52 results about "Piperidine derivative" patented technology

The invention relates to the field of medicinal chemistry, and particularly discloses a piperidine derivative as well as a pharmaceutical composition, application and a preparation method thereof. The piperidine derivative has the following general formula. The piperidine derivative can be effectively used for treating or preventing multiple sclerosis, and shows an unexpected synergistic effect in an animal model: the piperidine derivative not only can significantly improve neurological function impairment and promote recovery, but also can deeply reduce the levels of key proinflammatory cytokines IFN-gamma and IL-17 at the same time. The invention provides a novel small molecule candidate drug with central permeability, neuroprotection and comprehensive immune regulation functions for treatment of multiple sclerosis.

Disclosed are methods of treating cavernous angiomas including cavernous angiomas with symptomatic hemorrhage with a 4-substituted piperidine derivative. Also disclosed are methods wherein administering the therapeutically effective amount of a 4-substituted piperidine derivative results in a Cmax of between about 3 ng / ml and about 60 ng / ml; and wherein a Tmax is achieved of between about 0.5 hours and about 1 hour of administering of a 4-substituted piperidine derivative.

The invention relates to the technical field of organic synthesis, and relates to a synthesis method of an N-substituted piperidine / homopiperidine derivative and a prepared product, and the synthesis method comprises the following steps: in the presence of a catalyst and a solvent, dialdehyde, primary amine and hydrogen react to obtain the N-substituted piperidine / homopiperidine derivative; the catalyst comprises a carrier and an active component loaded on the carrier, and the active component of the catalyst is selected from at least one of Pd, Pt, Ru, Ni and Co. The method has the advantages of mild reaction conditions, high conversion rate of the raw material dialdehyde and high selectivity of the products piperidine and the homopiperidine derivative, and is a process route with important practical application value.

This application relates to the field of medicinal chemistry, specifically disclosing a piperidine derivative, a pharmaceutical composition, its uses, and a method for preparation. The piperidine derivative has the structure of general formula (I). This piperidine derivative can significantly improve the learning and memory abilities of Aβ-induced Alzheimer's disease model rats and effectively reduce acetylcholinesterase activity in brain tissue, providing a potential candidate for the development of novel Alzheimer's disease treatments.

The present invention relates to a pharmaceutical composition comprising an aryl piperidine derivative compound or a pharmaceutically acceptable salt thereof for use in the treatment or prevention of tankyrase-related cancer diseases. The pharmaceutical composition inhibits the enzymatic activity of tankyrase (TNKS), inhibits the expression of a beta-catenin target gene and the protein expression of active beta-catenin, stabilizes AXIN2 protein levels, and exhibits anti-cancer activity in a cancer cell line, so that the compound can be used as an anti-cancer agent, in particular as an anti-cancer agent. And elicits synergistic effects in combination therapy with other anti-cancer agents.

The present invention relates to the field of pharmacy, and in particular to compounds of formula (I) as pharmaceutically active compounds. Compounds of formula (I) have been proven for the first time to be particularly useful for the treatment of depression and eating disorders related to depression, or diseases with depressive pathology as well as for the treatment of appetite related side effects of antidepressants and antipsychotics.

The invention relates to an application of pimozide in preparation of a population effect inhibitor. The invention verifies that pimozide can inhibit the population effect of bacteria through a violaceum violaceum luminescence method, and further proves that pimozide can inhibit the population effect of pseudomonas aeruginosa and the generation of virulence factors through the inhibition of biological back membrane formation and the inhibition effect of virulence factor generation. The compound is expected to be developed into a clinically available group effect inhibitor, and has an important research value for solving the problems of bacterial infection and drug resistance.

Disclosed in the present invention are a cyclohexyl-substituted piperidine derivative, a pharmaceutical composition comprising same, and a use thereof. The cyclohexyl-substituted piperidine derivative is a compound as represented by general formula (I), a stereoisomer thereof or a pharmaceutically acceptable salt thereof. The definition of substituents in general formula (I) is stated in detail in the description. The compound and the composition of the present invention can be used for treating a variety of diseases or disorders associated with an NOP receptor.

The present invention relates to a piperidine derivative compound and a use thereof. The piperidine derivative compound of the present invention exhibits excellent inhibitory activity against FLT3, and thus can be usefully employed in the treatment or prevention of FLT3-related diseases.

A composition containing silicon nanoparticles having a hindered piperidine derivative free radical scavenger on the surface of the silicon nanoparticles. A process for preparing silicon nanoparticles having a hindered piperidine derivative radical scavenger on the surface of the silicon nanoparticles, the process comprising producing silicon nanoparticles using a VHFLPP process that collects the silicon nanoparticles in a trapping fluid when preparing the silicon nanoparticles, and wherein a hindered piperidine derivative free radical scavenger is provided in the trap fluid before, during and / or after collecting the silicon nanoparticles such that the silicon nanoparticles and the hindered piperidine derivative free radical scavenger are present together in the trap fluid.

Novel 1,4-disubstituted piperidine derivatives, a method of synthesizing said compounds, a pharmaceutical composition comprising said compounds and a suitable carrier, and a method of using the compounds. The 1,4-disubstituted piperidine derivatives compounds, identified as PDE5 inhibitors, are useful for the treatment of erectile dysfunction.

The present invention relates to aromatic heterocyclic cyclohexylaminoalkylpiperidine derivatives, methods for their preparation and their use. Specifically, the present invention relates to 5-HT 1A The present invention provides a compound represented by general formula (I), a stereoisomer thereof, a tautomer thereof, or a pharmaceutically acceptable salt thereof, which is used for activating receptors and dopamine D2 and D3 receptor activity, and for use in the manufacture of a medicament for Parkinson's disease, as well as a method for producing the compound. [Formula 1] JPEG2025526807000132.jpg2058

The application discloses a hindered amine polymer material and a preparation method and application thereof. The hindered amine polymer material is a modified polyester prepared through copolymerization of an oligomer polyester and a piperidine derivative, wherein the oligomer polyester is an oligomer PBT or an oligomer PET; or, the hindered amine polymer material is prepared through copolymerization of an oligomer polymer, wherein the oligomer polymer is prepared through polycondensation of terephthalic acid or dimethyl terephthalate, a diol and a piperidine derivative, wherein the diol is 1,4-butanediol or ethylene glycol; and the piperidine derivative has a structure shown in formula I or formula II. Compared with a conventional physically mixed polymer material, the weather resistance and migration resistance of the polymer material prepared through copolymerization are significantly improved.

This invention discloses an anti-diffusion agent for PCB glass substrates, its preparation method, and its application, relating to the field of printed circuit board manufacturing technology. The anti-diffusion agent comprises the following components in mass concentrations: 0.5-2.5% surface enhancer, 0.5-2.5% bonding agent, 1.0-3.0% wetting agent, 0.5-2.5% stabilizer, 0.2-1.5% co-solvent, and the balance being water. The surface enhancer is a sulfonate compound containing fluorine and silicon functional groups, the bonding agent is a nitrazole compound containing sulfur functional groups, the wetting agent is a benzyl alcohol compound containing hydroxyl functional groups, the stabilizer is a piperidine derivative, and the co-solvent is an ether solvent. This invention provides an anti-diffusion agent for PCB glass substrates that can reduce the surface tension of the glass substrate, strengthen the interfacial adhesion between the substrate and the ink, fundamentally inhibit the diffusion of ink on the substrate surface, and significantly improve the product yield of the solder resist process.

The present invention relates to methods for treating inflammatory bowel disease (IBD). Particularly, the present invention relates to use of specific inhibitors of Voltage-Dependent Anion Channel (VDAC1), such as piperazine- and / or piperidine-derivatives, among others, e.g., peptides and oligonucleotides, for treating IBD.

Disclosed are methods of treating cavernous angiomas including cavernous angiomas with symptomatic hemorrhage with a 4-substituted piperidine derivative. Also disclosed are methods wherein administering the therapeutically effective amount of a 4-substituted piperidine derivative results in a Cmax of between about 3 ng / ml and about 60 ng / ml; and wherein a Tmax is achieved of between about 0.5 hours and about 1 hour of administering of a 4-substituted piperidine derivative.

Described herein are 1,4-substituted piperidine compounds according to Formula I that have demonstrated activity as fatty acid synthase inhibitors. Also described herein are pharmaceutical compositions containing the described 1,4-substituted piperidine compounds. Also described herein are methods of treating diseases mediated by fatty acid synthase, by administering one or more of the compounds or pharmaceutical formulations described herein. Also described herein are methods of synthesizing the described 1,4-substituted piperidine compounds and synthetic intermediates useful in those syntheses.

The invention belongs to the field of biological medicine, and particularly relates to a 3-(dimethylaminomethyl) piperidine compound and a preparation method, a pharmaceutical composition and application thereof. The invention provides a compound as shown in a formula (I) or a stereoisomer, a geometric isomer, a tautomer, a deuterated compound, a nitrogen oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or prodrugs of the stereoisomer, the geometric isomer, the tautomer, the deuterated compound, the nitrogen oxide, the solvate, the metabolite and the pharmaceutically acceptable salt of the compound as shown in the formula (I), and also provides a preparation method of the compound. The invention also relates to application in preparation of medicines for treating pain diseases. According to the compound, the selectivity to KOR and DOR and the druggability of the compound are improved while good MOR agonistic activity is maintained, and certain activity is shown in an in-vivo pharmacological experiment.

The invention relates to a piperidine derivative as shown in a formula (I), and an isotope form, a stereoisomer, a tautomer, a cis-trans-isomer, pharmaceutically acceptable salt, a pharmaceutically acceptable solvate, a hydrate, a prodrug and a polymorphic substance of the piperidine derivative. The compound has a good application prospect in the aspect of preparing medicines for preventing and / or treating TXNIP activity mediated diseases.

The disclosure relates to compounds of formula I, wherein A, B, and R1 have the meaning given in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula (I) exhibit GPR183 antagonistic activity and are thus useful in the treatment or prevention of disorder, condition, or disease where GRP183 antagonist is indicated to be useful.

The present invention relates to the use of METTL3 inhibitors piperidine derivatives of formula (I), for the treatment of carcinomas.

This application relates to the field of medicinal chemistry, specifically disclosing a piperidine derivative and its pharmaceutical composition, uses, and preparation method. The piperidine derivative has the following general formula: [Formula omitted]. This piperidine derivative can be effectively used to treat or prevent multiple sclerosis, exhibiting unexpected synergistic effects in animal models: it not only significantly improves neurological function impairment and promotes recovery, but also simultaneously and profoundly reduces the levels of key pro-inflammatory cytokines IFN-γ and IL-17. This invention provides a novel small molecule drug candidate for the treatment of multiple sclerosis that combines central penetration, neuroprotection, and comprehensive immunomodulation.

: Title: Antibacterial Application of Pyrrolidin-Piperdine Derivatives Containing Composition to Inhibit Helicobacter Pylori Replication, Preparation Method Thereof The present disclosure proposes a method for identification, optimizing, and preparing a therapeutic molecule (MA01027) for inhibiting cytotoxin-associated gene A (CagA) protein of Helicobacter pylori. The therapeutic molecule specifically targets and binds to a particular protein of interest, thereby enhancing the efficacy and specificity of the treatment. The therapeutic molecule is optimized for its binding affinity and selectivity for the target protein. The therapeutic molecule involves combining specific reactants under controlled conditions to achieve high yields and purity of the therapeutic molecule. The therapeutic molecule preparation includes purification steps to isolate the therapeutic molecule from the reaction mixture using standard techniques, thereby ensuring a high-quality final product. The therapeutic molecule binds to the CagA protein of H. pylori, inhibiting its replication by more than 90% and eliminating H. pylori-associated hemolysis.

The composition contains silicon nanoparticles having a hindered piperidine derivative free radical scavenger on the surface of the silicon nanoparticles. A process for making silicon nanoparticles having a hindered piperidine derivative free radical scavenger on the surface of the silicon nanoparticles, the process comprising producing silicon nanoparticles using a VHFLPP process and collecting the silicon nanoparticles in a capture fluid as they are made, wherein the hindered piperidine derivative free radical scavenger is provided in the capture fluid before, during, or after collecting the silicon nanoparticles such that the silicon nanoparticles and the hindered piperidine derivative free radical scavenger are present together in the capture fluid.

The invention discloses ether-containing low-melting-point copolyamide resin as well as a preparation method and application thereof, the ether-containing low-melting-point copolyamide resin is mainly prepared from the following components: caprolactam, amino undecanoic acid, ether-containing diamine, ether-containing binary acid, a catalyst and a piperidine derivative, and deionized water is taken as a reaction medium. The preparation method comprises the following steps: (1) adding ether-containing diamine, ether-containing binary acid and deionized water into a reaction kettle, and stirring to form salt; (2) adding caprolactam, aminoundecanoic acid, a catalyst and a piperidine derivative into the reaction kettle, replacing air in the reaction kettle with inert gas, and performing condensation polymerization; and (3) filling inert gas, and discharging. The copolyamide resin disclosed by the invention has the characteristics of high toughness, high weather resistance, low melting point, low water absorption and the like, few byproducts are produced, an extraction process is not needed, the production process is simple, and the copolyamide resin is suitable for industrial continuous production and can be applied to the fields of preparation of automobile parts, metal surface coatings, composite materials and the like.

The application discloses an asymmetric catalytic synthesis method of chiral 3-amino piperidine and derivatives thereof, and relates to the technical field of asymmetric catalysis, which comprises the following steps: (1) a mixture containing compound 2 and iodine is reacted to obtain intermediate 3; (2) a mixture containing intermediate 3 and a sulfilimine compound is subjected to a free radical asymmetric cross-coupling reaction to obtain chiral compound 4; (3) chiral compound 4 is subjected to desulfilimine protection to obtain intermediate 5; and (4) intermediate 5 is subjected to deprotection to obtain 3-amino piperidine; the intermediate 5 is a 3-amino piperidine derivative. The application is aimed at important synthesizers such as chiral 3-amino piperidine and derivatives thereof, and the synthesizers are rapidly synthesized through a free radical asymmetric cross-coupling method; a free radical asymmetric cross-coupling reaction catalyzed by copper and a chiral anion ligand is utilized to construct chiral 3-amino piperidine and derivatives thereof under mild conditions.

The application belongs to the technical field of medicines, and particularly relates to a 1,3-disubstituted piperidine derivative and a preparation method and application thereof. The application provides a 1,3-disubstituted piperidine derivative and a preparation method and application thereof, wherein the 1,3-disubstituted piperidine derivative is a non-adenosine DOT1L inhibitor; the use of an adenosine or adenosine-like mother nucleus is avoided in the structure, the metabolic stability is higher, the properties are stable, the 1,3-disubstituted piperidine derivative is easy to store, the preparation route is simple and easy to implement, and the 1,3-disubstituted piperidine derivative is easy to purify.

The invention provides an MWF molecular sieve as well as a preparation method and application thereof, and belongs to the technical field of molecular sieve synthesis. The preparation method comprises the following steps: mixing an aluminum source, an inorganic metal alkali source, water, a silicon source and a structure-directing agent to obtain gel; and carrying out hydrothermal crystallization on the gel to obtain the MWF molecular sieve. According to the present invention, the piperazine derivative or the piperidine derivative is adopted as the structure-directing agent, the sodium hydroxide and the potassium hydroxide are adopted as the inorganic alkali source, and the aluminosilicate MWF molecular sieve can be synthesized by using the one-step hydrothermal crystallization method, such that the cost is low, the yield is high, and the prepared MWF molecular sieve has characteristics of high crystallinity and good stability compared with the existing structure-directing agent-based MWF molecular sieve synthesis method; the MWF molecular sieve prepared by the method has a wide SiO2 / Al2O3 molar ratio window (SiO2 / Al2O3 = 5-20), the structure does not collapse after the structure-directing agent is removed by high-temperature roasting, the thermal stability is good, and the application of the MWF molecular sieve in the fields of catalysis and adsorption is expanded.

Described herein are spiropiperidine compounds according to Formula I that have demonstrated activity as fatty acid synthase inhibitors. Also described herein are pharmaceutical compositions containing the described spiropiperidine compounds, and methods of treating diseases mediated by fatty acid synthase, by administering one or more of the compounds or pharmaceutical formulations described herein. Also described herein are methods of synthesizing the compounds described, including the described spiropiperidine compounds and synthetic intermediates that are useful in those syntheses.

The present invention relates to a method for the electrochemical synthesis of methylene quinone compounds, comprising reacting an aldehyde-substituted ring A compound, a phenol derivative, and a secondary amine under electrolytic conditions. The present invention utilizes a one-pot electrochemical oxidation process to synthesize methylene quinone compounds, resulting in high yields, simple operation, low production costs, and an environmentally friendly synthesis route with potential for large-scale industrial production. In a preferred embodiment of the present invention, a piperidine derivative is used as the secondary amine catalyst, significantly reducing the catalyst dosage. When preparing methylene quinone compounds using the electrolytic method, the yield is significantly improved compared to conventional heating methods when ring A is a heteroaromatic ring.