XenoPort, Inc. Patent applications |
Patent application number | Title | Published |
20160113879 | ORAL DOSAGE FORMS OF METHYL HYDROGEN FUMARATE AND PRODRUGS THEREOF - Improved oral dosage forms of methyl hydrogen fumarate and prodrugs thereof are disclosed. Methods of treating diseases such as multiple sclerosis and psoriasis using such dosage forms are also disclose. | 04-28-2016 |
20160090353 | 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 pharmaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders. | 03-31-2016 |
20150353483 | CRYSTALLINE FORM OF y-AMINOBUTYRIC ACID ANALOG - A crystalline form of a γ-aminobutyric acid analog, and methods of preparing same, are provided. | 12-10-2015 |
20150313865 | ANHYDROUS AND HEMIHYDRATE CRYSTALLINE FORMS OF AN (R)-BACLOFEN PRODRUG, METHODS OF SYNTHESIS AND METHODS OF USE - Crystalline (3R)-4-{[(1S)-2-methyl-1-(2-methylpropanoyloxyl)propoxy]carbonylamino}-3-(4-chlorophenyl)butanoic acid anhydrate and crystalline (3R)-4-{[(1S)-2-methyl-1-(2-methylpropanoyloxyl)propoxy]carbonylamino}-3-(4-chlorophenyl)butanoic acid hemihydrate, pharmaceutical compositions comprising such compounds, methods of making and methods of using the same are disclosed. | 11-05-2015 |
20150158809 | METHOD OF MAKING 1-(ACYLOXY)-ALKYL CARBAMATE COMPOUNDS - Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided. | 06-11-2015 |
20150157590 | COCRYSTALS OF (N,N-DIETHYLCARBAMOYL)METHYL METHYL (2E)BUT-2-ENE-1,4-DIOATE - Disclosed herein are cocrystals of (N,N-Diethylcarbamoyl)methyl methyl (2E)but-2-ene-1,4-dioate, which is a prodrug of methyl hydrogen fumarate. | 06-11-2015 |
20140350018 | Methods of Administering Monomethyl Fumarate and Prodrugs Thereof Having Reduced Side Effects - Methods of reducing undesirable side effects during therapeutic treatment using monomethyl fumarate and prodrugs of monomethyl fumarate are disclosed. | 11-27-2014 |
20140348915 | Oral Dosage Forms of Methyl Hydrogen Fumarate and Prodrugs Thereof - Improved oral dosage forms of methyl hydrogen fumarate and prodrugs thereof are disclosed. Methods of treating diseases such as multiple sclerosis and psoriasis using such dosage forms are also disclosed. | 11-27-2014 |
20140348914 | Oral Dosage Forms of Methyl Hydrogen Fumarate and Prodrugs Thereof - Improved oral dosage forms of methyl hydrogen fumarate and prodrugs thereof are disclosed. Methods of treating diseases such as multiple sclerosis and psoriasis using such dosage forms are also disclosed. | 11-27-2014 |
20140284245 | PHARMACEUTICAL COMPOSITIONS OF DIMETHYL FUMARATE - Pharmaceutical compositions and dosage forms of dimethyl fumarate containing low levels of certain impurities are disclosed. | 09-25-2014 |
20140275250 | Methods of Administering Monomethyl Fumarate - Methods of therapeutic treatment using monomethyl fumarate are disclosed. | 09-18-2014 |
20140243544 | METHOD OF MAKING 1-(ACYLOXY)-ALKYL CARBAMATE COMPOUNDS - Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided. | 08-28-2014 |
20140235710 | CRYSTALLINE FORM OF y-AMINOBUTYRIC ACID ANALOG - A crystalline form of a γ-aminobutyric acid analog, and methods of preparing same, are provided. | 08-21-2014 |
20140179778 | COCRYSTALS OF (N,N-DIETHYLCARBAMOYL)METHYL METHYL (2E)BUT-2-ENE-1,4-DIOATE - Disclosed herein are cocrystals of (N,N-Diethylcarbamoyl)methyl methyl (2E)but-2-ene-1,4-dioate, which is a prodrug of methyl hydrogen fumarate. | 06-26-2014 |
20140066501 | Anhydrous and Hemihydrate Crystalline Forms of an (R)-Baclofen Prodrug, Methods of Synthesis and Methods of Use - Crystalline (3R)-4-{[(1S)-2-methyl-1-(2-methylpropanoyloxy)propoxy]carbonylamino}-3-(4-chlorophenyl)butanoic acid anhydrate and crystalline (3R)-4-{[(1S)-2-methyl-1-(2-methylpropanoyloxy)propoxy]carbonylamino}-3-(4-chlorophenyl)butanoic acid hemihydrate, pharmaceutical compositions comprising such compounds, methods of making and methods of using the same are disclosed. | 03-06-2014 |
20140065211 | Oral Dosage Forms of Methyl Hydrogen Fumarate and Prodrugs Thereof - Improved oral dosage forms of methyl hydrogen fumarate and prodrugs thereof are disclosed. Methods of treating diseases such as multiple sclerosis and psoriasis using such dosage forms are also disclosed. | 03-06-2014 |
20140057918 | Methods of Use for Monomethyl Fumarate and Prodrugs Thereof - Methods of therapeutic treatment using monomethyl fumarate and prodrugs of monomethyl fumarate are disclosed. | 02-27-2014 |
20140057917 | Methods of Administering Monomethyl Fumarate and Prodrugs Thereof Having Reduced Side Effects - Methods of reducing undesirable side effects during therapeutic treatment using monomethyl fumarate and prodrugs of monomethyl fumarate are disclosed. | 02-27-2014 |
20140056978 | Oral Dosage Forms of Methyl Hydrogen Fumarate and Prodrugs Thereof - Improved oral dosage forms of methyl hydrogen fumarate and prodrugs thereof are disclosed. Methods of treating diseases such as multiple sclerosis and psoriasis using such dosage forms are also disclosed. | 02-27-2014 |
20140056973 | Oral Dosage Forms Having a High Loading of a Methyl Hydrogen Fumarate Prodrug - Oral dosage forms and granulations with a high loading of a methyl hydrogen fumarate prodrug are disclosed. | 02-27-2014 |
20140051705 | Morpholinoalkyl Fumarate Compounds, Pharmaceutical Compositions, and Methods of Use - Morpholinoalkyl fumarates, pharmaceutical compositions comprising the morpholinoalkyl fumarates, and methods of using morpholinoalkyl fumarates and pharmaceutical compositions for treating neurodegenerative, inflammatory, and autoimmune disorders including multiple sclerosis, psoriasis, irritable bowel disorder, ulcerative colitis, arthritis, chronic obstructive pulmonary disease, asthma, Parkinson's disease, Huntington's disease, and amyotrophic lateral sclerosis are disclosed. | 02-20-2014 |
20130203753 | MORPHOLINOALKYL FUMARATE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE - Morpholinoalkyl fumarates, pharmaceutical compositions comprising the morpholinoalkyl fumarates, and methods of using morpholinoalkyl fumarates and pharmaceutical compositions for treating neurodegenerative, inflammatory, and autoimmune disorders including multiple sclerosis, psoriasis, irritable bowel disorder, ulcerative colitis, arthritis, chronic obstructive pulmonary disease, asthma, Parkinson's disease, Huntington's disease, and amyotrophic lateral sclerosis are disclosed. | 08-08-2013 |
20130184344 | LEVODOPA PRODRUG MESYLATE HYDRATE - Crystalline (2R)-2-phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate, hydrate, methods of making the hydrate, pharmaceutical compositions containing the hydrate, and methods of using the hydrate to treat diseases or disorders such as Parkinson's disease are provided. | 07-18-2013 |
20130131355 | 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-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described. | 05-23-2013 |
20130102641 | 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 pharmaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders. | 04-25-2013 |
20130041026 | ANHYDROUS AND HEMIHYDRATE CRYSTALLINE FORMS OF AN (R)-BACLOFEN PRODRUG, METHODS OF SYNTHESIS AND METHODS OF USE - Crystalline (3R)-4-{[(1S)-2-methyl-1-(2-methylpropanoyloxy)propoxy]carbonylamino}-3-(4-chlorophenyl)butanoic acid anhydrate and crystalline (3R)-4-{[(1S)-2-methyl-1-(2-methylpropanoyloxy)propoxy]carbonylamino}-3-(4-chlorophenyl)butanoic acid hemihydrate, pharmaceutical compositions comprising such compounds, methods of making and methods of using the same are disclosed. | 02-14-2013 |
20120296109 | Levodopa Prodrugs, and Compositions 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 disease are provided. | 11-22-2012 |
20120190861 | 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. | 07-26-2012 |
20120157523 | 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, multiple sclerosis, inflammatory bowel disease, and arthritis are disclosed. | 06-21-2012 |
20120095003 | METHODS OF USING PRODRUGS OF METHYL HYDROGEN FUMARATE AND PHARMACEUTICAL COMPOSITIONS THEREOF - 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, multiple sclerosis, inflammatory bowel disease, and arthritis are disclosed. | 04-19-2012 |
20120082645 | 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-ribofuranosyl cytidine prodrugs and pharmaceutical compositions thereof to treat viral diseases such as hepatitis C. | 04-05-2012 |
20120035258 | METHODS OF USING PRODRUGS OF PREGABALIN - 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. | 02-09-2012 |
20120016021 | METHODS OF TREATING FRAGILE X SYNDROME, DOWN'S SYNDROME, AUTISM AND RELATED DISORDERS - Disclosed herein are methods of treating fragile X syndrome, fragile X-associated tremor/ataxia syndrome, Down's syndrome and other forms of mental retardation, and/or autism comprising administering a GABA | 01-19-2012 |
20120010425 | 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-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described. | 01-12-2012 |
20110313036 | CRYSTALLINE FORM OF y-AMINOBUTYRIC ACID ANALOG - A crystalline form of a γ-aminobutyric acid analog, and methods of preparing same, are provided. | 12-22-2011 |
20110294879 | METHOD OF TREATMENT OF FRAGILE X SYNDROME, DOWN'S SYNDROME, AUTISM AND RELATED DISORDERS - Disclosed herein are methods of treating fragile X syndrome, fragile X-associated tremor/ataxia syndrome, Down's syndrome and/or autism, comprising administering a prodrug of acamprosate to a subject suffering therefrom, wherein, in certain embodiments, the acamprosate prodrugs comprise compounds of Formula (I). | 12-01-2011 |
20110224295 | 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. | 09-15-2011 |
20110201817 | 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. | 08-18-2011 |
20110130454 | PRODRUGS OF GAMMA-AMINO ACID, ALPHA-2-DELTA LIGANDS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF - Prodrugs of alpha-2-delta ligands, pharmaceutical compositions of prodrugs of alpha-2-delta ligands, methods of making prodrugs of alpha-2-delta ligands, and methods of using prodrugs of alpha-2-delta ligands and pharmaceutical compositions of prodrugs of alpha-2-delta ligands to treat various diseases are disclosed. | 06-02-2011 |
20110124705 | PRODRUGS OF ALPHA-2-DELTA LIGANDS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF - Prodrugs of alpha-2-delta ligands, pharmaceutical compositions of prodrugs of alpha-2-delta ligands, methods of making prodrugs of alpha-2-delta ligands, and methods of using prodrugs of alpha-2-delta ligands and pharmaceutical compositions of prodrugs of alpha-2-delta ligands to treat various diseases are disclosed. | 05-26-2011 |
20110028544 | 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. | 02-03-2011 |
20110021628 | CRYSTALLINE FORM OF y-AMINOBUTYRIC ACID ANALOG - A crystalline form of a γ-aminobutyric acid analog, and methods of preparing same, are provided. | 01-27-2011 |
20110021571 | ACYLOXYALKYL CARBAMATE PRODRUGS, METHODS OF SYNTHESIS AND USE - The disclosures herein relate generally to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, pharmaceutical compositions thereof, methods of making prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, methods of using prodrugs of (±)-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 (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof which are suitable for oral administration and to sustained release oral dosage forms thereof. | 01-27-2011 |
20110009483 | 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)-cyclohexanecarboxylic acid and pharmaceutical compositions thereof to treat or prevent various diseases or disorders are disclosed. Acyloxyalkyl carbamate prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid and pharmaceutical compositions thereof suitable for oral and topical administration and for administration using sustained release dosage forms are also disclosed. | 01-13-2011 |
20100267946 | 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 pharmaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders. | 10-21-2010 |
20100255093 | SUSTAINED RELEASE ORAL DOSAGE FORMS OF AN R-BACLOFEN PRODRUG - Sustained release oral dosage forms of an R-baclofen prodrug are disclosed. | 10-07-2010 |
20100226981 | ORAL DOSAGE FORMS HAVING A HIGH LOADING OF A GABAPENTIN PRODRUG - Sustained release oral dosage forms with a high loading of a gabapentin prodrug are disclosed. | 09-09-2010 |
20100197953 | 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. | 08-05-2010 |
20100173992 | 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. | 07-08-2010 |
20100137442 | Sustained Release Particulate Oral Dosage Forms of (R)-Baclofen and Methods of Treatment - Sustained release particulate oral dosage forms of (R)-baclofen prodrugs and methods of treating a disease comprising orally administering such dosage forms are disclosed. | 06-03-2010 |
20100137255 | 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 administering prodrugs of creatine phosphate analogs, or pharmaceutical compositions thereof are disclosed. | 06-03-2010 |
20100087667 | METHODS OF SYNTHESIZING 1-(ACYLOXY)-ALKYL CARBAMATE PRODRUGS - The present disclosure relates to methods of synthesizing 1-(acyloxy)-alkyl carbamate prodrugs and to intermediates used in the methods. | 04-08-2010 |
20100087536 | 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 prodrug and crystalline forms thereof and pharmaceutical compositions thereof to treat diseases or disorders such as headache pain, post-chemotherapy or post-operative surgery nausea and vomiting, neurodegenerative disorders, and mood disorders. | 04-08-2010 |
20100081830 | METHODS OF SYNTHESIZING N-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. | 04-01-2010 |
20100056632 | CRYSTALLINE FORM OF y-AMINOBUTYRIC ACID ANALOG - A crystalline form of a γ-aminobutyric acid analog, and methods of preparing same, are provided. | 03-04-2010 |
20100048651 | 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, multiple sclerosis, inflammatory bowel disease, and arthritis are disclosed. | 02-25-2010 |
20100041882 | 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 the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up. | 02-18-2010 |
20100036148 | 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)-cyclohexanecarboxylic acid and pharmaceutical compositions thereof to treat or prevent various diseases or disorders are disclosed. Acyloxyalkyl carbamate prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid and pharmaceutical compositions thereof suitable for oral and topical administration and for administration using sustained release dosage forms are also disclosed. | 02-11-2010 |
20100016254 | 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 prevent diseases or disorders such as cancer or viral infections. | 01-21-2010 |
20100004332 | 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. | 01-07-2010 |
20090326067 | 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 disease are provided. | 12-31-2009 |
20090312424 | AROMATIC PRODRUGS OF PROPOFOL, COMPOSITIONS AND USES THEREOF - Prodrugs of propofol, methods of making prodrugs of propofol, pharmaceutical compositions of prodrugs of propofol and methods of using prodrugs of propofol and pharmaceutical compositions thereof to treat or prevent diseases or disorders such as migraine headache pain and post-chemotherapy or post-operative surgery nausea and vomiting are disclosed herein. | 12-17-2009 |
20090306036 | METHODS OF SCREENING AGENTS, CONJUGATES OR CONJUGATE MOIETIES FOR TRANSPORT 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 agents that either alone, or as a result of linkage to a conjugate moiety, are substrates of the PEPT2 transporter. The invention also provides conjugates comprising a pharmaceutical agent which is linked to a conjugate moiety that is a substrate for a PEPT2 transporter. | 12-10-2009 |
20090286763 | AMINO ACID DERIVED PRODRUGS OF PROPOFOL, COMPOSITIONS AND USES THEREOF - The present invention provides propofol prodrugs, methods of making propofol prodrugs, pharmaceutical compositions of propofol prodrugs and methods of using propofol prodrugs and pharmaceutical compositions thereof to treat or prevent diseases or disorders such as migraine headache pain and post-chemotherapy or post-operative surgery nausea and vomiting. | 11-19-2009 |
20090286759 | 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 acid and analogs thereof, and pharmaceutical compositions comprising acyloxyalkyl carbamate prodrugs 3-aminopropylphosphinic acid and analogs thereof for treating diseases or disorders such as mild cognitive impairment, cognitive impairment associated with Alzheimer's disease Alzheimer's disease, depression, anxiety, and epilepsy are disclosed. Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, which are suitable for oral administration and sustained release oral dosage forms are also disclosed. | 11-19-2009 |
20090280999 | 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 or more antibodies complexed with the expressed protein and which have an open binding site for a target protein. Thus, a segment of the nucleic acid encodes for an epitope that is shared by the expressed polypeptide and the target protein. The reagents can be utilized individually or as part of a library or an array to bind target proteins within protein samples to form one or more complexes. By determining the sequence of the segment of the heterologous nucleic acid of a package within a complex, one can identify the target protein since the segment encodes for an epitope that is shared by the expressed and target proteins. | 11-12-2009 |
20090270493 | 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 of using cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs. | 10-29-2009 |
20090239950 | 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 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. | 09-24-2009 |
20090221442 | SUBSTRATES AND SCREENING METHODS FOR TRANSPORT PROTEINS - A variety of methods for assaying libraries of test compounds as ligands and/or substrates of transport proteins, including both carrier-type and receptor-type transport proteins, are provided. Both in vitro and in vivo screening methods are disclosed. Also provided are methods for screening DNA libraries to identify members that encode transport proteins. Pharmaceutical compositions including compounds identified via the screening methods are also provided. | 09-03-2009 |
20090216037 | Synthesis of Acyloxyalkyl Carbamate Prodrugs and Intermediates Thereof - Methods for synthesis of | 08-27-2009 |
20090215809 | 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. | 08-27-2009 |
20090209465 | MCT1 Transporters Expressed in Blood Brain Barrier Cells - MCT1 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 MCT1 transporter, and therefore a candidate substrate for crossing the blood brain barrier. The assays are useful in screening for therapeutic, cytotoxic or imaging compounds used in the treatment or diagnosis of neurological diseases. | 08-20-2009 |
20090197958 | Sustained Release Particulate Oral Dosage Forms of (R) Baclofen and Methods of Treatment - Sustained release particulate oral dosage forms of (R)-baclofen prodrugs and methods of treating a disease comprising orally administering such dosage forms are disclosed. | 08-06-2009 |
20090192325 | 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. | 07-30-2009 |
20090192225 | Acyloxyalkyl Carbamate Prodrugs of Alpha-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 thereof to treat a disease are disclosed. Acyloxyalkyl carbamate prodrugs of α-amino acids suitable for oral administration using sustained release dosage forms are also disclosed. | 07-30-2009 |
20090192222 | 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. | 07-30-2009 |
20090148884 | LAT1 TRANSPORTERS EXPRESSED IN BLOOD BRAIN BARRIER CELLS - LAT1 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 LAT1 transporter, and therefore a candidate substrate for crossing the blood brain barrier. The assays are useful in screening for therapeutic, cytotoxic or imaging compounds used in the treatment or diagnosis of neurological diseases. | 06-11-2009 |
20090137834 | 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. | 05-28-2009 |
20090124582 | 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 thereof, methods of making prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof, methods of using prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof and pharmaceutical compositions thereof for treating or preventing diseases or disorders such as spasticity or gastroesophageal reflux disease are disclosed. Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof and sustained release oral dosage forms thereof, which are suitable for oral administration, are also disclosed. | 05-14-2009 |
20090118365 | Use of Prodrugs of GABA B Agonists for Treating Neuropathic and Musculoskeletal Pain - Methods of treating neuropathic pain, musculoskeletal pain, and back spasm associated with musculoskeletal pain in a patient comprising orally administering a therapeutically effective dose of a prodrug of a GABA | 05-07-2009 |
20090099253 | Internally Masked Neopentyl Sulfonyl Ester Cyclization Release Prodrugs of Acamprosate, Compositions Thereof, and Methods of Use - Internally masked 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 enhanced oral bioavailability and methods of using acamprosate prodrugs to treat neurodegenerative disorders, psychotic disorders, mood disorders, anxiety disorders, somatoform disorders, movement disorders, substance abuse disorders, binge eating disorder, cortical spreading depression related disorders, tinnitus, sleeping disorders, multiple sclerosis, and pain are disclosed. | 04-16-2009 |
20090076141 | Use of Propofol Prodrugs for Treating Neuropathic Pain - Methods of treating alcohol neuropathic pain in a patient comprising orally administering a therapeutically effective amount of a propofol prodrug having high oral bioavailability are disclosed. | 03-19-2009 |
20090041806 | USE OF PRODRUGS OF GABA ANALOGS, ANTISPASTICITY AGENTS, AND PRODRUGS OF GABA B RECEPTOR AGONISTS FOR TREATING SPASTICITY - Methods of treating spasticity by administering a colonically absorbable prodrug of a GABA analog having antispastic activity that is not directly mediated by the GABA | 02-12-2009 |
20090005444 | USE OF PROPOFOL PRODRUGS FOR TREATING ALCOHOL WITHDRAWAL, CENTRAL PAIN, ANXIETY OR PRURITUS - Methods of treating alcohol withdrawal, central pain, anxiety, or pruritus in a patient comprising orally administering a therapeutically effective amount of a propofol prodrug having high oral bioavailability are disclosed. | 01-01-2009 |
20090005352 | Prodrugs of Propofol, Compositions and Uses Thereof - The present invention provides propofol prodrugs, methods of making propofol prodrugs, pharmaceutical compositions of propofol prodrugs and methods of using propofol prodrugs and pharmaceutical compositions thereof to treat or prevent diseases or disorders such as migraine headache pain and post-chemotherapy or post-operative surgery nausea and vomiting. | 01-01-2009 |
20080242723 | ACYLOXYALKYL CARBAMATE PRODRUGS OF SULFINIC ACIDS, METHODS OF SYNTHESIS, AND USE - Acyloxyalkyl carbamate prodrugs of 3-aminopropylsulfinic acid and analogs thereof, pharmaceutical compositions of 3-aminopropylsulfinic acid and analogs thereof, methods of making prodrugs of 3-aminopropylsulfinic acid and analogs thereof, methods of using prodrugs of 3-aminopropylsulfinic acid and analogs thereof, and pharmaceutical compositions thereof for treating or preventing diseases or disorders such as spasticity or gastroesophageal reflux disease are disclosed. Acyloxyalkyl carbamate prodrugs of 3-aminopropylsulfinic acid and analogs thereof and sustained release oral dosage forms thereof, which are suitable for oral administration, are also disclosed. | 10-02-2008 |