30 results about "Hydroxizinum" patented technology

The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.

The invention discloses diosgenin hydroxamic acid derivatives and their preparation method and application. Diosgenin is used as a lead compound to prepare a series of hydroxamic acid derivatives through corresponding chemical reactions, and the anti-tumor effect of the derivatives Applications. Pharmacological experiments show that: all synthesized diosgenin hydroxamic acid derivatives are treated with CCK8 method against SW620 (human colon adenocarcinoma cells), H358 (human non-small cell lung cancer cells), HCT‑116 (human colorectal adenocarcinoma cells) and Aspc‑1 (human metastatic pancreatic cancer cells) were tested for antiproliferative activity in vitro. Experimental results show that most of the derivatives have better anti-tumor activity than diosgenin on cells.

Compounds of formula I are provided:R1 is an alkoxy or O(CH2)pX, p is an integer from 2 to 3 and X is OH, NH2, or CO2H, m is an integer from 0 to 5, n is an integer from 0 to 5, each R2 is independently selected from hydrogen, alkenyl, hydroxyalkyl, alkoxymethyl, heterocyclyl, hetereocyclylmethyl, amino, amido, hydroxamido, any of which may be optionally substituted with one or more of acyl, alkyl, alkoxy, hydroxyalkyl, or halogen, each R3 is independently selected from hydrogen, halogen, alkyl, alkenyl, carboxy, hydroxymethyl, amido, and at least one of R2 and R3 is not hydrogen.

The invention discloses a beta-carboline derivative containing hydroximic acid as well as a preparation method and a medical application thereof. The product has the structure as shown in the general formula I. The compound can be combined with other antitumor drugs such as alkylating agents, antimetabolites, topoisomerase inhibitors, mitotic inhibitors and DNA intercalating agents and additionally can be combined with radiotherapy. The invention also discloses a pharmaceutical composition containing the compound with the general formula I as well as medical application thereof, particularly application of preparation of antitumor medicines, Alzheimer disease medicines and Parkinson disease medicines. The other antitumor medicines or radiotherapy can be administrated with the compound at the same time or in different times. The combination therapy can generate the synergistic effect, so that the treatment effect is improved.

The invention relates to a hydroximic acid sulfonic acid compound as well as a preparation method and application thereof. The hydroximic acid sulfonic acid compound has a structural formula shown as a formula (I) in the description. The hydroximic acid sulfonic acid compound provided by the invention not only has an excellent flotation effect at a low temperature, but also is low in reagent consumption, can be used as a collecting agent to realize flotation of phosphine ore, fluorite and scheelite in a low-temperature and high-calcium-magnesium environment, and has an excellent flotation effect.

The invention discloses a 4-aminoquinazoline compound containing a morpholinyl aromatic heterocycle and a hydroximic acid structure and a preparation method of the 4-aminoquinazoline compound, and particularly discloses a 4-aminoquinazoline compound containing a morpholinyl aromatic heterocycle and a hydroximic acid structure and a preparation method of the 4-aminoquinazoline compound containing a morpholinyl aromatic heterocycle and a hydroximic acid structure. 2, 6-diamine is amidated with dicarboxylic acid monomethyl ester and subjected to a substitution reaction with hydroxylamine to obtain the 4-aminoquinazoline compound (formula 1) containing morpholinyl heteroaromatic rings and hydroximic acid structures and having various structures, X, Y and Z are independently N or CH, R is H, Cl, OCH3 or 4-morpholinyl, and L is (CH2) 2, (CH2) 3, (CH2) 4, o-C6H4, p-C6H4 or (CH2) 6. The method is mild in reaction condition, high in target product yield, safe, simple and convenient to operate, free of toxic and harmful thionyl chloride and environment-friendly, and an efficient, simple and green method is provided for synthesizing the 4-aminoquinazoline compound containing morpholinyl aromatic heterocycle and hydroximic acid structures. The invention provides a theoretical basis and clinical application value for designing and developing novel anti-drug-resistance micromolecular multi-target antitumor drugs. Formula 1.

The invention discloses method for preparing(iso)hydroxamic acid salt or (iso)hydroxamic acid. The method for preparing (iso)hydroxamic acid salt or (iso)hydroxamic acidcomprises the steps that analkali, a hydroxylamine salt, and an organic carboxylic acid ester are directly subjected to hybrid reaction without an extra solvent, and thusan (iso) hydroxamic acid salt product is obtained; and or after the reaction is completed, a reaction system is cooled, an acid is added to the reaction system to obtain (iso)hydroxamic acid.According to themethod for preparing (iso)hydroxamic acid salt or (iso)hydroxamic acid,the (iso)hydroxamic acid salt or the (iso)hydroxamic acidcan be obtainedwith near atomic economy without additional organic solvents or water being added, environment-friendly effectis achieved, simpleness and efficiency are achieved, and industrial production is advantageous.

The invention relates to the technical field of enzyme inhibitors, in particular to a hydroxamic acid derivative and its preparation method and application. The hydroxamic acid group in the hydroxamic acid derivatives provided by the present invention is chelated with the active zinc ion in the active region of the LpxC enzyme, and contains a hydrophobic side chain combined with the hydrophobic channel in the LpxC enzyme, the above two The content of the aspect ensures that the hydroxamic acid derivatives have better bactericidal activity and lower toxicity to LpxC; the present invention also provides a preparation method of the hydroxamic acid derivatives, and the preparation method has a short reaction time , high yield.

The invention provides an application method of an ester-based hydroximic acid collecting agent to mineral flotation, and belongs to the technical field of mineral flotation. The structure of the ester-based hydroximic acid collecting agent is shown in the formula I shown in the specification, wherein in the formula I, R is a C1-C17 alkane base or C2-C17 alkylene. Due to the fact that the molecule of the ester-based hydroximic acid collecting agent contains an ester base and a hydroximic acid base, more ligating atoms and more coordinating groups are obtained, through chelation and metal ions, the more stable complex compound can be formed or strong adsorption is formed on the surfaces of metal oxide minerals, and floatation recycling of rare earth ores, titanic iron ores, scheelite, wolframite, scheelite and wolframite mixture ores or tin ores ca be strengthened; compared with an existing hydroximic acid collecting agent, due to the fact that the ester base exists in the molecule, the beneficial effects of being good in biodegradability, small in poisonousness and friendly to the environment are achieved.

The invention discloses a method for synthesizing a hydroximic acid compound. The method comprises the step of subjecting an organic carboxylic acid compound with a structure represented by a formula(I) shown in the description and a hydroxylamine compound with a structure represented by a formula (II) shown in the description to a grinding reaction in the presence of a coupling reagent, therebypreparing the hydroximic acid compound with a structure represented by a formula (III) shown in the description. According to the method, the technical problems that a large amount of organic solventis used, the reaction temperature is high, wastes are plenty, the aftertreatment is complicated, environmental protection is adverse and the like are solved, and the method has the advantages that thesource of the raw materials is wide, the cost is low, the operation is simple, the efficiency is high, the product is easy to separate, the yield is high, industrial production is easy to achieve andthe like.

The invention discloses a hydroxamic acid-organic phosphoric acid multi-ligand metal complex collecting agent, and a preparation method and an application thereof. The hydroxamic acid-organic phosphoric acid multi-ligand metal complex collecting agent is obtained by a coordination reaction of hydroxamic acid-sulfonic acid multi-ligand composite micelles, prepared from hydroxamic acid salt and organic phosphoric acid, and metal ions. The hydroxamic acid-organic phosphoric acid multi-ligand metal complex collecting agent has extremely high selective collecting capacity on cassiterite, achieves selective flotation separation of cassiterite and gangue minerals, and fundamentally solves the technical problem of difficult flotation separation of cassiterite and gangue minerals.