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54 results about "Sigma-1 receptor" patented technology
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The sigma-1 receptor (σ₁R), one of two sigma receptor subtypes, is a chaperone protein at the endoplasmic reticulum (ER) that modulates calcium signaling through the IP3 receptor. In humans, the σ₁ receptor is encoded by the SIGMAR1 gene.
Use of compounds binding to the sigma receptor for the treatment of diabetes-associated pain
The present invention refers to the use of compounds active on the sigma receptor for the production of a medicament for the treatment of diabetes-associated pain.
Owner:LAB DEL DR ESTEVE SA
Sigma receptor inhibitors
Owner:ESTEVE PHARMA SA
Sigma Receptor Inhibitors
The invention relates to compounds of formula (I) having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.
Owner:ESTEVE PHARMA SA
Use of Compounds Binding to the Sigma Receptor for the Treatment of Metabolic Syndrome
InactiveUS20090181976A1Organic active ingredientsMetabolism disorderSigma-1 receptorReceptor for activated C kinase 1
The present invention refers to the use of compounds binding to the sigma receptor for the treatment of metabolic syndrome.
Owner:LAB DEL DR ESTEVE SA
Sigma receptor inhibitors
The invention relates to compounds of formula (I) having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.
Owner:ESTEVE PHARMA SA
Sigma ligands for neuronal regeneration and functional recovery
InactiveUS20060052386A1Promote recoveryPromote regenerationOrganic active ingredientsNervous disorderHuntingtons choreaRisk stroke
The invention discloses methods and compositions useful for facilitating neuronal regeneration and functional recovery in neurodegenerative diseases. The methods and compositions utilize ligands for the sigma receptor, wherein the ligand is preferably AGY-94806, or salts, or solvates thereof. These molecules can be delivered alone or in combination with agents which treat or prevent neurodegenerative diseases such as those caused by ischemic stroke, diabetic peripheral neuropathy, cancer therapy induced neuropathy, multiple sclerosis, amyotrophic lateral sclerosis, traumatic brain injury, spinal cord injury, Huntington's disease or Parkinson's disease. In other methods, the sigma receptor ligands are administered after stroke to facilitate functional recovery. The administration of the sigma receptor ligands effects faster functional recovery.
Owner:MS SCI CORP
Non-human mutant mammals deficient in Sigma receptors and their applications
ActiveUS20050132429A1Preventing and reducing and alleviating side effectEliminate side effectsNervous disorderCell receptors/surface-antigens/surface-determinantsNervous systemControl animal
The genome of the non-human mutant mammal, deficient in an endogenous Sigma receptor, contains a mutation that comprises a disruption in an endogenous Sigma rteceptor gene, wherein said gene disruption gives rise to a mutant lacking detectable levels of endogenous Sigma receptor. The mutant may be used as a control animal for in vivo tests, as well as a source of cells that can be used in in vitro tests, Mutants deficient in the Sigma-1 receptor can be used as models for in vivo study of disorders of the central nervous system, memory alterations, stress conditions and drug addictions, analgesia processes and neuroprotection. Mutants deficient in the Sigma-2 receptor can be used to study diagnostic or therapeutic tools to fight cance and / or degenerative processes and / or to design compounds capable of preventing, reducing or alleviating the secondary pathology associated with administration of neuroleptic agents.
Owner:ESTEVE PHARMA SA
Sigma receptor inhibitors
Owner:ESTEVE PHARMA SA
Pyrazole derivatives as sigma receptor inhibitors
InactiveUS20090264442A1Reduction and increase and maintenanceBiocideNervous disorderDiseaseSigma-1 receptor
The invention relates to compounds of formula Ihaving pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.
Owner:LAB DEL DR ESTEVE SA
Sigma ligands for neuronal regeneration and functional recovery
InactiveUS20110152284A1Promote recoveryPromote regenerationBiocideNervous disorderHuntingtons choreaSigma-1 receptor
The invention discloses methods and compositions useful for facilitating neuronal regeneration and functional recovery in neurodegenerative diseases. The methods and compositions utilize ligands for the sigma receptor, wherein the ligand is preferable AGY-94806, or salts or solvates thereof. These molecules can be delivered alone or in combination with agents which treat or prevent neurodegenerative diseases such as those caused by ischemic stroke, multiple sclerosis, amyotrophic lateral sclerosis, traumatic brain injury, Huntington's disease, or Parkinson's disease. In other methods, the sigma receptor ligands are administered after stroke to facilitate functional recovery. The administration of the sigma receptor ligands effects functional recovery.
Owner:WIELOCH TADEUSZ +2
Methods and compositions utilizing an alternative splice variant of the sigma-1 receptor
InactiveUS7049425B2Cell receptors/surface-antigens/surface-determinantsSugar derivativesCancer cellSigma-1 receptor
A new variant of the sigma-1 (σ1)receptor is useful in screening compounds useful in the imaging and treatment of proliferative masses (i.e., tumors). This new variant, named sigma—1β (σ1β) finds particular use in the non-invasive diagnosis of cancer and more particularly in the diagnosis of proliferative cancer cells.
Owner:WAKE FOREST UNIV
Sigma ligands for neuronal regeneration and functional recovery
Owner:MS SCI CORP
Application of benzoazepine compounds in preparation of drugs for prevention or treatment of epilepsy
ActiveCN102895233AHas antiepileptic effectPrevent overactivationNervous disorderHeterocyclic compound active ingredientsBenzeneAntiepileptic drug
The present invention discloses an application of benzoazepine compounds, pharmaceutically acceptable salts or solvates thereof in preparation of drugs for prevention or treatment of epilepsy, wherein the benzazepine compound has the following general structural formula, an anti-epilepsy effect of the compounds is related to an allosterism activation sigma-1 receptor, and good treatment prospects of the compounds as full-novel anti-epilepsy drugs are showed.
Owner:SUZHOU UNIV +1
Sigma 1 receptor bound tricarbonyl cyclopentadiene ligand compound, and preparation method and application of ligand compound
InactiveCN103435655AHigh labeling rateHigh radiochemical purityRadioactive preparation carriersGroup 7/17 element organic compoundsRheniumTechnetium
The invention relates to a sigma 1 receptor bound tricarbonyl cyclopentadiene ligand compound, and a preparation method and an application of the ligand compound. A structural general formula of the ligand compound is shown as (I) as shown in the specification, wherein n is equal to 3 or 5, and M is rhenium or technetium-99m. The tricarbonyl cyclopentadiene ligand compound has high affinity and moderate selectivity to a sigma 1 receptor, and is an initially found sigma 1 receptor ligand with nanomolar affinity. After labeled by technetium-99m, the ligand compound has a higher labeling rate, high radiochemical purity and excellent biological properties, is applicable to an SPECT (single photon emission computed tomography) tracer, breaks through the low brain uptake bottleneck of a 99 mTc labeled sigma 1 receptor tracer, and has wide clinical application prospects.
Owner:BEIJING NORMAL UNIVERSITY
Sigma receptor inhibitors
The invention refers to compounds of general formula (I)having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.
Owner:ESTEVE PHARMA SA
Fluorine-18-labeled spiropiperidine sigma-1 receptor compound and its preparation method and use
InactiveCN102659796AHigh affinityHigh selectivityOrganic chemistryRadioactive preparation carriersBiological propertyImaging agent
The invention discloses a fluorine-18-labeled spiropiperidine sigma-1 receptor compound and its preparation method and use. The preparation method comprises synthesis of a receptor ligand Spiro-OCH3(R=OCH3), synthesis of a receptor ligand Spiro-PEG1-F, synthesis of a compound intermediate Spiro-OH, synthesis of a receptor ligand Spiro-PEG2-F, synthesis of a receptor ligand Spiro-PEG3-F, synthesis of a labelled precursor Spiro-PEGn(n=1)-OTs, synthesis of a labeled precursor Spiro-PEGn(n=3)-OTs and preparation of the fluorine-18-labelled spiropiperidine sigma-1 receptor compound. The fluorine-18-labelled spiropiperidine sigma-1 receptor compound has high affinity and selectivity to a sigma-1 receptor. Through fluorine-18 labeling, the fluorine-18-labelled spiropiperidine sigma-1 receptor compound has a high labeling rate, high radiochemical purity and excellent biological properties and can be widely used for preparation of a positron imaging agent.
Owner:BEIJING NORMAL UNIVERSITY
Method to identify ligands for sigma-1 receptors
InactiveUS20150010917A1Cell receptors/surface-antigens/surface-determinantsSugar derivativesCellular modelSigma-2 receptor
An assay for identifying ligands of the σ1 receptor based on a fusion protein comprising the σ1 receptor flanked by two fluorophores, so that said fluorophores are capable of producing constitutive FRET when no ligand is bound to the σ1 receptor. The fusion protein of the invention also allows the simultaneous determination whether the newly determined ligand is an agonist or an antagonist. Said fusion protein has been expressed in a cell, giving rise to a new cellular model useful for identifying σ1 receptor ligands, and additionally for discriminating between agonists and antagonists.
Owner:LAB DEL DR ESTEVE SA
Sigma receptor stimulant polypeptide and application
InactiveCN106366165AElevated BDNF contentReduce forced swim timePeptide-nucleic acidsNervous disorderStimulantBrain-derived neurotrophic factor
The invention relates to the field of medicine, in particular to polypeptide with the effects of stimulating a Sigma-1 receptor, up-regulating the brain-derived neurotrophic factor level and relieving the depressive symptom. The sequence of the polypeptide is a brand-new sequence, and the polypeptide has the advantage of being capable of increasing the BDNF content in chronic unpredictable stress model rat brain tissue. The pharmacological result shows that the polypeptide can relieve the depressive symptom of acute and chronic depression model animals. The polypeptide can serve as an effective candidate treatment method for clinical depression and has potential new medicine development value.
Owner:SUZHOU PULUODA BIOLOGICAL SCI & TECH
INHIBITORS OF THE INTERACTION OF THE SIGMA-1 RECEPTOR WITH hERG FOR USE IN THE TREATMENT OF CANCER
InactiveUS20130317226A1Modulate the maturation and the membrane stability of hERGNervous disorderOrganic chemistryMedicineSigma-1 receptor
The present invention relates to the use of the Sigma-1 receptor (Sig1R) in the context of the post-transcriptional regulation of the membrane expression of ion channels.The present invention can be used in the field of the treatment of diseases involving ion channels. These are, for example, nervous system diseases, neurodegenerative diseases, heart diseases, and cancer.
Owner:CENT NAT DE LA RECHERCHE SCI +1
Sigma-1 receptor ligand with acetylcholinesterase
Owner:SAMARITAN PHARMA +1
Sigma-1 receptor ligands and methods of use
The invention provides compounds of formula I and compositions thereof. The invention further provides methods of using the compounds and compositions. The compounds of the invention can provide high affinity binding to sigma-1 receptors in a mammal. The compounds can exhibit selectivity for the sigma-1 receptor over the sigma-2 receptor. The compounds and compositions of the invention can also be used to treat conditions that involve the sigma-1 receptor, such as addiction, cardiovascular conditions, and cancer, for example, cancer of the breast, lung, prostate, ovarian, colorectal, or the CNS.
Owner:WISCONSIN ALUMNI RES FOUND
Novel thiazole derivative or salt, isomer, preparation method and application thereof
ActiveCN112341404AHas an analgesic effectExtended half-lifeOrganic active ingredientsNervous disorderAntagonismEthylic acid
The invention discloses a novel thiazole derivative or salt, an isomer, a preparation method and application thereof. A compound shown as a formula (I) has a Sigma 1 receptor antagonism effect, and has strong in vitro affinity to sigma 1R in the aspect of in vitro receptor affinity. Meanwhile, in D2L radioactive ligand binding analysis and 5HT-1A receptor, CB1 receptor and CB2 receptor cAMP tests,the affinity to the receptors is poor, and high receptor selectivity is shown. Mouse acetic acid twisting tests show that the compound has an analgesic effect. Through rat oral administration pharmacokinetic experiments, it can be known that the compound is long in half-life period, low in clearance rate and large in AUClast; Cmax can be quickly reached after oral administration, and the compoundis extremely quick to absorb and suitable for medicine.
Owner:CHENGDU EASTON BIOPHARMACEUTICALS CO LTD
Gabapentinoids and sigma receptor ligands combinations
InactiveUS20160310501A1EffectiveReduced dosOrganic active ingredientsNervous disorderGabapentinoidSigma-2 receptor
The invention refers to a synergistic combination comprising a Sigma ligand of general formula (I), and a Gabapentinoid, a medicament comprising said active substance combination, and the use of said active substance combination for the manufacture of a medicament, particularly for the prophylaxis and / or treatment of pain.
Owner:ESTEVE PHARMA SA
Use of compounds active on the sigma receptor for the treatment of mecanical allodynia
The present invention refert to the use of compounds active on the sigma receptor for the treatment of mechanical allodynia.
Owner:LAB DEL DR ESTEVE SA
Serotonin-norepinephrine reuptake inhibitors (SNRIS) and sigma receptor ligands combinations
InactiveUS20160310500A1Not show side effectNot improveOrganic active ingredientsNervous disorderNorepinephrine reuptake inhibitorAdrenergic
The invention refers to a synergistic combination comprising a Sigma ligand of general formula (I), and a Serotonin-Norepinephrine Reuptake Inhibitor (SNRI), a medicament comprising said active substance combination, and the use of said active substance combination for the manufacture of a medicament, particularly for the prophylaxis and / or treatment of pain.
Owner:LAB DEL DR ESTEVE SA
Enantiomers Of Tetrahydro-N,N-Dimethyl-2,2-Diphenyl-3-Furanmethanamine (Anavex2-73) And Use Thereof In The Treatment Of Alzheimer's Disease And Other Disorders Modulated By The Sigma 1 Receptor
Owner:ANAVEX LIFE SCI CORP
Novel use of sigma-1 receptor agonist compounds
ActiveUS20190209575A1Reduce in quantityPromote degradationAmine active ingredientsDiseaseSigma-1 receptor
Compositions and methods for the prevention, inhibition, and / or treatment of progressive fibrosis present in various fibroproliferative disorders. Embodiments relate to the use of Sigma-1 receptor agonists for use in the treatment of prevention of progressive fibrosis characterized by the over proliferation of ECM producing cells, e.g. myofibroblasts and by the excessive deposition of ECM components in a medical or disease condition. Preferred Sigma-1 agonists are disclosed.
Owner:SIGMADRUGS KFT
Tetrahydroxy furfuryl piperazine compound bonded with sigma-1 receptor and preparation method and application of compound
ActiveCN106220590ASuitable affinitySuitable selectivityIsotope introduction to heterocyclic compoundsRadioactive preparation carriersBiological propertyBenzaldehyde
The invention provides a tetrahydroxy furfuryl piperazine compound bonded with a sigma-1 receptor and a preparation method and application of the compound. The structural formula of the compound is shown as the formula (I) (please see the formula I in the description), wherein R is F, 18F, I or OCH2CH2F. The ligand compound of the tetrahydroxy furfuryl piperazine sigma-1 receptor has proper affinity and selectivity for the sigma-1 receptor and is one of few sigma-1 receptor ligands with nanomole-scale affinity and low fat solubility. When the R group in the compound of the formula (I) is 18F, 18 F is marked in two steps through p-fluorine[18F]benzaldehyde. The compound has high marking rate, high radiochemical purity and excellent biological property, can be applied to a PET developing tracer agent, and has wide clinical application prospects.
Owner:BEIJING NORMAL UNIVERSITY
Substituted pyrazolo[1,5-a]pyridines, their preparation and use as medicaments
ActiveUS20150031678A1Effective of painEffective treatmentBiocideSenses disorderSigma-1 receptorPyridine
![Substituted pyrazolo[1,5-a]pyridines, their preparation and use as medicaments](https://images-eureka.patsnap.com/patent_img/dd372ad6-dcc2-4d25-b3c8-b6519b9b77e1/US20150031678A1-20150129-C00001.PNG "Substituted pyrazolo[1,5-a]pyridines, their preparation and use as medicaments")
![Substituted pyrazolo[1,5-a]pyridines, their preparation and use as medicaments](https://images-eureka.patsnap.com/patent_img/dd372ad6-dcc2-4d25-b3c8-b6519b9b77e1/US20150031678A1-20150129-C00002.PNG "Substituted pyrazolo[1,5-a]pyridines, their preparation and use as medicaments")
![Substituted pyrazolo[1,5-a]pyridines, their preparation and use as medicaments](https://images-eureka.patsnap.com/patent_img/dd372ad6-dcc2-4d25-b3c8-b6519b9b77e1/US20150031678A1-20150129-C00003.PNG "Substituted pyrazolo[1,5-a]pyridines, their preparation and use as medicaments")
Owner:ESTEVE PHARMA SA
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