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公开(公告)号：US20180305310A1
公开(公告)日：2018-10-25
申请号：US16022019
申请日：2018-06-28
IPC分类号： C07D207/16 , C07D209/18
摘要： Augmented or synergized anti-inflammatory constructs are disclosed including anti-inflammatory amino acids covalently conjugated with other anti-inflammatory molecules such as nonsteroidal anti-inflammatory drugs, vanilloids and ketone bodies. Further conjugation with a choline bioisostere or an additional anti-inflammatory moiety further augments the anti-inflammatory activity.
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公开(公告)号：US10752582B2
公开(公告)日：2020-08-25
申请号：US16022019
申请日：2018-06-28
IPC分类号： C07D207/16 , C07D209/18 , A61K47/54 , A61K47/55
摘要： Augmented or synergized anti-inflammatory constructs are disclosed including anti-inflammatory amino acids covalently conjugated with other anti-inflammatory molecules such as nonsteroidal anti-inflammatory drugs, vanilloids and ketone bodies. Further conjugation with a choline bioisostere or an additional anti-inflammatory moiety further augments the anti-inflammatory activity.
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公开(公告)号：US20170143836A1
公开(公告)日：2017-05-25
申请号：US15365088
申请日：2016-11-30
发明人： Jeffrey D. Laskin , Diane E. Heck , Mou-Tuan Huang , Karine Fabio , Jeffrey C. Lacey , Sherri C. Young , Pramod Mohanta , Christophe Gullion , Ned D. Heindel
IPC分类号： A61K31/695 , C07F7/08 , C07D209/28 , A61K31/192 , A61K31/405 , A61K9/00 , C07C69/96 , C07C229/42
CPC分类号： C07F7/0812 , A61K9/0014 , A61K31/19 , A61K31/192 , A61K31/196 , A61K31/405 , A61K47/54 , A61K47/55 , C07C69/96 , C07C229/42 , C07C2602/10 , C07D209/28 , C07F7/081
摘要： A new family of therapeutics which provides a controlled-release delivery platform for non-steroidal anti-inflammatory agents on an ester or an ester-carbonate backbone is disclosed herein. These agents are reversible inhibitors of acetylcholinesterase and are thus useful for clinical conditions benefiting from inflammation suppression and cholinergic intervention. These compounds are of the general formula wherein n=0, 1; X═C, Si, and N+ and NSAID=ibuprofen, naproxen, indomethacin and diclofenac. Other embodiments are also disclosed.
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公开(公告)号：US20170044096A1
公开(公告)日：2017-02-16
申请号：US15334882
申请日：2016-10-26
IPC分类号： C07C237/06 , C07D209/18 , C07D207/16 , C07C271/12
CPC分类号： C07D207/16 , A61K47/542 , A61K47/543 , A61K47/55 , C07D209/18
摘要： Augmented or synergized anti-inflammatory constructs are disclosed including anti-inflammatory amino acids covalently conjugated with other anti-inflammatory molecules such as nonsteroidal anti-inflammatory drugs, vanilloids and ketone bodies. Further conjugation with a choline bioisostere or an additional anti-inflammatory moiety further augments the anti-inflammatory activity.
摘要翻译： 公开了增强或协同的抗炎构建体，其包括与其它抗炎分子如非甾体抗炎药，香草醛和酮体共价缀合的抗炎氨基酸。 与胆碱生物电子等排物或其它消炎部分的进一步共轭进一步增加了抗炎活性。
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公开(公告)号：US11731991B2
公开(公告)日：2023-08-22
申请号：US16991440
申请日：2020-08-12
IPC分类号： C07F7/08 , A61K31/405 , A61K31/196 , A61K31/19 , A61K47/55 , A61K9/00 , A61K31/192 , C07C69/96 , C07C229/42 , C07D209/28 , A61K47/54
CPC分类号： C07F7/0812 , A61K9/0014 , A61K31/19 , A61K31/192 , A61K31/196 , A61K31/405 , A61K47/54 , A61K47/55 , C07C69/96 , C07C229/42 , C07D209/28 , C07F7/081 , C07C2602/10
摘要： Augmented or synergized anti-inflammatory constructs are disclosed including anti-inflammatory terpenes and/or vanilloids covalently conjugated to one another so that the activity of the conjugate is greater than the sum of its parts. Also disclosed are methods of improving the potency of an anti-inflammatory terpene or vanilloid by linking it to another anti-inflammatory terpene or vanilloid via a carbamate linkage, where the potency of the conjugate is greater than the sum of its parts.
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公开(公告)号：US10570161B2
公开(公告)日：2020-02-25
申请号：US15365088
申请日：2016-11-30
发明人： Jeffrey D. Laskin , Diane E. Heck , Mou-Tuan Huang , Karine Fabio , Carl J. Lacey , Sherri C. Young , Pramod Mohanta , Christophe Guillon , Ned D. Heindel
IPC分类号： C07F7/08 , A61K31/405 , A61K31/196 , A61K31/19 , A61K47/55 , A61K47/54 , A61K9/00 , A61K31/192 , C07C69/96 , C07C229/42 , C07C209/28 , C07D209/28
摘要： A new family of therapeutics which provides a controlled-release delivery platform for non-steroidal anti-inflammatory agents on an ester or an ester-carbonate backbone is disclosed herein. These agents are reversible inhibitors of acetylcholinesterase and are thus useful for clinical conditions benefiting from inflammation suppression and cholinergic intervention. These compounds are of the general formula wherein n=0, 1; X=C, Si, and N+ and NSAID=ibuprofen, naproxen, indomethacin and diclofenac. Other embodiments are also disclosed.
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公开(公告)号：US20200369688A1
公开(公告)日：2020-11-26
申请号：US16991440
申请日：2020-08-12
IPC分类号： C07F7/08 , A61K31/405 , A61K31/196 , A61K31/19 , A61K47/55 , A61K47/54 , A61K9/00 , A61K31/192 , C07C69/96 , C07C229/42 , C07D209/28
摘要： Augmented or synergized anti-inflammatory constructs are disclosed including anti-inflammatory terpenes and/or vanilloids covalently conjugated to one another so that the activity of the conjugate is greater than the sum of its parts. Also disclosed are methods of improving the potency of an anti-inflammatory terpene or vanilloid by linking it to another anti-inflammatory terpene or vanilloid via a carbamate linkage, where the potency of the conjugate is greater than the sum of its parts.
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公开(公告)号：US09512068B2
公开(公告)日：2016-12-06
申请号：US14776857
申请日：2014-03-14
IPC分类号： C07C261/00 , C07C269/00 , C07C271/00 , C07C271/52 , A61K47/48 , A61K31/132 , A61K31/198 , A61K31/27 , A61K31/4015 , A61K31/405 , C07C271/16 , C07C271/22 , C07C271/48 , C07D207/16 , C07D209/26 , C07C271/12 , C07C271/34 , C07C271/50
CPC分类号： C07C271/52 , A61K31/132 , A61K31/198 , A61K31/27 , A61K31/4015 , A61K31/405 , A61K47/542 , C07C271/12 , C07C271/16 , C07C271/22 , C07C271/34 , C07C271/48 , C07C271/50 , C07C2601/16 , C07C2602/42 , C07D207/16 , C07D209/26
摘要： Augmented or synergized anti-inflammatory constructs are disclosed including terpenes covalently conjugated with other anti-inflammatory molecules such as nonsteroidal anti-inflammatory drugs, vanilloids, amino acids and polyamines; and anti-inflammatory molecules covalently conjugated with specific amino acids. For the latter, further conjugation with a choline bioisostere further augments the anti-inflammatory activity.
摘要翻译： 公开了增强或协同的抗炎构建体，包括与其它抗炎分子如非甾体抗炎药，香草素，氨基酸和多胺共价共轭的萜烯; 和与特定氨基酸共价结合的抗炎分子。 对于后者，与胆碱生物电子等排进一步缀合进一步增加抗炎活性。
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公开(公告)号：US20160031804A1
公开(公告)日：2016-02-04
申请号：US14776857
申请日：2014-03-14
IPC分类号： C07C271/52 , C07C271/50 , C07C271/12 , C07C271/48 , C07C271/16 , C07C271/34 , C07C271/22
CPC分类号： C07C271/52 , A61K31/132 , A61K31/198 , A61K31/27 , A61K31/4015 , A61K31/405 , A61K47/542 , C07C271/12 , C07C271/16 , C07C271/22 , C07C271/34 , C07C271/48 , C07C271/50 , C07C2601/16 , C07C2602/42 , C07D207/16 , C07D209/26
摘要： Augmented or synergized anti-inflammatory constructs are disclosed including terpenes covalently conjugated with other anti-inflammatory molecules such as nonsteroidal anti-inflammatory drugs, vanilloids, amino acids and polyamines; and anti-inflammatory molecules covalently conjugated with specific amino acids. For the latter, further conjugation with a choline bioisostere further augments the anti-inflammatory activity.
摘要翻译： 公开了增强或协同的抗炎构建体，包括与其它抗炎分子如非甾体抗炎药，香草素，氨基酸和多胺共价共轭的萜烯; 和与特定氨基酸共价结合的抗炎分子。 对于后者，与胆碱生物电子等排进一步缀合进一步增加抗炎活性。
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