Abstract: Disclosed are compounds of Formula (I): or a salt thereof, wherein: R1, R2, R3, R4, R5, and m are defined herein. Also disclosed are methods of using such compounds to inhibit the activity of one or both of diacylglycerol kinase alpha (DGK?) and diacylglycerol kinase zeta (DGK?), and pharmaceutical compositions comprising such compounds. These compounds are useful in the treatment of viral infections and proliferative disorders, such as cancer.

Abstract: This invention discloses the use of aza-tryptanthrin derivatives as an IDO1 and/or TDO inhibitors, and the derivatives are represented by the general Formula (I). The compounds represented by the Formula (I) have inhibitory effects on indoleamine-2,3-dioxygenase 1 (IDO1) and/or tryptophan-2,3-dioxygenase (TDO), and can be used for treating diseases having the pathological features of IDO1 and/or TDO-mediated tryptophan metabolism, including but not limited to tumors, autoimmune disease, infectious diseases, Alzheimer's disease, depression, anxiety.

Abstract: Disclosed are an azaphenalene-3-one derivative, its preparation method and its application, in the field of pharmaceutical synthesis. The derivative has the following Formula (I), wherein R is H, 2-fluoroethylamino, 2,2,2-trifluoroethylamino, diethylamino, pyrrolidinyl, imidazolyl, piperidinyl, morphinolinyl, 4-methylaminopiperidinyl, 4-dimethylaminopiperidinyl, (1-methylpiperidin-4-yl)methylamino, (1-phenylpiperidin-4-yl)methylamino, (1-benzylpiperidin-4-yl)methylamino, or 7-fluoro-3,4-dihydroisoquinoline-2(1H)-yl. The preparation method of the azaphenalene-3-one derivative is simple, the yield is high, post-treatment is easy, and purity is high. The derivative has high inhibitory activity against PARP enzyme. It establishes a foundation for researching better anti-tumor drugs using PARP inhibitors.

Abstract: The present invention relates to co-crystals of ibrutinib and a pharmaceutical composition comprising the same as well as a method of preparing the same.

Abstract: The present invention relates to compounds of formula I, wherein R1 is phenyl, lower alkyl, C3-6-cycloalkyl, —CH2—C3-6-cycloalkyl, or bridged C3-5-cycloalkyl, optionally substituted by one, two or three substituents, selected from halogen, lower alkyl or lower alkyl substituted by halogen; R2 is hydrogen, halogen, lower alkoxy, lower alkyl substituted by halogen or lower alkoxy substituted by halogen; R3 is a five membered heteroaryl group, selected from wherein R6 is hydrogen or lower alkyl; R7 is halogen or lower alkyl; R8 is hydrogen or lower alkyl; R9 is hydrogen or lower alkyl; R4 is lower alkyl or lower alkyl substituted by hydroxy; R5/R5? is independently from each other hydrogen or lower alkyl; -( )n- is —CH2— or —CH2CH2— for n being 1 or 2; X is CH or N; or to pharmaceutically active acid addition salts thereof, to racemic mixtures or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof.

Abstract: Described herein are compounds that inhibit ALK2 and its mutants, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.

Abstract: The invention relates to compounds which are suitable for the treatment of cancer, an immune disease, Parkinson's disease, Cardiac Hypertrophy or Type-2 diabetes and to pharmaceutical compositions containing such compounds. The invention further relates to a kit of parts comprising such compounds.

Abstract: The present invention is directed to compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein the substituents R1, R3, R6, R7, and b are as defined herein. The invention is also directed to pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, and methods of preparing the compounds.

Abstract: Described are coelenterazine analogues, methods for making the analogues, kits comprising the analogues, and methods of using the compounds for the detection of luminescence in luciferase-based assays.

Abstract: The present invention relates to a method for synthesizing a 3-phenyl-2,3,4,8,9,10-hexahydropyrano[2,3-f]chromene derivative and an optical isomer thereof, and an intermediate Compound which may be used for the synthesis method, and when the method and the intermediate Compound are used, the 3-phenyl-2,3,4,8,9,10-hexahydropyrano[2,3-f]chromene derivative and the optical isomer thereof may be effectively synthesized.

Abstract: A compound represented by the general formula (1) below or a pharmacologically acceptable salt thereof: [In the formula (1), R1 and R2 may be the same or different and each represents a hydrogen atom, a halogen atom, a hydroxyl group, a carboxy group, a cyano group, an optionally substituted C1-6 alkyl group et al.; R3 represents a hydrogen atom; R4 represents an optionally substituted 4- to 10-membered monocyclic heterocyclic group containing 1 to 4 heteroatoms selected from an oxygen atom, a nitrogen atom, and a sulfur atom; X represents a group represented by the following formula: —CH2—, —CH2—CH2—, —CH2—CH2—CH2—, or —CH2—O—CH2—; and Z represents a hydrogen atom or a hydroxyl group].

Abstract: The present invention relates to compounds of formulae I and H, or pharmaceutically acceptable salts or esters thereof. Further aspects of the invention relate to pharmaceutical compositions and therapeutic uses of said compounds in the treatment of diseases of uncontrolled cell growth, proliferation and/or survival, inappropriate cellular immune responses, inappropriate cellular inflammatory responses, or neurodegenerative disorders, preferably tauopathies, even more preferably, Alzheimer's disease.

Abstract: Compounds of formula (I) wherein R1, R2, A1 and A2 are as described herein, compositions including the compounds and methods of using the compounds as autotaxin inhibitors.

Abstract: A series of substituted fused pentacyclic benzimidazole derivatives, and analogues thereof, being potent modulators of human TNF? activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.

Abstract: Provided is a compound which is bioapplicable and amyloid-selective, and is useful as an amyloid oxygenation catalyst applicable not only to A? peptides but also to other amyloids, and a preventive/therapeutic drug for an amyloid-related disease using the same.

Abstract: The present invention relates to a complex comprising at least one lanthanide (Ln) and at least one compound (C) comprising a unit of formula (I) below: said unit of formula (I) being covalently connected to at least one antenna which absorbs at a wavelength ranging from 500 nm to 900 nm.

Abstract: Compounds of formula (I) are inhibitors of LMP7 and can be employed, inter alia, for the treatment of an autoimmune disorder or hematological malignancies.

Abstract: Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.

Abstract: This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.

Abstract: Disclosed herein are boronate intermediates in the synthesis of antimicrobial compounds and the use and preparation thereof. Some embodiments relate to crystalline boronate salt derivatives and their use in the synthesis of therapeutic compounds.

Abstract: The present invention relates to a process for preparing isocyanate containing alkoxysilane groups, in which, in the sequence of steps A) to D), A) alkoxysilanoalkylamine is reacted with urea in the presence of an alcohol, optionally in the presence of at least one catalyst, to give alkoxysilanoalkylurethane, B) simultaneously or successively, if used, the catalyst is removed and/or deactivated, and low boilers, medium boilers and/or high boilers are removed, C) purified alkoxysilanoalkylurethane is thermally cleaved to release isocyanate containing alkoxysilane groups and by-product, leaving bottoms material, and D) isocyanate containing alkoxysilane groups and by-product are separated from one another and from bottoms material and collected, in which, in step C), i) the bottoms material is wholly or partly discharged from the cleavage apparatus, ii) subjected to thermal treatment and/or purification and/or an aftertreatment in the presence of alcohol and iii) the material removed, after thermal treatment

Abstract: A new class of cyclotrisiloxanes having alkyl ether substituents on one, two, or three of the ring silicon atoms and a method for their preparation are provided. These compounds undergo living anionic ring-opening polymerization to generate unique polymer structures. A new class of hydridosilylethylcyclotrisiloxanes is also described.

Abstract: Preparation of O,O-dimethyl phosphoramidothioate and O,O-dimethyl phosphoroamidothioate. A process of making O,O-dimethyl phosphoroamidothioate is described including reacting sulfur with PCl3 to form PSCl3, reacting the PSCl3 formed with methanol to form O-methyl phosphorodichloridothioate, and reacting the O-methyl phosphorodichloridothioate formed with methyl lye to form O,O-dimethyl phosphorochloridothioate in solution in CH2Cl2, and reacting the O,O-dimethyl phosphorochloridothioate formed with sodium hydroxide and ammonium hydroxide to form O,O-dimethyl phosphoroamidothioate in solution in CH2Cl2. Reacting the O,O-dimethyl phosphoroamidothioate formed with catalytic dimethyl sulfate to form methamidophos, and reacting the methamidophos formed with acetic anhydride to form N-(methoxy-methylsulfanylphosphoryl) acetamide is also described. Throughout the process, the O,O-dimethyl phosphorochloridothioate and the O,O-dimethyl phosphoroamidothioate formed are maintained in solution in CH2Cl2 at all times.

Abstract: This invention features compounds that modulate the activity of liver X receptors, pharmaceutical compositions including the compounds of the invention, and methods of utilizing those compositions for modulating the activity of liver X receptors in the treatment of cancer.

Abstract: The present invention is in the field of processes for the generation of thin inorganic films on substrates, in particular atomic layer deposition processes. The present invention relates to a process comprising bringing a compound of general formula (I) into the gaseous or aerosol state and depositing the compound of general formula (I) from the gaseous or aerosol state onto a solid substrate, wherein M is Mn, Ni or Co, X is a ligand which coordinates M, n is 0, 1, or 2, R1, R2 are an alkyl group, an alkenyl group, an aryl group or a silyl group, m is 1, 2, or 3, R3, R4, and R5 are an alkyl group, an alkenyl group, an aryl group, an alkoxy group, or an aryloxy group, and p is 1, 2 or 3.

Abstract: The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula I: The invention also provides pharmaceutically acceptable compositions containing the compounds and methods of using the compositions in the treatment of bacteria infections. Finally, the invention provides processes for making compounds of the invention.

Abstract: Labeled nucleotide analogs comprising at least one avidin protein, at least one dye-labeled compound, and at least one nucleotide compound are provided. The analogs are useful in various fluorescence-based analytical methods, including the analysis of highly multiplexed optical reactions in large numbers at high densities, such as single molecule real time nucleic acid sequencing reactions. The analogs are detectable with high sensitivity at desirable wavelengths. They contain structural components that modulate the interactions of the analogs with DNA polymerase, thus decreasing photodamage and improving the kinetic and other properties of the analogs in sequencing reactions. Also provided are nucleotide and dye-labeled compounds of the subject analogs, as well as intermediates useful in the preparation of the compounds and analogs. Compositions comprising the compounds, methods of synthesis of the intermediates, compounds, and analogs, and mutant DNA polymerases are also provided.

Abstract: Disclosed are methods of separating the diastereoisomers of gemcitabine-[phenyl-(benzoxy-L-alaninyl)]-phosphate (NUC-1031), or salts thereof, using crystallisation. In particular, crystallisation from isopropyl alcohol provides gemcitabine-[phenyl-(benzoxy-L-alaninyl)]-(S)-phosphate in high diastereoisomeric purity: Also disclosed is a crystalline form of gemcitabine-[phenyl-(benzoxy-L-alaninyl)]-(S)-phosphate.

Abstract: Methods of preparing synthetic oligonucleotides containing at least one phosphotriester linkage conjugated to a monosaccharide are disclosed, where the synthetic oligonucleotides are prepared from nucleosidic phosphoramidite building blocks, preferably followed by removal of protecting groups to provide monosaccharide-conjugated oligonucleotides.

Abstract: Provided are a new crystal form of fludarabine phosphate, a preparation method therefor, a pharmaceutical composition containing same, and an application thereof in preparing medicine. Crystal forms I and II of the fludarabine phosphate have excellent properties in terms of solubleness, dissolution rate, chemical stability, and processing adaptability.

Abstract: The invention relates to double-stranded ribonucleic acid (dsRNA) compositions targeting the COL1A1, TGF-?, and SMAD2/3 genes, and methods of using such dsRNA compositions to inhibit expression of COL1A1, TGF-?, and SMAD2/3.

Abstract: Methods and devices are provided herein for surfaces for de novo nucleic acid synthesis which provide for low error rates. In addition, methods and devices are provided herein for increased nucleic acid mass yield resulting from de novo nucleic acid synthesis.

Abstract: The present invention relates to C-3 novel triterpenone with C-28 urea derivatives of formula (I); or pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable hydrates, tautomers, stereoisomers, prodrugs, compositions or combination thereof, wherein R1, R2, R3, W, J and X are as defined herein. The present invention also relates to pharmaceutical compositions comprising compounds of formula (I) useful for the treatment of viral diseases and particularly HIV mediated diseases.

Abstract: Solid supports for use in solid-phase peptide synthesis (SPPS) are provided. The solid supports may include a resin and a protected linker coupled to the resin. The linker may be an N-mercaptoethoxyglycine, an N-mercaptopropoxyglycine, an N-mercaptobutoxyglycine, and/or another suitable linker. Kits for use in SPPS are also provided. The kits may include a solid support, a solution including a thiol or a selenol, one or more pluralities of protected amino acids, and/or a wash buffer. Methods of SPPS are also provided. The methods may include providing a solid support including a resin coupled to a protected linker.

Abstract: The present invention relates to a device for separating and/or isolating substances in or from a mixture with improved utilization of the capacity of chromatographic media, the device comprising a first chromatography system, a second chromatography matrix downstream of the first chromatography system, and a sensor for detecting the substances present in the fluid. Furthermore, the present invention relates to both the use of said device and a method for separating and/or isolating substances in or from a mixture in a fluid.

Abstract: Provided is a method of treating a protein to be renatured, including: (1) mixing the protein to be renatured with a denaturing solution containing a denaturing reagent; (2) incubating a resulting mixture at such a low temperature that the denaturing agent is gradually precipitated from the denaturing solution, resulting in a decreasing concentration gradient of the denaturing agent and an increasing concentration of a renatured protein or its precursor in the denaturing solution with a decreasing volume; and (3) obtaining at least one of the renatured protein and its precursor.

Abstract: The present invention provides a method for extracting ?-polylysine (?-PL) and its hydrochloride salt from fermentation broth, which belongs to the field of bio-separation engineering. ?-PL and its hydrochloride salt are produced from fermentation broth through sequential solid-liquid separation, ultrafiltration, two-stage ion exchange, nanofiltration, evaporation concentration and drying techniques. Technologies of membrane filtration and two-stage ion exchange are applied to the preparation of ?-PL and its hydrochloride salt in the present invention, and the invention are characterized by reduced cost, improved automation, and increased product yield and purity, and the method of the present invention would be more suitable for industrial production.

Abstract: The present invention provides peptides containing a structure in which a portion of the dominant negative peptide of BIG3 which inhibits the interaction between BIG3 and PHB2 is substituted with stapling structure(s). Peptides of the present invention have excellent cell growth inhibitory actions. Furthermore, their cell growth inhibitory actions continue for a longer time than the actions of peptides without stapling structures. Therefore, these peptides have features suitable for clinical applications in cancer therapy.

Abstract: Disclosed are peptides and peptidomimetics that in some embodiments include the amino acid sequence KRGARST or (SEQ ID NO: 1), AKRGARSTA or (SEQ ID NO: 2), or CKRGARSTC (SEQ ID NO: 3).

Abstract: The peptide of the present invention performs a function, which is the same as or similar to that of natural interleukin (IL)-3, and has superior skin permeability due to the small size thereof. In addition, the peptide of the present invention suppresses the activation of NF-?B and nuclear transition by inhibiting the receptor activator of nuclear factor kappa-B ligand (RANKL)-RANK signaling pathway, and suppresses the expression of a RANKL or an inflammatory cytokine-induced tartrate-resistant acid phosphatase (TRAP), cathepsin K, or TNF receptor type 1 or type 2, thereby inhibiting osteoclast differentiation depending on the treatment concentration. Moreover, the peptide of the present invention can contribute to osteoblast differentiation by promoting the expression of osteoblast differentiation markers such as osteocalcin (OCN), osteoprotegerin (OPG), bone sialoprotein (BSP), or osteopontin (OPN).

Abstract: Provided herein is a multitarget-directed bio-inorganic hybrid structure. The hybrid structure is based on carbon nanotubes, and includes: carbon nanotubes; and two or more peptides bound to a surface of the carbon nanotubes and each independently interacting with different target molecules.

Abstract: The present disclosure relates to a class of engineered polypeptides having a binding affinity for interleukin-6, and provides an IL-6 binding polypeptide comprising the sequence EEX3X4AWX7EIH X11 LPNLX16X17X18QX20 X21AFIX25X26LX28X29. The present disclosure also relates to the use of such an IL-6 binding polypeptide as a therapeutic, prognostic and/or diagnostic agent.

Abstract: Provided herein are genetically modified arenaviruses suitable as vaccines against neoplastic diseases or cancer. The invention also relates to pharmaceutical compositions and methods for the prevention or treatment of certain infections causing neoplastic diseases or cancer, such as infections with oncogenic viruses. Specifically, provided herein are pharmaceutical compositions, vaccines, and methods of preventing or treating diseases and conditions caused by and associated with infections with Human Papillomavirus (HPV), such as cervical cancer, anogenital cancer, head and neck cancer and skin cancers. Also provided herein are immunotherapies for the treatment of a neoplastic disease, such as a neoplastic disease caused by infection with oncogenic viruses.

Abstract: The present invention relates to compositions comprising improved flagellin derived constructs and methods of using the same in the treatment of various diseases.

Abstract: Nucleotide sequences are disclosed that encode novel chimeric insecticidal proteins exhibiting Lepidopteran inhibitory activity. Particular embodiments provide compositions and transformed plants, plant parts, and seeds containing the recombinant nucleic acid molecules encoding one or more of the chimeric insecticidal proteins.

Abstract: The present invention relates to a process for conjugation of an antigen.

Abstract: New insecticidal proteins, nucleotides, peptides, their expression in plants, methods of producing the peptides, new processes, production techniques, new peptides, new formulations, and new organisms, a process which increases the insecticidal peptide production yield from yeast expression systems. The present invention is also related and discloses selected endotoxins we call cysteine rich insecticidal peptides (CRIPS) which are peptides derived from Bacillus thuringiensis (Bt) and their genes and endotoxins in combination with toxic peptides known as Inhibitor Cystine Knot (ICK) genes and peptides as well as with other types of insecticidal peptides such as trypsin modulating oostatic factor (TMOF) peptide sequences used in various formulations and combinations; of both genes and peptides, useful for the control of insects.

Abstract: Provided herein are compositions and methods for the treatment of cancer by activating the spindle assembly checkpoint (SAC) in cells. In particular, dimerized Mps1 and Spc105/KNL1 constructs are provided as tunable activators of SAC, allowing for control of chromosome segregation accuracy and prevention of aneuploidies that are common in cancer.

Abstract: A method is provided for capillary stabilization and vascular regeneration in retinal tissue. Capillary regeneration is accomplished with a protein that is a truncated norrin protein (synthetic). The truncated norrin protein has a longer half-life in the eye than native wild norrin proteins. Specific versions of the truncated norrin protein lack a cleavage site that an enzyme in the eye use to cleave to native norrin proteins and thereby shorten the useful life of the protein. The provided method encourages vascular development with an exogenous treatment of truncated norrin that have been investigated in oxygen-induced retinopathy (OIR) mice. The therapeutic feasibility of intravitreal injection of the norrin protein and its effect on retinal development by activating Wnt-signaling has also been shown.

Abstract: The present invention relates to cytokine fusion proteins and to nucleic acid molecules encoding such cytokine fusion proteins. The present invention further relates to cells, non-human organisms, pharmaceutical compositions and kits comprising the cytokine fusion proteins or the nucleic acid molecules encoding them, as well as to their use as medicaments.