Abstract: 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.
Type:
Grant
Filed:
August 14, 2009
Date of Patent:
August 17, 2010
Assignee:
XenoPort, Inc.
Inventors:
Noa Zerangue, Bernd Jandeleit, Yunxiao Li, Mark A. Gallop
Abstract: Prodrugs of levodopa, methods of making prodrugs of levodopa, methods of using prodrugs of levodopa, and compositions of prodrugs of levodopa are disclosed.
Type:
Application
Filed:
February 2, 2009
Publication date:
August 5, 2010
Applicant:
XenoPort, Inc.
Inventors:
Jia-Ning Xiang, Mark A. Gallop, Cindy X. Zhou, Mark Nguyen, Xuedong Dai, Jianhua Li, Kenneth C. Cundy, Nelson L. Jumbe
Abstract: 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.
Type:
Grant
Filed:
January 18, 2007
Date of Patent:
August 3, 2010
Assignee:
XenoPort, Inc.
Inventors:
Randall A. Scheuerman, Mark A. Gallop, Kenneth C. Cundy, Ronald W. Barrett
Abstract: 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.
Abstract: 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.
Type:
Grant
Filed:
July 21, 2009
Date of Patent:
July 6, 2010
Assignee:
XenoPort, Inc.
Inventors:
Mark A. Gallop, Feng Xu, Thu Phan, Usha Dilip, Ge Peng
Abstract: 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 incontinence.
Abstract: 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.
Abstract: Sustained release particulate oral dosage forms of (R)-baclofen prodrugs and methods of treating a disease comprising orally administering such dosage forms are disclosed.
Abstract: 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.
Type:
Application
Filed:
February 3, 2010
Publication date:
June 3, 2010
Applicant:
XenoPort, Inc.
Inventors:
Noa Zerangue, Qingzhi Gao, William J. Dower
Abstract: 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 therapeutic, and optionally prolonged therapeutic, systemic blood concentrations of the drugs upon oral administration of the drug-compound conjugate. Also disclosed are pharmaceutical compositions containing and methods of using such compounds.
Type:
Grant
Filed:
September 26, 2005
Date of Patent:
June 1, 2010
Assignee:
XenoPort, Inc.
Inventors:
Laxminarayan Bhat, Mark A. Gallop, Bernd Jandeleit
Abstract: 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.
Abstract: 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 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.
Abstract: 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 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.
Abstract: 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 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.
Abstract: 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 incontinence.
Abstract: 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.
Type:
Application
Filed:
October 2, 2009
Publication date:
April 8, 2010
Applicant:
XenoPort, Inc.
Inventors:
Feng Xu, Mark A. Gallop, Vivek Sasikumar, Usha Dilip
Abstract: 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 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.
Abstract: 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.
Type:
Application
Filed:
August 7, 2009
Publication date:
April 1, 2010
Applicants:
XenoPort, Inc., Glaxo Group Limited
Inventors:
Stephen P. Raillard, Suresh K. Manthati, Peng Liu, Qunying Dai, Hao Yin
Abstract: 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.
Type:
Grant
Filed:
June 6, 2007
Date of Patent:
March 23, 2010
Assignee:
XenoPort, Inc.
Inventors:
Noa Zerangue, Qingzhi Gao, William J. Dower