68 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.

The disclosure provides at least one compound, tautomer, deuterated derivative, or pharmaceutically acceptable salt chosen from compounds of Formula I, tautomers thereof, deuterated derivatives of those compounds or tautomers, and pharmaceutically acceptable salts of any of the foregoing, compositions comprising the same, and methods of using the same, including uses in treating APOL1-mediated diseases, including pancreatic cancer, focal segmental glomerulosclerosis (FSGS), and / or non-diabetic kidney disease (NDKD).

The invention discloses an anti-diffusion agent for a PCB glass substrate and a preparation method and application thereof, and relates to the technical field of printed circuit board manufacturing. The anti-diffusion agent is prepared from the following components in mass concentration: 0.5 to 2.5 percent of a surface reinforcing agent, 0.5 to 2.5 percent of a bonding agent, 1.0 to 3.0 percent of a wetting agent, 0.5 to 2.5 percent of a stabilizing agent, 0.2 to 1.5 percent of a cosolvent and the balance of water, the surface enhancer is a sulfonate compound containing a fluorine functional group and a silicon functional group, the bonding agent is an azole compound containing a sulfur functional group, the wetting agent is a benzyl alcohol compound containing a hydroxyl functional group, the stabilizer is a piperidine derivative, and the cosolvent is an ether solvent. According to the anti-diffusion agent for the PCB glass substrate, the surface tension of the glass substrate can be reduced, the interface bonding force between the substrate and ink can be enhanced, the diffusion phenomenon of jet printing ink on the surface of the substrate can be fundamentally inhibited, and the product yield of a solder resist process can be remarkably improved.

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.

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, 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 1,4-substituted piperidine compounds and synthetic intermediates useful in those syntheses.

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 disclosure relates to 6-substituted quinoline-2-piperidine derivatives for use in the treatment and / or prevention of tuberculosis.

2-substituted piperidine derivatives of formula (I), processes for their preparation, pharmaceutical compositions comprising these compounds, and pharmaceutical uses for the treatment of diseases or conditions. # imgabs0 #

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 an aromatic heterocycle-fused cyclohexyl aminoalkyl piperidine derivative, a preparation method and use thereof. Specifically, the present invention provides a compound of general formula (I), a stereoisomer thereof, a tautomer thereof, or a pharmaceutically acceptable salt thereof, and a preparation method therefor, use thereof for activating the activities of a 5-HT1A receptor and dopamine D2 and D3 receptors, and use thereof in the preparation of a medicament for Parkinson's disease.

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.

There are disclosed certain piperidine derivatives of Formula (I), and pharmaceutically acceptable salts thereof, together with compositions containing them and their use in therapy. The compounds are inhibitors of the and nicotinamide N-methyl transferase (NNMT) are thereby particularly useful in the treatment or prophylaxis of, for example chronic kidney disease, acute kidney injury or heart failure.

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.

Provided is an active energy ray-curable coating composition which, when applied to a printed matter (especially a printed matter printed by an electrophotographic method), has a small load on the environment, exhibits excellent adhesion, and can impart excellent glossiness. This active energy ray-curable coating composition contains a resin, an ethylenically unsaturated compound, an initiator, and a polymerization inhibitor. The resin includes an amine-modified styrene (meth)acrylic resin. The contained amount of the amine-modified styrene (meth)acrylic resin is 5-30 mass%. The ethylenically unsaturated compound includes at least one of acryloyl morpholine or vinylcaprolactam. The total of the contained amount of at least one of acryloyl morpholine or vinylcaprolactam is 41 mass% or more. The polymerization inhibitor contains a piperidine derivative. The piperidine derivative is contained in an amount of 0.05-1 mass% and has a viscosity of 40-380 mPa·s at 25°C.

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.