公开(公告)号：WO2005019163A3

公开(公告)日：2005-03-03

申请号：PCT/US2004/027330

申请日：2004-08-20

Applicant: XENOPORT, INC. ,  GALLOP, Mark, A. ,  YAO, Fenmei ,  LUDWIKOW, Maria, J. ,  PHAN, Thu ,  PENG, Ge

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

IPC: C07C271/22

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.

公开(公告)号：WO0232376A3

公开(公告)日：2003-09-04

申请号：PCT/US0142613

申请日：2001-10-05

Applicant: XENOPORT INC ,  GALLOP MARK A ,  CUNDY KENNETH C ,  ZHOU CINDY X

Inventor： GALLOP MARK A ,  CUNDY KENNETH C ,  ZHOU CINDY X

IPC: A61K38/00 ,  A61K47/48 ,  C07C237/12 ,  C07C237/20 ,  C07C323/60 ,  C07D207/16 ,  C07D233/54 ,  C07K5/02 ,  C07J9/00 ,  A61K31/56 ,  A61K31/58 ,  C07J17/00 ,  C07J33/00 ,  C07J41/00 ,  C07J43/00

CPC classification number: C07D233/64 ,  A61K38/00 ,  A61K47/554 ,  A61K47/64 ,  A61K47/65 ,  C07C237/12 ,  C07C237/20 ,  C07C323/60 ,  C07C2601/14 ,  C07D207/16 ,  C07K5/0205 ,  C07K5/06 ,  C07K5/08

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 translation: 本发明涉及在给予动物后提供治疗性或预防性药物的持续全身浓度的化合物。 本发明还涉及包括使用这些化合物的药物组合物和方法。

公开(公告)号：WO2003020214A3

公开(公告)日：2003-03-13

申请号：PCT/US2002/027458

申请日：2002-08-29

Applicant: XENOPORT, INC. ,  BHAT, Laxminarayan ,  GALLOP, Mark, A. ,  JANDELEIT, Bernd

Inventor： BHAT, Laxminarayan ,  GALLOP, Mark, A. ,  JANDELEIT, Bernd

IPC: C07J9/00

Abstract: Disclosed are compounds that exhibit high transport across the intestinal wall of an animal. The compounds may optionally be linked to drugs that are poorly absorbed or poorly transported across the intestinal wall after oral administration to provide for enhanced therapeutic, and optionally prolonged therapeutic, systemic blood concentrations of the drugs upon oral administration of the drug-compound conjugate. Also disclosed are pharmaceutical compositions containing and methods of using such compounds.

公开(公告)号：WO2002100344A2

公开(公告)日：2002-12-19

申请号：PCT/US2002/018493

申请日：2002-06-11

Applicant: XENOPORT, INC. ,  GALLOP, Mark, A. ,  CUNDY, Kenneth, C. ,  SCHEUERMAN, Randall, A. ,  BARRETT, Ronald, W.

Inventor： GALLOP, Mark, A. ,  CUNDY, Kenneth, C. ,  SCHEUERMAN, Randall, A. ,  BARRETT, Ronald, W.

IPC: A61K

CPC classification number: C07D233/64 ,  A61K38/00 ,  A61K47/64 ,  C07C237/12 ,  C07C237/20 ,  C07C317/50 ,  C07C323/59 ,  C07C323/60 ,  C07C2601/14 ,  C07D207/16 ,  C07K5/0205 ,  G01N33/566

Abstract: This invention is directed to compounds that provide for sustained systemic concentrations of GABA analogs following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.

Abstract translation: 本发明涉及在给予动物后提供持续的全身浓度的GABA类似物的化合物。 本发明还涉及包括使用这些化合物的药物组合物和方法。

公开(公告)号：WO1995035278A1

公开(公告)日：1995-12-28

申请号：PCT/US1995007878

申请日：1995-06-22

Applicant: AFFYMAX TECHNOLOGIES N.V. ,  GALLOP, Mark, A. ,  MURPHY, Martin, A.

Inventor： AFFYMAX TECHNOLOGIES N.V.

IPC: C07D207/12

CPC classification number: C07D207/16 ,  B01J2219/00592 ,  B01J2219/0072

Abstract: Disclosed are methods for synthesizing very large collections of diverse pyrrolidine compounds and derivatives thereof on solid supports and synthetic compound libraries comprising pyrrolidine groups and derivatives thereof prepared by such methods.

Abstract translation: 公开了用于在固体支持物上合成非常大量的各种吡咯烷化合物及其衍生物的方法，其包含通过这些方法制备的吡咯烷基团及其衍生物的合成化合物文库。

公开(公告)号：WO2009052191A1

公开(公告)日：2009-04-23

申请号：PCT/US2008/080009

申请日：2008-10-15

Applicant: XENOPORT, INC. ,  LI, Yunxiao ,  JANDELEIT, Bernd ,  GALLOP, Mark A. ,  ZERANGUE, Noa ,  VIRSIK, Peter A. ,  FISCHER, Wolf-nicolas

Inventor： LI, Yunxiao ,  JANDELEIT, Bernd ,  GALLOP, Mark A. ,  ZERANGUE, Noa ,  VIRSIK, Peter A. ,  FISCHER, Wolf-nicolas

IPC: C07D307/33 ,  C07D307/88 ,  C07D309/30 ,  C07D311/76 ,  C07D317/32 ,  C07D317/36 ,  C07D333/64 ,  A61P25/00 ,  A61K31/335 ,  A61K31/381

CPC classification number: C07D311/76 ,  C07D307/33 ,  C07D307/88 ,  C07D309/30 ,  C07D317/32 ,  C07D317/36 ,  C07D333/64

Abstract: Internally masked 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.

Abstract translation: 本发明公开了含有阿坎酸盐的内部掩蔽的新戊基磺酰基酯前体药物，包含这些前药的药物组合物，以及使用这些前药及其组合物治疗疾病的方法。 特别地，表现出增强的口服生物利用度的阿坎酸酯前药和使用阿坎酸类前药治疗神经变性疾病，精神病性障碍，情绪障碍，焦虑症，躯体形式障碍，运动障碍，物质滥用障碍，暴饮暴食症，皮质扩张抑郁症相关疾病，耳鸣的方法 ，睡眠障碍，多发性硬化和疼痛。

公开(公告)号：WO2009033079A1

公开(公告)日：2009-03-12

申请号：PCT/US2008/075472

申请日：2008-09-05

Applicant: XENOPORT, INC. ,  JANDELEIT, Bernd ,  LI, Yunxiao ,  GALLOP, Mark A. ,  ZERANGUE, Noa ,  VIRSIK, Peter A. ,  FISCHER, Wolf-nicolas

Inventor： JANDELEIT, Bernd ,  LI, Yunxiao ,  GALLOP, Mark A. ,  ZERANGUE, Noa ,  VIRSIK, Peter A. ,  FISCHER, Wolf-nicolas

IPC: C07C309/15 ,  A61K31/255 ,  A61P25/00

CPC classification number: C07C309/15

Abstract: Masked nitrogen-substituted and oxygen-substituted neopentyl sulfonyl ester prodrugs of acamprosate of formulae (I) and (III), 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 disorders, cortical spreading depression related disorders, tinnitus, sleeping disorders, multiple sclerosis and pain are disclosed.

Abstract translation: 公开了式（I）和（III）的阿卡波酸的掩蔽的氮取代和氧取代的新戊基磺酰酯前药，包含这些前药的药物组合物，以及使用这些前药及其组合物治疗疾病的方法。 特别地，表现出增强的口服生物利用度的阿坎酸酯前药和使用阿坎酸酯前药治疗神经变性疾病，精神障碍，情绪障碍，焦虑症，躯体形式障碍，运动障碍，物质滥用障碍，暴饮暴食症，皮质扩张抑郁症相关疾病，耳鸣的方法 ，睡眠障碍，多发性硬化和疼痛。

公开(公告)号：WO2009033061A1

公开(公告)日：2009-03-12

申请号：PCT/US2008/075453

申请日：2008-09-05

Applicant: XENOPORT, INC. ,  JANDELEIT, Bernd ,  LI, Yunxiao ,  GALLOP, Mark, A. ,  ZERANGUE, Noa ,  VIRSIK, Peter, A. ,  FISCHER, Wolf-Nicolas

Inventor： JANDELEIT, Bernd ,  LI, Yunxiao ,  GALLOP, Mark, A. ,  ZERANGUE, Noa ,  VIRSIK, Peter, A. ,  FISCHER, Wolf-Nicolas

IPC: C07C309/15 ,  C07D213/30 ,  C07D295/088 ,  A61K31/255 ,  A61K31/5377 ,  A61K31/4406 ,  A61P25/00

CPC classification number: C07C309/15

Abstract: Masked carboxylate neopentyl sulfonyl ester prodrugs of acamprosate of formula (I), 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 disorders, cortical spreading depression related disorders, tinnitus, sleeping disorders, multiple sclerosis and pain are disclosed.

Abstract translation: 公开了式（I）的阿坎酸盐，包含这些前药的掩蔽的羧酸新戊酰磺酰酯前体药物，以及使用这些前药及其组合物治疗疾病的方法。 特别地，表现出增强的口服生物利用度的阿坎酸酯前药和使用阿坎酸酯前药治疗神经变性疾病，精神障碍，情绪障碍，焦虑症，躯体形式障碍，运动障碍，物质滥用障碍，暴饮暴食症，皮质扩张抑郁症相关疾病，耳鸣的方法 ，睡眠障碍，多发性硬化和疼痛。

公开(公告)号：WO2009033054A1

公开(公告)日：2009-03-12

申请号：PCT/US2008/075444

申请日：2008-09-05

Applicant: XENOPORT, INC. ,  JANDELEIT, Bernd ,  LI, Yunxiao ,  GALLOP, Mark A. ,  ZERANGUE, Noa ,  VIRSIK, Peter A. ,  FISCHER, Wolf-Nicolas

Inventor： JANDELEIT, Bernd ,  LI, Yunxiao ,  GALLOP, Mark A. ,  ZERANGUE, Noa ,  VIRSIK, Peter A. ,  FISCHER, Wolf-Nicolas

IPC: C07C309/15 ,  C07F9/09 ,  A61K31/255 ,  A61K31/661 ,  A61P25/00

CPC classification number: C07C309/15

Abstract: Pantoic acid ester neopentyl sulfonyl ester prodrugs of acamprosate of formula (I), 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 disorders, cortical spreading depression related disorders, tinnitus, sleeping disorders, multiple sclerosis and pain are disclosed.

Abstract translation: 公开了式（I）的阿卡波酸，包含这些前药的药物组合物的泛酸酯新戊基磺酰酯前药，以及使用这些前药及其组合物治疗疾病的方法。 特别地，表现出增强的口服生物利用度的阿坎酸酯前药和使用阿坎酸酯前药治疗神经变性疾病，精神障碍，情绪障碍，焦虑症，躯体形式障碍，运动障碍，物质滥用障碍，暴饮暴食症，皮质扩张抑郁症相关疾病，耳鸣的方法 ，睡眠障碍，多发性硬化和疼痛。

公开(公告)号：WO2008013860A3

公开(公告)日：2008-03-13

申请号：PCT/US2007016739

申请日：2007-07-26

Applicant: XENOPORT INC ,  DAI XUEDONG ,  GANGAKHEDKAR ARCHANA ,  JIANG JIA-NING ,  GALLOP MARK A

Inventor： DAI XUEDONG ,  GANGAKHEDKAR ARCHANA ,  JIANG JIA-NING ,  GALLOP MARK A

IPC: A61K31/27 ,  C07C271/22 ,  C07C271/24 ,  C07C271/34 ,  C07C271/36

CPC classification number: C07C271/16 ,  C07C271/24 ,  C07C271/34 ,  C07C271/36 ,  C07C2601/02 ,  C07C2601/14

Abstract: Acyloxyalkyl carbamate prodrugs of a-amino acids, pharmaceutical compositions thereof, methods of making acyloxyalkyl carbamate prodrugs of a-amino acids and methods of using acyloxyalkyl carbamate prodrugs of a-amino acids, and pharmaceutical compositions thereof to treat a disease are disclosed. Acyloxyalkyl carbamate prodrugs of a-amino acids suitable for oral administration using sustained release dosage forms are also disclosed.

Abstract translation: 公开了α-氨基酸的氰氧基烷基氨基甲酸酯前药，其药物组合物，制备α-氨基酸的酰氨基烷基氨基甲酸酯前药的方法和使用α-氨基酸的氨基甲酰氨基酸前药的方法及其药物组合物来治疗疾病。 还公开了适用于使用持续释放剂型的口服给药的α-氨基酸的氨基氧基烷基氨基甲酸酯前药。