Xenoport, Inc.

Arbor Pharmaceuticals, LLC

Maria J Ludwikow

Mark A Gallop

Fenmei Yao

Ge Peng

Thu Phan

Stephen P Raillard

Suresh Kumar Manthati

Xuedong Dai

Randall A Scheuerman

Seema Rani Bhat

The disclosures herein relate generally to acyloxyalkyl carbamate prodrugs of (&#xb1;)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, pharmaceutical compositions thereof, methods of making prodrugs of (&#xb1;)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, methods of using prodrugs of (&#xb1;)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, and pharmaceutical compositions thereof for treating or preventing common diseases and/or disorders such as spasticity and/or acid reflux disease. The disclosures herein also relate to acyloxyalkyl carbamate prodrugs of (&#xb1;)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof which are suitable for oral administration and to sustained release oral dosage forms thereof.

Acyloxyalkyl carbamate prodrugs, methods of synthesis and use

Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof

Methods of enzymatically resolving acyloxyalkyl thiocarbonates useful in the synthesis of acyloxyalkyl carbamate prodrugs are disclosed.

Enantiomerically resolving acyloxyalkyl thiocarbonates used in synthesizing acyloxyalkyl carbamate prodrugs

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Cupertino, CA, United States of America

Maria J Ludwikow