Abstract: Amorphous and polymorphic of palonosetron hydrochloride are disclosed that can be characterized by X-ray powder diffraction patterns, thermal properties, purity and methods of manufacture. These forms of palonosetron hydrochloride can be produced from solution or by solid state interconversions. The forms can be used in pharmaceutical formulations: particularly preferred uses of these formulations are in prevention and treatment of nausea and emesis arising from chemotherapy or postoperative side effects. The forms can optionally be used as mixtures of the crystalline and/or amorphous forms.

Abstract: The present invention relates to novel benzimidazole derivatives of the general formula (I), processes for their preparation and their use for the production of pharmaceutical compositions for the treatment of diseases and indications that are connected with the receptor EP4.

Abstract: Amine substituted pyrimidine compounds and forms thereof that inhibit the function and reduce the level of B-cell specific Moloney murine leukemia virus integration site 1 (Bmi-1) protein and methods for their use to inhibit Bmi-1 function and reduce the level of Bmi-1 to treat a cancer mediated by Bmi-1 are described herein.

Abstract: The present invention relates to crystalline and amorphous forms of 6-fluoro-2-[4-(pyridin-2-yl)but-3-yn-1-yl]imidazo[1,2-a]pyridine mono-phosphate salt and methods of making these solid forms thereof. The invention compounds are modulators of mGlu5 which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGlu5 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGlu5 is involved.

Abstract: The present invention relates to a compound useful as a selective inhibitor of PI3K?. 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 relates to fluoro-9-methyl-?-carbolines, their preparation as well as their medical use and pharmaceutical compositions containing fluoro-9-methyl-?-carbolines.

Abstract: This disclosure relates to a one-step method for preparing the tau radiopharmaceutical, [18F]T807, using an unprotected or protected precursor (e.g., tert-butyl 7-(6-nitropyridin-3-yl)-5H-pyrido[4,3-b]indole-5-carboxylate).

Abstract: The present invention relates to the 3,7-diazabicyclo[3.3.1]nonane carboxamides and process for preparation thereof. The present invention further relates to the compounds of general formula 1 possessing anti-thrombotic (anti-platelet) activities. The invention also relates to use of these moieties as inhibitors of collagen induced platelet adhesion and aggregation mediated through collagen receptors both in vitro and in vivo. Further, invention also relates these class of compounds exhibiting anti-platelet efficacy through dual mechanism inhibited both collagen as well as U46619 (thromboxane receptor agonist) induced platelet aggregation.

Abstract: Disclosed are compounds that inhibit breast cancer resistance protein (BCRP), of which compound (I-1), ((3S, 6S, 12aS)-6-isobutyl-9-methoxy-3-methyl-2,3,6,7, 12, 12a- hexahydropyrazino[1?,2?: 1,6]pyrido[3,4-b]indole-1,4-dione) or a pharmaceutically acceptable salt thereof, and the compound 12, ((3S,6S,12aS)-6-isobutyl-9-methoxy-3,10- dimethyl-2,3,6,7,12, 12a-hexahydropyrazino[1?,2?: 1,6]pyrido[3,4- b] indole-1,4-dione) or a pharmaceutically acceptable salt thereof. Also disclosed are methods of inhibiting BCRP or decreasing BCRP activity and methods of determining potential BCRP substrates.

Abstract: Described herein are compounds of Formula (A), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.

Abstract: The present invention discloses compounds according to Formula I: Wherein R1a, R1b, R2, R4, R5, R6, R7, R8, W, X, Y, Z, Cy, and the subscript a are as defined herein. The present invention relates to compounds inhibiting autotaxin (NPP2 or ENPP2), methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of diseases involving fibrotic diseases, proliferative diseases, inflammatory diseases, autoimmune diseases, respiratory diseases, cardiovascular diseases, neurodegenerative diseases, dermatological disorders, and/or abnormal angiogenesis associated diseases by administering the compound of the invention.

Abstract: Disclosed are a method for preparing an intermediate for producing high-purity pemetrexed and a method for producing high-purity pemetrexed using the intermediate, and more specifically, a method for preparing pemetrexed diethyl ester, which is an intermediate for producing pemetrexed, or a salt thereof with high purity, and to a method for producing pemetrexed disodium salt with high purity using the intermediate.

Abstract: The present invention relates generally to the field of antimicrobial compounds and to methods of making and using them. These compounds are useful for treating, preventing, reducing the risk of, and delaying the onset of microbial infections in humans and animals.

Abstract: Proteinopathies result from the proteasome not acting efficiently enough to eliminate harmful proteins and prevent the formation of the pathogenic aggregates. As described herein, inhibition of proteasome-associated deubiquitinase Usp14 results in increased proteasome efficiency. The present invention therefore provides novel compositions and methods for inhibition of Usp14, enhancement of proteasome activity and treatment of proteinopathies.

Abstract: The invention provides compounds that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from those of the compound not attached to the water-soluble oligomer.

Abstract: A method for producing a highly pure PMDA comprises at least the following steps: (1) a step of preparing a raw material solution by dissolving a raw material of a pyromellitic dianhydride in an acetic acid solvent, (2) a step of preparing a precursor pyromellitic dianhydride by recrystallizing the pyromellitic dianhydride in the prepared raw material solution and separating the acetic acid solvent, (3) a step of performing a degassing treatment on the precursor pyromellitic dianhydride by stirring the precursor pyromellitic dianhydride in a fluidized state while heating under reduced-pressure conditions, and (4) a step of taking out the pyromellitic dianhydride subjected to the degassing treatment.

Abstract: Methods of synthesizing intermediates useful for the synthesis of halichondrin B analogs are described.

Abstract: Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1 (7-36) and GLP-1 (9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.

Abstract: Disclosed are a fused pyrimidine compound, an intermediate, a preparation method therefor, and a composition and an application thereof. The present invention provides a fused pyrimidine compound shown in formula I, pharmaceutically acceptable salt, hydrate, solvate, and an optical isomer or prodrug of the compound. The present invention further provides applications of the fused pyrimidine compound shown in formula I, the pharmaceutically acceptable salt, the hydrate, solvate, and the optical isomer or the prodrug of the compound in the preparing drugs for curing and/or preventing a kinase-related disease. The fused pyrimidine compound I of the present invention is an efficient PI3 kinase depressor, and can be used to prepare drugs for preventing and/or curing cell-proliferation diseases such as cancer, infection, inflammation, and an autoimmune disease.

Abstract: The present invention in one embodiment provides a compound of Formula I: (I), or a pharmaceutically acceptable salt thereof, wherein Y1, Y2 and Y3 are each independently selected from hydrogen and deuterium; R1, R2, and R3 are each methyl and are independently substituted with 0 to 3 deuterium; and R4 is t-butyl and is substituted with 0 to 9 deuterium; provided that if R1, R2 and R3 are each —CH3, and R4 is —C(CH3)3, then at least one of Y1 and Y2 is deuterium.

Abstract: The compounds and salts of the present invention inhibit kinases, especially the anaplastic lymphoma kinase (ALK) and the HGF receptor tyrosine kinase (RTK) c-Met, and are useful for treating or ameliorating abnormal cell proliferative disorders, such as cancer.

Abstract: The present invention is directed to 2,2-difluorodioxolo compounds that are antagonists of A2A receptor. The present invention is also directed to uses of the 2,2-difluorodioxolo compounds described herein in the potential treatment or prevention of neurological disorders and diseases in which A2A receptor are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds and to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which A2A receptors are involved.

Abstract: The present invention includes novel compounds, and compositions comprising same, useful for preventing or treating an HIV-1 infection in a subject in need thereof. The present invention further includes a novel method of preventing or treating an HIV-1 infection in a subject in need thereof, comprising administering to the subject an effective amount of a compound and/or composition of the invention. In certain embodiments, the subject is further administered at least one additional therapeutic agent.

Abstract: An object of the present invention is to enable the synthesis of various fluorine-containing compounds having an organic group at both terminals of their tetrafluoroethylene structure (—CF2—CF2—). The present invention provides a fluorine-containing complex compound including a fluorine-containing organic metal compound represented by formula (1a): R1—CF2—CF2-M1??(1a) wherein M1 is a metal selected from the group consisting of copper, zinc, nickel, iron, cobalt, and tin; and R1 represents an organic group, and at least one ligand selected from the group consisting of pyridine ring-containing compounds and phosphines.

Abstract: Compounds, methods of making the compounds and methods of using the compounds are generally described herein. The compounds are generally of formula R1R2N—ZnY LiY, wherein R1 and R2 are independently selected from H, aryl, heteroaryl containing one or more heteroatoms, alkyl, alkenyl, alkynyl, and silicon derivatives thereof; and each Y is independently selected from F, Cl, Br, I, CN, SCN, NCO, HalO3, HalO4, NO3, BF4, PF6, H, an alcoholate of formula OR5, a carboxylate of formula R5CO2; a thiolate of formula SR5, R5P(O)O2, SCOR5, SCSR5, OnSR5 and NOn, wherein n=2 or 3; wherein R5 is selected from substituted or unsubstituted aryls or heteroaryls containing 3 to 24 carbon atoms and one or more heteroatoms selected from B, O, N, S, Se, P, linear, branched or cyclic, substituted or unsubstituted alkyls, alkenyls, alkynyls or H; and wherein Hal is a halogen selected from Cl, Br and I.

Abstract: A metallacrown complex has the formula: Ln(III)[12-MC-4]2[24-MC-8], wherein MC is a metallacrown macrocycle with a repeating sub-unit consisting of a transition metal (M(II)) and a hydroxamic acid (HA) ligand that produces a ligand-based charge transfer state when incorporated into the metallacrown complex. In an example of a method for making the metallacrown complex, a hydroxamic acid (HA) ligand that is to produce a ligand-based charge transfer state when incorporated into the metallacrown complex, a transition metal salt, and a rare-earth salt are dissolved in a solvent to form a solution. A base is added to the solution. The solution is stirred at a predetermined temperature for a predetermined time. The solution is exposed to a purification method to produce crystals of the metallacrown complex.

Abstract: The technology described herein relates to pinacolyl boronate substituted stilbenes for the treatment of cancers, e.g. cancers expressing abnormally high levels of SREBP 1.

Abstract: Compounds and method of preparation of Si—X and Ge—X compounds (X?N, P, As and Sb) via dehydrogenative coupling between the corresponding unsubstituted silanes and amines (including ammonia) or phosphines catalyzed by metallic catalysts is described. This new approach is based on the catalytic dehydrogenative coupling of a Si—H and a X—H moiety to form a Si—X containing compound and hydrogen gas (X?N, P, As and Sb). The process can be catalyzed by transition metal heterogenous catalysts such as Ru(0) on carbon, Pd(0) on MgO) as well as transition metal organometallic complexes that act as homogeneous catalysts. The —Si—X products produced by dehydrogenative coupling are inherently halogen free. Said compounds can be useful for the deposition of thin films by chemical vapor deposition or atomic layer deposition of Si-containing films.

Abstract: The present invention relates to a novel ligand compound, a preparation method thereof, a transition metal compound including the ligand compound, and a preparation method thereof. The ligand compound of novel structure according to the present invention and the transition metal compound including the same may be used as a polymerization reaction catalyst for preparing olefin polymers.

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

Abstract: Compounds of the formulae, (I), wherein each variable is as defined herein are provided which are useful in (i) diagnostic methods for detecting and/or identifying cells presenting PSMA; (2) compositions comprising a compound of the invention together with a pharmaceutically acceptable carrier, excipient, and/or diluent; (3) methods for inhibiting or treating prostrate cancer; and (4) methods for blocking or destabilizing neovasculature of a tumor.

Abstract: A method of producing 4-(((6S,9S)-1-(benzylcarbamoyl)-2,9-dimethyl-4,7-dioxo-8-(quinolin-8-ylmethyl)octahydro -1H-pyrazino[2,1-c][1,2,4]triazin-6-yl)methyl)phenyl dihydrogen phosphate, including a step of adding a reaction mixture 1 containing (6S,9S)-N-benzyl-6-(4-hydroxybenzyl)-2,9-dimethyl-4,7-dioxo-8-(quinolin-8-ylmethyl)octahydro -1H-pyrazino[2,1-c][1,2,4]triazine-1-carboxamide, triethylamine and a solvent to a reaction mixture 2 containing a phosphorylating agent and a solvent.

Abstract: The present invention relates to a voriconazole sodium phosphate hydrate, polymorphs thereof, a preparation method thereof, and use thereof, wherein the voriconazole phosphate salt hydrate prepared by using an isopropanol-water system, ethanol-water system, or an ethanol system comprises different crystal forms. And these kinds of crystal forms have favorable water solubility and stability and feature a simple manufacturing process. The voriconazole phosphate salt hydrate is principally used for treatment of fungal infections.

Abstract: The invention comprises a compound characterized by a general formula (1). wherein X is a group described by a general formula wherein is with l being 0 or 1, is a —alkyl with p being or is a —alkyl with q being or 4, and wherein Z is a group described by a general formula wherein with l being 0 or 1, Kr is a —alkyl with r being 0, 1, 2, 3 or 4, Kt is a —alkyl with t being 0, 1, 2, 3 or 4, wherein each OM is an organometallic compound independently selected from each other from the group of an unsubstituted or substituted metal sandwich compound, an unsubstituted or substituted half metal sandwich compound or a metal carbonyl compound and their use.

Abstract: The present invention provides a method of recovering dsRNA, from which a surfactant and endotoxin have been removed simultaneously, which includes mixing the surfactant and dsRNA, and contacting the mixture with a hydrophobic adsorptive resin or activated carbon.

Abstract: The present invention provides a compound of Formula I or hydrate thereof, useful for the treatment of diabetes.

Abstract: Provided are certain derivatives of amphotericin B (AmB) characterized by reduced toxicity and retained anti-fungal activity. Certain of the derivatives are C16 urea derivatives of AmB. Certain of the derivatives are C3, C5, C8, C9, C11, C13, or C15 deoxy derivatives of AmB. Certain of the derivatives include C3? or C4? modifications of the mycosamine appendage of AmB. Also provided are methods of making AmB derivatives of the invention, pharmaceutical compositions comprising AmB derivatives of the invention, and methods of use of AmB derivatives of the invention.

Abstract: Described herein are 5-position modified cytosine nucleotides and nucleosides as well as phosphoramidites and triphosphates derivatives thereof. Further provided are methods of making and using the same, and compositions and uses of the modified nucleosides as part of a nucleic acid molecule (e.g., aptamer).

Abstract: The present invention relates to obeticholic acid: or a pharmaceutically acceptable salt, solvate or amino acid conjugate thereof. Obeticholic acid is useful for the treatment or prevention of a FXR mediated disease or condition, cardiovascular disease or cholestatic liver disease, and for reducing HDL cholesterol, for lowering triglycerides in a mammal, or for inhibition of fibrosis. The present invention also relates to processes for the synthesis of obeticholic acid.

Abstract: The present invention relates to a method for preventing the unfolding of a (poly)peptide during drying and/or inducing the (re-)folding of a (poly)peptide after drying, comprising the step of embedding the (poly)peptide in an aqueous solution, wherein the solution comprises (i) at least three different amino acids; or (ii) at least one dipeptide or tripeptide; and wherein the solution is free or substantially free of (a) sugar; and (b-i) protein; and/or (b-ii) denaturing compounds; and (c) silanes.

Abstract: It is provided an improved process for preparing peptide epoxy ketones, including novel compounds that can be used as intermediates in the process for preparing Carfilzomib and other peptide epoxy ketones.

Abstract: The present invention relates to a peptaibol having sequence AcAib-Asn-Aib-Leu-Aib-Pro-Aib-Asn-Leu-Pro-Ileuol, isolated from endophytic fungus Trichoderma longibrachiatum having accession number MTCC 5721. The peptaibol is named as brachiating D. The present also related to a process for isolating the peptaibol from and use of the peptaibol as a pharmacologically active compound as a strong immunosuppressants and as an anticancer agents.

Abstract: A pharmaceutical composition for preventing or treating an ocular surface disease is disclosed, wherein the pharmaceutical composition includes, as an active component, collagen type II ?1 based peptide GQDGLAGPK isolated from chondrocyte-derived extracellular matrix (CDEM). In an alkaline burn animal mode treated with peptide GQDGLAGPK, the occurrence of corneal opacification is reduced as well as the expression of angiogenic factors (e.g., CD31 and VEGF). In addition, the expression of inflammatory markers (e.g., macrophages, TNF?, ICAM-1, VCAM-1, and MMP-9) is reduced while the expression of inflammation-inducing factor (e,g,, NF-?B) is suppressed. The peptide GQDGLAGPK according to the present invention may be applied to a pharmaceutical composition for preventing or treating an ocular surface disease (e.g., a corneal disease).

Abstract: The invention provides peptides that can reactivate p53 mutants efficiently and specifically, as well as methods that allow the identification, selection and isolation of such peptides, in a precise, cost and time effective manner. In particular, there are provided mutant p53 reactivating peptides that can restore the native wild type p53 folding, and hence the tumor suppressor activity, to the mutant p53 protein. Such peptides are useful for treating various conditions and diseases in which p53 is mutated.

Abstract: In some aspects, the present invention provides cell-reactive compstatin analogs and compositions comprising cell-reactive compstatin analogs. In some aspects, the invention further provides methods of using cell-reactive compstatin analogs, e.g., treat a complement-mediated disorder, e.g., to inhibit complement-mediated damage to a cell, tissue, or organ. In some aspects, the invention provides long-acting compstatin analogs and compositions comprising long-acting compstatin analogs. In some aspects, the invention further provides methods of using long-acting compstatin analogs, e.g., to treat a complement-mediated disorder, e.g., to inhibit complement-mediated damage to a cell, tissue, or organ. In some aspects, the invention provides targeted compstatin analogs and compositions comprising targeted compstatin analogs. In some aspects, the invention further provides methods of using targeted compstatin analogs, e.g., to treat a complement-mediated disorder, e.g.

Abstract: The present invention relates to a novel cyclohexapeptide, to a method for the preparation of said cyclohexapeptide and to the use of said cyclohexapeptide.

Abstract: In some aspects, the present invention cell-penetrating compstatin analog and compositions comprising cell-penetrating compstatin analog. In some aspects, the invention further provides methods of using cell-penetrating compstatin analogs treat a complement-mediated disorder, e.g., to inhibit complement-mediated damage to a cell, tissue, or organ, to inhibit production or release of biologically active C3 cleavage products.

Abstract: Immunogenic compositions relating to DNA launched suicidal flaviviruses and methods of administering the same are described herein.

Abstract: Methods are described for predicting ancestral sequences for viruses or portions thereof. Also described are predicted ancestral sequences for adeno-associated virus (AAV) capsid polypeptides. The disclosure also provides methods of gene transfer and methods of vaccinating subjects by administering a target antigen operably linked to the AAV capsid polypeptides.

Abstract: The invention provides a Pseudomonas exotoxin A (PE) comprising an amino acid sequence having a substitution of one or more B-cell and/or T-cell epitopes. The invention further provides related chimeric molecules, as well as related nucleic acids, recombinant expression vectors, host cells, populations of cells, and pharmaceutical compositions. Methods of treating or preventing cancer in a mammal, methods of inhibiting the growth of a target cell, methods of producing the PE, and methods of producing the chimeric molecule are further provided by the invention.