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:
Grant
Filed:
August 11, 2011
Date of Patent:
February 19, 2013
Assignee:
XenoPort, Inc.
Inventors:
Mark A. Gallop, Xuedong Dai, Randall A. Scheuerman, Stephen P. Raillard, Suresh K. Manthati, Fenmei Yao, Thu Phan, Maria Ludwikow, Ge Peng, Seema Bhat
Abstract: Crystalline (3R)-4-{[(1S)-2-methyl-1-(2-methylpropanoyloxy)propoxy]carbonylamino}-3-(4-chlorophenyl)butanoic acid anhydrate and crystalline (3R)-4-{[(1S)-2-methyl-1-(2-methylpropanoyloxy)propoxy]carbonylamino}-3-(4-chlorophenyl)butanoic acid hemihydrate, pharmaceutical compositions comprising such compounds, methods of making and methods of using the same are disclosed.
Type:
Application
Filed:
August 10, 2012
Publication date:
February 14, 2013
Applicant:
XENOPORT, INC.
Inventors:
Stephen P. Raillard, Suresh K. Manthati, Sudhir Joshi
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:
July 13, 2010
Date of Patent:
February 12, 2013
Assignee:
XenoPort, Inc.
Inventors:
Noa Zerangue, Bernd Jandeleit, Yunxiao Li, Mark A. Gallop
Abstract: 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:
Grant
Filed:
October 14, 2011
Date of Patent:
February 5, 2013
Assignee:
Xenoport, Inc.
Inventors:
Mark A. Gallop, Kenneth C. Cundy, Cindy X. Zhou, Fenmei Yao, Jia-Ning Xiang
Abstract: Gamma-amino-butyric acid derivatives that are GABAB receptor ligands, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives and pharmaceutical compositions thereof for treating diseases are disclosed.
Type:
Grant
Filed:
April 16, 2010
Date of Patent:
January 1, 2013
Assignee:
XenoPort, Inc.
Inventors:
Feng Xu, Mark A. Gallop, Ge Peng, Thu Phan, Usha Dilip, David J. Wustrow
Abstract: Catechol protected levodopa diester prodrugs pharmaceutical, compositions comprising catechol protected levodopa diester prodrugs, and methods of using such prodrugs and pharmaceutical compositions for treating diseases such as Parkinson's disease are provided.
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: (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.
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:
Grant
Filed:
December 7, 2010
Date of Patent:
September 4, 2012
Assignee:
XenoPort, Inc.
Inventors:
Fenmei Yao, Mark A. Gallop, Ronald W. Barrett, Peter A. Virsik
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:
April 5, 2012
Publication date:
July 26, 2012
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: 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:
October 14, 2011
Publication date:
June 21, 2012
Applicant:
XenoPort, Inc.
Inventors:
Archana Gangakhedkar, Xuedong Dai, Noa Zerangue, Peter A. Virsik
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:
February 3, 2010
Date of Patent:
June 19, 2012
Assignee:
XenoPort, Inc.
Inventors:
Noa Zerangue, Qingzhi Gao, William J. Dower
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.
Abstract: Pantoic acid ester neopentyl sulfonyl ester prodrugs of acamprosate, pharmaceutical compositions comprising such prodrugs, and methods of using such prodrugs and compositions thereof for treating diseases are disclosed. In particular, acamprosate prodrugs exhibiting enhanced oral bioavailability and methods of using acamprosate prodrugs to treat neurodegenerative disorders, psychotic disorders, mood disorders, anxiety disorders, somatoform disorders, movement disorders, substance abuse disorders, binge eating disorder, cortical spreading depression related disorders, tinnitus, sleeping disorders, multiple sclerosis, and pain are disclosed.
Type:
Grant
Filed:
September 5, 2008
Date of Patent:
May 1, 2012
Assignee:
XenoPort, Inc.
Inventors:
Bernd Jandeleit, Yunxiao Li, Mark A. Gallop, Noa Zerangue, Peter A. Virsik, Wolf-Nicolas Fischer
Abstract: 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:
Grant
Filed:
July 1, 2010
Date of Patent:
May 1, 2012
Assignee:
XenoPort, Inc.
Inventors:
Mark A. Gallop, Kenneth C. Cundy, Cindy X. Zhou, Fenmei Yao, Jia-Ning Xiang, Ian R. Ollman, Fayang G. Qiu
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:
April 27, 2011
Date of Patent:
April 24, 2012
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
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:
October 14, 2011
Publication date:
April 19, 2012
Applicant:
XenoPort, Inc.
Inventors:
Archana Gangakhedkar, Xuedong Dai, Noa Zerangue, Peter A. Virsik
Abstract: The present disclosure provides 2?-C-methyl-ribofuranosyl cytidine prodrugs, methods of making 2?-C-methyl-ribofuranosyl cytidine prodrugs, pharmaceutical compositions of 2?-C-methyl-ribofuranosyl cytidine prodrugs, and methods of using 2?-C-methyl-ribofuranosyl cytidine prodrugs and pharmaceutical compositions thereof to treat viral diseases such as hepatitis C.
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:
Grant
Filed:
August 19, 2009
Date of Patent:
April 3, 2012
Assignee:
XenoPort, Inc.
Inventors:
Archana Gangakhedkar, Xuedong Dai, Noa Zerangue, Peter A. Virsik