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:
Application
Filed:
June 30, 2009
Publication date:
October 29, 2009
Applicant:
XenoPort, Inc.
Inventors:
Mark A. Gallop, Jia-Ning Xiang, Fenmei Yao, Laxminarayan Bhat
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:
Grant
Filed:
August 24, 2007
Date of Patent:
October 27, 2009
Assignee:
XenoPort, Inc.
Inventors:
Mark A. Gallop, Ge Peng, Thomas F. Woiwode, Kenneth C. Cundy
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:
March 24, 2006
Date of Patent:
October 13, 2009
Assignee:
XenoPort, Inc.
Inventors:
Kenneth C. Cundy, Mark A. Gallop, Cindy X. Zhou
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:
July 19, 2005
Date of Patent:
October 13, 2009
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: 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.
Type:
Application
Filed:
June 8, 2009
Publication date:
September 24, 2009
Applicant:
XenoPort, Inc.
Inventors:
Mark A. Gallop, Jia-Ning Xiang, Fenmei Yao, Laxminarayan Bhat, Cindy X. Zhou
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:
October 12, 2007
Date of Patent:
September 22, 2009
Assignee:
XenoPort, Inc.
Inventors:
Noa Zerangue, Bernd Jandeleit, Yunxiao Li, Mark A. Gallop
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:
February 27, 2009
Publication date:
September 17, 2009
Applicant:
XenoPort, Inc.
Inventors:
Ronald W. Barrett, William J. Dower, Mark Gallop, Thomas F. Woiwode, Steven E. Cwirla
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:
September 13, 2007
Date of Patent:
September 8, 2009
Assignee:
XenoPort, Inc.
Inventors:
Mark A. Gallop, Feng Xu, Thu Phan, Usha Dilip, Ge Peng
Abstract: 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.
Type:
Application
Filed:
July 14, 2008
Publication date:
September 3, 2009
Applicant:
XenoPort, Inc.
Inventors:
William J. Dower, Mark Gallop, Ronald W. Barrett, Kenneth C. Cundy, Tania Chernov-Rogan
Abstract: 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.
Type:
Application
Filed:
January 23, 2009
Publication date:
August 27, 2009
Applicant:
XenoPort, Inc.
Inventors:
Fenmei Yao, Mark A. Gallop, Ronald W. Barrett, Peter A. Virsik
Abstract: 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.
Type:
Application
Filed:
February 20, 2009
Publication date:
August 27, 2009
Applicant:
XenoPort, Inc.
Inventors:
Mark A. Gallop, Xuedong Dai, Randall A. Scheuerman, Stephen P. Raillard, Suresh K. Manthati, Fenmei Yao, Thu Phan, Maria J. Ludwikow, Ge Peng, Seema Bhat
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.
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.
Abstract: 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.
Type:
Grant
Filed:
October 24, 2007
Date of Patent:
August 11, 2009
Assignee:
XenoPort, Inc.
Inventors:
Mark A. Gallop, Fenmei Yao, Maria J. Ludwikow, Thu Phan, Ge Peng
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.
Type:
Application
Filed:
February 1, 2008
Publication date:
August 6, 2009
Applicant:
XenoPort, Inc.
Inventors:
Srikonsda SASTRY, Kenneth C. Cundy, Manshiu Leung
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:
January 12, 2006
Date of Patent:
August 4, 2009
Assignee:
XenoPort, Inc.
Inventors:
Mark A Gallop, Jia-Ning Xiang, Fenmei Yao, Laxminarayan Bhat
Abstract: 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.
Type:
Application
Filed:
January 23, 2009
Publication date:
July 30, 2009
Applicant:
XenoPort, Inc.
Inventors:
Fenmei Yao, Mark A. Gallop, Ronald W. Barrett, Peter A. Virsik
Abstract: Acyloxyalkyl carbamate prodrugs of ?-amino acids, pharmaceutical compositions thereof, methods of making acyloxyalkyl carbamate prodrugs of ?-amino acids and methods of using acyloxyalkyl carbamate prodrugs of ?-amino acids, and pharmaceutical compositions thereof to treat a disease are disclosed. Acyloxyalkyl carbamate prodrugs of ?-amino acids suitable for oral administration using sustained release dosage forms are also disclosed.
Type:
Application
Filed:
April 1, 2009
Publication date:
July 30, 2009
Applicant:
XenoPort, Inc.
Inventors:
Xuedong Dai, Archana Gangakhedkar, Jia-Ning Xiang, Mark A. Gallop