Eli Lilly and Company

Marvin M Hansen

Benjamin Alan Anderson

Allen R Harkness

Michael J Martinelli

David Lee Varie

Milton J Zmijewski

Jeffrey Thomas Vicenzi

James Denmore Copp

Francis O Ginah

Paul Leslie Ornstein

Thomas Edward Mabry

Kumiko Takeuchi

Owen Brendan Wallace

Vincent Patrick Rocco

Yanping Xu

Nancy June Snyder

Douglas P Kjell

Bret E Huff

Patrick Gianpietro Spinazze

Julie Kay Bush

Nancy Kay Harn

Daniel James Koch

Renhua Li

Todd Jonathan Kohn

John Xiaoqiang He

Nicholas Allan Honigschmidt

Susan M Reutzel

Vien V Khau

Uko Effiong Udodong

M Brian Arnold

Carl F Bertsch

Brian James Slattery

Daniel Edward Verral, Ii

John Leo Grutsch, Jr

The present invention discloses novel compounds of Formula I: (I) having 11-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11-HSD type 1 activity. 

Inhibitors of 11-beta-hydroxysteroid dehydrogenase 1

The present invention provides compounds of formula (I): which are useful for treating depression, anxiety, and alleviating the symptoms caused by withdrawal or partial withdrawal from the use of tobacco or of nicotine. 

Indole derivatives for the treatment of depression and anxiety

The instant invention provides a novel process for preparing benzyl-substituted rhodanine derivatives. Also provided are novel benzyl-substituted thiolamides and benzyl-substituted hemithioacetals. Such compounds are useful as intermediates in preparing the compounds by the process of the instant invention.

Process for preparing benzyl-substituted rhodanine derivatives

Alternate crystal form of Tazofelone

The present invention provides phosphonylating agents and phosphonylation conditions that are compatible with the acid- and base-sensitive compounds and which promote a regioselective and reproducible conversion to a phosphonate compound. Also provided are intermediates that may be used to prepare phosphonate derivatives of cyclic peptides antifungal agent and a process for converting the phosphonates to the desired phosphonic acid prodrugs.

Cyclic peptide antifungal agents

The invention relates to benzopyranol derivatives which are intermediates in a process for stereoselectively forming N-substituted dihydro-2,3 benzodiazopines which are useful as AMPA receptor antagonists. The process includes an opening reduction step which sets the stereochemistry of the intermediates and the final compounds to the desired enantiomer. The reduction step may be carried out by an enzymatic reduction.

Benzopyranol derivatives

A process for stereoselectively forming N-substituted dihydro-2,3 benzodiazepines which are useful as AMPA receptor antagonists. The process includes an opening reduction step which sets the stereochemistry of the intermediates and the final compounds to the desired enantiomer. The reduction step may be carried out by an enzymatic reduction.

Stereoselective process for producing dihydro-2,3-benzodiazepine

Dihydro-2,3-benzodiazepine derivatives

This invention provides novel decahydroisoquinoline compounds which are useful as excitatory amino acid receptor antagonists and in the treatment of neurological disorders. This invention also provides synthetic methods for preparing decahydroisoquinolines, as well as, novel intermediates in the synthesis thereof.

Process for preparing isoquinoline compounds

The instant invention provides a novel process for preparing benzyl-substituted rhodanine derivatives. The process is particularly useful for synthesizing the enantiomers of such derivatives. Also provided are novel benzyl-substituted mercaptopropanoic acids and benzyl-substituted thiazolidinones. Such compounds are useful for treating inflammatory bowel disease and, accordingly, the present invention provides a method of treating inflammatory bowel disease in mammals utilizing such novel compounds as well as pharmaceutical compositions containing same.

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Indianapolis, IN, United States of America

Marvin M Hansen