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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:US12128013B2
公开(公告)日:2024-10-29
申请号:US18236795
申请日:2023-08-22
发明人: Todd Brady , Scott Young , William A. Kinney , Kenneth J. Mandell
IPC分类号: A61K31/137 , A61K8/41 , A61K8/44 , A61K8/49 , A61K31/13 , A61K31/197 , A61K31/423 , A61K31/435 , A61K31/438 , A61K31/47 , A61Q19/00 , A61Q19/08 , C08K5/04 , C08K5/08 , C08K5/18
CPC分类号: A61K31/137 , A61K8/41 , A61K8/44 , A61K8/49 , A61K8/4926 , A61K31/13 , A61K31/197 , A61K31/423 , A61K31/435 , A61K31/438 , A61K31/47 , A61Q19/00 , A61Q19/08 , C08K5/04 , C08K5/08 , C08K5/18
摘要: The present invention provides for the treatment, prevention, and/or reduction of a risk of a disease, disorder, or condition in which aldehyde toxicity is implicated in the pathogenesis, including ocular disorders, skin disorders, conditions associated with injurious effects from blister agents, and autoimmune, inflammatory, neurological and cardiovascular diseases by the use of a primary amine to scavenge toxic aldehydes, such as MDA and HNE.
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公开(公告)号:US20240350479A1
公开(公告)日:2024-10-24
申请号:US18436555
申请日:2024-02-08
申请人: Purdue Pharma L.P.
发明人: Michele Hummel , Donald J. Kyle , Garth Whiteside
IPC分类号: A61K31/485 , A61K9/00 , A61K9/16 , A61K9/24 , A61K9/70 , A61K31/05 , A61K31/135 , A61K31/137 , A61K31/445 , A61K31/4468 , A61K31/451 , A61K31/4748 , A61K38/07
CPC分类号: A61K31/485 , A61K31/135 , A61K31/137 , A61K31/4468 , A61K31/451 , A61K31/4748 , A61K38/07 , A61K9/0019 , A61K9/167 , A61K9/209 , A61K9/7023 , A61K31/05 , A61K31/445
摘要: Disclosed in certain embodiments is a method of treating or preventing an opioid-induced adverse pharmacodynamic response comprising administering to a patient in need thereof an effective amount of buprenorphine.
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公开(公告)号:US20240335400A1
公开(公告)日:2024-10-10
申请号:US18289326
申请日:2022-05-04
发明人: Estelle BEGUIN , Patricia QUARTON , Jeffrey KATSTRA , David ALTREUTER , Juan Jaramillo MONTEZCO , Manjeet PIMPARADE
IPC分类号: A61K31/137 , A61K9/00 , A61K47/34
CPC分类号: A61K31/137 , A61K9/0065 , A61K47/34
摘要: Provided are gastric residence systems comprising at least one drug-eluting component comprising methadone or a salt thereof, 35-50 wt % polycaprolactone, and 0.5-3 wt % poloxamer, and a rate-modulating release film coating the at least one co-extruded drug eluting component. The gastric residence systems comprising at least one drug-eluting component are configured to be maintained within a stomach of a human body for at least 48 hours and to release methadone for at least 48 hours, such that the at least one drug eluting component with the rate-modulating release film is configured to release at least 10% of the methadone or the salt thereof after the first 24 hours of residence within the stomach.
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公开(公告)号:US12109204B2
公开(公告)日:2024-10-08
申请号:US16972184
申请日:2019-06-05
发明人: Rachelle H. Crosbie , Cynthia Shu
IPC分类号: A61K31/4439 , A61K31/137 , A61K31/40 , A61K31/404 , A61K31/427 , A61K31/439 , A61K31/4418 , A61K31/4422 , A61K31/498 , A61K31/522 , A61K31/525 , A61K31/565 , A61K31/7076 , A61P21/06
CPC分类号: A61K31/4439 , A61K31/137 , A61K31/40 , A61K31/404 , A61K31/427 , A61K31/439 , A61K31/4418 , A61K31/4422 , A61K31/498 , A61K31/522 , A61K31/525 , A61K31/565 , A61K31/7076 , A61P21/06
摘要: Provided herein are methods for treating and preventing a disease related to diminution or dysfunction of a dystrophin-related complex in a subject in need thereof, comprising administering to the subject a compound that increases sarcospan. Also provided herein are pharmaceutical compositions comprising a compound that increases sarcospan, or a pharmaceutically acceptable salt or ester thereof, useful for the treatments described herein.
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公开(公告)号:US20240325380A1
公开(公告)日:2024-10-03
申请号:US18741475
申请日:2024-06-12
申请人: TMTRx, Inc.
发明人: Phillip R. Torralva
IPC分类号: A61K31/485 , A61K31/137 , A61K31/18 , A61K31/225 , A61K31/40 , A61K31/4166 , A61K31/4178 , A61K31/454 , A61K31/46 , A61K31/517 , A61K31/5377 , A61K31/5517 , A61P25/36
CPC分类号: A61K31/485 , A61K31/137 , A61K31/18 , A61K31/225 , A61K31/40 , A61K31/4166 , A61K31/4178 , A61K31/454 , A61K31/46 , A61K31/517 , A61K31/5377 , A61K31/5517 , A61P25/36
摘要: Compositions are provided including a Mu opioid receptor antagonist, and an α2-adrenergic receptor agonist; or an α1 adrenergic receptor antagonist, together with one or more of a mu (or opioid receptor subtype) antagonist or agonist, (2) a vasopressor, (3) an anticholinergic agent and/or cholinergic agents, (4) a combined alpha-1 adrenergic antagonist and anticholinergic, (5) a paralytic or muscle relaxant, (6) a respiratory accelerant, (7) a GABA complex antagonist, (8) an anti-seizure/membrane stabilizer agent, (9) an α1 adrenergic receptor agonist, and/or (10) an α2 adrenergic receptor agonist; and a pharmaceutically acceptable carrier. Also provided are methods of preventing or reversing effects in a subject (including muscle and chest wall rigidity, laryngospasm, WCS, and/or respiratory depression) arising from intentional or accidental opioid or opiate exposure.
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公开(公告)号:US20240315989A1
公开(公告)日:2024-09-26
申请号:US17698361
申请日:2022-03-18
发明人: Angela M. Reiersen , Eric Lenze
IPC分类号: A61K31/137 , A61P31/00
CPC分类号: A61K31/137 , A61P31/00
摘要: Among the various aspects of the present disclosure is the provision of methods of treating or preventing COVID-19 or effects thereof in a subject comprising: administering a therapeutically effective amount of a pharmaceutical agent comprising one or more of a sigma-1 receptor (S1R) agonist or antagonist, a cationic amphiphilic drug, a selective serotonin reuptake inhibitor (SSRI), or functional inhibitor of acid sphingomyelinase (FIASMA), such as fluvoxamine.
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8.
公开(公告)号:US20240315988A1
公开(公告)日:2024-09-26
申请号:US18385468
申请日:2023-10-31
发明人: Marino Nebuloni , Patrizia Colombo
IPC分类号: A61K31/135 , A61K9/14 , A61K9/16 , A61K31/047 , A61K31/137 , A61K31/55 , A61K47/02 , A61K47/10 , A61K47/12 , A61K47/26
CPC分类号: A61K31/135 , A61K9/145 , A61K9/1623 , A61K9/1688 , A61K9/1694 , A61K31/047 , A61K31/137 , A61K47/02 , A61K47/10 , A61K47/12 , A61K47/26 , A61K31/55
摘要: The present invention relates to pharmaceutical compositions and methods of manufacturing the same, comprising a eutectic of Cyclobenzaprine HCl and mannitol or Amitriptyline HCl and mannitol.
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公开(公告)号:US12097170B2
公开(公告)日:2024-09-24
申请号:US17249642
申请日:2021-03-08
发明人: Steven M. Cope , Allan E. Titus
CPC分类号: A61K31/137 , A61J1/10 , A61J1/1468 , A61M5/002 , B65D75/28 , B65D81/266 , A61J1/14 , A61J1/1475 , A61M1/14 , A61M5/14
摘要: A packaged, sealed container system for stable storage of a formulation of an oxygen-sensitive pharmaceutical compound, the packaged, sealed container system comprising a primary container including therein a formulation of an oxygen-sensitive pharmaceutical compound, a secondary outer container comprising a first flexible sheet layer, an opposing second flexible sheet layer, and a seal disposed along a common peripheral edge of the first and second flexible sheet layers, such that the primary container is disposed between and enclosed by the first and second flexible sheet layers of the secondary outer container. An oxygen scavenger is also disposed between and enclosed by the first and second flexible sheet layers of the secondary outer container. The oxygen scavenger is in fluid communication with the contents of the primary container.
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公开(公告)号:US12090246B2
公开(公告)日:2024-09-17
申请号:US17064390
申请日:2020-10-06
IPC分类号: A61L24/10 , A61K31/137 , A61L15/32 , A61L24/00 , A61L31/04
CPC分类号: A61L24/104 , A61K31/137 , A61L24/001 , A61L24/0015 , A61L24/0031 , A61L2300/104 , A61L2300/404 , A61L2300/418 , A61L2400/04
摘要: The present invention provides an improved tissue adhesive to repair defects in soft tissue. Following ASTM standard tests, crosslinked methacryloyl-substituted gelatin hydrogels of the present invention (GelSEAL) were shown to exhibit adhesive properties, i.e. wound closure strength, shear resistance and burst pressure, that were superior to clinically used fibrin- and poly(ethylene glycol)-based glues. Chronic in vivo experiments in rats proved GelSEAL to effectively seal large lung leakages without additional sutures or staples, presenting improved performance as compared to fibrin and poly(ethylene glycol) glues. Furthermore, subcutaneous implantation in rats revealed high biocompatibility of GelSEAL as evidenced by low inflammatory host response. Advantageously, the tissue adhesives of the present invention are low cost and easy to produce, making them a promising substance to be used as a sealant for fluid leakages in soft tissue, as well as an easily tunable platform to further optimize the adhesive characteristics.
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