53 results about "Sigma-1 receptor" patented technology

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.

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.

The present invention refers to the use of compounds binding to the sigma receptor for the treatment of metabolic syndrome.

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.

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.

The invention relates to compounds of formula I

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.

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.

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.

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.

A novel compound and method for preventing or treating neurodegenerative diseases by inhibiting acetylcholinesterase and binding the sigma-1 receptor are disclosed. Dimethylcarbamic acid 2,3-bis-dimethylcarbamoyloxy-6-[4-(4-ethyl-piperazin-yl)-butyryl]-phenyl ester and its derivatives represent a novel therapeutic strategy against beta-amyloid peptide induced neurotoxicity, in inhibiting acetylcholinesterase, in improving cholinergic transmission, in binding the sigma-l receptor, and in releasing a metabolite that is active both as a sigma-1 receptor ligand and an antioxidant.

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.

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.

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.

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.

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.

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.

The present invention relates to new substituted pyrazolo[1,5-a]pyridine having a great affinity for sigma receptors, especially sigma-1 receptor, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments.