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1. 发明公开

US20240051979A1 TREPROSTINIL PRODRUGS 审中-公开
公开(公告)号：US20240051979A1
公开(公告)日：2024-02-15
申请号：US18120110
申请日：2023-03-10
申请人： United Therapeutics Corporation
发明人： Kenneth Robert Phares , Hitesh Batra , Liang Guo
IPC分类号： C07F9/6574 , C07C59/72 , C07D207/16 , C07D211/60 , C07D265/30 , C07D317/40 , C07D321/12 , C07F9/09
CPC分类号： C07F9/65744 , C07C59/72 , C07D207/16 , C07D211/60 , A61K9/0019 , C07D317/40 , C07D321/12 , C07F9/09 , C07D265/30
摘要： Provided are novel prodrugs of treprostinil, as well as methods of making and methods of using these prodrugs.

2. 发明授权

US11857657B2 Diarylalkanes as potent inhibitors of binuclear enzymes 有权
公开(公告)号：US11857657B2
公开(公告)日：2024-01-02
申请号：US17113193
申请日：2020-12-07
申请人： Unigen, Inc.
发明人： Qi Jia , Ji-Fu Zhao
IPC分类号： C07C39/15 , A61K8/34 , A61K31/015 , A61K31/05 , A61K31/085 , A61K31/09 , A61K31/357 , A61K31/40 , A61K31/704 , C07C39/367 , C07C45/67 , C07C49/835 , C07C215/74 , C07D321/12 , A61K8/31 , A61K8/9789 , A61K8/9794 , C07C43/23 , A61Q19/02 , C07C41/26 , C07C41/32 , A61K8/49
CPC分类号： A61K8/347 , A61K8/31 , A61K8/4973 , A61K8/9789 , A61K8/9794 , A61K31/015 , A61K31/05 , A61K31/085 , A61K31/09 , A61K31/357 , A61K31/40 , A61K31/704 , A61Q19/02 , C07C39/15 , C07C39/367 , C07C41/26 , C07C41/32 , C07C43/23 , C07C45/673 , C07C49/835 , C07C215/74 , C07D321/12 , A61K2800/782 , Y02A50/30 , C07C45/673 , C07C49/835
摘要： The present invention implements a strategy that combines an enzyme inhibition assay with a chemical dereplication process to identify active plant extracts and the particular compounds—diarylalkanes and/or diarylalkanols within those extracts that specifically inhibit binuclear enzyme function. Included in the present invention are compositions of matter comprised of one or more of diarylalkanes and/or diarylalkanols, which inhibit the activity of binuclear enzymes, particularly tyrosinase and which prevent melanin overproduction. The present invention also provides a method for inhibiting the activity of a binuclear enzyme, particularly tyrosinase and a method for preventing and treating diseases and conditions related to binuclear enzyme function. The present invention further includes a method for preventing and treating melanin overproduction and diseases and conditions of the skin related thereto. The method for preventing and treating diseases and conditions related to binuclear enzyme function and melanin overproduction is comprised of administering to a host in need thereof an effective amount of a composition comprising one or more diarylalkanes and/or diarylalkanols synthesized and/or isolated from one or more plants together with a pharmaceutically acceptable carrier.

3. 发明申请

US20210387987A1 Crosslinked Polymers with Tunable Coefficients of Thermal Expansion 有权
公开(公告)号：US20210387987A1
公开(公告)日：2021-12-16
申请号：US17344717
申请日：2021-06-10
申请人： National Technology & Engineering Solutions of Sandia, LLC
发明人： Erica Marie Redline , Chad Staiger , David R. Wheeler , Leah Appelhans , Jeffrey C. Foster
IPC分类号： C07D471/14 , C08K5/17 , C08K5/053 , C08K5/23 , C07C211/60 , C07D321/12
摘要： Curatives and their resulting thermosets and other crosslinked polymers can reduce thermal expansion mismatch between an encapsulant and objects that are encapsulated. This can be accomplished by incorporating a negative CTE moiety into the thermoset resin or polymer backbone. The negative CTE moiety can be a thermal contractile unit that shrinks as a result of thermally induced conversion from a twist-boat to chair or cis/trans isomerization upon heating. Beyond CTE matching, other potential uses for these crosslinked polymers and thermosets include passive energy generation, energy absorption at high strain rates, mechanophores, actuators, and piezoelectric applications.

4. 发明授权

US11198898B2 Chemical tools for imaging phospholipase D activity 有权
公开(公告)号：US11198898B2
公开(公告)日：2021-12-14
申请号：US16131798
申请日：2018-09-14
申请人： CORNELL UNIVERSITY
发明人： Jeremy Baskin , Timothy Bumpus , Dongjun Liang
IPC分类号： C12Q1/42 , C07C233/60 , C07C33/05 , C07C43/196 , C07C235/08 , C07D321/12 , C07D313/18
摘要： A method for detecting phospholipase D (PLD) activity in a cell, comprising: (i) stimulating endogenous PLD in said cell for said PLD to catalyze a transphosphatidylation reaction between phosphatidylcholine or a derivative thereof and an exogenous functionalized alcohol to form a phosphatidyl alcohol, wherein the functionalized alcohol possesses a first functional group that can react with and form a bond to a functionalized detectable label having a second functional group reactive with the first functional group, and said phosphatidyl alcohol contains said first functional group in available form; (ii) reacting said phosphatidyl alcohol with said functionalized detectable label under conditions where said functionalized detectable label reacts, via its second functional group, with the first functional group to form a linkage between said detectable label and said phosphatidyl alcohol so as to form a labeled phosphatidyl alcohol containing said detectable label; and (iii) detecting said labeled phosphatidyl alcohol.

5. 发明授权

US11084813B2 High penetration drugs and their compositions thereof for treatment of Parkinson diseases 有权
公开(公告)号：US11084813B2
公开(公告)日：2021-08-10
申请号：US15634272
申请日：2017-06-27
申请人： Techfields Pharma Co., Ltd.
发明人： Chongxi Yu , Lina Xu
IPC分类号： C07D471/04 , C07C271/16 , C07C271/22 , C07D321/12 , C07C219/10 , C07C219/14 , C07C219/28 , C07C229/12 , C07C327/30 , C07C229/58 , C07D455/02 , C07C237/06 , C07C237/20 , C07D207/16 , C07K5/083 , C07D211/62 , C07K5/097 , A61K31/137 , C07C229/36 , A61K31/195 , A61K31/198 , A61K31/277 , C07C317/44 , A61K31/197 , A61K31/24 , A61K31/40 , C07C219/06 , C07C219/32 , C07C237/08 , C07C327/36 , C07C217/60
摘要： One aspect of the invention provides a composition of novel high penetration compositions (HPC) or a high penetration prodrug (HPP) for treatment of Parkinson's disease. The HPCs/HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPCs/HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

6. 发明申请

US20210085580A1 DIARYLALKANES AS POTENT INHIBITORS OF BINUCLEAR ENZYMES 有权
公开(公告)号：US20210085580A1
公开(公告)日：2021-03-25
申请号：US17113193
申请日：2020-12-07
申请人： Unigen, Inc.
发明人： Qi Jia , Ji-Fu Zhao
IPC分类号： A61K8/34 , A61K31/015 , A61K31/05 , A61K31/085 , A61K31/09 , A61K31/357 , A61K31/40 , A61K31/704 , C07C39/15 , C07C39/367 , C07C45/67 , C07C49/835 , C07C215/74 , C07D321/12 , A61K8/31 , A61K8/9789 , A61K8/9794 , C07C43/23 , A61Q19/02 , C07C41/26 , C07C41/32 , A61K8/49
摘要： The present invention implements a strategy that combines an enzyme inhibition assay with a chemical dereplication process to identify active plant extracts and the particular compounds—diarylalkanes and/or diarylalkanols within those extracts that specifically inhibit binuclear enzyme function. Included in the present invention are compositions of matter comprised of one or more of diarylalkanes and/or diarylalkanols, which inhibit the activity of binuclear enzymes, particularly tyrosinase and which prevent melanin overproduction. The present invention also provides a method for inhibiting the activity of a binuclear enzyme, particularly tyrosinase and a method for preventing and treating diseases and conditions related to binuclear enzyme function. The present invention further includes a method for preventing and treating melanin overproduction and diseases and conditions of the skin related thereto. The method for preventing and treating diseases and conditions related to binuclear enzyme function and melanin overproduction is comprised of administering to a host in need thereof an effective amount of a composition comprising one or more diarylalkanes and/or diarylalkanols synthesized and/or isolated from one or more plants together with a pharmaceutically acceptable carrier.

7. 发明申请

US20170233365A1 CYCLOOCTENES FOR BIOORTHOGONOL REACTIONS 审中-公开
公开(公告)号：US20170233365A1
公开(公告)日：2017-08-17
申请号：US15502806
申请日：2015-08-11
申请人： The General Hospital Corporation
发明人： Scott A. Hilderbrand , Balazs R. Varga , Ralph Weissleder
IPC分类号： C07D321/12 , C07D413/12 , C07D263/52 , C07C43/196 , C07D405/12
CPC分类号： C07D321/12 , C07C43/196 , C07C2601/18 , C07D207/46 , C07D263/52 , C07D405/12 , C07D413/12
摘要： This disclosure relates to trans-cyclooctene compounds and methods of using the same in bioorthogonal labeling experiments.

8. 发明申请

US20160002157A1 NOVEL HIGH PENETRATION DRUGS AND THEIR COMPOSITIONS THEREOF FOR TREATMENT OF PARKINSON DISEASES 有权
标题翻译：新型高渗透药物及其治疗帕金森病的组合物
公开(公告)号：US20160002157A1
公开(公告)日：2016-01-07
申请号：US14854616
申请日：2015-09-15
申请人： SUZHOU TECHFIELDS MEDICAL LTD.
发明人： Chongxi YU , Lina XU
IPC分类号： C07C317/44 , C07C271/22 , C07D211/62 , C07D471/04 , C07D321/12 , A61K31/40 , C07C219/32 , C07C219/06 , C07C327/36 , A61K31/24 , A61K31/197 , A61K31/277 , C07C237/08 , C07D207/16
CPC分类号： C07D471/04 , A61K31/137 , A61K31/195 , A61K31/197 , A61K31/198 , A61K31/24 , A61K31/277 , A61K31/40 , C07C217/60 , C07C219/06 , C07C219/10 , C07C219/14 , C07C219/28 , C07C219/32 , C07C229/12 , C07C229/36 , C07C229/58 , C07C237/06 , C07C237/08 , C07C237/20 , C07C271/16 , C07C271/22 , C07C317/44 , C07C327/30 , C07C327/36 , C07C2602/08 , C07D207/16 , C07D211/62 , C07D321/12 , C07D455/02 , C07K5/0806 , C07K5/0823 , A61K2300/00
摘要： One aspect of the invention provides a composition of novel high penetration compositions (HPC) or a high penetration prodrug (HPP) for treatment of Parkinson's disease. The HPCs/HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPCs/HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
摘要翻译：本发明的一个方面提供了用于治疗帕金森病的新型高渗透组合物（HPC）或高渗透性前药（HPP）的组合物。 HPC / HPP能够在穿过生物屏障之后转化为亲本活性药物或药物代谢物，因此可以对母体药物或代谢物可以进行的处理。此外，HPP能够达到母体药物可能无法进入或在目标区域提供足够浓度的区域，从而进行新的治疗。 HPC / HPP可以通过各种施用途径施用于受试者，例如局部递送至具有高浓度或系统地施用于生物受试者的病症的作用部位并以更快的速率进入总体循环。

9. 发明授权

US09126913B2 Diarylalkanes as potent inhibitors of binuclear enzymes 有权
标题翻译：二芳基烷烃作为双核酶的有效抑制剂
公开(公告)号：US09126913B2
公开(公告)日：2015-09-08
申请号：US14209814
申请日：2014-03-13
申请人： Unigen, Inc.
发明人： Qi Jia , Ji-Fu Zhao
IPC分类号： A61K31/075 , C07C43/23 , A61K31/015 , A61K31/05 , A61K31/085 , A61K31/09 , A61K31/357 , A61K31/40 , A61K31/704 , C07C39/15 , C07C39/367 , C07C45/67 , C07C49/835 , C07C215/74 , C07D321/12 , A61K8/34 , A61Q19/02 , C07C41/26 , C07C41/32
CPC分类号： A61K8/347 , A61K8/31 , A61K8/4973 , A61K8/97 , A61K31/015 , A61K31/05 , A61K31/085 , A61K31/09 , A61K31/357 , A61K31/40 , A61K31/704 , A61K2800/782 , A61Q19/02 , C07C39/15 , C07C39/367 , C07C41/26 , C07C41/32 , C07C43/23 , C07C45/673 , C07C49/835 , C07C215/74 , C07D321/12 , Y02A50/406 , Y02A50/411
摘要： The present invention implements a strategy that combines an enzyme inhibition assay with a chemical dereplication process to identify active plant extracts and the particular compounds—diarylalkanes and/or diarylalkanols within those extracts that specifically inhibit binuclear enzyme function. Included in the present invention are compositions of matter comprised of one or more of diarylalkanes and/or diarylalkanols, which inhibit the activity of binuclear enzymes, particularly tyrosinase and which prevent melanin overproduction. The present invention also provides a method for inhibiting the activity of a binuclear enzyme, particularly tyrosinase and a method for preventing and treating diseases and conditions related to binuclear enzyme function. The present invention further includes a method for preventing and treating melanin overproduction and diseases and conditions of the skin related thereto. The method for preventing and treating diseases and conditions related to binuclear enzyme function and melanin overproduction is comprised of administering to a host in need thereof an effective amount of a composition comprising one or more diarylalkanes and/or diarylalkanols synthesized and/or isolated from one or more plants together with a pharmaceutically acceptable carrier.
摘要翻译：本发明实现了一种将酶抑制测定与化学去除方法结合以鉴别活性植物提取物和特异性抑制双核酶功能的那些提取物中的二芳基烷烃和/或二芳基链烷醇的策略。包括在本发明中的是由一种或多种二芳基烷烃和/或二芳基链烷醇组成的物质组合物，其抑制双核酶，特别是酪氨酸酶的活性，并且其防止黑色素过量产生。本发明还提供了抑制双核酶，特别是酪氨酸酶的活性的方法，以及用于预防和治疗与双核酶功能相关的疾病和病症的方法。本发明还包括一种预防和治疗与其相关的黑色素过量产生及其疾病和病症的方法。用于预防和治疗与双核酶功能和黑色素过量产生相关的疾病和病症的方法包括向有需要的宿主施用有效量的包含一种或多种二芳基烷烃和/或二芳基链烷醇的组合物，所述二芳基烷烃和/或二芳基链烷醇合成和/或分离自更多的植物和药学上可接受的载体。

10. 发明申请

US20130252909A1 TANNIN INHIBITORS OF HIV 有权
标题翻译：艾滋病毒T宁抑制剂
公开(公告)号：US20130252909A1
公开(公告)日：2013-09-26
申请号：US13788691
申请日：2013-03-07
申请人： UNIVERSITY OF IOWA RESEARCH FOUNDATION
发明人： George A. Kraus , Wendy Maury
IPC分类号： C07H15/04 , C07D321/12 , C07H3/02 , C07H13/08
CPC分类号： A61K31/70 , A61K31/22 , A61K31/365 , A61K31/366 , C07D321/12 , C07H3/02 , C07H13/08 , C07H15/04
摘要： The invention provides a method to prevent or treat HIV-infection with synthetic tannins, and pharmaceutical compositions comprising synthetic tannins.
摘要翻译：本发明提供了用合成单宁预防或治疗HIV感染的方法，以及包含合成单宁的药物组合物。

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