157 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 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 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.

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 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 present invention relates to 2-aminoquinolines of formula I

wherein R¹, R² and R³ are as defined in the specification, as 5-HT_5A receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of CNS disorders.

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.

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.

The invention discloses a compound acidifying corrosion inhibitor containing a quinoline derivative and novel mannich base. The compound acidifying corrosion inhibitor is prepared from the following components in parts by weight: 12 to 20 parts of a main agent A of the corrosion inhibitor and 12 to 20 parts of a main agent B of the corrosion inhibitor, wherein the main agent A of the corrosion inhibitor is generated through a reaction of benzotriazole, benzaldehyde and piperidine; the main agent B of the corrosion inhibitor is generated through a reaction of 3-aminoquinoline and benzyl chloride; and in addition, the compound acidifying corrosion inhibitor further comprises propargyl alcohol, heavy alkylbenzene sulfonate, potassium iodide, cuprous chloride, peregal O, formic acid, acetanilide, triethanolamine and a solvent. The acidifying corrosion inhibitor has the advantages of good slow-release effect, easiness in storage and transportation, high stability and environmental friendliness; in addition, the slow-release property of the acidifying corrosion inhibitor can be maintained for 3 days or longer under the condition that the temperature is 160 DEG C, so that the acidifying construction quality under the condition that the temperature is 160 DEG C is effectively improved; and in addition, the acidifying corrosion inhibitor has higher compatibility with a common oilfield acidification system.

The invention relates to a synthetic method of 2, 9-dinitro-4, 7-dimethyl-1, 10-phenanthroline, and belongs to the technical field of organic chemistry. The method comprises the following steps: stirring and mixing nitrobenzene and SnCl2.2H2O, filling with hydrogen, adding iron powder and hydrochloric acid, reacting under certain conditions to obtain aniline, respectively mixing aniline with hydrogen peroxide and benzoyl chloride and adding ethanol, stirring and heating, adding nitric acid, heating, adding chlorosuccinimide in a dropwise manner, mixing with a hydrochloric acid and water mixed solution, carrying out water bath heating, adding zinc powder, stirring and reacting, adding a sodium hydroxide solution, and distilling the obtained solution to obtain a distillate which is 4-methyl-8-aminoquinoline; and heating 4-methyl-8-aminoquinoline, benzoyl chloride and to reflux, cooling to room temperature, slowly adding nitric acid in a dropwise manner, filtering, mixing the obtained filtrate with stannous chloride, heating, adding zinc powder and hydrochloric acid, and carrying out stirring and pumping filtration, and carrying out vacuum drying to obtain 2, 9-dinitro-4, 7-dimethyl-1, 10-phenanthroline. The method has the advantages of mild reaction conditions, simple operation and low cost.