公开(公告)号：US20170334862A1

公开(公告)日：2017-11-23

申请号：US15522741

申请日：2015-10-27

申请人： Claus Selch Larsen

发明人： Claus Selch Larsen ,  Susan Weng Larsen ,  Mette Agergaard Thing ,  Jesper Langgaard Kristensen ,  Henrik Jensen ,  Jesper Ostergaard

IPC分类号： C07D233/60 ,  A61K45/06 ,  A61K31/4164

CPC分类号： C07D233/60 ,  A61K31/4164 ,  A61K45/06 ,  C07D233/61

摘要： The present invention relates to a compound of formula (I): wherein R1 is R3-IPU and R2 is the acyloxy residue of diclofenac, and specified by the following structures: wherein OH—R3-IPU is selected from and R4 and R5 may be the same or different selected from H and CH3 and salts, solvates and hydrates thereof.

公开(公告)号：US09809557B2

公开(公告)日：2017-11-07

申请号：US14355010

申请日：2012-10-31

申请人： Claus Selch Larsen

发明人： Claus Selch Larsen ,  Susan Weng Larsen ,  Mette Agergaard Thing ,  Jesper Langgaard Kristensen ,  Henrik Jensen ,  Jesper Østergaard

IPC分类号： A61K31/44 ,  C07D235/06 ,  A61K47/48 ,  C07C219/10 ,  C07C219/32 ,  C07C229/42 ,  C07D487/04 ,  C07D233/61 ,  C07D235/16 ,  C07D235/18 ,  C07D213/55

CPC分类号： C07D235/06 ,  A61K47/54 ,  A61K47/545 ,  C07C219/10 ,  C07C219/32 ,  C07C229/42 ,  C07D213/55 ,  C07D233/61 ,  C07D235/16 ,  C07D235/18 ,  C07D487/04

摘要： The present invention relates to novel depot formulations (prodrugs) comprising an immobility promoting unit linked via an ester to an active pharmaceutical ingredient, i.a. common NSAIDs. The novel depot formulations are suitable for intra-articular injections and are soluble at slightly acidic pH to facilitate ease of injection, and sparingly soluble at physiological pH thereby precipitating at the site of administration. The precipitate will slowly dissolve and the active drug is released from dissolved depot formulation following esterase mediated cleavage of the ester link between the immobility promoting unit and the active pharmaceutical agent.

公开(公告)号：US20160074523A1

公开(公告)日：2016-03-17

申请号：US14787601

申请日：2014-04-28

申请人： Claus Selch LARSEN

发明人： Claus Selch Larsen ,  Susan Weng Larsen ,  Mette Agergaard Thing ,  Jesper Langgaard Kristensen ,  Henrik Jensen ,  Jesper Østergaard

IPC分类号： A61K47/48 ,  A61K31/196 ,  A61K31/192 ,  A61K45/06

CPC分类号： A61K47/545 ,  A61K31/192 ,  A61K31/196 ,  A61K45/06 ,  A61K47/54

摘要： The present invention relates to a compound of formula (I): wherein R1 is R3-IPU and R2 is the acyloxy residue of diclofenac or naproxen, and specified by the following structures (A) wherein OH—R3-IPU is selected from (B) and R4 and R5 may be the same or different selected from (C) and salts, solvates and hydrates thereof.

摘要翻译： 本发明涉及式（I）化合物：其中R1为R3-IPU，R2为双氯芬酸或萘普生的酰氧基，并由以下结构（A）表示，其中OH-R3-IPU选自（B ）和R 4和R 5可以相同或不同，选自（C）及其盐，溶剂合物和水合物。

公开(公告)号：US09937262B2

公开(公告)日：2018-04-10

申请号：US14787601

申请日：2014-04-28

申请人： Claus Selch Larsen

发明人： Claus Selch Larsen ,  Susan Weng Larsen ,  Mette Agergaard Thing ,  Jesper Langgaard Kristensen ,  Henrik Jensen ,  Jesper Østergaard

IPC分类号： C07D233/64 ,  C07D233/54 ,  C07C229/58 ,  C07C229/56 ,  A61K31/4174 ,  A61K31/4164 ,  A61K31/196 ,  A61K31/192 ,  A61K47/48 ,  A61K45/06

CPC分类号： A61K47/545 ,  A61K31/192 ,  A61K31/196 ,  A61K45/06 ,  A61K47/54

摘要： The present invention relates to a compound of formula (I): wherein R1 is R3-IPU and R2 is the acyloxy residue of diclofenac or naproxen, and specified by the following structures (A) wherein OH—R3-IPU is selected from (B) and R4 and R5 may be the same or different selected from (C) and salts, solvates and hydrates thereof.

公开(公告)号：US10266499B2

公开(公告)日：2019-04-23

申请号：US15522741

申请日：2015-10-27

申请人： Claus Selch Larsen

发明人： Claus Selch Larsen ,  Susan Weng Larsen ,  Mette Agergaard Thing ,  Jesper Langgaard Kristensen ,  Henrik Jensen ,  Jesper Ostergaard

IPC分类号： A61K31/4172 ,  A61K31/4164 ,  A61K31/196 ,  A61K31/192 ,  C07D233/60 ,  C07C229/58 ,  C07C229/56 ,  C07D233/61 ,  A61K45/06

摘要： The present invention relates to a compound of formula (I): wherein R1 is R3—IPU and R2 is the acyloxy residue of diclofenac, and specified by the following structures: wherein OH—R3—IPU is selected from and R4 and R5 may be the same or different selected from H and CH3 and salts, solvates and hydrates thereof.

公开(公告)号：US20140315960A1

公开(公告)日：2014-10-23

申请号：US14355010

申请日：2012-10-31

申请人： Claus Selch LARSEN

发明人： Claus Selch Larsen ,  Susan Weng Larsen ,  Mette Agergaard Thing ,  Jesper Langgaard Kristensen ,  Henrik Jensen ,  Jesper Østergaard

IPC分类号： C07D487/04 ,  C07D213/55 ,  C07C219/10 ,  C07D235/06 ,  C07C219/32 ,  A61K47/48 ,  C07C229/42 ,  C07D233/61

CPC分类号： C07D235/06 ,  A61K47/54 ,  A61K47/545 ,  C07C219/10 ,  C07C219/32 ,  C07C229/42 ,  C07D213/55 ,  C07D233/61 ,  C07D235/16 ,  C07D235/18 ,  C07D487/04

摘要： The present invention relates to novel depot formulations (prodrugs) comprising an immobility promoting unit linked via an ester to an active pharmaceutical ingredient, i.a. common NSAIDs. The novel depot formulations are suitable for intra-articular injections and are soluble at slightly acidic pH to facilitate ease of injection, and sparingly soluble at physiological pH thereby precipitating at the site of administration. The precipitate will slowly dissolve and the active drug is released from dissolved depot formulation following esterase mediated cleavage of the ester link between the immobility promoting unit and the active pharmaceutical agent.

摘要翻译： 本发明涉及包含通过酯与活性药物成分连接的不动促进单元的新型贮库制剂（前药），例如， 常见的NSAIDs。 新的贮库制剂适用于关节内注射，并且在微酸性pH下可溶，以便于注射，并且在生理pH下微溶，由此在给药部位沉淀。 在酯酶介导的不动性促进单元和活性药剂之间的酯连接的切割下，沉淀将缓慢溶解并且活性药物从溶解的贮库制剂中释放。