976 results about "Quinolizine" patented technology

The invention relates to the field of medicinal chemistry, in particular to a substituted quinolinone compound targeting KRASG12D and application of the substituted quinolinone compound. Pharmacological tests prove that the affinity effect of the synthesized compound on a KRASG12D mutant is superior to that of a lead compound KAL-21404358. The compounds WY1-014 and WY1-062 have ideal inhibition effects on cells of human lung cancer (A549), human melanoma (A375) and human colon cancer (LOVO). The compound WY1-062 has excellent anti-tumor activity, and the activity of the compound WY1-062 is superior to that of cis-platinum.

The invention relates to chemical compounds useful as inhibitors of class II phosphoinositide 3- kinase (PI3K) signalling. The invention further relates to the medical use of inhibitors of class II phosphoinositide 3-kinase (PI3K) signalling in the treatment of medical conditions associated with defective and / or pathologic class II phosphoinositide 3-kinase (PI3K) signaling, such as stroke, a cardiovascular disease related to endothelial cell dysfunction, cancer, cancer metastasis, myopathy and diabetes.

The invention discloses an environment-friendly flame-retardant polyester yarn and a preparation method thereof, and relates to the technical field of textile, and the environment-friendly flame-retardant polyester yarn is prepared from the following raw materials in parts by weight: 100 parts of polyester chips, 10-15 parts of a flame-retardant polymer containing an organic salt structure, 1-3 parts of an antioxidant, 0.8-2 parts of a lubricant, 1-2 parts of benzotriazole sodium and 0.8-1.2 parts of quinoline yellow. The flame-retardant polymer containing the organic salt structure comprises a structural unit introduced by the following monomers: bis (3-aminophenyl) (3, 5-bis (trifluoromethyl) phenyl) phosphine oxide, 3, 7-diamino-5-phenylphenazine chloride and 3, 5-isoxazole dicarboxylic acid. The environment-friendly flame-retardant polyester yarn is good in ultraviolet aging resistance and flame retardance, high in strength and sufficient in softness.

8-Hydroxy quinoline derivative compounds for enhancing telomerase reverse transcriptase (TERT) expression, and methods for using the same, are provided. These compounds and methods find use in a variety of applications in which increased expression of telomerase reverse transcriptase is desired.

The invention relates to the field of food and health care products, and discloses a composition for dispelling effects of alcohol and protecting liver, which comprises 20-100 parts of ampelopsis grossedentata leaf extract; 50 to 200 parts of a radix puerariae extract; 10-50 parts of a semen hoveniae extract; 10-50 parts of a turmeric extract; 10 to 100 parts of a yeast extract; 5-50 parts of a licorice extract; and 5 to 20 parts of pyrroloquinoline quinone disodium salt. The ampelopsis grossedentata leaf extract, the kudzuvine root extract and the hovenia dulcis thunb extract are utilized, alcohol decomposition is promoted, the blood ethanol concentration is reduced, and drunkenness symptoms are relieved. Puerarin improves activity of liver metabolic enzymes, accelerates discharge of ethanol and acetaldehyde, and reduces liver damage. The anti-oxidation effects of dihydromyricetin and PQQ can eliminate alcohol metabolism free radicals and protect liver cells. The components such as puerarin, hovenia dulcis thunb, curcumin and glycyrrhizic acid jointly promote liver cell regeneration, inflammation and oxidative damage are reduced, the levels of ALT and AST in serum are reduced, and liver health is maintained.

The present invention refers to an antagonist of imidazoline-1 receptor (I1R) for use in the prevention and / or treatment of an autoinflammatory or autoimmune disease in a human subject, selected from the group consisting of (±)-2-endo-amino-3-exo- isopropylbicyclo[2.2.1]heptane (synonym: AGN192403), N-benzylguanidine, 2-(2- Fluoro-5-methylphenyl)-4,5-dihydro-1H-imidazole (synonym: S23757), 2-(2-chloro-4-iodo-phenylamino)-5-methyl-pyrroline (synonym: LNP911), 1-(4, 5-dihydro-1H-imidazol- 2-yl)isoquinoline (synonym: BU98008), 5-[2-bromophenoxy)methyl]-4,5-dihydro-1,3- oxazol-2-amine (synonym: S23515), 6-methylamino-2methylheptene (synonym: isometheptene), and 4-chloro-2,3-dihydro-2-oxo-1,3-benzothiazol-3-ylacetic acid (synonym: benazolin). Also, to the use of Imidazole propionate in the diagnosis of an autoinflammatory or autoimmune disease in a subject, and further to a method of diagnosis of atherosclerosis comprising assessing the level of ImP in a blood sample and determining whether said level is above or below a value of 41nM.

The invention discloses a colorectal cancer radiotherapy sensitization medicine and application thereof, belongs to the field of biological medicine, and particularly relates to a colorectal cancer radiotherapy sensitization medicine which comprises active pharmaceutical ingredients and a solvent, the active pharmaceutical ingredients comprise doxorubicin and a nitrogen-containing compound, the nitrogen-containing compound comprises quinoline-6-carbohydrazide and N-benzyloxymethyl-4-nitroimidazole, and the nitrogen-containing compound comprises quinoline-6-carbohydrazide and The colorectal cancer radiotherapy sensitization medicine disclosed by the invention focuses on a key driving gene FOXP4 for colorectal cancer radiotherapy resistance, and FOXP4 protein is degraded through a ubiquitin-proteasome way, so that not only can the sensitivity of tumor cells to radiotherapy be remarkably improved and tumor growth be inhibited, but also damage to normal tissues is reduced; moreover, the problem of drug resistance easily generated by a traditional method is effectively avoided, the research and development cost is greatly reduced, clinical transformation is accelerated, and the method has a good clinical application prospect.

The invention discloses an 8-hydroxyquinoline derivative platinum complex as well as a synthesis method and application thereof. According to the invention, an 8-hydroxyquinoline derivative platinum complex is used as an active ligand and reacts with cis-Pt (DMSO) 2Cl2 to synthesize the 8-hydroxyquinoline derivative platinum complex. The 8-hydroxyquinoline derivative platinum complex has a good inhibition effect on human breast cancer cells MDA-MB-231, shows excellent in-vivo and in-vitro anti-tumor activity, has potential medicinal value, and is expected to be used for preparing various anti-tumor drugs.

The present invention discloses an infrared-shielding polyurethane glass film and a preparation method thereof, relating to the field of polymer materials technology. When preparing the infrared-shielding polyurethane glass film, the present invention comprises reacting an organic nickel complex and 3-imidazole-1-propionic acid to produce a functionalized crosslinker; sequentially reacting 4-aminophenylacetonitrile with 3-hydroxypropyl acrylate and quinoline-4-carboxaldehyde to produce a UV-absorbing monomer; reacting polypropylene glycol, a UV-absorbing monomer, 1,4-butanediol, and 4-chloromethyl-1,3-phenylenediisocyanate to polymerize to produce polyurethane; reacting tungsten-doped titanium dioxide and chloropropyltriethoxysilane to produce modified titanium dioxide; and uniformly mixing the polyurethane, modified titanium dioxide, the functionalized crosslinker, and acetone, followed by coating and curing to produce the infrared-shielding polyurethane glass film. The infrared-shielding polyurethane glass film prepared by the present invention has excellent infrared shielding, anti-aging, antibacterial, and mechanical properties.

The invention relates to a [NN] bidentate coordination metal catalyst based on a quinoline skeleton as well as a preparation method and application of the [NN] bidentate coordination metal catalyst. According to the preparation method, quinoline-8-formaldehyde and aniline are directly subjected to aldehyde-amine condensation under the catalysis of p-TsOH, and a quinoline-imino ligand is synthesized. The [NN] bidentate coordination metal catalyst based on the quinoline skeleton is prepared by carrying out one-pot reaction on the obtained ligand and in-situ synthesized MMe4 (M is Ti, Zr or Hf). The quinoline skeleton [NN] bidentate coordination metal catalyst is used for polyolefin synthesis. The preparation method has the advantages of simple synthesis process, easily available raw materials, high product yield and high temperature resistance, is suitable for high-temperature solution polymerization, and can be used for preparing high-performance polyolefin elastomers.

The invention provides a biisoquinoline-based iron complex which has a structure as shown in a formula (I), and also provides a preparation method of the biisoquinoline-based iron complex and an application of the biisoquinoline-based iron complex as a catalyst for an anisole hydroxylation reaction. The invention further provides a method for preparing p-hydroxyanisole and co-producing o-hydroxyanisole. When the biisoquinoline-based iron complex provided by the invention is used for catalyzing hydroxylation reaction of anisole, excellent reaction activity and selectivity to hydroxyl products can be obtained, a new process thought is provided for industrial production of p-hydroxyanisole, and the biisoquinoline-based iron complex has very important economic value and social value, # imgabs0 #

The invention discloses an alkali-soluble dihydroquinoline phenazine organic active substance, an electrolyte containing the same and an application of the electrolyte, the alkali-soluble dihydroquinoline phenazine organic active substance has a molecular structural formula shown in a formula (I), in the molecular structural formula, R1, R2, R3, R4, R5, R6, R7 and R8 are respectively and independently selected from-H,-OH,-COOH,-SO3H,-Ar,-PO3H,-OCxH2xCOOH,-OCyH2ySO3H and-OCzH2zPO3H, and at least one alkali-soluble group is contained. The active material has the advantage of multi-electron transfer, can accumulatively transfer 4 equivalent electrons, and has the potential of constructing a high-energy-density flow battery.

Compounds, pharmaceutical compositions, kits, and methods for treating an inflammatory disease, disorder, or condition. The method includes administering to a patient in need thereof: an effective amount of a compound of formula (I), a pharmaceutically acceptable salt thereof, a prodrug thereof, or a metabolite thereof, and an effective amount of a S1P receptor modulator or a pharmaceutically acceptable salt thereof, to treat the inflammatory disease, disorder, or condition. The compound of formula (I) has the following formula:

Disclosed herein are a quinoline derivative, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof useful as a PI3Kα inhibitor, and a pharmaceutical composition comprising the same. Further disclosed herein is a method of treating cancer using a quinoline derivative, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof as a PI3Kα inhibitor.

The invention discloses a near-infrared dichroic dye, a liquid crystal composition and application of the near-infrared dichroic dye and the liquid crystal composition. The structural general formula of the disclosed dichroic dye is as shown in formula I in the specification. According to the invention, a hydrogenated quinoline ring, a hydrogenated benzopyran ring and a hydrogenated naphthalene ring are introduced into a molecular skeleton, so that the novel near-infrared dichroic dye with high light stability, high solubility, high order parameter and high light modulation capability is obtained. Compared with the near-infrared dichroic dye disclosed in the prior art, the absorption band is further subjected to red shift, and the light modulation capability is remarkably improved; ordering parameters are greatly improved, and the application bottleneck is solved.

Provided herein is the use of certain biomarkers, such as tryptophan and metabolites thereof for use in certain treatment methods. Suitable tryptophan metabolites that may serve as useful biomarkers include, for example, kynurenine (Kyn), kynurenic acid (KynA), and quinolinic acid. Such biomarkers may be used in identifying a subject who may benefit from treatment, predicting the responsiveness or monitoring the response of the subject to the treatment, or determining or adjusting the dosing or dosing regimen of the treatment to the subject.

The present disclosure provides a catalyst system capable of selectively hydrogenating (2, 3) / (4, 5) and (2, 3) / (5, 6) dienones with hydrogen. In particular, the present disclosure provides catalysts capable of providing high selectivity for reduction even in the absence of catalyst poisons such as pyridine, pyrazine, quinoline, and quinoxaline.

The present application provides a therapeutic combination of a quinoline derivative and an antibody, which comprises an immune checkpoint inhibitor and a tyrosine kinase inhibitor, wherein the tyrosine kinase inhibitor is a compound of formula I or a pharmaceutically acceptable salt thereof. The therapeutic combination in the present application shows good activity against lung tumor and liver tumor.

Disclosed are a kinase inhibitor and a pharmaceutical composition comprising the kinase inhibitor. The kinase inhibitor comprises a compound as represented by formula (I) or a pharmaceutically acceptable salt, solvate, ester, acid, metabolite, or prodrug thereof. The compound and composition above can inhibit wild-type KIT and / or mutant KIT tyrosine kinase activity and treat, prevent, or alleviate diseases, disorders, or conditions associated with wild-type KIT and / or mutant KIT kinase activity.

The invention discloses a flame-retardant polyester yarn and a preparation method thereof, and relates to the technical field of textile, the flame-retardant polyester yarn is prepared by blending flame-retardant functional fibers and basalt fibers according to the mass ratio of (8-10): 1; the flame-retardant functional fibers are prepared from the following raw materials: polyester chips, flame-retardant polyamide polycondensates, flame-retardant addition polymers, antioxidants and lubricants; the flame-retardant polyamide polycondensate comprises a structural unit introduced by the following monomers: 4, 4-diaminodiphenyl sulfide, 2, 3-quinoline dicarboxylic acid, and 3, 3 '-diamino-4, 4'-difluorodiphenyl sulfone; the polymerization inhibition addition polymer comprises structural units introduced by the following monomers: acrylamide, 4-acryloyl benzophenone hydroxybenzoate, diphenyl (4-vinyl phenyl) phosphine oxide, and 3-(1, 1-difluoro-2-propylene-1-yl)-2 (1H)-quinoxalinone. The yarn is good in mechanical property and damp-heat aging resistance and excellent in flame retardant property.

The invention relates to a cyclic ether modified 3-cyano-4-arylaminoquinoline derivative and a preparation method and application thereof, the cyclic ether modified 3-cyano-4-arylaminoquinoline derivative is a compound as shown in a formula I or pharmaceutically acceptable salt thereof, tests prove that the cyclic ether modified 3-cyano-4-arylaminoquinoline derivative has good in-vitro antitumor activity, and a basis is provided for further research and development of antitumor drugs. # imgabs0 #

The invention discloses a preparation and purification method and application of a quinoline derivative with biological activity, and belongs to the technical field of medicine synthesis. According to the key points of the technical scheme, the quinoline derivative molecule has a structure # imgabs0 #, wherein X is NH or empty (benzene rings are directly connected); r is an aromatic ring derivative or alkyl or other groups. The invention designs and synthesizes a quinoline derivative with a novel structure, and the compound has a relieving effect on LPS-induced microglial cell inflammation and has a certain inhibition effect on cervical cancer cells.

The present disclosure relates to compounds of formula (I) that are RXFP1 receptor agonists, compositions comprising the same, and methods of use thereof (e.g., for the treatment of heart failure, fibrosis, and related diseases, such as lung disease (e.g., idiopathic pulmonary fibrosis), renal disease (e.g., chronic kidney disease), or liver disease (e.g., nonalcoholic steatohepatitis and portal hypertension)). TIFF2024546944000073.tif59153

The invention discloses a demethylase ODM gene for synthesizing benzylisoquinoline alkaloids and application thereof, the demethylase ODM gene is an ODM1 gene or an ODM2 gene, the nucleotide sequence of the CDS region of the ODM1 gene is shown as SEQ ID NO: 1, and the nucleotide sequence of the CDS region of the ODM2 gene is shown as SEQ ID NO: 2. Aiming at the current situation that the research basis of a key gene for synthesizing corydalmine in rhizoma corydalis is weak, the ODM1 gene for catalyzing tetrahydropalmatine demethylation to specifically generate corydalmine and tetrahydrojatrorrhizine and the ODM2 gene for specifically generating tetrahydrojatrorrhizine are cloned from rhizoma corydalis for the first time. An important theoretical basis is provided for producing the corydalmine by utilizing a synthetic biological method in the future, and the corydalmine mutant has a wide application prospect and a great economic value.

The present application provides a therapeutic combination of a quinoline derivative and an antibody, which comprises an immune checkpoint inhibitor and a tyrosine kinase inhibitor, wherein the tyrosine kinase inhibitor is a compound of formula I or a pharmaceutically acceptable salt thereof. The therapeutic combination in the present application shows good activity against lung tumor and liver tumor.

The present invention describes a composition comprising an effective amount of a combination of two or more components selected from acacetin, ACT1 peptide, α-lipoic acid, alprostadil, anisomycin, apigenin, ascorbic acid, astragalus, berberine, β-lapachone, β-hydroxy-β-methylbutyrate, bacopa monnieri, catechins, catechols, chamomile, chrysin, coumestrol, curcumin, dinitrophenol, dinoprost, ellagic acid, (-)-epigallocatechin gallate, green tea extract, fisetin, genistein, ginsenoside RE, glabridin, 18-α-glycyrrhetinic acid, 18-β-glycyrrhetinic acid, glycyrrhizin, hydroquinone, isoquercetin (EMIQ), shan Phosphate, black bean anthocyanins, leucine, lithium, luteolin, luteolin, luteolin, melatonin, menadione, 1‑methylnicotinamide (MNA), methyl salicylate, myricetin, nicotinamide adenine dinucleotide, nicotinic acid (vitamin B3), nicotinamide (NAM), nicotinamide mononucleotide (NMN), nicotinamide riboside (NR), nicotinic acid adenine dinucleotide (NaAD), nicotinic acid mononucleotide (NaMN), parsley, phenylephrine, pokeweed mitogen, 15‑Δ prostaglandin J2, puromycin, quercetin, quinolinic acid, retinoic acid, trichostatin A, troxerutin, rutin, tryptophan, vitamin D3, withaferin A, wortmannin, and zinc (including its salts).

The present invention relates to a histone deacetylase inhibitor, which is a compound represented by a formula I or a pharmaceutically acceptable salt and a stereoisomer thereof, and the compound of the present invention has good HDAC inhibitory activity. In-vitro anti-tumor cell proliferation experiments show that the inhibitory activity of a plurality of compounds on a plurality of tumor cells exceeds that of a positive control drug SAHA. Therefore, part of the compounds have good HDACs inhibitory activity and anti-tumor cell proliferation activity, and can be used for guiding discovery of novel and efficient histone deacetylase inhibitors and anti-tumor active molecules. # imgabs0 #

The invention discloses silane modified polyether prepared from an ethoxyquin polymer, which is prepared by the following method: carrying out aminolysis reaction on the ethoxyquin polymer and epoxypropane to prepare amino alcohol; taking amino alcohol as an initiator, and carrying out polymerization reaction on the amino alcohol and epoxypropane to prepare ethyoxyl quinoline polyether polyol; the ethyoxyl quinoline polyether polyol, anhydride and epoxy organosiloxane are subjected to chemical modification, and the silane modified polyether is prepared. According to the method, resource utilization of the ethoxyquin distillation still residues is realized. Due to the introduction of a rigid nitrogen-containing heteroatom quinoline ring structure and an ester bond structure with high cohesive energy, the silane modified polyether prepared from the ethoxyquinoline polymer has the advantages of high strength, strong adhesion, moisture resistance, low odor, environmental protection, no solvent and the like after being cured, can be used for preparing glass cement, sealant, nail-free glue, ceramic tile adhesive and the like, and has wide application prospects. The method can be widely applied to building industry.

Disclosed herein is a solid Form A of 1-(6-ethyl-8-fluoro-4-methyl-3-(3-methyl-1,2,4-oxadiazol-5-yl)quinolin-2-yl)-N-(tetrahydro-2H-pyran-4-yl)piperidin-4-amine hydrochloride exhibiting at least X-ray lines (in degrees 2θ ± 0.2) at 4.30, 8.59, 12.88, 18.82 and 21.34 in a powder diffraction pattern when measured using Cu Kα radiation. The solid Form A is an antagonist of the kappa-opioid receptor (KOR) and is useful for treating conditions that benefit from the same. Compositions comprising the solid Form A, as well as related methods of use are also disclosed.

The invention relates to an aminoquinoline derivative, a pharmaceutical composition containing the aminoquinoline derivative, and a preparation method and application of the aminoquinoline derivative. Specifically, the invention relates to a compound shown as a formula I or a pharmaceutically acceptable salt, a stereoisomer, a tautomer or an isotope-labeled compound thereof, a pharmaceutical composition containing the compound, and a preparation method and application of the compound. # imgabs0 #