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: 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 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: 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: 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.

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.

Abstract: Compounds of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein; Y is halo, alkoxy, alkyl, or dialkylamino;a is 0, 1 or 2;b is an integer from 2-12 with the proviso that if b is 2 or 3 a cannot be 0; andX is selected from the group consisting of: --OH, OR.sup.1, --NH.sub.2, --NHR.sup.1, NR.sub.2.sup.1, ##STR2## and --NHCONHR.sup.2 in which each R.sup.1 is independently alkyl or cycloalkyl or in --NR.sub.2.sup.1, both R.sup.1 together are alkylene or form a piperazine ring optionally substituted at the ring N by alkyl or --CH.sub.2 CH.sub.2 OH; andR.sup.2 is alkyl, cycloalkyl, or optionally substituted phenyl;have antiinflammatory properties and are useful in the treatment of conditions characterized by inflammation and swelling.

Abstract: Compounds of the formula: ##STR1## and the pharmaceutically acceptable, non-toxic salts and esters (alkyl, 1-6C) thereof, wherein:X is O or S;R.sup.1 is selected from the group consisting of:(a) alkyl or cycloalkyl of 3-8 carbons,(b) ##STR2## in which Z is O, S or --CH.sub.2, and Y is lower alkyl (1-4C), lower alkoxy (1-4C), halo, or --CF.sub.3, and(c) ##STR3## in which Z and X are as herein defined; and R.sup.2 is hydrogen or methyl;exhibit prostaglandin-like activity and are, thus, useful as platelet aggregation inhibitors.

Abstract: Compounds of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein: Z is S;Y is halo, alkoxy, alkyl, or dialkylamino;a is 0, 1 or 2;b is an integer from 2-12 with the proviso that if b is 2 or 3, a cannot be 0, and with the further proviso that if X is OH, b cannot be 2-5 and with the further proviso that if X is --NH.sub.2, b cannot be 2-5; andX is selected from the group consisting of: --OH, OR.sup.1, --NH.sub.2, --NHR.sup.1, NR1/2, ##STR2## and --NHCONHR.sup.2 in which each R.sup.1 is independently alkyl or cycloalkyl or, in --NR1/2, both R.sup.1 s together are alkylene or form a piperazine ring optionally substituted at the ring N by alkyl or --CH.sub.2 CH.sub.2 OH; andR.sup.2 is alkyl, cycloalkyl, or optionally substituted phenyl;have antiinflammatory properties and are useful in the treatment of conditions characterized by inflammation and swelling.

Abstract: 5-benzoyl-7-halo-1,2-dihydro-3H-pyrrolo[1,2-a]-pyrrole-1-carboxylic acids, represented by the formula ##STR1## and the pharmaceutically acceptable non-toxic esters and salts thereof, wherein:R is hydrogen or lower alkyl;X is hydrogen, lower alkyl, lower alkoxyl, lower alkoxycarbonyl, carboxyl, lower alkylcarbonyl, sulfonic acid, sulfonic acid alkyl ester, fluoro, chloro, or bromo; and Y is chloro or bromo, which are novel, and 5-benzoyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids which are represented by the formula ##STR2## wherein X and R are as above defined except that X cannot be chloro or bromo, are prepared by decarboxylation of the corresponding 1,1 dicarboxylates. Intermediates in said preparation are also disclosed.

Abstract: 5-Substituted-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids of the formula ##STR1## wherein: X is hydrogen or lower alkyl; Ar is a moiety selected from the group consisting of ##STR2## in which: Y is oxygen or sulfur;R is hydrogen, methyl, chloro, or bromo, the R substitution being at the 3, 4 or 5 position of the ring;R.sup.1 is hydrogen, lower alkyl, lower alkoxyl, lower alkoxycarbonyl, lower alkylcarbonyl, fluoro, chloro or bromo, the R.sup.1 substitution being at any available position in the ring;R.sup.2 is hydrogen or lower alkyl;are prepared by .beta.-decarboxylation of the corresponding dialkyl-1,1-dicarboxylates. Certain substituted pyrroles are useful as intermediates for preparing the compounds of formula I.

Abstract: 5-benzoyl-7-halo-1,2-dihydro-3H-pyrrolo[1,2-a]-pyrrole-1-carboxylic acids, represented by the formula ##STR1## and the pharmaceutically acceptable non-toxic esters and salts thereof, wherein:R is hydrogen or lower alkyl;X is hydrogen, lower alkyl, lower alkoxyl, lower alkoxycarbonyl, carboxyl, lower alkylcarbonyl, sulfonic acid, sulfonic acid alkyl ester, fluoro, chloro, or bromo; and Y is chloro or bromo, which are novel, and 5-benzoyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids which are represented by the formula ##STR2## wherein X and R are as above defined except that X cannot be chloro or bromo, are prepared by decarboxylation of the corresponding 1,1 dicarboxylates. Intermediates in said preparation are also disclosed.

Abstract: 5-Substituted-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids of the formula ##STR1## wherein: X is hydrogen, lower alkyl, chloro or bromo; Ar is a moiety selected from the group consisting of ##STR2## in which: Y is oxygen or sulfur;R is hydrogen, methyl, chloro, or bromo, the R substitution being at the 3, 4 or 5 position of the ring;R.sup.1 is hydrogen, lower alkyl, lower alkoxyl, lower alkoxycarbonyl, lower alkylcarbonyl, fluoro, chloro or bromo, the R.sup.1 substitution being at any available position in the ring;R.sup.2 is hydrogen or lower alkyl;are prepared by .beta.-decarboxylation of the corresponding dialkyl-1,1-dicarboxylates. Certain substituted pyrroles are useful as intermediates for preparing the compounds of formula I.

Abstract: Delivery systems for releasing macromolecular active agents to a body site at a controlled rate for a prolonged period of time, comprising a cholesteric matrix permeable to passage of the macromolecular active agent by diffusion, are disclosed. The cholesteric matrix comprises cholesterol powder and cholesterol prills optionally in combination with a binding agent and a lubricating agent. The macromolecular active agent is dispersed throughout the matrix; macromolecules suitable for release from this delivery system have molecular weights of about 1300 to about 75,000 and are at least very slightly soluble in water.

Abstract: Methods of controlling fecal output and of appetite control, and compositions therefor, employing a fiber-containing mixture of cellulose with CMC, are described.

Abstract: Compounds of the formula: ##STR1## and the pharmaceutically acceptable, non-toxic salts and esters (alkyl, 1-6C) thereof, wherein:X is O or S;R.sup.1 is selected from the group consisting of:(a) alkyl or cycloalkyl of 3-8 carbons, ##STR2## R.sup.2 is hydrogen or methyl; exhibit prostaglandin-like activity and are, thus, useful as platelet aggregation inhibitors.