Merck + Co., Inc.

James V Heck

Burton G Christensen

Lovji D Cama

Frank P DiNinno

Michael N Chang

Yuan-Ching P Chiang

Ronald W Ratcliffe

Thomas N Salzmann

Mark L Greenlee

Shu S Yang

Alan D Adams

Michael D Lewis

W Alexander Andrus

John C Chabala

Michael J Szymonifka

Eugene D Thorsett

Donald W Graham

Robert R Wilkening

Milton L Hammond

Soumya P Sahoo

David H Shih

William J Leanza

Robert A Zambias

Kevin D Dykstra

Conrad Santini

Kothandaraman Shankaran

Kathryn L Thompson

Victoria K Lombardo

Julia K Boueres

Edward J Metzger

Substituted 5-aryl-2,4-thiazolidinediones or 5-aryl-2,4-oxazolidinediones that also carry a second substituent in the 5-position of the heterocyclic ring are potent agonists of PPAR, and are therefore useful in the treatment, control or prevention of diabetes, hyperglycemia, hyperlipidemia (including hypercholesterolemia and hypertriglyceridemia), atherosclerosis, obesity, vascular restenosis, and other PPAR &agr;, &dgr; and/or &ggr; mediated diseases, disorders and conditions.

Arylthiazolidinedione and aryloxazolidinedione derivatives

Compounds of the formula: ##STR1## where R is hydrogen, hydroxyl, alkyl or acyl, R' and R' together are oxo, hydroxyimino or alkoxyimino, and R' and R' independently are hydrogen, hydroxyl, acyloxy, or amino substituted by any of hydrogen, alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, alkoxycarbonyl, aralkoxycarbonyl, alkylsulfonyl or arylsulfonyl, and n is 0 or 1, and the pharmaceutically acceptable salts thereof. The compounds are macrolide antibiotics and are also useful as intermediates to the synthesis of other macrolide antibiotics. Pharmaceutical compositions and methods of their use are also provided for.

Homoerythromycin A derivatives modified at the 4'-and 8A-positions

A compound of the formula I is disclosed. ##STR1## R.sup.13 represents hydrogen, NH.sub.2, C1-4 alkyl, C1-4 alkylamino or di(C1-4)alkylamino-;

3-aryl or heteroaryl-7-heteroaralkylamido cephalosporin compounds,

A compound of the formula I is disclosed. ##STR1## R.sup.13 represents hydrogen, NH.sub.2, C1-4 alkyl, C1-4 alkylamino or di(C1-4) alkylamino-; Y represents CH or N; Y' represents (a) CR.sup.y 'R.sup.z ' with R.sup.y ' and R.sup.z ' hydrogen, C1-6 alkyl, C.sub.3-8 cycloalkyl or C.sub.1-6 alkyl substituted with C.sub.3-8 cycloalkyl, or (b) N substituted with OR.sup.14 with R.sup.14 representing H, C.sub.1-4 alkyl or C.sub.1-4 alkyl substituted with COOH. Ar represents: ##STR2## One of R.sup.1 and R.sup.2 independently represent H, W as defined below or one of the groups (a) through (d) below, and the other represents H or W. Pharmaceutical editions and methods of use are also included.

A compound of the formula I is disclosed. ##STR1## R.sup.13 represents hydrogen, NH.sub.2, C1-4 alkyl, C1-4 alkylamino or di(C1-4) alkylamino-; Y represents CH or N; Y' represents (a) CR.sup.y' R.sup.z' with R.sup.y' and R.sup.z' hydrogen, C1-6 alkyl, C.sub.3-8 cycloalkyl or C.sub.1-6 alkyl substituted with C.sub.3-8 cycloalkyl, or (b) N substituted with OR.sup.14 with R.sup.14 representing H, C.sub.1-4 alkyl or C.sub.1-4 alkyl substituted with COOH. Ar represents: ##STR2## One of R.sup.1 and R.sup.2 independently represent H, W as defined below or one of the groups (a) through (d) below, and the other represents H or W. Pharmaceutical compositions and methods of use are also included.

3-aryl of heteroaryl-7-heteroaralkylamido cephalosporin compounds,

Carbapenems of the formula ##STR1## are useful antibacterial agents.

(N-pyridiniumphenyl)-carbapenems

Disclosed are carbapenems of the formula ##STR1## which are 2-(9-fluorenonyl)-carbapenems useful as antibacterial agents. Intermediates for preparation of these compounds is also disclosed.

2-(9-fluorenonyl)-carbapenem intermediates

Triazolyl and tetrazolyl phenyl substituted carbapenems of the formula I are disclosed. ##STR1## One or two of the variables X, Y and Z represent nitrogen atoms. The heteroaryl ting may be charged or uncharged. Pharmaceutical compositions and methods of treatment are also disclosed.

Triazolyl and tetrazolyl phenyl substituted carbapenems, compositions

2-(N-imidazoliumphenyl)-carbapenems

Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or hydroxyl; R.sub.2 is hydrogen; hydroxyl or methyl, R.sub.3 is hydrogen or hydroxyl; R.sub.4 is C.sub.5 -C.sub.23 alkyl, C.sub.5 -C.sub.23 alkenyl, aryl or substituted aryl; R.sub.5 is --CH.sub.2 OH, --CH(CH.sub.3)OH, --CH(CH.sub.2 CONH.sub.2)OH; R.sub.6 is --CH.sub.2 OH or --CH(CH.sub.3)OH; R is --CH.sub.2 OH or --CH(CH.sub.3)OH; provided that when R.sub.4 is --(CH.sub.2).sub.8 CH(CH.sub.3)CH.sub.2 CH(CH.sub.3)C.sub.2 H.sub.5, R.sub.5 is --CH.sub.2 OH or --CH(CH.sub.3)OH. The compounds are useful as antimicrobial agents, especially as antifungal agents.

Cyclic hexapeptide compounds

2-biphenyl-carbapenem antibacterial agents

Carbapenems of the formula ##STR1## are useful intermediates in the preparation of 2-(9-fluorenonyl)-carbapenem antibacterial agents.

N-tetrazolyl beta-lactams of the Formula: ##STR1## and the pharmaceutically acceptable salts thereof wherein R.sup.2 is hydrogen, alkyl having 1 to 6 carbon atoms or carboalkoxy having 2 to 7 carbon atoms; and

N-tetrazolyl beta-lactams

This application relates to compounds of formula (I), which are useful as antihypercholesterolemic agents. ##STR1##

Beta-lactams as antihypercholesterolemics

Carbapenems of the formula ##STR1## wherein either the 2-fluoren-9-one or 3-fluoren-9-one is attached at the 2-position of the carbapenem are useful antibacterial agents.

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Scotch Plains, NJ, United States of America

James V Heck