86 results about "Dual inhibition" patented technology

Aryl alkanol piperazine derivatives of the formula and pharmaceutical compositions comprising the same. Also disclosed are methods for treating depression using the pharmaceutical compositon. Compounds of the invention have excellent dual inhibitory actions to the uptake of the mono-amines neurotransmitter, good antidepressant activities and minor side effects.

The present invention provides a novel method for simultaneously inhibiting the cyclooxygenase COX-2 and 5-lipoxygenase (5-LO) enzymes. The method for the simultaneous dual inhibition of COX-2 and 5-LO is comprised of administering a composition containing an individual and / or a mixture of multiple flavans isolated from a single plant or multiple plants in the Acacia genus of plants to a host in need thereof. The present also includes novel methods for the prevention and treatment of COX-2 and 5-LO mediated diseases and conditions. The method for preventing and treating COX-2 and 5-LO mediated diseases and conditions is comprised of administering to a host in need thereof an effective amount of a composition comprising an individual and / or a mixture of multiple flavans isolated from a single plant or multiple plants in the Acacia genus of plants and a pharmaceutically acceptable carrier. The present invention includes a method for isolating and purifying a composition of flavans having dual specificity for COX-2 and 5-LO from the Acacia genus of plants.

The invention relates to a method for culturing shortcut nitrification granular sludge by combining the dual inhibition of free ammonia (FA) and free nitrous acid (FNA), and belongs to the technical field of the biological denitrification of wastewater. The method comprises the following steps of: inoculating flocculent active sludge to a sequencing batch reactor (SBR), and pumping wastewater which contains chemical oxygen demand (COD) and ammonia nitrogen and serves as inflow from the bottom of the reactor; after a liquid level is reached, starting a stirrer and a blast blower to perform aerobic nitration, degrading organic matters and oxidizing the ammonia nitrogen to form nitrites; after the nitration is finished, stopping aerating and stirring, precipitating to obtain supernatant containing the nitrites, and discharging sewage from a drainage valve, wherein in the culture conditions, the temperature of the reactor is between 25 and 30 DEG C, NaHCO3 solution is added after aeration is performed for 30 minutes, so that the pH value is kept between 7.5 and 8.0, dissolved oxygen is between 3 and 5 mg / L, upflow is provided at the speed of between 1.0 and 1.5 cm / s, and sludge age is between 12 and 15 days; and culturing for 30 to 50 days to obtain the shortcut nitrification granular sludge. By the method, the removal efficiency of a denitrification system can be improved effectively, oxygen supply and denitrification carbon sources can be saved, the yield of the sludge can be reduced, the volume of the reactor can be reduced, and the construction and operating cost can be saved.

The present invention relates to a method for dual inhibition of sodium-dependent glucose cotransporter 1 (SGLT1) and sodium-dependent glucose cotransporter 2 (SGLT2) present in the intestine and kidney by using the compound of formula I or a pharmaceutically acceptable salt or a prodrug thereof:wherein ring A, ring B, X and Y have the same meanings as defined in the specification.

The present invention provides a novel method for simultaneously inhibiting the cyclooxygenase COX-2 and 5-lipoxygenase (5-LO) enzymes. The method for the simultaneous dual inhibition of COX-2 and 5-LO is comprised of administering a composition containing an individual and / or a mixture of multiple flavans isolated from a single plant or multiple plants in the Acacia genus of plants to a host in need thereof. The present also includes novel methods for the prevention and treatment of COX-2 and 5-LO mediated diseases and conditions. The method for preventing and treating COX-2 and 5-LO mediated diseases and conditions is comprised of administering to a host in need thereof an effective amount of a composition comprising an individual and / or a mixture of multiple flavans isolated from a single plant or multiple plants in the Acacia genus of plants and a pharmaceutically acceptable carrier. The present invention includes a method for isolating and purifying a composition of flavans having dual specificity for COX-2 and 5-LO from the Acacia genus of plants.

The present invention provides a method for the treatment of schizophrenia which comprises administering a compound of formula wherein the substituents are as described herein or a pharmaceutically active acid-addition salt thereof. In particular, the invention provides methods for treating both positive and negative symptoms of schizophrenia through dual inhibition of NK1 and NK3 receptors. The invention also provides novel compounds with formula I and methods for preparing compounds of the invention.

The invention discloses a functional sanitary towel containing a cannabidiol extractive and a manufacturing method thereof. The sanitary towel includes a sanitary towel body and an effect solution, the effect solution is prepared from, by weight, 0.002-0.008 part of a cannabidiol extractive, 5-9 parts of a penetration enhancer, 30-40 parts of traditional Chinese medicine agents, 1-5 parts of a lavender extractive, 0.05-0.2 part of nano-silver, 2-6 parts of a surface active agent and 90-100 parts of purified water. The cannabidiol extractive is added; the cannabidiol achieves the effects of relieving pain and resisting inflammatory due to dual inhibition of cyclooxygenase and lipoxygenase; by adding the penetration enhancer, penetration and absorption speed of effective ingredients on skinis increased, when a woman uses the sanitary towel, the antibacterial anti-inflammation and pain-relief effects are achieved rapidly; by adding the lavender extractive, the traditional Chinese medicine smell of the sanitary towel is effectively improved, and the comfort level of the user is improved.

The present disclosure provides methods and compositions for modulating an adaptive immune response without significantly affecting an innate immunity response in a subject by modulating a combination of an Immunophilin / Cyclophilin Family Member and an EMMPRIN Immunoglobulin Receptor Superfamily Member. The present invention also provides methods and compositions for treating a variety of clinical conditions by modulating an Immunophilin / Cyclophilin Family Member and an EMMPRIN Immunoglobulin Receptor Superfamily Member.

Compounds of Formula I potently inhibit both cyclooxygenase-2 and carbonic anhydrases. Inhibition of carbonic anhydrases by a cyclooxygenase-2 inhibitor may affect significantly the safety and efficacy profiles of such a dual inhibitor in the treatment of cyclooxygenase-2 mediated disorders, compared to a cyclooxygenase-2 inhibitor without carbonic anhydrase inhibitory activity.

Aryl alkanol piperazine derivatives of the formulaand pharmaceutical compositions comprising the same. Also disclosed are methods for treating depression using the pharmaceutical composition. Compounds of the invention have excellent dual inhibitory actions to the uptake of the mono-amines neurotransmitter, good antidepressant activities and minor side effects.

The present invention relates to a method for dual inhibition of sodium-dependent glucose cotransporter 1 (SGLT1) and sodium-dependent glucose cotransporter 2 (SGLT2) present in the intestine and kidney by using the compound of formula I or a pharmaceutically acceptable salt or a prodrug thereof:wherein ring A, ring B, X and Y have the same meanings as defined in the specification.

The invention discloses a novel NAMPT and IDO dual inhibitor, and a preparation method and medical applications thereof, and more specifically relates to a furazan compound, or pharmaceutically acceptable salts, solvates, prodrugs, esters, racemic compounds, and isomers of the furazan compound, and pharmaceutical compositions containing the furazan compound, and applications of the furazan compound or the pharmaceutical compositions in the field of anti-tumor drug preparation. According to the preparation method, reasonable combination of active segments of an IDO inhibitor and a NAMPT inhibitor is adopted so as to obtain the furazan kind IDO / NAMPT double target inhibitor. On one hand, the furazan kind IDO / NAMPT double target inhibitor is capable of realizing dual inhibition of NAD<+> biosynthesis, and possesses higher anti-tumor inhibition activity, and one the other hand, inhibition of IDO activity is capable of promoting T cell propagation effectively, so that the impurity of bodies on tumor cell attacks is improved. The furazan kind IDO / NAMPT double target inhibitor or the pharmaceutical compositions of the furazan kind IDO / NAMPT double target inhibitor are promising in application prospect, and are promising to be developed into anti-tumor drugs.

The invention belongs to the field of chemical medicine, and discloses a benzo nitrogen hetero-aromatic ring compound represented by formula I, or pharmaceutically acceptable salts, stereisomers, racemic compounds, prodrugs, or solvates thereof. The invention also discloses applications of the benzo nitrogen hetero-aromatic ring compound in preparation of drugs used for treating diseases caused byprotein kinase and / or nicotinamide phosphoribosyltransferase abnormal activity. The benzo nitrogen hetero-aromatic ring compound represented by formula I or the salts thereof possess tyrosine kinaseand Nampt double inhibition effects, can be taken as effective components in treatment or prevention of tumor, are excellent in curative effect, and low in toxic or side effect.

The invention discloses a tacrine-phenothiazine isodiad compound and a preparation method thereof, wherein the tacrine-phenothiazine isodiad compound has a structural formula shown by a general formula (I) and a general formula (II): the tacrine-phenothiazine isodiad compound is combined with tacrine and phenothiazine parent nucleuses which are used for effectively treating senile dementia, is added with a proper length of a linking group, has dual inhibition functions of Acetylcholinesterase (AchE) and tau protein hyperphosphorylation, is relatively lower in toxicity, and can be used for prevention and treatment of Alzheimer's Dieses (AD).

The present invention provides a compound represented by a formula I, or a pharmaceutically acceptable salt thereof, or a solvate thereof, which can selectively inhibit TDO and IDO1, and has an obvious inhibition effect on TDO and / or IDO1. Besides, the compound prepared by the invention has an obvious anti-tumor effect, also has a certain treatment effect on Parkinson's disease and Alzheimer's disease, and has a good application prospect in the field of medicine preparation.

The invention discloses a PARP-1 / PI3K double-target inhibitor or a pharmaceutically acceptable salt thereof, a preparation method and application thereof. According to the invention, the single active component can play a dual inhibition role on PARP-1 and PI3K, so that the dosage is reduced, the treatment effect is improved, and the toxic and side effects are reduced; and the dual inhibition effect on PARP-1 and PI3K is significant, the IC50 value of each target does not exceed 1.0 [mu]M, and the drug using the PARP-1 / PI3K double-target inhibitor as the active component can be used for treating a variety of cancers or tumors related to PARP-1 and / or PI3K.

The invention adopts a virtual medicine screening technology and a high-throughput screening technology, assesses the AChE inhibitory activity of more than ten thousand samples in a compound sample library and finds a batch of compounds with higher inhibitory activity by establishing a virtual acetylcholinesterase inhibitor screening method and an AChE activity detection method. Then according tothe pathological features of senile dementia, the compounds with higher AChE inhibitory activity are subject to butyryl choline esterase inhibitory activity detection. Research results show that bimolecular 3-piperidyl-ethyl phenyl ketone not only has comparatively high AChE inhibitory activity, but also has very strong BuChE inhibitory activity; the results of animal experiments prove that the bimolecular 3-piperidyl-ethyl phenyl ketone can remarkably improve aphronesia caused by scopolamine and sodium nitrite and can enhance the ability of learning and memory.

The invention provides an evodiamine derivative. The evodiamine derivative is prepared by taking an anthranilic acid compound and tryptamine as initial raw materials through a condensation reaction and a one-step ring closing reaction catalyzed by lewis acid. The evodiamine derivative prepared by the preparation method disclosed by the invention has dual inhibition effects on topoisomerase I / II, so a broad-spectrum anti-tumor effect is achieved. The derivative can induce apoptosis of cancer cells and retard proceeding to a G2 / M period in a concentration-dependent manner, and has an effect of inhibiting invasion and migration of cancer cells in vitro. The derivative has a good tumor growth inhibition effect in a nude mouse transplantation tumor model, has no obvious toxicity at a cell level and an animal level, has good safety and can be applied to preparation of anti-tumor drugs.

The invention belongs to the technical field of pharmacy, and in particular relates to novel application of (2E,6E)-2-(3,5-dimethoxy phenylidene)-6-(4-chlorphenyl methylene)cyclohexanone and a derivative thereof. With a moderate / high dose, the (2E,6E)-2-(3,5-dimethoxy phenylidene)-6-(4-chlorphenyl methylene)cyclohexanone and the derivative thereof provided by the invention can remarkably reduce the acute gouty arthritis mouse ankle joint swelling degree and the serum uric acid level, meanwhile have very good NLRP3 and TLR4 dual inhibition activity, have effects better than that of a positive control dexamethasone, can be used for preparing medicines for treating hyperuricemia or acute gouty arthritis, and is small in side effect and high in safety.

The invention provides methods of making and using compounds of the formula:or a pharmaceutically acceptable salt thereof; wherein n is an integer between 1 and 2 inclusively; m is an integer between 0 and 2 inclusively; X is selected from the group consisting of CH or N; R1 is selected from the group consisting of —CH2NH2, andR2 is selected from the group consisting of —H, —OH, —NH2 and acetyl; R3 is selected from the group consisting of —H, benzyloxycarbonyl and benzylsulfonyl; and R4 is selected from the group consisting of —OH,wherein p is an integer between 0 and 2 inclusively, Y is selected from the group consisting of —O—, —S—, —S(═O)—, —SO2—, methylene, —CH(OH)—, —CH(NH2)—, —CH(CH2—OH)—, —CH(CH2—NH2)— or —N(R6)—, R5 is selected from the group consisting of —H or a simple (C1-C3) alkyl and R6 is selected from the group consisting of —H, a simple (C1-C3) alkyl or a simple (C1-C3) acyl. These compounds are useful as anticoagulant agents as a result of their selective dual inhibition of thrombin and prothrombinase.

The invention discloses a preparation method and application of a photo-electrochemical thrombin aptamer sensor based on dual inhibition of PS@Au on ZnCdS, and belongs to the field of photo-electrochemical sensors. Zinc and cadmium co-doped sulfides, namely ZnCdS nanocrystals, are synthesized through a simple hydrothermal method, and through the rough surface and the large specific surface area ofZnCdS, the loading capacity of the ZnCdS is greatly improved, and the visible light absorption capacity of the ZnCdS is enhanced; the ZnCdS serves as a substrate material, the PS@Au serves as a secondary antibody marker, the PS@Au has good insulativity, thus transfer of photo-generated electrons is impeded, photocurrent signals are also effectively reduced through competition between the PS@Au and the ZnCdS to absorption of visible light, the sensitivity of the sensor is effectively improved through the dual-inhibition effect, and the detection limit of the sensor is lowered; and by combiningthe excellent selectivity of an aptamer, highly-sensitive detection of the thrombin aptamer is achieved, and important significance for analysis and detection of thrombin is achieved.

The invention discloses a histone deacetylase and microtubule dual target inhibitor and a preparation method thereof. The inhibitor is as shown in I) or II) in description, and the inhibitor has the dual inhibitory activity of microtubules and histone deacetylase simultaneously.

Inhibitors of HDAC and G9a inhibitors such as, for example, single compounds that inhibitor both HDAC and methyltransferase G9a (referred to herein as dual HDAC-G9a inhibitors, dual HDAC-G9a compounds, and dual HDAC-G9a inhibitor compounds) are described herein. For example, dual inhibitor compounds of Formulae I-III and methods of making and using thereof, are described herein. The dual inhibition activity of these compounds can provide inhibition of both histone deacetylase (HDAC) and histone methyltransferase G9a thereby providing anti-cancer effects.

The invention aims to provide a compound with single / double inhibitory activity on USP25 and USP28 proteases. The invention provides a compound shown as a formula I and a racemate, a stereoisomer, an isotope label, nitrogen oxide, a solvate, a polymorphic substance, a metabolite, a pharmaceutically acceptable salt or a prodrug of the compound.

The invention provides a targeted anti-tumor drug system and a preparation method thereof. The targeted anti-tumor drug system comprises an aptamer carrier and anti-tumor drugs immobilized onto the aptamer carrier, wherein the anti-tumor drugs are anthracycline antibiotics and porphyrin; and the aptamer carrier is an aptamer subjected to annealing treatment. The targeted anti-tumor drug system andthe preparation method thereof provided by the invention aim to perform targeted loading on dual anti-tumor drugs based on the guiding role and high-selectivity effect of the aptamer, and the aim ofrealizing dual inhibition of tumor proliferation is achieved by combining chemotherapy and photodynamic therapy.

The invention discloses a heterocyclic hydroxamic compound with a specific structure and pharmaceutically acceptable salts, isomers, prodrugs or solvates of the heterocyclic hydroxamic compound. A pharmaceutical composition contains the heterocyclic hydroxamic compound as an active ingredient. Experiments further prove that the compound and the pharmaceutical composition have dual inhibition effects on indoleamine 2, 3-dioxygenase and histone deacetylase, and can be applied to preparation of drugs for treating diseases related to abnormal regulation of 2, 3-indoleamine dioxygenase and histonedeacetylase. The diseases comprise cancer, neurodegenerative diseases, AIDS, senile dementia, malaria, diabetes and the like, and have a wide application prospect.

The invention discloses a drilling fluid, which comprises, by weight, 3-5% of bentonite, 0.1-0.5% of high viscosity sodium carboxymethyl cellulose, 0.1-0.6% of low viscosity sodium carboxymethyl cellulose, 0.05-0.3% of a fluid loss reducer, 0.3-2.0% of brown coal resin, 0.1-3.0% of KCl; 0.05-0.5% of Na2CO3, 1.0-5.0% of polymeric alcohol, 0.05-0.5% of cationic polyamine with coating effect (called cationic polyamine for short), 0.05-0.3% of an amino compound with filtrate loss reduction and inhibition effects (called amino compound for short), and the balance water. The drilling fluid system has dual inhibition effects, and good anti-collapse performance, can effectively solve clay shale hydrated dispersion expansion, borehole wall collapsing and other practical problems.

The invention relates to an aromatic amine compound and application thereof in the preparation of AR and BRD4 dual inhibitors and regulators. Specifically, the invention provides a compound shown as aformula I, and the compound has dual inhibition effects on AR and BRD4. The compound not only can inhibit proliferation of prostate cancer cell lines LNCaP / AR with multiple expression of androgen receptor AR, but also shows a good inhibition effect on prostate cancer cell lines VCaP and 22RV1, which are resistant to prostate cancer drugs (enzalutamide) on the market. The compound is used as a compound capable of simultaneously identifying AR and BRD4 double targets; can be used as an AR / BRD4 dual inhibitor, can also be used for preparing protein degradation targeting chimeras (PROTACs) for inducing AR / BRD4 dual-target degradation, and has a good application prospect in preparation of drugs for treating AR and BRD4 related diseases.