163 results about "Aminoquinoline" patented technology

The present invention is concerned with compounds of the general Formula I: and pharmaceutically acceptable salts thereof, which are useful as melanin concentrating hormone receptor antagonists, particularly MCH-1R antagonists. As such, compounds of the present invention are useful for the treatment or prevention of obesity or eating disorders associated with excessive food intake and complications thereof, osteoarthritis, certain cancers, AIDS wasting, cachexia, frailty (particularly in elderly), mental disorders stress, cognitive disorders, sexual function, reproductive function, kidney function, locomotor disorders, attention deficit disorder (ADD), substance abuse disorders and dyskinesias, Huntington's disease, epilepsy, memory function, and spinal muscular atrophy. Compounds of formula I may therefore be used in the treatment of these conditions, and in the manufacture of a medicament useful in treating these conditions. Pharmaceutical formulations comprising one of the compounds of formula (I) as an active ingredient are disclosed, as are processes for preparing these compounds.

The invention concerns an aminoquinoline-antibiotic hybrid compound of general formula (I): Q-(Y1)p-(U)p-(Y2)p-A: wherein Q represents an aminoquinoline, (Y1)p(U)p-(Y2)p'' is an optional spacer and A is an antibiotic residue. The invention enables the antibiotic residue activity to be unexpectedly enhanced.

The present invention is concerned with compounds of the general Formula I: and pharmaceutically acceptable salts thereof, which are useful as melanin concentrating hormone receptor antagonists, particularly MCH-1R antagonists. As such, compounds of the present invention are useful for the treatment or prevention of obesity or eating disorders associated with excessive food intake and complications thereof, osteoarthritis, certain cancers, AIDS wasting, cachexia, frailty (particularly in elderly), mental disorders stress, cognitive disorders, sexual function, reproductive function, kidney function, locomotor disorders, attention deficit disorder (ADD), substance abuse disorders and dyskinesias, Huntington's disease, epilepsy, memory function, and spinal muscular atrophy. Compounds of formula I may therefore be used in the treatment of these conditions, and in the manufacture of a medicament useful in treating these conditions. Pharmaceutical formulations comprising one of the compounds of formula (I) as an active ingredient are disclosed, as are processes for preparing these compounds.

The present invention is concerned with compounds of the general Formula I:and pharmaceutically acceptable salts thereof, which are useful as melanin concentrating hormone receptor antagonists, particularly MCH-1R antagonists. As such, compounds of the present invention are useful for the treatment or prevention of obesity or eating disorders associated with excessive food intake and complications thereof, osteoarthritis, certain cancers, AIDS wasting, cachexia, frailty (particularly in elderly), mental disorders stress, cognitive disorders, sexual function, reproductive function, kidney function, locomotor disorders, attention deficit disorder (ADD), substance abuse disorders and dyskinesias, Huntington's disease, epilepsy, memory function, and spinal muscular atrophy. Compounds of formula I may therefore be used in the treatment of these conditions, and in the manufacture of a medicament useful in treating these conditions. Pharmaceutical formulations comprising one of the compounds of formula (I) as an active ingredient are disclosed, as are processes for preparing these compounds.

The invention is directed to a method of inhibiting FLT3 tyrosine kinase activity or expression or reducing FLT3 kinase activity or expression in a cell or a subject comprising the administration of a farnesyl transferase inhibitor and a FLT3 kinase inhibitor selected from aminoquinoline and aminoquinazoline compounds of Formula I′: where R1, R2, R3, B, Z, Q, p, q and X are as defined herein. Included within the present invention is both prophylactic and therapeutic methods for treating a subject at risk of (or susceptible to) developing a cell proliferative disorder or a disorder related to FLT3.

The present invention relates to novel ophthalmic pharmaceutical compositions comprising an inflammation-treating amount of a 4-aminoquinoline compound, derivative, isomers, or chemical salts, and methods for using these compositions for the treatment of ocular inflammatory conditions by topical administration directly to the eye.

The invention relates to the synthesis of N-acyl-8-aminoquinoline derivatives and application thereof as fluorescent molecular probes. The invention takes 8-aminoquinoline as a matrix, can introduce substitutional groups at position 2, 4 and 5 of the quinoline matrix, and can acylate on an amino group to synthesize a series of novel acylaminoquinoline derivatives. The compounds with relatively simple structures and easy synthesis can be used for fluorescence detection of transition and heavy metal ions in solutions, show high sensitivity and selectivity, and are successfully applied to the fluorescence imaging detection of zinc ions in living cells. The compounds are expected to be widely applied in the fields such as analytical inspection of transition metal and heavy metal ions and the catalysis of metal complexes in biological tissues, cells, environment, medicine, and industrial and agricultural production and so on.

The invention relates to 3-cyan-6-aminoquinoline derivatives, a preparation method thereof and application thereof in medicines, in particular to new 3-cyan-6-aminoquinoline derivatives shown as a general formula (I) and medicinal salts thereof, and use thereof as a therapeutical agent, particularly a protein kinase inhibitor, wherein the definition of each substituent group in the general formula (I) is shown as the description. The formula (I) is shown in the description.

The invention discloses a 2-(2-pyridyl)-8-sulfonamidoquinoline derivative, a synthesis method and a method used for the fluorescence detection of metal ions in solutions and the microscopic fluorescence imaging detection of metal ions in cells. The derivative is prepared by reacting 2-(2-pyridyl)-8-sulfonamidoquinoline and a derivative thereof with sulfonyl chloride and can be used for the fluorescence detection of metal ions in water, alcohol, a DMF (dimethyl formamide) solvent or a DMSO (dimethylsulfoxide) solvent or a mixed solvent of the DMF solvent and the DMSO solvent and the microscopic fluorescence imaging detection of metal ions in microenvironments such as biological tissues, cells, and the like. The invention has the advantages that the metal ion bonding property and the light spectrum property of probe molecules are improved, and the probe molecules can selectively and fluorescently enhance the identification to metal ions such as Zn<2>+, Cd<2+>, and the like in neutral solutions containing water. The excitation wavelength of the probes is longer than 400nm, and the maximum emission wavelength reaches 600nm. The invention obtains a breakthrough progress in the aspect of promoting the working wavelength of TSQ (6methoxy8ptoluene sulfonamidoquinoline) fluorescence molecular probes to enter a visible light region.

Aminoquinoline-antibiotic hybrid compounds in the form of hybrid molecules QA, wherein Q is an aminoquinoline and A is an antibiotic or a resistance enzyme inhibitor, their synthesis and their uses as antibacterial agent. This compound is defined by the general formula (I): Q-(Y1)p—(U)p′—(Y2)p″-A  (I) in which Q represents an aminoquinoline, (Y1)p—(U)p′—(Y2)p″— is an optional spacer arm and A is an antibiotic, one of its derivatives or precursors, or a resistance enzyme inhibitor. The invention unexpectedly enables the activity of the antibiotic to be improved.

The present invention is directed to novel 2-amino-quinoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD), mild cognitive impairment, senility and / or dementia. The compounds of the present invention are inhibitors of β-secretase, also known as β-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2.

The present invention is directed to 2-amino-quinoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD) and related disorders. The compounds of the invention are inhibitors of β-secretase, also known as β-site cleaving enzyme and BACE, BACE1, Asp2 and memapsin2.

The present invention provides 2-aminoquinoline derivatives, which are represented by the general formula [I] [wherein, R1 and R2 represent lower alkyl groups, lower cycloalkyl groups, or R1 and R2 together form a fatty group with their bonded nitrogen atoms. group of nitrogen-containing heterocyclic rings, R3, R4, R6 and R7 represent hydrogen atoms, lower alkyl groups, etc., R8 represents lower alkyl groups, lower alkoxy groups, etc., and n represents an integer of 0 to 4]. The compound acts as an antagonist of the melanin aggregation hormone receptor, and is useful as a medicine for central diseases, circulatory diseases, and metabolic diseases.

The invention relates to a bis-triazene compound, in particular to 4,4'-bis(5-sulfo-8-hydroxyl-7-aminoquinoline azo)-3,5,3',5'-tetrabromo-diphenyl ether, a method for preparing the same and application thereof. The molecular structure formula of the 4,4'-bis(5-sulfo-8-hydroxyl-7-aminoquinoline azo)-3,5,3',5'-tetrabromo-diphenyl ether is shown as the right. The preparation method comprises the following steps: preparation of 5-sulfo-8-hydroxyquinoline, preparation of 5-sulfo-7-azobenzene-8-hydroxyquinoline, preparation of 5-sulfo-7-amino-8-hydroxyquinoline, bromination of 4,4'-diaminodiphenyl ether and diazotization of 4,4'-diamino-3,5,3',5'-tetrabromo-diphenyl ether, and coupling. The method has the advantages of simple method and low cost; and when being used for detecting heavy metal ions, the method has the characteristics of good selectivity, high sensitivity and stable performance.

The invention discloses a rhodamine B derivative containing an 8-aminoquinoline group, a preparation method, an application and a method for carrying out fluorescence analysis on Cr<3+> and Cu<2+>. The rhodamine B derivative containing the 8-aminoquinoline group is capable of selectively and quantitatively detecting chromium ions (Cr<3+>) in acetonitrile, and is capable of selectively and quantitatively detecting copper ions (Cu<2+>) in ethanol and generating an obvious fluorescence increment effect. The rhodamine B derivative containing the 8-aminoquinoline group is simple in synthesis method, and is capable of quantitatively detecting different heavy metal ions Cr<3+> and Cu<2+> in different solvents at high selectivity and high sensitivity, is a dual-functional fluorescence probe, and has a good application prospect in the fields of environment analysis and detection.

The invention discloses core-shell-structured nano-particles modified with 8-aminoquinoline derivative, and a preparation method and an application thereof. According to the invention, the core-shell-structured nano-particles with iron oxide as cores and silica as shells are modified with the 8-aminoquinoline derivative. The method comprises the steps that: ferric chloride hexahydrate and sodium acetate dissolved in ethylene glycol are placed under a sealed state, and are subjected to a reaction under the temperature of 200-210 DED C, such that a precipitate iron oxide nano-particles are obtained; the nano-particles are dispersed in ethanol; ammonia water, deionized water, ethanol and a tetraethyl orthosilicate ethanol solution are sequentially dropped into the solution; ultrasonic reaction is carried out, and nano-particles are obtained; the nano-particles are sequentially added into toluene, such that a suspension liquid is obtained; N-(quinolin-8-)-2-(3-triethoxysilyl-propylamino)-acetamide is dissolved in toluene, such that a QIOEt toluene solution is obtained; the two are mixed and are subjected to an ultrasonic process; and a reflux reaction is carried out under the temperature of 130-150DEG C, such that a target product is prepared. The product can be widely used for rapidly detecting trace amounts of divalent zinc ions in a solution.

The invention relates to 4-aminoquinoline and a 4-aminoquinoline compound which are applied to the technical field of medicines and applications of the compound, compounds, configurational isomers and configurational isomer mixtures or pharmacologically acceptable salts and / or hydrates of the compound in the general formula I. The compound provided by the invention has the obvious antitumor activity and can be used for preparing the medicines for treating and / or preventing tumor diseases. In addition, the compound is light in molecular weight, simple to composite and small in toxic and side effects.

The invention belongs to the technical field of functional material preparation, and discloses a preparation method and application of a palladium-ion-imprinted composite membrane for selectively separating palladium ions. Specifically, a base film is prepared by using polydimethylsiloxane, and the palladium-ion-imprinted composite membrane can be prepared by use of palladium ion as a template, 8-aminoquinoline and 4-vinylpyridine as ligands, hydroxyethyl methacrylate as a functional monomer, ethylene glycol dimethacrylate a crosslinking agent and azobisisobutyronitrile as an initiator by combination of a sacrificial template method and an ion-imprinting polymerization technique. Selective adsorption experiments are used to study the selective adsorption capacity of the prepared palladium-ion-imprinted composite membrane; selective permeation experiments are used to study the selective permeation capacity of the prepared palladium-ion-imprinted composite membrane for a target substance(palladium ion) and a non-target substance (cobalt ion, copper ion, cadmium ion and nickel ion). The results show that the palladium-ion-imprinted composite membrane prepared by the invention has high specific recognition ability and adsorption separation ability for the palladium ions.

The present invention relates to 2-aminoquinolines of formula Iwherein R1, R2 and R3 are as defined in the specification, as 5-HT5A receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of CNS disorders.

The invention discloses a preparation method of 2-methyl-8-aminoquinoline. The preparation method of 2-methyl-8-aminoquinoline comprises the step of ammoniating 2-methyl-8-bromoquinoline in a solvent at 60-120 DEG C under the action of catalyst and strong alkali to obtain the 2-methyl-8-aminoquinoline, wherein the catalyst is one or more selected out of copper acetylacetonate, iron acetylacetonate, cobalt acetylacetonate and zinc acetylacetonate, the solvent used is one or more selected out of dimethylsulfoxide, N, N-dimethylformamide, acetylacetone, tetrahydrofuran and N-methylpyrrolidone, and the strong alkali is one or more selected out of caesium carbonate, caesium hydroxide, potassium carbonate and potassium hydroxide. The preparation method of the intermediate 2-methyl-8-bromoquinoline comprises the step of performing a cyclization reaction on o-bromoaniline and crotonic aldehyde in a solvent in the presence of oxidant and mollient, so as to obtain the 2-methyl-8-bromoquinoline, wherein the oxidant is selected out of one or more of nitrobenzene, 2-nitrobromobenzene, ammonium ceric nitrate, vanadic acid and iron oxide, the mollient is selected out of one or more of glacial acetic acid, hydrochloric acid, ferrous sulfate and boric acid, and the solvent is selected out of one or more of hydrochloric acid, sulfuric acid and chlorobenzene.

Disclosed are sulfonamidoquinoline compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structureand pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein R1, R2, R3 and R4 are as described herein. In certain embodiments, a compound disclosed herein inhibits ubiquitination, and can be used to treat disease by blocking the degradation of tumor suppressors.

The present invention is directed to a new class of 6-sulfonamido-quinolin-2-one and 6-sulfonamido-2-oxo-chromene derivatives to their use as androgen antagonists, and to relieve conditions associated with inappropriate activation of the androgen receptor.

The invention discloses a method for synthesizing substituted phenylalanine and substituted phenyllactic acid derivatives by using palladium as a catalyst, which comprises the following steps: reacting raw materials nitrogen-terminal or oxygen-terminal completely-protected alanine or lactic acid, to the carboxyl terminal of which 8-aminoquinoline is introduced, and aryl iodide in an organic solvent at 75 DEG C for 3-24 hours, wherein the aryl iodide is used as an arylation reagent, palladium acetate or palladium trifluoracetate is used as a catalyst, and a silver salt is used as an additive; and purifying and separating by column chromatography to obtain the substituted phenylalanine and substituted phenyllactic acid derivatives. The invention has the advantages of mild reaction conditions and simple technique, and is convenient and simple to operate; and the product has high mono / diarylation selectivity.

Novel synthetic monomers that have the capacity to be assembled into defined oligomers which bind with sequence specificity to duplex Watson-Crick DNA via a triple helix motif are provided.

Various 2-aminoquinoline compounds as can be used, in vivo or in vitro, for selective inhibition of neuronal nitric oxide synthase.

The present invention is directed to 2-amino-quinoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD) and related disorders. The compounds of the invention are inhibitors of β-secretase, also known as β-site cleaving enzyme and BACE, BACE1, Asp2 and memapsin2.

The present invention relates to novel bisaminoquinoline compounds, pharmaceutical compositions comprising these novel compounds and methods for inhibiting autophagy in biological systems. Methods of treating cancer in patients in need using compounds and / or compositions according to the present invention alone or in combination with at least one additional anticancer agent represent additional aspects of the invention. Methods of treating disease states and / or conditions in which inhibition of autophagy plays a favorable treatment role including rheumatoid arthritis, malaria, antiphospholipid antibody syndrome, lupus, chronic urticaria and Sjogren's disease, with compounds according to the present invention represent additional aspects of the invention.

The invention discloses a preparation method of a compound containing a C(sp2)-Br bond, wherein the compound containing the C(sp2)-Br bond is a compound represented by a formula II. The method comprises the following steps: in the presence of a copper catalyst and a bromide, carrying out a constant-current electrolytic reaction on an 8-aminoquinoline amide derivative represented by a formula I andused as a substrate to obtain the compound containing the C(sp2)-Br bond and represented by the formula II. According to the preparation method disclosed by the invention, an expensive, toxic or dangerous oxidant can be prevented from being used, the C(sp2)-H bond compound can be converted into the product of the C(sp2)-Br bond at high selectivity, and the method is environment-friendly, high inyield, good in purity and suitable for industrial production.

The invention concerns an aminoquinoline-antibiotic hybrid compound of general formula (I): Q-(Y1)p-(U)p'-(Y2)p''-A; wherein Q represents an aminoquinoline, (Y1)p-(U)p'-(Y2)p'' is an optional spacer and A is an antibiotic residue. The invention enables the antibiotic residue activity to be unexpectedly enhanced.

The invention discloses a near-infrared fluorescent probe, preparation and an application of the near-infrared fluorescent probe in detection of transthyroxine tetramer protein. The structural formula of the near-infrared fluorescent probe is shown as a formula (I). The preparation method comprises the following steps: adding 2-aldehyde-6-dimethylaminoquinoline, 2-acetonitrile benzothiazole and tetrabutylammonium bromide into ethanol, carrying out a reflux reaction under the conditions of sealing and oil bath at 80 + / -5 DEG C, cooling to room temperature after the reaction is finished, standing to separate out a solid, carrying out suction filtration, and washing to obtain the near-infrared fluorescent probe. The fluorescent probe prepared in the invention has near-infrared emission wavelength, and can be used for detecting the content of transthyretin tetramer protein and diagnosing transthyretin familial amyloidosis.