985 results about "Piperidine" patented technology

The invention belongs to the technical field of bioengineering, and relates to a transaminase mutant, a recombinant genetically engineered bacterium and application of the transaminase mutant in catalytic synthesis of (R)-1-Boc-3-aminopiperidine.The transaminase mutant is obtained by conducting single-point or combined mutation on the 131 site and / or the 197 site of an amino acid sequence shown in SEQ ID NO.2; the mutation sites comprise that the 131 phenylalanine is mutated into aspartic acid, threonine or tyrosine, and / or the 197 lysine is mutated into arginine or leucine. Experimental results show that compared with wild type transaminase, the catalytic activity, the thermal stability and the organic solvent tolerance of the obtained mutants, especially single-point mutants MyTA1-F131Y and MyTA1-K197R and a combined mutant MyTA1-F131Y-K197R, are all remarkably improved, and compared with the wild type transaminase, the catalytic activity, the thermal stability and the organic solvent tolerance of the obtained mutants are all remarkably improved. The mutant MyTA1-F131Y-K197R can be used for efficiently catalyzing asymmetric amination of N-Boc-3-piperidone to synthesize (R)-1-Boc-3-aminopiperidine, the conversion rate of the (R)-1-Boc-3-aminopiperidine after the (R)-1-Boc-3-aminopiperidine reacts for 24 hours under the condition that the substrate concentration is 100 g / L can reach 90% or above, and the mutant MyTA1-F131Y-K197R has a good industrial application prospect.

The invention discloses an aldehyde reductase mutant and application thereof in synthesis of a dexmethylphenidate hydrochloride intermediate, and belongs to the field of molecular biology and enzyme engineering. The aldehyde reductase mutant, polynucleotide for coding the mutant, and the recombinant expression vector can express the aldehyde reductase mutant and are used for constructing a recombinant cell or a recombinant strain for expressing the aldehyde reductase mutant. The provided aldehyde reductase mutant can catalyze 2-phenyl-2-((R)-piperidine-2)-acetaldehyde into (R)-2-phenyl-2-((R)-piperidine-2)-1-ethanol, especially improves the stereoselectivity of (R)-2-phenyl-2-((R)-piperidine-2)-1-ethanol, solves the problems of strict conditions, complex reaction and high cost in the existing synthesis method, and has a wide application prospect in the field of synthesis of (R)-2-phenyl-2-((R)-piperidine-2)-1-ethanol. Wide application prospects are realized.

The invention relates to a method for preparing a nerofloxacin chiral piperidylamine intermediate, which comprises the following steps of: carrying out condensation reaction on 5-hydroxy nicotinic acid which is simple and easy to obtain and is used as a raw material and different alcohols, screening through a series of asymmetric catalytic hydrogenation conditions to obtain optimal reaction conditions, and under the conditions, carrying out reaction on various 3, 3 '-dihydroxy nicotinic acid and 3, 3'-dihydroxy nicotinic acid to obtain the nerofloxacin chiral piperidylamine intermediate. The 2, 5-disubstituted pyridine quaternary ammonium salt is reduced into a tetrahydropyridine product, and the C5 site enantioselectivity of the product is excellent. The preparation method comprises the following steps: selecting methyl (R)-1-benzyl-5-hydroxy-1, 4, 5, 6-tetrahydropyridine-3-carboxylic acid methyl ester as a substrate, completely hydrogenating by using platinum dioxide hydrogen, and then carrying out methyl ester reduction, dehydroxylation, Mitsunobu reaction and protecting group removal to obtain a key chiral intermediate for industrial synthesis of a quinolone antibacterial drug nemonofloxacin with high enantioselectivity and high yield.

The invention provides a novel hindered amine light stabilizer as well as a preparation method and application thereof, and relates to the field of light stabilizers. According to the preparation method of the novel hindered amine light stabilizer, specific dibasic acid dimethyl ester and 2, 2, 6, 6-tetramethylpiperidinol are used as raw materials, an alkane solvent or a benzene solvent is used as a solvent, and a catalytic reaction solution is obtained through a heating reaction under the condition of a catalyst; and neutralizing and washing the catalytic reaction liquid to obtain the novel hindered amine light stabilizer. According to the preparation method, ideal preparation effects (such as purity, yield and the like) can be achieved, meanwhile, the chroma of the product is effectively reduced, the problem that the product is prone to yellowing due to the fact that the hindered amine light stabilizer absorbs visible light is solved, and the compatibility and stability of the hindered amine light stabilizer and a high polymer material are further improved.

The invention relates to a thermoplastic molding composition (P) comprising: (A) thermoplastic polymer composition (A) comprising: (A-1) 10 to 50 wt.-% of graft copolymer (A-1), (A-2) 1 to 50 wt.-%, of thermoplastic polymer matrix (A-2) based on one or more vinylaromatic copolymers, (A-3) 20 to 50 wt.-%, of polymerized alkyl methacrylate component (A-3), and (A-4) 0 to 45 wt.-% of comonomer which is copolymerized with the at least one polymerized alkyl methacrylate component (A-3), where the sum of (A-1), (A-2), (A-3) and optional comonomers (A-4) is 83.2 to 99.8 wt.-%; (B) a hindered amine light stabilizer composition (B), comprising at least two of substances (B-1) to (B-3): (B-1) 0 to 0.9 wt.-%, of at least one hindered amine light stabilizer having a dipiperidine structure with at least one alkyl group at each of the 2 and 6 positions of the dipiperidine structure (B-2) 0 to 0.9 wt.-%, of a hindered amine light stabilizer mixture having a monopiperidine structure with at least one alkyl group at each of the 2 and 6 positions of the monopiperidine structure, and (B-3) 0 to 2 wt.-%, of at least one hindered amine light stabilizer having a polymeric structure comprising piperidine groups with at least one alkyl group at each of the 2 and 6 positions of the piperidine groups (C) 0 to 5 wt.-%, of one or more further additives (C), different from (B); and (D) 0 to 10 wt.-%, of colorants, dyes and / or pigments (D), different from (C); wherein the constituents (A) to (D) sum up to 100 wt.-% of the molding composition (P).

Disclosed herein are dosage forms comprising a VAV1 degrader. More specifically, disclosed herein are dosage forms comprising 3-(2-chloro-4'-(2-oxopyridin-1(2H)-yl)-[1,1'- biphenyl]-3-yl)piperidine-2,6-dione or a pharmaceutically acceptable salt thereof. These dosage forms are useful, e.g., for treating a subject (e.g., a human subject) having a disorder or disease that can be treated by reducing the level of VAV1, for example an inflammatory or autoimmune disorder, a transplantation setting disorder, or a cancer.

The application provides a hindered amine light stabilizer and a preparation method thereof, and the preparation method comprises the following steps: putting N, N-bis(2, 2, 6, 6-tetramethyl-4-piperidyl) 1, 6-hexanediamine and an organic solvent into a reaction bottle, heating to 50-80 DEG C, adding methyl acrylate into the system dropwise, obtaining an intermediate I through an addition reaction, and then obtaining a crude product through an ester exchange reaction of the intermediate I and tetramethylpiperidinol in the presence of a catalyst and an organic solvent, washing with water, decoloring, filtering, cooling and crystallizing, filtering and drying to obtain the product; the light stabilizer obtained by the application has multiple hindered amine functional groups, has good heat resistance and extraction resistance, and has good compatibility with resin.

Methods for treating patients with wAIHA comprising administering at least one compound chosen from (R)-2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile (rilzabrutinib) and pharmaceutically acceptable salts thereof are disclosed.

The invention relates to an alkenyl-substituted piperidine compound as well as a pharmaceutical composition, a preparation method and application thereof, and particularly provides the alkenyl-substituted piperidine compound as shown in a formula (I) which can be used for preparing medicines, especially medicines for preventing and / or treating complement bypass mediated diseases or symptoms. Each group in the formula (I) is as defined in the specification.

Provided herein are BTK inhibitors containing piperidine modified at the 3-position. Further disclosed are methods of making and using said BTK inhibitors.

The invention provides a composite diaphragm, a preparation method thereof and a secondary battery. The composite diaphragm comprises a base membrane and a coating arranged on at least one side of the base membrane, the material of the coating comprises a piperidinyl polymer, and the monomer structure of the piperidinyl polymer comprises a piperidine ring, at least one ester group, at least one alkenyl group and a group capable of forming hydrogen-bond interaction. According to the present invention, the coating of the specific type is arranged on the base film, such that the electrolyte wettability and the heat resistance required by the diaphragm can be met, the swelling rate of the diaphragm can be reduced, and the bonding strength between the diaphragm and the negative electrode plate can be improved so as to comprehensively improve the high-temperature cycle and the storage performance of the secondary battery.

The invention relates to the field of pipes, and discloses a high-flame-retardance MPP cable protection pipe and a preparation method thereof.The cable protection pipe comprises polypropylene resin, modified graphene oxide, modified maleic anhydride grafted polypropylene and auxiliaries; the modified graphene oxide is prepared by grafting a modified benzotriazole intermediate and a double-bond DOPO derivative substituted cyclotriphosphazene derivative into graphene oxide; the modified benzotriazole intermediate is prepared by grafting 2-(2, 4-dihydroxyphenyl)-2H-benzotriazole and ethyl bromoacetate, and then reacting with 2, 2, 6, 6-tetramethyl-4-piperidinol; the double-bond DOPO derivative is prepared through the reaction of DOPO-HQ and 4-vinyl benzyl chloride; the modified maleic anhydride grafted polypropylene is prepared by grafting octa-aminopropyl polyhedral oligomeric silsesquioxane prepared by a polycondensation reaction of 3-aminopropyltriethoxysilane and maleic anhydride grafted polypropylene. The pipe prepared by the invention has good mechanical properties, ultraviolet aging resistance, low-temperature toughness, heat resistance, flame retardance and wear resistance.

The invention provides deuterium-enriched piperidinyl-methyl-purine amines and related compounds, pharmaceutical compositions, their use for inhibiting NSD2, and their use in the treatment of a disease or condition, such as cancer.

The invention relates to the technical field of polyamide nanofiltration membranes, in particular to an acid and alkali resistant high-strength nanofiltration membrane and a preparation method thereof. The problem that the strength and the acid and alkali resistance of a polyamide nanofiltration membrane in the prior art cannot be considered at the same time is solved. The base membrane material of the polyamide nanofiltration membrane is modified polyethersulfone and is obtained by chemically bonding a carbon nanotube subjected to double surface modification by titanium dioxide sol-gel and a KH550 coupling agent in a polyester non-woven fabric, and the modulus of the material is improved by utilizing an inorganic-organic hybrid network; the functional layer of the polyamide nanofiltration membrane is made of modified polyamide, and the modified polyamide functional layer is formed by forming a polyamide matrix through polymerization reaction of 2, 2 '-disulfonic acid-4, 4'-diaminobiphenyl, piperazine and trimesoyl chloride and introducing 4-amino-2, 2, 6, 7-tetramethyl-1, 3-pentanediol at the same time. And the chemical resistance is improved by a free radical capturing group generated by 2, 2, 6, 6-tetramethylpiperidine and octa-isobutyl cage type silsesquioxane.

The invention relates to a piperidinedione compound as well as a pharmaceutical composition and application thereof, and particularly provides a piperidinedione compound shown in a formula (I) which can be used for preparing medicines, especially medicines for preventing and / or treating diseases or symptoms caused by or related to lymphocyte development or activity disorder. Each group in the formula (I) is as defined in the specification.

The invention relates to the field of sheath materials, and discloses an anti-aging sheath material for an electronic wire and a preparation method thereof, the sheath material comprises low density polyethylene, an ethylene-vinyl acetate copolymer, an ethylene-octene copolymer, ethylene propylene diene monomer, a triazine ring derivative, ammonium polyphosphate, modified nano silicon dioxide and an auxiliary agent; according to the triazine ring derivative, N-butyl-2, 2, 6, 6-tetramethyl-4-piperidylamine reacts with cyanuric chloride to prepare a triazine ring monosubstituent, hydrazine hydrochloride is used as a bridging agent to react with the triazine ring monosubstituent, and the triazine ring derivative and piperazine are polymerized to prepare the triazine ring derivative. The modified nano silicon dioxide is prepared by enabling 3-(3, 5-di-tert-butyl-4-hydroxyphenyl) propionyl chloride and 4-propenyloxy-2-hydroxybenzophenone to react, and carrying out free radical polymerization on the reaction product on the surface of the nano silicon dioxide. The synergistic effect of mechanical property, thermo-oxidative aging resistance, ultraviolet aging resistance and flame retardant property is realized.

Methods for treating Sickle Cell Disease (SCD) comprising administering a BTKi, such as at least one compound chosen from (R)-2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile (rilzabrutinib) and pharmaceutically acceptable salts thereof, are disclosed.

The invention discloses a 3-aryl piperidine-2, 6-diketone compound as shown in a general formula I or an enantiomer, a diastereoisomer, a raceme and a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the 3-aryl piperidine-2, 6-diketone compound, the compound is used as a VAV1 targeted molecular glue degradation agent, and can degrade VAV1 protein in a targeted manner, so that the VAV1 protein can be degraded in a targeted manner. The invention has the application of preparing medicines for treating and / or preventing inflammatory diseases and autoimmune diseases.

The invention discloses a high-barrier antibacterial plastic packaging film and a preparation method thereof, belongs to the technical field of film processing, and aims to solve the technical problem that the antibacterial property and barrier property of a plastic packaging film need to be further improved in the prior art. The composite material specifically comprises the following components in parts by weight: 60-80 parts of linear low-density polyethylene, 10-15 parts of a modified compatibilizer, 4-6 parts of a modified antibacterial capsule and 1-3 parts of an auxiliary additive. The preparation method comprises the following steps: oxidizing 2-methyl-2-acrylic acid-2, 2, 6, 6-tetramethyl-4-piperidinyl ester with sodium hypochlorite to obtain a modified precursor, and carrying out free radical polymerization reaction on the modified precursor, low-density polyethylene, glycidyl methacrylate and vinyl heptafluorobutyrate to form a compatibilizer with a block structure. The antibacterial property and barrier property of the plastic packaging film are improved, and the mechanical property of the plastic packaging film is also improved.

This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt thereof) that degrades Proto-oncogene VAV 1 protein (VAV1). The chemical entities are useful for treating subjects having a disorder or disease that can be treated by reducing the level of VAV1, such as cancer, inflammatory or autoimmune disorders.

A medicament for treatment or prevention of interstitial lung disease, and of a disease or symptom accompanied by systemic sclerosis in a subject, the medicament comprising, as an effective ingredient, 1-{2-[(3S,4R)-1-{[(3R,4R)-1-cyclopentyl-3-fluoro-4-(4-methoxyphenyl)pyrrolidin-3-yl]carbonyl}-4-(methoxymethyl)pyrrolidin-3-yl]-5-(trifluoromethyl)phenyl}piperidine-4-carboxylic acid, or a pharmaceutically acceptable salt or co-crystal thereof.

The present application relates to a kind of dimethylamine piperidine continuous synthesis dimethylamine piperidine method of oxy group, by using reaction raw material mixed solution into continuous flow packed bed reaction zone, i.e.catalyst layer;Reaction temperature is 20-80 ℃, normal pressure, feed liquid is the mixture of dimethylamine piperidine, hydrogen peroxide and deionized water, oxidation is carried out on the catalyst layer of continuous flow packed bed adiabatic reactor to make dimethylamine piperidine into dimethylamine piperidine oxy group, realize the continuous preparation of dimethylamine piperidine oxy group;The obtained reaction liquid is quenched, then filtered to remove solid particle quenching agent, vacuum distillation to remove water and vacuum rectification treatment obtain high-purity dimethylamine piperidine oxy group;The process scheme overcomes the series of deficiencies in the previous preparation process, such as complicated steps, low product purity, low production capacity in unit production time, realizes the continuous preparation of high-purity dimethylamine piperidine oxy group, with the characteristics of efficient, safe, green manufacturing.

This invention provides deuterium-enriched piperidinyl methylpurine amine salts, crystalline forms, pharmaceutical compositions, their use in inhibiting NSD2, and their use in treating diseases or ailments, such as cancer.

The invention discloses an ultrasonic response quaternary ammonium salt polymer antibacterial agent and a preparation method thereof. The ultrasonic response quaternary ammonium salt polymer is prepared by the following steps: carrying out substitution reaction on azodiisobutylimidazoline and acryloyl chloride, then carrying out addition polymerization reaction with 4-aminomethylpiperidine, and then carrying out quaternization reaction with bromohexane. The obtained ultrasonic response quaternary ammonium salt polymer can be decomposed under the ultrasonic action to generate alkyl radicals, and has the sterilization effect. In addition, quaternary ammonium salt modification can improve the water solubility and the positive charge density of the polymer, and further improves the antibacterial performance.

This invention relates to the field of polymer technology, specifically disclosing an oxyfluorene-containing polyaryl suspended side-chain anion exchange polymer. By introducing an oxyfluorene structure, this invention successfully overcomes the defects of traditional polyaryl ether materials, such as easy main chain breakage and degradation under strong alkaline conditions, thus improving the chemical and thermal stability of the material. The suspension side-chain strategy introduces benzene rings, quaternary ammonium groups, or piperidine cationic groups, effectively promoting microphase separation within the polymer and constructing efficient ion transport channels. This allows the membrane material to maintain a low swelling ratio while achieving good hydroxide ion conductivity, reaching up to 170.2 mS / cm at 80°C. The polymer exhibits excellent mechanical properties, with outstanding dry membrane tensile strength and excellent alkali resistance and durability. After immersion in a strong alkaline (KOH) solution at 80°C for over 1800 hours, its conductivity loss is minimal. The anion exchange membrane prepared by this invention has good application value in fuel cells and water electrolysis for hydrogen production, demonstrating strong commercial potential.

The application relates to the technical field of circuit conveying equipment, in particular to a fireproof polyvinyl chloride material and a preparation method thereof and a cable sheath pipe. The fireproof polyvinyl chloride material comprises the following raw materials in parts by weight: 90-110 parts of polyvinyl chloride, 10-20 parts of a compatilizer, 8-15 parts of ammonium polyphosphate and 5-8 parts of an ultraviolet aging resistant additive, wherein the ultraviolet aging resistant additive is a mixture of N,N"-bis(2,2,6,6-tetramethyl-4-piperidyl)-1,6-hexanediamine and a metal hydroxide. The fireproof polyvinyl chloride has excellent flame retardant performance and ultraviolet aging resistance.

The present invention relates to a pharmaceutical composition for treating myopia, preventing myopia and / or suppressing myopia progression, comprising (+)-11-[2-[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one or a salt thereof as an active ingredient, wherein the pharmaceutical composition is substantially free of (−)-11-[2-[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one or a salt thereof.

The present invention relates to compounds of formula (I) as RAS-PI3K modulators for use in methods of treatment of cancer, immunological disorders and wound healing. Preferred compounds are e.g. l-(([l,l'-biphenyl]-2-yl)sulfonyl)-4-fluoro-N-(3-(methylsulfonyl)allyl)piperidine-4-carboxamide derivatives.

The application discloses a 3-(5-(aminomethyl)-1-oxoisoindoline-2-yl)piperidine-2,6-dione derivative and a synthesis method and application thereof, and relates to a 3-(5-(aminomethyl)-1-oxoisoindoline-2-yl)piperidine-2,6-dione derivative which is a compound with the following general formula (I): wherein R1 is selected from,,,,,,,,, and R2 is selected from,,, and. The compound can significantly inhibit the proliferation of leukemia, multiple myeloma, lymphoma, breast cancer, liver cancer and the like at a low dose (nanomole), can effectively degrade IKZF1, IKZF3, BRD4, GSPT1 and CK1 alpha, and has the prospect of being developed into an anti-tumor drug. The application solves the problem that the existing malignant hematological disease treatment drugs have a high safety risk.