2885 results about "Piperidine" patented technology

The invention relates to a pharmaceutically acceptable salt of a benzothiophene substituted fused ring compound, and a crystal form and application thereof. Specifically, the present disclosure provides a pharmaceutically acceptable salt of 2-amino-7-fluoro-4-((5S, 5aS, 6S, 9R)-1-fluoro-12-((1-((4-(fluoromethylsubunit) piperidine-1-yl) methyl) cyclopropyl) methoxyl)-5-methyl-5a, 6, 7, 8, 9, 10-hexahydro-5H-4-oxa-3, 10a, 11, 13, 14-pentaaza-6, 9-methylbridged naphtho [1, 8-ab] heptano-2-yl) benzo [b] thiophene-3-formonitrile, a crystal form and a preparation method thereof, and a preparation method of the pharmaceutically acceptable salt, the crystal form and the preparation method thereof. Corresponding salts have good stability and can be better used for clinical treatment. # imgabs0 #

The present invention relates to four specific macrocyclic compounds for use as inhibitors of KRAS mutant for the treatment of cancer. Example (1): 1-[4-(dimethylamino)-4-methyl-pent-2-ynoyl]-N-[(1S)-1-[[(6S,8S,14S)-22-ethyl-25-fluoro-(21M)-21-[2-[(1S)-1-methoxyethyl]-3-pyridyl]-18,18-dimethyl-9,15-dioxo-5,16-dioxa-2,10,22,28-tetrazapentacyclo[18.5.2.12,6.110,14.023,27]nonacosa-1(26),20,23(27),24-tetraen-8-yl]carbamoyl]-2-methyl-propyl]-4-fluoro-N-methyl-piperidine-4-carboxamide.

The invention relates to a crystal form of a benzothiophene substituted fused ring compound and a preparation method thereof. Specifically, the invention provides a crystal form A and a crystal form D of 2-amino-7-fluoro-4-((5S, 5aS, 6S, 9R)-1-fluoro-12-((1-((4-(fluoromethylsubunit) piperidine-1-yl) methyl) cyclopropyl) methoxyl)-5-methyl-5a, 6, 7, 8, 9, 10-hexahydro-5H-4-oxa-3, 10a, 11, 13, 14-pentaaza-6, 9-methylbridged naphtho [1, 8-ab] heptano-2-yl) benzo [b] thiophene-3-formonitrile, and the crystal form A and the crystal form D have the advantages that the crystal form A and the crystal form D are good in stability; and the medicine can be better used for clinical treatment. # imgabs0 #

The invention relates to a pharmaceutically acceptable salt of a fused ring compound, and a crystal form and application thereof. Specifically, the present disclosure provides a pharmaceutically acceptable salt of 3-chloro-5-((5S, 5aS, 6S, 9R)-1-fluoro-12-((1-((4-(fluoromethylsubunit) piperidine-1-yl) methyl) cyclopropyl) methoxy)-5-methyl-5a, 6, 7, 8, 9, 10-hexahydro-5H-4-oxa-3, 10a, 11, 13, 14-pentaaza-6, 9-methylbridged naphtho [1, 8-ab] heptan-2-yl)-4-(trifluoromethyl) aniline, a crystal form, and a preparation method thereof, and a preparation method thereof. Corresponding salts have good stability and can be better used for clinical treatment. # imgabs0 #

The invention relates to a pharmaceutically acceptable salt of a fused ring compound, and a crystal form and application thereof. Specifically, the present disclosure provides a pharmaceutically acceptable salt of 3-chloro-5-((5S, 5aS, 6S, 9R)-1-fluoro-12-((1-((4-(fluoromethylsubunit) piperidine-1-yl) methyl) cyclopropyl) methoxy)-5-methyl-5a, 6, 7, 8, 9, 10-hexahydro-5H-4-oxa-3, 10a, 11, 13, 14-pentaaza-6, 9-methylbridged naphtho [1, 8-ab] heptan-2-yl)-4-(trifluoromethyl) aniline, a crystal form, and a preparation method thereof, and a preparation method thereof. Corresponding salts have good stability and can be better used for clinical treatment. # imgabs0 #

The invention relates to a crystal form of a benzothiophene substituted fused ring compound and a preparation method thereof. Specifically, the invention provides a crystal form E, a crystal form G and a crystal form H of 2-amino-7-fluoro-4-((5S, 5aS, 6S, 9R)-1-fluoro-12-((1-((4-(fluoromethylsubunit) piperidine-1-yl) methyl) cyclopropyl) methoxyl)-5-methyl-5a, 6, 7, 8, 9, 10-hexahydro-5H-4-oxa-3, 10a, 11, 13, 14-pentaaza-6, 9-methylbridged naphtho [1, 8-ab] heptano-2-yl) benzo [b] thiophene-3-formonitrile, and the crystal form E, the crystal form G and the crystal form H have the advantages that the stability is good; and the medicine can be better used for clinical treatment. # imgabs0 #

The invention relates to a pharmaceutically acceptable salt of a fused ring compound, and a crystal form and application thereof. Specifically, the present disclosure provides a pharmaceutically acceptable salt of 3-chloro-5-((5S, 5aS, 6S, 9R)-1-fluoro-12-((1-((4-(fluoromethylsubunit) piperidine-1-yl) methyl) cyclopropyl) methoxy)-5-methyl-5a, 6, 7, 8, 9, 10-hexahydro-5H-4-oxa-3, 10a, 11, 13, 14-pentaaza-6, 9-methylbridged naphtho [1, 8-ab] heptan-2-yl)-4-(trifluoromethyl) aniline, a crystal form, and a preparation method thereof, and a preparation method thereof. Corresponding salts have good stability and can be better used for clinical treatment. # imgabs0 #

The present disclosure relates to a pharmaceutically acceptable salt of a G12D inhibitor compound and a crystal form thereof. Specifically, provided in the present disclosure are a salt of 2-amino-4-((5S,5aS,6S,9R)-12-((1-((4-(difluoromethylene)piperidin-1-yl)methyl)cyclopropyl)methoxy)-1-fluoro-5-methyl-5a,6,7,8,9,10-hexahydro-5H-4-oxa-3,10a,11,13,14-pentaaza-6,9-methanonaphtho[1,8-ab]cyclohepten-2-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile and a crystal form thereof.

The present disclosure provides certain piperidinylpyridinylcarbonitrile derivatives, and pharmaceutically acceptable salts thereof, that are inhibitors of Glutaminyl-peptide cyclotransferase (QPCT) and glutaminyl-peptide cyclotransferase-like protein (QPCTL), and are therefore useful for the treatment of diseases treatable by inhibition of QPCT / L. Also provided are pharmaceutical compositions containing the same, and processes for preparing said compounds.

Embodiments of the present invention provide methods and intermediates for the large scale preparation of 2, 4, 6-trifluoro-N-[6-(1-methylpiperidine-4-carbonyl)-2-pyridyl] benzamide hemisuccinate, as well as formulations and product forms prepared by these methods. Embodiments of the present invention further provide for the preparation of lamidetan acetate (2, 4, 6-trifluoro-N-[6-(1-methylpiperidine-4-carbonyl)-2-pyridyl] benzamide acetate) and / or a pharmaceutical composition thereof, and / or the use of lamidetan acetate and formulations thereof in subcutaneous drug delivery.

The invention belongs to the technical field of anion exchange membranes, and relates to a cross-linked polyaromatic piperidine anion exchange membrane and a preparation method thereof. The exchange membrane structure comprises a copolymer structure of the following repetitive structural units, the selected rigid main chain polyaromatic hydrocarbon can ensure the mechanical strength of the anion exchange membrane, meanwhile, the toughness of the anion exchange membrane is further enhanced by adopting a cross-linked structure, and a formed cross-linked network can reduce swelling of the anion exchange membrane, so that the anion exchange membrane is more stable in performance. The mechanical performance is improved; according to the invention, ether-free skeleton polyaromatic hydrocarbon is selected as a main chain and has the characteristic of strong alkali-resistant stability, six-membered nitrogen heterocyclic ions are adopted as functional groups, and a large steric hindrance structure can hinder nucleophilic substitution and elimination reaction, so that the alkali-resistant stability of the anion exchange membrane is improved, and the service life of the anion exchange membrane is prolonged. And in the # imgabs0 #, X is equal to 0.05 to 0.15.

The invention provides a low-cost flow battery and an application thereof, a redox active substance of a positive electrode electrolyte of the low-cost flow battery contains a hydroxylamine cyclic structure group with hindered amine, and the hydroxylamine cyclic structure group with hindered amine is preferably selected from 1-hydroxy-2, 2, 6, 7, 8-tetramethyl-1, 3, 5-tetramethyl-1, 3, 5-tetramethyl-1, 3, 5-tetramethyl-1, 3, 5-tetramethyl-1, 3, 5-tetramethyl-1, 3, 5-tetramethyl-1, 3, 5-tetramethyl-1, one or more of a 1-oxo-2, 2, 6, 6-tetrasubstituted piperidine group, a 1-oxo-2, 2, 6, 6-tetrasubstituted piperidine group, a 1-oxo-2, 2, 6, 6-tetrasubstituted piperidine group, and a 1-oxo-2, 2, 6, 6-tetrasubstituted piperidinium group; a redox active substance of the negative electrode electrolyte contains one or more of a titanium element, a vanadium element, a chromium element, an iron element and a zinc element. The low-cost flow battery has the advantages of high output voltage, high energy density, environment friendliness and low cost, and has good application prospects and large-scale popularization potential in the field of energy storage.

The invention relates to the technical field of cationic polymers, in particular to a high-alkali-resistance polyarylene alkylene piperidine cationic polymer as well as a preparation method and application thereof. The preparation method of the high alkali resistance poly (arylene alkylene piperidine) cationic polymer comprises the following steps: carrying out catalytic polycondensation on 1-R6-3-piperidine formaldehyde or salt or hydrate thereof and an aromatic compound to obtain a polymer with a piperidine structure; and further performing ionization reaction to obtain the polyarylene alkylene piperidine cationic polymer. The anion exchange membrane prepared based on the piperidine cationic polymer has ultrahigh alkali resistance and excellent mechanical properties and ionic conductivity, and can be used in the electrochemical energy conversion fields of fuel cells, water electrolysis hydrogen production, carbon dioxide electroreduction, flow batteries and the like, and the separation fields of electrodialysis, water treatment and the like.

Disclosed herein are novel methods for preparing 2-[(3R)-2-[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, including various solvate forms and intermediates thereof. Also disclosed herein are novel solvate forms and intermediates of 2-[(3R)-2-[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.

Disclosed are naphthyl compounds comprising either a ureido piperidine-1 -carboxamide or a ureido piperidine-1 -carboxylate moiety, compositions thereof, and methods of use thereof, for treating or preventing a disease or disorder associated with abnormal levels of amino acids by modulation of SLC6A19 transport, such as phenylketonuria, hyperphenylalaninemia, diabetes and chronic kidney disease.

The invention discloses a PVC / CPE modified material and a preparation method thereof, and belongs to the technical field of high polymer materials. The PVC / CPE modified material comprises the following raw materials in parts by weight: 80-100 parts of PVC, 20-40 parts of CPE, 3-30 parts of a plasticizer, 2-4 parts of a modified flame-retardant anti-aging agent, 2-3 parts of a stabilizer and 3-5 parts of a lubricant. The preparation method comprises the following steps: preparing an intermediate 1 from organic silicon resin and 4-((4-(hydroxymethyl) phenyl) (phenyl) amino) benzaldehyde, preparing an intermediate 2 from the intermediate 1 and 9, 10-dihydro-9-oxa-10-phosphaphenanthrene-10-oxide, preparing an intermediate 3 from cyanuric chloride and N-butyl-2, 2, 6, 6-tetramethyl-4-piperidylamine, preparing an intermediate 4 from the intermediate 3, and preparing an intermediate 4 from the intermediate 4. And finally preparing the modified flame-retardant anti-aging agent from the intermediate 2 and the intermediate 3. The PVC / CPE modified material prepared by the invention has excellent anti-aging performance and flame retardant performance.

The invention provides a preparation method and application of a cobalt-based catalyst, and relates to the technical field of chemical production. The cobalt-based catalyst includes cobalt, a transition metal element, and a Group IIIA element other than aluminum. Transition metal elements and IIIA group elements except aluminum are introduced into the cobalt-based catalyst, and the electronic structure and active sites of the cobalt-based catalyst are changed. The method not only can cooperate with catalytic reaction and promote the formation and conversion of intermediates, but also can enhance the adsorption and activation capability on substrates, reduce the reaction activation energy and guide the reaction to be carried out along a specific path. Finally, the effect of efficiently harvesting the 2-methyl pentamethylene diamine and the 3-methylpiperidine at the same time is achieved.

Methods for treating immune thrombocytopenia 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 (PRN1008) and pharmaceutically acceptable salts thereof are disclosed. Pharmaceutical compositions comprising at least one compound chosen from PRN1008 and pharmaceutically acceptable salts thereof are also disclosed.

The invention discloses a preparation method of a GLP-1R agonist Orforglipron, which comprises the following reaction steps: carrying out four-step reaction on an oxopiperidine compound (1) and (4-fluoro-3, 5-dimethylphenyl) hydrazine (2) to obtain a compound 8, and carrying out seven-step reaction on 5-bromo-indolecarboxylic acid (9) to obtain a compound 17. Then, the compound 8 and a compound 17 are subjected to an acid amine condensation reaction, and Orforglipron (LY3502970) is obtained. The preparation method is relatively low in cost, easy to operate, relatively short in synthetic route and suitable for industrial production and application, and the total yield can reach 32%.

The invention provides a polymer, a cross-linked anion exchange membrane and a preparation method and application thereof. According to the polymer and the cross-linked anion exchange membrane, aryl compounds, trifluoroketone compounds and N-methylpiperidone are polymerized to form a main chain, the main chain has excellent rigidity and flexibility, a quaternary ammonium salt alkenyl compound is introduced as a cross-linking agent, cross-linking is completed through heating in the membrane forming process, and the cross-linked anion exchange membrane is prepared. The quaternary ammonium salt side chain introduced into the side chain has excellent hydrophilic and hydrophobic phase separation characteristics. The polymer and the cross-linked anion exchange membrane have excellent oxidation-reduction resistance and alkali resistance, have the characteristics of stable physical and chemical properties, excellent ion flux, excellent mechanical properties (the elongation at break is greater than 60%) and simple process, and can be widely applied to the fields of hydrogen production by water electrolysis and the like.

The invention relates to an anion exchange membrane based on isopropyl piperidone and biphenyl and a preparation method of a membrane electrode, the preparation method comprises the following steps: respectively dissolving an aromatic monomer and IPD in a first solvent, and mixing to obtain a mixed solution, the aromatic monomer being BP or TP; dropwise adding an acidic initiator into the mixed solution for reaction at the reaction temperature of-5 DEG C to 0 DEG C to obtain a nitrogen heterocyclic ring polymer intermediate; adding a quaternization reagent into the nitrogen-containing heterocyclic ring polymer intermediate to realize quaternization modification of nitrogen atoms to obtain a quaternization ionomer; and forming a film to obtain the AEM film. The preparation method of the membrane electrode comprises the following steps: respectively forming a cathode catalyst layer and an anode catalyst layer on two opposite sides of an AEM membrane through ultrasonic spraying to obtain the MEA. The AEM membrane and the MEA obtained according to the invention have the characteristics of excellent stability and high water electrolysis performance, can significantly improve the efficiency and durability of AEMWE, and are suitable for the fields of hydrogen production by water electrolysis and the like.

Disclosed are compounds, compositions, and methods useful for treating or preventing a disease or disorder associated with abnormal levels of amino acids by modulation of SLC6A19 transport.

Compounds of formula (II) and formula (I) which are inhibitors of QPCTL and QPCT: (II) and (I) are provided herein. Also provided are pharmaceutical compositions containing this compound, as well as compounds for use in methods of treating cancer, neurodegenerative, inflammatory or autoimmune diseases. Exemplary compounds are, for example, 3-(6-fluoropyridin-3-yl)-2-[4-(4-methyl-4H-1,2,4-triazol-3-yl)piperidin-1-yl]benzonitrile (Example 1): (1), and pharmacological data are provided. TIFF2025524039000368.tif70128

The invention relates to the technical field of fibers, and discloses an antibacterial and antistatic fiber material based on silver ions and halamine and a preparation method of the antibacterial and antistatic fiber material. The preparation method comprises the following steps: loading a methyl methacrylate-based polymer on the surface of a silver-loaded molecular sieve through an in-situ polymerization method, and grafting a halamine antibacterial monomer chlorinated piperidinol through an ester exchange reaction to obtain an antibacterial agent; the preparation method comprises the following steps: carrying out reaction polymerization on caprolactam, quaternized polyether, polyethylene glycol, 2, 6-dipicolinic acid and adipic acid to obtain an antistatic agent; an antibacterial agent, an antistatic agent and nano-silver are added into chemical fiber slices, the antibacterial and antistatic fiber material based on silver ions and halamine is prepared after melt spinning, and the chemical fiber slices are polyester slices or chinlon slices or polypropylene slices. The fiber material has excellent antibacterial and antistatic properties.

The invention provides a synthesis method of 6-(t-butyloxycarboryl)-3, 6-diazabicyclo [3.1. 1] heptane, which comprises the following steps: starting from N-benzyl-2, 6-piperidinedione, firstly forming a dibromide 1, then forming a bridge ring intermediate 2 under alkaline conditions, then removing benzyl to obtain an intermediate 3, then reducing dicarbonyl to form free amine 4, and finally synthesizing the 6-(t-butyloxycarboryl)-3, 6-diazabicyclo [3.1. 1] heptane. Then performing Boc protection on amino to obtain an intermediate 5, and performing debenzylation to form a target product. According to the synthesis method, few impurities are generated, and the product is easy to purify and high in purity, so that the total yield is increased, the unit cost is effectively reduced, and large-scale industrial production is facilitated.

Disclosed are a compound and pharmaceutically acceptable salts thereof, a pharmaceutical composition, and related methods for treating or preventing a disease or disorder associated with abnormal levels of amino acids via modulation of the SLC6A19 transporter.

Methods for treating children, adolescents and adults with persistent or chronic immune thrombocytopenia 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 belongs to the technical field of biological catalysis, and particularly relates to four R-transaminase and application thereof in asymmetric synthesis of chiral N-heterocyclic amine active drug intermediates. The amino acid sequences of the R-transaminase disclosed by the invention are shown as SEQ ID NO. 1, SEQ ID NO. 3, SEQ ID NO. 5 and SEQ ID NO. 7. Four kinds of R-transaminase are obtained through gene mining and screening, and recombinant escherichia coli is constructed and expressed by adopting a gene engineering technology. The obtained R-transaminase can be used for synthesizing chiral drug intermediates (R)-3-amino-N-Boc-pyrrole (1b) and (R)-3-amino-N-Boc-piperidine (2b) with high stereoselectivity, and has a good application prospect.