Bristol-myers Company

Bristol-myers Squibb Compnay

E. R. Squibb Sons, Inc.

Westwood Pharmaceuticals, Inc.

Richard A Partyka

Ronnie R Crenshaw

Thomas W Hudyma

Warren Neil Beverung, Jr

R Michael Lawrence

Dolatrai M Vyas

Scott A Biller

Terrence W Doyle

John E Lawson

Henry M Holava

Michael A Poss

Joseph Anthony Tino

Richard B Sulsky

David R Magnin

John K Dickson

George Michael Luke

Peter F Juby

Thomas A Montzka

John D Matiskella

Ramesh N Patel

Laszlo J Szarka

Thomas Andrew Jenks

Robert T Standridge

Henry Michael Holava

John Kenneth Dickson, Jr

Alex M Jelenevsky

Henry G Howell

Ronald Leslie Buchanan

Maxwell Gordon

Richard E Gregg

John R Wetterau, Ii

Alexander T Shulgin

Daru Young Sharp

Tetsuji Kametani

Gerry Kavadias

Elizabeth Janik

Terrance W Doyle

Kazuo Kigasawa

Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure ##STR1## wherein R.sup.1 to R.sup.7, Q, X and Y are as defined herein.

Inhibitors of microsomal triglyceride transfer protein and method

Methods for the enzymatic resolution of mixtures of enantiomers, such as .beta.-lactam compounds, which may be employed as intermediates in the preparation of taxanes such as taxol, the latter useful in the pharmaceutical field.

Lipase esterification processes for resolution of enantiomeric mixtures

Nucleic acid sequences, particularly DNA sequences, coding for all or part of the high molecular weight subunit of microsomal triglyceride transfer protein, expression vectors containing the DNA sequences, host cells containing the expression vectors, and methods utilizing these materials. The invention also concerns polypeptide molecules comprising all or part of the high molecular weight subunit of microsomal triglyceride transfer protein, and methods for producing these polypeptide molecules. The invention additionally concerns novel methods for preventing, stabilizing or causing regression of atherosclerosis and therapeutic agents having such activity. The invention concerns further novel methods for lowering serum liquid levels and therapeutic agents having such activity.

Nucleic acids encoding microsomal trigyceride transfer protein

Enzymatic processes for resolution of enantiomeric mixtures of compounds

A compound of formula I ##STR1## wherein X is sulfur or CH.sub.2 ;

Intermediates for cyclobutenedione substituted (1-carba)cephalosporin

A compound for formula I ##STR1## wherein X is sulfur or CH.sub.2 ;

Antibiotic C-3 cyclobutenedione substituted (1-carba) cephalosporin

Antibiotic C-3 cyclobutenedione substituted (1-carba)cephalosporin

The present invention provides novel mitomycin analogs containing a disulfide group and processes for the preparation thereof. These compounds are mitomycin A analogs in which the 7-alkoxy group bears an organic substituent incorporating a disulfide group. Mitomycin A is an antibiotic of established utility, and the 7-O-substituted mitosane analogs thereof have similar utility.

Substituted 7-oxomitosanes

Process for preparing mitomycin analogs

The compounds are of the class of 9-anilinoacridines, useful as antitumor agents and are analogs of m-AMSA. These compounds have the formula ##STR1## in which R.sup.1 is Br, Cl or CH.sub.3, and R.sup.2 is CH.sub.2 NHCH.sub.3, CH.sub.2 N(CHO)CH.sub.3 or CH.sub.2 NHCHO. Intermediate 3-substituted-9(10H)acridone-5-carboxylic acids are prepared by converting diphenylaminedicarboxylic acids via acyl chloride to dipiperidides, purifying the dipiperidides, treating said dipiperidides with phosphorous oxychloride in an inert organic solvent at a temperature in the range of about 70.degree. C. to 110.degree. C. to yield 9-acridine, subjecting said 9-acridine to mild acid hydroylsis to yield 9-acridone and thereafter hydroylzing said 9-acridones to the acid product.

Antitumor m-AMSA analog

Novel imidazole mercaptals of the formula ##STR1## wherein each m is independently zero or one; and R.sup.1 and R.sup.2 each are independently selected from (lower)alkyl, cycloalkyl, cycloalkyl(lower)alkyl, phenyl, phenyl(lower)alkyl, thienyl, thienyl(lower)alkyl, pyridyl and pyridyl(lower)alkyl, in which the phenyl and heterocyclic rings optionally may contain from 1 to 3 substituents, and acid addition salts thereof, are useful antimicrobial agents.

Sulfur-containing imidazoles

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Liverpool, NY, United States of America

Richard A Partyka