Abstract: A controlled release tablet for once-daily oral administration of about 500-1200 mg of naproxen or naproxen sodium, said tablet comprising a homogeneous matrix comprising about 4-9 weight percent of hydroxypropyl methylcellulose 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, and 0.1 to about 2 weight percent of a pharmaceutically acceptable lubricating agent, and optionally including a pharmaceutically acceptable coating.

Abstract: Compounds useful for treating inflammation, pain and swelling, represented by the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein: Y and Z are each independently halo, alkyl or alkoxy;l and m are each independently integers of 0-4;b is an integer of 2-12; andX is selected from the group consisting of:--NR.sup.1 R.sup.2, --NR.sup.1 (CH.sub.2 CH.sub.2 OH), ##STR2## in which R.sup.1 and R.sup.2 are independently H, alkyl or cycloalkyl;R.sup.3 is H, alkyl or CH.sub.2 CH.sub.2 OH; andn is an integer of 3-7.

Abstract: Compounds useful for treating inflammation, swelling and associated pain, represented by the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein: a is an integer of 0-3;b is an integer of 0-2;n is an integer of 3-12;each X and each Y are independently -halo, --R.sup.1, -alkoxy, or -phenyl; andB is selected from the group consisting of:--NR.sup.1 R.sup.2, --NR.sup.1 (CH.sub.2 CH.sub.2 OH), ##STR2## in which R.sup.1 and R.sup.2 are independently H, alkyl or cycloalkyl;R.sup.3 is H, alkyl or --CH.sub.2 CH.sub.2 OH; andm is an integer of 3-8.Novel compounds are those wherein n is at least 6 if both a and b are 0.

Abstract: Compounds of formulas (1) and (2): ##STR1## in which: X and Y are independently hydrogen, hydroxy, lower alkyl, lower alkoxy or halo, or X and Y taken together is methylenendioxy or ethylene-1,2-dioxy, andR is lower alkyl, optionally substituted phenyl, --(CH.sub.2).sub.m OR.sup.1 or --NR.sup.1 R.sup.2 wherein m is an integer of 1 to 6 and R.sup.1 and R.sup.2 are independently hydrogen or lower alkyl, or --NR.sup.1 R.sup.2 taken together is a heterocycle of the formula: ##STR2## wherein A is --CH.sub.2 --, --NR.sup.1 -- or oxygen, or a pharmaceutically acceptable salt thereof, are useful as .alpha..sub.2 -blockers, especially as antidepressants.

Abstract: Compounds useful in treating cardiovascular disorders such as thrombosis, hypertension and atherosclerosis are depicted in formulas (1), (2) and (3): ##STR1## wherein: A is --C.tbd.C--, trans --HC.dbd.CH--, --CH.sub.2 CH.sub.2 -- or --CH.dbd.CHCH.sub.2 --;X is lower alkoxy, hydroxy, or (2,2,2)-trifluoroethoxy;Y is hydrogen, exo-(lower alkyl) or endo-(lower alkyl);is an integer of 2-4;R.sub.1 is --CH.sub.2 OH, --CHO, --CO.sub.2 R or --CO.sub.2 H, and the olefin formed by the R.sub.1 (CH.sub.2).sub.n CH.dbd. moiety is either (E) or (Z);R.sub.2 is hydrogen or methyl, or optionally --CH.dbd.CH.sub.2 when A is --CH.dbd.CHCH.sub.2 --; andR.sub.3 is linear or branched alkyl, alkenyl or alkynyl having 5-10 carbon atoms, ##STR2## --(CH.sub.2).sub.m -phenyl or CH.sub.

Abstract: A method of treating rheumatoid arthritis which method comprises administering to a mammal in need of such treatment a therapeutically effective amount of a compound of the formula: ##STR1## and the pharmaceutically acceptable salts thereof, wherein:A is oxygen or sulfur;R.sup.1 is selected from the group consisting of H, ##STR2## in which Y is oxygen or sulfur:R.sup.2 is alkyl, haloalkyl or --NR.sup.4 R.sup.5, where R.sup.4 and R.sup.5 are independently H, alkyl, haloalkyl, cycloalkyl, phenyl optionally monosubstituted with halogen, hydroxy, carboxy, chlorocarbonyl, sulfonylamino, nitro, cyano, phenyl, alkyl, acyl, alkoxycarbonyl, acylamino, dialkylamino or dialkylaminoethoxycarbonyl, phenyl optionally disubstituted with hydroxy, carboxy, nitro or alkyl, or benzyl optionally substituted with dialkylamino;n is an integer from 0-6;R.sup.3 is H alkyl or a pharmaceutically acceptable cation;Q and R are independently H or --CO.sub.2 R.sup.

Abstract: Compounds having the formula ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the definitions given herein, are useful as antiarrhythmic agents.

Abstract: .alpha.-amino acids having a substituted .omega.-guanidino group are disclosed herein.

Abstract: Compounds useful for treating inflammatory diseases, in particular rheumatoid arthritis, represented by the formula: ##STR1## and the pharmaceutically acceptable salts thereof, wherein:R.sub.1 is H or lower alkyl having 1 to 6 carbon atoms;R.sub.2 is H, lower alkyl having 1 to 6 carbon atoms or ##STR2## in which R.sub.3 is H, lower alkyl having 1 to 6 carbon atoms or a pharmaceutically acceptable cation;R.sub.4 and R.sub.5 are each independently H or lower alkyl having 1 to 6 carbon atoms;X and Y are each independently O or S; andn is an integer of 1-6.

Abstract: Compounds useful in treating cardiovascular disorders such as thrombosis, hypertension, and atherosclerosis are compounds depicted in formulas (1), (2), and (3): ##STR1## wherein: Y is exo-(lower alkyl) or endo-(lower alkyl);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## or --(CH.sub.2).sub.m -phenyl 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## wherein X is ##STR4## 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: This invention concerns novel sustained release microcapsule compositions comprising water-soluble, hormonally active polypeptides and, optionally, a polymer hydrolysis modifying agent encapsulated in a biocompatible, biodegradable polymer.

Abstract: Synthetic nonpeptide and decapeptide LHRH antagonist analogs have a novel guanido-substituted, amidine, tertiary or quaternary amine water-soluble aminoacyl residue at position 6.

Abstract: 2-Oxy-4H-3,1-benzoxazin-4-ones represented by the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein: a is an integer of 0-4;A is a bond, or alkylene having one to eight carbon atoms;R is hydrogen, phenyl, imidazolyl or cycloalkyl having three to six carbon atoms, wherein the phenyl, imidazolyl or cycloalkyl ring is optionally substituted with 1-3 substituents independently selected from the group consisting of lower alkyl having one to four carbon atoms, lower alkoxy having one to four carbon atoms, --N(R.sup.1).sub.2, --NO.sub.2, halo or lower alkylthio having one to four carbon atoms, and,each R' is independently selected from the group consisting of lower alkyl having one to six atoms, lower alkenyl having two to six carbon atoms, lower alkoxy having one to six carbon atoms,lower alkylthio or halo-lower alkyl having one to four carbon atoms, halo, --NO.sub.2, --N(R.sup.1).sub.2, ##STR2## --NR.sup.1 COR.sup.2, and ##STR3## in which each R.sup.

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.