公开(公告)号：US11179355B2

公开(公告)日：2021-11-23

申请号：US15042906

申请日：2016-02-12

Applicant: Signature Therapeutics, Inc.

Inventor： Thomas E. Jenkins ,  Craig O. Husfeld ,  Julie D. Seroogy ,  Jonathan W. Wray

IPC: A61K31/165 ,  A61K9/00 ,  A61K31/24 ,  C07C279/14 ,  A61K31/16 ,  C07C237/22 ,  A61K45/06 ,  A61K47/54

Abstract: Pharmaceutical compositions and their methods of use are provided, where the pharmaceutical compositions comprise an amphetamine prodrug that provides enzymatically-controlled release of amphetamine or an amphetamine analog. The composition can further comprise an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of amphetamine or the amphetamine analog from the amphetamine prodrug so as to attenuate enzymatic cleavage of the amphetamine prodrug.

公开(公告)号：US20160235694A1

公开(公告)日：2016-08-18

申请号：US15042906

申请日：2016-02-12

Applicant: Signature Therapeutics, Inc.

Inventor： Thomas E. Jenkins ,  Craig O. Husfeld ,  Julie D. Seroogy ,  Jonathan W. Wray

IPC: A61K31/165 ,  A61K9/00 ,  A61K31/24

CPC classification number: A61K31/165 ,  A61K9/0019 ,  A61K9/0053 ,  A61K31/16 ,  A61K31/24 ,  A61K45/06 ,  A61K47/542 ,  A61K47/543 ,  C07C237/22 ,  C07C279/14 ,  A61K2300/00

Abstract: Pharmaceutical compositions and their methods of use are provided, where the pharmaceutical compositions comprise an amphetamine prodrug that provides enzymatically-controlled release of amphetamine or an amphetamine analog. The composition can further comprise an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of amphetamine or the amphetamine analog from the amphetamine prodrug so as to attenuate enzymatic cleavage of the amphetamine prodrug.

公开(公告)号：US20130210700A1

公开(公告)日：2013-08-15

申请号：US13686710

申请日：2012-11-27

Applicant: Signature Therapeutics, Inc.

Inventor： Thomas E. Jenkins ,  Craig O. Husfeld ,  Julie D. Seroogy ,  Jonathan W. Wray

IPC: A61K47/48 ,  A61K31/485

CPC classification number: C12Q1/37 ,  A61K31/485 ,  A61K47/556

Abstract: Pharmaceutical compositions and their methods of use are provided, where the pharmaceutical compositions comprise a phenol-modified opioid prodrug that provides enzymatically-controlled release of a phenolic opioid, and an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of the phenolic opioid from the phenol-modified opioid prodrug so as to modify enzymatic cleavage of the phenol-modified opioid prodrug.

Abstract translation: 提供了药物组合物及其使用方法，其中药物组合物包含提供酚类阿片样物质的酶控释放的酚修饰的阿片样物质前药，以及与介导酶控制的酶相互作用的酶抑制剂 从苯酚修饰的阿片样物质前药释放酚类阿片样物质，以改变苯酚修饰的阿片样物质前药的酶裂解。

公开(公告)号：US09499581B2

公开(公告)日：2016-11-22

申请号：US14593855

申请日：2015-01-09

Applicant: Signature Therapeutics, Inc.

Inventor： Thomas E. Jenkins ,  Craig O. Husfeld

IPC: A61K38/00 ,  C07K5/09 ,  A61K31/485 ,  A61K45/06 ,  C07D489/08 ,  C12Q1/37 ,  A61K31/155 ,  A61K31/195 ,  A61K31/245 ,  A61K31/445 ,  A61K31/4965 ,  A61K38/05 ,  A61K47/48

CPC classification number: C07K5/0815 ,  A61K31/155 ,  A61K31/195 ,  A61K31/245 ,  A61K31/445 ,  A61K31/485 ,  A61K31/4965 ,  A61K38/05 ,  A61K45/06 ,  A61K47/65 ,  C07D489/08 ,  C12Q1/37 ,  A61K2300/00

Abstract: The embodiments provide Compound KC-8, N-1-[3-(oxycodone-6-enol-carbonyl-methyl-amino)-2,2-dimethyl-propylamine]-arginine-glycine-malonic acid, or acceptable salts, solvates, and hydrates thereof. The present disclosure also provides compositions, and their methods of use, where the compositions comprise a prodrug, Compound KC-8, that provides controlled release of oxycodone. Such compositions can optionally provide a trypsin inhibitor that interacts with the enzyme that mediates the controlled release of oxycodone from the prodrug so as to attenuate enzymatic cleavage of the prodrug.

公开(公告)号：US20150297736A1

公开(公告)日：2015-10-22

申请号：US14692526

申请日：2015-04-21

Applicant: Signature Therapeutics, Inc.

Inventor： Thomas E. Jenkins ,  Craig O. Husfeld ,  Julie D. Seroogy ,  Jonathan W. Wray

IPC: A61K47/48 ,  A61K31/485

CPC classification number: A61K47/48023 ,  A61K9/51 ,  A61K31/485 ,  A61K47/4813 ,  A61K47/48246 ,  A61K47/54 ,  A61K47/555 ,  A61K47/64 ,  C07D489/02 ,  C07D489/08 ,  C12Q1/37 ,  G01N33/5088 ,  G01N33/9486 ,  G01N2333/976 ,  G01N2500/00

Abstract: Pharmaceutical compositions and their methods of use are provided, where the pharmaceutical compositions comprise an opioid prodrug that provides enzymatically-controlled release of an opioid, and an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of the opioid from the opioid prodrug so as to attenuate enzymatic cleavage of the opioid prodrug.

Abstract translation: 提供了药物组合物及其使用方法，其中药物组合物包含提供阿片样物质的酶控释放的阿片样前体药物和与介导阿片样物质的酶控释放的酶相互作用的酶抑制剂 来自阿片样前药，以减轻阿片样物质前药的酶切。

公开(公告)号：US09040032B2

公开(公告)日：2015-05-26

申请号：US13686725

申请日：2012-11-27

Applicant: Signature Therapeutics, Inc.

Inventor： Thomas E. Jenkins ,  Craig O. Husfeld ,  Julie D. Seroogy ,  Jonathan W. Wray

IPC: A61K31/74 ,  A61K47/48 ,  A61K9/51 ,  A61K31/485 ,  C07D489/02 ,  C07D489/08 ,  C12Q1/37 ,  G01N33/50 ,  G01N33/94

CPC classification number: A61K47/48023 ,  A61K9/51 ,  A61K31/485 ,  A61K47/4813 ,  A61K47/48246 ,  A61K47/54 ,  A61K47/555 ,  A61K47/64 ,  C07D489/02 ,  C07D489/08 ,  C12Q1/37 ,  G01N33/5088 ,  G01N33/9486 ,  G01N2333/976 ,  G01N2500/00

Abstract: Pharmaceutical compositions and their methods of use are provided, where the pharmaceutical compositions comprise an opioid prodrug that provides enzymatically-controlled release of an opioid, and an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of the opioid from the opioid prodrug so as to attenuate enzymatic cleavage of the opioid prodrug.

Abstract translation: 提供了药物组合物及其使用方法，其中药物组合物包含提供阿片样物质的酶控释放的阿片样前体药物和与介导阿片样物质的酶控释放的酶相互作用的酶抑制剂 来自阿片样前药，以减轻阿片样物质前药的酶切。

公开(公告)号：US09585963B2

公开(公告)日：2017-03-07

申请号：US14692526

申请日：2015-04-21

Applicant: Signature Therapeutics, Inc.

Inventor： Thomas E. Jenkins ,  Craig O. Husfeld ,  Julie D. Seroogy ,  Jonathan W. Wray

IPC: A61K31/74 ,  A61K47/48 ,  A61K9/51 ,  A61K31/485 ,  C07D489/02 ,  C07D489/08 ,  C12Q1/37 ,  G01N33/50 ,  G01N33/94

CPC classification number: A61K47/48023 ,  A61K9/51 ,  A61K31/485 ,  A61K47/4813 ,  A61K47/48246 ,  A61K47/54 ,  A61K47/555 ,  A61K47/64 ,  C07D489/02 ,  C07D489/08 ,  C12Q1/37 ,  G01N33/5088 ,  G01N33/9486 ,  G01N2333/976 ,  G01N2500/00

Abstract: Pharmaceutical compositions and their methods of use are provided, where the pharmaceutical compositions comprise an opioid prodrug that provides enzymatically-controlled release of an opioid, and an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of the opioid from the opioid prodrug so as to attenuate enzymatic cleavage of the opioid prodrug.

Abstract translation: 提供了药物组合物及其使用方法，其中药物组合物包含提供阿片样物质的酶控释放的阿片样前体药物和与介导阿片样物质的酶控释放的酶相互作用的酶抑制剂 来自阿片样前药，以减轻阿片样物质前药的酶切。

公开(公告)号：US09095627B2

公开(公告)日：2015-08-04

申请号：US14166719

申请日：2014-01-28

Applicant: Signature Therapeutics, Inc.

Inventor： Thomas E. Jenkins ,  Craig O. Husfeld

IPC: A61K38/00 ,  A61K47/00 ,  A61P23/00 ,  A61P25/04 ,  A61K47/48 ,  C07D489/02 ,  C07D489/08 ,  A61K31/485

CPC classification number: A61K47/48346 ,  A61K31/485 ,  A61K47/48246 ,  A61K47/64 ,  C07D489/02 ,  C07D489/08

Abstract: The embodiments provide prodrug compounds of Formulae I-XV. The present disclosure also provides compositions, and their methods of use, where the compositions comprise a prodrug compound of Formulae I-XV that provides controlled release of an opioid. Such compositions can optionally provide a trypsin inhibitor that interacts with the enzyme that mediates the controlled release of an opioid from the prodrug so as to attenuate enzymatic cleavage of the prodrug.

Abstract translation: 实施方案提供式I-XV的前药化合物。 本公开还提供组合物及其使用方法，其中组合物包含提供阿片样物质的受控释放的式I-XV的前药化合物。 这样的组合物可以任选地提供胰蛋白酶抑制剂，其与介导阿片样物质从前药的受控释放的酶相互作用，以减弱前体药物的酶切。

公开(公告)号：US08962547B2

公开(公告)日：2015-02-24

申请号：US14035871

申请日：2013-09-24

Applicant: Signature Therapeutics, Inc.

Inventor： Thomas E. Jenkins ,  Craig O. Husfeld

IPC: A61K38/00 ,  A61K47/48 ,  A61K31/485 ,  A61K45/06 ,  C07D489/08 ,  C12Q1/37 ,  A61K31/155 ,  A61K31/195 ,  A61K31/245 ,  A61K31/445 ,  A61K31/4965 ,  A61K38/05

CPC classification number: C07K5/0815 ,  A61K31/155 ,  A61K31/195 ,  A61K31/245 ,  A61K31/445 ,  A61K31/485 ,  A61K31/4965 ,  A61K38/05 ,  A61K45/06 ,  A61K47/65 ,  C07D489/08 ,  C12Q1/37 ,  A61K2300/00

Abstract: The embodiments provide Compound KC-8, N-1-[3-(oxycodone-6-enol-carbonyl-methyl-amino)-2,2-dimethyl-propylamine]-arginine-glycine-malonic acid, or acceptable salts, solvates, and hydrates thereof. The present disclosure also provides compositions, and their methods of use, where the compositions comprise a prodrug, Compound KC-8, that provides controlled release of oxycodone. Such compositions can optionally provide a trypsin inhibitor that interacts with the enzyme that mediates the controlled release of oxycodone from the prodrug so as to attenuate enzymatic cleavage of the prodrug.

Abstract translation: 实施方案提供化合物KC-8，N-1- [3-（羟考酮-6-烯醇 - 羰基 - 甲基 - 氨基）-2,2-二甲基 - 丙胺] - 精氨酸 - 甘氨酸 - 丙二酸，或其可接受的盐，溶剂合物 ，及其水合物。 本公开还提供了组合物及其使用方法，其中组合物包含提供羟考酮的受控释放的前药，化合物KC-8。 这样的组合物可以任选地提供胰蛋白酶抑制剂，其与介导羟考酮从前药的受控释放的酶相互作用，以减弱前药的酶裂解。

公开(公告)号：US20140206597A1

公开(公告)日：2014-07-24

申请号：US14166719

申请日：2014-01-28

Applicant: Signature Therapeutics, Inc.

Inventor： Thomas E. Jenkins ,  Craig O. Husfeld

IPC: A61K47/48 ,  A61K31/485

CPC classification number: A61K47/48346 ,  A61K31/485 ,  A61K47/48246 ,  A61K47/64 ,  C07D489/02 ,  C07D489/08

Abstract: The embodiments provide prodrug compounds of Formulae I-XV. The present disclosure also provides compositions, and their methods of use, where the compositions comprise a prodrug compound of Formulae I-XV that provides controlled release of an opioid. Such compositions can optionally provide a trypsin inhibitor that interacts with the enzyme that mediates the controlled release of an opioid from the prodrug so as to attenuate enzymatic cleavage of the prodrug.

Abstract translation: 实施方案提供式I-XV的前药化合物。 本公开还提供组合物及其使用方法，其中组合物包含提供阿片样物质的受控释放的式I-XV的前药化合物。 这样的组合物可以任选地提供胰蛋白酶抑制剂，其与介导阿片样物质从前药的受控释放的酶相互作用，以减弱前体药物的酶切。