Eli Lilly and Company

Akebia Therapeutics, Inc.

Lilly Icos LLC

James Denmore Copp

Francis O Ginah

Marvin M Hansen

Jason Scott Sawyer

Mark W Orme

Michael J Martinelli

Philip Arthur Hipskind

John M Janusz

Boris Gorin

Jan Oudenes

Douglas P Kjell

Bret E Huff

Craig Edward Dixon

Michael A Staszak

Christopher M Lanthier

Sung Y Cho

Alan Quigbo Lu

Brian James Slattery

Roger W Tharp-Taylor

Guy J Hansen

Gregg A Tharp

Disclosed are processes for preparing [(3-hydroxypyridine-2-carbonyl)amino]-alkanoic acids, derivatives, inter alia, 5-aryl substituted and 5-heteroaryl substituted [(3-hydroxypyridine-2-carbonyl]amino}acetic acids. Further disclosed are methods for making prodrugs of [(3-hydroxypyridine-2-carbonyl)-amino]acetic acids, for example, [(3-hydroxypyridine-2-carbonyl]amino}acetic acid esters and {[3-hydroxypyridine-2-carbonyl]amino}acetic acid amides. The disclosed compounds are useful as prolyl hydroxylase inhibitors or for treating conditions wherein prolyl hydroxylase inhibition is desired.

Process for preparing [(3-hydroxypyridine-2-carbonyl)amino] alkanoic acids, esters and amides

Compounds of general structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents as inhibitors of phosphodiesterase 5 cardiovascular disorders 

Chemical compounds

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

This invention provides novel compound of the formula ##STR1## which is neurokinin receptor antagonist.

Bis-piperidinyl non-peptidyl neurokinin receptor antagonists

3-Exomethylenecepham sulfoxide esters are obtained in improved yields via cyclization of 3-methyl-2-(4-chlorosulfinyl-2-oxo-3-acylamino-1-azetidinyl)-3-butenoic acid esters under anhydrous conditions with stannic chloride in the presence of both an oxo compound, e.g., an ether such as diethyl ether, a ketone such as acetone or methylethyl ketone, and an unsaturated compound, e.g., an alkene such as 1- or 2-hexene, a non-conjugated alkadiene such as 1,4-hexadiene, a cycloalkene such as cyclohexene, an allene, or a non-conjugated cycloalkadiene such as 1,4-cyclohexadiene.

Process for 3-exomethylenecepham sulfoxide esters

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Greenwood, IN, United States of America

James Denmore Copp