Abstract: The invention provides tricyclic sulfonamide compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.

Abstract: The invention relates to 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride, its new crystalline forms, its therapeutic usage for treatment of diseases mediated by EGFR kinase and its combinatory therapeutic usage together with other therapeutic agents. The invention also provides synthetic methods for preparation of 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride, its new crystalline forms, and the relevant synthetic intermediates for synthesis of 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride.

Abstract: Disclosed are bicyclic group substituted pyrimidine compounds, pharmaceutical acceptable salts thereof or stereoisomers thereof. Also disclosed are preparation methods, pharmaceutical formulations, and pharmaceutical compositions of the compounds, and use of the compounds, pharmaceutical formulations, and pharmaceutical compositions for preparing a medicament for treating and/or preventing sexual dysfunction diseases and diseases with lower urinary tract symptoms.

Abstract: The present invention relates to a novel hexahydrodibenzo[a,g]quinoline compound represented by general formula (I) and its derivatives, enantiomer, diastereoisomer, raceme and mixtures thereof, as well as pharmaceutically acceptable salts thereof. The present invention further relates to a method for preparing the compound, and the compound has good prevention and treatment effect on neurological diseases, especially diseases associated with dopamine receptor and 5-hydroxytryptamine receptor. The bioactivity experiment demonstrates that, the compound is expected to be developed into a novel and potent chemical entity for treating diseases associated with dopamine receptor and 5-hydroxytryptamine receptor, especially schizophrenia, Parkinson's disease, drug addiction, migraine and so on.

Abstract: Novel N-substituted norcantharimide derivatives are disclosed herein. The novel N-substituted norcantharimide derivatives are useful as lead compounds for manufacturing a medicament or a pharmaceutical composition for treating cancer, particularly for treating leukemia.

Abstract: Provided for in the instant application are two additional forms of rifaximin, namely rifaximin polymorphic forms APO-III and APO-IV. Also provided are allegedly novel processes for preparing the previously disclosed rifaximin polymorphic forms APO-I and APO-II. Rifaximin is a non-aminoglycoside antibiotic that has previously been found to be useful for the treatment of traveller's diarrhea caused by Escherichia coli bacteria, as well as in the treatment of irritable bowel syndrome, diverticular disease, hepatic encephalopathy, pyogenic skin infections and as an antibacterial prophylactic prior to colon surgery.

Abstract: The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.

Abstract: The present invention relates to the synthesis and application of novel chiral/achiral substituted methyl formyl reagents to modify pharmaceutical agents and/or biologically active substances to modify the physicochemical, biological and/or pharmacokinetic properties of the resulting compounds from the unmodified original agent.

Abstract: The present invention relates to compounds of formula (I) or salts, racemates, isomers and/or prodrugs thereof useful in the treatment of viral infections, in particular respiratory syncytial viral (RSV) infections. The present invention also relates to processes for preparing the compounds and intermediates used in their preparation.

Abstract: The present invention relates to novel derivatives of 6,7-dihydro-3H-oxazolo[3,4-a]pyrazine-5,8-dione represented by formula (I): and a mixture of these derivatives. The present invention also encompasses the pharmaceutical compositions comprising an effective amount of a said compounds, object of the present invention, as well as to the use of the compounds and/or derivatives as a phosphodiesterase enzyme inhibitor, and the use of the compounds and/or derivatives in the treatment of erectile dysfunction, disorders and/or conditions treatable with relaxation of tissues and disorders treatable with phosphodiesterase inhibitors, more particularly PDE-5 inhibitor. A further objective of the present invention is to provide a medication comprising a therapeutically effective amount of said compound and a method of treating using the said novel compounds.

Abstract: Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.

Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: The ?-ketoimine ligand is represented by the following formula 1: wherein R1 and R2 are each independently a C1-C5 alkyl group. A metal complex compound includes the ?-ketoimine ligand. A method of forming the ?-ketoimine ligand and a method of forming a thin film using the metal complex compound including ?-ketoimine ligand are provided.

Abstract: The ?-ketoimine ligand is represented by the following formula 1: wherein R1 and R2 are each independently a C1-C5 alkyl group. A metal complex compound includes the ?-ketoimine ligand. A method of forming the ?-ketoimine ligand and a method of forming a thin film using the metal complex compound including ?-ketoimine ligand are provided.

Abstract: An organohalosilane represented by formula I, where R1, R2, and R3 independently, at each occurrence, represent —(CH2)xCH3 where x is an integer from 0 to 5, or a halogen substituent where the halogen is F or Cl, and at least one substituent from R1, R2, and R3 is the halogen substituent; R4 is a C1-C5 alkoxyl or a tertiary amine represented by —NR5R6, where R5 and R6 independently, at each occurrence, represent a same or different C1-C5 alkyl; m is an integer from 1 to 20; and n is an integer from 0 to 5. The organohalosilane is used for preparation of an electrolyte solution of a non-aqueous lithium ion battery.

Abstract: The invention relates to the preparation of chiral compounds, in particular to the preparation of chiral compounds which may be used as intermediates for the preparation of anti-diabetic agents, preferably sitagliptin.

Abstract: The invention relates to silicon compounds having formula (I): (RfCH2CH2)2-n[R(OCH2CHR?)mOR?]nSiX2??(I). In formula (I), Rf is a linear or branched perfluorinated hydrocarbon having 4 or more carbon atoms, R is a methyl or ethyl group, R? is H or CH3, m is an integer of 1 to about 24, R? is a hydrocarbon bridge having 1 to about 11 carbon atoms, n is an integer from 0 to 2, and X is H, Cl or an alkoxy group. The inventive materials may be used to produce siloxanes or silicones by hydrolytic condensation and have utility in surface modification.

Abstract: The invention provides a conjugated diene structure-containing organosilicon compound having formula (1): R1nX3-nSi-A-CR2?CR2—CR2?CH2??(1) wherein R1 is a monovalent hydrocarbon group, X is halogen or organoxy, n is 0, 1 or 2, R2 is hydrogen or a monovalent hydrocarbon group, and A is a divalent hydrocarbon group. The organosilicon compound is prepared by reacting a conjugated diene structure-bearing olefin compound with a hydrogensilyl-containing compound in the presence of a platinum catalyst and an acid amide compound, organic amine salt compound, nitrile compound, aromatic hydroxy compound, or carboxylic acid compound.

Abstract: The present invention discloses a transition metal compound having a novel structure and including a heteroatom, a catalyst composition including the same, and a method for preparing polymers using the same. The transition metal compound according to an embodiment of the present invention has good copolymerization properties, and a polymer having a low density may be prepared using thereof. Thus, a copolymer having various uses may be prepared.

Abstract: The invention relates to novel caged ceramide 1-phosphate (C1P), caged ceramide 1-phosphate derivatives(C1P), and the method of using them for delivering C1P intracellularly in vitro and in vivo, for research and therapeutic purposes. Therapeutic purposes include treatment of diseases associated with cell death, such as neurodegerative diseases, including Alzheimer's disease. The disclosed compositions may also be used for wound healing.

Abstract: An activated carbon having a high catalytic activity as an oxidation catalyst or a decomposition catalyst, and use therefor are provided. The activated carbon has (a) an oxygen content in a range from 1.40 to 4.30% by mass, (b) a nitrogen content in a range from 0.90 to 2.30% by mass, (c) a sulfur content in a range from 0.50 to 1.20% by mass, and (d) a hydrogen content in a range from 0.40 to 0.65% by mass. The activated carbon may have at least one characteristic of (e) an amount of an acidic surface functional group of 0.10 to 0.36 meq/g, (f) an amount of a basic surface functional group of 0.50 to 1.30 meq/g, and (g) a benzene adsorption capacity of 25 to 50%. The activated carbon catalyzes an oxidation reaction of N-(phosphonomethyl)iminodiacetic acid with a peroxide (e.g., hydrogen peroxide) and achieves an efficient production of N-(phosphonomethyl)glycine even after repetitive use. The activated carbon also efficiently decomposes a chloramine.

Abstract: A method to cleave C—C and C—O bonds in ?-O-4 linkages in lignin or lignin sub-units is described. The method includes oxidizing at least a portion of secondary benzylic alcohol groups in ?-O-4 linkages in the lignin or lignin sub-unit to corresponding ketones and then leaving C—O or C—C bonds in the oxidized lignin or lignin sub-unit by reacting it with an organic carboxylic acid, a salt of an organic carboxylic acids, and/or an ester of an organic carboxylic acids. The method may utilize a metal or metal-containing reagent or proceed without the metal or metal-containing reagent.

Abstract: This invention relates to certain dendrimer compounds. In particular, this invention relates to novel dendrimer compounds that can be elaborated to give increasingly large and complex compounds. These elaborated compounds can be attached to, or can encapsulate within, active agent(s) so as to beneficially modify the characteristics of that active agent. Alternatively, the elaborated compounds can themselves be beneficially modified into therapeutic agents by the attachment of inactive agents.

Abstract: The present invention provides a manufacturing method that can easily manufacture a compound known as photoresponsive (photocoupling) nucleic acids at high yield in a shorter period of time than that of the conventional technology. The present invention relates to a method of manufacturing a photoresponsive nucleic acid which includes a step of reacting a nucleic acid having groups represented by the Formula I, the Formula III, the Formula IV, or the Formula V and a compound represented by the Formula II, or reacting a nucleic acid having groups represented by the Formula VI, the Formula VIII, the Formula IX, or the Formula X and a compound represented by the Formula VII by heating them by microwaves in the presence of a metal catalyst, a basic substance, and a solvent.

Abstract: Disclosed is a method for selective synthesis of 1,2-cis-?-linked glycosides which does not require the use of the specialized protecting group patterns normally employed to control diastereoselectivity. Thioglycoside acceptors can be used, permitting iterative oligosaccharide synthesis. The approach eliminates the need for lengthy syntheses of monosaccharides possessing highly specialized and unconventional protecting group patterns.

Abstract: Prodrugs of C-17-heterocyclic-steroidal drugs providing improved oral bioavailability and phamacokinetics are described. The drugs are inhibitors of human CYP 17 enzyme, as well as potent antagonists of both wild type and mutant androgen receptors (AR), and are useful for the treatment of urogenital and/or androgen-related cancers, diseases and/or conditions, such as human prostate cancer, breast cancer, and prostate hyperplasia. The disclosure describes methods of synthesizing and using the prodrugs in cancer therapy.

Abstract: The invention concerns a material composed of a porous support on which functionalized nanoparticles are grafted by covalent bonding, characterized in that at least part of the nanoparticles grafted by covalent bonding is housed inside surface pores of the support, and in that the support is silica-based and is in the form of porous particles of heterogeneous shape and size, the size of the particles being larger than 1 ?m and preferably within the range of 5 to 200 ?m. The invention further concerns a growth method for oligonucleotides or peptides characterized in that growth is performed on a material formed of a porous support on which functionalized nanoparticles are grafted by covalent bonding, characterized in that at least a part of the nanoparticles grafted by covalent bonding is housed inside surface pores of the support.

Abstract: The present invention provides a method for manufacturing a virus-free protein drug, comprising (a) a filtration step of filtering a virus-containing protein solution through a small-pore size virus removal membrane to obtain a virus-free protein solution, the filtration step (a) comprising (q) a low-pressure filtration step of filtering the solution through the small-pore size virus removal membrane at a filtration pressure of 0.30 kgf/cm2 or lower to obtain the virus-free protein solution, wherein the solution prior to filtration in the low-pressure filtration step (q) has a pH (X) and a salt ionic strength (Y (mM)) that satisfy the following equations 1 and 5: 0?Y?150X?590 (Equation 1) and 3.5?X?8.0 (Equation 5) or the following equations 4 and 5: Y=0 (Equation 4) and 3.5?X?8.0 (Equation 5).

Abstract: One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.

Abstract: The invention relates to synthetic peptide amide ligands of the kappa opioid receptor and particularly to agonists of the kappa opioid receptor that exhibit low P450 CYP inhibition and low penetration into the brain. The synthetic peptide amides of the invention conform to the structure of formula I: Pharmaceutical compositions containing these compounds are useful in the prophylaxis and treatment of pain and inflammation associated with a variety of diseases and conditions. Such treatable pain includes visceral pain, neuropathic pain and hyperalgesia. Inflammation associated with conditions such as IBD and IBS, ocular and otic inflammation, other disorders and conditions such as pruritis, edema, hyponatremia, hypokalemia, ileus, tussis and glaucoma are treatable or preventable with the pharmaceutical compositions of the invention.

Abstract: The present invention relates to methods and reagents for use in site-selective modification of proteins having lysine residues with functionalized peptides using a chemoenzymatic microbial transglutaminase-mediated reaction. The functionalized proteins may be used for study or therapeutic uses.

Abstract: The present invention relates to a peptide analog or a pharmaceutically acceptable salt thereof with excellent moisturizing effect, and use thereof for moisturization. More specifically, the present invention relates to a novel peptide analog or a pharmaceutically acceptable salt thereof, a method for preparation thereof, a moisturizing cosmetic composition comprising the same as an active ingredient, and a pharmaceutical composition for prevention and treatment of xeroderma.

Abstract: EphA2 T-cell epitope are provided herein. The epitopes include peptides corresponding to specific fragments of human EphA2 protein containing one or more T-cell epitopes, and conservative derivatives thereof. The EphA2 T-cell epitopes are useful in an assay, such as an ELISPOT assay, that may be used to determine and/or quantify a patient's immune responsiveness to EphA2. The epitopes also are useful in methods of modulating a patient's immune reactivity to EphA2, which has substantial utility as a treatment for cancers that overexpress EphA2, such as renal cell carcinoma (RCC). The EphA2 epitopes also can be used to vaccinate a patient against EphA2, by in vivo or ex vivo methods.

Abstract: Provided are activated collagen scaffold materials as well as their special fused active restoration factors useful for promoting tissue repair, such as bone damage repair or nerve injury repair. The special fused active restoration factors are fusion proteins comprising a collagen-binding domain (CBD) at N-/C-terminus of cytokines, wherein the collagen-binding domain is a polypeptide consisting of 7-27 amino acid residues with a conservative sequence shown in SEQ ID NO:12 at N-terminus.

Abstract: The invention relates to methods for altering biological parameters in a subject, such as reducing blood pressure in a subject, by displacing CLIP, using a CLIP inhibitor. The methods are useful for treating disorders such as preeclampsia and high blood pressure.

Abstract: The present invention discloses novel peptides derived from the IL-1 receptor antagonist protein (IL1 RA), capable of binding to the cell surface IL-1 receptor 1 (IL1 R1) and interfere with the binding of IL-1 to IL1 R1. This binding thus effectively antagonizes the inflammatory effects of IL-1, such as by reducing TNF-alpha secretion from macrophages. This is of potential use as an anti-inflammatory factor throughout the human body, including the central nervous system. The use of said peptides as anti-inflammatory agents for treatment of pathological conditions wherein IL-1 plays a prominent role, such as inflammatory conditions of the body and the central nervous system, is thus an aspect of the present invention.

Abstract: A therapeutic composition comprising (1) a complementary peptide comprising a sequence complementary to a major immunogenic region of an acetylcholine receptor (AChR) involved in myasthenia gravis (MG), the sequence being SEQ ID NO:1 (with modified tryptophan in position 8 carrying at least one 2,4,6-trimethoxybenzyl group as hydrocarbonation), (2) a complementary peptide having at least a sequence SEQ ID NO:2, which is complementary to a T-cell recognition site of the acetylcholine receptor, and (3) at least one carrier, may be used in the therapeutic or prophylactic treatment of myasthenia gravis in mammals.

Abstract: The novel omp-1 gene cluster encoding twenty one Ehrlichia ewingii (EE) proteins was isolated and sequenced completely. This invention relates to isolated E. ewingii (EE) polypeptides, isolated polynucleotides encoding EE polypeptides, probes, primers, isolated antibodies and methods of their production, immunogenic compositions and vaccines, as well as methods of using the EE polypeptides, antibodies, probes, and primers for the purpose of diagnosis, therapy and production of vaccines against E. ewingii.

Abstract: A biologically derived polymer that facilitates the solubilization and protection of small molecules for use in drug delivery, in which the polymer is a protein polymer. A biologically derived polymer that facilitates the solubilization and protection of small molecules for use in drug delivery, incorporating fluorinated amino acids into the protein polymer for visualization and detection by 19F NMR, 19F MRS, and 19F MRI.

Abstract: Antimicrobial peptides set forth in SEQ ID Nos: 1-5 are described. The peptides have activity against Gram positive bacteria and against Gram negative bacteria. A bactericidal composition is also provided, which may comprise an amount between 0.5 ?g/mL and 1024 ?g/mL of the peptides and excipients.

Abstract: Methods for purifying human Calciviruses are disclosed, including Noroviruses and Sapoviruses.

Abstract: The present invention provides a recombinant yeast system for expressing the glycoprotein E2 of classical swine fever virus (CSFV), in which the expression level of yE2 is improved by codon optimization and shortening coding region of E2 gene. The truncated E2 subunits are used as major active ingredient in anti-CSFV vaccines and useful diagnostic blocking ELISA kits for CSFV infection with easy manipulation and low cost.

Abstract: The present invention relates to a novel trimeric OprF/I fusion protein comprising a portion of the Pseudomonas aeruginosa outer membrane protein F which is fused with its carboxy terminal end to a portion of the amino terminal end of the Pseudomonas aeruginosa out membrane protein I, wherein said portion of the Pseudomonas aeruginosa outer membrane protein F comprises the amino acids 190-342 of SEQ ID NO: 1 and wherein said portion of the Pseudomonas aeruginosa outer membrane protein I comprises the amino acids 21-83 of SEQ ID NO: 2, and further to a novel Opr F/I fusion protein which contains a disulphide bond pattern, preferably selected from the group consisting of (a) Cys18-Cys27-bond, (b) Cys18-Cys27-bond and Cys33-Cys47-bond, and (c) Cys18-Cys47 and Cys27-Cys33-bond, and to immunogenic variants thereof having at least 85% identity to the amino acid sequence of SEQ ID NO: 3.

Abstract: The invention relates to a microorganism which produces and/or secretes an organic-chemical compound, wherein the microorganism has increased expression, compared to the particular starting strain, of one or more protein subunits of the ABC transporter having the activity of a trehalose importer, said microorganism being capable of taking up trehalose from the medium; and to a method for the production of an organic-chemical compound, using the microorganism according to the invention, wherein accumulation of trehalose in the fermentation broth is reduced or avoided.

Abstract: The invention relates to novel polypeptides which are recognized by anti-Trichinella antibodies. Said polypeptides can be used particularly for detecting anti-Trichinella antibodies and in trichinosis prevention.

Abstract: The present invention provides fusion polypeptides comprising polypeptide ligands that are modified by circular permutation and fused to at least one polypeptide fusion partner wherein such fusion polypeptides have new, improved or enhanced biological functions or activities. Such improvements include, but are not limited to, increased binding affinity, increased activity, increased agonist activity (super agonist), antagonist activity, increased accessibility, increased flexibility of the active site, increased stability, broader and/or changed substrate specificity, and combinations thereof.

Abstract: Pentameric CRP is produced at a high efficiency by transferring DNA, which encodes monomeric CRP, into a silkworm to thereby construct a transgenic silkworm and then collecting and purifying pentameric CRP that is produced by the transgenic silkworm constructed above.

Abstract: A cell culture media for plasmid production is provided for increased production of a recombinant GDF-5 (rhGDF-5) protein. Also provided herein is a method of making a cell culture media for plasmid production and a method for growing a plasmid vector. The methods of enhancing production and protein expression of rhGDF-5 protein as disclosed are cost-effective, time-saving and are of manufacturing quality.

Abstract: In T lymphocytes, p38 mitogen activated protein kinase (MAPK) can be activated through an alternative pathway that involves phosphorylation at tyrosine 323. Disclosed herein is the identification of a minimal region of the growth arrest and DNA damage-inducible alpha (Gadd45?) protein that is required for binding to and inhibition of tyrosine 323-phosphorylated p38 in T cells. The disclosed Gadd45? polypeptides inhibit proliferation of T cells in response to T cell receptor stimulation, inhibit differentiation of T cells into Th1 or Th17 cells, inhibit the production of proinflammatory cytokines, and reduce tumor formation and growth of inflammatory cancers, such as pancreatic cancer.