公开(公告)号：EP2419401A2

公开(公告)日：2012-02-22

申请号：EP10714502.1

申请日：2010-04-16

申请人： XenoPort, Inc.

发明人： XU, Feng ,  GALLOP, Mark A. ,  PENG, Ge ,  PHAN, Thu ,  DILIP, Usha ,  WUSTROW, David J.

IPC分类号： C07C229/34 ,  C07C229/42 ,  C07C233/81 ,  C07D213/53 ,  C07D233/64 ,  C07C311/21 ,  C07D317/48 ,  C07F9/30 ,  A61K31/195 ,  A61P11/00 ,  A61P43/00 ,  A61K31/381 ,  A61K31/341 ,  A61K31/662 ,  A61K31/4402 ,  A61K31/44 ,  A61K31/505 ,  A61K31/426 ,  A61K31/4164 ,  A61K31/4184

CPC分类号： C07C255/59 ,  C07C229/34 ,  C07C229/38 ,  C07C229/42 ,  C07C229/58 ,  C07C229/60 ,  C07C233/81 ,  C07C237/30 ,  C07C255/58 ,  C07C311/21 ,  C07C317/48 ,  C07D213/30 ,  C07D213/74 ,  C07D333/24 ,  C07D333/70 ,  C07F9/301 ,  C07F9/306 ,  C07F9/582

摘要： Gamma-amino-butyric acid derivatives of formula (I) that are GABA
B receptor ligands, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives and pharmaceutical compositions thereof for treating diseases are disclosed. R
5 is chosen from -COOH, -SOOH, and -P(O)(OH)R
8 wherein R
8 is chosen from hydrogen and C
1-4 alkyl.

摘要翻译： 公开了作为GABA B受体配体的式（I）的γ-氨基丁酸衍生物，包含此类衍生物的药物组合物，以及使用这些衍生物和其药物组合物治疗疾病的方法。 R 5选自-COOH，-SOOH和-P（O）（OH）R 8，其中R 8选自氢和C 1-4烷基。

公开(公告)号：EP1660440B1

公开(公告)日：2012-02-22

申请号：EP04781926.3

申请日：2004-08-20

申请人： XenoPort, Inc.

发明人： GALLOP, Mark, A. ,  YAO, Fenmei ,  LUDWIKOW, Maria, J. ,  PHAN, Thu ,  PENG, Ge

IPC分类号： C07C271/22 ,  A61K31/195

CPC分类号： C07C271/22 ,  C07C2601/08 ,  C07C2601/14 ,  C07D213/79 ,  C07D307/30 ,  C07D333/38

摘要： 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.

摘要翻译： 本文的公开内容通常涉及（.plusmn。）4氨基3（4氯苯基）丁酸及其类似物的酰氧基烷基氨基甲酸酯前药，其药物组合物，制备（.plusmn。）4氨基3（4氯苯基）丁酸 其酸和类似物，其用于（.plusmn。）4氨基3（4氯苯基）丁酸及其类似物的前药的方法及其用于治疗或预防常见疾病和/或病症如痉挛和/或酸的药物组合物 反流疾病。 本文的公开内容还涉及适于口服给药的（.plusmn）4氨基3（4氯苯基）丁酸及其类似物的氨基氧基烷基氨基甲酸酯产物及其缓释口服剂型。

公开(公告)号：EP1660440A2

公开(公告)日：2006-05-31

申请号：EP04781926.3

申请日：2004-08-20

申请人： Xenoport, Inc.

发明人： GALLOP, Mark, A. ,  YAO, Fenmei ,  LUDWIKOW, Maria, J. ,  PHAN, Thu ,  PENG, Ge

IPC分类号： C07C271/22 ,  A61K31/195

CPC分类号： C07C271/22 ,  C07C2601/08 ,  C07C2601/14 ,  C07D213/79 ,  C07D307/30 ,  C07D333/38

摘要： 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.

公开(公告)号：EP1716115B1

公开(公告)日：2013-02-27

申请号：EP04815821.6

申请日：2004-12-30

申请人： XenoPort, Inc.

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

IPC分类号： C07D207/40

CPC分类号： C07D207/46 ,  C07D207/404 ,  C07D207/416

公开(公告)号：EP1716115A2

公开(公告)日：2006-11-02

申请号：EP04815821.6

申请日：2004-12-30

申请人： Xenoport, Inc.

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

IPC分类号： C07D207/40

CPC分类号： C07D207/46 ,  C07D207/404 ,  C07D207/416

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.