Xenoport, Inc.

Arbor Pharmaceuticals, LLC

Xero Port, Inc.

Fenmei Yao

Mark A Gallop

Jia-Ning Xiang

Cindy X Zhou

Ge Peng

Maria J Ludwikow

Thu Phan

Stephen P Raillard

Kenneth C Cundy

Suresh Kumar Manthati

Laxminarayan Bhat

Xuedong Dai

Randall A Scheuerman

Seema Rani Bhat

Mark Quang Nguyen

Fayang Gregory Qiu

Ronald W Barrett

Peter Virsik

Ian R Ollman

Ian R Ollmann

Peter A Virsik

Fayang G Qiu

Maria Ludwikow

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

The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using pharmaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders.

Methods of using prodrugs of pregabalin

Catechol protected levodopa diester prodrugs pharmaceutical, compositions comprising catechol protected levodopa diester prodrugs, and methods of using such prodrugs and pharmaceutical compositions for treating diseases such as Parkinson's disease are provided.

Catechol protected levodopa diester prodrugs, compositions, and methods of use

Levodopa dimethyl-substituted diester prodrugs pharmaceutical, compositions comprising levodopa dimethyl-substituted diester prodrugs, and methods of using such prodrugs and pharmaceutical compositions for treating diseases such as Parkinson's disease are provided.

Levodopa dimethyl-substituted diester prodrugs, compositions, and methods of use

A crystalline form of a (3S)-aminomethyl-5-hexanoic acid prodrug and methods of preparing a crystalline form of a (3S)-aminomethyl-5-hexanoic acid prodrug, and methods of using a crystalline form of a (3S)-aminomethyl-5-hexanoic acid prodrug are provided.

Crystalline form of a (3S)-aminomethyl-5-methyl-hexanoic acid prodrug and methods of use

Prodrugs of GABA analogs, compositions and uses thereof

The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.

Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions 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

The present invention provides cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs, methods of making cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs. The present invention also provides methods of using cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs.

Cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs, compositions and uses thereof

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Mountain View, CA, United States of America

Fenmei Yao