Assignee: Xenoport, Inc.

Location: Santa Clara, CA
No. of patents: 86

Number	Title	Issue Date
8168623	Prodrugs of GABA analogs, compositions and uses 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 pha...	05/01/2012
8168617	Complex pantoic acid ester neopentyl sulfonyl ester cyclization release prodrugs of acamprosate, compositions thereof, and methods of use Pantoic acid ester neopentyl sulfonyl ester prodrugs of acamprosate, pharmaceutical compositions comprising such prodrugs, and methods of using such prodrugs and compositions thereof for treating diseases are disclosed. In particular, acamprosate prodrugs exhibiting...	05/01/2012
8163958	Levodopa prodrugs, and compositions and uses thereof Prodrugs of levodopa, methods of making prodrugs of levodopa, methods of using prodrugs of levodopa, and compositions of prodrugs of levodopa are disclosed. ...	04/24/2012
8148414	Prodrugs of methyl hydrogen fumarate, pharmaceutical compositions thereof, and methods of use Prodrugs of methyl hydrogen fumarate, pharmaceutical compositions comprising prodrugs of methyl hydrogen fumarate, and methods of using prodrugs of methyl hydrogen fumarate and pharmaceutical compositions thereof for treating diseases such as psoriasis, asthma, mult...	04/03/2012
8143437	Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions 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 readil...	03/27/2012
8114909	Treating or preventing restless legs syndrome using prodrugs of GABA analogs Disclosed herein are methods of using prodrugs of gamma aminobutyric acid (GABA) analogs and pharmaceutical compositions thereof to treat or prevent restless legs syndrome in humans, and pharmaceutical compositions of prodrugs of GABA analogs useful in treating or p...	02/14/2012
8067455	Amino acid derived prodrugs of propofol, compositions, uses and crystalline forms thereof The present invention provides a prodrug of propofol and crystalline forms thereof, methods of making the propofol prodrug and crystalline forms thereof, pharmaceutical compositions of the propofol prodrug and crystalline forms thereof, methods of using the propofol...	11/29/2011
8062870	Enantiomerically resolving acyloxyalkyl thiocarbonates used in synthesizing acyloxyalkyl carbamate prodrugs Methods of enzymatically resolving acyloxyalkyl thiocarbonates useful in the synthesis of acyloxyalkyl carbamate prodrugs are disclosed. ...	11/22/2011
8058260	2′-C-methyl-ribofuranosyl cytidine prodrugs, pharmaceutical compositions and uses thereof The present disclosure provides 2′-C-methyl-ribofuranosyl cytidine prodrugs, methods of making 2′-C-methyl-ribofuranosyl cytidine prodrugs, pharmaceutical compositions of 2′-C-methyl-ribofuranosyl cytidine prodrugs, and methods of using 2′-C-methyl-ribofuran...	11/15/2011
8048917	Prodrugs of GABA analogs, compositions and uses 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 pha...	11/01/2011
8026279	Crystalline form of γ-aminobutyric acid analog A crystalline form of a γ-aminobutyric acid analog, and methods of preparing same, are provided. ...	09/27/2011
8017776	Methods for synthesis of acyloxyalkyl compounds Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require t...	09/13/2011
8003809	Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof 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-hydroxysuccinimid...	08/23/2011
7994218	Simple pantoic acid ester neopentyl sulfonyl ester cyclization release prodrugs of acamprosate, compositions thereof, and methods of use Pantoic acid ester neopentyl sulfonyl ester prodrugs of acamprosate, pharmaceutical compositions comprising such prodrugs, and methods of using such prodrugs and compositions thereof for treating diseases are disclosed. In particular, acamprosate prodrugs exhibiting...	08/09/2011
7989641	Methods of synthesizing -hydroxysuccinimidyl carbonates The present disclosure relates to methods of synthesizing N-hydroxysuccinimidyl-carbonate intermediates from the corresponding sulfones useful in the preparation of 1-(acyloxy)-alkyl carbamate prodrugs. ...	08/02/2011
7968597	Levodopa prodrug mesylate, compositions thereof, and uses thereof (2R)-2-Phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate and crystalline form thereof, methods of making the same, pharmaceutical compositions thereof, and methods of using the same to treat diseases or disorders such as Parkinson's dis...	06/28/2011
7956212	Levodopa prodrugs, and compositions and uses thereof Prodrugs of levodopa, methods of making prodrugs of levodopa, methods of using prodrugs of levodopa, and compositions of prodrugs of levodopa are disclosed. ...	06/07/2011
7935686	Acyloxyalkyl carbamate prodrugs, methods of synthesis, and use Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof, pharmaceutical compositions comprising acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs th...	05/03/2011
7919454	Methods of treating using conjugates transported by a PEPT2 transporter The invention provides methods of screening agents, conjugates or conjugate moieties, linked or linkable to agents, for capacity to be transported as substrates through the PEPT2 transporter. The invention also provides methods of treatment involving delivery of age...	04/05/2011
7893105	Levodopa prodrug mesylate, compositions thereof, and uses thereof (2R)-2-Phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate and crystalline form thereof, methods of making the same, pharmaceutical compositions thereof, and methods of using the same to treat diseases or disorders such as Parkinson's dis...	02/22/2011
7872046	Crystalline form of a (3S)-aminomethyl-5-methyl-hexanoic acid prodrug 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. ...	01/18/2011
7868043	Mesophasic forms of (3S)-aminomethyl-5-methyl-hexanoic acid prodrugs and methods of use Mesophasic forms of (3S)-aminomethyl-5-hexanoic acid prodrugs and methods of preparing and methods of using mesophasic forms of (3S)-aminomethyl-5-hexanoic acid prodrugs are provided. ...	01/11/2011
7868041	Cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs, compositions and uses thereof 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 o...	01/11/2011
7829592	Catechol protected levodopa diester prodrugs, compositions, and methods of use 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. ...	11/09/2010
7803785	Gemcitabine prodrugs, pharmaceutical compositions and uses thereof The present invention provides gemcitabine prodrugs, methods of making gemcitabine prodrugs, pharmaceutical compositions of gemcitabine prodrugs and methods of using gemcitabine prodrugs and pharmaceutical compositions of using gemcitabine prodrugs to treat or preve...	09/28/2010
7799829	Acyloxyalkyl carbamate prodrugs of α-amino acids, methods of synthesis and use Acyloxyalkyl carbamate prodrugs of α-amino acids, pharmaceutical compositions thereof, methods of making acyloxyalkyl carbamate prodrugs of α-amino acids and methods of using acyloxyalkyl carbamate prodrugs of α-amino acids, and pharmaceutical compositions thereo...	09/21/2010
7790708	Prodrugs of GABA analogs, compositions and uses 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 pha...	09/07/2010
7777070	Acyloxyalkyl carbamate prodrugs of tranexamic acid, methods of synthesis and use Acyloxyalkyl carbamate prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid, pharmaceutical compositions thereof, methods of making prodrugs of trans-4-(aminomethyl)-cyclohexane-carboxylic acid, and methods of using prodrugs of trans-4-(aminomethyl)-cyclohex...	08/17/2010
7767649	Amino acid conjugates providing for sustained systemic concentrations of GABA analogues This invention is directed to compounds that provide for sustained systemic concentrations of GABA analogs following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds. ...	08/03/2010
7749985	Acyloxyalkyl carbamate prodrugs, methods of synthesis and use Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, methods of making acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, methods of using acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic ac...	07/06/2010
7741062	Epitope-captured antibody display Reagents and methods for detecting target proteins in a sample are provided. The reagents include a replicable genetic package, a protein displayed on an exterior surface of the package that is expressed from a heterologous nucleic acid borne by the package, and one...	06/22/2010
7727976	Bile-acid derived compounds for enhancing oral absorption and systemic bioavailability of drugs Disclosed are compounds that exhibit high transport across the intestinal wall of an animal. The compounds may optionally be linked to drugs that are poorly absorbed or poorly transported across the intestinal wall after oral administration to provide for enhanced t...	06/01/2010
7709527	Levodopa dimethyl-substituted 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.	05/04/2010
7704696	Screening of compounds for OCTN2 transporter activity OCTN2 is consistently expressed at high levels in brain microvessel endothelial cells. Disclosed herein are assays for determining whether a test material/molecule is a substrate for, and/or is actively transported by, the OCTN2 transporter, and therefore a candidat...	04/27/2010
7704695	Screening of compounds for BGT1 transporter activity BGT1 is consistently expressed at high levels in brain microvessel endothelial cells. Disclosed herein are assays for determining whether a test material/molecule is a substrate for, and/or is actively transported by, the BGT1 transporter, and therefore a candidate ...	04/27/2010
7700652	Treating urinary incontinence using prodrugs of GABA analogs Disclosed herein are methods of using prodrugs of GABA analogs and pharmaceutical compositions thereof to treat and/or prevent urinary incontinence in humans, and pharmaceutical compositions of prodrugs of GABA analogs useful in treating and/or preventing urinary in...	04/20/2010
7700300	Screening of compounds for GAT2 transporter activity GAT2 is consistently expressed at high levels in brain microvessel endothelial cells. Disclosed herein are assays for determining whether a test material/molecule is a substrate for, and/or is actively transported by, the GAT2 transporter, and therefore a candidate ...	04/20/2010
7691584	Screening of compounds for OCT3 transporter activity OCT3 is consistently expressed at high levels in brain microvessel endothelial cells. Disclosed herein are assays for determining whether a test material/molecule is a substrate for, and/or is actively transported by, the OCT3 transporter, and therefore a candidate ...	04/06/2010
7683043	Creatine phosphate analog prodrugs, compositions and uses thereof Membrane permeable prodrugs of creatine phosphate analogs, pharmaceutical compositions comprising membrane permeable prodrugs of creatine phosphate analogs, and methods of treating diseases such as ischemia, heart failure, and neurodegenerative disorders comprising ...	03/23/2010
7678782	Bile-acid derived compounds for enhancing oral absorption and systemic bioavailability of drugs Disclosed are methods for providing enhanced systemic blood concentrations of orally delivered drugs that are incompletely translocated across the intestinal wall of an animal. Also disclosed are methods for the sustained release of drugs, whether poorly or readily ...	03/16/2010

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Assignee: Xenoport, Inc.