Abstract: The invention discloses novel 42-0-(heteroalkoxyalkyl) rapamycin compounds of formula (1) and process for preparation thereof. These compounds are useful in the treatment of hyperproliferative vascular diseases such as restenosis and atherosclerosis Wherein, R denotes 3, 4 and 5 membered 3-hydroxy heteroalkoxyalkyl compounds selected from Tetrahydrofuran-3-ol, Oxetan-3-ol, Tetrahydropyran-3-ol, Tetrahydro-4- methyl furan-3-ol, Tetrahydro-2,5,5-trimethyl furan-3-ol, Tetrahydro-2,5-diethyl-2-methyl furan-3-ol, Tetrahydro-6-methoxy-2-methyl 2H-Pyran-3-ol and Tetrahydro-2,2-dimethyl-6-phenyl 2H-Pyran-3-ol.

Abstract: A method for preparing a dialkyloxydianhyrohexitol (dimethylisosorbide) composition by etherification of dianhydrohexitol (isosorbide). The aim is to achieve a “clean” method that avoids the use of a methylation agent such as dimethyl sulfate or methyl chloride, which generates stoechiometric quantities of salts, or expensive dialkyl-carbonates, wherein only one of the two methyl groups participates in the preparation of mixed isosorbide ethers. The method involves using at least one O-alkylation agent and a catalyst including an acid or an acid salt, preferably a catalyst having Lewis or BrØnsted acid properties. A device for carrying out the method wherein the device includes a vaporization oven and a reaction oven is also described.

Abstract: A process is described for making isohexides, comprising dehydrating one or more hexitols with an acid catalyst to form a crude dehydration product mixture including one or more isohexides, further processing the mixture to separate out one or more fractions of a greater purity or higher concentration of at least one of the isohexides, and hydrogenating at least one of a) the crude dehydration product mixture, b) a neutralized crude dehydration product mixture, following a neutralization of the crude dehydration product mixture, c) the product mixture following a neutralization step and further following a step to remove ionic species therefrom, d) a greater purity or higher concentration fraction, and e) a lesser purity or concentration fraction, by reaction with a hydrogen source in the presence of a hydrogenation catalyst. Hydrogenation improves the color and/or color stability of the material, especially of a finished isohexide product.

Abstract: The present invention relates to a method of ameliorating the drawbacks of anti-platelet drug named clopidogrel. The method of the present invention comprises administration of an (S)oxo-clopidogrel or its derivative of the Formula IIA in its free or pharmaceutically acceptable salt form for alleviating the symptoms of thrombosis or embolism by inhibiting blood platelet aggregation. Compositions for use in such methods are also provided.

Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

Abstract: The invention therefore relates to compounds of the formula I in which A, X, Y, R1, R2 and R3 have the given meanings. The compounds of the formula I are suitable, for example, for wound healing.

Abstract: The present invention relates to antibacterial compounds of formula I: wherein all variable substituents are defined as described herein, which are useful for the treatment of bacterial infections.

Abstract: A process for preparing a compound represented by formula (Y1) or (Y2) wherein Rx is an optionally substituted carbocyclyl lower alkyl, or the like or a salt thereof, using a novel process for preparing a pyridone derivative represented by formula (X4) wherein R1d, R2d, and R4d are as defined herein.

Abstract: The invention relates to novel pyrimidinone-based heterocyclic compounds which are parasite growth inhibitors, having the general formula (I) in which Y is a morpholine chosen from three bridged morpholines, L is a bond or a linker, n=0 or 1 and R2 is a methyl group when n=0 and a hydrogen atom when n=1. Process for the preparation thereof and therapeutic use thereof.

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: This invention relates to hydrolysable silanes useful in the modification of elastomers, and as coupling agents for diene elastomer compositions containing a filler. In particular the invention relates to novel hydrolysable silanes containing an aziridine ring herein named (Az).

Abstract: The present invention relates to a method for separating organohalosilanes. The method includes introducing a mixture including at least a first organohalosilane and a second organohalosilane onto a chromatographic bed including a stationary phase. The method also includes passing a liquid mobile phase through the chromatographic bed to produce an eluate including at least one fraction enriched in the first organohalosilane and at least one fraction enriched in the second organohalosilane.

Abstract: The invention includes processes for the synthesis of amphetamine, dexamphetamine, methamphetamine, derivatives of these, including their salts, and novel precursors and intermediates obtained thereby, by synthesizing aziridine phosphoramidate compounds in specified solvents at specified temperatures, and then converting to a novel aryl or aryl-alkyl phosphoramidate precursors using an organometallic compound such as a copper salt, where the novel aryl or aryl-alkyl phosphoramidate precursor is then easily converted to the target compounds using known reactions.

Abstract: The present invention relates to a new use of a cinnamaldehyde derivative of formula (I) for treating glomerulonephritis (GN). Particularly, the present invention discloses that the cinnamaldehyde derivative of formula (I) is effective in treating glomerulonephritis (GN), which can alleviate various symptoms and signs of GN, including reducing proteinuria, serum blood urea nitrogen (BUN), glomerular cell proliferation, and renal macrophage/lymphocyte infiltration, etc.

Abstract: This invention relates to carbamate-containing or thiocarbamate-containing galacto-pyranosyl compounds useful as therapeutic agents and being represented by the structural formula (II), wherein: X is O or S, R is selected from the group consisting of C1-8 alkyl, C3-10 cycloalkyl, aryl-C1-4 alkyl, heterocyclyl-C1-4 alkyl, cycloalkyl-C1-4 alkyl, aryl and heterocyclyl, wherein R is optionally substituted with one or more R9; R2, R3, R4, R6 and R7 are independently selected from the group consisting of hydroxyl and protected hydroxyl groups; R5 is selected from the group consisting C6-30 alkyl and arylalkyl; R8 is C6-30 alkyl; and each R9 is independently selected from the group consisting of halogen, hydroxy, trifluoromethyl, trifluoromethoxy, C1-8alkoxy, C1-6 alkyl, cyano, methylthio, phenyl, phenoxy, chloromethyl, dichloromethyl, chloro-difluoromethyl, acetyl, nitro, benzyl, heterocyclyl and di-C1-4 alkyl-amino, or a pharmaceutically acceptable salt thereof.

Abstract: The invention relates to compositions of nicotinoyl ribosides and nicotinamide riboside derivatives and their methods of use. In some embodiments, the invention relates to methods of making nicotinoyl ribosides. In some embodiments, the invention relates to pharmaceutical compositions and nutritional supplements containing a nicotinoyl riboside. In further embodiments, the invention relates to methods of using nicotinoyl ribosides and nicotinamide riboside derivatives that promote the increase of intracellular levels of nicotinamide adenine dinucleotide (NAD+) in cells and tissues for improving cell and tissue survival.

Abstract: Phosphorodiamidate derivatives of e.g. gemcitabine are provided for use in treating cancer. In one embodiment, the two amidate motifs each comprises NR?R? where R? is H and R? is CR5R6CO2R7, where R6 is H, R5 is the side chain, including H and C1, of a naturally occurring alpha amino acid, and R7 is branched or unbranched, substituted or unsubstituted, acyclic or cyclic alkyl, including t-butyl-CH2-, benzyl and C3 to C6 cycloalkyl. Formula (I).

Abstract: The present invention provides modified nucleosides, analogs thereof and oligomeric compounds prepared therefrom. More particularly, the present invention provides modified nucleosides and analogs thereof that are useful for incorporation at the terminus of an oligomeric compound. Such oligomeric compounds can also be included in a double stranded composition. In some embodiments, the oligomeric compounds provided herein are expected to hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.

Abstract: The invention provides compounds of formula I, wherein R1, R2 and R3 have values defined in the specification and a pharmaceutically acceptable salt thereof; or an optical isomer thereof; or a mixture of optical isomers, as well as compositions comprising such compounds and therapeutic methods that utilize such compounds and/or compositions.

Abstract: The present invention relates to a method for reducing the amount of steryl glycoside in an oil or fat (e.g. a biofuel substrate) and/or a biofuel, the method comprising admixing one or more enzymes with an oil or fat comprising steryl glycoside; such that said one or more enzymes degrades the steryl glycoside. The one or more enzymes is preferably an enzyme which is capable of hydrolysing the glycosidic bond in a steryl glycoside. Suitably the enzyme may be a glycosidase enzyme and/or a ?-glucosidase and/or an amyloglucosidase.

Abstract: The sulfated oxysterol 5-cholesten-3?, 25-diol 3-sulphate, a nuclear cholesterol metabolite that decreases lipid biosynthesis and increases cholesterol secretion and degradation, is provided as an agent to lower intracellular and serum cholesterol and/or triglycerides, and to prevent or treat lipid accumulation-associated inflammation and conditions associated with such inflammation. Methods which involve the use of this sulfated oxysterol to treat conditions associated with high cholesterol and/or high triglycerides and/or inflammation (e.g. hypercholesterolemia, hypertriglyceridemia, non-alcoholic fatty liver diseases, atherosclerosis, etc.) are also provided.

Abstract: A composition for use in inhibiting the binding of a Norovirus to the histo-blood group antigen on the surface of epithelia is disclosed. The composition may contain a therapeutically effective amount of a binding-inhibiting compound and a carrier and/or excipient. The compounds may competitively bind a Norovirus that has the capability of binding with the histo-blood group antigens of secretor blood type, including A, B, AB, and O blood types. The compositions may be administered to a human prior to or after infection by a Norovirus, to prevent, ameliorate, or reduce the effects of an infection.

Abstract: Disclosed are the general structural formula of LQC-Y as well as the synthesis and use thereof. Pharmacological experiments demonstrated the marked antitumor effect of such compounds. Single day administration of LQC-Y3 to mice at a maximum dose of 6000 mg/kg showed no toxicity response during the 14-day continuous observation period, indicating the high safety of the compounds, and the compounds can be used to prepare medicaments for preventing and treating carcinomas such as liver cancer, lung cancer.

Abstract: Large-scale downstream processing of secreted recombinant proteins is provided in a single device, wherein the contents of a plurality of bioreactors are combined simultaneous to their harvesting and purification resulting in significant savings of time and the cost of manufacturing.

Abstract: A novel method for processing soluble plant leaf proteins is described. While leaf proteins are considered potentially the most abundant source of protein in nature, the lack of efficient processing techniques for leaf proteins has limited their commercial use. The method described in this patent provides a means of extracting and purifying leaf proteins from plants which is suitable for leaf protein production on an industrial scale.

Abstract: The present invention features crystalline forms of Compound I. In one embodiment, a crystalline form of Compound I has characteristic peaks in the PXRD pattern as shown in any one of FIGS. 1-4.

Abstract: The present invention relates to conformationally constrained homo- and heterodimeric mimetics of Smac with function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs), the invention also relates to the use of these compounds in therapy, wherein the induction of apoptotic cell death is beneficial, especially in the treatment of cancer, alone or in combination with other active ingredients.

Abstract: A compound as represented by Formula (I) is provided, wherein groups are defined in the description. The compound is used as HCV protease inhibitor for treating HCV infection.

Abstract: The invention relates to methods of use of synthetic peptide amides that are ligands of the kappa opioid receptor in the treatment and prevention of kappa opioid receptor-associated diseases and conditions; and particularly to uses of these agonists in the prophylaxis, inhibition and treatment of pain, inflammation and pruritis associated with a variety of diseases, disorders and conditions. Inflammatory conditions preventable or treatable by the methods of the invention include diseases and conditions associated with elevated levels of a proinflammatory cytokines, such as TNF-?, IL-1?, IL-6, MMP-1 and MMP-3.

Abstract: A novel structural class of highly N-methylated linear lipopeptide compounds useful for the treatment of parasitic disease.

Abstract: Embodiments of the present invention provide for novel therapies, pharmaceutical compositions and methods for insulin independence utilizing a new optimized hamster Reg3 gamma peptide, which is new to the art and has not previously been considered for development in the 30 year history since its discovery. Methods, pharmaceutical compositions and therapies novel to the prior art are utilized in this invention to render patients with recent onset and existing type 1 diabetes insulin independent by an optimized hamster Reg3 gamma peptide and an immune tolerance agent for type 1 patients to become insulin independent and used alone without an immune tolerance agent for type 2 diabetes. While not wishing to be bound by theory, optimized Reg3 gamma peptides increases beta cell generation by its demonstrated properties shown within of transforming ductal pancreatic cells into new islets.

Abstract: The present invention provides methods and compositions for treating and/or preventing a cytomegalovirus infection in a subject, comprising administering to the subject an effective amount of a cytomegalovirus interleukin-10 (IL-10) protein modified to have reduced functional activity while retaining immunogenicity. The present invention further provides nucleic acid molecules encoding a cytomegalovirus IL-10 protein or fragment thereof of this invention as well as vectors comprising such nucleic acids. Also provided herein are neutralizing antibodies that specifically bind cmvIL-10.

Abstract: Compositions and methods for conferring pesticidal activity to bacteria, plants, plant cells, tissues and seeds are provided. Compositions comprising a coding sequence for a toxin polypeptide are provided. The coding sequences can be used in DNA constructs or expression cassettes for transformation and expression in plants and bacteria. Compositions also comprise transformed bacteria, plants, plant cells, tissues, and seeds. In particular, isolated toxin nucleic acid molecules are provided. Additionally, amino acid sequences corresponding to the polynucleotides are encompassed, and antibodies specifically binding to those amino acid sequences. In particular, the present invention provides for isolated nucleic acid molecules comprising nucleotide sequences encoding the amino acid sequence shown in SEQ ID NO:2-5, or the nucleotide sequence set forth in SEQ ID NO: 1, as well as variants and fragments thereof.

Abstract: A method of producing bioproducts from a feedstock in a system configured to produce ethanol and distillers grains from a fermentation product is disclosed. A system configured to process feedstock into a fermentation product and bioproducts including ethanol and meal is disclosed. A bioproduct produced from a fermentation product produced from a feedstock in a biorefining system is disclosed.

Abstract: An expression system, including a host cell, a synthetic spider silk polypeptide-encoding nucleotide sequence, at least one synthetic tRNA molecule-encoding nucleotide sequence or a synthetic serine hydroxymethyl transferase (SHMT)-encoding nucleotide sequence.

Abstract: The present inventions are compositions and methods of using at least a portion of an isolated and purified ?-crystallin polypeptide that includes one or more ?-pleated sheets and that prevents neurotoxicity and amyloidogenesis.

Abstract: Methods for diagnosis of non-small cell lung cancers by detection of endogenous peptides in exhaled breath condensate (EBC) are provided. Diagnostic peptides derived from dermcidin (DC) are provided. A specific dermcidin-derived peptide E-R11, having the sequence ENAGEDPGLAR (SEQ ID NO:2), is provided. E-R11 peptide levels in EBC, as measured by mass spectrometry (MS), are highly diagnostic of non-small cell lung cancers. A method for inhibiting growth of lung cancer cells by inhibiting DCD expression by RNA interference also is provided.

Abstract: Secreted eIF5A protein which is useful for diagnosis, prevention, and treatment of various diseases induced by an oxidative stress.

Abstract: The present invention provides methods and compositions for treating bladder cancer. In particular, the present invention provides a fusion protein comprising a toxin moiety that is linked to an epithelial growth factor (EGF) moiety. The toxin moiety and the EGF moiety can be linked optionally via a linker. Typically, the fusion protein is administered intravesically into the cancerous bladder.

Abstract: The present invention relates to a fusion protein comprising a skin-penetrating peptide, a polynucleotide encoding the fusion protein, an expression vector comprising the polynucleotide, a transformant comprising the expression vector, a method for preparing the fusion protein, a cosmetic composition for improving skin conditions, which comprises the fusion protein, and a pharmaceutical composition for external skin use, which comprises the fusion protein. The fusion protein of the invention comprises a skin-penetrating peptide bound to a physiologically active protein. The fusion protein significantly enhances the skin penetration and skin retention of the physiologically active protein while maintaining or enhancing the ability of the physiologically active protein to synthesize a material showing physiologically active effects. Thus, it can be widely used as an active ingredient in functional cosmetic compositions and pharmaceutical compositions for external skin use.

Abstract: Provided are methods of treating a mammal undergoing sepsis or at risk for sepsis. Also provided are methods of preventing or treating a physiologic effect of sepsis in a mammal. Additionally provided is the use of milk fat globule epidermal growth factor-factor VIII (MFG-E8) for the manufacture of a medicament for preventing or treating a physiologic effect of sepsis in a mammal, and the use of milk fat globule epidermal growth factor-factor VIII (MFG-E8) for the treatment of a mammal having sepsis or at risk for sepsis.

Abstract: The emergence of mutations in tyrosine kinases following treatment of cancer patients with molecular-targeted therapy represents a major mechanism of acquired drug resistance. Here, we describe a mutation in the serpentine receptor, Smoothened (SMO), which results in resistance to a Hedgehog (Hh) pathway inhibitor in medulloblastoma. A single amino acid substitution in a conserved aspartic acid residue of SMO maintains Hh signaling, but results in the inability of the Hh pathway inhibitor, GDC-0449, to bind SMO and suppress the pathway. This mutation was not only acquired in a GDC-0449-resistant mouse model of medulloblastoma, but was identified in a Medulloblastoma patient following relapse on GDC-0449. The invention provides screening methods to detect SMO mutations and methods to screen for drugs that specifically modulate mutant SMO exhibiting drug resistance.

Abstract: The present invention is further directed to methods and compositions for modulating the activity of the Toso protein. The invention further encompasses treatment of disorders associated with inflammation, autoimmune disorders, and cancer using compositions that include a soluble Toso protein.

Abstract: Disclosed herein are an N-terminal modified PEG-TRAIL conjugate and a preparation method and use thereof. The PEG-TAIL conjugate has pharmaceutical activity identical or similar to that of native TRAIL (TNF-related apoptosis-inducing ligand) with extended in vivo half-life and enhanced stability. Compared to native TRAIL, the PEG-TAIL conjugate exhibits high solubility and solution stability, with highly improved pharmacokinetic profiles. Thus, the PEG-TAIL conjugate may be very useful for preventing and treating proliferative diseases and autoimmune diseases.

Abstract: Factor V peptides and methods of use thereof are disclosed.

Abstract: The present invention relates to modified coagulation factors. In particular, the present invention relates to modied Factor VIII molecules having decreased cellular uptake.

Abstract: Disclosed are compositions and methods of making non-glycosylated transferrin protein in transgenic monocot plants.

Abstract: Antibodies that specifically bind influenza virus hemagglutinin A (HA), and antigen binding fragments thereof are disclosed herein. In several embodiments, these antibodies are broadly neutralizing. Nucleic acids encoding these monoclonal antibodies, vectors including these nucleic acids, and host cells transformed with these vectors are also disclosed. Compositions are disclosed that include these antibodies, antigen binding fragments, nucleic acids, vectors and host cells. Method of using these antibodies, and antigen binding fragments, nucleic acids, vectors and host cells, such as for diagnosis and treatment of an influenza virus infection are also provided.

Abstract: Individual monoclonal antibodies and fragments that bind a conserved epitope of the G protein of RSV and which are minimally immunogenic when administered to a human subject, are useful in treating RSV infections.

Abstract: The invention provides antibodies and functional equivalents thereof which are capable of specifically binding RSV, and means and methods for producing them.