Eli Lilly and Company

John Kevin Shadle

Jill A Panetta

Michael LeRoy Phillips

John Robert Rizzo

Benjamin Alan Anderson

David Lee Varie

Lawrence Joseph Heinz, Ii

John Allan Rieck, Iii

Jon Kevin Reel

Richard L Simon

Celia A Whitesitt

William H Lunn

Sandra K Sigmund

William F Heath, Jr

Lawrence J Heinz

This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.

Methods of using novel compounds as neuro-protective agents

Methods of using compounds as neuro-protective agents

Compounds useful as neuro-protective agents

This invention provides novel benzylidene rhodanines which are useful as agents in treating or preventing conditions associated with &bgr;-amyloid peptide. This invention further provides methods of treating or preventing Alzheimer's Disease which comprises administering to a mammal in need thereof an effective amount of one or more of the benzylidene rhodanines of the present invention.

Treatment of alzheimer's disease employing inhibitors of cathepsin D

A method of protecting a warm-blooded mammal from the progression of Alzheimer's disease, which comprises administering an effective amount of a compound of general formula. ##STR1## in which: R.sup.1 represents an optionally substituted aromatic or heteroaromatic group;

Inhibitors of amyloid beta-protein production

This invention provides novel benzylidene rhodanines which are useful as agents in treating or preventing conditions associated with .beta.-amyloid peptide. This invention further provides methods of treating or preventing Alzheimer's Disease which comprises administering to a mammal in need thereof an effective amount of one or more of the benzylidene rhodanines of the present invention.

Benzylidene rhodanines

The present invention provides novel urea, thiourea and guanidine derivatives, pharmaceutical formulations thereof and a method of using same to prevent diabetic complications.

Urea, thiourea and guanidine derivatives

Broad spectrum cephalosporin betaine antibiotics represented by the formula ##STR1## wherein R' is a heterocyclic ring, e.g. 2-aminothiazol-4-yl, 2-amino-1,3,5-thiadiazol-4-yl, or 2-aminopyridin-6-yl; R' is C.sub.1 -C.sub.4 alkyl, especially methyl, a substituted carbamoyl group, or a carboxy-substituted alkyl or cycloalkyl group; and R.sub.1 is isoquinolinium or a substituted isoquinolinium group are provided. Compounds wherein R.sub.1 is isoquinolinium are preferred especially syn-7-[2-(2-aminothiazol-4-yl)-2-methoxyiminoacetamido]-3-(isoquinolinium- 2-ylmethyl)-3-cephem-4-carboxylate. Pharmaceutical formulations and a method for treating infectious diseases comprising the use of the antibiotics are described.

Cephalosporin betaines

Cephalosporin antibiotics represented by the formula ##STR1## wherein R is hydrogen, C.sub.1 -C.sub.4 alkyl or a carboxy substituted alkyl group; R.sub.1 is H or C.sub.1 -C.sub.4 alkyl; n is 0, 1 or 2; and A and A' independently are hydrogen, C.sub.1 -C.sub.4 alkyl or allyl; and pharmaceutically acceptable salts thereof are broad spectrum antibiotics useful in the treatment of gram positive and gram negative infections of mammals.

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Fishers, IN, United States of America

John Kevin Shadle