The present invention is related to an L nucleic acid that binds to an SDF-1.

The present disclosure relates to non-naturally occurring polypeptides useful for preparing Ezetimibe, polynucleotides encoding the polypeptides, and methods of using the polypeptides.

A cytosine analog, a method of preparation of a cytosine analog, a DNA methyltransferase 1 inhibitor, and a method for DNA methylation inhibition, is provided for the treatment of diseases associated with deviations from normal DNA methylation. The analog of cytosine may be comprised of 1, N4, 5 and 6-substituted derivatives of cytosine or 5,6-dihydrocytosine, wherein the analog can be described by the chemical formula where R1 is H, R3, R4, 2'-deoxyribosyl, R4 is alkyl or aryl, X is N or C, wherein if X in the analog of formula I is N, then R5 is no substituent and if X in the analog of formula I and/or II is C or if X in the analog of formula II is N, then R5 and R6 are independently alkyl, aryl, hydroxyalkyl, aminoalkyl, hydroxyl, carboxyl, amino group, alkoxyl, aryloxyl, aminoalkyl, aminoaryl, thio group, sulfonyl, sulfinyl or halogen.

RNA interference is provided for inhibition of Frizzled Related Protein-1 mRNA expression, in particular, for treating patients having glaucoma or at risk of developing glaucoma.

The present invention relates to the field of cardiology. More specifically, the present invention provides methods and compositions for inducing proliferation of cardiomyocytes. In a specific embodiment, a method for inducing proliferation of cardiomyocytes comprises the step of administering an effective amount of an ALMS1 inhibitor.

A composition comprising an SL0101 [kaempferol 3-O-(3″,4″-di-O-acetyl-α-L-rhamnopyranoside)] derivative compound that has enhanced ability to inhibit RSK activity, relative to the parent compound is provided. The compounds have utility for treating any disease or conditions characterized or associated with excess or undesirable RSK activity. For example the RSK inhibitors of the present invention can be used to reduce the proliferation of neoplastic cells or for inhibiting the establishment or maintenance of an intracellular pathogenic infection by pathogens whose pathogenicity derives in part from the pathogen's ability to impede endosomal/phagosomal maturation in the host cell.

The present disclosure generally relates to dry solid matrices for the extraction, stabilization, and storage of nucleic acids, particularly RNA, in a dry format under ambient conditions for a prolonged period of time. Methods for collecting and recovering the nucleic acids stored in the dry solid matrix are also described.

Security measures for tokens comprise storing security rules associated with a generated token in a memory. A processor, communicatively coupled to the memory, accesses the security rules associated with the generated token and determines whether to encrypt the generated token by applying at least a portion of the security rules to the generated token. The processor encrypts the generated token. An interface, communicatively coupled to the processor, communicates the encrypted token to a mobile device associated with a user.

A data processing system on an integrated circuit includes a core that performs switching operations responsive to a system clock that draws current from the power supply network. An IR-drop detector includes a resistor ladder having outputs representative of an IR-drop caused by the core during the switching operations. The system further includes a plurality of amplifiers coupled to the outputs indicative of the IR-drop, a plurality of flip-flops coupled to the amplifiers, and a variable clock generator. The variable clock generator outputs a sampling clock comprising a group consisting of a variable phase or a variable frequency to the plurality of flip-flops. The flip-flops are triggered by the sampling clock so that the IR-drop at a time during a clock cycle of the system clock can be detected, and the peak IR-drop value for can be tracked.

A system, methods and server for monitoring health and safety of individuals in a population and sending alert notifications when exceptions are detected include comparing biometric data obtained from the individuals to a biometric model generated for the individual through computer-learning methods. Biometric data may be gathered by wireless biometric sensor devices which transmit biometric data to receiver devices, which relay the biometric data to a server. The biometric model may be maintained in the server and include nominal and threshold biometric parameters for each individual based on biometric sensor data gathered or analyzed over a period of time. An alert may be issued by the server when an individual's biometric data is outside a threshold in the biometric model. The transmitted alert may depend upon the nature of the exception, user settings and past notification experience. Alerts may be escalated when not answered within defined durations.

An intracorporeal marker, for marking a site within living tissue of a host, includes an outer body portion of biodegradable material. An inner body portion is located in the outer body portion. The inner body portion includes biological material that becomes calcified in the living tissue of the host over time. An agent interacts with the biological material to promote calcification of the biological material of the inner body portion in the living tissue of the host.

A biometric monitoring device measuring various biometric information is provided that allows the person to take and/or display a heart rate reading by a simple user interaction with the device, e.g., by simply touching a heart rate sensor surface area or moving the device in a defined motion pattern. Some embodiments of this disclosure provide biometric monitoring devices that allow a person to get a quick heart rate reading without removing the device or interrupting their other activities. Some embodiments provide heart rate monitoring with other desirable features such as feedback on data acquisition status.

The described invention provides a disposable handheld biopsy device for taking biopsies, the biopsy device comprising a tissue cutting assembly which has features to control the tissue length that will be severed by the cutting assembly; and a vacuum assembly which has features to control the vacuum level. The disposable handheld biopsy device of the described invention is simple, lightweight, portable, and cost effective to manufacture and dispose of.

The subject of the present invention are novel esters of (acyloxymethyl)acrylamide, a pharmaceutical composition containing them and their use in the production of drugs for the prophylaxis or treatment of oncogenic diseases and diseases connected with increased cell proliferation.

The invention provides certain bis-acylated hydroxylamine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.

A method for inhibiting the crystal growth rate of an amide compound present in a molten polyolefin-based resin and a method for producing a polyolefin-based resin molded article are provided. A phenol compound is incorporated into an amide compound-containing polyolefin-based resin such that a weight ratio, amide compound:phenol compound, is 60:40 to 10:90.

An object of the present invention is to improve the stability of an ethylenically unsaturated compound having an isocyanate group in the molecule by preventing a polymerization of the ethylenically unsaturated compound. The present invention relates to a stabilizing composition for an isocyanate group-containing ethylenically unsaturated compound, comprising: an isocyanate group-containing ethylenically unsaturated compound (A) which comprises one or more isocyanate groups and one or more ethylenically unsaturated groups in the molecule; and a stabilizing agent (B) which is a compound in which at least one of the ethylenically unsaturated groups in the compound (A) is replaced with an alkyl group which may have a substituent.

The invention provides a process for the synthesis of a polycarbonate, the process comprising the step of reacting carbon dioxide with at least one epoxide in the presence of a catalyst of formula (I) and a chain transfer agent. The invention also provides a polymerization system for the copolymerization of carbon dioxide and at least one epoxide comprising a catalyst of formula (I) and a chain transfer agent, polycarbonates produced by the inventive process, a block copolymer comprising a polycarbonate produced by the inventive process, and a method of producing the block copolymer. The invention also relates to novel catalysts of formula (III).

The present invention relates to organometallic compounds useful in the treatment of metastasis. The organometallic compounds comprise a ligand that is covalently bound to a bioactive compound, which is an inhibitor of a resistance pathway or a derivative thereof. Preferably, the organometallic compounds are half-sandwich (“piano-stool”) compounds. The compounds of the present invention offer a high variability with respect to the bioactive compound and to the nature of the ligand bound to a central transition metal.

The present invention relates to a stable mixture comprising surface-modified particles which are obtained by reacting metal oxide or semimetal oxide particles with at least one compound selected from among silicon-comprising compounds bearing at least one metaloxy radical and optionally further alkoxy and/or hydroxy radical(s) and at least one solvent, at least one surface-active substance or a mixture thereof, a process for producing the mixture, the use of these particles in systems in which they are brought into contact with at least one solvent, where the mass ratio of solvent to modified particle is greater than 500, and also the use of these particles in agglomeration-deagglomeration cycles.

A substituted phenoxyethyl(isopropyl)acyloxyalkyl phosphonate having phosphorusheterocyclic ring and having herbicidal activity, with a general formula of I, wherein R represents 5,5-dimethyl-1,3,2-dioxaphosphorinan-2-one-2-yl, or 1-oxo-1-phospha-2,6,7-trioxabicyclo[2,2,2]octan-4-yl, or 1-sulfo-1-phospha-2,6,7-trioxabicyclo 2,6,7-trioxabicyclo[2,2,2]octan-4-yl; R1 represents H, C1-C4 alkyl, phenyl, furyl, pyridyl, or phenyl substituted with methyl, methoxyl, nitro or chloro; R2 represents H, methyl, and methyl only if R in the general formula I is 1-sulfo-1-phospha-2,6,7-trioxabicyclo[2,2,2]octan-4-yl as phosphorusheterocyclic ring; X and Y represent H, halogen, C1-C4 alkyl or trifluoromethyl, and X and Y are the same or different. The compounds according to the present invention may be used as active component of dicotyledonous broadleaf weed herbicides.

Provided is a compound which has strong and sustaining intraocular pressure lowering action and, further, has no fear of side effect on eyes. Since a compound represented by the formula (I): wherein definition of each group is as described in the specification, or a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering action and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc.

A compound with a diphenylmethane moiety having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney is disclosed. A pharmaceutical composition including the compound as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes is disclosed. A method for preparing the compound, and a method for preventing or treating metabolic disorders, particularly diabetes, by using the compound is provided.

The invention relates to a process for preparing 1-aryl-pyrazol-3-one intermediates, tautomers, and salts thereof, to novel intermediates, and to the use of the intermediates in the preparation of sigma receptor inhibitors.

Disclosed in the present invention is a novel histone deacetylase inhibitor of benzamides and use thereof. The inhibitor has good efficacy in treating diseases caused by abnormal gene expression, such as tumors, endocrine disorders, immune system diseases, genetic diseases and nerve system diseases. The histone deacetylase inhibitor of benzamides is a compound of the following general chemical structural formula (I) or a salt thereof.

The present invention is directed to a novel process for the preparation of compounds having inhibitory activity against sodium-dependent glucose transporter (SGLT) being present in the intestine or kidney.

Steroid compounds having increased resistance against metabolism and increased water solubility are disclosed, together with methods for their production. These substances are suitable for the manufacture of pharmaceuticals for the treatment of steroid related or steroid induced CNS disorders and for use in methods of prevention, alleviation or treatment of such disorders.

Bile acids and related compositions and methods of synthesis and use. More specifically, deoxycholic acid and related compositions, said compositions being free of all moieties of animal origin and free of pyrogenic moieties.

Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-17 bicyclic amines of triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II and III: These compounds are useful for the treatment of HIV and AIDS.

A way to formulate prasterone to both increase its oral bioavailability, and decrease the variability of its oral bioavailability. In contrast to the approach taught by the prior art, the instant approach is amenable to scale-up to commercial scale. Further, the resulting product is amenable to analysis using standard, known quantitative analytical techniques; thus, unlike the prior art approach, the instant approach may be used to manufacture a product in conformity with applicable regulatory standards.

Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-3 cycloalkenyl triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II, III and IV: wherein X can be a C4-8 cycloalkyl, C4-8 cycloalkenyl, C4-9 spirocycloalkyl, C4-9 spirocycloalkenyl, C4-8 oxacycloalkyl, C4-8 dioxacycloalkyl, C6-8 oxacycloalkenyl, C6-8 dioxacycloalkenyl, C6-9 oxaspirocycloalkyl, or C6-9 oxaspirocycloalkenyl ring. These compounds are useful for the treatment of HIV and AIDS.

The present invention relates to processes for the crystallisation and for the preparation and isolation of a novel crystalline form of fusidic acid, to the use of said processes in the manufacture of pharmaceutical formulation or medicament, and to the use of said crystalline fusidic acid form for the treatment of bacterial infections.

A hydrophobic cationic steroidal anti-microbial (ceragenin) compound forms an amphiphilic compound having a hydrophobic sterol face and a hydrophilic cationic face. The hydrophobic CSA also includes a hydrophobic substituent that gives the ceragenin compound a CLogP value of at least 6.5.

Tissue slices and whole organisms offer substantial challenges to fluorescence imaging. Autofluorescence and absorption via intrinsic chromophores, such as flavins, melanin, and hemoglobins, confound and degrade output from all fluorescent tags. An “optical window,” farther red than most autofluorescence sources and in a region of low hemoglobin and water absorbance, lies between 650 and 900 nm. This valley of relative optical clarity is an attractive target for fluorescence-based studies within tissues, intact organs, and living organisms. Novel fluorescent tags were developed herein, based upon a genetically targeted fluorogen activating protein and cognate fluorogenic dye that yields emission with a peak at 733 nm exclusively when complexed as a “fluoromodule”. This tool improves substantially over previously described far-red/NIR fluorescent proteins in terms of brightness, wavelength, and flexibility by leveraging the flexibility of synthetic chemistry to produce novel chromophores.

Novel active compound combinations comprising a carboxamide of the general formula (I) (group 1) in which A, R1, R2 and R3 are as defined in the description,and the active compound groups (2) to (23) listed in the description have very good fungicidal properties.

The present invention relates to novel active compound combinations comprising, firstly, at least one known compound of the formula (I) in which R1 and A have the meanings given in the description and, secondly, at least one further known active compound from groups (2) to (27) listed in the description, which combinations are highly suitable for controlling animal pests such as insects and unwanted acarids and also phytopathogenic fungi.

The present invention relates to compositions, in particular within a fungicide composition, which comprises (A) a dithiino-tetracarboximide of formula (I) and a further fungicidally active compound (B). Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and to the treated seed.

The present invention generally relates to a method for minimizing the formation of insoluble salts of phenoxy herbicides. The method comprises (1) mixing a compatibility agent, amine salts of phenoxy acid herbicides, and a chemical containing non-amine cations in a aqueous system to form a stable and non-nozzle plugging solution; and (2) application of said stable and non-nozzle plugging solution onto target plants.

The present invention relates to compositions, in particular within a fungicide composition, which comprises (A) a dithiino-tetracarboximide of formula (I) and a further fungicidally active compound (B). Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and to the treated seed.

The present invention relates to compositions, in particular within a fungicide composition, which comprises (A) a dithiino-tetracarboximide of formula (I) and a further fungicidally active compound (B). Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and to the treated seed.

Compositions and methods, including novel homogeneous microparticulate suspensions, are described for treating natural surfaces that contain bacterial biofilm, including unexpected synergy or enhancing effects between bismuth-thiol (BT) compounds and certain antibiotics, to provide formulations including antiseptic formulations. Previously unpredicted antibacterial properties and anti-biofilm properties of disclosed BT compounds and BT compound-plus-antibiotic combinations are also described, including preferential efficacies of certain such compositions for treating certain gram-positive bacterial infections, and distinct preferential efficacies of certain such compositions for treating certain gram-negative bacterial infections.

An inhibitor for tobacco axillary bud growth, the inhibitor containing one or more cell division inhibitors selected from pyridine-based compounds and benzamide-based compounds. This inhibitor may further include an aliphatic alcohol having 6 to 20 carbon atoms in combination with the one or more cell division inhibitors.

Penoxsulam, 2-(2,2-difluoroethoxy)-N-(5,8-dimethoxy[1,2,4]-triazolo[1,5-c]pyrimidin-2-yl)-6-(trifluoromethyl)benzenesulfonamide, is useful in controlling broadleaf weeds and sedges in turfgrass and in vine and orchard floors.

The present invention relates to a pyridazinone compound of the formula (I): wherein R1 represents hydrogen, a C1-6 alkyl group, and the like, R2 represents halogen, a cyano group, a nitro group, a C1-6 alkoxy group, and the like, G represents hydrogen, and the like, Z represents halogen, a cyano group, a nitro group, a C1-6 alkyl group, and the like, and n represents an integer of 1-5 useful as an active ingredient in a herbicide and a noxious arthropod controlling agent.

Bioactive agrichemical concentrates and compositions having improved bioactivity comprising combinations of acid solutions and conventional bioactive agrichemical actives or formulations.

Herbicidal injury caused by 6-trisubstituted phenyl)-4-amino-2-pyridinecarboxylates in wheat and barley is reduced with the use of low rates of cloquintocet.

Provided herein are herbicidal compositions containing (a) aminopyralid or an agriculturally acceptable salt or ester thereof and (b) propanil. The compositions provide synergistic weed control of undesirable vegetation, e.g., in rice, wheat, barley, oats, rye, sorghum, corn or maize, oilseed rape/canola, vegetables, pastures, grasslands, rangelands, fallowland, turf, tree and vine orchards, industrial vegetation management or rights-of-way.

This invention describes the use of S-abscisic acid (S-ABA) and ethylene producing-agents such as ethephon to synergistically improve red color in grapes and to alter the sensory characteristics of wine.

The methods described herein enable the evaluation of compounds on subjects to assess their therapeutic efficacy or toxic effects. The target of analysis is the underlying biochemical process or processes (i.e., metabolic process) thought to be involved in disease pathogenesis. Molecular flux rates within the one or more biochemical processes serve as biomarkers and are quantitated and compared with the molecular flux rates (i.e., biomarker) from control subjects (i.e., subjects not exposed to the compounds). Any change in the biomarker in the subject relative to the biomarker in the control subject provides information to evaluate therapeutic efficacy of an administered drug or a toxic effect and to develop the compound further if desired. In one aspect of the invention, stable isotope-labeled substrate molecules are administered to a subject and the label is incorporated into targeted molecules in a manner that reveals molecular flux rates through metabolic pathways of interest.

The present invention relates to a polymerization-curable composition for the preparation of biodegradable, biocompatible, cross-linked polymers on the basis of polyvinyl alcohol comprising: 5 to 100% by weight of (a) vinyl ester monomer(s) of one of the general formulas (I) to (III): wherein X is oxygen, sulfur, nitrogen, or phosphorus; n is 1 to 1000, at least 20% of the n being ≧2; the R1 are selected from hydrogen; straight, branched or cyclic, saturated or unsaturated, n-valent hydrocarbon groups having 1 to 30 carbon atoms, which optionally have heteroatoms and are optionally substituted with one or more substituents selected from —OH, —COON, —CN, —CHO, and ═O, and n-valent radicals of biodegradable, biocompatible oligomers and polymers; m is an integer from 1 to 5; the R2 are selected from hydrogen, —OH, ═O, and the options listed for R1; and the R3 are selected from hydrogen, —OH, and the options listed for R1; 0 to 50% by weight of ethylenically unsaturated co-monomers; 0 to 10% by weight of (a) polymerization initiator(s); and 0 to 95% by weight of solvent(s).