Elan Pharmaceuticals, Inc.

Ashley C Guinn

Jay S Tung

Michael A Pleiss

Darren B Dressen

Jing Wu

Albert W Garofalo

David W G Wone

Eugene D Thorsett

Varghese John

Lawrence Y Fang

Roy K Hom

R Jeffrey Neitz

Shumeye Mamo

Andrea Gailunas

Martin Neitzel

Jennifer Marugg

Lee H Latimer

John Alan Tucker

Jennifer Sealy

Scott A Jenkins

This invention is directed to acylated amino acid amidyl pyrazoles and related compounds of Formula I. The invention is also directed to a pharmaceutical formation comprising such compound or in a pharmaceutically acceptable salt form thereof. The invention is further directed to a method for inhibiting &#x3b2;-amyloid peptide release and/or synthesis, a method for inhibiting &#x3b3;-secretase activity, and a method for treating neurological disorders associated with &#x3b2;-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula I. The compounds of Formula I are useful in the prevention and treatment of Alzheimer's disease.

Acylated amino acid amidyl pyrazoles and related compounds

Disclosed are compounds that are bradykinin Breceptor antagonists and are useful for treating diseases, or relieving adverse symptoms associated with disease conditions, in mammals mediated by bradykinin Breceptor. Certain of the compounds exhibit increased potency and are also expected to exhibit increased duration of action.

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Disclosed are compounds of formula I and II that are bradykinin Breceptor antagonists and are useful for treating diseases, or relieving adverse symptoms associated with disease conditions, in mammals mediated by bradykinin Breceptor. Certain of the compounds exhibit increased potency and are also expected to exhibit increased duration of action. 

Dipeptide derived inhibitors of the &#x3b2;-secretase enzyme are provided which are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A&#x3b2; peptide in a mammal. The compounds of the invention provide useful methods of treatment by administration of these inhibitors to reduce A&#x3b2; peptide formation and in pharmaceutical compositions.

Dipeptide inhibitors of &#x3b2;-secretase

This invention is directed to a class of compounds (Formula I) including hydroxyalkanoyl amino pyrazoles, hydroxyalkanoyl amino thiadiazoles, hydroxyalkanoyl amino acid esters, hydroxyalkanoyl amino acid amides, hydroxyalkanoyl amino alcohols, hydroxyalkanoyl amino ketoes, hydroxyalkanoyl amino hydantoins, hydroxyalkanoyl anilines, and hydroxyalkanoyl derivatives of privileged structures. The invention is also directed to a pharmaceutical formation comprising such compound in a pharmaceutically acceptable salt form or prodrug thereof. The invention is further directed to a method for inhibiting &#x3b2;-amyloid peptide release and/or synthesis, a method for inhibiting &#x3b3;-secretase activity and a method for treating neurological disorders associated with &#x3b2;-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula I. The compounds of Formula I are useful in the prevention and treatment of Alzheimer's disease.

Hydroxyalkanoyl aminopyrazoles and related compounds

This invention is directed to a class of compounds (Formula I) including succinoyl amino pyrazoles, succinoyl amino thiadiazoles, succinoyl amino acid esters, succinoyl amino acid amides, succinoyl amino alcohols, succinoyl amino ketones, succinoyl amino hydantoins, succinoyl anilines, and succinoyl derivatives of privileged structures. The invention is also directed to a pharmaceutical formation comprising such compound in a pharmaceutically acceptable salt form or prodrug thereof. The invention is further directed to a method for inhibiting &#x3b2;-amyloid peptide release and/or synthesis, a method for inhibiting &#x3b3;-secretase activity and a method for treating neurological disorders associated with &#x3b2;-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula I. The compounds of Formula I are useful in the prevention and treatment of Alzheimer's disease.

Succinoyl aminopyrazoles and related compounds

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Pacifica, CA, United States of America

Ashley C Guinn