-
公开(公告)号：WO2010149760A3
公开(公告)日：2011-09-29
申请号：PCT/EP2010059039
申请日：2010-06-24
申请人： SHIRE LLC , FRANKLIN RICHARD , GOLDING BERNARD T , TYSON ROBERT G
IPC分类号： C07C233/64 , A61K31/155 , A61K31/165 , A61K31/17 , A61P9/06 , C07C237/08 , C07C275/16 , C07C279/14 , C07C323/60 , C07D213/81 , C07D213/82
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。
-
2.发明申请
公开(公告)号：WO2011007247A1
公开(公告)日：2011-01-20
申请号：PCT/IB2010/001747
申请日：2010-07-16
IPC分类号： A61K31/55 , C07D223/04 , 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施用相关。 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键合的阿片样物质止痛剂组成，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。
-
公开(公告)号：WO2010149760A2
公开(公告)日：2010-12-29
申请号：PCT/EP2010/059039
申请日：2010-06-24
IPC分类号： C07C233/64
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AMINO ACID AND PEPTIDE PRODRUGS OF OPIOID ANALGESICS WITH REDUCED GI SIDE-EFFECTS 审中-公开具有减少胃肠道功能障碍的阿片类药物的氨基酸和肽类产品
公开(公告)号：WO2009092073A3
公开(公告)日：2010-02-18
申请号：PCT/US2009031408
申请日：2009-01-19
申请人： SHIRE LLC , FRANKLIN RICHARD , GOLDING BERNARD T , TYSON ROBERT G
IPC分类号： A61K47/48 , A61P25/04 , C07D223/04 , C07D489/08 , C07D489/12
CPC分类号： C07D223/04 , A61K47/542 , A61K47/65 , C07D489/08 , C07D489/12
摘要： 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 peptide of 1-5 amino acids in length, 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： 本发明涉及减少受试者胃肠道副作用的方法，胃肠道副作用与阿片样物质镇痛剂的给药有关。 所述方法包括向受试者口服阿片样物质前药或其药学上可接受的盐，其中阿片样物质前药由通过氨基甲酸酯键与长度为1-5个氨基酸的肽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
公开(公告)号：WO2011007247A8
公开(公告)日：2012-07-19
申请号：PCT/IB2010001747
申请日：2010-07-16
申请人： SHIRE LLC , FRANKLIN RICHARD , GOLDING BERNARD T , TYSON ROBERT G
IPC分类号： A61K31/55 , A61P25/04 , C07D223/04
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施用相关。 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。
-
公开(公告)号：WO2011011766A1
公开(公告)日：2011-01-27
申请号：PCT/US2010/043166
申请日：2010-07-23
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。
-
公开(公告)号：WO2010100477A3
公开(公告)日：2010-09-10
申请号：PCT/GB2010/050353
申请日：2010-03-01
IPC分类号： C07C269/02 , C07C271/54 , A61K47/48 , A61P25/04
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.
-
8.发明申请
公开(公告)号：WO2009092071A3
公开(公告)日：2010-02-11
申请号：PCT/US2009031404
申请日：2009-01-19
申请人： SHIRE LLC , FRANKLIN RICHARD , GOLDING BERNARD T , TYSON ROBERT G
IPC分类号： A61K47/48 , A61P25/04 , C07D223/04 , C07D489/08 , C07D489/12
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种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AMINO ACID AND PEPTIDE PRODRUGS OF OPIOID ANALGESICS WITH REDUCED GI SIDE-EFFECTS 审中-公开具有减少胃肠道功能障碍的阿片类药物的氨基酸和肽类产品
公开(公告)号：WO2009092073A2
公开(公告)日：2009-07-23
申请号：PCT/US2009/031408
申请日：2009-01-19
IPC分类号： C07D489/08 , C07D223/04 , C07D489/12 , A61P25/04 , A61K47/48
CPC分类号： C07D223/04 , A61K47/542 , A61K47/65 , C07D489/08 , C07D489/12
摘要： 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 peptide of 1-5 amino acids in length, 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： 本发明涉及减少受试者胃肠道副作用的方法，胃肠道副作用与阿片样物质镇痛剂的给药有关。 所述方法包括向受试者口服阿片样物质前药或其药学上可接受的盐，其中阿片样物质前药由通过氨基甲酸酯键与长度为1-5个氨基酸的肽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。
-
公开(公告)号：WO2011033296A1
公开(公告)日：2011-03-24
申请号：PCT/GB2010/051544
申请日：2010-09-15
IPC分类号： 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： 具有氨基酸或短肽的胍法酰胺的前药，含有这些前药的药物组合物以及用胍法酰前药在治疗ADHD / ODD（注意缺陷多动障碍和对抗性蔑视障碍）中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。
-
-
-
-
-
-
-
-
-
搜索结果
14 条记录 (耗时 0.015 秒)
