Abbott Laboratories Corporation

Abbvie Inc.

Robert M Leanna

Rodger F Henry

Thomas B Borchardt

Geoff G Zhang

Shuang Chen

Madhup K Dhaon

Michael Rasmussen

Larry Bartelt

Shekhar Viswanath

John K Pratt

Chih-hung Lee

Arthur Gomtsyan

John R Koenig

Howard E Morton

Anthony K Fung

Erol K Bayburt

Robert G Schmidt

William R Baker

Kirill A Lukin

Russell Drew Cink

Daniel J Plata

Gilles Chambournier

Margaret Chi-Ping Hsu

Chih-Hung Lee

Margaret Hsu

Russel D Cink

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

A process for preparing a crystalline rapamycin analog includes: combining the rapamycin analog with an organic medium to form a mixture; incubating the mixture until the rapamycin analog crystallizes; and recovering the crystalline rapamycin analog. The organic medium can be a solvent, and the process can include causing the rapamycin analog to dissolve into the solvent, and incubating the solvent until the rapamycin analog crystallizes. The following can also be performed: forming a slurry of crystalline rapamycin analog; stirring the rapamycin analog mixture until the rapamycin analog crystallizes; saturating the rapamycin analog solution; forming a supersaturated rapamycin analog solution; combining an antisolvent with the rapamycin analog and the solvent to form a biphasic mixture, and incubating the biphasic mixture to cause a liquid-liquid phase split.

Methods of manufacturing crystalline forms of rapamycin analogs

Provided is a rapamycin analog composition including a crystalline form of a rapamycin analog. The crystal can be a hydrate. dehydrate, solvate, or desolvate. The rampamycin analog can have a structure of Formula 1, which is optionally a prodrug, salt, derivative, or combination thereof: 

Crystalline forms of rapamycin analogs

A rapamycin analog composition includes a crystalline form of a rapamycin analog. The crystal can be a hydrate, dehydrate, solvate, or desolvate. The rapamycin analog can have a structure of Formula 1, which is optionally a prodrug, salt, derivative, or combination thereof: 

The present invention relates to intermediates useful in a process for the preparation of a compound of the formula: ##STR1## wherein R.sub.2a is hydrogen or loweralkyl, R.sub.2b is hydrogen, loweralkyl, cycloalkyl or phenyl and R.sub.1 is cycloalkyl, cycloalkylalkyl, phenyl or benzyl. These intermediates are compounds of the formula: ##STR2## wherein P.sub.2 is an O-protecting group, P.sub.3 is an N-protecting group and R.sub.1, R.sub.2a and R.sub.2b are defined as above.

Substantially isomerically pure hexane or hexene compounds

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Grayslake, IL, United States of America

Robert M Leanna