Abstract: This invention relates to 4-substituted 7-aza-indolin-2-ones and their use as protein kinase inhibitors.

Abstract: Disclosed are novel pyrazolobenzodiazepines having the formula 1

Abstract: The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.

Abstract: Disclosed are novel pyrazolobenzodiazepines having the formula and the pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and R4 are as defined herein. These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. These compounds and their pharmaceutically acceptable salts, and prodrugs of said compounds, are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer, more particularly, the treatment or control of breast, colon, lung and prostate tumors. Also disclosed are pharmaceutical compositions containing the compounds of formula I as well as intermediates useful in the preparation of the compounds of formula I.

Abstract: The present invention relates to (2-oxindol-3-ylidenyl)acetic acid derivatives which modulate the activity of protein kinases and are therefore useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.

Abstract: The present invention relates to compounds of the formula ##STR1## wherein R.sup.1 is an acyl group derived from a carboxylic acid, hydrogen, or an amino protecting group;R.sup.2 is hydrogen, hydroxy, lower alkyl-Q.sub.p -, cycloalkyl, lower alkoxy, lower alkenyl, cycloalkenyl, lower alkynyl, aralkyl-Q.sub.p -, aryl-Q.sub.p -, aryloxy, aralkoxy or a heterocyclic ring, the lower alkyl, cycloalkyl, lower alkoxy, lower alkenyl, cycloalkenyl, lower alkynyl, aralkyl, aryl, aryloxy, aralkoxy and the heterocyclic ring being unsubstituted or substituted with at least one group selected from carboxy, amino, nitro, oxo, cycloalkyl, cyano, lower alkyl, lower alkoxy, hydroxy, halogen, --CONR.sup.4 R.sup.5, --N(R.sup.5)COOR.sup.9, R.sup.5 CO--, R.sup.5 OCO-- or R.sup.5 COO-- where R.sup.4 is hydrogen, lower alkyl, or cycloalkyl; R.sup.5 is hydrogen or lower alkyl; R.sup.9 is lower alkyl, lower alkenyl or a carboxylic acid protecting group;Q is --CO-- or --SO.sub.

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: There are presented antibacterial cephalosporins having broad antimicrobial activity as well as intermediates for their formation, such compounds having the formula ##STR1## wherein X is ##STR2## R is hydrogen or a carboxylic acid protecting group; R.sub.1 is hydrogen or an acyl group;R.sub.2 is hydrogen or lower alkoxy; andR.sub.3 is carbocyclic aryl or alkyl carbocyclic aryl substituted on the ring with two or more of hydroxy and/or lower alkanoyl ester groups, with halogen being an optional additional ring substituent;as well as the corresponding readily hydrolyzable esters, pharmaceutically acceptable salts and hydrates of these compounds where R is hydrogen.

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: 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: 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 enantiomeric systhesis from ascorbic acid of (3S,4S)-3-amino-4-carbamoyloxymethyl-2-azetidinone-1-sulfate, an intermediate for an antibiotic compound.

Abstract: 6-Amidinopenicillanic acid derivatives wherein one of the nitrogen atoms of the amidino group is part of a heterocyclic ring having on a side chain an unsubstituted heterocyclic ring containing 2 to 3 nitrogen atoms, and being useful as an antibiotic.

Abstract: 6-Amidinopenicillanic acid derivatives wherein one of the nitrogen atoms of the amidino group is part of a heterocyclic ring having on a side chain an unsubstituted heterocyclic ring containing 2 to 3 nitrogen atoms, and being useful as an antibiotic.

Abstract: A novel enantiomeric synthesis from ascorbic acid of (3S,4S)-3-amino-4-carbamoyloxymethyl-2-azetidinone-1-sulfate, an intermediate for an antibiotic compound.

Abstract: A process for the Raney nickel desulfurization of penicillins is described. In the process of the invention, amino penicillanic acid or derivatives thereof are reacted with Raney nickel under controlled conditions of temperature and time to yield azetidinones which are useful as intermediates for the synthesis of monocyclic beta-lactam antibiotics.

Abstract: 6-Amidinopenicillanic acid derivatives wherein one of the nitrogen atoms of the amidino group is part of a heterocyclic ring having on a side chain an unsubstituted heterocyclic ring containing 2 to 3 nitrogen atoms, and being useful as an antibiotic.