Abstract: Compounds that modulate the oxidoreductase enzyme indoleamine 2,3-dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided.

Abstract: Compounds that modulate the oxidoreductase enzyme indoleamine 2,3-dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided.

Abstract: A novel crystalline form of (S)—N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide, pharmaceutical compositions containing said crystalline form and the use of said crystalline form in the treatment of pain, cancer, inflammation, neurodegenerative disease or Trypanosoma cruzi infection are disclosed. In some embodiments, the novel crystalline form comprises a stable polymorph of (S)—N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate. The present invention is further directed to a process for the preparation of the novel crystalline form.

Abstract: Improved processes for making hydrocodone and hydromorphone as well as their 8,14-dihydrothebaine and 8,14-dihydrooripavine derivatives and salts are disclosed.

Abstract: Improved processes for making hydrocodone and hydromorphone as well as their 8,14-dihydrothebaine and 8,14-dihydrooripavine derivatives and salts are disclosed.

Abstract: This invention relates to the discovery of novel polymorphic forms of naltrexone, including solvates, hydrates, anhydrous and other crystalline forms and combinations thereof. These novel forms of naltrexone impart advantages in pharmaceutical formulations incorporating them, including sustained release, or long acting, formulations.

Abstract: Provided are Icotinib maleate (the compound of Formula I) and polymorph forms thereof, and methods of preparing and using them.

Abstract: The invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine for the treatment of diseases, disorders associated with the modulation of calcium release-activated calcium (CRAC) channel. The invention also relates to pharmaceutical compositions containing such compounds in treating diseases disorders associated with calcium release-activated calcium (CRAC) channel modulators.

Abstract: The present invention provides compounds of formula (I), wherein: R1 is unsubstituted C1-C6 alkyl; La is substituted or unsubstituted C1-C6 alkyl linker, substituted or unsubstituted C3-C10 carbocycle, substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S, or substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S; and R2 and R3 are each, independently, H, substituted or unsubstituted C1-C6 alkyl, or substituted or unsubstituted C6-C10 aryl; or alternatively, R2 and R3, together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S or a substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S.

Abstract: Disclosed is a compound of formula 1, or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, R7, R7?, R8, R9, R10, R11, R12 and R13 are as disclosed herein. Also, disclosed is a process for the preparation of the compound of formula 1, or a pharmaceutically acceptable salt thereof, and intermediates used therein. The compound of formula 1 can be used in the preparation of halichondrin analogs, such as Eribulin; and a process for its preparation from the compound of formula 1 is also disclosed.

Abstract: Provided herein, inter alia, are compositions and methods useful for treating hyperproliferative diseases, including cancer and non-malignant hyperproliferative diseases.

Abstract: The present disclosure provides a method of purifying pharmaceutical compositions consisting essentially of STAT3 inhibitors from a mixture of compounds, pharmaceutical compositions comprising STAT3 inhibitors used to inhibit STAT3 in tumor cells, and certain pharmaceutically acceptable salts thereof, and methods of use.

Abstract: The thieno[2,3-b]pyridines of general formula (I), wherein R1 is Me, C6H5, 3,4,5-(OMe)3C6H2, NH2; R2 is H, CN, COMe, COOC1-4alkyl, COOC2H4OMe, COOC2H4OPr(n); R3 is C6H4R6, 3,4-OCH2O—C6H3; 2-furanyl; R6 is 4-Cl, 4-NO2, 4-N(C1-4alkyl)2, 3-(C1-4alkyloxy), 4-(C1-4alkyloxy), 3,4-(C1-4alkyloxy)2, 3,4,5-(C1-4alkyloxy)3; R4 is NH2, NHCOMe; R5 is CN, COMe, COC6H4R7; CO-(2-naphthyl); R7 is H, 4-F, 4-Cl, 3-OMe, 4-OMe, 2,4-(OMe)2, 3,4,5-(OMe)3 as multidrug resistance modulators to increase the effectiveness of chemotherapy in cancer treatment.

Abstract: The present disclosure relates generally to thienopyrimidine and thienopyridine compounds and methods of use thereof. In particular embodiments, the present disclosure provides compositions comprising thienopyrimidine and thienopyridine compounds of Formula 2: and methods of use to inhibit the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins.

Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity, particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.

Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.

Abstract: The present invention relates to novel compounds of the formula I which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.

Abstract: The present invention relates to a process of preparing a Grignard reagent comprising reacting magnesium particulates in a fluid bed reactor. The present invention further relates to a continuous process comprising fluidizing magnesium particulates in a reactor, forming the Grignard reagent continuously, and reacting the Grignard reagent with a substrate.

Abstract: Disclosed are compounds and methods of making said compounds comprising a zinc oxide molecule chemically bound to one or more molecules having an acidic hydrogen, such as an organic acid. The invention also provides compositions comprising such compounds and methods of preparing such compounds. The compounds of the invention may be provided in, for example, topical skin formulations, pharmaceutical compositions, or delivery systems for active ingredients.

Abstract: The present invention relates to metal oxide precursors comprising i) at least one metal atom selected from the group consisting of In, Ga, Zn and Sn, ii) at least one non-photocrosslinkable ligand and iii) at least one photocrosslinkable ligand, to liquid coating compositions comprising the precursors, and to their use.

Abstract: The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of disease.

Abstract: An object of the present invention is to provide a silicon oligomer having a novel function that has not been achieved by a conventional condensation product of water and a tetraalkoxysilane. Provided are a silicon oligomer represented by the following formula (I) and a production method therefor: wherein R1 to R10 each independently is an alkyl group or a hydroxyalkyl group, each having 1 to 4 carbon atoms; X1 to X3 each independently is a group represented by the following formula (II); n is 0 or 1; and m is an integer of 1 to 3 when n is 0, and m is 1 when n is 1: wherein A is an alkylene group having 2 to 4 carbon atoms which may be branched, and l is an integer of 1 to 3.

Abstract: Silicone compounds, delivery compositions, compositions, packaged products and displays comprising such silicone compounds, and processes for making and using such benefit agent delivery compositions, compositions, packaged products and displays. Such compositions have improved deposition and retention properties that may impart improved benefit characteristics to a composition and/or situs.

Abstract: Titanium-containing film forming compositions are disclosed as well as methods of synthesizing the same and methods of forming Titanium-containing films on substrates via vapor deposition processes using the Titanium-containing film forming compositions. The Titanium-containing film forming compositions comprise a precursor having the formula Ti(R5Cp)2(L), wherein each R is independently H, an alkyl group, or R?3Si, with each R? independently being H or an alkyl group; L is selected from the group consisting of formamidinates (NR,R?-fmd) or amidinates (NR, R?-amd).

Abstract: The present invention relates to a phosphorus containing alcohol, obtainable or obtained by a process comprising the reaction of at least one alcohol with a phosphorus containing compound of the general formula (I) as defined herein, as well as the process for preparing a phosphorus containing alcohol, comprising the reaction of at least one alcohol with a phosphorus containing compound of the general formula (I). Furthermore, the present invention relates to the use of a phosphorus containing alcohol as disclosed herein as a flame retardant, to a process for the preparation of a polyurethane and the polyurethane as such.

Abstract: A compound has Formula I: A, B, C, D, W, X, Y, and Z are independently selected from hydrogen, optionally substituted C1-C6 alkyl, optionally substituted C1-C6 alkoxy, aryl, aldehyde, protected aldehyde, CH, N, O, S, null, and bond; Q is selected from aldehyde, protected aldehyde, and null, at least one of A, B, C, D, W, X, Y, Z, or Q is an aldehyde or protected aldehyde; the bonds between each of A-B, B-C, C-D, W-X, X-Y, and Y-Z are selected from single bond, double bond, triple bond, and no bond; L is a linker selected from a C1-C12 alkyl, aralkyl, and aryl, any of which is optionally substituted; one or more methylene unit (CH2) of the C1-C12 alkyl is optionally replaced by any combination of oxygen, carbonyl(C?O), and NH; and R1 and R2 are independently selected from —NR3R4, halogen, C1-C8 alkoxy, aralkoxy, alkenyloxy, alkynyloxy, and OCH2CH2CN; R3 and R4 are independently a C1-C4, straight chain or branched alkyl group.

Abstract: The present invention relates to azine metal phosphates, compositions containing the same, a process for preparing the same and their use as flame retardants. Typical representatives are (A-H)+)[MtPO4](+).2H2O and (Mel-H)(+)[AlP2O7](+) (where A=melamine or guanidine, Mel=melamine and Mt=Mg or Zn).

Abstract: Provided herein are novel carbon-monoxide releasing molecules (CO-RMs) of the Formula (I): and esters, amides, salts, solvates and hydrates thereof; wherein R1 and R2 are as described herein. Also provided are pharmaceutical compositions comprising these compounds, methods of their preparation, and their use in the treatment of liver disease and inflammation.

Abstract: Methods for obtaining purified lignin and the lignin that can be obtained by the methods are described. Methods include processing pretreated lignocellulosic biomass feedstock to recover the lignin and provide a lignin composition with a very low level of impurities such as metals and ash. In addition, the lignin recovered from the process can have a narrow molecular weight distribution and, depending upon the specific stages utilized in the process, can have a predetermined molecular weight. The process includes one or more separation stages in which a lignin-containing feedstock is mixed with a solvent solution. The mixture fractionates to form a solvent-rich liquid phase and a lignin-rich liquid phase, the lignin being partitioned across the phases according to the molecular weight of the lignin. Furthermore, the metal salts of the pretreated lignocellulosic biomass feedstock also partition across the phases.

Abstract: The invention relates to lipochitooligosaccharides obtainable from arbuscular mycorrhizal fungi, and which are useful for stimulating arbuscular mycorrhizal symbiosis, and lateral root formation.

Abstract: The invention relates to processes for preparing (S,S)-secoisolariciresinol diglucoside and (R,R)-secoisolariciresinol diglucoside and compositions comprising the same.

Abstract: The present invention provides a method for preparing epirubicin and an intermediate adaptive to the method. The preparation method may include: reacting tert-Butyldimethylsilyl chloride with N-trifluoroacetyl adriamycin to obtain a first compound N-trifluoroacetyl-14-O-tert-Butyldimethylsilyl adriamycin; oxidizing the first compound to obtain a second compound 4?-ketone-N-trifluoroacetyl-14-O-tert-Butyldimethylsilyladriamycin; reducing the second compound to obtain a third compound N-trifluoroacetyl-14-O-tert-Butyldimethylsilyl epirubicin; and performing deprotection and hydrolysis reactions on the third compound to obtain epirubicin. The method of the present invention needs low cost, fewer reaction steps, provides high yield and high product purity, and avoids serious pollution caused by a bromination reaction in a conventional method.

Abstract: The present disclosure provides cytidine derivative dimers, salts and compositions of the cytidine derivative dimers, and methods of making and using the cytidine derivative dimers that are useful for treating a neoplasm in mammalian subjects. A cytidine derivative dimer may have the following general formula (I): By molecularly designing such cytidine-based compounds, the disclosed cytidine-based derivative dimers/salts show significant inhibiting effects on HCT-116 human colon cancer cells, and exhibit strong growth inhibiting effects on HCT-116 human colon cancer xenografts grown in nude mice. The disclosed cytidine derivative dimers/salts provide high anti-tumor activity with low toxicity and are useful for treating cancers.

Abstract: The invention provides phosphoramidate prodrugs for targeting and treating liver disease, including liver cancer, hepatocellular carcinoma, and hepatitis.

Abstract: The present invention provides novel anhydrous polymorph forms of 2R,3S,4R,5R)-5-(6-(cyclopentylamino)-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl nitrate (Compound A). The present invention also provides processes for preparation of the anhydrous polymorphic forms of compound A.

Abstract: The present invention relates to a method for preparing metal nanostructures using DNA, and more particularly, to a method for preparing metal nanostructures, in which a self-assembling DNA is used as a frame, and thus the orientation, shape and size of the nanostructures are easily controlled compared to conventional bottom-up methods. Metal nanostructures prepared by the method show excellent localized surface plasmon resonance properties, and thus can be used as fluorescent substances in drug delivery, biomedical imaging, supersensitive biosensors, etc.

Abstract: Bile acids and related compositions and methods of synthesis and use. More specifically, deoxycholic acid and related compositions, said compositions being free of all moieties of animal origin and free of pyro-genic moieties.

Abstract: The present invention relates to a peptide-resin conjugate of Formula (2), wherein: Pr1 is selected from H, alkyl, aryl, aralkyl, acyl, aroyl and a protecting group; Y is a direct bond; or an optionally protected natural or unnatural amino acid residue; or a peptide comprising 2 to 200 natural or unnatural amino acid residues, each of which is optionally protected; Dia is a natural or unnatural diamino acid; A is a polymer resin conjugated to the side chain amino function of the diamino acid; X is an optionally protected natural or unnatural amino acid residue; or a peptide comprising 2 to 15 natural or unnatural amino acid residues, each of which is optionally protected; R1, and R2 are each independently selected from H, alkyl, aryl, aralkyl, NH2, NH—CO—NH2. Further aspects of the invention relate to a process of preparing peptide-resin conjugates of Formula (2), and their use in the preparation of peptides.

Abstract: Processes are provided for recovering and purifying refolded recombinant proteins produced in heterologous host cells, which includes the step of refolding the protein in a high pH buffer.

Abstract: The purpose of the present invention is to provide a pharmaceutical composition that is useful for the treatment of diseases that are caused by an increase in bone resorption and that does not cause serious side effects even when used in combination with another drug. The present invention relates to: an ?-oxoacyl aminocaprolactam derivative that is represented by formula (I) (in the formula, X is —O— or —N(R1)— and R1 represents an alkoxycarbonyl group having 1-10 carbon atoms); and a bone resorption inhibitor containing the ?-oxoacyl aminocaprolactam derivative.

Abstract: Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.

Abstract: The present invention refers to the development of a Peptide Nucleic Acid (PNA) probe for the detection and discrimination of Aspergillus fumigatus in different types of samples. PNA is a synthetic molecule analogue to DNA that, due to its physicochemical properties, allows a faster analysis with higher sensitivity than the DNA probes. These probes are combined with Fluorescence in situ hybridization (FISH), a molecular biology technique that allows the detection of Aspergillus fumigatus in diverse clinical samples, such as blood, serum, sputum, bronchoalveolar lavage fluid and biopsies. The combination of these two technologies rendered the FISH procedure faster, simpler and more efficient. The present invention also includes the development of the kit of detection and respective procedure for the Aspergillus fumigatus identification in clinical samples.

Abstract: Provided are a peptide that enables surface treatment of a scaffold for tissue repair that makes it possible to accelerate the repair of living tissue without using a material that negatively affects the repair of living tissue, a complex containing this peptide, a scaffold for tissue repair surface treated using this peptide or this complex, a surface treatment method for a scaffold for tissue repair using this peptide or this complex, and a treatment solution or set of treatment solutions to be used in this surface treatment method. Surface treatment of a scaffold for tissue repair is conducted by combining glycosaminoglycan and a peptide containing adhesive sites and basic sites each comprising predetermined amino acid residues.

Abstract: Provided are a hormone secretion modulator including a peptide derived from telomerase, more particularly, a peptide including an amino acid sequence of SEQ ID NO: 1, an amino acid sequence having a sequence identity of at least 80% with SEQ ID NO: 1, or a fragment thereof, a pharmaceutical composition including the hormone secretion modulator, and a use of the pharmaceutical composition for treatment, alleviation, or prevention of diseases caused by excessive or deficient levels hormones.

Abstract: The present disclosure provides compounds which are immunomodulators and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.

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: The present invention relates to a biosynthetic random coil polypeptide or a biosynthetic random coil polypeptide segment or biosynthetic conjugate, wherein said biosynthetic random coil polypeptide, said biosynthetic random coil polypeptide segment or said biosynthetic conjugate comprises an amino acid sequence consisting solely of proline and alanine amino acid residues, wherein said amino acid sequence consists of at least about 50 proline (Pro) and alanine (Ala) amino acid residues. Said at least about 50 proline (Pro) and alanine (Ala) amino acid residues may be (a) constituents) of a heterologous polypeptide or an heterologous polypeptide construct. Also uses and methods of use of these biosynthetic random coil polypeptides or polypeptide segments or said conjugates are described.

Abstract: The present invention is directed to a recombinant fusion antigen gene, a recombinant fusion antigen protein and a subunit vaccine composition having the same against infection of porcine reproductive and respiratory syndrome virus (PRRSV). A recombinant fusion antigen gene, which encodes glycoprotein GP5 with truncated N?-terminal decoy epitope, a linker sequence and membrane protein M, followed by codon optimization, is expressed by a baculovirus expression system in vitro, thereby enhancing a yield of the recombinant fusion antigen protein. The recombinant fusion antigen protein can be applied in a subunit vaccine composition, for providing vaccinated animals with better protection ability without the risks of virulent spread and virulent recovery.

Abstract: Provided in embodiments of the present invention is a vaccine composition including an immune amount of attenuated live vaccine, inactivated vaccine, subunit vaccine, synthetic peptide vaccine, or genetically engineered vaccine of the porcine pseudorabies virus strain. The vaccine composition can effectively induce antibody generation, and prevent infections of virulent strains of the porcine pseudorabies virus, and provides effective protection for pigs.

Abstract: The present invention relates to a secretagogue compound derived from oxalate degrading bacteria, for use in the treatment of an oxalate related disease and/or oxalate related imbalance in a subject, wherein the administration of the secretagogue results in a reduction of urinary oxalate and/or plasma oxalate in the subject. The invention further relates to a pharmaceutical composition comprising such a secretagogue compound, a method for treating a subject suffering from an oxalate related disease, and to a method for preparing a secretagogue.