Patents Assigned to XenoPort
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Publication number: 20050170394Abstract: GLUT1 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 GLUT1 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: ApplicationFiled: December 30, 2004Publication date: August 4, 2005Applicant: Xenoport, Inc.Inventor: Noa Zerangue
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Publication number: 20050170393Abstract: OATPB 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 OATPB 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: ApplicationFiled: December 30, 2004Publication date: August 4, 2005Applicant: Xenoport, Inc.Inventor: Noa Zerangue
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Publication number: 20050170392Abstract: OAT3 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 OAT3 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: ApplicationFiled: December 30, 2004Publication date: August 4, 2005Applicant: Xenoport, Inc.Inventor: Noa Zerangue
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Publication number: 20050170391Abstract: TAUT1 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 TAUT1 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: ApplicationFiled: December 30, 2004Publication date: August 4, 2005Applicant: Xenoport, Inc.Inventor: Noa Zerangue
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Publication number: 20050148564Abstract: This invention is directed to compounds that provide for sustained systemic concentrations of therapeutic or prophylactic agents following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.Type: ApplicationFiled: February 9, 2005Publication date: July 7, 2005Applicant: XenoPort, Inc.Inventors: Kenneth Cundy, Mark Gallop, Cindy Zhou
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Patent number: 6900192Abstract: This invention is directed to compounds that provide for sustained systemic concentrations of therapeutic or prophylactic agents following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.Type: GrantFiled: October 5, 2001Date of Patent: May 31, 2005Assignee: XenoPort, Inc.Inventors: Kenneth C. Cundy, Mark A. Gallop, Cindy X. Zhou
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Publication number: 20050100968Abstract: The present invention provides a variety of methods for synthesizing, encoding and decoding compounds in a combinatorial library. One step or cycle in the synthetic methods of the invention is a self-encoding step in which different pairs of components, each pair with a known and different molecular weight difference, are reacted with supports, whereby two compounds differing in molecular weight are formed on each support. The molecular weight difference between the two compounds on the support encodes for a particular component pair. Libraries of compounds formed according to the methods of the invention are also provided.Type: ApplicationFiled: September 10, 2004Publication date: May 12, 2005Applicant: XenoPort, Inc.Inventors: Mark Gallop, William Dower, Ron Barrett
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Publication number: 20050042658Abstract: 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: ApplicationFiled: July 27, 2004Publication date: February 24, 2005Applicant: XenoPort, Inc.Inventors: William Dower, Steven Cwirla
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Publication number: 20050032135Abstract: MCT1 and MCT4 are expressed at higher levels in many cancer cells than comparable normal cells of the same tissue. Disclosed herein are assays for determining whether a test material/molecule is a substrate for, and/or is actively transported by, the MCT1 and/or MCT4, as well as inhibitors and substrates of MCT1 and/or MCT4, methods of isolating the same, and methods of using the same for treatment or diagnosis of cancer.Type: ApplicationFiled: July 6, 2004Publication date: February 10, 2005Applicant: Xenoport, Inc.Inventors: Noa Zerangue, Laxminarayan Bhat
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Patent number: 6833140Abstract: The present invention provides an extended release oral dosage form of prodrugs of gabapentin and other GABA analogs, which dosage forms exhibit reduced toxicity. The dosage forms are particularly useful in administering those prodrugs of gabapentin and other GABA analogs that are metabolized to form an aldehyde. The dosage forms of the invention are useful for treating or preventing diseases and/or disorders for which the parent gabapentin or other GABA analog are known to be therapeutically effective.Type: GrantFiled: June 11, 2002Date of Patent: December 21, 2004Assignee: Xenoport, Inc.Inventors: Kenneth C. Cundy, Mark A. Gallop
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Patent number: 6818787Abstract: 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.Type: GrantFiled: June 11, 2002Date of Patent: November 16, 2004Assignee: Xenoport, Inc.Inventors: Mark A. Gallop, Kenneth C. Cundy, Cindy X. Zhou, Fenmei Yao, Jia-Ning Xiang
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Publication number: 20040161424Abstract: The invention provides several new transporter proteins, nucleic acids encoding them and methods of using the transporters to screen agents, conjugates or conjugate moieties, linked or linkable to agents, for capacity to be transported as substrates through the transporters. The invention also provides methods of treatment involving oral delivery of agents that either alone, or as a result of linkage to a conjugate moiety, are substrates of one of the transporter.Type: ApplicationFiled: January 22, 2004Publication date: August 19, 2004Applicant: XenoPortInventors: Noa Zerangue, Christopher J. Paddon
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Patent number: 6777239Abstract: 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: GrantFiled: April 17, 2002Date of Patent: August 17, 2004Assignee: XenoPort, Inc.Inventors: William J. Dower, Steven E. Cwirla
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Publication number: 20030228619Abstract: Methods of screening a library of compounds are disclosed herein. The methods include providing a library of differing complexes. Each complex includes a compound and a peptide nucleic acid tag encoding one or more synthesis steps by which the compound was made, the compounds and the tags encoding them differing between the different complexes. Usually, the complex is cleavably bound to a support. One preferred support is polyethylene glycol (PEG), and optionally the PEG support is attached to a dendrimer. The library of differing complexes is then contacted with a molecular target (e.g., a receptor or enzyme). A complex(es) that bind to the target is isolated. The isolated complex(es) is contacted with a nucleic acid that hybridizes to the tag of the complex. The tag is decoded from the identity of the nucleic acid that hybridizes to the tag, thereby identifying the compound which binds to the target.Type: ApplicationFiled: May 22, 2003Publication date: December 11, 2003Applicant: XenoPort, Inc.Inventor: Michael C. Needels
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Publication number: 20030158089Abstract: Disclosed herein are conjugates comprising a therapeutic agent (e.g., a drug) which is linked to a conjugate moiety that is itself, or itself in combination with the agent, is a good substrate for the sodium dependent multi-vitamin transporter (SMVT). The conjugates have a molecular weight below 1500 daltons and exhibit increased uptake via SMVT through the cells lining the gastrointestinal lumen, and hence higher bioavailability, when administered orally compared to the therapeutic agent itself Also disclosed are methods of delivering agents that, as a result of linkage to a conjugate moiety, are good substrates of the SMVT transporter. Further disclosed are methods of screening conjugates or conjugate moieties, linked or linkable to a therapeutic agent, for capacity to be transported as substrates through the SMVT transporter.Type: ApplicationFiled: January 23, 2003Publication date: August 21, 2003Applicant: XenoPort, Inc.Inventors: Mark A. Gallop, Kenneth C. Cundy, Noa Zerangue, Feng Xu
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Publication number: 20030158254Abstract: Methods of modifying therapeutic compounds such as drugs to be substrates for active transporters expressed in epithelial cells lining the lumen of the human colon are disclosed. The transporters expressed in the human colon include the sodium dependent multi-vitamin transporter (SMVT), and monocarboxylate transporters 1 and 4 (MCT 1 and MCT 4). The modified compounds can themselves be pharmacologically active, or upon cleavage of a chemical moiety after uptake from the colon, can be metabolized to form a compound that is pharmacologically active (e.g., a prodrug). The modified compounds disclosed herein are suitable for use in extended release oral dosage forms, particularly those that release drug over periods of greater than about 2-4 hours following administration.Type: ApplicationFiled: January 23, 2003Publication date: August 21, 2003Applicant: XenoPort, Inc.Inventors: Noa Zerangue, Kenneth C. Cundy, Mark A. Gallop
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Publication number: 20030017964Abstract: 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: ApplicationFiled: June 11, 2002Publication date: January 23, 2003Applicant: Xenoport, Inc.Inventors: Noa Zerangue, Tracy Dias, William J. Dower
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Publication number: 20020192690Abstract: 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: ApplicationFiled: April 17, 2002Publication date: December 19, 2002Applicant: XenoPortInventors: William J. Dower, Steven E. Cwirla