42 results about "Transport inhibitor" patented technology

Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT inhibition.

Disclosed is a herbicidal mixture comprising (a) at least one herbicide compound selected from the pyrimidines of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof:whereinR1 is cyclopropyl, 4-Br-phenyl or 4-Cl-phenyl;X is Cl or Br;R2 is H, C1-C14 alkyl, C2-C14 alkoxyalkyl, C3-C14 alkoxyalkoxyalkyl, C2-C14 hydroxyalkyl or benzyl; and(b) at least one additional herbicide or herbicide safener compound selected from the group consisting of (b1) ACCase inhibitors, (b2) AHAS inhibitors, (b3) photosystem II inhibitors, (b4) photosystem I electron diverters, (b5) PPO inhibitors, (b6) EPSP synthase inhibitors, (b7) GS inhibitors, (b8) VLCFA inhibitors, (b9) auxin mimics, (b10) auxin transport inhibitors, (b11) other herbicides selected from the group consisting of flamprop-M-methyl, flamprop-M-isopropyl, difenzoquat, DSMA, MSMA, bromobutide, flurenol, cinmethylin, cumyluron, dazomet, dymron, methyldymron, etobenzanid, fosamine-ammonium, isoxaflutole, asulam, clomazone, mesotrione, metam, oxaziclomefone, oleic acid, pelargonic acid and pyributicarb, (b12) herbicide safeners selected from the group consisting of benoxacor, 1-bromo-4-[(chloromethyl)sulfonyl]benzene, cloquintocet-mexyl, cyometrinil, dichlormid, 2-(dichloromethyl)-2-methyl-1,3-dioxolane, fenchlorazole-ethyl, fenclorim, flurazole, fluxofenim, furilazole, isoxadifen-ethyl, mefenpyr-diethyl, methoxyphenone, naphthalic anhydride and oxabetrinil, and their salts. Also disclosed is a method for controlling the growth of undesired vegetation comprising contacting the vegetation or its environment with a herbicidally effective amount of a mixture of the invention (e.g., as a composition described herein).

The invention discloses a super-elevation pumping marine concrete. The super-elevation pumping marine concrete is prepared from cement, fly ash, mineral powder, gravel, river sand, a hydration temperature rising regulation and control material, a corrosive ion transport inhibitor, a state modified material, an ultra dispersed water reducing shrinkage plasticity-maintaining additive and water in proportion. According to the super-elevation pumping marine concrete, by means of the hydration temperature rising regulation and control material, cracking caused by low high performance concrete, insufficient hydration and drying shrinkage in later period can be effectively avoided; by means of the hydration temperature rising inhibiting component, adiabatic temperature rising of the concrete can be lowered, and cracking generated by the temperature stress is reduced; by adopting the corrosive ion transport inhibitor, the pore structure of the concrete can be optimized, transport paths of ions such as Mg<2+> and Cl<->, and the concrete is better served in marine salt spray environment; the state modified material has the specific ball effect and water retention characteristic, and the phenomena of segregation and pipe blocking occurring in the super-elevation pumping process are avoided. The concrete is suitable for super-elevation pumping marine buildings and has the important engineering application value.

The present invention relates to herbicidally active compositions, which comprise 3-[5-(difluoromethoxy)-1-methyl-3-(trifluoromethyl)pyrazol-4-ylmethylsulfonyl]-4,5-dihydro-5,5-dimethyl-1,2-oxazole [common name pyroxasulfone] and at least one herbicide B and at least one herbicide B which is selected from group consisting of synthetic auxins and auxin transport inhibitors.The invention furthermore relates to a method for controlling undesirable vegetation, which comprises applying an herbicidal composition according to the present invention to the undesirable plants. Application can be done before, during and / or after, preferably during and / or after, the emergence of the undesirable plants. The herbicide A and the at least one herbicide B can be applied simultaneously or in succession.

Methods for identifying modulators of fatty acid transport and / or uptake, comprising contacting, under conditions favorable for fatty acid uptake, a putative modulator, e.g., an inhibitor with a system comprising genetic material encoding a fatty acid transport mediator (“TTM”), particularly FAA1, FAA2, FAA3, FAA4, FAT1, fadL, fadD, FATP, CD36 and FABP, or orthologs, homologs, isoforms, variants, analogs, derivatives or fragments thereof, and combinations thereof, or fatty acid transport mediator proteins (“TTMps”), e.g., Faa1p, Faa2p, Faa3p, Faa4p, Fat1p, FadL, fatty acyl CoA synthetase, FATP, CD36 and FABP, or orthologs, homologs, isoforms, variants, analogs, derivatives or fragments thereof, and combinations thereof, and determining the effect of the putative modulator. The test system may be a cell such as Saccharomyces cerevisiae, E. coli, H. sapiens, etc. or an in vitro system.

A filling apparatus for a grouting system. The filling apparatus comprises a first fill tube and a second fill tube. The first fill tube is discrete from the second fill tube. The first fill tube is disposed for transporting resin mastic and the second fill tube is disposed for transporting initiator. A portion of the first fill tube has an inlet opening through which an injection quill extends interiorly and downwardly through the first fill tube. The injection quill is disposed for transporting inhibitor. This disclosure also relates to a method for adjusting gel time of a grouting system used for anchoring a reinforcing member in an opening, a grouting system for anchoring a reinforcing member in an opening, and a method for anchoring a reinforcing member in a mine.

The present invention describes the design, synthesis and therapeutic use of a variety of novel inhibitors of polyamine transport. The main feature of this class of transport inhibitors is to incorporate a linker or side chain that prevents the uptake of polyamines and helps to conjugate polyamine analogs to form dimers with high inhibitory potency against polyamine uptake. These new compounds incorporate features that are designed to maximize their chemical and metabolic stability and their ability to bind to the polyamine transporter, and to minimize their toxicity by preventing their absorption by the cells. The purpose of such inhibitors is to prevent the uptake or salvaging of circulating polyamines by rapidly proliferating cells such as tumor cells, in order to potentiate the effect of therapeutic inhibitors of polyamine biosynthesis such as alpha-difluoromethylornithene.

The invention discloses a medicine for inhibiting geminivirus carried and transmitted by bemisia tabaci, application and a method for controlling geminivirus transmission. The medicine comprises one or a combination of an early internal transport inhibitor and a cytoskeleton inhibitor. According to study, early internal transport proteins and cytoskeleton proteins of bemisia tabaci and coding genes of the proteins can serve as targets for inhibiting geminivirus carried and transmitted by bemisia tabaci, by virtue of an inhibitor BrefA or after genes of the early internal transport proteins and cytoskeleton proteins are subjected to RNA interference silent expression, the ability of the bemisia tabaci for carrying and transmitting the geminivirus can be effectively inhibited, so that field transmission of the geminivirus can be effectively controlled.

A filling apparatus for a grouting system. The filling apparatus comprises a first fill tube and a second fill tube. The first fill tube is discrete from the second fill tube. The first fill tube is disposed for transporting resin mastic and the second fill tube is disposed for transporting initiator. A portion of the first fill tube has an inlet opening through which an injection quill extends interiorly and downwardly through the first fill tube. The injection quill is disposed for transporting inhibitor. This disclosure also relates to a method for adjusting gel time of a grouting system used for anchoring a reinforcing member in an opening, a grouting system for anchoring a reinforcing member in an opening, and a method for anchoring a reinforcing member in a mine.

Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT inhibition.

The invention discloses a nano-precursor medium transport inhibitor and a preparation method thereof. The nano-precursor dielectric transport inhibitor comprises a nano-precursor, a dispersant, a crystal nucleus growth regulator, a stabilizer and water. The nano-precursor is a mixture of one or more of C1-22 organic carboxylate esters and C1-22 organic carboxylate salts. The preparation method hassimple processes and is easy to implement. The product has the characteristics of environmental protection and high efficiency and is very suitable for corrosion protection of reinforced concrete structures in a plurality of complex harmful ion-eroded environments such as saline-alkali land and ocean.

Compounds or compositions that are inhibitors and / or ligands of nucleoside transporters; and methods of treating cancer, heart disease and stroke, as well as AIDS and other infectious diseases

Described are compositions and methods to mitigate alternate bearing of perennial crops by use of a natural metabolite. In particular, the present disclosure provides a natural metabolite in the presence or absence of an auxin transport inhibitor to increase floral intensity (flower number) of the return bloom in the spring following the setting of a heavy on-crop to increase the yield of the putative off-crop year and, thus, increase cumulative crop yield. Additionally the present disclosure provides a natural metabolite in combination with one or both of a growth promoting type of plant growth regulator, and a hormone biosynthesis, transport or function inhibiting type of plant growth regulator.

The invention relates to an application of a cholesterol transport inhibitor in preparation of a reagent for inhibiting viruses from entering cells through clathrin-mediated viral endocytosis. The invention also relates to an application of the cholesterol transport inhibitor in preparation of a medicine resistant to enveloped virus infection. The novel applications of the cholesterol transport inhibitor discovered by the invention have important significance for biology, particularly viral research and drug development.

The invention generally relates to the field of monocarboxylate transport modulators, e.g., monocarboxylate transport inhibitors, and more particularly to new substituted-quinolone compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in treating, modulating, forestalling and / or reducing physiological conditions associated with monocarboxylate transport activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, obesity, diabetes, cardiovascular diseases, tissue and organ transplant rejection, and malaria.

The invention provides a biosensor for detecting transport, and application of the biosensor. Specifically, a method provided by the invention comprises the following steps: (a) providing a detectionsystem, wherein the detection system comprises (a1) a biosensor; (a2) a detection solution; (b) mixing the detection system with a substance to be detected and a transport inhibitor, or mixing the detection system with the substance to be detected and a transport substrate so as to form a first mixed solution; (c) optionally placing the first mixed solution for a period of time t; (d) separating the biosensor from the first mixed solution to obtain a separated biosensor; (e) detecting to obtain a transport detection result of the substance to be detected, or obtain a result of influence of thesubstance to be detected on a transporter. The biosensor is simple and convenient to operate as well as efficient and rapid in detection.

The present invention relates to chemical compounds that selectively inhibit glucose transporter 1 (GLUT1), to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.

Compounds or compositions that are inhibitors and / or ligands of nucleoside transporters; and methods of treating cancer, heart disease and stroke, as well as AIDS and other infectious diseases.

The invention discloses a sweet cherry branching agent and a preparation method and application thereof. According to the sweet cherry branching agent, different proportions of different plant hormones (cytokinin, gibberellin, brassinosteroid and the like) are designed, and the branching agent added with 20 kinds of formulas of materials with different proportions, such as an auxin inhibitor, a strigolactone inhibitor and silver nitrate is designed, through screening, it is found that five formulas can significantly improve the branching capacity of axillary buds of sweet cherries, that is, the branching number is significantly increased; and the five formulas are smeared on axillary buds of annual branches growing in summer growth seasons of the sweet cherries respectively, and the resultshows that the branching capacity of axillary buds growing in summer of sweet cherries can be remarkably improved by the branching agent composed of cytokinin, gibberellins, brassinosteroid, a strigolactone inhibitor, anethylene synthesis inhibitor and silver nitrate and two branching agents obtained by adding an auxin transport inhibitor on the basis of the branching agent formula.

These compounds are glutamine transporter inhibitors, e.g., alanine, serine, cysteine-preferring transporter 2 (ASCT2) inhibitors. Glutamine transporter inhibitors are useful to treat a variety of diseases, disorders, or conditions including cancer.

Disclosed herein are herbicidal compositions comprising a herbicidally effective amount of (a) a pyridine carboxylic acid herbicide or an agriculturally acceptable N-oxide, salt or ester thereof, and (b) a synthetic auxin herbicide, an auxin transport inhibitor, agriculturally acceptable salts or esters thereof, or combinations thereof. Also disclosed herein are methods of controlling undesirable vegetation which comprise applying to vegetation or an area adjacent the vegetation or applying to soil or water to prevent the emergence or growth of vegetation (a) a pyridine carboxylic acid herbicide or an agriculturally acceptable N-oxide, salt or ester thereof, and (b) a synthetic auxin herbicide, an auxin transport inhibitor, agriculturally acceptable salts or esters thereof, or combinations thereof, wherein (a) and (b) are each added in an amount sufficient to provide a herbicidal effect.

The invention generally relates to the field of monocarboxylate transport modulators, e.g., monocarboxylate transport inhibitors, and more particularly to new substituted-quinolone compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in treating, modulating, forestalling and / or reducing physiological conditions associated with monocarboxylate transport activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, obesity, diabetes, cardiovascular diseases, tissue and organ transplant rejection, and malaria.

The invention relates to an application of a cholesterol transport inhibitor U18666A as a sensitizer in preparation of an anti-tumor product. The invention discloses an application of GPNA and U18666A drug combination in tumor resistance, U18666A improves the killing effect of GPNA on tumor cells, and a new method for overcoming the defect that the anti-tumor drug effect of GPNA is reduced is provided. The application specifically comprises the following steps: (1) the GPNA and U18666A combined medication has a better anti-tumor effect; 2, the U18666A is used for increasing the sensitivity of tumor cells to glutamine limitation; 3, GPNA and U18666A are combined for use, so that the inhibition effect of GPNA on tumor cell proliferation can be enhanced; and 4, the GPNA and U18666A are combined for use, so that the death of tumor cells is remarkably promoted. Compared with the prior art, the pharmaceutical composition has a more remarkable anti-tumor effect.

The invention relates to an application of an anion transport inhibitor 4, 4 '-diisothiocyanatostilbene-2, 2'-disulfonic acid in preparation of medicines for preventing and / or treating obesity, and belongs to the technical field of new applications of medicines. The anion transport inhibitor 4, 4 '-diisothiocyano stilbene-2, 2'-disulfonic acid can be applied to preparation of drugs for effectively treating obesity, obesity caused by high-fat diet is effectively relieved, weight is reduced, accumulation of visceral fat, scapular fat and epididymis fat is reduced, and abnormal glucose metabolism caused by obesity is effectively relieved. The application of the anion transport inhibitor 4, 4 '-diisothiocyano stilbene-2, 2'-disulfonic acid in preparation of the medicine for treating obesity is disclosed for the first time, and the anion transport inhibitor 4, 4 '-diisothiocyano stilbene-2, 2'-disulfonic acid has an unexpected effect in the aspect of inhibiting obesity.

Disclosed herein are compositions comprising (a) a pyridine carboxylate herbicide or an agriculturally acceptable N-oxide, salt, or ester thereof and (b) a synthetic auxin herbicide, an auxin transport inhibitor, agriculturally acceptable salts or esters thereof, or combinations thereof. Also disclosed herein are methods of controlling undesirable vegetation, comprising applying, to vegetation or an area adjacent the vegetation or applying in soil or water to control the emergence or growth of vegetation, (a) a pyridine carboxylate herbicide or an agriculturally acceptable N-oxide, salt, or ester thereof and (b) a synthetic auxin herbicide, an auxin transport inhibitor, agriculturally acceptable salts or esters thereof, or combinations thereof.

The present invention relates to herbicidally active compositions, which comprise 3-[5-(difluoromethoxy)-1-methyl-3-(trifluoromethyl)pyrazol-4-ylmethylsulfonyl]-4,5-dihydro-5,5-dimethyl-1,2-oxazole [common name pyroxasulfone] and at least one herbicide B and at least one herbicide B which is selected from group consisting of synthetic auxins and auxin transport inhibitors.The invention furthermore relates to a method for controlling undesirable vegetation, which comprises applying an herbicidal composition according to the present invention to the undesirable plants. Application can be done before, during and / or after, preferably during and / or after, the emergence of the undesirable plants. The herbicide A and the at least one herbicide B can be applied simultaneously or in succession.