61 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 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 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.

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 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 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 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.

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.

This invention discloses a cobalt-catalyzed migration asymmetric spirocyclic cyclocyclization method for quinoline compounds. This method utilizes a cobalt and ligand combination catalysis to achieve migration asymmetric spirocyclic cyclocyclization of quinoline compounds, belonging to the fields of organic chemistry and medicinal chemistry. Under the influence of a cobalt source, chiral ligands, achiral ligands, reducing agents, and additives, this invention enables the reaction of aryl / alkenyl-substituted quinolines / intramolecularly migrating quinolines with different alkynes in organic solvents, yielding a series of spirocyclic chiral dihydroquinoline compounds with excellent enantioselectivity and good yields. This invention only requires different ligands to regulate the reaction, enabling migration asymmetric dearomatization spirocyclic cyclocyclization from aryl to aryl, migration asymmetric dearomatization spirocyclic cyclocyclization from aryl to alkenyl, and intramolecular migration asymmetric dearomatization spirocyclic cyclocyclization reactions. It has a wide substrate applicability and produces diverse product structures, providing a novel and universal method for the systematic synthesis of chiral spirocyclic dihydroquinoline compounds.

The invention disclosed herein relates to azaquinoline compounds of formula (I), pharmaceutical compositions containing such compounds; and the use of such compounds to treat diseases or conditions mediated by Enhancer of Zeste Homolog 2 (EZH2), Polycomb Repressive Complex 2 (PRC2), or a combination thereof. [Case 1] TIFF2023538159000045.tif2859

Formula (I): TIFF2025538180000077.tif32153 (wherein L, R1, R2, R3 and R4 are defined herein) or a salt thereof. Also disclosed are methods of using the compounds as inhibitors of TLR9, and pharmaceutical compositions containing the compounds. These compounds are useful for treating, preventing, or slowing the progression of fibrosis.

The invention discloses a synthesis method of a chiral 1-aryl isoquinoline compound, namely a synthesis method of a chiral 1-aryl isoquinoline compound QUINOLs and a synthesis method of a chiral 1-aryl isoquinoline compound QUINAPs. According to the synthesis method, the chiral 1-aryl isoquinoline compound QUINOLs with pure enantiomers is efficiently constructed from a racemic 1-aryl isoquinoline compound under the mild conditions of heating and no inert gas protection, and the chiral 1-aryl isoquinoline compound QUINOLs is used as a raw material and is synthesized in the presence of a catalyst and a ligand which are cheap and easy to obtain, so that the chiral 1-aryl isoquinoline compound QUINOLs with pure enantiomers is obtained. The chiral 1-aryl isoquinoline compound QUINAPs can be obtained through derivation. The method provided by the invention has the advantages of mild conditions, no need of expensive metals and chiral ligands, simple operation and industrial application prospects.

This disclosure provides compounds containing 6- (pyrimidin-4-yl) quinoline structure, the use thereof for selectively inhibiting the activity of CDK4, and pharmaceutical compositions comprising the compounds as treatment of various diseases including cancer.

The invention relates to a tetrahydroquinoline compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein A is (C3-C7)cycloalkyl; (C3-C7)heterocycloalkyl comprising from 1 to 3 heteroatoms selected from O, N, and S; (C1-C7)alkyl, (C1-C7) heteroalkyl comprising from 1 to 3 heteroatoms selected from O, N, and S; an optionally substituted phenyl ring or an optionally substituted (5-9)-membered heteroaromatic ring comprising from 1 to 3 heteroatoms selected from O, N, and S; R is H, (C1-C4) alkyl; (C1-C3)alkoxy(C1-C3)alkyl, (C3-C7)cycloalkyl; R1 and R2 are, independently from each other, 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 with bis(dimetilamino)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, halogen-CH2—, (C1-C3)alkyl; a group NH—CH2—R4 wherein R4 is an optionally substituted phenyl 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 of or a pharmaceutically acceptable salt thereof according to the invention is a disruptor of the FANCM / BTR interaction so as to hamper the FANCM localization to telomeres, preferably in the treatment of tumours.