treatment of elevated intraocular pressure such as glaucoma.

Abstract: An external bond at the 6-position of a 3,4,5,6-tetrahydro-2H-pyran-2-one, as found in the 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors, is readily epimerized by treating an amide of the corresponding hydroxy acid with a sulfonyl chloride reagent.

Abstract: 5-[2(or 3)-Hydroxyphenylsulfonyl]thiophene-2-sulfonamides are useful for the topical treatment of elevated intraocular pressure. Ophthalmic compositions including drops and inserts are disclosed.

Abstract: The compound 6(R)-[2-8(S)(2,2-dimethylbutyryloxy)-2(S),6(S)-dimethyl-1,2,3,4,4a(S),5,6, 7,8,8a(S)-decahydronaphthyl-1(S)ethyl]-4(R)-hydroxy-3,4,5,6-tetrahydro-2H-p yran-2-one is prepared in two steps from mevinolin and comprise reduction of the two double bonds and C-methylation of the 8(S)-(2-methylbutyryloxy) group to form the 2,2-dimethylbutyryloxy group. The two steps can be performed in either order.

Abstract: This invention relates to a novel process for the preparation of 3-hydroxy-3-methylglutarylcoenzyme A (HMG-CoA) reductase inhibitors which contain a 4-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-one moiety, such as compactin and mevinolin, by utilizing an alkyl 4-halo-3(S)-hydroxybutanoate as a chiral synthon for the stereospecific introduction of the 4-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-one moiety.

Abstract: Mevinolin, compactin and dihydro- and tetrahydro derivatives thereof are converted to more active HMG-CoA reductase inhibitors by C-methylation of the natural 2(S)-methylbutyryloxy side chain to form a 2,2-dimethylbutyryloxy side chain.

Abstract: The invention relates to an assembly for preparing and dispensing a solution and to the stopper for such an assembly, said assembly comprising a first bottle containing a first liquid component, with an elongated head; a second bottle containing a second component, liquid or solid; a stopper for this second bottle presenting a recess whose shape is homologous of the head of the first bottle, and in which said head is for example screwed. The bottom of the recess is constituted by a membrane of deformable material comprising an axial orifice which is hermetically closed, in the absence of deformation of the membrane, by the natural radial constriction of the material of the membrane. By screwing the first bottle in the stopper, the membrane is axially deformed and the orifice is radially distended, thus allowing the two bottles to be placed in communication in reversible manner. The invention also relates to a process for making the stopper.