Abstract: The present invention relates to use of two microRNAs in detection of lung cancer prognosis and in medicine preparation. Particularly, the invention relates to a composition comprising two small RNA molecules microRNA-150 and microRNA-886-3p, a device comprising the composition used in detection of lung cancer prognosis and in preparation of medicaments for inhibiting mammal and human lung cancer metastasis. Specifically, the expression levels of microRNA-150 and microRNA-886-3p can be used as the prognostic criteria of lung cancer prognosis, wherein high expression level of the gene combination indicates favorable therapeutic effect. The invention also relates to a device detecting the expression levels of microRNA-150 and microRNA-886-3p in mammalian and human lung cancer and a method for detecting the expression levels of microRNA-150 and microRNA-886-3p in samples.

Abstract: Methods of reducing spontaneous mutation rate of a cell in a subject in need thereof by reducing endogenous levels of miR-155 are described.

Abstract: The invention relates to a double-stranded ribonucleic acid (dsRNA) for inhibiting the expression of the Factor VII gene.

Abstract: The present disclosure provides, inter alia, formulation compositions comprising modified nucleic acid molecules which may encode a protein, a protein precursor, or a partially or fully processed form of the protein or a protein precursor. The formulation composition may further include a modified nucleic acid molecule and a delivery agent. The present invention further provides nucleic acids useful for encoding polypeptides capable of modulating a cell's function and/or activity.

Abstract: Novel cyclic phosphoramidate prodrugs of drugs of formula I their use in delivery of drugs to the liver, their use in enhancing oral bioavailability, and their method of preparation are described.

Abstract: The present invention provides a shark-like chondroitin sulphate and a process for the preparation thereof. In particular, the present invention relates to a shark-like chondroitin sulphate, having a very low amount of 4-sulphate, a high charge density and a biological activity comparable to natural chondroitin sulphates. The invention also relates to a process for the preparation of said shark-like chondroitin sulphate affording substantially higher productivities and better reproducibility of product quality. The shark-like chondroitin sulphate of the invention shows a high molecular mass and its in vitro biological and anti-inflammatory effectiveness has been shown to be comparable to that of natural products making this polysaccharide potentially useful as a drug in pharmaceutical preparations and nutraceuticals.

Abstract: Ophthalmic solutions containing arabinogalactans with a protective activity on the corneal epithelium, particularly suitable for use as artificial tears stimulating the recovery of corneal lesions and also particularly useful for contact lens users, containing from 1% to 10% by weight of arabinogalactan in an aqueous solution and possible other excipients, among which tonicity-adjusting agents, pH correctors, buffers and preservatives, except for benzalkonium chloride. The compositions according to the invention have a virtually negligible viscosity, but are sufficiently mucoadhesive to assure a considerable permanence time in the area of application. Besides being well-tolerated, the aforesaid compositions have considerable re-epithelization capacity.

Abstract: A method for constructing a compound of immunologically modified nanotubes and method for using the compound to deliver immunoadjuvants to tumor cells and to produce targeted, synergistic photophysical and immunological reactions for cancer treatment. To prepare the immunologically modified nanotubes, carbon nanotubes are dissolved in a solution of glycated chitosan, an immunostimulant, hence using glycated chitosan as a surfactant for rendering the aqueous solution of nanotubes stable. The compound can be used for treatment of cancer. The method includes steps of intratumorally administering immunologically modified nanotubes and administering laser irradiation of the target tumor. The nanotube serves as a carrier to deliver immunoadjuvants to the tumor cells and serves as a light-absorbing agent in a cell body of a tumor in a host.

Abstract: A method for reversing gelation of hydrophobically modified biopolymer attached to vesicle or cell membranes. The gelation of hydrophobically modified biopolymer attached to vesicles or cell membranes is reversed by application of a supramolecule, such as cyclodextrin, to the gelled composition. The supramolecule disrupts the interactions between the hydrophobically modified biopolymer and the vesicle or cell membrane, without affecting the structure of the membrane or the hydrophobically modified polymer to which the hydrophobic substituents are attached. A kit for treating wounds that includes a hydrophobically modified biopolymer and a supramolecule. The hydrophobically modified biopolymer is used to stop bleeding and the supramolecule is used to remove the hydrophobically modified biopolymer.

Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.

Abstract: Disclosed herein are formulations and methods of manufacture of compounds of formula (E): wherein X and Y independently represent leaving groups and A+ is an ammonium cation.

Abstract: The present invention is directed to a stabilized cross-linked hydrogel matrix comprising a first high molecular weight component and a second high molecular weight component that are covalently linked, and at least one stabilizing or enhancing agent, wherein the first high molecular weight component and the second high molecular weight component are each selected from the group consisting of polyglycans and polypeptides. This stabilized hydrogel matrix may be prepared as bioactive gels, pastes, slurries, cell attachment scaffolds for implantable medical devices, and casting or binding materials suitable for the construction of medical devices. The intrinsic bioactivity of the hydrogel matrix makes it useful as a gel or paste in multiple applications, including as a cell attachment scaffold that promotes wound healing around an implanted device, as gels and pastes for induction of localized vasculogenesis, wound healing, tissue repair, and regeneration, as a wound adhesive, and for tissue bulking.

Abstract: The present invention relates to thiazole derivatives of formula I and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.

Abstract: Phosphoramidate alkylator prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents.

Abstract: Provided is a lotion that exhibits high percutaneous absorption inherent in maxacalcitol, allows the maxacalcitol to be stable, and exhibits less dripping when it is applied to heads. A basic oil-in-water emulsion lotion containing 22-oxa-1?, 25-dihydroxyvitamin D3, medium-chain triglyceride, a nonionic surfactant, and a water-soluble thickener and a method of treatment of skin disorders using the same.

Abstract: Compounds of formula I are provided where X1, X2, and X3 are independently selected from H or hydroxy protecting groups. Such compounds may be used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.

Abstract: Optionally substituted 4,5,7,8-tetrahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-2H-imidazo[1,2-a]pyrrolo[3,4-e]pyrimidine or 4,5,7,8,9-pentahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-2H-pyrimido[1,2-a]pyrrolo[3,4-e]pyrimidine compounds or Compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising the same.

Abstract: Compositions containing micronized tanaproget, or a pharmaceutically acceptable salt thereof, and ethinyl estradiol and methods of preparing the same are provided. Also provided are kits containing the compositions, methods of contraception and hormone replacement therapy including administering a composition containing micronized tanaproget and ethinyl estradiol.

Abstract: Compounds and compositions, and methods of use thereof, for treatment and/or prevention of multiple sclerosis, including symptoms associated with multiple sclerosis, and/or treatment and/or prevention of other disease/disorder affecting the nervous system (e.g. central, peripheral) or muscle including symptoms thereof, comprising administering to a subject in need thereof daptomycin and/or daptomycin-related lipopeptide.

Abstract: New aminooxime derivatives at position 3 of 2- and/or 4-substituted androstanes and androstenes, processes for their preparation, and to pharmaceutical compositions containing them for the treatment of cardiovascular disorders, such as heart failure and hypertension. In particular compounds having the general formula (I) are described, where the radicals have the meanings described in detail in the application.

Abstract: A method of inhibiting blood platelet aggregation in a mammal is provided. The method comprises the administration of a platelet aggregation inhibiting amount of a modified amino acid or pharmaceutically acceptable salt thereof.

Abstract: The invention relates to diazo bicyclic mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.

Abstract: Compounds of Formula I, including pharmaceutically acceptable salts thereof: wherein A is selected from the group consisting of: are useful as HIV attachment inhibitors.

Abstract: The present invention relates to small molecule potentiators of metabotropic receptors, in particular of the mGlu2 receptor. The present invention also relates to the use of these compounds for the prevention or treatment of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The present invention thus provides compounds of formula I and variables defined herein.

Abstract: Compositions, kits, and methods for the treatment or prevention of ocular allergies and inflammation and the symptoms thereof containing alcaftadine or a pharmaceutically acceptable salt thereof.

Abstract: The present invention is concerned with spiro-dihydrotetraazabenzoazulenes, i.e. spiro-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes of formula I wherein R1, R2, R3, X, Y, Z, m and n are as described herein. The compounds according to the invention act as V1a receptor modulators and are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.

Abstract: The present invention provides a novel benzodiazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The benzodiazepine compound of the invention is represented by General Formula (1) wherein R1, R2, R3, and R4 are each independently hydrogen or lower alkyl; R2 and R3 may be linked to form lower alkylene; Al is lower alkylene optionally substituted with one or more hydroxy; and R5 is group represented by wherein R6 and R7 are each independently hydrogen or organic group; XA and XB are each independently bond, lower alkylene, etc.

Abstract: The invention provides a compound of the formula (1): or a salt, solvate, N-oxide or tautomer thereof.

Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.

Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.

Abstract: The object aims to find a novel pharmacological activity of a novel 1,2,3,4-tetrahydroquinoxaline derivative which contains, as a substituent, a phenyl group having a sulfonic acid ester structure introduced therein. A compound represented by general formula (1) or a salt thereof is useful as a glucocorticoid receptor agonist, particularly as a therapeutic agent for diseases against which a glucocorticoid receptor agonist (e.g., a steroid) is believed to be effective, such as inflammatory bone/joint diseases, inflammatory ophthalmic diseases (inflammatory ophthalmic diseases in the anterior or posterior segment of an eye).

Abstract: The present invention relates to a specific salt of a dihydropteridione derivative, namely the trihydrochloride salt of the compound N-[trans-4-[4-(cyclopropylmethyl)-1-piperazinyl]cyclohexyl]-4-[[(7R)-7-ethyl-5,6,7,8-tetrahydro-5-methyl-8-(1-methylethyl)-6-oxo-2-pteridinyl]amino]-3-methoxy-benzamide, to its crystallization in the form of an hydrate with water, to a process for the manufacture thereof, and to the use thereof in a pharmaceutical composition.

Abstract: This invention comprises the novel compounds of formula (I) wherein R1, R2, R3 and X have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.

Abstract: External preparations for athlete's foot treatment capable of enhancing patient's compliance and capable of reducing the symptom of rubefaction, comprising an anti-trichophyton drug mixed with at least one compound selected from among 1-menthol, menthol analogue compounds and bactericidal compounds.

Abstract: The use of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine in the treatment of pain and residual symptoms in depression is provided.

Abstract: Disclosed is a compound which has both an angiotensin-II receptor antagonistic activity and a PPAR? activation activity and is useful as a prophylactic and/or therapeutic agent for hypertension, heart diseases, angina pectoris, cerebrovascular disorders, cerebral circulatory disorders, ischemic peripheral circulatory disorders, renal diseases, arteriosclerosis, inflammatory diseases, type-2 diabetes, diabetic complications, insulin resistance syndrome, syndrome X, metabolic syndrome and hyperinsulinemia. [In the formula, A represents a 5- to 10-membered heteroaryl group; R1 and R2 independently represent a C1-6 alkyl group; and each of R3 to R5 is absent or represents H, a halogen atom, OH, NO2, a halo-C1-6 alkyl group, a (substituted) C1-6 alkoxy group, a (substituted) C3-6 cycloalkyloxy group, or a 5- to 10-membered heteroaryl group.

Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

Abstract: A compound of Formula I in free or salt or solvate form, where R1, R2, R3, R4, R5, R6, R7, R8 and R9 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

Abstract: The present application relates to novel amides and thioamides, to processes for preparation thereof and to the use thereof for controlling animal pests, in particular arthropods and especially insects.

Abstract: The invention provides novel substituted pyridopyrimidines represented by Formula I or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as inhibitors of the phosphoinositide 3? OH kinase family (PI3K) for the treatment of inflammatory diseases, cancer, cardiovascular diseases, allergy, asthma and autoimmune disorders.

Abstract: Concentrated methotrexate solutions are described which are suitable for the use of an active substance in the production of a parenterally administered medicament for the treatment of inflammatory autoimmune diseases. The methotrexate is added to a pharmaceutically acceptable solvent at a concentration of more than 30 mg/ml. The invention also relates to a ready-made syringe and a carpule containing such a pharmaceutical solution formulation, as well as a pen injector comprising such a carpule and/or a ready-made syringe.

Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R3 are as defined herein, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).

Abstract: The invention relates to compounds of general formula 1 to processes for the production thereof, to pharmaceutical preparations containing said compounds and/or physiologically compatible salts and/or solvates which can be produced therefrom as well as to the pharmaceutical use of said compounds, the salts or solvates thereof as inductors of apoptosis in the case of non-solid malignant tumors of the hematopoietic system, in particular in the case of leukemias and lymphomas, more particularly in the case of leukemic B lymphocytes.

Abstract: The present invention is directed to dihydrobenzoquinazilinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

Abstract: The present invention relates to a method of combating animal pests which comprises contacting the animal pests, their habit, breeding ground, food supply, plant, seed, soil, area, material or environment in which the animal pests are growing or may grow, or the materials, plants, seeds, soils, surfaces or spaces to be protected from animal attack or infestation with a pesticidally effective amount of at least one 6-halogeno[1,2,4]triazolo[1,5-a]-pyrimidine of the general formula (I), wherein X, R1, R2, R3 and R4 are as defined in claim 1 and/or the agriculturally useful salts thereof.

Abstract: 1H-Pyrrolo[2,3-b]pyridine compounds are inhibitors of cell proliferation/cell vitality and can be employed for the treatment of tumors.

Abstract: Described herein are spiperone derivative compounds which have been found to be useful in methods of stimulating CaCC and treating disorders (or symptoms thereof) associated with CaCC including cystic fibrosis, wherein a compound of the invention is administered to a subject.

Abstract: Indenoisoquinolinone derivatives (I), the manufacturing method and the medical use thereof, which belong to pharmaceutical chemistry and organic chemistry field, are disclosed. These compounds can be used for treating several medical symptoms related to postmenopausal syndrome, uterine fibers deterioration and aortic smooth muscle cells proliferation, especially ER-(+) depend breast cancer. Meanwhile, these compounds can also be used for treating glioma and lung cancer, and have inhibiting effect on tumor metastasis effect on tumor metastasis.

Abstract: An extended release oral dosage form comprising as active substance tacrolimus or a pharmaceutically active analogue thereof for a once daily immunosuppressive treatment of a patient in need thereof, preferable a kidney or liver transplant patient. The dosage form releases the active substance over an extended period of time. It also provides improved pharmacokinetic parameters due to an extended and constant in vivo release including substantial decreased peak concentrations, despite increased bioavailability, substantial extended times for maximal concentration, and higher minimal concentrations when compared with conventional immediate release dosage forms and a recent modified release tacrolimus dosage form.

Abstract: Disclosed herein are R-7-(3-aminomethyl-4-methoxyimino-3-methyl-pyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid and L-aspartic acid salt, process for the preparation thereof and pharmaceutical composition comprising the same for antimicrobial. Because the R-7-(3-aminomethyl-4-methoxyimino-3-methyl-pyrrolidin-1-yl) -1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid and L-aspartic acid salt is more soluble and less toxic and has less side effects as an antimicrobial agent than hydrochloride and the other salts (D-aspartate and phosphate) conventionally used, the salt may be useful for oral and injectable administration.