20 results about "Pipequaline" patented technology

The invention discloses application of a thiophene pyrimidone derivative in preparation of a medicine for treating Alzheimer's disease, and belongs to the technical field of medicines, and the thiophene pyrimidone derivative is 2-[(4-methylpiperidine-1-yl) methyl]-3-(tetrahydrofuran-2-yl methyl)-5-(thiophene-2-yl) thieno [2, 3-d] pyrimidine-4-ketone. According to the application of the thiophene pyrimidinone derivative in preparation of the medicine for treating the Alzheimer's disease, 2-[(4-methylpiperidine-1-yl) methyl]-3-(tetrahydrofuran-2-yl methyl)-5-(thiophen-2-yl) thieno [2, 3-d] pyrimidin-4-one has an efficient inhibition effect on BChE, can remarkably improve the cognitive function defect of an AD model, and can be used for preparing the medicine for treating the Alzheimer's disease. A novel efficient BChE targeting candidate inhibitor is provided for the field of AD treatment.

Disclosed herein are combinations comprising an GLP-1R agonist and an inhibitor of menin. Also described are combinations of specific GLP-1R agonists and irreversible inhibitors or reversible inhibitors of menin. Also described are methods of using the combinations for the treatment of diabetes, obesity and overweight condition.

Provided herein are methods of using 2-(2,6-dioxopiperidin-3yl)-4-(2-fluoro-4-(3-morpholinoazetidin-1-yl)methyl)benzyl)amino)isoindoline-1,3-dione, or an enantiometer, a mixture of enantiomers, a tautomer, an isotopolog, or a pharmaceutically acceptable salt thereof, alone or in combination with obinutuzumab, for treating, preventing or managing chronic lymphocytic leukemia / small lymphocytic lymphoma.

A system comprising pipemidic acid-1,3,4-thiadiazole hybrid derivatives with a thiadiazole group at position C-6 of the pipemidic acid skeleton, synthesized and structurally determined by IR-, 1 H-NMR-, 13 Confirmed by C-NMR and mass spectrometry.

The invention relates to a benzopiperidine biquaternary ammonium salt compound and application thereof in medicine, in particular to a compound shown in a general formula (I) or a stereoisomer, a racemate, a tautomer, pharmaceutically acceptable salt, an intermediate and a pharmaceutical composition of the compound, and application of the compound in preparation of neuromuscular blocking drugs.

The present invention relates to homopiperazinyl and homopiperidinyl quinazolin-4(3H)-one derivatives having dual pharmacological activity towards both the α2δ subunit of the voltage-gated calcium channel and the sigma-1 (σ1) receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.

The new compound 3-(1-(2,3-dichloro-4-methoxyphenyl) ethyl)-1-methyl-l-(l,3,3-trimethylpiperidin-4-yl)urea monohydrochloride salt has a high capability to permeate through the blood-brain barrier and to display, at central nervous system level, a consistent ghrelin agonist activity; the compound is effective in the treatment and / or prevention of a medical condition mediated by the ghrelin receptor in the central nervous system. In particular, in experimental tests, the compound has shown high efficacy in the treatment of neurotoxic damage, with a useful combined pattern of neuroprotective effects both at central and peripheral level. The compound is further useful in the treatment of conditions which require a reduction of the heart rate. The compound is pharmacologically active at low to moderate doses, thus showing a favourable therapeutic index.

This invention relates to the field of pharmaceutical technology, specifically to a 6-(6-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)quinazoline-4-amine derivative, its preparation method, and its applications. This invention utilizes a "conformation-locking" and "drug-likeness optimization" strategy to optimize the 4-position side chain of quinazoline into conformationally defined structures such as dihydroindanol and fluoropiperidine, thereby reducing P-gp recognition through conformational rigidity. Simultaneously, the introduction of groups such as cyclopropylformyl groups reduces off-target toxicity, thus broadening the therapeutic window. The 6-(1H-pyrrolo[2,3-b]pyridin-3-yl)quinazoline-4-amine derivative provided by this invention simultaneously achieves potent DYRK1A inhibition, high kinase selectivity, low microglial cytotoxicity, significant anti-neuroinflammatory effects, good blood-brain barrier permeability, and oral bioavailability. Furthermore, it is a novel small-molecule inhibitor that can be validated for cognitive improvement in AD animal models, possessing significant clinical value and urgent application needs.

The invention discloses an N-(3 / 4-((6-substituted pyrimidine-4-yl) amino) phenyl) amide derivative and application thereof, and belongs to the field of medical chemistry. The structural formula of the compound is as follows: R1 is 4-methyl-1H-imidazole-1-group, 3-methyl-1H-pyrazole-1-group or 4-methyl-1H-pyrazole-1-group, R2 is 4-methyl-1H-imidazole-1-group, and R3 is 3-methyl-1H-pyrazole-1-group; r2 is a linear alkyl group, a cycloalkyl group, a 1-methylpiperidine-4-group, a morpholinyl ethyl group, a substituted or unsubstituted phenyl group, a substituted or unsubstituted styryl group, a substituted or unsubstituted phenethyl group, a phenylpropyl group, a phenylbutenyl group, a 6-bromo-pyridine-2-group, a (benzo [d] [1, 3] dioxol-5-group) vinyl group or a (thiophene-2-group) methyl group. The invention relates to a novel Nur77 targeted giant vesicle type death inducer which is suitable for single-drug treatment of lung cancer or is combined with other targeted / immune / chemotherapeutic drugs to improve the curative effect and reduce the drug resistance risk. And the Nur77 can be expanded to breast cancer, liver cancer and other Nur77 related tumors.

The present invention belongs to the field of biopharmaceuticals and provides a κ-opioid receptor agonist having the following formula, its stereoisomers, and pharmaceutically acceptable salts thereof. The κ-opioid receptor agonist has high selectivity for the κ-opioid receptor, its activity is 3 to 15 times that of diferikephalin, and has high pharmacological activity, and can be used for the treatment, prevention and / or remission of pruritus, and / or analgesia. D-Phe-AA1-AA2-D-Lys-4-aminopiperidine-4-carboxamide-AA3-AA4-AA5 [Formula I].

This invention belongs to the field of drug development technology, specifically relating to the application of 1-((4-cyclohexylphenyl)sulfonyl)-N-(4-fluorobenzyl)-4-methylpiperidine-4-carboxamide in the preparation of drugs for treating nervous system diseases. The purpose of this invention is to provide a drug with low toxicity and side effects that can target SLC11A2 to treat or improve nerve cell damage. The technical solution of this invention is the application of 1-((4-cyclohexylphenyl)sulfonyl)-N-(4-fluorobenzyl)-4-methylpiperidine-4-carboxamide in the preparation of drugs for treating nervous system diseases. This invention demonstrates that the compound 1-((4-cyclohexylphenyl)sulfonyl)-N-(4-fluorobenzyl)-4-methylpiperidine-4-carboxamide has low toxicity and side effects, and can protect or improve nerve cell damage by targeting SLC11A2; providing a new option for preparing drugs to treat or improve nerve cell damage.

The present invention addresses the problem of providing: a mutant L-pipecolic acid hydroxylase for producing cis-5-hydroxy-L-pipecolic acid in a highly productive and highly selective manner by hydrating L-pipecolic acid; and a novel method for industrially producing cis-5-hydroxy-L-pipecolic acid from L-pipecolic acid in a highly productive and low-cost manner. The present invention provides a mutant L-pipecolic acid hydroxylase that has an amino acid sequence in which a specific amino acid mutation is introduced in the amino acid sequence represented by SEQ ID NO: 2.

The novel compound 3-(1-(2,3-dichloro-4-methoxyphenyl)ethyl)-1-methyl-1-(1,3,3-trimethylpiperidin-4-yl)urea monohydrochloride has high permeability, is able to cross the blood-brain barrier and shows consistent ghrelin agonist activity at the level of the central nervous system; the compound is effective in the treatment and / or prevention of medical conditions mediated by ghrelin receptors in the central nervous system. In particular, in experimental tests, the compound shows high efficacy in the treatment of neurotoxic injuries and has an effective neuroprotective action combination pattern at both central and peripheral levels. The compound is also useful in the treatment of diseases requiring a reduction in heart rate. The compound has pharmacological activity at low to moderate doses, thus showing a good therapeutic index.

Provided herein are methods of using (S)-2-(2,6-dioxopiperidin-3-yl)-4-((2-fluoro-4-((3-morpholinoazetidin-1-yl)methyl)benzyl)amino)isoindoline-1,3-dione, or an enantiomer, mixture of enantiomers, tautomer, isotopolog, or pharmaceutically acceptable salt thereof, in combination with a second active agent for treating, preventing or managing hematological malignancies. The second active agent is one or more of an HDAC inhibitor, a BCL2 inhibitor, a BTK inhibitor, an mTOR inhibitor, a PI3K inhibitor, a PKCβ inhibitor, a SYK inhibitor, a JAK2 inhibitor, an Aurora kinase inhibitor, an EZH2 inhibitor, a BET inhibitor, a hypomethylating agent, a DOT1L inhibitor, a HAT inhibitor, a WDR5 inhibitor, a DNMT1 inhibitor, an LSD-1 inhibitor, a G9A inhibitor, a PRMT5 inhibitor, a BRD inhibitor, a SUV420H1 / H2 inhibitor, a CARM1 inhibitor, a PLK1 inhibitor, an NEK2 inhibitor, an MEK inhibitor, a PHF19 inhibitor, a PIM inhibitor, an IGF-1R inhibitor, an XPO1 inhibitor, a BIRC5 inhibitor, or a chemotherapy.

A method of treatment of mental disorder of a subject includes the steps of: normalizing an expression of both DRD1 and DRD5, which belong to DRD1-like family, of the subject to a preset standard level. The DRD1 / 5 level and expression can be increased or decreased bidirectionally by targeting an upstream promoter sequence of DRD1 / 5. The promoter activity of DRD1 / 5 can be attenuated by using an antipsychotic which directly targets the DRD1 / 5 promoter. The antipsychotics being used are typical and / or atypical antipsychotic medications such as Haloperidol,Risperidone, Clozapine and Cariprazine. The treatment is also useful for the subject with an impaired constitutive expression of DRD1 / 5 gene. The method can be used to treat schizophrenia, autism, depression, mania and bipolar disorders by normalizing the DRD1 / 5 expression level. The promoter gene sequencing of DRD1 and / or DRD5 can also be used for quantitative mental health screening through comparing with a standard sequence database.

The application discloses application of a thienopyrimidinone derivative in preparation of a drug for treating Alzheimer's disease, belongs to the technical field of medicines, and the thienopyrimidinone derivative is 2-[(4-methylpiperidin-1-yl)methyl]-3-(tetrahydrofuran-2-ylmethyl)-5-(thiophen-2-yl)thieno[2,3-d]pyrimidin-4-one. The application adopts the above-mentioned application of the thienopyrimidinone derivative in preparation of the drug for treating Alzheimer's disease, 2-[(4-methylpiperidin-1-yl)methyl]-3-(tetrahydrofuran-2-ylmethyl)-5-(thiophen-2-yl)thieno[2,3-d]pyrimidin-4-one has a high inhibition effect on BChE, and can significantly improve cognitive function defects of an AD model, thereby providing a new high-efficiency BChE target candidate inhibitor for the AD treatment field.

The present invention describes methods of treating Huntington's disease in a subject in need thereof. The method comprising administrating to the subject in need thereof a therapeutically effective amount of 2-[3-(2,2,6,6-tetramethylpiperidin-4-yl)-3H-[1,2,3]triazolo[4,5-c]pyridazin-6-yl]-5-(2H-1,2,3-triazol-2-yl)phenol or a pharmaceutically acceptable salt thereof.

The application provides a sorafenib derivative, a preparation method and application thereof, and a medicine, and relates to the technical field of pharmacy. 2 The boron atom sp of the sorafenib derivative provided by the application has a broad-spectrum cytotoxicity on tumor cells, and the cytotoxicity on human normal L02 cells is low.