84 results about "Quinolinium Compounds" patented technology

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

The application discloses a trifluoromethyl alkyl quinoline compound, a synthesis method and anti-tumor application in the field of organic synthesis and medicinal chemistry, which is synthesized from trifluoropropylene quinoline or N-benzoyl pyrrole (A) and redox active ester (B) as raw materials, dimethyl sulfoxide as a solvent, dihydropyridine as an electron donor, and under visible light irradiation, a trifluoromethyl alkyl quinoline and analogues (C) are synthesized at a high yield. The specific reaction formula is as follows: The compounds provided by the application all have excellent anti-tumor activity and low toxicity to normal cells, and therefore have application prospects for preparing anti-tumor drugs.

The invention disclosed herein relates to a method for treating a disease or condition mediated by Enhancer of Zeste Homolog 2 (EZH2), Polycomb Repressive Complex 2 (PRC2), or a combination EZH2 and PRC2, comprising administering to a subject in need thereof a therapeutically effective amount of the compound of Formula (I), or a stereoisomer, enantiomer, enantiomeric mixture or a pharmaceutically acceptable salt thereof;

The present invention provides a salt of a dioxane quinoline compound, a crystal form thereof, preparation methods therefor and uses thereof. Specifically, the present invention relates to N-(3-fluoro-4-((5-(3-morpholinopropoxy)-2,3-dihydro-[1,4]dioxano[2,3-f]quinolin-10-yl)oxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, a crystal form thereof and preparation methods therefor, and uses in the preparation of a drug as an inhibitor of tyrosine kinases (e.g. VEGFR-2 and c-MET, etc.).

The present invention provides a method for preparing polysubstituted 1,2,3,4-tetrahydroquinoline, which relates to the technical field of the synthesis of chemical intermediates for medicines and natural compounds. In the present invention, o-N-acylphenyl MBH carbonate and an unsaturated olefin are used as raw materials, and under the action of a Lewis base catalyst, a [4+2] cycloaddition reaction occurs in an organic solvent to generate a polysubstituted 1,2,3,4-tetrahydroquinoline compound. The diastereoselectivity and regioselectivity of the product are high. Without the need for a metal catalyst, the reaction product can be obtained in one step. The reaction conditions are mild, and it only needs to be stirred at room temperature in an organic solvent. The raw materials are easily available, the cost is low, the process is stable and the yield is high. The operation and post-treatment are simple. Moreover, the product can be prepared in gram scale and further derivatized and transformed, providing a reference for drug research and development.

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.

Isoquinoline compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an isoquinoline compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions / disorders / diseases due to mutations or dysregulation of the Wnt pathway and / or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.

The present disclosure provides compounds containing a 6-(pyrimidin-4-yl) quinoline structure, their use for selective inhibition of CDK4 activity, and pharmaceutical compositions comprising these compounds that can treat various diseases, including cancer.

The present disclosure provides compounds containing a 6-(pyrimidin-4-yl) quinoline structure, their use for the selective inhibition of CDK4 activity, and pharmaceutical compositions comprising the compounds as the treatment of various diseases, including cancer.

Provided aza-quinoline compounds of Formula (I), pharmaceutical compositions comprising such compounds; and the use of such compounds for treating a disease or condition mediate by Enhancer of Zeste Homolog 2 (EZH2), Polycomb Repressive Complex 2 (PRC2), or a combination thereof.

The invention discloses a kind of 3 trifluoromethyl tetrahydroquinoline compound and its preparation method, belong to the field of organic synthesis technology. The present invention introduces trifluoromethyl group directly into tetrahydroquinoline compound, combines the important medicinal value of tetrahydroquinoline compound and the characteristic that trifluoromethyl can enhance the biological activity of compound. The present invention also provides a kind of preparation method of 3 trifluoromethyl tetrahydroquinoline compound, with N alkenyl aniline as raw material, with cheap and easily available CF3Br as trifluoromethyl source, under the action of visible light induction and photocatalyst and alkali, by the intramolecular free radical tandem cyclization reaction of olefin, one-step synthesis contains trifluoromethyl tetrahydroquinoline compound, and obtains mainly 3 trifluoromethyl tetrahydroquinoline compound, simultaneously with the characteristics such as simple reaction steps, high atom utilization rate, simple operation, mild reaction conditions and high reaction yield.

Provided is a plant disease control composition having a broad spectrum against various plant pathogens, and shows excellent controlling effects (synergistic controlling effects) which cannot be expected from a single component alone. The plant disease control composition includes (Group a) at least one quinoline compound represented by the formula:(wherein R1, R2: an alkyl which may be substituted, an aryl which may be substituted, etc.; R3, R4: H, an alkyl which may be substituted, etc.; X: halogen, an alkyl which may be substituted, etc.; Y: halogen, alkyl, etc.; n: 0 to 4; m: 0 to 6) or a salt thereof, and at least one of fungicidal compounds selected from the group consisting of a Strobilurin series compound, a triazole series compound, etc., as effective ingredients.

3H-pyrazolo[4,3-f]quinoline compounds that inhibit interferon gene-stimulating factor (STING); compositions comprising the same compounds; and their use for the treatment of STING-related diseases, such as STING-related inflammatory diseases, autoimmune diseases, diabetes, cancer, traumatic brain injury, and fibrosis.

The present invention provides novel quinoline compounds that are inhibitors of mitochondrial RNA polymerase for treating various diseases such as cancer and others associated with metabolic disorders and mitochondrial dysfunction.

The present invention relates to a tetrahydroquinoline compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein A is a (C3-C7) cycloalkyl; a (C3-C7) heterocycloalkyl group comprising from 1 to 3 heteroatoms selected from the group consisting of O, N and S; (C1-C7) alkyl groups; a (C1-C7) heteroalkyl group comprising from 1 to 3 heteroatoms selected from the group consisting of O, N and S; an optionally substituted benzene ring or an optionally substituted (5-9) membered heteroaromatic ring comprising from 1 to 3 heteroatoms selected from the group consisting of O, N and S; r is H, (C1-C4) alkyl, (C1-C3) alkoxy (C1-C3) alkyl, (C3-C7) cycloalkyl; r1 and R2 are independently selected from the group consisting of H, NO2, CN, halogen, (C1-C4) alkyl, (C2-C4) alkenyl, (C1-C4) alkoxy (C1-C4) alkyl, (C3-C7) cycloalkyl (C1-C4) alkyl, (C1-C4) alkyl substituted by a (5-9) membered heteroaromatic ring comprising from 1 to 3 heteroatoms selected from O, N and S, amino optionally substituted by bis (dimethylamino) methylene, pyridyl, trifluoromethyl-SO2-, (C1-C3) alkyl-SO2-, a group NH-CO-R3, wherein R3 is selected from the group consisting of benzyl, (C3-C7) cycloalkyl (C1-C4) alkyl, phenyl, vinyl, halo-CH2-, (C1-C3) alkyl; a group NH-CH2-R4, wherein R4 is an optionally substituted benzene ring or an optionally substituted (5-9) membered heteroaromatic ring comprising from 1 to 3 heteroatoms selected from O, N and S; or R1 and R2 together form an optionally substituted aromatic ring comprising 6 carbon atoms. The tetrahydroquinoline compound according to the invention or a pharmaceutically acceptable salt thereof is a disrupting agent of the FANCM / BTR interaction in order to hinder the localization of FANCM at the telomere, preferably in the treatment of tumors. # imgabs0 #

The invention belongs to the technical field of medicines, and particularly relates to a quinoline compound with an integrin alpha5beta1 inhibition function and application of the quinoline compound in fibrosis and fibrosis-related diseases. Specifically, the invention provides a compound, and the compound has a structural general formula as shown in the specification or a pharmaceutically acceptable salt, solvate or hydrate thereof: # imgabs0 #. The compound has obvious inhibitory activity on integrin alpha5beta1, so that the compound can be used for obstacles, diseases or symptoms mediated by the integrin alpha5beta1, and tests prove that the compound has an obvious treatment effect on various fibrosis diseases, so that the compound has a good practical application value.

The application provides a temperature-sensitive helical polymer based on a quinoline structure and a preparation method and application thereof, and relates to the technical field of organic synthesis.The preparation method of the temperature-sensitive helical polymer based on the quinoline structure comprises the following steps: synthesis of 8-(aminomethyl)-4-isobutoxyquinoline-2-carboxylic acid polymer; crude product purification; and synthesis of chiral 8-(aminomethyl)-4-isobutoxyquinoline-2-carboxylic acid polymer.The length of the helical structure is improved, and the transmission performance of the helical structure as an artificial ion channel is improved.In the synthesis of the temperature-sensitive compound, a functionalized quinoline compound is innovatively used as a structure main body of a helical molecule, a series of homopolymers are formed through a PyBOP polymerization mode, and the existence of the benzyl group in the helical structure unit makes the polymer with the helical structure have repeatable and stable responsiveness to temperature, so that the polymer can be used for preparing a temperature-sensitive ion channel.

The invention discloses a preparation method for synthesizing trifluoromethyl-substituted chromonoquinoline, comprising the steps of adding a palladium catalyst, a ligand, norbornene, an additive, trifluoroethylimidoyl chloride, and 3-iodochromone to an organic solvent, reacting at 110 to 130° C. for 16 to 30 hours, and after completion of the reaction, post-processing to obtain the trifluoromethyl-substituted chromonoquinoline compound. The preparation method is simple to operate, has inexpensive and readily available starting materials, high reaction efficiency, and a wide substrate range. Trifluoromethyl-substituted chromonoquinoline compounds substituted with different groups can also be synthesized through substrate design, thereby facilitating operation and broadening the practicality of the method.

Imidazo[4,5-c]quinoline compounds having a substituent that is attached at the N-1 position by a branched group, single enantiomers of the compounds, pharmaceutical compositions containing the compounds, and methods of making the compounds are disclosed. Methods of use of the compounds as immune response modifiers, for inducing cytokine biosynthesis in humans and animals, and in the treatment of diseases including infectious and neoplastic diseases are also disclosed.

The invention discloses a catalytic synthesis method of a chiral polysubstituted hydroquinoline compound, and belongs to the field of organic synthesis. The method comprises the following steps: at 0-40 DEG C, respectively taking alcohol or halogenated hydrocarbon as a solvent, adding a metal copper catalyst and a chiral ligand, reacting for 0.5-2 hours under the protection of nitrogen, cooling to-60-0 DEG C, then sequentially adding o-aminophenyl nitrone, propargyl alcohol ester and alkali, and reacting for 6-48 hours to obtain the chiral polysubstituted hydroquinoline compound as shown in a formula 1 or 2. According to the present invention, the chiral polysubstituted hydroquinoline compound is synthesized by using the o-aminophenyl nitrone and the propargyl alcohol ester as the reactants through the catalysis of the cheap metal copper catalyst and the chiral ligand, and the method has advantages of simple operation, low cost, excellent enantioselectivity and excellent diastereoselectivity. # imgabs0 #

The present invention relates to a compound of Formula (I), or pharmaceutically acceptable salt thereof, wherein the variables are as defined herein. The invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating plasmodium related diseases such as malaria.

The invention discloses a bridged biquinoline compound and a preparation method and application thereof.The compound has a certain killing effect on colon cancer cells, lung cancer cells, liver cancer cells, gastric cancer cells, cervical cancer cells and breast cancer cells, the killing effect on the colon cancer cells is especially obvious, and the killing effect on the colon cancer cells is remarkably superior to that of positive control drugs chloroquine and cis-platinum; in addition, the bridged biquinoline compound has small toxic and side effects, solves the problem of large toxic and side effects of traditional platinum antitumor drugs such as cis-platinum and the like, and can be prepared into antitumor drugs for application. The preparation method of the bridged biquinoline compound is simple and efficient, industrial production can be realized, and the bridged biquinoline compound has great application value in tumor resistance.

The purpose of the present invention is to provide an adsorbent for removing a first transition metal, a method for producing an adsorbent, an adsorption cartridge containing an adsorbent, a method for removing a first transition metal by using an adsorption cartridge, and a method for producing an aqueous solution from which a first transition metal has been removed by using an adsorption cartridge.　An adsorbent for removing a first transition metal from an aqueous solution containing the first transition metal, said adsorbent containing activated carbon which supports a quinolinol compound or a dihydroxynaphthalene compound therein, wherein the supported amount of the quinolinol compound or the dihydroxynaphthalene compound relative to 1g of the activated carbon is 300-1,750 μmol / g.

The application discloses a heating-promoted synthesis method of 2-trifluoromethyl-substituted quinoline compounds, which comprises the following steps: adding trifluoroacetimidate sulfonium leaf, amine and triphenylphosphine difluoroacetate into an organic solvent, and reacting at 70-90 DEG C for 20-30 hours; after the reaction is completed, post-treatment is carried out to obtain the 2-trifluoromethyl-substituted quinoline compounds. The preparation method is simple in operation, the starting material is cheap and easy to obtain, the reaction does not need any catalyst and additive, and only needs ordinary heating in an air atmosphere to smoothly proceed, so that the application of the method is widened, the method meets the concept of green chemistry, and has good atom economy.

The invention provides a synthesis method of an indazolo [2, 3-a] quinoline compound, which is characterized in that o-nitrobenzaldehyde and aniline are taken as starting raw materials, and the indazolo [2, 3-a] quinoline compound with various substituent groups is successfully synthesized through three-step reaction of synthesis of 2-aryl indazole, synthesis of 3-bromo-2-aryl indazole and synthesis of the indazolo [2, 3-a] quinoline compound. And by introducing the halogenated 2-phenyl indazole intermediate, the yield is remarkably improved. The synthesis method provided by the invention has the advantages of cheap and easily available raw materials, mild reaction conditions and good industrialization prospects.

Disclosed herein are new dosage regimens for deuterium-substituted benzoquinoline compounds, and methods for the treatment of abnormal muscular activity, movement disorders, and related conditions.

The invention relates to a synthesis method of a quinoline meta-carboxylated derivative. The chemical structural formula of the derivative is shown as a formula 3. The synthesis method comprises the following steps: by taking a compound quinoline nitrogen-oxide in a formula 1 and a compound butynedioic acid diester in a formula 2 as reaction raw materials, adding a dehydrating agent molecular sieve, and finally adding a tetrahydrofuran solvent for heating and stirring reaction; and after TLC monitors that the quinoline nitrogen-oxide compound shown in the formula 1 is completely converted, transferring a reaction solution to a silica gel plate by using a dropper, expanding PE / EA until the Rf value is 0.2-0.4, airing the silica gel plate at room temperature, scraping off and collecting silica gel, eluting by using DCM / EA, evaporating out a solvent, and purifying to obtain the quinoline nitrogen-oxide compound shown in the formula 1. According to the method, meta-position carboxylation of the quinoline compound is completed through one-pot synthesis, the method has the advantages of being high in atom economy, mild in reaction condition, environmentally friendly, low in cost, high in conversion rate and the like, meanwhile, later functional group modification is directly conducted on a molecular skeleton, and a new thought can be provided for later design optimization of medicine molecules.

The invention discloses a method for preparing a quinoline compound, which comprises the following steps: by taking an o-amino aryl alkynol compound as a raw material and 1, 2-dichloroethane as a solvent, realizing electrochemical participated cyclization reaction of the o-amino aryl alkynol compound, and reacting under the action of electrochemical oxidation reduction to obtain the quinoline compound. Under the condition of no catalyst, oxidant and additive, the reaction is carried out by using the cheap and easily available o-amino aryl alkynol compound as the raw material only through the electrode redox effect, the self-cyclization reaction of the o-amino aryl alkynol is realized, and the target product quinoline compound is smoothly obtained; 1, 2-dichloroethane is preferably selected as a solvent in the reaction, the reaction condition is mild, the operation is simple, and the method has the advantages of economy, greenness and high efficiency.