Abstract: The present invention relates generally to prodrugs of fused GABA analogs, pharmaceutical compositions of prodrugs of fused GABA analogs, methods of making prodrugs of fused GABA analogs and methods of using prodrugs of fused GABA analogs and pharmaceutical compositions of prodrugs of fused GABA analogs to treat or prevent various diseases.
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:
August 28, 2002
Date of Patent:
May 30, 2006
Assignee:
XenoPort, Inc.
Inventors:
Laxminarayan Bhat, Mark A. Gallop, Bernd Jandeleit
Abstract: 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:
Grant
Filed:
February 9, 2005
Date of Patent:
May 23, 2006
Assignee:
XenoPort, Inc.
Inventors:
Kenneth C. Cundy, Mark A. Gallop, Cindy X. Zhou
Abstract: Replicable genetic packages and collections thereof that display various compounds are provided. In some instances, the replicable genetic packages include nucleic acid tags that serve to record a characteristic of the compound or compounds that are attached to the replicable genetic package. The invention further provides a number of different methods for using the replicable genetic packages to screen a library of compounds for a desired biological activity.
Type:
Grant
Filed:
September 29, 2000
Date of Patent:
May 2, 2006
Assignee:
Xenoport, Inc.
Inventors:
Ronald W. Barrett, William J. Dower, Mark Gallop, Thomas F. Woiwode, Steven E. Cwirla
Abstract: 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.
Type:
Grant
Filed:
March 20, 2003
Date of Patent:
April 11, 2006
Assignee:
Xenoport, Inc.
Inventors:
Mark A Gallop, Jia-Ning Xiang, Fenmei Yao, Laxminarayan Bhat
Abstract: This invention is directed to methods for providing sustained systemic concentrations of therapeutic or prophylactic agents such as GABA analogs following oral administration to animals. This invention is also directed to compounds and pharmaceutical compositions that are used in such methods.
Type:
Grant
Filed:
October 5, 2001
Date of Patent:
January 31, 2006
Assignee:
XenoPort, Inc.
Inventors:
Kenneth C. Cundy, Mark A. Gallop, Cindy X. Zhou
Abstract: 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.
Abstract: SMVT is consistently expressed at high levels in cancer cells. Disclosed herein are assays for determining whether a test material/molecule is a substrate for, and/or is transported by, the SMVT transporter, and therefore a candidate substrate for transport into cancer cells. The assays are useful in screening for cytotoxic agents or imaging components used in the treatment or diagnosis of cancer.
Abstract: GLUT1 is consistently expressed at high levels in cancer cells. Disclosed herein are assays for determining whether a test material/molecule is a substrate for, and/or is transported by, the GLUT1 transporter, and therefore a candidate substrate for transport into cancer cells. The assays are useful in screening for cytotoxic agents or imaging components used in the treatment or diagnosis of cancer.
Abstract: GLUT3 is consistently expressed at high levels in cancer cells. Disclosed herein are assays for determining whether a test material/molecule is a substrate for, and/or is transported by, the GLUT3 transporter, and therefore a candidate substrate for transport into cancer cells. The assays are useful in screening for cytotoxic agents or imaging components used in the treatment or diagnosis of cancer.
Abstract: ENT1 is consistently expressed at high levels in cancer cells. Disclosed herein are assays for determining whether a test material/molecule is a substrate for, and/or is transported by, the ENT1 transporter, and therefore a candidate substrate for transport into cancer cells. The assays are useful in screening for cytotoxic agents or imaging components used in the treatment or diagnosis of cancer.
Abstract: LAT1 is consistently expressed at high levels in cancer cells. Disclosed herein are assays for determining whether a test material/molecule is a substrate for, and/or is transported by, the LAT1 transporter, and therefore a candidate substrate for transport into cancer cells. The assays are useful in screening for cytotoxic agents or imaging components used in the treatment or diagnosis of cancer.
Abstract: GLUT5 is consistently expressed at high levels in cancer cells. Disclosed herein are assays for determining whether a test material/molecule is a substrate for, and/or is transported by, the GLUT5 transporter, and therefore a candidate substrate for transport into cancer cells. The assays are useful in screening for cytotoxic agents or imaging components used in the treatment or diagnosis of cancer.
Abstract: This invention is directed to methods for providing sustained systemic concentrations of therapeutic or prophylactic agents such as GABA analogs following oral administration to animals. This invention is also directed to compounds and pharmaceutical compositions that are used in such methods.
Abstract: Replicable genetic packages and collections thereof that display various compounds are provided. In some instances, the replicable genetic packages include nucleic acid tags that serve to record a characteristic of the compound or compounds that are attached to the replicable genetic package. The invention further provides a number of different methods for using the replicable genetic packages to screen a library of compounds for a desired biological activity.
Type:
Application
Filed:
July 22, 2005
Publication date:
November 17, 2005
Applicant:
Xenoport, Inc.
Inventors:
Ronald Barrett, William Dower, Mark Gallop, Thomas Woiwode, Steven Cwirla
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:
Grant
Filed:
June 11, 2002
Date of Patent:
October 18, 2005
Assignee:
XenoPort
Inventors:
Noa Zerangue, Tracy Dias, William J Dower
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:
May 20, 2005
Publication date:
September 29, 2005
Applicant:
XenoPort, Inc.
Inventors:
Noa Zerangue, Tracy Dias, William Dower
Abstract: Methods and compositions for treating or preventing local pain or discomfort, particularly local neuropathic pain via topical application directly to skin or mucosal tissue at the site of pain or discomfort are disclosed. Compositions comprising prodrugs of gamma amino butyric acid analogs, such as prodrugs of gabapentin or pregabalin, and optionally a topical anesthetic agent are also disclosed.
Abstract: 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.
Abstract: 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.