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1.
公开(公告)号:US20240358727A1
公开(公告)日:2024-10-31
申请号:US18635427
申请日:2024-04-15
发明人: Kirin D. Gada , Leigh D. Plant
IPC分类号: A61K31/683 , A61K31/10 , A61K31/132 , A61K31/137 , A61K31/235 , A61K31/265 , A61K31/27 , A61K31/365 , A61K31/58 , A61K31/685 , A61K31/7036 , A61P9/06 , G01N33/50
CPC分类号: A61K31/683 , A61K31/10 , A61K31/132 , A61K31/137 , A61K31/235 , A61K31/265 , A61K31/27 , A61K31/365 , A61K31/58 , A61K31/685 , A61K31/7036 , A61P9/06 , G01N33/502
摘要: Voltage-gated sodium (NaV) channels are densely expressed in most excitable cells and activate in response to depolarization, causing a rapid influx of Na+ ions that initiates the action potential. The voltage-dependent activation of NaV channels is followed almost instantaneously by fast inactivation, setting the refractory period of excitable tissues. The gating cycle of NaV channels is subject to tight regulation, with perturbations leading to a range of pathophysiological states. The gating properties of most ion channels are regulated by the membrane phospholipid, phosphatidylinositol (4,5) bisphosphate (PI(4,5)P2). However, it is not known whether PI(4,5)P2 modulates the activity of NaV channels. Here, we utilize optogenetics to activate specific, membrane-associated phosphoinositide (PI)-phosphatases that dephosphorylate PI(4,5)P2 while simultaneously recording NaV1.4 channel currents. We show that dephosphorylating PI(4,5)P2 left-shifts the voltage-dependent gating of NaV1.4 to more hyperpolarized membrane potentials, augments the late current that persists after fast inactivation, and speeds the rate at which channels recover from fast inactivation. These effects are opposed by exogenous diC8PI(4,5)P2. We provide evidence that PI(4,5)P2 is a negative regulator that tunes the gating behavior of NaV1.4 channels.
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公开(公告)号:US12090138B2
公开(公告)日:2024-09-17
申请号:US17588033
申请日:2022-01-28
发明人: He Sun , Xijun Yan , Naifeng Wu , Kaijing Yan , Yonghong Zhu , Shunnan Zhang , Xiaolin Bai , Xiaohui Ma , Yi He , Ting Li , Lei Li
IPC分类号: A61K31/357 , A61K9/08 , A61K9/16 , A61K9/48 , A61K31/205 , A61K31/355 , A61K31/683 , A61K36/488 , A61K36/82 , A61K47/24 , A61P1/16
CPC分类号: A61K31/357 , A61K9/08 , A61K9/1617 , A61K9/1682 , A61K9/48 , A61K31/205 , A61K31/355 , A61K31/683 , A61K36/488 , A61K36/82 , A61K47/24 , A61P1/16 , A61K2236/19
摘要: A pharmaceutical composition is prepared from the following raw materials (in parts by weight): silybin (8.75-60), phospholipid (15-65), a Pu'er tea extract (25-200), and vitamin E (6.25-40). The composition has the effect of treating non-alcoholic fatty liver diseases.
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公开(公告)号:US20240189366A1
公开(公告)日:2024-06-13
申请号:US18541250
申请日:2023-12-15
发明人: Inge Bruheim , Snorre Tilseth , Daniele Mancinelli
IPC分类号: A61K35/612 , A23L33/115 , A61K9/00 , A61K9/48 , A61K31/122 , A61K31/20 , A61K31/202 , A61K31/215 , A61K31/23 , A61K31/235 , A61K31/575 , A61K31/683 , A61K31/685 , A61K45/06 , C11B3/00
CPC分类号: A61K35/612 , A23L33/115 , A61K9/0053 , A61K9/48 , A61K9/4825 , A61K9/4858 , A61K31/122 , A61K31/20 , A61K31/202 , A61K31/215 , A61K31/23 , A61K31/235 , A61K31/575 , A61K31/683 , A61K31/685 , A61K45/06 , C11B3/006 , A23V2002/00
摘要: This invention discloses new krill oil compositions characterized by having high amounts of phospholipids, astaxanthin esters and/or omega-3 contents. The krill oils are obtained from krill meal using supercritical fluid extraction in a two stage process. Stage 1 removes the neutral lipid by extracting with neat supercritical CO2 or CO2 plus approximately 5% of a co-solvent. Stage 2 extracts the actual krill oils by using supercritical CO2 in combination with approximately 20% ethanol. The krill oil materials obtained are compared with commercially available krill oil and found to be more bioeffective in a number of areas such as anti-inflammation, anti-oxidant effects, improving insulin resistances and improving blood lipid profile.
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公开(公告)号:US12004868B2
公开(公告)日:2024-06-11
申请号:US16432498
申请日:2019-06-05
发明人: Lawrence Helson , George M. Shopp , Annie Bouchard
IPC分类号: A61B5/00 , A61B5/364 , A61K9/00 , A61K9/127 , A61K31/12 , A61K31/445 , A61K31/4545 , A61K31/506 , A61K31/683
CPC分类号: A61B5/4848 , A61B5/364 , A61K9/0019 , A61K9/127 , A61K31/12 , A61K31/445 , A61K31/4545 , A61K31/506 , A61K31/683 , A61B2503/42
摘要: Compositions and methods are provided for preventing one or more cardiac channelopathies or conditions resulting from irregularities or alterations in cardiac patterns, or both, in a human or animal subject comprising: one or more pharmacologically active agents that causes at least one of IKr channel inhibition or QT prolongation by inhibiting the activity of an ether-a-go-go-related gene (hERG); and one or more liposomes, wherein the liposomes are empty liposomes and administered prior to, concomitantly, or after administration of the pharmacologically active agent.
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公开(公告)号:US20240180936A1
公开(公告)日:2024-06-06
申请号:US18515734
申请日:2023-11-21
发明人: Basil RIGAS
IPC分类号: A61K31/683 , A61P25/02
CPC分类号: A61K31/683 , A61P25/02
摘要: The invention features methods of preventing and/or treating neuropathic pain associated with chemotherapy-induced peripheral neuropathy (CIPN).
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6.
公开(公告)号:US20240091251A1
公开(公告)日:2024-03-21
申请号:US18241303
申请日:2023-09-01
发明人: Nate Larson , Robert G. Strickley
IPC分类号: A61K31/724 , A61K9/00 , A61K9/19 , A61K31/683 , A61K47/40 , A61K47/69 , A61P31/12
CPC分类号: A61K31/724 , A61K9/0019 , A61K9/19 , A61K31/683 , A61K47/40 , A61K47/6951 , A61P31/12
摘要: The present disclosure provides a composition comprising Compound 1, or a pharmaceutically acceptable salt thereof, cyclodextrin, and, optionally, pH adjusting agents.
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公开(公告)号:US11865143B2
公开(公告)日:2024-01-09
申请号:US15915439
申请日:2018-03-08
发明人: Inge Bruheim , Snorre Tilseth , Daniele Mancinelli
IPC分类号: A61K35/612 , A61K9/48 , A61K31/215 , A23L33/115 , A61K31/122 , A61K31/23 , A61K31/683 , A61K31/685 , A61K45/06 , C11B3/00 , A61K31/202 , A61K31/20 , A61K31/235 , A61K9/00 , A61K31/575
CPC分类号: A61K35/612 , A23L33/115 , A61K9/0053 , A61K9/48 , A61K9/4825 , A61K9/4858 , A61K31/122 , A61K31/20 , A61K31/202 , A61K31/215 , A61K31/23 , A61K31/235 , A61K31/575 , A61K31/683 , A61K31/685 , A61K45/06 , C11B3/006 , A23V2002/00 , A61K31/23 , A61K2300/00 , A61K31/683 , A61K2300/00 , A61K31/685 , A61K2300/00 , A61K31/122 , A61K2300/00
摘要: This invention discloses new krill oil compositions characterized by having high amounts of phospholipids, astaxanthin esters and/or omega-3 contents. The krill oils are obtained from krill meal using supercritical fluid extraction in a two stage process. Stage 1 removes the neutral lipid by extracting with neat supercritical CO2 or CO2 plus approximately 5% of a co-solvent. Stage 2 extracts the actual krill oils by using supercritical CO2 in combination with approximately 20% ethanol. The krill oil materials obtained are compared with commercially available krill oil and found to be more bioeffective in a number of areas such as anti-inflammation, anti-oxidant effects, improving insulin resistances and improving blood lipid profile.
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8.
公开(公告)号:US20230310469A1
公开(公告)日:2023-10-05
申请号:US18023600
申请日:2021-08-30
申请人: Accencio LLC
发明人: Kevin Brown , Kevin Brogle
IPC分类号: A61K31/683 , A61K31/708 , A61K31/55 , A61K31/4375 , A61K31/522 , A61K9/00
CPC分类号: A61K31/683 , A61K31/708 , A61K31/55 , A61K31/4375 , A61K31/522 , A61K9/0014
摘要: The present disclosure relates to methods of treating at least one symptom of a coronavirus infection, or preventing an acute inflammatory response, e.g., a cytokine storm in a coronavirus patient, in particular a SARS-CoV-19 patient, by administering a Toll-Like-Receptor (TLR) agonist, in particular a TLR-7 or TLR-8 agonist.
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公开(公告)号:US11771710B2
公开(公告)日:2023-10-03
申请号:US17323260
申请日:2021-05-18
申请人: SRX CARDIO, LLC
IPC分类号: A61K31/675 , C07F9/59 , C07F9/6518 , A61K45/06 , A61K31/41 , A61K31/454 , A61K31/4245 , A61K31/683 , A61K38/00 , A61K38/05 , C07D401/12 , C07D403/12 , C07D413/14 , C07F9/653 , C07K5/065
CPC分类号: A61K31/675 , A61K31/41 , A61K31/4245 , A61K31/454 , A61K31/683 , A61K38/005 , A61K38/05 , A61K45/06 , C07D401/12 , C07D403/12 , C07D413/14 , C07F9/59 , C07F9/6518 , C07F9/65312 , C07K5/06078
摘要: This invention is related to the field of PCSK9 biology and the composition and methods of use of small molecule ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small molecule compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small molecule ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small molecule ligands that can raise LDL levels.
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公开(公告)号:US20230151048A1
公开(公告)日:2023-05-18
申请号:US17604451
申请日:2019-03-21
发明人: Junbiao CHANG , Jinfa DU , Kaikai ZHU , Kai WANG , Jianyong LI , Chunxia ZHANG
IPC分类号: C07H19/16 , A61P31/18 , A61K31/7076 , A61K31/7068 , C07H19/06 , A61K31/683 , A61K31/505 , A61K31/5383 , A61K31/553 , A61K38/16 , A61K31/675
CPC分类号: C07H19/16 , A61K31/505 , A61K31/553 , A61K31/675 , A61K31/683 , A61K31/5383 , A61K31/7068 , A61K31/7076 , A61K38/162 , A61P31/18 , C07H19/06 , C07B2200/13
摘要: The present invention discloses a crystal form, a preparation method and an application of a 4′-substituted nucleoside compound I having the following structure, including salts, prodrugs, and compositions thereof. Animal pharmacokinetic studies demonstrated that the effective drug concentrations of Compound Ia and Compound Ig in HIV target cells, peripheral blood mononuclear cells (PBMC), were effective in inhibiting HIV replication after 7 and 5 days, respectively. Therefore, Compound I can be used as a long-acting drug for preventing and treating AIDS. R is selected from ethynyl, azide, and cyano groups, X is selected from hydrogen and fluorine, and B is selected from B1 and B2.
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