Eli Lilly and Company

Patrick C May

Dustin James Mergott

The present invention provides a method of treating a cognitive or neurodegenerative disease, comprising administering to a patient in need of such treatment an effective amount of a compound of the formula I, or a pharmaceutically acceptable salt thereof; in combination with an effective amount of an anti-N3pGlu Abeta monoclonal antibody. 

Combination Alzheimer therapy using anti-N3pGlu Abeta antibodies + a BACE inhibitor

This invention encompasses methods for the inhibition of Alzheimer's Disease comprising administering to a human in need thereof an effective amount of a compound of Formula I ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethylenemino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof. The present invention also provides methods of increasing TGF-.beta. expression in the brain, comprising administering to a human in need thereof an effective amount of a compound of formula 1. The present invention also provides methods of inhibiting the .beta.-amyloid peptide mediated neurotoxicity or inflammatory response associated with Alzheimer's Disease (AD) comprising administering to a human in need thereof an effective amount of a compound of formula 1.

Methods of inhibiting Alzheimer's Disease

This invention encompasses methods for the inhibition of Alzheimer's Disease comprising administering to a human in need thereof an effective amount of a compound of Formula I ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethylenemino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof. The present invention also provides methods of increasing TGF-.beta. expression in the brain, comprising administering to a human in need thereof an effective amount of a compound of formula 1. The present invention also provides methods of inhibiting the .beta.-amyloid peptide mediated neurotoxicity or inflammatory response associated with Alzheimer's Disease (AD) comprising administering to a human in need thereof an effective amount of a compound of formula 1.

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Carmel, IN, United States of America

Patrick C May