Patents Assigned to XenoPort
  • Bile-acid derived compounds for enhancing oral absorption and systemic bioavailability of drugs
    Patent number: 7678782
    Abstract: 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 bioavailable via oral delivery to animals. Still further, disclosed are compounds and pharmaceutical compositions that are used in such methods.
    Type: Grant
    Filed: July 11, 2006
    Date of Patent: March 16, 2010
    Assignee: XenoPort, Inc.
    Inventors: Mark A. Gallop, Kenneth C. Cundy
  • CRYSTALLINE FORM OF y-AMINOBUTYRIC ACID ANALOG
    Publication number: 20100056632
    Abstract: A crystalline form of a ?-aminobutyric acid analog, and methods of preparing same, are provided.
    Type: Application
    Filed: August 26, 2009
    Publication date: March 4, 2010
    Applicant: XenoPort, Inc.
    Inventors: Tono Estrada, Stephen P. Raillard, Christine Frauenfelder, Uwe Zacher
  • Screening of compounds for CAT1 transporter activity
    Patent number: 7670782
    Abstract: CAT1 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 CAT1 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.
    Type: Grant
    Filed: July 25, 2006
    Date of Patent: March 2, 2010
    Assignee: XenoPort, Inc.
    Inventor: Noa Zerangue
  • Levodopa prodrugs, and compositions and uses thereof
    Patent number: 7671089
    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: Grant
    Filed: December 11, 2007
    Date of Patent: March 2, 2010
    Assignee: XenoPort, Inc.
    Inventors: Jia-Ning Xiang, Mark A. Gallop, Cindy X. Zhou, Mark Nguyen, Xuedong Dai, Jianhua Li, Kenneth C. Cundy, Nelson L. Jumbe
  • PRODRUGS OF METHYL HYDROGEN FUMARATE, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USE
    Publication number: 20100048651
    Abstract: 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.
    Type: Application
    Filed: August 19, 2009
    Publication date: February 25, 2010
    Applicant: XenoPort, Inc.
    Inventors: Archana Gangakhedkar, Xuedong Dai, Noa Zerangue, Peter A. Virsik
  • METHODS FOR SYNTHESIS OF ACYLOXYALKYL COMPOUNDS
    Publication number: 20100041882
    Abstract: 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.
    Type: Application
    Filed: August 10, 2009
    Publication date: February 18, 2010
    Applicant: XenoPort, Inc.
    Inventors: Laxminarayan Bhat, Mark A. Gallop
  • Methods for synthesis of acyloxyalkyl compounds
    Patent number: 7662987
    Abstract: 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.
    Type: Grant
    Filed: July 15, 2004
    Date of Patent: February 16, 2010
    Assignee: XenoPort, Inc.
    Inventors: Laxminarayan Bhat, Mark A. Gallop
  • Acyloxyalkyl Carbamate Prodrugs of Tranexamic Acid, Methods of Synthesis and Use
    Publication number: 20100036148
    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: Application
    Filed: August 14, 2009
    Publication date: February 11, 2010
    Applicant: XenoPort, Inc.
    Inventors: Noa Zerangue, Bernd Jandeleit, Yunxiao Li, Mark A. Gallop
  • GEMCITABINE PRODRUGS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
    Publication number: 20100016254
    Abstract: 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.
    Type: Application
    Filed: September 9, 2009
    Publication date: January 21, 2010
    Applicant: XenoPort, Inc.
    Inventors: Mark A. Gallop, Ge Peng, Thomas F. Woiwode, Kenneth C. Cundy
  • Amino acid conjugates providing for sustained systemic concentrations of GABA analogues
    Patent number: 7645797
    Abstract: Compounds that provide for sustained systemic concentrations of GABA analogs following oral administration to animals are disclosed. Pharmaceutical compositions including, and methods using, such compounds are also disclosed.
    Type: Grant
    Filed: May 28, 2008
    Date of Patent: January 12, 2010
    Assignee: XenoPort, Inc.
    Inventors: Mark Gallop, Kenneth C. Cundy, Randall A. Scheuerman, Ronald W. Barrett, Noa Zerangue
  • Prodrugs of propofol, compositions and uses thereof
    Patent number: 7645792
    Abstract: 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.
    Type: Grant
    Filed: June 26, 2007
    Date of Patent: January 12, 2010
    Assignee: XenoPort, Inc.
    Inventors: Mark Gallop, Feng Xu
  • Levodopa Prodrugs, and Compositions and Uses Thereof
    Publication number: 20100004332
    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: September 14, 2009
    Publication date: January 7, 2010
    Applicant: XenoPort, Inc.
    Inventors: Jia-Ning Xiang, Mark A. Gallop, Cindy X. Zhou, Mark Nguyen, Xuedong Dai, Jianhua Li, Kenneth C. Cundy
  • Levodopa Prodrug Mesylate, Compositions Thereof, and Uses Thereof
    Publication number: 20090326067
    Abstract: (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.
    Type: Application
    Filed: June 22, 2009
    Publication date: December 31, 2009
    Applicant: XenoPort, Inc.
    Inventors: Jia-Ning Xiang, Xuedong Dai, Cindy X. Zhou, Jianhua Li, Mark Q. Nguyen
  • AROMATIC PRODRUGS OF PROPOFOL, COMPOSITIONS AND USES THEREOF
    Publication number: 20090312424
    Abstract: 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.
    Type: Application
    Filed: July 7, 2009
    Publication date: December 17, 2009
    Applicant: XenoPort, Inc.
    Inventors: Mark A. Gallop, Feng Xu
  • METHODS OF SCREENING AGENTS, CONJUGATES OR CONJUGATE MOIETIES FOR TRANSPORT BY A PEPT2 TRANSPORTER
    Publication number: 20090306036
    Abstract: 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.
    Type: Application
    Filed: February 20, 2009
    Publication date: December 10, 2009
    Applicant: XenoPort, Inc.
    Inventors: Noa Zerangue, Tracy Dias, William J. Dower
  • SVCT2 transporters expressed in blood brain barrier cells
    Patent number: 7625718
    Abstract: SVCT2 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 SVCT2 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.
    Type: Grant
    Filed: July 25, 2006
    Date of Patent: December 1, 2009
    Assignee: XenoPort, Inc.
    Inventor: Noa Zerangue
  • AMINO ACID DERIVED PRODRUGS OF PROPOFOL, COMPOSITIONS AND USES THEREOF
    Publication number: 20090286763
    Abstract: 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.
    Type: Application
    Filed: May 18, 2009
    Publication date: November 19, 2009
    Applicant: XenoPort, Inc.
    Inventors: Feng Xu, Mark A. Gallop, Vivek Sasikumar
  • ACYLOXYALKYL CARBAMATE PRODRUGS, METHODS OF SYNTHESIS AND USE
    Publication number: 20090286759
    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: Application
    Filed: July 21, 2009
    Publication date: November 19, 2009
    Applicant: XenoPort, Inc.
    Inventors: Mark A Gallop, Feng Xu, Thu Phan, Usha Dilip, Ge Peng
  • Amino acid derived prodrugs of propofol, compositions, uses and crystalline forms thereof
    Patent number: 7619110
    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: Grant
    Filed: December 22, 2005
    Date of Patent: November 17, 2009
    Assignee: XenoPort, Inc.
    Inventors: Feng Xu, Mark A. Gallop, Vivek Sasikumar, Usha Dilip
  • Epitope-Captured Antibody Display
    Publication number: 20090280999
    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.
    Type: Application
    Filed: April 7, 2009
    Publication date: November 12, 2009
    Applicant: XenoPort, Inc.
    Inventors: William J. Dower, Steven E. Cwirla