36 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 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.).

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.

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 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.

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.

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.

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.

The present invention relates to a fuel composition comprising at least 50% by mass, relative to the total mass of the composition, of one or more paraffinic hydrocarbon cuts consisting of fatty acids and / or hydrogenated fatty acid esters (HEFAs) and at least 0.05% by mass, relative to the total mass of the composition, of one or more compounds corresponding to formula (I) or formula (II) below: (I), (II). This composition is useful for powering any internal combustion engine of a land, sea, air or space vehicle and in particular an aircraft or rocket engine.

This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a quindoline (or similar) structure which function as stabilizers of G-quadruplex (G4) formation, and their use as therapeutics for the treatment of cancer (e.g., castration-resistant prostate cancer), and other conditions mediated by G4 stabilization.

The present invention covers new quinoline compounds of general formula (I):in which A, R1, R2, R3, R4, R5, R6, and Q are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment, control and / or prevention of diseases, in particular of helminth infections, as a sole agent or in combination with other active ingredients.

The present invention provides a salt of a dioxanequinoline compound, its crystalline form, its preparation method, and its use. 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, its crystalline form, its preparation method, and its use in preparing a medicament as a tyrosine kinase (e.g., VEGFR-2, c-MET, etc.) inhibitor. [C1] TIFF2025541949000023.tif43156

Quinoline compounds are disclosed that have a formula represented by the following; and wherein Cy, R1, R4a, R4b, and n are as described herein. The compounds may be prepared as compositions, e g., pharmaceutical compositions, or as dosage forms, e.g., pharmaceutical dosage forms, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, diabetes complications, inflammation, and neurodegeneration, obesity, cancer, ischemia / reperfusion injury, cardiovascular disease, COVID-19 complications, and other diseases related to RAGE activity.

This invention belongs to the field of organic synthesis and relates to a green synthetic method for tetrahydroquinoline compounds. The method uses 2,9-dimethyl-1,10-phenanthroline as a ligand and zinc powder as a reducing agent under a carbon dioxide atmosphere to selectively reduce and construct the tetrahydroquinoline skeleton. This strategy does not require high-pressure hydrogen or precious metal catalysts, the reaction conditions are mild, and the safety risks are low. Compared with existing technologies, this invention has the following advantages: First, it is green and environmentally friendly, using carbon dioxide as the reduction promoting medium, resulting in fewer byproducts; second, it is economical and efficient, using inexpensive zinc powder instead of precious metal catalysts, resulting in low raw material costs, simple operation, and suitability for industrial applications; third, it has excellent selectivity, accurately reducing the target site, ensuring product purity and yield; fourth, the conditions are mild, requiring no high-pressure equipment, and the process is easy to scale up. This invention provides a safe, economical, and green new synthetic route for tetrahydroquinoline compounds, which has important application value in the fields of organic synthesis and pharmaceutical intermediate preparation.

The invention relates to fungicidal mixtures comprising at least one substituted quinoline (compound I) and at least one active compound II in a weight ratio of 15: 1 to 1: 15.

To provide quinoline compounds or salts thereof. [Solution] A quinoline compound or a salt thereof having a structure represented by a specific formula (I): a compound having a structure in which an E3 ubiquitin ligase binding domain is linked to the 6th position of the quinoline skeleton via a linker, a compound having a structure in which an E3 ubiquitin ligase binding domain is linked to the 5th position of the quinoline skeleton via a linker, or a compound having a structure in which an E3 ubiquitin ligase binding domain is linked to the 8th position of the quinoline skeleton via a linker.

The invention provides a novel preparation method of a pyrazoloquinoline compound, which comprises the following step: reacting a 1, 6-eneyne compound with a hydrazine compound under the condition of normal-pressure air to generate the pyrazoloquinoline compound. The synthesis method is simple and rapid in preparation process, and does not need inert gas protection and use of a catalyst, so that the synthesis method is expected to be used for industrial production.

The invention discloses a method for producing quinoline nitrogen oxide, a catalyst and a synthesis method of the catalyst. The method comprises the following steps: carrying out nitrogen oxidation reaction on a quinoline compound and an oxidizing agent under the action of a catalyst to obtain quinoline nitrogen oxide; the catalyst is a titanium-silicon mesoporous material, and the average pore size of the catalyst is 2-30nm; wherein all titanium elements exist in the form of tetra-coordinated titanium. The method has the advantages of simple preparation process, mild conditions, green reaction conditions, high selectivity of quinoline nitrogen oxide and easiness in product separation.

The present invention relates to compounds of Formula I, processes for their preparation, pharmaceutical compositions containing them as active ingredients, methods of treating disease conditions associated with protein kinase related cancers, their use as medicaments for producing an inhibitory effect on the reduction of mTor, pi3k in warm-blooded animals such as humans.