Abbott Laboratories Corporation

Larry Bartelt

Rodger F Henry

Thomas B Borchardt

Geoff G Zhang

Shuang Chen

Madhup K Dhaon

Michael Rasmussen

Robert M Leanna

Shekhar Viswanath

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: 

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Larry Bartelt