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1. 发明申请

US20120202756A1 USE OF PRODRUGS TO AVOID GI MEDIATED ADVERSE EVENTS 审中-公开
标题翻译：使用产品避免GI介入的不良事件
公开(公告)号：US20120202756A1
公开(公告)日：2012-08-09
申请号：US13253677
申请日：2011-10-05
申请人： Richard Franklin , Martin Quibell , Robert G. Tyson , Bernard T. Golding
发明人： Richard Franklin , Martin Quibell , Robert G. Tyson , Bernard T. Golding
IPC分类号： A61K31/7056 , C07H15/14 , C07C229/22 , C07C229/60 , C07D211/46 , C07D211/22 , C07D417/12 , C07D403/12 , A61K31/4164 , A61K31/225 , A61K31/24 , A61K31/445 , A61K31/554 , A61K31/506 , A61P31/04 , A61P9/06 , A61P25/28 , A61P19/02 , A61P25/24 , A61P35/00 , A61P19/10 , A61P31/12 , A61P3/10 , C07D233/94
CPC分类号： C07C279/26 , A61K31/4375 , C07C233/47 , C07C233/54 , C07C2601/14 , C07D211/32 , C07D211/46 , C07D233/94 , C07D285/135 , C07D307/20 , C07D403/12 , C07D405/12 , C07D417/12 , C07D471/04 , C07D501/60 , C07F9/3873 , C07H15/04
摘要： The present invention relates to prodrugs of a wide variety of drugs and pharmaceutical compositions containing such prodrugs. Methods for minimizing locally mediated (from within the gut lumen) adverse gastrointestinal events associated with the underivatised drug and increasing the sustainment of plasma drug levels with the aforementioned prodrugs are also provided. Thus, the present invention relates to the use of prodrugs of a wide diversity of drugs (other than opioids) to transiently inactivate them and so reduce directly, locally mediated adverse gastrointestinal (GI) side-effects normally evident after administration of the parent compound. Additionally, such prodrugs may confer improved pharmacokinetics.
摘要翻译：本发明涉及各种药物的前药和含有这些前药的药物组合物。还提供了用于使局部介导的（来自肠内腔）最小化与未发病药物相关的不良胃肠道事件和用上述前药增加血浆药物水平的维持的方法。因此，本发明涉及广泛多样的药物（阿片样物质除外）的前体药物使用以使其短暂失活，并因此降低在给予母体化合物后通常明显的局部介导的不良胃肠道（GI）副作用。此外，这样的前药可以赋予改善的药代动力学。

2. 发明申请

US20120270847A1 NOVEL CARBAMATE AMINO ACID AND PEPTIDE PRODRUGS OF OPIATES AND USES THEREOF 审中-公开
标题翻译：新型卡氨酸氨基酸和肽类的优点及其用途
公开(公告)号：US20120270847A1
公开(公告)日：2012-10-25
申请号：US13383831
申请日：2010-07-16
申请人： Richard Franklin , Bernard T. Golding , Robert G. Tyson
发明人： Richard Franklin , Bernard T. Golding , Robert G. Tyson
IPC分类号： A61K31/55 , C07D223/04 , A61K31/625 , C07D403/12 , C07D411/12 , A61P25/04 , C07D405/12
CPC分类号： C07D223/04
摘要： Carbamate linked prodrugs of meptazinol and other opioid analgesics are provided. The prodrug moiety may comprise a single amino acid or short peptide. Additionally, the present invention relates to methods for reducing gastrointestinal side effects in a subject, the gastrointestinal side effects being associated with the administration of an opioid analgesic. The methods comprise orally administering an opioid prodrug or pharmaceutically acceptable salt thereof to a subject, wherein the opioid pro-drug is comprised of an opioid analgesic covalently bonded through a carbamate linkage to a prodrug moiety, and wherein upon oral administration, the prodrug or pharmaceutically acceptable salt minimizes at least one gastrointestinal side effect associated with oral administration of the opioid analgesic alone. Compositions for use with the method are also provided.
摘要翻译：提供了美珠坚醇和其他阿片样镇痛药的氨基甲酸酯连接前体药物。前药部分可以包含单个氨基酸或短肽。另外，本发明涉及减少受试者胃肠道副作用的方法，胃肠副作用与阿片类镇痛剂的给药有关。所述方法包括将阿片样物质前药或其药学上可接受的盐口服给予受试者，其中所述阿片类药物由通过氨基甲酸酯键与前药部分共价结合的阿片样物质止痛剂组成，并且其中口服给药前药或药学上可接受的盐使与单独的阿片样物质镇痛剂的口服给药相关的至少一种胃肠道副作用最小化。还提供了与该方法一起使用的组合物。

3. 发明申请

US20110028552A1 MEXILETINE AMINO ACID AND PEPTIDE PRODRUGS AND USES THEREOF 审中-公开
标题翻译：梅毒素氨基酸和肽类产品及其用途
公开(公告)号：US20110028552A1
公开(公告)日：2011-02-03
申请号：US12823066
申请日：2010-06-24
申请人： Richard Franklin , Bernard T. Golding , Robert G. Tyson
发明人： Richard Franklin , Bernard T. Golding , Robert G. Tyson
IPC分类号： A61K31/197 , C07C237/08 , A61K31/165 , C07C271/54 , A61P29/00 , A61P9/06
CPC分类号： C07C381/12 , C07C237/08 , C07C279/14
摘要： The present invention concerns prodrugs of mexiletine (and mexiletine's active metabolite) with amino acids or peptides and pharmaceutical compositions containing such prodrugs. Methods for providing pain relief, treating arrhythmia, decreasing the adverse GI side effects associated with mexiletine, increasing the bioavailability of mexiletine, and improving the pharmacokinetic reproducibility of mexiletine with the aforementioned prodrugs are also provided. Oligopeptides incorporating lysine or arginine residues attached directly or indirectly through a glycine residue are also described herein.
摘要翻译：本发明涉及美西律（和美西律的活性代谢物）与氨基酸或肽的前药以及含有这些前药的药物组合物。还提供了提供疼痛缓解，治疗心律失常，减少与美西律相关的不良GI副作用，增加美西律的生物利用度，以及改善美西律与前述药物的药代动力学再现性的方法。通过甘氨酸残基直接或间接连接的赖氨酸或精氨酸残基的寡肽也在本文中描述。

4. 发明申请

US20110015182A1 NOVEL CARBAMATE AMINO ACID AND PEPTIDE PRODRUGS OF OPIOIDS AND USES THEREOF 审中-公开
标题翻译：新型卡氨酸氨基酸和肽类物质及其用途
公开(公告)号：US20110015182A1
公开(公告)日：2011-01-20
申请号：US12837788
申请日：2010-07-16
申请人： Richard Franklin , Bernard T. Golding , Robert G. Tyson
发明人： Richard Franklin , Bernard T. Golding , Robert G. Tyson
IPC分类号： A61K31/55 , C07D223/04 , C07D405/12 , C07D403/12 , C07D411/12 , C07D223/10 , A61P25/04
CPC分类号： C07D223/04
摘要： Carbamate linked prodrugs of meptazinol and other opioid analgesics are provided. The prodrug moiety may comprise a single amino acid or short peptide. Additionally, the present invention relates to methods for reducing gastrointestinal side effects in a subject, the gastrointestinal side effects being associated with the administration of an opioid analgesic. The methods comprise orally administering an opioid prodrug or pharmaceutically acceptable salt thereof to a subject, wherein the opioid prodrug is comprised of an opioid analgesic covalently bonded through a carbamate linkage to a prodrug moiety, and wherein upon oral administration, the prodrug or pharmaceutically acceptable salt minimizes at least one gastrointestinal side effect associated with oral administration of the opioid analgesic alone. Compositions for use with the method are also provided.
摘要翻译：提供了美珠坚醇和其他阿片样镇痛药的氨基甲酸酯连接前体药物。前药部分可以包含单个氨基酸或短肽。另外，本发明涉及减少受试者胃肠道副作用的方法，胃肠副作用与阿片类镇痛剂的给药有关。所述方法包括将阿片样物质前药或其药学上可接受的盐口服给予受试者，其中所述阿片样物质前药由通过氨基甲酸酯键与前药部分共价结合的阿片类止痛剂组成，并且其中口服给药时，所述前药或药学上可接受的盐使与阿片类镇痛药单独口服给药相关的至少一种胃肠道副作用最小化。还提供了与该方法一起使用的组合物。

5. 发明申请

US20120178666A1 PRODRUGS OF GUANFACINE 审中-公开
标题翻译：关系准则
公开(公告)号：US20120178666A1
公开(公告)日：2012-07-12
申请号：US13496316
申请日：2010-09-15
申请人： Richard Franklin , Robert G. Tyson , Bernard T. Golding , Rhys Whomsley
发明人： Richard Franklin , Robert G. Tyson , Bernard T. Golding , Rhys Whomsley
IPC分类号： A61K38/05 , C07D233/88 , C07D207/277 , C07D239/22 , A61K31/197 , A61K31/4172 , A61K31/513 , A61P25/00 , A61P9/00 , A61P9/12 , A61P29/00 , A61P25/18 , A61P25/22 , A61P25/30 , A61P1/00 , C07D207/16 , C07C271/66 , A61K31/401 , A61K31/4015 , A61K31/27 , A61K31/166 , C07C279/22
CPC分类号： C07C279/22 , C07B2200/07 , C07C279/24
摘要： Prodrugs of guanfacine with amino acids or short peptides, pharmaceutical compositions containing such prodrugs and a method for providing therapeutic benefit in the treatment of ADHD/ODD (attention deficient hyperactivity disorder and oppositional defiance disorder) with guanfacine prodrugs are provided herein. Additionally, methods for minimizing or avoiding the adverse gastrointestinal side effects associated with guanfacine administration, as well as improving the pharmacokinetics of guanfacine are provided herein.
摘要翻译：本发明提供了具有氨基酸或短肽的胍法辛的前药，含有这些前药的药物组合物和用胍法酰前药治疗ADHD / ODD（注意缺陷多动障碍和对抗性蔑视障碍）提供治疗益处的方法。此外，本文提供了用于最小化或避免与胍法卡因给药相关的不良胃肠道副作用以及改善胍法辛的药代动力学的方法。

6. 发明申请

US20100286186A1 NOVEL DICARBOXYLIC ACID LINKED AMINO ACID AND PEPTIDE PRODRUGS OF OPIOIDS AND USES THEREOF 审中-公开
标题翻译：新型二羧酸连接氨基酸和肽类物质及其用途
公开(公告)号：US20100286186A1
公开(公告)日：2010-11-11
申请号：US12753042
申请日：2010-04-01
申请人： Richard Franklin , Bernard T. Golding , Robert G. Tyson
发明人： Richard Franklin , Bernard T. Golding , Robert G. Tyson
IPC分类号： A61K31/485 , C07D489/08 , C07D489/04 , A61P1/00 , A61P25/36 , A61P43/00
CPC分类号： C07D223/04 , A61K31/485 , A61K31/55 , C07D489/02
摘要： The present invention concerns dicarboxylic acid linked amino acid and peptide prodrugs of opioid analgesics and pharmaceutical compositions containing such prodrugs. Methods for providing pain relief, decreasing the adverse GI side effects of the opioid analgesic and increasing the bioavailability of the opioid analgesic with the aforementioned prodrugs are also provided. In one embodiment, prodrugs having the amino acid side chains of valine, leucine, isoleucine and glycine; and mono-, di- and tripeptides thereof are provided.
摘要翻译：本发明涉及二羧酸连接的氨基酸和阿片类镇痛药的肽前药以及含有这些前药的药物组合物。还提供了提供疼痛缓解的方法，降低阿片类止痛剂的不良GI副作用并增加阿片类镇痛药与前述药物的生物利用度。在一个实施方案中，具有缬氨酸，亮氨酸，异亮氨酸和甘氨酸的氨基酸侧链的前药; 并提供其一，二和三肽。

7. 发明申请

US20100227921A1 AMINO ACID AND PEPTIDE CARBAMATE PRODRUGS OF TAPENTADOL AND USES THEREOF 审中-公开
标题翻译：氨基酸和肽的碳酸氢钠制剂及其用途
公开(公告)号：US20100227921A1
公开(公告)日：2010-09-09
申请号：US12714828
申请日：2010-03-01
申请人： Richard Franklin , Bernard T. Golding , Robert G. Tyson
发明人： Richard Franklin , Bernard T. Golding , Robert G. Tyson
IPC分类号： A61K31/27 , C07C271/54 , A61P29/00
CPC分类号： C07C269/02 , C07C271/54
摘要： Prodrugs of tapentadol with amino acids or short peptides, pharmaceutical compositions containing such prodrugs and a method for providing pain relief with the tapentadol prodrugs are provided herein. Prodrugs having side chains of valine, leucine, isoleucine and glycine amino acids and mono-, di- and tripeptides thereof are preferred. Additionally, methods for avoiding or minimizing the adverse gastrointestinal side effects associated with tapentadol administration, as well as increasing the oral bioavailability of tapentadol are provided herein.
摘要翻译：提供了具有氨基酸或短肽的他喷他多的前药，含有这些前药的药物组合物以及用于给他汀类药物前体药物缓解的方法。具有缬氨酸，亮氨酸，异亮氨酸和甘氨酸氨基酸侧链的前药优选其单 - ，二 - 和三肽。此外，本文提供了避免或最小化与他喷他多施用相关的不利胃肠道副作用的方法，以及增加他喷他多的口服生物利用度。

8. 发明申请

US20090186832A1 AMINO ACID PEPTIDE PRO-DRUGS OF PHENOLIC ANALGESICS AND USES THEREOF 审中-公开
标题翻译：苯丙胺类药物及其用途
公开(公告)号：US20090186832A1
公开(公告)日：2009-07-23
申请号：US12356028
申请日：2009-01-19
申请人： Richard Franklin , Bernard T. Golding , Robert G. Tyson
发明人： Richard Franklin , Bernard T. Golding , Robert G. Tyson
IPC分类号： A61K38/05 , C07C271/50 , C07D223/04 , A61K31/55 , C07D489/08 , A61K31/485 , A61K31/4355
CPC分类号： C07D223/04 , A61K47/542 , A61K47/65 , C07D489/08 , C07D489/12
摘要： Prodrugs of meptazinol and other phenolic analgesics exhibiting low oral bioavailability with amino acids or lower peptides, pharmaceutical compositions containing such prodrugs and a method for providing pain relief with such prodrugs are provided. In addition, the present invention relates to methods for increasing the oral bioavailability of a phenolic analgesic. The method comprises orally administering a phenolic analgesic prodrug, wherein the phenolic analgesic is bound to an amino acid or peptide via a carbamate linkage, to a subject in need thereof. Prodrugs having side chains of valine, leucine, isoleucine and glycine amino acids and mono-, di- and tripeptides thereof are preferred.
摘要翻译：提供了与氨基酸或低级肽表现出低口服生物利用度的精蛋白酚和其它酚类止痛剂的药物，含有这些前药的药物组合物以及用这些前药提供疼痛缓解的方法。此外，本发明涉及增加酚类止痛剂的口服生物利用度的方法。该方法包括口服施用酚类止痛前药，其中酚类止痛剂通过氨基甲酸酯键与氨基酸或肽结合，得到有需要的受试者。具有缬氨酸，亮氨酸，异亮氨酸和甘氨酸氨基酸侧链的前药优选其单 - ，二 - 和三肽。

9. 发明申请

US20120196933A1 MEXILETINE PRODRUGS 审中-公开
公开(公告)号：US20120196933A1
公开(公告)日：2012-08-02
申请号：US13335914
申请日：2011-12-22
申请人： Richard Franklin , Bernard T. Golding , Robert G. Tyson
发明人： Richard Franklin , Bernard T. Golding , Robert G. Tyson
IPC分类号： A61K31/205 , C07C279/12 , A61P25/00 , C07C317/50 , A61P21/00 , C07C237/20 , A61K31/165
CPC分类号： A61K31/138 , C07C237/08 , C07C237/22 , C07C271/16 , C07C279/14 , C07C317/48 , C07C323/60 , C07C381/12 , C07D211/58 , C07D339/04 , C07D495/04
摘要： The present invention concerns prodrugs of mexiletine (and mexiletine's active metabolite) pharmaceutical compositions containing such prodrugs. Methods for treating myotonic conditions, while reducing the inherent adverse GI side effects associated with mexiletine, increasing the bioavailability of mexiletine, and improving the pharmacokinetic reproducibility of mexiletine with the aforementioned prodrugs are also provided.
摘要翻译：本发明涉及含有此类前药的美西律（和美西律的活性代谢物）药物组合物的前药。还提供了治疗强直条件的方法，同时减少与美西律相关的固有不良GI副作用，增加美西律的生物利用度，以及改善美西律与前述药物的药代动力学再现性。

10. 发明申请

US20120184532A1 GALANTAMINE AMINO ACID AND PEPTIDE PRODRUGS AND USES THEREOF 审中-公开
标题翻译：甘氨酸氨基酸和肽类产品及其用途
公开(公告)号：US20120184532A1
公开(公告)日：2012-07-19
申请号：US13386335
申请日：2010-07-23
申请人： Richard Franklin , Bernard T. Golding , Robert G. Tyson
发明人： Richard Franklin , Bernard T. Golding , Robert G. Tyson
IPC分类号： A61K31/55 , A61P25/28 , A61P1/12 , A61P1/08 , C07D491/048 , A61P1/00
CPC分类号： C07D491/06
摘要： Prodrugs of galantamine or its 3-hydroxy metabolite with amino acids or short peptides, pharmaceutical compositions containing such prodrugs and methods for treating a memory or cognition disorder with the galantamine prodrugs are provided herein. Prodrugs having side chains of valine, phenylalanine, tyrosine or para amino benzoic acid and mono-, di- and tripeptides thereof are preferred. Additionally, methods for avoiding or minimizing the adverse gastrointestinal side effects associated with galantamine administration, as well as improving the pharmacokinetics of galantamine are provided herein.
摘要翻译：本文提供加兰他敏或其具有氨基酸或短肽的3-羟基代谢物的前药，含有这些前药的药物组合物和用加兰他敏前药治疗记忆障碍或认知障碍的方法。具有缬氨酸，苯丙氨酸，酪氨酸或对氨基苯甲酸侧链的前药和其一，二和三肽是优选的。此外，本文提供了用于避免或最小化与加兰他敏施用相关的不良胃肠道副作用以及改善加兰他敏的药代动力学的方法。

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