Abbott Laboratories Corporation

Abbvie Inc.

Margaret Chi-Ping Hsu

Chih-hung Lee

Arthur Gomtsyan

John R Koenig

Kirill A Lukin

Marvin Robert Leanna

Russell Drew Cink

Dilinie P Fernando

Erol K Bayburt

Robert G Schmidt

Gilles Chambournier

Anthony Ralph Haight

Richard J Perner

Brian J Kotecki

Matthew John Peterson

Howard E Morton

Yi-Yin Ku

James J Napier

Steven J Wittenberger

Jien-Heh J Tien

Steven A King

David R Hill

David A Riley

Daniel J Plata

Michael Rasmussen

Bikshandarkoil A Narayanan

Eric J Stoner

Arthur J Cooper

Robert M Leanna

Maureen Ann McLaughlin

Elaine C Lee

Prasad S Raje

Tim Grieme

Mahendra N Deshpande

Weijang Zhang

David Riley

Matthew J Peterson

Marvin R Leanna

Maureen A Mclaughlin

Dilini Fernando

The present invention relates to a process of preparing indazolyl ureas that are useful as antagonists of the vanilloid receptor subtype 1 (VR1).

Process for the preparation of indazolyl ureas that inhibit Vanilloid subtype 1 (VR1) receptors

The present invention discloses novel compounds of general formula (I) or a pharmaceutically acceptable salt or prodrug thereof (in which X-X, R-R, Z-Zand Arare defined herein), a method for inhibiting the VR1 receptor in mammals using these compounds, a method for controlling pain in mammals, and pharmaceutical compositions including those compounds and a process for making those compounds.

Fused compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor

The present invention discloses novel compounds of general formula (I) 

The present invention is directed to compounds of formula (I) wherein variables W, X, Y, D, A, n, R, Rand Rare as defined in the description.

Antagonists of the vanilloid receptor subtype 1 (VR1) and use thereof

Process for the preparation of indazolyl ureas that inhibit Vanilloid subtype1 (VR1) receptors

An efficient arylation technique for use in the synthesis of erythromycin derivatives, involving a modified Heck reaction which employs less than six mole percent of palladium catalyst and no phosphine is disclosed. With this modified Heck reaction, an O-alkenylaryl macrolide can be obtained in a much shorter reaction time than under conventional Heck reaction conditions. The modified Heck reaction can be utilized in a method for phosphine-free arylation of an O-allylic erythromycin derivative, in a method for preparing an O-alkenylaryl erythromycin A derivative, or in a method for preparing a 2', 4&#x2033;-hydroxyl protected 6-O-alkenylaryl erythromycin A derivative.

Arylation method for the functionalization of O-allyl erythromycin derivatives

In one aspect, the invention relates to a process for preparing 6-O-substituted erythromycin derivatives comprising reacting 2&prime;-substituted and optionally 4&Prime;-substituted 9-oxime erythromycin derivatives with an alkylating agent in the presence of a palladium catalyst and phosphine. In another aspect, the invention relates to processes for preparing 6-O-substituted erythromycin ketolides using the palladium-catalyzed alkylation reaction.

Process for preparing 6-o-substituted erythromycin derivatives

Growing community of inventors

Lake Forest, IL, United States of America

Margaret Chi-Ping Hsu