190 results about "Inositol phosphate" patented technology

The invention relates generally to methods for inhibiting angiogenesis. More particularly, methods for inhibiting angiogenesis comprise selectively inhibiting phosphoinositide 3-kinase delta (PI3Kδ) activity in endothelial cells. The methods may comprise administration of one or more cytotoxic therapies including but not limited to radiation, chemotherapeutic agents, photodynamic therapies, radiofrequency ablation, anti-angiogenic agents, and combinations thereof.

The present invention relates to selective inhibitors of phosphoinositide (PI) 3-kinase β, use of the selective inhibitors in anti-thrombotic therapy, and a method for screening compounds useful for the new anti-thrombotic therapy by detecting selective inhibitory activity of PI 3-kinase β of the compound. The invention also relates to novel compounds that are inhibitors of PI 3-kinase.

The present invention relates to a method for treating cancer using p38 / JTV-1 and a method for screening pharmaceutical composition for treating cancer. More particularly, this invention relates to the method for treating cancer, which comprises administering the effective amount of p38 / JTV-1 protein or a nucleic acid encoding for said protein to the patient and the method for screening a pharmaceutical composition for treating cancer characterized by selecting a substance having an effect on the increase of the activity of the p38 / JTV-1 protein and the intracellular level thereof.The method according to the invention can be effectively used to treat cancer through the mechanism of suppressing the proliferation of cancer cells by binding to FBP (FUSE-binding protein) and thereby promoting the ubiquitination of FBP to downregulate c-myc gene, which is a proto-oncogene, and the mechanism of promoting the apoptosis of cells by binding to PDK-1 (phosphoinositide-dependent protein) and thereby inhibiting the phosphorylation of AKT (serine / threonine kinase). Also, p38 / JTV-1 can be used as a target for screening of new anticancer agents, by virtue of such regulation mechanisms of p38 / JTV-1.

The methods and compositions disclosed herein concern the synthesis of a novel class of “two-headed” phospholipid-phosphoinositide hybrids possessing a carbon backbone, such as 2,3-diacylthreitol, erythritol or a synthetic module. The second phospholipid head group allows introduction of a biochemical or chemical moiety in a position orthogonal in space to those occupied by the phosphoinositide head group and the two acyl chains. The diacyl moieties allow for the incorporation of Pea-PIP2 into a lipid bilayer, while the Ptdlns(4,5)P2 moiety in the aqueous layer is specifically recognized by lipid binding proteins. In alternative embodiments of the invention, reporters, for example biotin, fluorophores and / or spin labels, are attached to the free amino group of the head groups of such molecules to specifically target the reporters to the lipid-water interface.

Morpholino-substituted pyridopyrimidine, quinolone, and benzopyranone derivatives inhibit phosphoinositide (PI) 3-kinase, an enzyme that regulates platelet-adhesion processes. As a consequence, the compounds in question have anti-thrombotic activity, as well as other pharmaceutical properties. The compounds claimed are represented by formula (I), (II) and (III). PI 3-kinase generates 3-phosphorylated PI second messengers which stimulate platelet adhesion under blood-flow conditions. Because platelet adhesion is a necessary step in the formation of a thrombus, inhibition by these compounds of PI 3-kinase under such conditions inhibits or prevents thrombus formation. The compounds are useful in treating PI 3-kinase-dependent conditions including cardiovascular diseases such as coronary artery occlusion, stroke, acute coronary syndrome, acute myocardial infarction, vascular restenosis, atherosclerosis, and unstable angina; respiratory diseases such as asthma, chronic obstructive pulmonary diseases (COPD), and bronchitis; inflammatory disorders; neoplasms including cancers such as glioma, prostate cancer, small cell lung cancer, and breast cancer, and diseases linked to disordered white blood cell function, such as autoimmune and inflammatory diseases.

The invention relates to a composition that includes myo-inositol hexaphosphate applied by topical administration for utilisation in the treatment or prevention of a disease associated with the development of heterogeneous nucleants in a soft tissue. Said composition can be used for manufacturing a drug for the treatment of a disease associated with the development of heterogeneous nucleants in a soft tissue

The present invention relates to combination therapy with drugs, such as microtubule inhibitors, PARP inhibitors, Bruton kinase inhibitors or PI3K inhibitors, with antibodies or immunoconjugates against HLA-DR or Trop-2. Where immunoconjugates are used, they preferably incorporate SN-38 or pro-2PDOX. The immunoconjugate may be administered at a dosage of between 1 mg / kg and 18 mg / kg, preferably 4, 6, 8, 9, 10, 12, 16 or 18 mg / kg, more preferably 8 or 10 mg / kg. The combination therapy can reduce solid tumors in size, reduce or eliminate metastases and is effective to treat cancers resistant to standard therapies, such as radiation therapy, chemotherapy or immunotherapy. Preferably, the combination therapy has an additive effect on inhibiting tumor growth. Most preferably, the combination therapy has a synergistic effect on inhibiting tumor growth.

The invention belongs to the field of metal corrosion and protection and discloses a preparation method of an anticorrosive polyurea coating. The preparation method comprises processes of preprocessing a metal structure, removing oil, performing sand blasting, treating a metal surface, drying, spraying bottom polyurea paint and spraying surface polyurea paint. The preparation method is characterized in that an inositol phosphate solution is adopted in the metal surface treatment to form a chemical conversion film of inositol phosphate on the surface a the metal structure substrate; the bottom polyurea paint is aromatic polyurea paint; the surface polyurea paint is an aliphatic polyurea paint; the metal comprises steel, aluminum alloy and a zinc-plated steel structure; and the coating is 500-1500 mu m thick, the bottom layer is 300-1200 mu m thick, the surface layer is 200-400 mu m thick, and the bonding strength of the coating is higher than 10MPa. The preparation method provided by the invention is simple in process, convenient to operate and free from coating a primer.

This invention is directed to an acidic beverage composition, comprising; (A) a hydrated protein material having a combination of an inositol-6-phosphate content, an inositol-5-phosphate content, an inositol-4-phosphate content and an inositol-3-phosphate content of less than 8.0 μmol / g, with (B) a hydrated protein stabilizing agent and (C) at least one acid comprising a fruit juice, a vegetable juice, citric acid, malic acid, tartaric acid, lactic acid, ascorbic acid, glucono delta lactone or phosphoric acid, wherein the acidic beverage composition has a pH of from 3.0 to 4.5.

Described herein are benzoxazepin oxazolidinone compounds with phosphoinositide-3 kinase (PI3K) modulation activity or function having the Formula I structure:or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such PI3K modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon PI3K dysregulation.

The invention discloses a photoresist cleaning agent composition, which contains alcohol amine compound, water-soluble polar organic solvent and water, and also contains one or several selected from inositol phosphate ester and inositol phosphate salt. The cleaning agent composition can effectively remove photoresist on a semiconductor wafer, etched or ash incinerated photoresist residues or other residues, simultaneously has weak corrosion for metals such as aluminum, copper and the like and nonmetallic materials such as silicon oxide and the like, and has good application prospect in the microelectronic field such as cleaning of semiconductor wafers and the like.

The instant application relates to deazapurines, thienopyrimidines and furopyrimidines with zinc-binding moiety based derivatives and their use in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.

The instant application relates to deazapurines, thienopyrimidines and furopyrimidines with zinc-binding moiety based derivatives and their use in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.

The present invention relates to a method for identifying therapeutic agents for reducing and monitoring the growth, erosion, rupture or stability of an atherosclerotic plaque comprising the analysis of the differential expression of at least two genes coding proteins chosen among among Stearoyl CoA desaturase, Phosphatidic acid phosphate, and Phosphoinositide-specific-phospholipase-B1, eventually in association with the analysis of the differential expression of at least one gene coding a protein choosen in the group comprising Aldose reductase and aldehyde reductase, Sphingomyelinase, Acid ceramidase, Ceramide glucosyl transferase, Sphingosin phosphate liase, Thymosine beta 4, Aldehyde dehydogenase, ATPase Ca++ binding protein and CD163.

A lipid assay method, kit, and apparatus involving exposure of a protein, having a lipid recognition motif that interacts with a target lipid and a competing lipid, to a solution containing the competing lipid, and determining whether the target lipid is present in the solution. The target lipid has a stronger affinity to the lipid recognition motif than does the competing lipid. The lipid recognition motif is preferably a pleckstrin homology (PH) domain, with the target lipid being a phosphoinositide. The assay determines activity of a lipid kinase, the target lipid being a phosphorylation product of a reaction between the lipid kinase and a substrate lipid. The assay can be a cancer screening method for detection of cancer cells, where detection of certain levels of a PI(3,4,5)P3 target lipid is an indicator of a cancer cell.

The invention discloses a water-soluble electric contact lubricating protective agent improving the pluggable resistance of an electronic element and a use method thereof. The water-soluble electric contact lubricating protective agent comprises the following components in parts by weight: 10-15 parts of fatty alcohol and inositol phosphate, 3-6 parts of natural phospholipid, 3-8 parts of corrosion inhibitor, 10-20 parts of composite surfactant system, 15-25 parts of chelating agent, and 10-20 parts of detergent. A protective agent is adopted to lubricate the electronic element, and the protective agent is firstly diluted by 10-100 times with pure water, and preferably 100 / 8-100 / 4. Soaking technology is adopted for lubrication, the temperature is 20-60 DEG C, the time is 30-90 seconds, the drying temperature of a workpiece subjected to lubrication is 80-150 DEG C, and the time is 30-120 seconds. After the electronic element is treated by the protective agent disclosed by the invention, through a pluggable force test, an abrasion test and a salt fog test, the results show that the friction of the electronic element is obviously reduced, the pluggable resistance is obviously enhanced, and the long-term reliability of products is obviously improved.

The invention relates to new triazines (G=Q=U are N), pyrimidines (two out of G, Q and U are N), and pyridopyrimidines (one of G and U together with R2 forms an anullated pyridine ring) of formula (I) carrying a spirocyclic substituent, wherein E1 is CR4 or N; X1 is CHR4, CH2CH2, NR4, NR4→0, or O; and the other substituents are as defined in the specification. The compounds inhibit phosphoinositide 3-kinase (PI3K), mammalian target of rapamycin (mTOR), DNA-PK and ATM kinase, and may be used as therapeutic agents or diagnostic probes. The invention also relates to methods of using the compounds for treatment of associated pathological conditions.

The invention discloses a silver ion sterilizing dispersible tablet which comprises the following components by weight percent: 10-40% of main materials, 0.5-5% of bonding agent, 15-45% of filling agent, 10-40% of disintegrating agent, 0-35% of effervescing agent, 0.1-3% of flow aid and 0.5-5% of lubricating agent, wherein the main materials comprise one or combination of two of nanometer silver particles and complex silver ions, as well as gamma-aminobutyric acid, inositol hexaphosphate and glutathione. The silver ion sterilizing dispersible tablet enters into a single-cell bacterial body by utilizing the silver ions to interfere metabolism of the single-cell bacterial body and damage protein capsid and DNA (deoxyribonucleic acid) molecules of the single-cell bacterial body so as to kill the single-cell bacterial body. When the bacterial body is inactivated, the silver ions drift away for re-sterilizing, so that the anti-bacterial effect is lasting. Meanwhile, the sterilizing effect of the silver ions is not influenced by drug resistance, so that the killing effect of pathogenic bacteria with drug resistance is good and new drug resistance is not produced at the same time due to mechanism of action.

The present invention is directed to a nutritional formula for feeding human infants comprising isolated soy protein wherein the isolated soy protein has (a) a degree of hydrolysis of from about 0.5% up to about 30%; (b) a combination of an inositol-6-phosphate content, an inositol-5-phosphate content, an inositol-4-phosphate content and an inositol-3-phosphate content of less than about 8.0 μmol / g soy protein on a moisture free basis; and (c) a nitrite content of less than about 10 parts per million. Optionally, the isolated soy protein for the nutritional formula has a free amino acid content of up to about 25%. Further, the isolated soy protein for the nutritional formula optionally has a calcium content of from about 1.0% up to about 12%.

Pathogenic effector proteins which include one or more RxLR, dEER, Pexel or analogous motifs are blocked from entry into plant or animal cells by binding one or more of the motifs with a blocking compound which prevents binding of phosphoinositides or other polar lipids to the motifs which is a prerequisite for translocation of the pathogenic effector proteins into the plant or animal cell. The blocking compounds can take a variety of forms including synthetic peptides or the hydrophilic head-groups of phosphoinositides, phosphatidic acids, phospholipids, or sphingolipids. Suitable blocking compounds can be identified by assays demonstrating binding to RxLR, dEER, Pexel or analogous motifs. In addition, pathogenic effector proteins can be identified by analyzing whether they contain structural RxLR motifs using hidden markov modeling.

The invention provides a preparation method of autologous natural killer cell proliferation and culture. The preparation method of the autologous natural killer cell proliferation and culture is characterized in that mononuclear cells of a cancer patient are amplified and activated to obtain natural killer cells after the mononuclear cells are transfected by 3- phosphoinositide-dependent protein kinase-1 and CD122 and under the effect of K562 cells which are expressed stably serve as trophoblast cells and interleukin 2, proliferation times of the natural killer cells are above 2500, phenotype of CD16+ / CD56+ is above 90%, and in-vivo and in-vitro tests show that the natural killer cells have an anti-tumor and have quite high killer toxicity. The invention also provides a kit which is used for autologous natural killer cell proliferation and culture and is obtained by using the preparation method. The kit has an efficient anti-tumor function.

The present invention relates to methods of treating Alzheimer's Disease which utilize agents that increase neuronal phosphotidylinositol 4,5-biphosphate (PIP2), and to differentiated stem cell-based assay systems that may be used to identify agents that modulate phosphoinositide levels and thereby treat a variety of diseases. It is based, at least in part, on the discovery that edelfosine, an agent that increases PIP2 levels by inhibiting an enzyme that catalyzes PIP2 breakdown, decreases levels of neurotoxic A&bgr;42 peptide, particularly in cells expressing a mutant presenilin gene associated with Familial Alzheimer's Disease.

The invention provides an anti-cancer sustained-release agent co-carrying glucocorticoid and chemotherapeutic drugs and belongs to sustained-release injections. The anti-cancer sustained-release agent comprises sustained-release microspheres and a solvent, wherein, the sustained-release microspheres comprise anti-cancer active components and sustained-release auxiliary materials; and the solvent is a particular solvent containing a suspending agent. The glucocorticoid is selected from prednisolone, methylprednisolone, dexamethasone, betemethasone, triamcinolone acetonide or triamcinolone acetonide; the chemotherapeutic drugs are selected from phosphoinositide 3-kinase inhibitor, pyrimidine analogues and the like; the sustained-release auxiliary materials are biocompatible high-polymers, such as polylactic acid and the copolymers thereof, polyethylene glycol, carboxyl-terminated polylactic acid copolymers, polyfatty acid dimer-sebacic acid copolymers, poly(erucic acid dimer-sebacic acid), poly(fumaric-co-sebacic acid), polifeprosan and the like; and the suspending agent with the viscosity being 100cp to 3,000cp (at the temperature of 20 to 30 DEG C) is selected from sodium carboxymethyl cellulose and the like. The anti-cancer active components and the sustained-release microspheres can further be prepared into sustained-release implants which can effectively inhibit the growth of tumors, alleviate edema and improve the curative effects of radiotherapy and chemotherapy by intra-tumor or peri-tumor injection or placement.

Provided herein methods of screening for potential antidepressant compounds effective to increase production of cellular CDP-diacylglycerol and synthesis of inositol phospholipid in depression-related areas of the brain. Also, provided are methods of diagnosing and treating depressive or mood disorders in a subject by administering these screened antidepressant compounds. Further provided is a method of determining the therapeutic efficacy of an antidepressant drug regimen by comparing the ratio of CDP-diacylglycerol / inositol phosphate after treatment to a basal ratio in a subject.

Disclosed is a compound anticancer slow release agent which comprises slow release microspheres and dissolvent, wherein the slow release microballoons comprise anti-cancer active constituents and slow release auxiliary materials, the dissolvent being specific dissolvent containing suspension adjuvant. The anticancer effective ingredients include Aclarubicin, Idarubicin, Doxorubicin, Epirubicin, Valtaxin, Pirarubicin, Losaxantrone, Losoxantrone and / or anticancer antibiotic synergistic agents selected from phosphoinositide-3-kinase inhibitor, pyrimidine analogues and / or DNA restoration enzyme inhibitor, the slow release auxiliary materials are selected from polylactic acid copolymer EVAc, or sebacic acid copolymer, the viscosity of the suspension adjuvant is 100-3000cp (at 20-30 deg C). The slow release microspheres can also be prepared into slow release implanting agent for lowering down the whole body toxicity reaction of the medicament when locally dispensing on the tumor, and for selectively increasing the tumor local medicinal concentration.

The invention relates to compound orthophthalaldehyde disinfectant, and a preparation method and application thereof. The compound orthophthalaldehyde disinfectant is prepared from orthophthalaldehyde (1), tetrakis hydroxymethyl phosphonium sulfate (2), inositol phosphate (3), a penetrating agent (4), ampholyticsurfactant (5) and deionized water (6). The compound orthophthalaldehyde disinfectant is characterized by that each 1000ml compound orthophthalaldehyde disinfectant comprising 1.0 to 102.4g of the orthophthalaldehyde and 1.3 to 133.3g of inositol phosphate. The compound orthophthalaldehyde disinfectant can kill enteropathogenic bacteria, pyogenic cocci, hepatitis virus, avian influenza virus, various epidemic diseases, bacterial spore and the like, and is applicable to performing sterilization on articles in farms, environments, air, ground, water, epidemic focus, health and epidemic prevention and the like.