209 results about "Quinolizidines" patented technology

The invention relates to the field of medicinal chemistry, in particular to quinoline compounds or pharmaceutically acceptable salts, isomers, solvates, compositions and medical application thereof. Pharmacological tests prove that the quinoline compound disclosed by the invention has a relatively good affinity effect on KRASG12D-cRaf. When the concentration is 10 M, the compound C1, the compound C3, the compound C4, the compound C6, the compound C11, the compound C12, the compound C13, the compound C16, the compound C22 and the compound C23 have a certain inhibition effect on KRASG12D-cRaf. Particularly, the compound C1 and the compound C12 both show a strong inhibition effect on KRASG12D-cRaf.

To provide a cation-dyeable polyester fiber structure, a production method of the same, and a uniform for medical use.SOLUTION: A cation-dyeable polyester fiber structure includes a cationic dye, a quinoline compound, and an ultraviolet absorber, where 0.03 mass% or more and 0.80 mass% or less of the quinoline compound is included to a mass of the cation-dyeable polyester fiber structure, a color difference ΔE between before and after irradiating the cation-dyeable polyester fiber structure with ultraviolet carbon arc lamplight is 2.0 or lower, and an antibacterial activity value A50 after 50 times of high temperature acceleration washing is larger than a standard cloth growth value F in an antibacterial evaluation method described in an SEK mark textile product certification standard.SELECTED DRAWING: None

The invention discloses a functional fracturing fluid directly prepared from flow-back fluid of complex water quality. The fracturing fluid is prepared by directly adding a salt-tolerant polymer and an ion trapping agent into the flow-back fluid. The addition amount of the salt-tolerant polymer accounts for 0.15-0.3% of the total mass of the fracturing fluid, and the addition amount of the ion trapping agent is 100-500ppm. The salt-tolerant polymer is prepared by copolymerization of acrylamide, a salt-tolerant monomer and an allyl quinoline monomer, and the molecular weight of the polymer is 4-15 million. The salt-tolerant monomer is acrylamide polyoxyethylene sodium benzenesulfonate or acrylamide sodium sulfonate. The ion trapping agent is prepared from amino trimethylene phosphonic acid, diethylene triamine penta (methylene phosphonic acid), ethylene glycol bis (2-aminoethyl ether) tetraacetic acid, p-methylphenyl diethanol amine, 2, 3-epoxypropyl trimethyl ammonium chloride, fatty alcohol-polyoxyethylene ether, citric acid and tetrahydrofurfuryl acrylate. The fracturing fluid can be directly prepared from the flow-back fluid, the flow-back fluid does not need to be pretreated, and repeated utilization of the fracturing flow-back fluid is achieved.

Provided are a cyanoquinoline-targeting protein degradation molecule, a preparation method therefor and a use thereof. Particularly, the present invention relates to a compound represented by general formula (I), a preparation method therefor, a pharmaceutical composition comprising the compound, and a use of the compound as a protein degradation targeting chimera of an androgen receptor in preparation of medicaments for treating related diseases (including prostate cancer, breast cancer, and spinal and bulbar muscular atrophy) controlled by the androgen receptor, wherein the definitions of the substituents in general formula (I) are the same as those in the description.

The present application relates to the technical field of small molecule drugs, in particular to a isoquinoline drug and its application in improving or treating digestive tract tumors, and aims to provide a compound, a pharmaceutical composition containing the compound and its application in treating colorectal cancer and gastric cancer, and provides a 3,13-position substituted berberine derivative, the drug itself has less toxicity and does not affect the growth of normal human cells, and has a good application prospect in the development of novel antitumor drugs, especially in the development of anti-digestive tract tumor drugs.

The present invention provides a fiber structure having excellent antibacterial properties and washing durability, and a method for producing the same. [Solution] A textile structure having polyamide fibers and containing a dye, a quinoline-based compound, and a phenol derivative, wherein the textile structure contains 0.04% by mass or more of the quinoline-based compound relative to the mass of the textile structure, and even after 10 standard washes in accordance with the "SEK Mark Textile Product Washing Method," the textile structure contains 0.04% by mass or more of the quinoline-based compound relative to the mass of the textile structure, and 0.20% by mass or more and 4.00% by mass or less of the phenol derivative relative to the mass of the textile structure.

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 invention discloses a synthesis method of a quinoline compound, which comprises the following steps: carrying out [4 + 2] cyclization reaction on a compound 1 and a compound 2 in an organic solvent at 90-110 DEG C, and purifying to obtain the target quinoline compound. According to the method disclosed by the invention, the intermediate is generated from enaminone under a high-temperature condition, then the intermediate reacts with the reactant 1 to obtain a new intermediate, then the new intermediate is subjected to intermolecular cyclization and dehydration to obtain the target product, the reaction is green, no additive or catalyst is needed, and the reaction condition is mild.

The application discloses a quinoline small molecule blended modified polymer dielectric material and a preparation method and application thereof, and belongs to the technical field of capacitor films. The preparation raw materials comprise quinoline derivatives, polymethyl methacrylate, styrene-methyl methacrylate copolymer, polyetherimide, polypropylene and N-methyl pyrrolidone solution, and the preparation steps comprise blending and film preparation. The blending solution or eutectic mixture is prepared through blending, and the polymer dielectric film is prepared through a flow casting method or bidirectional stretching. The prepared quinoline small molecule blended modified polymer dielectric film has excellent electrical properties, can reduce the leakage current of the polymer material, has high DC breakdown field strength, high energy storage density and low energy loss, and is easy to realize large-scale production.

The present invention relates to a Ru-Ni bimetallic catalyst for the selective hydrogenation of a quinoline organic hydrogen storage carrier, and a preparation method therefor and the use thereof. In the catalyst, carbon nitride is used as a carrier, and metal nanoparticles Ru and Ni serve as active components and are jointly loaded on the carbon nitride carrier; and the carbon nitride is prepared by mixing carbon tetrachloride, ethidene diamine and nano-silica, reacting same to obtain a carbon nitride polymer, then calcining same at 750-850ºC, performing a desilicification treatment, and then filtering and drying same. The catalyst provided in the present application has good catalytic hydrogenation performance in the selective hydrogenation of the quinoline organic hydrogen storage carrier and can achieve the omission of a solvent in a reaction system; the reaction is simple, green and environmentally friendly, and the gravimetric hydrogen storage density of the system can be maximally ensured when a quinoline compound is used as an organic hydrogen carrier; moreover, the catalyst also has a good cycling stability.

Disclosed is a quinoline compound and a use thereof. A quinoline derivative of the present invention is a compound having phosphodiesterase 3A (PDE3A) inhibitory activity, has important potential therapeutic value, and is used in the treatment of cerebrovascular diseases or in dementia drugs.

This invention provides an aminoisoquinoline derivative and its application in the preparation of antiviral drugs. The invention reveals that the aminoisoquinoline derivative exhibits significant inhibitory effects against various RNA and DNA viruses, demonstrating broad-spectrum activity. This small-molecule inhibitor has low toxicity and does not affect the normal growth of host cells. It shows good antiviral efficacy even at low concentrations. The results of this invention indicate that the compound has the potential to be used in the preparation of antiviral drugs and has promising clinical application prospects.

The invention relates to chloropyrrolo [4, 3, 2-de] quinoline alkaloids as well as a preparation method and application thereof. The structural formula of the quinoline alkaloid is shown in the specification. The obtained chloro-pyrrolo [4, 3, 2-de] quinoline alkaloids I-1-I-20 have anti-plant virus activity, and especially can inhibit tobacco mosaic virus and potato Y virus. The invention develops an efficient synthesis method of the pyrrolo [4, 3, 2-de] quinoline derivative, and lays a foundation for biological activity research of the pyrrolo [4, 3, 2-de] quinoline compound. # imgabs0 #

The invention relates to an inhibitor containing quinoline derivatives as well as a preparation method and application of the inhibitor. In particular, the present invention relates to a compound containing quinoline derivatives, a preparation method thereof, a pharmaceutical composition containing the compound, and a use thereof in treatment of cancer diseases.

The application belongs to the field of chemical medicines, and particularly relates to a quinoline compound, a preparation method and use thereof and a pharmaceutical composition thereof. The application provides a quinoline compound shown in formula I, which has excellent DNA methyltransferase 1 (DNMT1) inhibitory activity and good selectivity, can be used as a novel DNMT1 inhibitor, and provides a new option for drug development and application of diseases driven by DNMT1. Formula I.

The present invention relates to quinoline-based compounds. The compounds of the invention are suitable for the prevention and / or treatment of a disease such as a helminthic infection. The compounds of the invention are in particular suitable for the long-term prevention and / or treatment of a disease. Further, the invention relates to a pharmaceutical composition which can also be used to prevent and / or treat a disease, in particular in long-term.

The invention relates to the technical field of small molecule drugs, in particular to an isoquinoline drug and application thereof to improvement or treatment of fungal infection. The isoquinoline medicine has good bacteriostatic activity on candida albicans, further research and observation of the compound have an inhibition effect on adhesion, hypha formation, biofilm formation, pathogenicity and the like of the candida albicans, and the result shows that the 10, 13-substituted berberine derivative can be used for preventing and / or treating fungal infection, especially candida albicans infection.

The present invention relates to compounds of formula (I) which are inhibitors of activin receptor-like kinase 5 (ALK5) and related uses.

Disclosed are compounds of Formula I, methods of using the compounds for inhibiting KRAS activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with KRAS activity such as cancer.

The application belongs to the technical field of rubber, and particularly relates to an environment-friendly weather-resistant high-wear-resistance handrail belt rubber material and a preparation method thereof. The rubber material comprises, in terms of weight parts, 80-95 parts of styrene-butadiene rubber, 5-20 parts of butadiene rubber, 70-90 parts of carbon black, 6-9 parts of active agent, 3-5 parts of environment-friendly paraffin oil or naphthenic oil, 4-7 parts of anti-aging agent composition, 1-2 parts of accelerator and 1.5-2.5 parts of vulcanizing agent. The anti-aging agent composition is a combined system of p-phenylenediamine anti-aging agent and quinoline anti-aging agent. Through the synergistic effect of the rubber combined system, the gradation optimization of the reinforcing system and the synergistic effect of the anti-aging agent composition, the application simultaneously realizes high wear resistance, excellent weather resistance (ozone and thermal oxygen aging resistance), low-temperature toughness at-45 DEG C and environment-friendly performance of PAHs <= 10 ppm, and the comprehensive performance is significantly better than that of the existing handrail belt material, and the eight-year service life requirement of public places can be met.

The invention provides an application of a quinoline derivative as shown in a formula (1) in preparation of drugs for treating acute lung injury and resisting inflammation. It is found for the first time that the quinoline derivative has the function of a P2Y6R antagonist, has an obvious antagonistic effect on P2Y6R-related inflammation and can be used for preparing P2Y6R-related anti-inflammatory drugs.

The invention belongs to the technical field of pesticide chemistry, and relates to a quinoline derivative containing a piperazine structure and a preparation method and application thereof. The invention provides a quinoline derivative containing a piperazine structure, and the quinoline derivative has broad-spectrum inhibitory activity on phytopathogens such as plant pathogenic fungi, especially has excellent inhibitory activity on valsa mali, sclerotinia sclerotiorum, botrytis cinerea, gaeumannomyces graminis and magnaporthe oryzae. The bactericide is expected to be developed into a novel green bactericide which is efficient, safe, economical and environment-friendly.

The present invention provides phthalide isoquinoline alkaloids and pharmaceutically acceptable salts thereof and applications thereof, pharmaceutical compositions and applications thereof, and relate to the field of biomedical technology. The phthalide isoquinoline alkaloids and pharmaceutically acceptable salts thereof provided by the present invention have the same chirality at C-1, C-9 and C-7', can significantly promote the occurrence of autophagic flux, are low-toxic and low-side-effect autophagic activators with development potential, are of great significance for the development of drugs for the treatment of neurodegenerative diseases, and have good application prospects in the application of drugs for the treatment of diseases related to autophagic flux and in the preparation of AMPK agonists. The preparation method of the phthalide isoquinoline alkaloids provided by the present invention does not require chemical synthesis, and is obtained by extracting the summer corms as a traditional bulk medicinal material as a raw material. The raw material source is wide, the acquisition is convenient, the cost is low, it conforms to the concept of inheritance and development of traditional Chinese medicine, the operation is simple, the production cost is low, and it is suitable for industrial production.

The invention relates to the field of biological medicine, in particular to a benzofuran [2, 3-b] quinoline derivative as well as a preparation method and application thereof in resisting renal fibrosis. The structure of the benzofuran [2, 3-b] quinoline derivative, the optical isomer thereof or the pharmaceutical salt thereof is shown as a formula (I): # imgabs0 #, wherein R1 is selected from C1-C8 alkoxy, halogen, a 3-8 membered aliphatic heterocyclic ring, a substituted 3-8 membered aliphatic heterocyclic ring and-NR3R4; r2 is selected from = O, hydroxyl and hydrogen; the substituent group of the substituted 3-8-membered aliphatic heterocyclic ring is selected from C1-C8 alkyl, C1-C8 alkyl ester group, = O and 3-8-membered aliphatic ring. A plurality of derivatives with novel structures are synthesized, the derivatives have the potential of becoming anti-renal fibrosis drugs, renal fibrosis is relieved by dual regulation and control of TGF-beta1 / Smad2 / Smad3 and PI3K / AKT signal pathways, and a new strategy and thought are provided for treatment of CKD.

The application relates to the preparation field of quinoline compounds and discloses a method for preparing a quinoline compound shown in formula (I), which comprises the following steps: in the presence of inert high-boiling-point polyether solvents, substituting a compound shown in formula (III) with 3,5-dichloroaniline to obtain a compound shown in formula (II), and then performing ring closure reaction to obtain the compound shown in formula (I), wherein X1, X3, X4, X5 and X6 are each independently -CN or -COOR'; R' is C1-C4 alkyl; wherein X1 is same as at least one of X3, X4, X5 and X6; X3 and X4 are same or different, X5 and X6 are same or different; X2 is a hydroxyl group or an amino group; R1 and R2 are each independently hydrogen or C1-C4 alkyl; and R1 and R2 are same or different. The method has the advantages of low reaction temperature, low cost and high yield, and is beneficial to industrialization.

The invention discloses a substituted quinoline compound and a preparation method and application thereof.The preparation method includes the steps that thionyl chloride and a specific intermediate react, DCM and other solvents are adopted, and pyridine, polyphosphoric acid, ethyl alcohol, acetyl chloride and other reagents are used in the reaction process. The structure of the obtained product is confirmed by a nuclear magnetic hydrogen spectrum, bactericidal activity tests are carried out on the obtained 29 target products, and the results show that the compound has a significant inhibition effect on a variety of plant pathogens at a concentration of 50 ppm, and especially shows excellent bactericidal activity in the aspects of pyricularia grisea, sclerotinia sclerotiorum and the like. In addition, the compounds have certain herbicidal activity.

The application discloses a catalytic synthesis method of chiral polysubstituted hydrogenated quinoline compounds, and belongs to the field of organic synthesis. The application comprises the following steps: at 0-40 DEG C, alcohol or halogenated alkane is used as a solvent, a copper metal catalyst and a chiral ligand are added, and reaction is carried out under nitrogen protection for 0.5-2 hours; the temperature is lowered to-60-0 DEG C; then, o-aminophenyl nitrone, propargyl alcohol ester and alkali are sequentially added; and reaction is carried out for 6-48 hours, so as to obtain a chiral polysubstituted hydrogenated quinoline compound shown in formula 1 or 2. The application realizes, for the first time, synthesis of chiral polysubstituted hydrogenated quinoline compounds by using o-aminophenyl nitrone and propargyl alcohol ester as reactants, and by using a cheap copper metal catalyst and a chiral ligand, the method is simple in operation, low in cost, and has excellent enantioselectivity and diastereoselectivity.

The present invention relates to novel 1-arylisoquinoline compounds and their use in preparing anti-plant pathogenic fungicides. These isoquinoline compounds have the structure of Formula (I): #imgabs0#, wherein Ar is selected from aromatic groups such as benzene, naphthalene, biphenyl, thiophene, furan, pyrazole, thiazole, and pyridine; and R1-R4 is selected from hydrogen, halogen, hydroxyl, trifluoromethyl, C1-C6 alkyl, and C1-C6 alkoxy. The compounds described herein exhibit significant inhibitory activity against various plant pathogenic fungi and can be used to prepare fungicides for controlling crop diseases.

The invention provides a 2, 8-disubstituted quinoline macrocyclic compound with a structure as shown in a formula I or a pharmaceutically acceptable salt or a stereoisomer thereof, and a preparation method and application of the 2, 8-disubstituted quinoline macrocyclic compound. Compared with a 2, 8-disubstituted quinazoline lead compound, the 2, 8-disubstituted quinoline macrocyclic compound disclosed by the invention has better PDGFR alphaD842V kinase inhibition activity and anti-tumor effect, also has better inhibition effect on PDGFR alphaD842V / G680R mutant kinase and PDGFR alphaG680R mutant kinase, shows very strong anti-proliferative activity in corresponding Ba / F3-PDGFR alpha stable strain cells, and can be used for preparing anti-tumor drugs. The compound can play a good role in inhibiting tumor cells, and can be used for preparing drugs for preventing or treating PDGFRalpha kinase mediated diseases (such as tumors). # imgabs0 #