Eli Lilly and Company

Allen R Harkness

Marvin M Hansen

Michael J Martinelli

Paul Leslie Ornstein

Bret E Huff

Susan M Reutzel

Vien V Khau

M Brian Arnold

Uko Effiong Udodong

Carl F Bertsch

Daniel Edward Verral, Ii

John Leo Grutsch, Jr

A physical form of (R)-7-acetyl-5-(4-aminophenyl)-8,9-dihydro-8-methyl-7H-1,3-dioxolo&lsqb;4,5-h&rsqb;&lsqb;2,3&rsqb;benzodiazepine having an X-ray powder diffraction pattern with d spacings at 10.61, 8.83, 6.78, 5.83, 4.13 and 3.74 &angst;. The compound is useful as an AMPA antagonist.

Physical form of dihydro-2,3-benzodiazepine derivative

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

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.

Process for preparing benzyl-substituted rhodanine derivatives

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Indianapolis, IN, United States of America

Allen R Harkness