公开(公告)号：US11136342B2

公开(公告)日：2021-10-05

申请号：US16459430

申请日：2019-07-01

申请人： Acorda Therapeutics, Inc.

发明人： Naweed Muhammad ,  Keith R. Bley

IPC分类号： C07F9/09 ,  A61K31/661 ,  A61K47/54 ,  C07C233/25 ,  C07F9/11

摘要： The present invention provides carbonate prodrugs which comprise a carbonic phosphoric anhydride prodrug moiety attached to the hydroxyl or carboxyl group of a parent drug moiety. The prodrugs may provide improved physicochemical properties over the parent drug. Also provided are methods of treating a disease or condition that is responsive to the parent drug using the carbonate prodrugs, as well as kits and unit dosages.

公开(公告)号：US09289501B2

公开(公告)日：2016-03-22

申请号：US14629324

申请日：2015-02-23

申请人： Acorda Therapeutics, Inc.

发明人： Naweed Muhammad ,  Keith R. Bley

IPC分类号： A61K31/664 ,  C07F9/06 ,  A61K47/48 ,  A61K31/661 ,  C07F9/09

CPC分类号： C07F9/096 ,  A61K31/661 ,  A61K47/548 ,  C07C233/25 ,  C07F9/11

摘要： The present invention provides carbonate prodrugs which comprise a carbonic phosphoric anhydride prodrug moiety attached to the hydroxyl or carboxyl group of a parent drug moiety. The prodrugs may provide improved physicochemical properties over the parent drug. Also provided are methods of treating a disease or condition that is responsive to the parent drug using the carbonate prodrugs, as well as kits and unit dosages.

公开(公告)号：US10442826B2

公开(公告)日：2019-10-15

申请号：US15962934

申请日：2018-04-25

申请人： Acorda Therapeutics, Inc.

发明人： Naweed Muhammad ,  Keith R. Bley

IPC分类号： A61K45/06 ,  A61K31/661 ,  A61K9/00 ,  C07F9/09

摘要： The present invention provides water-soluble acetaminophen prodrugs and formulations which may be suitable for parenteral administration. Methods of treating a disease or condition responsive to acetaminophen (such as fever and/or pain) using the acetaminophen prodrugs, as well as kits, unit dosages, and combinations with additional pharmaceutical agent(s) are also provided.

公开(公告)号：US09981998B2

公开(公告)日：2018-05-29

申请号：US15077802

申请日：2016-03-22

申请人： Acorda Therapeutics, Inc.

发明人： Naweed Muhammad ,  Keith R. Bley

IPC分类号： A61K31/661 ,  A61K45/06 ,  A61K9/00 ,  C07F9/09

CPC分类号： C07F9/094 ,  A61K9/0019 ,  A61K31/661 ,  A61K45/06 ,  C07F9/091

摘要： The present invention provides water-soluble acetaminophen prodrugs and formulations which may be suitable for parenteral administration. Methods of treating a disease or condition responsive to acetaminophen (such as fever and/or pain) using the acetaminophen prodrugs, as well as kits, unit dosages, and combinations with additional pharmaceutical agent(s) are also provided.

公开(公告)号：US20160024126A1

公开(公告)日：2016-01-28

申请号：US14629324

申请日：2015-02-23

申请人： Acorda Therapeutics, Inc.

发明人： Naweed Muhammad ,  Keith R. Bley

IPC分类号： C07F9/09

CPC分类号： C07F9/096 ,  A61K31/661 ,  A61K47/548 ,  C07C233/25 ,  C07F9/11

摘要： The present invention provides carbonate prodrugs which comprise a carbonic phosphoric anhydride prodrug moiety attached to the hydroxyl or carboxyl group of a parent drug moiety. The prodrugs may provide improved physicochemical properties over the parent drug. Also provided are methods of treating a disease or condition that is responsive to the parent drug using the carbonate prodrugs, as well as kits and unit dosages.

摘要翻译： 本发明提供碳酸酯前药，其包含与母体药物部分的羟基或羧基连接的碳酸磷酸酐前药部分。 前药可以提供比母体药物更好的物理化学性质。 还提供了治疗使用碳酸酯前药对母体药物有反应的疾病或病症以及试剂盒和单位剂量的方法。

公开(公告)号：US09951001B2

公开(公告)日：2018-04-24

申请号：US15150099

申请日：2016-05-09

申请人： Acorda Therapeutics, Inc.

发明人： Naweed Muhammad ,  Keith R. Bley ,  Jeffrey Tobias

IPC分类号： C07C323/52 ,  A61K31/195 ,  A61K31/485 ,  A61K45/06 ,  A61K9/00 ,  A61K31/216

CPC分类号： C07C323/52 ,  A61K9/0053 ,  A61K31/195 ,  A61K31/216 ,  A61K31/485 ,  A61K45/06 ,  A61K2300/00

摘要： The present invention provides hepatoprotectant acetaminophen mutual prodrugs, which have an acetaminophen moiety covalently linked to a second moiety that may act as a hepatoprotectant against acetaminophen hepatotoxicity. Additionally, acetaminophen mutual prodrugs may have improved water solubility which may provide better suitability for parenteral and other dosage forms relative to administration of acetaminophen. Also provided are methods of treating a disease or condition that is responsive to acetaminophen (such as fever, pain and ischemic injury) using hepatoprotectant acetaminophen mutual prodrugs, as well as kits and unit dosages.

公开(公告)号：US20170008916A1

公开(公告)日：2017-01-12

申请号：US15017329

申请日：2016-02-05

申请人： Acorda Therapeutics, Inc.

发明人： Naweed Muhammad ,  Keith R. BLEY

IPC分类号： C07F9/09 ,  C07F9/11 ,  C07C233/25

CPC分类号： C07F9/096 ,  A61K31/661 ,  A61K47/548 ,  C07C233/25 ,  C07F9/11

摘要： The present invention provides carbonate prodrugs which comprise a carbonic phosphoric anhydride prodrug moiety attached to the hydroxyl or carboxyl group of a parent drug moiety. The prodrugs may provide improved physicochemical properties over the parent drug. Also provided are methods of treating a disease or condition that is responsive to the parent drug using the carbonate prodrugs, as well as kits and unit dosages.

摘要翻译： 本发明提供碳酸酯前药，其包含与母体药物部分的羟基或羧基连接的碳酸磷酸酐前药部分。 前药可以提供比母体药物更好的物理化学性质。 还提供了治疗使用碳酸酯前药对母体药物有反应的疾病或病症以及试剂盒和单位剂量的方法。

公开(公告)号：US11021498B2

公开(公告)日：2021-06-01

申请号：US16565173

申请日：2019-09-09

申请人： Acorda Therapeutics, Inc.

发明人： Naweed Muhammad ,  Keith R. Bley

IPC分类号： A61K9/00 ,  A61K45/06 ,  A61K31/661 ,  C07F9/09 ,  A61P29/02 ,  A61P29/00 ,  A61P9/00 ,  A61P9/10 ,  A61P25/04 ,  A61P25/00 ,  A61P43/00

摘要： The present invention provides water-soluble acetaminophen prodrugs and formulations which may be suitable for parenteral administration. Methods of treating a disease or condition responsive to acetaminophen (such as fever and/or pain) using the acetaminophen prodrugs, as well as kits, unit dosages, and combinations with additional pharmaceutical agent(s) are also provided.

公开(公告)号：US10377779B2

公开(公告)日：2019-08-13

申请号：US15592048

申请日：2017-05-10

申请人： Acorda Therapeutics, Inc.

发明人： Naweed Muhammad ,  Keith R. Bley

IPC分类号： A61K47/54 ,  A61K31/661 ,  C07F9/09 ,  C07C233/25 ,  C07F9/11

摘要： The present invention provides carbonate prodrugs which comprise a carbonic phosphoric anhydride prodrug moiety attached to the hydroxyl or carboxyl group of a parent drug moiety. The prodrugs may provide improved physicochemical properties over the parent drug. Also provided are methods of treating a disease or condition that is responsive to the parent drug using the carbonate prodrugs, as well as kits and unit dosages.

公开(公告)号：US09750707B2

公开(公告)日：2017-09-05

申请号：US14255630

申请日：2014-04-17

申请人： Acorda Therapeutics, Inc.

发明人： Naweed Muhammad ,  Gene Curtis Jamieson ,  Keith R. Bley ,  Sanjay Chanda

IPC分类号： A61F13/00 ,  A61K31/165 ,  A61K9/00 ,  A61K9/08 ,  A61K9/107 ,  A61K9/127 ,  A61K47/08 ,  A61K47/10 ,  A61K45/06 ,  A61K47/12

CPC分类号： A61K31/165 ,  A61K9/0014 ,  A61K9/08 ,  A61K9/1075 ,  A61K9/127 ,  A61K45/06 ,  A61K47/08 ,  A61K47/10 ,  A61K47/12

摘要： Compositions are provided that contain a TRPV1 agonist, such as capsaicin, and a solvent system. Topical application of the composition results in rapid delivery of agonist to the dermis and epidermis. Method of using the compositions for reducing nociceptive nerve fiber function in subjects, and for treatment of capsaicin-responsive conditions are also provided.