Abstract: This invention covers a compound of the formula ##STR1## wherein R is hydrogen, lower alkyl or a pharmaceutically acceptable, non-toxic salt of a compound wherein R is hydrogen; and X is hydrogen, halo, trifluoromethyl, lower alkyl or lower alkoxy; and the wavy lines represent the .alpha. or .beta. configuration with the proviso that when one wavy line is .alpha. the other is .beta..

Abstract: Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are each independently --H or lower alkoxy;R.sub.3 and R.sub.4 are each independently lower alkyl; andR.sub.5 and R.sub.6 are each --OCH.sub.3, or together form --OCH.sub.2 O-- or --OCH.sub.2 CH.sub.2 O--and pharmaceutically acceptable acid addition salts thereof are calcium channel blockers useful for treating cardiovascular disorders including angina, hypertension and congestive heart failure.

Abstract: Novel 5-aroyl-6-methylthio-, 6-methylsulfinyl-, or 6-methylsulfonyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids represented by the formulas ##STR1## and the pharmaceutically acceptable, non-toxic esters and salts thereof, whereinR.sub.1 is lower alkylthio, lower alkylsulfinyl, or lower alkylsulfonyl;R.sub.2 is hydrogen, hydroxy, lower alkyl, vinyl, cyclohexyl, cyclopropyl, lower alkoxy, fluoro, chloro, bromo, trifluoromethyl, trifluoromethoxy, nitro, amino, lower alkylcarbonylamino, lower alkylthio, lower alkylsulfonyl, or lower alkylsulfinyl;X is oxygen, sulfur, N--R.sub.3 where R.sub.3 is hydrogen or lower alkyl.This invention describes intermediates of the process and the process for the production of these compounds and their pharmaceutically acceptable non-toxic salts and pharmaceutical composition thereof. The claimed compounds are useful as anti-inflammatories and analgesics in mammals.

Abstract: Compounds useful in treating cardiovascular disorders such as thrombosis, hypertension, and atherosclerosis are compounds depicted in formulas (1), (2), and (3): ##STR1## wherein: n is 2 or 3;R.sub.1 is CH.sub.2 OH, CHO, CO.sub.2 R or CO.sub.2 H;R.sub.2 is hydrogen or methyl; andR.sub.3 is linear or branched alkyl having 5-10 carbon atoms, ##STR2## optionally substituted with lower alkyl, lower alkoxy, trifluoromethyl, or halogen,in whicha is 0, 1 or 2;b is 3-7;m is 1 or 2; andR is ##STR3## in which each R.sub.4 is independently hydrogen or lower alkyl having 1-6 carbon atoms,and the pharmaceutically acceptable, non-toxic salts and esters thereof.

Abstract: A method for enhancing the immunogenicity of an antigen is emulsifying it with a polyoxypropylene-polyoxyethylene block polymer, a glycol ether-based surfactant, a metabolizable non-toxic oil, isoosmotic saline, and an immunopotentiating amount of an immunostimulating glycopeptide.

Abstract: Combinations of 9-(1,3-dihydroxy-2-propoxymethyl) guanine or a pharmaceutically acceptable salt thereof, with .beta.-interferon show a surprisingly high degree of synergism in their activity against viral infections.

Abstract: This invention discloses novel glycosides which are potent inhibitors of cholesterol absorption and therefore useful in treating hypercholesterolemia and atherosclerosis. Particularly useful in this respect is glycoside tigogenin cellobioside. The method of use for treatment of hypercholesterolemia and atherosclerosis, and the suitable pharmaceutical compositions are also disclosed.

Abstract: This invention relates to a process for making an enantiomer or racemic mixture of a compound of the formula ##STR1## wherein R is hydrogen, lower alkyl or a pharmaceutically acceptable, non-toxic salt of a compound wherein R is hydrogen; X is hydrogen, halo, trifluoromethyl, lower alkyl or lower alkoxy, and the wavy lines represent the .alpha. or .beta. configuration with the proviso that when one wavy line is a .alpha. the other is .beta.; novel intermediates useful for preparing these compounds; and processes for making the intermediates.

Abstract: This invention provides a method for inhibiting angiogenesis in mammals. A pharmaceutically acceptable formulation containing a compound of the formula ##STR1## where X.sub.1 X.sub.2 and X.sub.3 are H, C1, or F and X.sub.3 must be H if the substituent of R.sub.1 is .alpha.OH;R.sup.1 is chosen from the group consisting of hydroxyl and hydrogen;R.sub.2 is chosen from the group of alkyloxy or thioalkyls wherein said alkyls have less than 5 carbon atomsR.sub.3 is H or an alkyl having less than 6 carbon atoms, is administered to the mammal having undesirable angiogenesis.The wavy line at C-16 refers to either .alpha. or .beta..

Abstract: Novel dihydropyridine derivatives which are useful for treating congestive heart failure, hypertension, and angina have the formula 1: ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein: n is an integer from 0 to 8;Y is --O, --NH, --NR.sub.2, --S, --S(O), --S(O).sub.2, or a bond;R.sub.1 and R.sub.2 are each independently A.sub.1, A.sub.2, A.sub.3 or A.sub.4 where:A.sub.1 is --(CH.sub.2).sub.m (CHOH).sub.p CH.sub.2 OH;A.sub.2 is --(CH.sub.2).sub.q CH.sub.(3-r) [(CH.sub.2).sub.s OH].sub.r ;A.sub.3 is --(CH.sub.2).sub.q CH.sub.(3-r) [(CH.sub.2).sub.p COOR.sub.3 ].sub.r ; andA.sub.4 is --(CH.sub.2).sub.m COOR.sub.3 ; where:m is an integer from 1 to 8;p is an integer from 0 to 4;q is an integer from 0 to 8;r is 2 or 3;s is an integer from 1 to 4; andR.sub.3 is H or alkyl of 1 to 18 carbon atoms;R.sub.4 is --NO.sub.2, --CF.sub.3, or halo; andR.sub.5 is lower alkyl or --CH.sub.2 CH.sub.2 OCH.sub.3.

Abstract: Novel compound of the formula ##STR1## wherein n is an integer of 1 to 8;R.sub.1 is hydrogen or alkyl of 1-6 carbons;R.sub.2 is hydrogen;R.sub.3 is hydrogen, alkyl of 1-6 carbons, phenyl, benzyl, hydroxy lower alkyl, carbamoyl alkyl, carboxyalkyl, alkoxycarbonylalkyl;R.sub.4 is hydrogen, alkyl of 1-6 carbons, benzyl, or hydroxy lower alkyl;Y is hydrogen, alkyl of 1 to 4 carbon atoms, halo or lower alkoxy;any of its optical isomers, the mixture thereof, or the pharmaceutically acceptable acid addition salt.These compounds are inhibitors of thromboxane synthetase and cyclic AMP phosphodiesterase and are therefore potential cardiovascular agents particularly useful as platelet aggregation inhibitors and anti-thrombotic agents. Accordingly, these compounds will preferably be useful in treating cardiovascular disorders with thrombotic complications. However, they also possess vasodilatory, antisecretory, antihypertensive, inotropic and antimetastatic activities.

Abstract: A novel pharmaceutical composition which comprises an acid salt of a thieno-pyridine derived compound, a pharmaceutically acceptable, non-volatile organic acid (particularly citric acid) and optionally other suitable pharmaceutical excipients.

Abstract: Synthetic nona-peptide and deca-peptide LHRH antagonist analogs have a novel guanido-substituted, amidine, tertiary or quaternary aminoacyl residue at position 6.

Abstract: A controlled release tablet for once-daily oral administration of about 500-1200 mg of naproxen or naproxen sodium, said tablet being a homogeneous matrix comprising about 4-9 weight percent of hydroxypropylmethylcellulose having a number average molecular weight in the range of from about 80,000 to about 130,000, about 81-96 weight percent naproxen or naproxen sodium, 0.1 to about 2 weight percent of a pharmacetucailly acceptable lubricating agent, and 0 to about 8 weight percent of other pharmaceutically acceptable excipients.

Abstract: Novel compounds of the general formula ##STR1## and the pharmaceutically acceptable esters and acid addition salts thereof, wherein:R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are each independently hydrogen, lower alkyl, lower alkoxy, cyano, trifluoromethyl, halo, lower alkylthio, lower alkyl sulfinyl, lower alkyl sulfonyl, N-optionally substituted alkylamido, except that when R.sup.1 is methyl, R.sup.4 is not methyl; orR.sup.2 and R.sup.3 together form --OCH.sub.2 O--;R.sup.6, R.sup.7, R.sup.8, R.sup.9 and R.sup.10 are each independently hydrogen, lower acyl, aminocarbonylmethyl, cyano, lower alkyl, lower alkoxy, trifluoromethyl, halo, lower alkylthio, lower alkyl sulfinyl, lower alkyl sulfonyl, di-lower alkyl amino; orR.sup.6 and R.sup.7 together form --CH.dbd.CH--CH.dbd.CH--;R.sup.7 and R.sup.8 together form --OCH.sub.2 O--;R.sup.11 and R.sup.12 are each independently hydrogen or lower alkyl; andW is oxygen or sulfur.

Abstract: Novel 5-(4-vinyl- or 4-ethynylbenzoyl)-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids represented by the formula ##STR1## and the pharmaceutically acceptable, non-toxic alkyl esters and salts thereof, wherein R is vinyl or ethynyl, and Y is hydrogen, a lower alkyl group having from 1 to 6 carbon atoms, chloro or bromo.

Abstract: Novel compounds of the general formula: ##STR1## and the pharmaceutically acceptable esters and acid addition salts thereof, wherein:R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8 and R.sup.9 are each independently hydrogen, lower alkyl, lower alkoxy, trifluoromethyl, halo, lower alkylthio, lower alkyl sulfinyl, lower alkyl sulfonyl; orR.sup.2 and R.sup.3 together form --OCH.sub.2 O--; andR.sup.10 and R.sup.11 are each independently hydrogen or lower alkyl.These compounds combine .beta.-blockade and calcium entry blockade properties in the same compound and therefore are useful in therapy in the treatment of cardiovascular diseases, including hypertension, arrhythmias and variant and exercise induced angina.

Abstract: This invention relates to a method of treatment of ocular hypertension and to a topical ophthalmic pharmaceutical composition useful for management of ocular hypertension.When administered topically to an eye with increased intraocular pressure, .+-.2-[(3,4-methylenedioxy)phenethyl]-5-[(3-carboxamido-4-hydroxy)-.alpha. -hydroxybenzyl]pyrrolidines effectively decrease intraocular pressure, inhibit the deterioration of the eye due to intraocular hypertension or glaucoma and relieve the symptoms of already existing glaucoma or other ophthalmic disease.

Abstract: Compounds useful in treating cardiovascular disorders are the carboxylic acids depicted in formulas (1) and (2) ##STR1## as well as their pharmaceutically acceptable, non-toxic salts and esters, wherein:n is an integer from one to four;R.sub.1 is hydroxy;R.sub.2 is hydrogen; orR.sub.1 and R.sub.2 together are an oxo group;R.sub.3 is ##STR2## wherein A is --CH.sub.2 --CH.sub.2 --; trans--CH.dbd.CH--; --C.tbd.C--; andR.sub.4 is linear or branched alkyl of one to twelve carbons, preferably 1-10 carbons, most preferably 3-8 carbons, cycloalkyl of three to eight carbons; phenyl optionally substituted with one or two identical substituents selected from the group consisting of lower alkyl, lower alkoxy, hydroxy, trifluoromethyl, and halo; or phenylloweralkyl optionally substituted with one or two identical substituents selected from the group consisting of lower alkyl, lower alkoxy, hydroxy, trifluoromethyl, and halo.

Abstract: A compound of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof are potent antihypertensive agents and are therefore useful as cardiovascular system regulators. These compounds are also useful as bronchodilators.