Abstract: The present invention provides oral formulations of poorly bioavailable and/or poorly absorbable, and/or poorly water soluble therapeutic agents. The invention features harmaceutical composition including a biopolymer, a therapeutic agent, for example an antimicrobial agent such as ceftriaxone, and an absorption enhancer, for example a polyoxyethylene alkyl ether absorption enhancer. Methods of making and using the pharmaceutical compositions is also described.

Abstract: The present invention provides oral formulations of poorly bioavailable and/or poorly absorbable, and/or poorly water soluble therapeutic agents. The invention features pharmaceutical composition including a biopolymer, a therapeutic agent, for example an antimicrobial agent such as ceftriaxone, and an absorption enhancer, for example a polyoxyethylene alkyl ether absorption enhancer. Methods of making and using the pharmaceutical compositions is also described.

Abstract: The present invention provides oral formulations of poorly bioavailable and/or poorly absorbable, and/or poorly water soluble therapeutic agents. The invention features pharmaceutical composition including a biopolymer, a therapeutic agent, for example an antimicrobial agent such as ceftriaxone, and an absorption enhancer, for example a polyoxyethylene alkyl ether absorption enhancer. Methods of making and using the pharmaceutical compositions is also described.

Abstract: There are presented antibacterial cephalosporine having broad antimicrobial activity, having the formula ##STR1## wherein R is hydrogen or a carboxylic acid-protecting group: R.sub.1 represents a substituted piperazinyl group of formula ##STR2## or a substituted pyrrolidinylamino group of formula ##STR3## or a substituted pyrrolidinylmethylamino group of formula ##STR4## where the piperazinyl or pyrrolidinyl group may be optionally substituted with one or more lower alkyl groups, and where Q represents a substituted quinolinyl or naphthyridinyl group: R.sub.2 is selected from the group consisting of hydrogen, lower alkoxy, lower alkylthio and amido; R.sub.3 is hydrogen or an acyl group: and m is 0, 1 or 2, but preferably 0; as well as the corresponding readily hydrolyzable esters. pharmaceutically acceptable salts and hydrates of these compounds.

Abstract: There are presented antibacterial cephalosporins having broad antimicrobial activity as well as intermediates for their formation, such compounds having the formula ##STR1## wherein R is hydrogen or a carboxylic acid-protecting group; R.sub.1 is a substituted piperazinium group of the formula ##STR2## in which Q represents a substituted quinolinyl or naphthyridinyl group and the piperazine nucleus may be optionally substituted with one or more lower alkyl groups; R.sub.2 is selected from the group consisting of hydrogen, lower alkoxy, lower alkylthio and amido; R.sub.3 is hydrogen or an acyl group; and m is 0, 1 or 2, preferably 0;as well as the corresponding readily hydrolyzable esters, pharmaceutically acceptable salts and hydrates of these compounds.

Abstract: The invention relates to antibacterially active 5-amino-3-(.beta.-D-ribofuranosyl)imidazo[4,5-d][1,3]thiazin-7(3H)-one, also referred to as 1-thiaguanosine, a composition and method comprising the same and processes and intermediates for the preparation of 1-thiaguanosine and 5-amino-3-(.beta.-D-ribofuranosyl)imidazo[4,5-d][1,3]oxazin-7(3H)-one, also referred to as oxanosine, a known compound.

Abstract: Antibacterial compounds of the formula ##STR1## in which R.sub.1 is a cyclic or secondary acyclic amino group which independently has antibacterial activity;R.sub.2 is hydrogen, lower alkoxy, lower alkylthio or formamido;R.sub.3 is hydrogen or an organic group bonded through carbon, oxygen, sulfur or nitrogen;R.sub.4 is an electronegative acidic group; or R.sub.3 and R.sub.4 together form a heterocycle; andR.sub.5 is hydrogen or lower alkyl, except when R.sub.3 and R.sub.4 form a heterocycle, in which case R.sub.5 is hydrogen only; and methods of using same.

Abstract: Antibacterial compounds of the formula ##STR1## in which R.sub.1 is a cyclic or secondary acyclic amino group which independently has antibacterial activity:R.sub.2 is hydrogen, lower alkoxy, lower alkylthio or formamido;R.sub.3 is hydrogen or an organic group bonded through carbon, oxygen, sulfur or nitrogen;R.sub.4 is an electronegative acidic group; or R.sub.3 and R.sub.4 together form a heterocycle; andR.sub.5 is a hydrogen or lower alkyl, except when R.sub.3 and R.sub.4 form a heterocycle, in which case R.sub.5 is hydrogen only; and methods of using same.

Abstract: There are presented anti-bacterial cephalosporins having broad antimicrobial activity of the formula ##STR1## wherein R.sub.1 is an antibiotically active quinolonyl; R.sub.2 is selected from the group consisting of hydrogen, lower alkoxy, amino, lower alkylthio and amido; R.sub.3 is selected from the group consisting of hydrogen, and acyl group, and m is 0, 1 or 2 and the readily hydrolysable esters or salts of these compounds and hydrates of the compounds of formula I or of their esters or salts.

Abstract: A process for synthesizing 3-acryloxymethyl antibacterialcephalosporin compounds of formula ##STR1## wherein R is hydrogen or a carboxylic acid protecting group; R.sup.1 is hydrogen or an acyl group; R.sup.2 is hydrogen or lower alkoxy; and R.sup.3 is carbocyclic aryl substituted on the ring with one or more members selected from the group consisting of hydroxy, lower alkyl, amino, cyano, lower alkoxy, halogen and alkylcarboxy,as well as the corresponding readily hydrolyzable esters, pharmaceutically acceptable salts and hydrates of these compounds where R is hydrogen, in which a 2-carboxylic acid 3-hydroxymethyl cephalosporin compound is first treated with an organic base to form an organic salt therewith, followed by acylation of the 3-hydroxymethyl substituent.

Abstract: Compounds of the formula ##STR1## wherein A is ##STR2## in which R.sub.1 is acyl, R.sub.2 is hydrogen, lower alkyl, lower alkoxy-carbonyl or aminocarbonyl, R.sub.3 is hydrogen or lower alkyl, R.sub.4 and R.sub.4, are each hydrogen, lower alkyl, lower alkoxy, aryl, aryloxy or aralkyl, as well as the pharmaceutically acceptable salts of such compounds, are useful as antibacterial agents for combatting infections in mammals.

Abstract: Compounds of the formula ##STR1## wherein A is one of the following: ##STR2## in which R.sub.1, is acyl, R.sub.2 is hydrogen, lower alkyl, lower alkoxycarbonyl or aminocarbonyl, R.sub.3 is hydrogen or lower alkyl and R.sub.4 and R.sub.4 ' are hydrogen, lower alkyl, lower alkoxy, acyl or aralkyl, as well as pharmaceutically acceptable salts of such compounds, are useful as antibacterial agents.

Abstract: There are presented compounds of the formula ##STR1## wherein R.sub.2, R.sub.3, R.sub.4 and m are as described herein.

Abstract: A novel family of .beta.-lactam antibacterials, synthetic methods and intermediates useful in the production of such antibacterials, and the use of such compounds as antibacterials are disclosed. The novel compounds have the formula ##STR1## wherein, Z.sup.1 is a group --OR.sup.1, --NR.sup.3 R.sup.4, or --SR.sup.5 ;Z.sup.2 is a group --OR.sup.2, --NR.sup.3 R.sup.4, or --SR.sup.6 ;R.sup.1 and R.sup.2 may be either the same or different and each is H, lower alkyl, aralkyl, aryl or heteroaryl;R.sup.3 and R.sup.4 may be either the same or different and each is H, lower alkyl, aralkyl, aryl or heteroaryl;R.sup.5 and R.sup.6 may be either the same of different and each is H, lower alkyl, aralkyl, aryl or heteroaryl;R.sup.7 is H, lower alkyl, or lower alkoxycarbonyl; and,R.sup.8 is acyl;as well as pharmaceutically acceptable salts thereof.

Abstract: A .beta.-lactamase inhibitor of the formula ##STR1## and the pharmaceutically acceptable salts thereof are presented. Also presented are intermediates and synthetic processes for the manufacture of the formula I compound.The compound inhibits the activity of enzymes which inactivate certain .beta.lactam antibiotics.

Abstract: The amino acid 2-amino-4-(2-aminoethoxy)-trans-but-3-enoic acid can be conveniently prepared via novel intermediates from a 2,2'-disubstituted diethyl ether and a dialkyl N-protected amidomalonate starting material using a multi-step process. Preferred starting materials are bis-2-chloroethyl ether and diethyl acetamidomalonate. The process, in a preferred embodiment, proceeds through the key intermediate ethyl-2-acetamido-4-[2-(2-phthalimido)ethoxy]-but-2-enoate.

Abstract: The present invention is directed to compounds of the formula ##STR1## wherein R.sub.1 is lower alkyl and R.sub.2 is lower alkyl or aryl. Also provided are methods for preparation of these compounds. The compounds of formula I above are useful as plant growth regulants.