Abstract: The present invention relates to compounds of formula (I): and to salts thereof, wherein R1, R2, and Q have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of bromodomains. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various bromodomain-mediated disorders.

Abstract: The present disclosure generally relates to compounds and pharmaceutical compositions which may be used in methods of treating a hepatitis B virus infection.

Abstract: The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4, R5 and Ar are as described herein, compositions including the compounds and methods of using the compounds.

Abstract: The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.

Abstract: The present invention provides compounds of Formula (Ia): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

Abstract: The invention relates to substituted 6-anilino-9-heterocyclylpurine derivatives of formula I wherein R denotes one to five substituents independently selected from the group hydrogen, halogen, hydroxy, amino, alkyloxy and alkyl group, R2 is selected from the group comprising amino, halogen, hydroxy, thio, and alkylthio group, Cyc is five- or six-membered heterocyclic ring containing one oxygen atom. The derivatives are useful for inhibition of plant stress.

Abstract: Hsp90 inhibitors havin are rovided havin the formula: (I) with a 2?,4?,5?-substitution pattern on the right-side aryl moiety. X1 represents two substituents, which may be the same or different, disposed in the 4? and 5? positions on the aryl group, wherein X1 is selected from halogen, alkyl, alkoxy, halogenated alkoxy, hydroxyalkyl, pyrollyl, optionally substituted aryloxy, alkylamino, dialkylamino, carbamyl, amido, alkylamido dialkylamido, acylamino, alkylsulfonylamido, trihalomethoxy, trihalocarbon, thioalkyl, SO2alkyl, COO alkyl, KH2, OH, CN, SO2X5, NO2, NO, C?SR2 NSO2X5, C?OR2, where X5 is F, NH2, alkyl or H, and R2 is alkyl, NH2, NH-alkyl or O-alkyl, C1 to C6 alkyl or alkoxy; or wherein X1 has the formula —O—(CH2)n—O—, wherein n is an integer from O to 2, preferably 1 or 2, and one of the oxygens is bonded at the 5?-position and the other at the 4?-position of the aryl ring. The compounds are useful in cancer therapy and as radioimaging ligands.

Abstract: Disclosed are compounds active towards nuclear receptors, pharmaceutical compositions containing the compounds and use of the compounds in therapy.

Abstract: The present invention relates to novel crystalline forms of 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-car boxylic acid dimethylamide(compound I), its salts, and process for preparation thereof. Crystalline forms in the present invention have good stability, low hygroscopicity, good processability, easy treatability and other favorable properties. In addition, the process is simple, low cost, and has an important value for future optimization and development of the drug.

Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I, or pharmaceutically acceptable salts thereof, Formula I or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula I in the treatment of Btk mediated disorders.

Abstract: Diazene-directed modular synthesis is described for the preparation Csp2-Csp3 and Csp3-Csp3 linkages where one or more stereogenic quaternary carbon centers are formed. The disclosed methods are directed to the preparation of compounds of Formula (I), or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, from compounds of Formula (II): wherein R1-R5 and q are as defined independently for each occurrence herein. A wide variety of compounds can be accessed in this manner, including oligocyclotryptamines, where the stereochemistry of each subunit is beneficially secured before fragment coupling.

Abstract: The present invention relates to compounds which may be useful as inhibitors of PTPN11 for the treatment or prevention of cancer and other PTP-mediated diseases. Disclosed herein are new compounds and compounds based on pyrazolopyrazines and their application as pharmaceuticals for the treatment of disease.

Abstract: Compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections are provided. The compounds and compositions are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.

Abstract: Provided herein are Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions, comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.

Abstract: Compounds of formula (I) that are capable of acting as purine receptor antagonists, pharmaceutical compositions including the compounds, and methods of making the compounds, are disclosed. The compounds and compositions can be used in treating or preventing disorders related to purine receptor hyperfunctioning.

Abstract: The present invention covers [8-(phenylsulfonyl)-3,8-diazabicyclo[3.2.1]oct-3-yl](1H-1,2,3-triazol-4-yl)methanone compounds of general formula (I): in which R1, R2, R3, R4 and R5 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of disorders, in particular of gynecological disorders, hyperproliferative disorders, metabolic disorders, or inflammatory disorders as a sole agent or in combination with other active ingredients.

Abstract: The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-c]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis), kits, methods of synthesis, and products-by-process.

Abstract: The disclosure relates to processes for reducing the amount of a compound of formula (I) or a salt or a solvate thereof present in a composition comprising compounds of formulae (I) and (II) or a salt or a solvate thereof.

Abstract: The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract: The disclosure provides compounds and methods for treating cancer by inhibiting the formation of cancer cells resistant to paclitaxel by preventing the formation of GBP1:PIM1 protein interaction during a chemotherapeutic treatment. These compounds and methods are able to treat cancer individually or in conjunction with paclitaxel.

Abstract: The present invention relates to bis-thienobenzothienothiophene compounds and a process for their preparation. More in particular, the present invention relates to a new angular bis-thienobenzothienothiophene compound and the process for its preparation wherein said process comprises reacting at least one dihalogenated dithiophene compound with at least one terminal alkyne and the subsequent double annulation reaction. Said bis-thienobenzothienothiophene compounds can be appropriately functionalized and polymerized to produce electron donor compounds that can be advantageously used in the construction of photovoltaic devices or semiconductor polymers. Furthermore, said bis-thienobenzothienothiophene compounds, after functionalization, may be advantageously used as spectral converters in luminescent solar concentrators.

Abstract: In certain aspects, the invention provides a method for treating a disease or condition in a subject, the method comprising co-administering to a subject in need thereof a therapeutically effective amount of at least one ULK1-inhibiting pyrimidine, and a therapeutically effective amount of an mTOR inhibitor.

Abstract: The present invention relates to novel compounds of formula (A) and (B) as modulators of GPR-119, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of GPR-119 mediated diseases or disorders with them.

Abstract: The present invention relates to a water-soluble, simple, stable tris(N-(tert-butyl)acetamide) cyclen-based europium complex HGEu001 which exhibits the specific subcellular localization in the primary cilium with a quantum yield as high as 10% in water and a lifetime of 0.56 ms lifetime. In particular, the present invention provides simplicity of the design and synthesis of a complex. Comprehensive studies were performed in numerous cell lines, such as HeLa, SN-K-SH and MRC5; the motif structure, HGEu002, has also been synthesized as the negative control for in vitro imaging studies. The two photon in vitro imaging were done in three dimensions to emphasize on the specific localization in primary cilium of HGEu001. This is one of the very limited examples for direct primary cilium imaging.

Abstract: To provide a near-infrared absorption composition which contains a squarylium compound having excellent solvent solubility, a cured film which uses the near-infrared absorption composition, a near-infrared cut filter, a solid-state imaging device, an infrared sensor, and a compound. A near-infrared absorption composition includes a compound represented by the following Formula (1) and a resin. R1 and R2 each independently represent “—S1-L1-T1” or the like, R3 and R4 each independently represent a hydrogen atom or an alkyl group, X1 and X2 each independently represent an oxygen atom or —N(R5)—, R5 represents a hydrogen atom or the like, Y1 to Y4 each independently represent a substituent, p and s each independently represent an integer of 0 to 3, and q and r each independently represent an integer of 0 to 2; and S1 represents an arylene group or the like, L1 represents an alkylene group or the like, and T1 represents an alkyl group or the like.

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: 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: The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of inflammatory diseases and other diseases involving elevated levels of cytokines and proinflammatory mediators.

Abstract: Organofunctional silicon particles are covalently functionalized on their surface with at least one organic compound, for example a plurality of —O—(C1-C48)-alkyl compounds. The functionalization of the surface of the silicon particles makes it possible to adjust the properties of fluids in terms of their profile of properties by addition of the modified silicon particles. For instance, the alkoxy-functionalized silicon particles may preferably be added to a motor oil as additives for reducing viscosity.

Abstract: A silicone oil having a mean molecular weight average greater than about 20,000 Daltons, with no more than about 3% to about 4% of the total silicone oil by weight being comprised of components having a molecular weight less than about 15,000 Daltons. In some embodiments, the silicone oil is used in intraocular lens devices.

Abstract: The present disclosure is directed to novel methods of treating type-1 or type-2 diabetes by inactivating TLR2 and TLR4 genes together in cells capable of producing insulin and/or regenerating ? cells, and providing the cells to a subject in need thereof.

Abstract: Iridium (III) complexes are described together with methods to prepare and use such complexes. Also described are devices that utilize the iridium (III) complexes.

Abstract: Disclosed herein are catalyst compositions containing bicyclic bridged metallocene compounds. These catalyst compositions can be used for the polymerization of olefins. For example, ethylene polymers produced using these catalyst compositions can be characterized by low molecular weights and high melt flow rates, and can be produced without the addition of hydrogen.

Abstract: The present invention relates to processes for the preparation of ertugliflozni. The present invention also provides compounds of Formula (III), Formula (IV), and Formula (VII), processes for their preparation, and their use for the preparation of ertugliflozin. The processes of the present invention involve protecting the ertugliflozin intermediate compound with a suitable protecting group which provides ertugliflozin having high purity and yield.

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 pyrogenic moieties.

Abstract: Described herein are neuroactive steroids of the Formula (II): or a pharmaceutically acceptable salt thereof; wherein A, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5, R6 and are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment, e.g., such for inducing sedation and/or anesthesia.

Abstract: Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (I) and (III): where R1, R2, R3, R3?, R4, R6a, R6a, R11a, and R11b are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, insomnia, anxiety, depression, traumatic brain injury (TBI), stress, and epilepsy.

Abstract: An improved method for coupling amino acids into peptides or peptidomimetics is disclosed that includes the steps of combining an amino acid, a carbodiimide, an activator additive, and a base at less than 1 equivalent compared to the amino acid to be activated; and carrying out the activation and coupling at a temperature greater than 30° C.

Abstract: The present invention provides a novel method for manufacturing a protein, particularly where said protein is to be coupled with another molecule. The invention further provides a method for industrial scale protein manufacturing to obtain proteins, e.g., for therapeutic purposes.

Abstract: Provided is a method for making the compound of Formula 1. Various compounds utilized in that method are also provided, as are methods of making those compounds. Also provided is a compound having the formula XO—CO—(CH2)nNH2, where n is an integer greater than 2. A method of making that compound is additionally provided. Further provided is a method of making a prodrug of a bioactive compound.

Abstract: Certain embodiments of the invention provide a compound of formula (I): R1—C(?O)—W—X—Y—Z—N(R2)2 ??(I) or a salt thereof, wherein R1, R2, W, X, Y and Z are as defined herein, as well as methods of use thereof.

Abstract: The present invention relates to a stapled peptide, a preparation method thereof and the use thereof, and more specifically to an amphipathic alpha-helical stapled peptide comprising hydrophobic amino acids and hydrophilic amino acids, a preparation method thereof, and the use thereof for intracellular delivery of an active substance.

Abstract: The invention provides natural IgM antibody inhibitors that may be used to treat various inflammatory diseases or disorders.

Abstract: The present disclosure provides a compound of Formula I or its stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. The present disclosure also relates to process of preparation of vancomycin-sugar conjugates of Formula I, its stereoisomers, prodrugs, pharmaceutically acceptable salts thereof, and to pharmaceutical compositions containing them. The compounds of the present disclosure are useful in the treatment, prevention or suppression of diseases mediated by microbes.

Abstract: The invention relates to isolated antibodies that bind to specific peptides and to their use in the diagnosis of celiac disease.

Abstract: The invention encompasses components from microbial cells which are useful for antibody production, including peptides, polypeptides comprising these peptides, polynucleotides which encode these peptides or polypeptides, and antibodies directed to these peptides, polypeptides, or polynucleotides. The invention also encompasses to expression vectors and host cells for producing these peptides, polypeptides, polynucleotides, and antibodies. The invention further encompasses methods and compositions, especially vaccine compositions, for detecting, targeting, and inhibiting microbial cells, especially methanogen cells, using one or more of the disclosed peptides, polypeptides, polynucleotides, antibodies, expression vectors, and host cells.

Abstract: A recombinant H7 hemagglutinin derived from Chinese hamster ovary (CHO) cell. The recombinant H7 hemagglutinin includes a H7 hemagglutinin domain, a GCN4-pII trimerization motif, and a His-tag. The recombinant H7 hemagglutinin can be prepared as a protective vaccine composition with a pharmaceutically acceptable adjuvant. H7 hemagglutinin specific antibodies are elicited, and protection against H7N9 influenza virus is provided.

Abstract: The present invention relates to an RhtB (homoserine/homoserine lactone export transporter) protein variant having an enhanced ability to export O-phosphoserine (OPS) that is a precursor of L-cysteine, a polynucleotide encoding the protein, a vector comprising the polynucleotide, an OPS-producing microorganism comprising the protein variant, a method of producing O-phosphoserine using the microorganism, and a method for preparing cysteine or its derivatives, which comprises reacting O-phosphoserine, produced by the method above, with a sulfide in the presence of O-phosphoserine sulfhydrylase (OPSS) or a microorganism that expresses OPSS.

Abstract: The present invention relates to an RhtB (homoserine/homoserine lactone export transporter) protein variant having an enhanced ability to export O-phosphoserine (OPS) that is a precursor of L-cysteine, a polynucleotide encoding the protein, a vector comprising the polynucleotide, an OPS-producing microorganism comprising the protein variant, a method of producing O-phosphoserine using the microorganism, and a method for preparing cysteine or its derivatives, which comprises reacting O-phosphoserine, produced by the method above, with a sulfide in the presence of O-phosphoserine sulfhydrylase (OPSS) or a microorganism that expresses OPSS.

Abstract: A system, including methods and compositions, for treatment of ischemia.