Abstract: Naphthyridine and quinoline compounds having the formula: ##STR1## wherein A is CH or N; Z is an amine having the formula: ##STR2## R is o,p-difluorophenyl or p-fluorophenyl; and R.sub.1 is hydrogen or a carboxy protecting group. The compounds of the invention have antibacterial activity and improved solubility and pharmacokinetic properties.

Abstract: A process for the preparation of enantiomerically homogeneous aminopyrrolidinyl naphthyridine carboxylic acids and quinolone carboxylic acids, and for the preparation of intermediates that are useful in the production of these carboxylic acids.

Abstract: A method and a composition for treating or reducing and/or controlling intraocular pressure comprising administering an effective amount of a renin inhibiting compound of the formula: ##STR1## wherein A is a substituent; W is CO or CHOH and U is CH.sub.2 or NR.sub.2 wherein R.sub.2 is hydrogen or loweralkyl; with the proviso that when W is CHOH then U is CH.sub.2 ; R.sub.1 is loweralkyl, cycloalkyl, benzyl, (alpha, alpha)-dimethylbenzyl, 4-hydroxybenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, phenethyl, 1-benzyloxyethyl, phenoxy, thiophenoxy or anilino; R.sub.3 is loweralkyl, loweralkenyl, ((alkoxy)alkoxy)alkyl, carboxyalkyl, (thioalkoxy)alkyl, benzyl or heterocyclic ring substituted methyl; and R.sub.4 is a substituted amino group; or pharmaceutically acceptable salts or esters thereof.

Abstract: The invention relates to novel solution and suspension aerosol formulations comprising LHRH analogs.

Abstract: Compounds of the formula: ##STR1## where R.sub.1 is amino or methyl; R.sub.2 is C.sub.1 -C.sub.2 alkyl; R.sub.3 is one or more substituents selected from hydrogen, halogen or trihalomethyl; R.sub.4 is one or more substituents selected from hydrogen, halogen, trihalomethyl, C.sub.1 to C.sub.4 alkoxy or C.sub.1 to C.sub.4 alkyl; and M is hydrogen, a pharmaceutically acceptable cation, aroyl, or C.sub.1 to C.sub.6 alkoyl are inhibitors of 5- and/or 12-lipoxygenase enzymes.

Abstract: A process for making urokinase derivatives having a sulfhydryl group incorporated into a remnant of urinary plasminogen activator. The process comprises reducing disulfide bridges in the presence of arginine and incorporating a desired compound having a sulfhydryl containing group into the structure through the formation of a disulfide bridge.

Abstract: The present invention includes compounds represented by the formula: ##STR1## wherein R.sub.1 is a hydroxy, a C.sub.1 to C.sub.6 alkoxy, benzoxy, or an alkylcarbonyloxymethoxy group, or R.sub.3 together with R.sub.1 forms a group of the formula --Y--NH-- where Y is oxygen or sulfur; or R.sub.3 is hydrogen; A is nitrogen or CR.sub.2, where R.sub.2 is hydrogen, or halogen, or R.sub.2 together with R forms a group of the formula --X--CH.sub.2 --CH(R.sub.6)-- or --X--CH.sub.2 --CH.dbd.CH.sub.2, wherein X is CH.sub.2, O, S, NH, or NCH.sub.3, and R.sub.6 is hydrogen, alkyl, or C.sub.1 -C.sub.3 haloalkyl; or R is (1) a C.sub.1 to C.sub.4 alkyl, (2) lower cycloalkyl, (3) alkylamino, (4) haloalkyl, (5) an aromatic heterocyclic ring or (6) a substituted phenyl group; and Z is a carbocyclic group;or a pharmaceutically acceptable salt thereof. The compounds of the present invention are useful as antibacterial agents.

Abstract: A method of preventing the fracture of coated drug granules during the compression of the granules into a commercially acceptable tablet matrix is disclosed. The method involves incorporating into the matrix, along with the granules, from about 10% to about 50% by weight microcrystalline cellulose.

Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 is (1) hydrogen, (2) C.sub.1 to C.sub.4 alkyl, (3) C.sub.2 to C.sub.4 alkenyl, or (4) NR.sub.2 R.sub.3, wherein R.sub.2 and R.sub.3 are independently selected from (1) hydrogen, (2) C.sub.1 to C.sub.4 alkyl and (3) hydroxyl, but R.sub.2 and R.sub.3 are not simultaneously hydroxyl;wherein X is oxygen, sulfur, SO.sub.2, or NR.sub.4, wherein R.sub.4 is (1) hydrogen, (2) C.sub.1 to C.sub.6 alkyl, (3) C.sub.1 to C.sub.6 alkoyl, (4) aroyl, or (5) alkylsulfonyl;A is selected from C.sub.1 to C.sub.6 alkylene and C.sub.2 to C.sub.6 alkenylene;n is 1-5;Y is selected independently at each occurrence from (1) hydrogen, (2) halogen, (3) hydroxy, (4) cyano, (5) halosubstituted alkyl, (6) C.sub.1 to C.sub.12 alkyl, (7) C.sub.2 to C.sub.12 alkenyl, (8) C.sub.1 to C.sub.12 alkoxy, (9) C.sub.3 to C.sub.8 cycloalkyl, (10) C.sub.1 -C.sub.8 thioalkyl, (11) aryl, (12) aryloxy, (13) aroyl, (14) C.sub.1 to C.sub.12 arylalkyl, (15) C.sub.2 to C.sub.12 arylalkenyl, (16) C.sub.1 to C.

Abstract: A tablet providing enhanced delivery of an acid-sensitive drug in conjunction with an acid-stable drug is disclosed. The tablet is made up of a matrix containing a major proportion of an acid-stable drug, and a minor proportion of microcrystalline cellulose. Embedded in the matrix are coated granules containing at least about 90% of an acid-sensitive drug by weight, exclusive of the coating, and having a particle size of from about 10 to about 40 mesh. The granules of acid-sensitive drug have an acid resistant and/or enteric coating selected to dissolve in less than sixty minutes at a pH of 5.5 or greater.

Abstract: A process for the preparation of enantiomerically homogeneous aminopyrrolidinyl naphthyridine carboxylic acids and quinolone carboxylic acids, and for the preparation of intermediates that are useful in the production of these carboxylic acids. The compounds are useful as anti-bacterials.

Abstract: The invention relates to renin inhibiting compounds of the formula ##STR1## wherein A is hydrogen; loweralkyl; arylalkyl; OR.sub.10 or SR.sub.10 wherein R.sub.10 is hydrogen, loweralkyl or aminoalkyl; NR.sub.11 R.sub.12 wherein R.sub.11 and R.sub.12 are independently selected from hydrogen, loweralkyl, aminoalkyl, cyanoalkyl and hydroxyalkyl; ##STR2## wherein B is NH, alkylamino, S, O, CH.sub.2 or CHOH and R.sub.13 is loweralkyl, cycloalkyl, aryl, arylalkyl, alkoxy, alkenyloxy, hydroxyalkoxy, dihydroxyalkoxy, arylalkoxy, arylalkoxyalkyl, amino, alkylamino, dialkylamino, (hydroxyalkyl)(alkyl)amino, (dihydroxyalkyl)(alkyl)amino, aminoalkyl, alkoxycarbonylalkyl, carboxyalkyl, N-protected aminoalkyl, alkylaminoalkyl, (N-protected)(alkyl)aminoalkyl, dialkylaminoalkyl, (heterocyclic) alkyl or a substituted or unsubstituted heterocyclic; W is CO or CHOH and U is CH.sub.2 or NR.sub.2 with the proviso that when W is CHOH then U is CH.sub.2 ; R.sub.1 is loweralkyl, cycloaklylmethyl, benzyl, .alpha.,.alpha.

Abstract: The invention relates to novel aerosol formulations comprising LHRH analogs, a lipophilic counterion, solvent and propellant and, optionally, surfactant, valve lubricant, an antioxidant and flavor and fragrance.

Abstract: A controlled, slow release, solid pharmaceutical preparation includes at least one active ingredient and a blend of sodium alginate and sodium-calcium alginate.

Abstract: The invention relates to renin inhibiting compounds of the formula ##STR1## wherein A is ##STR2## wherein B is thiomorpholino, morpholino, 4-sulfonylmorpholino, 3,4-dihydroxypyrrolidino, alkoxy or loweralkyl and C is NH or CH.sub.2 ; R.sub.1, R.sub.3 and R.sub.7 are independently selected from loweralkyl or lipophilic or aromatic amino acid side chains; R.sub.2, R.sub.4, and R.sub.6 are independently selected from hydrogen or loweralkyl; R.sub.5 is phenyl, isopropyl, cyclohexyl, 1,3-dioxan-2-yl; 1,3-dioxolan-2-yl, loweralkyl, 1,3-dithiolan-2-yl or 1,3-dithian-2-yl; X is hydrogen, loweralkyl or --CH.sub.2 OR.sub.8, wherein R.sub.8 is hydrogen, loweralkyl or alkaryl; and R.sub.9 is hydrogen, loweralkyl, hydroxy, hydroxyalkyl, difluoro, alkoxy, allyl, alkaryloxy or thioalkyl and pharmaceutically acceptable salts thereof.

Abstract: The invention relates to renin inhibiting compounds of the formula ##STR1## wherein A is hydrogen; loweralkyl; arylalkyl; Or.sub.10 wherein R.sub.10 is hydrogen or loweralkyl; NR.sub.11 R.sub.12 wherein R.sub.11 and R.sub.12 are independently selected from hydrogen and loweralkyl; or R.sub.13 --CO--B wherein B is NH, O, CH.sub.2, HNCH.sub.2 and R.sub.13 is loweralkyl, alkoxy, arylalkoxy, arylalkoxyalkyl, amino, alkylamino, dialkylamino, aminoalkyl, N-protected aminoalkyl, hydroxylated dialkylamino, (heterocyclic)alkyl or a substituted or unsubstituted heterocyclic, carboxyalkyl, or lower alkyl carboxyalkyl esters; W is N or CH: U,V may be the following combinations H,OH; OH,H; H,H; or when taken together as O represents a carbonyl with the provisos that if U,V.dbd.H,OH, then W=CH, and if U,V.dbd.O then W.dbd.N; R.sub.1 , R.sub.3 and R.sub.5 are loweralkyl or hydrophilic, lipophilic or aromatic amino acid side chains and may be the same or different; R.sub.2, R.sub.4, R.sub.7, R.sub.8 and R.sub.

Abstract: Compounds of the formula: ##STR1## wherein R1 is hydrogen, C1 to C4 alkyl, C2 to C4 alkenyl, or NR2R3, wherein R2 and R3 are independently selected from hydrogen, C1 to C4 alkyl and hydroxyl, but R2 and R3 are not simultaneously hydroxyl;X is oxygen, sulfur, CO2, or NR4, wherein R4 is hydrogen, C1 to C6 alkyl, C1 to C6 alkoyl or aroyl;A is selected from C1 to C6 alkylene and C2 to C6 alkenylene;Y is selected independently at each occurrence from hydrogen, halogen, hydroxy, cyano, nitro, halosubstituted alkyl, C1 to C12 alkyl, C2 to C12 alkenyl, C1 to C12 alkoxy, C3 to C8 cycloalkyl, aryl, aryloxy, aroyl, C1 to C12 arylalkyl, C2 to C12 arylalkenyl, C1 to C12 arylalkoxy, C1 to C12 arylthicalkoxy, and substituted derivatives of aryl, aryloxy, aroyl, C1 to C12 arylalkyl, C2 to C12 arylalkenyl, C1 to C12 arylalkoxy, or C1 to C12 arylthioalkoxy, wherein C12 alkyl, alkoxy, and halosubstituted alkyl; n is a number having the values 0-4; when n=0 then Y=hydrogen;and M is hydrogen, a pharmaceutically acceptable cation,

Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 is (1) hydrogen, (2) C.sub.1 to C.sub.4 alkyl, (3) C.sub.2 to C.sub.4 alkenyl, or (4) NR.sub.2 R.sub.3, wherein R.sub.2 and R.sub.3 are independently selected from (1) hydrogen, (2) C.sub.1 to C.sub.4 alkyl and (3) hydroxyl, but R.sub.2 and R.sub.3 are not simultaneously hydroxyl;X is (1) oxygen, (2) sulfur, (3) SO.sub.2, or (4) NR.sub.4, wherein R.sub.4 is (1) hydrogen, (2) C.sub.1 to C.sub.6 alkyl, (3) C.sub.1 to C.sub.6 alkyl or (4) aroyl;A is selected from C.sub.1 to C.sub.6 alkylene and C.sub.2 to C.sub.6 alkenylene; n is 0-4;Y is selected independently at each occurrence from (1) hydrogen, (2) halogen, (3) hydroxy, (4) cyano, (5) halosubstituted alkyl, (6) C.sub.1 to C.sub.12 alkyl, (7) C.sub.2 to C.sub.12 alkenyl, (8) C.sub.1 to C.sub.12 alkoxy, (9) C.sub.3 to C.sub.8 cycloalkyl, (10) aryl, (11) aryloxy, (12) aroyl, (13) C.sub.1 to C.sub.12 arylalkyl, (14) C.sub.2 to C.sub.12 arylalkenyl, (15) C.sub.1 to C.sub.12 arylalkoxy, (16) C.sub.1 to C.sub.

Abstract: Compositions which comprise a complex of carbomer (acrylic acid polymers) and erythromycin or a derivative thereof such as 6-O-methylerythromycin, are disclosed. The compositions provide nontoxic, palatable dry and liquid dosage forms for oral administration.