专利号:US-9353057-B2 优先权日:2003-12-30 标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof 发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA 权利人:XENOPORT INC 摘要: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.
专利号:US-7423169-B2 优先权日:2001-06-11 标 题:Methods for synthesis of acyloxyalkyl derivatives of GABA analogs 发明人:RAILLARD STEPHEN P; ZHOU CINDY X; YAO FENMEI; MANTHATI SURESH KUMAR; XIANG JIA-NING; GALLOP MARK A 权利人:XENOPORT INC 摘要:The synthesis of 1-(acyloxy)-alkyl carbamates of GABA analogs from 1-haloalkyl carbamates of GABA analogs are described. Also described are new 1-haloalkyl carbamates of GABA analogs.
专利号:EP-2354120-A1 优先权日:2003-08-20 标题 :Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof 发明人:GALLOP MARK A; YAO FENMEI; LUDWIKOW MARIA J; PHAN THU; PENG GE 权利人:XENOPORT INC 摘要:The present invention relates to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-fluorophenyl)butanoic acid and analogs thereof, pharmaceutical compositions thereof, methods of making prodrugs of (±)-4-amino-3-(4-fluorophenyl)butanoic acid and analogs thereof, methods of using prodrugs of (±)-4-amino-3-(4-tluorophenyl)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 present invention also relates to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-fluorophenyl)butanoic acid and analogs thereof which are suitable for oral administration and to sustained release oral dosage forms thereof.
专利号:US-7232924-B2 优先权日:2001-06-11 标题 :Methods for synthesis of acyloxyalkyl derivatives of GABA analogs
专利号:US-7799829-B2 优先权日:2006-07-28 标 题 :Acyloxyalkyl carbamate prodrugs of α-amino acids, methods of synthesis and use 发明人:DAI XUEDONG; GANGAKHEDKAR ARCHANA; XIANG JIA-NING; GALLOP MARK A 权利人:XENOPORT INC 摘要:Acyloxyalkyl carbamate prodrugs of α-amino acids, pharmaceutical compositions thereof, methods of making acyloxyalkyl carbamate prodrugs of α-amino acids and methods of using acyloxyalkyl carbamate prodrugs of α-amino acids, and pharmaceutical compositions thereof to treat a disease are disclosed. Acyloxyalkyl carbamate prodrugs of α-amino acids suitable for oral administration using sustained release dosage forms are also disclosed.
专利号:US-7749985-B2 优先权日:2006-09-15 标 题 :Acyloxyalkyl carbamate prodrugs, methods of synthesis and use 发明人:GALLOP MARK A; XU FENG; PHAN THU; DILIP USHA; PENG GE 权利人:XENOPORT INC 摘要: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.
参考文献:10.1007/s11095-013-0976-9 摘要:Pierrat P, Kereselidze D, Wehrung P, Zuber G, Pons F, Lebeau L. Bioresponsive Deciduous-Charge Amphiphiles for Liposomal Delivery of DNA and siRNA. Pharmaceutical Research. 2013 Feb 01;30(5):1362–79. doi: 10.1007/s11095-013-0976-9.