98results about How to "Good selective inhibition" patented technology

The invention discloses a 4-carbamate-3-methoxy cinnamic acid cyclamine alkyl amide compound, and a preparation method and application thereof. The compound prepared in the invention has low toxic and side effect, and can treat neurodegenerative diseases including, but not limited to, vascular dementia, the Alzheimer's disease, the Parkinson's disease, the Huntington's disease, HIV-associated dementia, multiple sclerosis, amyotrophic lateral sclerosis, neuropathic pain, glaucoma and the like.

The invention belongs to the technical field of medicines, and in particular relates to a compound taking thieno-pyrimidone as mother nuclide or a salt thereof, a preparation method and a combination of the compound and application of the compound used as a DPP-IV (dipeptidyl peptidase) inhibitor in preventing or treating diseases benefiting from the DPP-IV inhibition. The compound provided by the invention has the advantages that the preparation process is simple, the raw material is easily available, the compound is suitable for large-scale production, and in-vitro experiment verifies that the compound has good selective inhibition action on the DPP-IV, and hardly has any influence on the activities of DPP-VIII and DPP-IX while effectively inhibiting the activity of the DDP-IV, thereby predicting that the medicine prepared from the compound has very low toxicity and an outstanding advantage.

The invention discloses a specific inhibitor application in complex sulfide ore. The inventive organic compound contains mineral-philic group -SH, hydrophilic group -COOH, -OH, -SO3, etc. in molecular structure, which fully shows the inhibiting property against pyrrhotite, pyrite and chalcopyrite in complex sulfide ore flotation separation, and is a high selectivity desulphurizing inhibitor. Compared with the prior inorganic inhibitors such as cyanide, lime, zinc sulfate, trisodium phosphate, dichromate, potassium permanganate, sodium sulfide, sulfite, etc., the inventive inhibitor has the advantages of low usage amount, good index and no pollution.

The invention belongs to the technical field of medicines, relates to a high-efficient DPP (dipeptidyl peptidase)-IV inhibitor, and specifically relates to a compound taking uracil as a mother nucleus, or a salt thereof, a preparation method, a composition and an application of the compound as the DPP-IV inhibitor in prevention or treatment of diseases which benefit from DPP-IV inhibition. The compound disclosed by the invention has a very good selective inhibition effect against DPP-IV and has very low cardiotoxicity, thereby being a DPP-IV inhibitor type medicament with great prospects.

The invention discloses a fused cyanopyridine compound shown as a general formula I-1 or I-2, or a pharmaceutically acceptable salt thereof, or an enantiomer, a diastereoisomer, a tautomer, a torsional isomer, a solvate, a polymorphic substance or a prodrug thereof, and a preparation method and a pharmaceutical application of the fused cyanopyridine compound, wherein the definition of each group is shown in the specification.

The invention belongs to the technical field of organic synthesis and particularly relates to a cyclamine alkylamide ferulate compound as well as a preparation method and application thereof. The preparation method comprises the following steps: enabling potassium phthalimide serving as a start raw material to react with 1-substituted-4-haloalkyl piperidine under the effects of a solvent and alkali to obtain a phthalimide alkylamine compound; performing hydrazinolysis of the phthalimide alkylamine compound and hydrazine hydrate to obtain a primary amine compound; and adding ferulic acid, a condensing agent and a solvent into the primary amine compound for a condensation reaction to obtain a product of cyclamine alkylamide ferulate compound. The cyclamine alkylamide ferulate compound provided by the invention is of a simple chemical structure, the chemical reactions in the preparation process are thorough, the product yield is high, the operation is convenient, the cost is low, and the product can be used for perfectly treating the neurodegenerative diseases.

The invention discloses a beneficiation method for improving comprehensive recovery indexes of complex low-grade molybdenum polymetallic ores, and particularly relates to comprehensive recovery of valuable elements such as molybdenum, copper and sulfur in low-grade molybdenum ores. According to the method, the effective flotation separation of molybdenite, chalcopyrite and pyrite can be realized,and the comprehensive recovery indexes of the low-grade molybdenum ores are improved. The method comprises the following steps of primary ore grinding, molybdenum (molybdenite) flotation, secondary ore grinding (rough molybdenum copper concentrate regrinding), copper (chalcopyrite) flotation, and sulfur (pyrite) flotation. The method is stable and effective in reagent regime and beneficiation process flow and high in adaptability. By using the beneficiation method, high-quality molybdenite, chalcopyrite and pyrite are obtained from the complex, difficult-to-select and low-grade molybdenum polymetallic ore with associated copper / sulfur, and the comprehensive recovery indexes of sulfide minerals are excellent. The adopted reagent is non-toxic and harmless, has little influence on the environment, and is an excellent beneficiation method.

A novel quinazoline nitrogen mustard compound is characterized in that: one end is provided with a nitrogen mustard alkylating group; the other end is provided with a 6, 7-substituted quinazoline structure; a substituent R1 is located at a site 4 of a quinazoline matrix, and represents 2-, 3-, 4- nitrogen mustard substituent; and substituents R2, R3 are located at site 6 and 7 of a quinazoline matrix, and represent methoxyethoxy, methoxy, morpholine propoxy, 3-etrahydrofuran oxygen group and hydroxyl group. The compound has a structure shown as a formula A. Experiments show that the compound can cause cross-linking of DNA, and is a bifunctional alkylating agent. In vivo antitumor activity experiment show that the compound has good activity; furthermore, the compound has the advantage of low toxicity, which a nitrogen mustard drug is lack of. At the same time, the compound is easy for synthesis, has high total yield. Advantages of the compound show that it has great potential to become a drug for treatment of cancer.

The invention relates to application of an efficient calcium-containing gangue mineral inhibitor to scheelite flotation. The inhibitor is an organic phosphoric acid type compound, production is simple, and performance is stable and reliable. According to the application, the inhibitor is applied to scheelite flotation for the first time, and traditional sodium silicate can be replaced to conduct selective inhibition on difficultly-separated calcium type gangue minerals in particular to calcite, fluorite and the like. The efficient calcium-containing gangue mineral inhibitor is simple and efficient in ingredient, high in selective inhibitory effect, small in using quantity and extremely low in cost.

The invention provides a novel JAK (Janus kinase) selective inhibitor and a preparation method thereof and use thereof, in particular, the invention discloses a compound having the structure represented by the formula I or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, hydrate or solvate thereof which can be used as the JAK kinase inhibitor.

The invention discloses pyrrolopyrimidine derivatives as protein kinase inhibitors and application thereof, and geometric isomers or pharmaceutically acceptable salts, hydrates, solvates or prodrugs of the pyrrolopyrimidine derivatives. In-vivo and in-vitro biological tests prove that, the compound can be used as a protein kinase inhibitor, especially can inhibit PAK4 kinase, and has a high-selectivity inhibition effect on the PAK4 kinase in a PAKs family. The activity of the PAK4 kinase in cells can be reduced or inhibited; meanwhile, the compound can also be used as the protein kinase inhibitor and can be used for inhibiting kinases such as GCK, GLK, HPK1 and TYK2 related to human autoimmunity; the compound is applied to drugs for treating and / or preventing diseases mediated by PAKs family kinase, especially hyper-proliferative diseases and / or virus-induced infectious diseases and / or cardiovascular diseases and diseases caused by autoimmunity.

The invention relates to the mineral concentration and floatation technology, in particular to application of hydroxypropyl starch ether in fluorite ore flotation. A floatation method of fluorite ore comprises the steps of grinding the fluorite ore comprising barite and calcite minerals, feeding the ground fluorite ore into a flotation machine, stirring the fluorite ore for pulp mixing, adjusting the pH value of ore pulp through HC1, NaOH or Na2CO3 until the pH value is greater than or equal to 7, stirring the ore pulp, adding hydroxypropyl starch ether inhibitors for guaranteeing that the concentration of the ore pulp ranges from 20 mg / L to 200 mg / L, and stirring the ore pulp for 2-5 minutes; adding sodium oleate serving as collecting agents, carrying out stirring and then carrying out gas filling and bubble scraping, wherein the amount of the sodium oleate is 20-400 mg / L. The hydroxypropyl starch ether is good in ability to restrain barite and calcite and has the advantages of being friendly to environment, wide in source, low in cost and obvious in effect.

The invention belongs to the ilmenite flotation technology, and particularly relates to a pyroxene peridotite type ilmenite depressing agent and a preparation method of the pyroxene peridotite type ilmenite depressing agent. The preparation method of the pyroxene peridotite type ilmenite depressing agent comprises the step of carrying out oscillation, stir and curing on a mixed solution formed by sodium silicate, ferric nitrate and sulfuric acid to obtain the pyroxene peridotite type ilmenite depressing agent, wherein oscillation, stir and curing are carried out for 30-40min. The obtained pyroxene peridotite type ilmenite depressing agent comprises, by weight, 5-15 parts of the sodium silicate, 5-15 parts of the ferric nitrate and 1-10 parts of the sulfuric acid. The pyroxene peridotite type ilmenite depressing agent obtained through the preparation method has a good selective depressing effect on olivine and pyroxene, and has extremely important significance in obtaining of good technical indexes of titanium flotation of pyroxene peridotite type ilmenite.

The invention relates to the technical field of biological fresh-keeping agents, in particular to a safe healthy meat low-temperature cold storage fresh-keeping agent. The fresh-keeping agent comprises the following components in percentage by mass: 5-9.5% of a cactus flower extract, 0.8-2.3% of chitosan, 0.9-1.5% of a phosphoric acid buffer solution, 0.3-0.6% of tea polyphenols, 0.2-1.1% of potassium sorbate, 0.2-0.5% of lysozyme, 0.3-0.9% of a bacteriostasis protein solution and the balance of deionized water, wherein the cactus flower extract is polysaccharide substances extracted from receptacle tubes and ovaries of cactus flowers, and has favorable film formation effects and moisture absorption; and bacteriostasis protein contains one or more kinds of ovotransferrin, lactoferrin, yolkimmunoglobulin and transferrin. The fresh-keeping agent is prepared from biomaterials, is good in fresh keeping effects, is easy to eliminate, is small in influence on meat quality and is quite safeand healthy.

The present invention relates to a compound represented by Formula [I]: wherein X is O, S, NH or CH2; Y1, Y2, Y3, Y4 and Y5, which may be identical or different, are each CH or N; however, at least one of Y1, Y2, Y3, Y4 and Y5 is N; Z1 and Z2, which may be identical or different, are each CH or N; n is an integer from 1 to 3; R1 is a C3-C8 cycloalkyl group, a C6-C10 aryl group, an aliphatic heterocyclic ring or an aromatic heterocyclic ring, or a bicyclic aliphatic saturated hydrocarbon group; R2 and R3, which may be identical or different, are each a hydrogen atom, a lower alkyl group, a lower alkenyl group, a C3-C8 cycloalkyl group, a C6-C10 aryl group, an aromatic heterocyclic ring, or the like; and R4 is a hydrogen atom, a lower alkyl group, a C3-C6 cycloalkyl group or the like, or a pharmaceutically acceptable salt or ester thereof, and a selective inhibitor against Cdk4 and / or Cdk6 or an anticancer agent containing the compound or a pharmaceutically acceptable salt or ester thereof.

The invention belongs to the technical field of medicines, and particularly relates to compounds which are shown as a general formula I and in which pyrrolopyrimidone is taken as a parent nucleus or salts thereof, a method for preparing the compounds, a composition, and use of the compounds as dipeptidyl peptidase-IV (DPP-IV) inhibitors in the prevention or treatment of diseases which benefit from DPP-IV inhibition. The preparation process for the compounds is simple, raw materials are readily available, and the method is suitable for industrialized production; through in-vitro experiments, the compounds have a good effect of selectively inhibiting DPP-IV, and almost do not affect the activities of DPP-VIII and DPP-IX when the activity of the DPP-IV is effectively inhibited; and the compounds are expected to have low toxicity after being developed into medicines, and have outstanding advantages.

The invention discloses a flotation separation agent system for copper-molybdenum mixed concentrates and application of the flotation separation agent system. The flotation separation agent system forthe copper-molybdenum mixed concentrates comprises a copper mineral inhibitor, a molybdenum mineral collector and a foaming agent in a copper-molybdenum flotation separation process. The copper mineral inhibitor comprises the following components in parts by weight: 3-7 parts of sodium hydroxide, 3-6 parts of hydrogen peroxide, 15-25 parts of sodium thioglycolate, 2-5 parts of pentasodium diethylenetriaminepentaacetate and a proper amount of water; the molybdenum mineral collector comprises the following components in parts by weight: 20-30 parts of kerosene and 5-10 parts of tert-dodecyl mercaptan; and the foaming agent is 2-hexanol. The inhibitor and the collector are high in selective adsorption capacity, the synergy performance is excellent, the activity of groups of the foaming agentis high, formed foams are crisp and compact, and the mineralization effect is good. According to the flotation separation agent system for copper and molybdenum, the floatability difference between molybdenum minerals and copper minerals in the complex copper and molybdenum mixed concentrates difficult to separate can be greatly improved, the mutual content of the copper and the molybdenum is effectively reduced, the separation index is excellent, adopted agents are nontoxic and harmless, and the influence on the environment is small.

The invention relates to an ore dressing technology, in particular to application of cationic etherified starch in scheelite flotation. According to the application, a used depressing agent cationic etherified starch can inhibit scheelite flotation, the floatable difference of gangue minerals such as fluorite, calcite and aluminosilicate and scheelite is remarkably improved, reverse flotation separation of the gangue minerals and the scheelite is achieved, and the problem of difficult separation of the scheelite and the gangue minerals such as fluorite, calcite and aluminosilicate is solved. The used depressing agent is conductive to the improvement of scheelite concentrate grade and recovery rate, a flotation process is shortened, the production cost is reduced, and the comprehensive resource utilization level is improved.

The invention relates to a substituted bicyclic aromatic heterocyclic amine inhibitor as well as a preparation method and application thereof. Specifically, the compound has a structure as shown in a formula (I), the invention further discloses a preparation method of the compound and application of the compound as an SOS1 inhibitor, and the compound has a very good selective inhibition effect on SOS1 and has better pharmacodynamic and pharmacokinetic performance and lower toxic and side effects.

The invention discloses a saturated six-membered ring heterocyclic compound as well as a preparation method and application thereof. The invention discloses a saturated six-membered ring heterocycliccompound shown as a general formula I, or pharmaceutically acceptable salt thereof, or an enantiomer, a diastereoisomer, a tautomer, a torsional isomer, a solvate, a polymorphic substance or prodrug thereof, as well as a preparation method and a pharmaceutical application of the saturated six-membered ring heterocyclic compound. The definition of each group is as described in the specification.

The invention discloses a combined inhibitor for silicate gangue mineral in the flotation process of Ti-containing mineral and an application of the inhibitor. The combined inhibitor consists of one or more of organic sulfonate, oxalic acid, water glass, a water glass and oxalic acid mixture and sodium fluosilicate, wherein organic sulfonate mainly comprises aromatic sulfonate and a polymer thereof. Compared with common silicate gangue mineral inhibitors for flotation of Ti-containing mineral at preset, the inhibitor has a better selective inhibition function on the silicate gangue mineral, strongly inhibits floatation of gangue mineral in the floatation process and has a weaker inhibition function on Ti-containing useful mineral than oxalic acid, water glass, the water glass and oxalic acid mixture and the sodium fluosilicate, and the recovery rate of the Ti-containing useful mineral concentrate can be increased under the condition that the selectivity of the Ti-containing mineral floatation separation process. The inhibitor has a better effect than conventional gangue mineral inhibitors for floatation of ilmenite when used for separating ilmenite from the gangue mineral.

The invention discloses an epoxidase-2 selective inhibitor as well as a preparation method and application thereof. According to the epoxidase-2 selective inhibitor, with substituted benzamide and a substituted benzoic acid derivative as raw materials, a 4-[3,5-bis(substituted-phenyl)-1-(1,2,4-triazole)] benzenesulfonic acid derivative is obtained through condensation reaction and ring closing reaction of a p-hydrazino-benzenesulfonic acid derivative. The epoxidase-2 selective inhibitor has the beneficial effects that the epoxidase-2 selective inhibitor has a significant selective inhibiting effect on epoxidase COX-2 activity, and is capable of obviously inhibiting foot swelling in mice caused by carrageenin; and a target compound is expected to become a medicine for treating inflammation, rheumatoid arthritis, and diseases related to epoxidase-2.

The invention relates to a compound shown in a formula I or a salt, a preparation and a composition thereof and application of the compound serving as a dipeptidyl peptidase-IV (DPP-IV) inhibitor to the prevention or treatment of diseases which benefit from DPP-IV inhibition. The compound has a simple preparation process, is readily available in raw materials and is suitable for large-scale industrial production; and in-vitro experiments verify that the compound has a good selective inhibition effect on the DPP-IV, and influences the activity of DPP-VIII and DPP-IX scarcely while the activity of the DPP-IV is inhibited effectively, so after the compound is developed to form medicaments, the toxicity is far lower than that of a control medicament, and the compound has prominent advantages.

The invention relates to a selective Janus kinase 2 (JAK2) inhibitor and application thereof. Specifically, the invention relates to a compound shown as the following formula I (please see the specifications for the formula) and application of the compound to treatment of JAK2 mediated related diseases and preparation of drugs for treating the JAK2 mediated related diseases.

The invention discloses a C-triaryl glucoside compound with the structure shown in the formula I as shown in the description, or an optical isomer thereof, or pharmaceutically acceptable salt, co-crystallization composite, hydrate, solvate or prodrug molecule thereof. The compound disclosed by the invention has a very good selective inhibition effect on SGLT-2, has an obvious promotion effect on releasing of animal urine sugar, can effectively reduce blood glucose and meanwhile cannot result in the risks of weight increase, hypoglycemia and the like. The compound disclosed by the invention haslittle influence on the activity of SGLT-1 while effectively inhibiting the activity of SGLT-2, can be expected that the toxicity is low when being developed into drugs, and has obvious medication advantage.

The invention belongs to the technical field of medicines, relates to a preparation method of a high-efficient DPP (dipeptidyl peptidase)-IV inhibitor, and specifically relates to a compound taking uracil as a mother nucleus, or a pharmaceutically acceptable salt thereof, a preparation method, a composition and an application of the compound as the DPP-IV inhibitor in prevention or treatment of diseases which benefit from DPP-IV inhibition. The compound disclosed by the invention has a very good selective inhibition effect against DPP-IV and has very low cardiotoxicity, thereby being a DPP-IV inhibitor type medicament with great prospects.

The invention relates to a beneficiation technology, in particular to application of hydroxypropyl starch ether in scheelite flotation. According to the application, the flotation inhibitor, namely the hydroxypropyl starch ether can be used for inhibiting the scheelite flotation, the floatability difference of gangue minerals such as fluorite, calcite and aluminosilicate minerals and scheelite canbe remarkably improved, reverse flotation separation of the gangue minerals from the scheelite is realized, and the problem that the scheelite and the gangue minerals such as the calcite, the fluorite and the aluminosilicate minerals are difficult to separate is solved. The flotation inhibitor used in the application is beneficial to the improvement of the grade and the recovery rate of scheeliteconcentrate, the flotation process is shortened, production cost is reduced, and comprehensive utilization level of resources is improved.

The invention belongs to the technical field of medicine, and relates to a (N-1,2,3,4-tetrahydroisoquinolinyl)-feruloylagmatine compound, and a preparation method and application thereof. The structure is as shown in a formula I (the formula I is as shown in the description). The (N-1,2,3,4-tetrahydroisoquinolinyl)-feruloylagmatine compound provided by the invention has excellent butyrylcholine esterase inhibiting activity, remarkable Abeta1-42 aggregation inhibiting activity, anti-oxidation activity and high neuroprotective activity on PC12 cell injury induced by hydrogen peroxide in in-vitro experiments; and the (N-1,2,3,4-tetrahydroisoquinolinyl)-feruloylagmatine (I) compound is a multi-target-point inhibitor, further shows a good effect of treating alzheimer disease in in-vivo experiments, and has low toxicity and a good clinical application prospect.