Mark A. Gallop - Los Altos CA, US Xuedong Dai - San Jose CA, US Randall A. Scheuerman - Santa Clara CA, US Stephen P. Raillard - Mountain View CA, US Suresh K. Manthati - Cupertino CA, US Fenmei Yao - Mountain View CA, US Thu Phan - Fremont CA, US Maria Ludwikow - Cupertino CA, US Ge Peng - Mountain View CA, US Seema Bhat - Santa Clara CA, US
Assignee:
XenoPort, Inc. - Santa Clara CA
International Classification:
C07D 207/46
US Classification:
548542
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.
Gemcitabine Prodrugs, Pharmaceutical Compositions And Uses Thereof
Mark A. Gallop - Los Altos CA, US Ge Peng - Mountain View CA, US Thomas F. Woiwode - San Carlos CA, US Kenneth C. Cundy - Redwood City CA, US
Assignee:
XenoPort, Inc. - Santa Clara CA
International Classification:
A01N 43/04 A61K 31/70 C07H 19/06
US Classification:
514 49, 514 43, 536 281, 536 284
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 thereof to treat or prevent diseases or disorders such as cancer or viral infections.
Acyloxyalkyl Carbamate Prodrugs, Methods Of Synthesis And Use
Mark A. Gallop - Los Altos CA, US Fenmei Yao - Mountain View CA, US Maria J. Ludwikow - Cupertino CA, US Thu Phan - Fremont CA, US Ge Peng - Mountain View CA, US
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.
Synthesis Of Acyloxyalkyl Carbamate Prodrugs And Intermediates Thereof
Mark A. Gallop - Santa Clara CA, US Xuedong Dai - San Jose CA, US Randall A. Scheuerman - Santa Clara CA, US Stephen P. Raillard - Mountain View CA, US Suresh K. Manthati - Cupertino CA, US Fenmei Yao - Mountain View CA, US Thu Phan - Fremont CA, US Maria Ludwikow - Cupertino CA, US Ge Peng - Mountain View CA, US Seema Bhat - Santa Clara CA, US
Assignee:
XenoPort, Inc. - Santa Clara CA
International Classification:
C07D 207/46
US Classification:
548542
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.
Acyloxyalkyl Carbamate Prodrugs, Methods Of Synthesis And Use
Mark A. Gallop - Los Altos CA, US Fenmei Yao - Mountain View CA, US Maria J. Ludwikow - Cupertino CA, US Thu Phan - Fremont CA, US Ge Peng - Mountain View CA, US
Assignee:
XenoPort, Inc. - Santa Clara CA
International Classification:
A61K 31/235
US Classification:
514533
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.
Acyloxyalkyl Carbamate Prodrugs, Methods Of Synthesis And Use
Mark A. Gallop - Los Altos CA, US Feng Xu - Palo Alto CA, US Thu Phan - Fremont CA, US Usha Dilip - Sunnyvale CA, US Ge Peng - Mountain View CA, US
Assignee:
XenoPort, Inc. - Santa Clara CA
International Classification:
C07C 271/06 A61K 31/662
US Classification:
560115, 514119
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.
Gemcitabine Prodrugs, Pharmaceutical Compositions And Uses Thereof
Mark A. Gallop - Santa Clara CA, US Ge Peng - Mountain View CA, US Thomas F. Woiwode - San Carlos CA, US Kenneth C. Cundy - Redwood City CA, US
Assignee:
XenoPort, Inc. - Santa Clara CA
International Classification:
A01N 43/04 A61K 31/70
US Classification:
514 50, 514 43, 514 49, 514 51, 536 281, 536 284
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.
Acyloxyalkyl Carbamate Prodrugs, Methods Of Synthesis And Use
Mark A. Gallop - Los Altos CA, US Feng Xu - Palo Alto CA, US Thu Phan - Fremont CA, US Usha Dilip - Sunnyvale CA, US Ge Peng - Mountain View CA, US
Assignee:
XenoPort, Inc. - Santa Clara CA
International Classification:
A61K 31/66 C07F 9/02
US Classification:
514120, 514121, 558177, 558178
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.