Abstract: The present invention provides a dihydropyridazine-3,5-dione derivative or a salt thereof, or a solvate of the compound or the salt, a pharmaceutical drug, a pharmaceutical composition, a sodium-dependent phosphate transporter inhibitor, and a preventive and/or therapeutic agent for hyperphosphatemia, secondary hyperparathyroidism, chronic renal failure, chronic kidney disease, and arteriosclerosis associated with vascular calcification comprising the compound as an active ingredient, and a method for prevention and/or treatment.

Abstract: Disclosed are substituted pyrrolo[2,3-d]pyrimidine compounds. The disclosed compounds are shown to be useful in inhibiting the growth of cancer cell lines and treating cancer and cell proliferative disorders.

Abstract: Provided are crystalline forms of N-[4-[2-(2-amino-4,7-dihydro-4-oxo-1H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]ben-zoyl]-L-glutamic acid, pemetrexed diacid, and processes for the preparation thereof.

Abstract: Described herein are compounds of Formula (I) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Methods of using the compounds or pharmaceutical compositions thereof for treating diseases are also provided.

Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

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

Abstract: The present invention provides arylo-fused thienopyrimidine compounds, compositions thereof, and methods of using the same.

Abstract: An improved process for preparation of Olanzapine pamoate monohydrate from Olanzpaine is disclosed which comprises mixing at room temperature a solution of olanzapine prepared in water in presence of an acid, with a solution of pamoic acid prepared in water in presence of a base; stirring and maintaining the reaction mixture for a sufficient time till precipitation of solid and drying the solid to obtain olazapine pamoate monohydrate.

Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure, kidney disease, edema, and conditions associated with excessive salt and water retention.

Abstract: A fused heterocyclic compound represented by formula (1) or an N-oxide thereof has an excellent control effect on pests: wherein A1 represents N or the like, A2 represents NR6 or the like, A3 represents CR12 or the like, R1 represents a C1 to C6 chain hydrocarbon group or the like, R2, R4 and R5 are the same or different and represent a C1 to C3 alkyl group optionally having one or more halogen atoms or the like, R3 represents a C1 to C6 chain hydrocarbon group or the like, R6 represents a C1 to C6 chain hydrocarbon group or the like, any one set of R9 and R10, R10 and R11, and R11 and R12 in R9, R10, R11 and R12, together with the carbon atoms to which they are bound, forms a ring, and n represents 0, 1 or 2.

Abstract: Processes for the preparation of the compound of formula II and intermediate compounds for use in the processes.

Abstract: The present invention provides methods for obtaining purified rapamycin derivatives, including purified Biolimus A9. A crystalline form of Biolimus A9 is also described.

Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.

Abstract: The present invention provides compounds of formula I, wherein the variables R1, R2, R5 and b are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

Abstract: Provided are compounds of Formula (I), or pharmaceutically acceptable salts thereof, wherein i.a. Ring A is phenylene or 5- to 6-membered heteroarylene; Ring B is phenylene, 5- to 6-membered heterocycloalkylene or 5- to 6-membered heteroarylen; R4 is absent, heteroarylene, arylene, C1-3 alkylene, or R4 and R3 taken together with the nitrogen to which they are bound form a 3- to 7-membered heterocycloalkyl ring; R5 is absent, C(0)NR51, NR52 or 0; R6 is C2-10 alkylene or alkenylene, wherein one or two of the carbon atoms in the alkylene chain is optionally replaced by an 0, S, SO, SO2 or NR61, and wherein two of the carbon atoms in the alkylene chain are optionally connected by a two or three carbon atom alkylene chain to form a 5- to 7-membered ring; R7 is absent, NR71 or O. The compounds are IRAK4 inhibitors useful for the treatment of inflammatory diseases.

Abstract: Provided are amido spirocyclic amide and sulfonamide compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.

Abstract: The present application relates to novel benzyl-substituted pyrazolopyridines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.

Abstract: A zinc complex characterized in exhibiting an octahedral structure and being configured from repeating units represented by general formula (I): wherein L represents a linker region, and R1 represents a C1-4 alkyl group, which can have a halogen atom.

Abstract: The present invention is directed to multinuclear lanthanides chiral clusters, based on phenyl-oxazoline-amide (POxA) ligands, and to methods of use thereof. The chiral clusters of this invention are highly fluorescent with high stability.

Abstract: The invention is directed to the preparation of fluorinated compounds and their use in organic synthesis. In particular, the invention is directed to methods of reacting compounds of structure with Rf—CH?N2 or (CF3)2C?N2 to form a perfluoroalkylate or -arylated compounds, and products derived from these reactions, where X, YB, and Rf are described herein.

Abstract: Provided is a method for efficiently producing alkoxysilanes that are useful as various functional chemicals. In order to produce alkoxysilanes efficiently, an ethoxy- or methoxysilane and an alcohol are caused to react using, as a catalyst, for instance an inorganic solid acid having a regular-pore and/or layered structure. Zeolites, montmorillonites or the like can be used as the inorganic solid acid. When a zeolite is used as the catalyst, the silica/alumina ratio of the zeolite ranges preferably from 5 to 1000. The reaction can be promoted through irradiation of microwaves.

Abstract: The present invention relates generally to a surface functionalized porous containing material and method of making thereof.

Abstract: Provided herein are novel substituted thieno[3,2-d]pyrimidine-6-carboxamide sirtuin inhibitors and methods of use thereof. The sirtuin inhibitors may be used for inhibiting a sirtuin-mediated biological process, and, e.g. for treating and/or preventing diseases and disorders including, but not limited to cancer, neurodegenerative disease and inflammation. Also provided herein are pharmaceutical compositions comprising these sirtuin inhibitors and compositions comprising a sirtuin inhibitor in combination with another therapeutic agent.

Abstract: A method of ?-hydride elimination and subsequent 2,1-insertion from a transient nickel(II) acrylate hydride intermediate (Structure I). Also addressed is treatment of (dppe)Ni(CH(CH3)CO2BArf3) with a nitrogen containing base to produce a diphosphine nickel(0) ?2-acryl borate adduct.

Abstract: The present invention provides a canagliflozin complex. The complex is provided with an adsorbent selected from activated carbon, silica gel, ionic or non-ionic polymer and a cyclodextrin or derivatives thereof. The invention also provides a process for the preparation of canagliflozin and its intermediates thereof. The invention further provides a process for the purification of canagliflozin.

Abstract: There is provided an efficient and excellent preparation method of an ?-halo-tetraacyl-glucose which is suitable for industrial preparation, which comprises reacting D-glucose or lower alkyl D-glucoside with a reactive derivative of a carboxylic acid and a metal halide to prepare the ?-halo-tetraacyl-glucose represented by the formula (III): wherein R represents an optionally substituted lower alkyl group or an optionally substituted aryl group, and X represents a halogen atom, in one step, and the resulting ?-halo-tetraacyl-glucose (III) can be converted into a compound of the formula (I) or a salt thereof by subjecting to a conventional method.

Abstract: Provided are cyanogenic compositions for treating diseases, such as infectious diseases.

Abstract: The present invention relates to pharmaceutical compositions for rectal administration comprising fidaxomicin and to a process for preparing the pharmaceutical compositions for rectal administration. The invention also relates to an aerosol canister comprising a foamable pharmaceutical composition comprising fidaxomicin for rectal administration and to the treatment or maintenance of remission of infections such as diarrhea caused by Clostridium difficile.

Abstract: In some embodiments, the compositions and methods relate to compounds isolated from plants in the Salviniaceae family, pharmaceutical compositions comprising the same, and methods of using the same.

Abstract: The present invention provides fluorine substituted tricyclic nucleosides of formula (I) wherein: the substituents are as defined in the claims. The present invention further provides oligomeric compounds prepared therefrom. Incorporation of one or more of the tricyclic nucleosides into an oligomeric compound enhances one or more properties of the oligomeric compound. Such oligomeric compounds can also be included in double stranded compositions.

Abstract: Provided herein are compounds, compositions and methods for the treatment of liver disease and conditions, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.

Abstract: A method of deprotecting a solid support bound polynucleotide includes the step of contacting the polynucleotide with a composition comprising a diamine under conditions sufficient to deprotect the 2?-protected ribonucleotide residue. The solid support bound polynucleotide has at least one 2?-protected ribonucleotide residue, which has the following structure: wherein BP is a protected or unprotected heterocycle; R12 is a protecting group selected from a hydrocarbyl, a substituted hydrocarbyl, an aryl, and a substituted aryl; X is O or S; and PG is a thionocarbamate protecting group.

Abstract: Described herein are compounds, methods of making such compounds, pharmaceutical compositions, and medicaments comprising such compounds, and methods of using such compounds to treat androgen receptor mediated diseases or conditions. In some embodiments, the solid matrix comprises a polymer. In some embodiments, the polymer is soluble in an aqueous solution. In particular embodiments, the aqueous solution is water. In other embodiments, the aqueous solution has a pH of 5.0 or greater.

Abstract: A process is described wherein, by employing 17?-(3-hydroxypropyl) -63,7?3;15?,16?-dimethylene-5?-androstane-3?,5,17?-triol (II) as starting product, in a single stage reaction there is obtained drospirenone, (I), whereby the reaction is achieved using gaseous oxygen as the stoichiometric oxidant in the presence of a catalytic system containing (i) TEMPO or a derivative thereof (ii) a ferric salt (Fe3+) and (iii) NaCl. The product drospirenone is a known synthetic steroid with progestogenic, antimineralocorticoid and antiandrogenic action, that is useful for preparing pharmaceutical compositions with contraceptive action.

Abstract: The present invention provides methods for reducing and/or evaluating the immunogenic potential of a therapeutic protein preparation. The present invention further provides pharmaceutical compositions of therapeutic proteins and methods of treatment with the same, the compositions having low immunogenic potential and/or improved efficacy. The invention achieves these goals by evaluating therapeutic protein preparations for subvisible protein particulates, which can contribute significantly to the overall immunogenic potential of the protein preparation. Further, by maintaining the content of such subvisible protein particulates to below an immunogenic threshold level, the resulting pharmaceutical composition is less likely to result in a loss of tolerance (e.g., upon repeated administration), thereby improving both the safety and efficacy profile of the therapeutic.

Abstract: The present invention discloses latent thioester functionalities attached to the C-terminus of a first polypeptide, or a first fragment thereof having a Cys residue at its N-terminus, and a process using this functionality for the preparation of polypeptide thioesters, in particular of ubiquitin thioesters, this process comprising preparing a polypeptide or a fragment thereof, being attached to a latent thioester functionality, which can then be ligated with a second polypeptide fragment, followed by selective activation of the latent thioester functionality group, to provide the requested polypeptide thioester. There are also provided the polypeptides obtained by this method, specific unnatural amino acids useful to be incorporated within the polypeptide thioesters, and kits for preparing them.

Abstract: Provided herein are methods for refolding denatured protein (e.g., from inclusion bodies) that do not require the use of a denaturing agent. Exemplary methods use a high pH for solubilizing denatured protein, followed by a decrease in pH for refolding the proteins.

Abstract: The invention pertains to process for manufacturing whey protein concentrate (WPC) from whey, said process involving (a) providing acidified whey; (b) increasing the pH of said acidified whey using one or more carbonate salt(s), preceded and/or followed by ultrafiltration, and (c) subjecting the ultrafiltered carbonate-containing whey to spray drying. A WPC is provided having improved functional properties, particularly increased gel strength and reduced salt sensitivity (i.e. meaning that the functional properties of the WPC are affected by salt to a lesser extent).

Abstract: A method of purifying an antibody composition comprises application of anion exchange chromatography late in the purification process. An ultrafiltration/diafiltration-purified antibody composition is subjected to anion exchange chromatography (AEX) to form a pharmaceutically-pure antibody composition.

Abstract: A method includes (i) adding allantoin in a supersaturating amount to a protein preparation including a desired protein and at least one endotoxin as a contaminant, (ii) removing solids after the adding step to provide a sample for further purification by void exclusion chromatography on a packed particle bed of electropositive particles in a column, the packed particle bed having an interparticle volume, (iii) applying a sample volume to the packed particle bed, wherein the electropositive particles support void exclusion chromatography, and wherein the sample volume is not greater than the interparticle volume, and (iv) eluting a purified sample including the desired protein and a reduced amount of the endotoxin. The method is optionally carried out with only the allantoin treatment or only the void exclusion chromatography.

Abstract: The embodiments provide prodrug compounds of Formulae I-XVII. The present disclosure also provides compositions, and their methods of use, where the compositions comprise a prodrug compound of Formulae I-XVII that provides controlled release of an active agent. Such compositions can optionally provide a trypsin inhibitor that interacts with the enzyme that mediates the controlled release of an active agent from the prodrug so as to attenuate enzymatic cleavage of the prodrug.

Abstract: The invention relates to methods for treating depression, anxiety, and other related diseases by administering a peptide NMDAR partial agonist.

Abstract: The disclosure provides methods of preventing, ameliorating or treating disruption of mitochondrial function and symptoms thereof. The methods provide administering aromatic-cationic peptides in effective amounts to prevent, treat or ameliorate the disruption of mitochondrial oxidative phosphorylation in a cell such as that found in a subject suffering from, or predisposed to a mitochondrial disease or disorder. In some embodiments, the methods comprise administering to a subject suffering from, or at risk for a mitochondrial disease or disorder, an effective amount of an aromatic-cationic peptide to subjects in need thereof.

Abstract: The present invention relates to novel polypeptides having satiety hormone releasing activity (e.g., cholecystokinin (CCK) and/or glucagon-like peptide-1 (GLP-1) releasing activity).

Abstract: The present invention relates to methods and compositions for treating disease related to disorders of bone remodeling. In particular, the present invention relates to compositions and methods for treating rheumatoid arthritis.

Abstract: Disclosed herein is a composition comprising at least one polymyxin or a salt thereof represented by formula (I) wherein R1 is an aliphatic linear or branched C6-C10 acyl group, or (I?) R5 is —CH(CH3)2, —CH2CH(CH3)2, —CH(CH3)CH2CH3, or —CH2C6H5; R6 is —CH(CH3)2, —CH2CH(CH3)2, or —CH(CH3)CH2CH3; each of R2, R3, R4, R7 and R8 is either —(CH2)XCH2NH2 or —(CH2)xCH2N(CH2SO3M)2; wherein x is 0 or 1; wherein M is a monovalent cation; and wherein at least three of R2, R3, R4, R7 and R are —(CH2)xCH2N(CH2SO3M)2.

Abstract: This disclosure relates to therapeutic agents comprising polypeptides and peptides that include the amino acid sequence motif arginine-lysine-aspartic acid [RKD] and their use in the treatment of conditions associated with abnormal angiogenesis.

Abstract: The invention relates to tumour therapy. In one aspect, the present invention relates to conjugates of an amatoxin and a target-binding moiety, e.g. an antibody, connected by certain linkages, which are useful in the treatment of cancer and other disorders and diseases. In a further aspect the invention relates to pharmaceutical compositions comprising such conjugates.

Abstract: A cyclosporin derivative which is a compound of formula (I), or a pharmaceutically acceptable salt thereof, for use in the treatment or prevention of a viral infection: wherein: A represents (F(II)) or (F(III)) B represents methyl or ethyl, R2 represents ethyl or isopropyl, R4 represents —CH2CH(CH3)CH3, —CH2CH(CH3)CH2CH3, —CH(CH3)CH3 or —CH(CH3)CH2CH3, and either (a) one of R1 and R1* represents hydrogen and the other represents methyl, and R3 represents —L3-G3, or (b) one of R1 and R1* represents hydrogen and the other represents and R3 represents H, wherein L1 and L3 represent a direct bond, a C1-C6 alkylene group or a C2-C6 alkenylene group; and G1 and G3 represent a hydrogen atom, a —COOR? group, or a phenyl moiety which is unsubstituted or substituted by one, two or three substituents selected from a halogen atom, a —COOR? group, a —CONR?R? group, a hydroxyl group, a C1-C6 alkyl group and a C1-C6 alkoxy group, wherein R? and R? are the same or different and represent hydrogen or a C1-C6 alkyl group, prov

Abstract: A pharmaceutical composition for use in killing and/or inhibiting the growth and/or proliferation of a microorganism in a subject in need thereof, or for treating a subject afflicted with a microbial infection is disclosed. The composition comprises: (a) an effective amount of an isolated peptide, wherein the peptide comprises the arginine-rich carboxy-terminal region of hepatitis B virus core protein (HBc) and exhibits an antimicrobial activity; and (b) a pharmaceutically acceptable carrier. The peptide exhibits an activity against Gram-negative bacteria, Gram-positive bacteria, and/or fungi.