Abstract: The present invention provides a pharmaceutical composition, as an effective ingredient, a urea compound having a protein kinase inhibitory activity and containing a 3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one skeleton, and a pharmaceutically acceptable salt thereof.

Abstract: The present disclosure relates to stimulators of soluble guanylate cyclase (sGC), pharmaceutical formulations comprising them and their uses thereof, alone or in combination with one or more additional agents, for treating various diseases, wherein an increase in the concentration of nitric oxide (NO) or an increase in the concentration of cyclic Guanosine Monophosphate (cGMP), or both, or an upregulation of the NO pathway is desirable.

Abstract: Novel compounds of Formula I methods of manufacturing the compounds and their use in therapeutic treatments are presented.

Abstract: The present invention is directed to processes for preparing beta 3 agonists of Formula (I) and Formula (II) and their intermediates. The beta 3 agonists are useful in the treatment of certain disorders, including overactive bladder, urinary incontinence, and urinary urgency.

Abstract: The present invention provides compounds useful as inhibitors of Btk, compositions thereof, and methods of using the same.

Abstract: The presently described technology provides compositions comprising aryl carboxylic acids and, for example NSAIDs, chemically conjugated to oxycodone (4,5-?-epoxy-14-hydroxy-17-methylmorphinan-6-one) to form novel prodrugs/compositions of oxycodone, including benzoates, salicylates, propionates, fenamates, and acetates, which have a decreased potential for abuse of oxycodone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

Abstract: In one aspect, the present disclosure provides new analogs of uncialamycin. The present disclosure also provides novel synthetic pathways to obtaining uncialamycin and analogs thereof. Additionally, the present disclosure also describes methods of use of uncialamycin and analogs thereof. In another aspect, the present disclosure provides antibody-drug conjugates which may be used to treat cancer or another disease or disorder.

Abstract: Described herein are crystalline forms of Compound 1 useful for the prevention and treatment of angiogenic ocular conditions; methods of treating a disease comprising; processes for preparing; and kits comprising, the same.

Abstract: Described herein are crystalline forms of Compound 1 useful for the prevention and treatment of angiogenic ocular conditions; methods of treating a disease comprising; processes for preparing; and kits comprising, the same.

Abstract: Described herein are crystalline forms of Compound 1 useful for the prevention and treatment of angiogenic ocular conditions; methods of treating a disease comprising; processes for preparing; and kits comprising, the same.

Abstract: Disclosed herein are cyanated compounds of the formula (I) wherein at least one of the radicals R2, R3, R4 and R5 is CN, and the remaining radicals are selected from hydrogen, chlorine and bromine; X is O, S, SO or SO2; m is 0, 1, 2, 3 or 4; 10 is selected from bromine, chlorine, cyano, —NRaRb, C1-C24-alkyl, C1-C24-haloalkyl, C1-C24-alkoxy, C1-C24-haloalkoxy, C3-C24-cycloalkyl, heterocycloalkyl, heteroaryl, C6-C24-aryl, C6-C24-aryloxy, C6-C24-aryl-C1-C10-alkylene, etc.; A is a diradical selected from diradicals of the general formulae (A.1), (A.2), (A.3), and (A.4) wherein R6, (R7)n, (R8)o and (R9)p are as defined in the claims and in the description. Also disclosed are color converters containing at least one polymer as a matrix material and at least one cyanated compound of formula (I) or mixtures thereof as a fluorescent dye, the use of the color converters, and lighting devices containing an LED and at least one color converter.

Abstract: The present application relates to novel thieno[2,3-d]pyrimidine-2,4-dione (“thienouracil”) derivatives bearing a particular type of (azaheterocyclyl)methyl substituent, to processes for the preparation thereof, to the use thereof alone or in combinations for treatment and/or prevention of diseases and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially for treatment and/or prevention of pulmonary and cardiovascular disorders and of cancer.

Abstract: The present invention relates to compounds which are inhibitors of non-apoptotic regulated cell death, and to pharmaceutical compositions containing such compounds. Furthermore, the present invention relates to the use of such compounds and pharmaceutical compositions in therapy, in particular in the treatment of a condition, disorder or disease that is characterised by non-apoptotic regulated cell-death or where non-apoptotic regulated cell-death is likely to play or plays a substantial role.

Abstract: Described herein are tricyclic compounds with phosphoinositide-3 kinase (PI3K) modulation activity or function having the Formula I structure: or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such PI3K modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon PI3K dysregulation.

Abstract: The present invention relates to a process for synthesis of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol abbreviated THIP, having the INN name gaboxadol, starting from pyrrolidin-2-one. The process comprises a new direct process to obtain the intermediate dimethyl 5-hydroxy-3,6-dihydropyridine-1,4(2H)-5 dicarboxylate or the intermediate diethyl 5-hydroxy-3,6-dihydropyridine-1,4(2H)-dicarboxylate.

Abstract: The present invention is directed to a process for making Tetracyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein X1, X2, R1, R2 and R3 are defined above herein. The present invention is also directed to compounds that may be useful as synthetic intermediates in the process of the invention.

Abstract: The present invention relates to sodium (2R,5S,13aR)-7,9-dioxo-10-((2,4,6-trifluorobenzyl)carbamoyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1?,2?:4,5]pyrazino[2,1-b][1,3]oxazepin-8-olate Form I.

Abstract: Crystalline polymorphous forms of rifaximin (INN) antibiotic named rifaximin cc and rifaximin ?, and a poorly crystalline form named rifaximin ?, useful in the production of medicinal preparations containing rifaximin for oral and topical use and obtained by means of a crystallization carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a determinate temperature and for a determinate period of time, followed by a drying carried out under controlled conditions until reaching a settled water content in the end product, are the object of the invention.

Abstract: Crystalline polymorphous forms of rifaximin (INN), referred to as rifaximin ? and rifaximin ?, and a poorly crystalline form referred to as rifaximin ?, useful in the production of medicaments containing rifaximin for oral and topical use and obtained by means of a crystallization process carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a fixed temperature and for a fixed period of time, followed by a drying under controlled conditions until reaching a precise water content in the end product, are the object of the invention.

Abstract: Broad spectrum beta-lactamase inhibitors. Certain inhibitors also exhibit potent antibiotic activity in addition to beta-lactamase inhibition. Compounds of the invention are designed such that on cleavage of the beta-lactam ring reactive moieties are generated which can inactivate beta-lactamase. Also provided are methods of making beta-lactamase inhibitors and beta-lactam antibiotics exhibiting such inhibition. Additionally provided are pharmaceutical compositions for treatment or prevention of bacterial infections and methods of treatment of such infections.

Abstract: The present invention provides a new process for the preparation of a substituted imidazothiazolone compound. The process of the present invention uses a fluoride-free Lewis acid which is cheap and friendly to environment, and provide high selectivity and yield.

Abstract: The present invention relates to compounds of formula (I), wherein R1, R2 and R3 are as described herein, and their prodrugs or pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.

Abstract: Monomeric bimetal hydroxycitric acid (HCA) compounds are provided. The subject compounds include a divalent metal (X) bonded to the carboxylic acids of C2 and C3 and a monovalent metal (Y) bonded to the carboxylic acid of C1. Also provided are methods of preparing the subject compounds from a dimeric starting material (e.g., X3(HCA)2) which include acidifying the dimer to produce a monomeric intermediate which is subsequently neutralized with YOH base. Methods of alleviating at least one symptom associated with a target disease or condition in a subject are provided. Also provided are compositions including the subject monomeric bimetal HCA compounds which find use in a variety of therapeutic applications.

Abstract: A reaction method comprising combining a carbonyl-substituted arylboronic acid or ester and an ?-effect amine in aqueous solution at a temperature between about ?5 C to 55 C, and a pH between 2 and 8 to produce an adduct. A process is also provided comprising: contacting a boron compound having a boron atom bonded to a sp2 hybridized carbon conjugated with a cis-carbonyl, the boron having at least one labile substituent, with an ?-effect amine, in a solvent for a time sufficient to form an adduct, which may proceed to further products.

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: Nanocomposite silicon and carbon compositions. These compositions can be made from polymer derived ceramics, and in particular, polysilocarb precursors. The nanocomposite can have non-voids or be nano-void free and can form larger macro-structures and macro-composite structures. The nanocomposite can contain free carbon domains in an amorphous SiOC matrix.

Abstract: The invention relates to [bis(trihydrocarbylsilyl)aminosilyl]-functionalized styrene and a method for its preparation. The invention further relates to the use of the styrene derivative in the preparation of a copolymer thereof.

Abstract: An electrolyte for a lithium secondary battery, the electrolyte including: a compound represented by Formula 1; a lithium salt; and an organic solvent, wherein an amount of the compound represented by Formula 1 is less than about 3.0 weight percent, based on a total weight of the electrolyte: wherein, in Formula 1, R1 to R15 are each independently selected from hydrogen, fluorine, a C1-C10 alkyl group, and a C6-C10 aryl group.

Abstract: Compounds useful as fluorescent or colored dyes are disclosed. The compounds have the following structure (I): or a stereoisomer, tautomer or salt thereof, wherein R1, R2, R3, R4, R5, L1, L3, L4, L6, L7, L8, M1, M2, q, w and n are as defined herein. Methods associated with preparation and use of such compounds are also provided.

Abstract: Compounds of Formula I: and their pharmaceutically acceptable salts are useful for the inhibition of HIV reverse transcriptase. The compounds may also be useful for the prophylaxis or treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antiviral agents, immunomodulators, antibiotics or vaccines.

Abstract: The present invention relates to metal complexes having a metal atom of groups 13 to 15 and at least one ligand, where the ligand comprises at least one anionic coordination group having at least one oxygen and/or nitrogen atom via which the metal atom is coordinated, and the ligand comprises at least one triarylamine group, to processes for preparation thereof and to the use thereof in electronic devices, especially in organic electroluminescent devices, called OLEDs (OLED=organic light emitting diode). The present invention also further relates to organic electroluminescent devices comprising these metal complexes.

Abstract: A novel iridium complex which can be applied in an organic electroluminescent light emitting device, an organic electrochemical light emitting device, or the like, and which is thermally stable and has excellent sublimabilities. An iridium complex characterized by being represented by General Formula (1) (in General Formula (1), R1 to R11 and R13, R14, and R18 represent a hydrogen atom, an alkyl group with 1 to 30 carbon atoms, an aryl group with 6 to 30 carbon atoms, a halogen atom, or a cyano group; R12, R15 to R17 and R19 represent a hydrogen atom, an alkyl group with 1 to 30 carbon atoms, a halogen atom, or a cyano group; the alkyl group may be substituted with an aryl group, a halogen atom, or a cyano group; the aryl group may be substituted with an alkyl group, a halogen atom, or a cyano group; adjacent R12 to R19 may bind to each other to form a condensed ring; and m is an integer of 1 or 2, n is an integer of 1 or 2, and m+n is 3).

Abstract: Organometallic compounds and organic electroluminescence devices employing the same are provided. The organometallic compound has a chemical structure represented below: In Formula (I), one of R1 and R2 is trimethylsilyl (TMS) and the other is hydrogen, at least one of R3 and R4 is fluorine or C1-6 alkyl, or one of R3 and R4 is fluorine and the other is C1-6 alkyl, n is 2 or 3, and m is 0 or 1, wherein n+m=3.

Abstract: A process for the hydrogenation of a substrate comprising a carbon heteroatom double bond in the presence of a transition metal complex comprising a tridentate or bisdentate-ligand containing a nitrogen, sulphur and phosphorus atom, of which at least the N- and P- and optionally also the S-atom coordinates with the transition metal.

Abstract: Pt(IV) compounds include a mitochondria targeting moiety. One example of a Pt(IV) compound having a mitochondria targeting moiety is a Pt(IV) cisplatin-based compound. Upon reduction, the mitochondrial targeting moieties are released resulting in a Pt(II) therapeutic agent. Pt(IV) compounds including a mitochondria targeting moiety can be included in nanoparticles. The compounds or nanoparticles can be used to treat, for example, cancer.

Abstract: An object of the present invention is to provide a trans-resveratrol derivative that resists isomerization to the cis-form. Another object of the present invention is to provide a trans-resveratrol derivative that has no toxicity against cells and has sufficient antioxidative properties and/or a sufficient whitening effect. This object can be achieved by a method for producing a trans-resveratrol polysaccharide, the method comprising the step of bringing a trans-resveratrol glucoside into contact with sugar in the presence of ?-cyclodextrin glucanotransferase.

Abstract: Methods and compositions using E-selectin antagonists are provided for the treatment and prevention of diseases and disorders treatable by inhibiting binding of E-selectin to an E-selectin ligand. Described herein are E-selectin antagonists including, for example, glycomimetic compounds, antibodies, aptamers and peptides that are useful in methods for treatment of cancers, and treatment and prevention of metastasis, inhibiting infiltration of the cancer cells into bone marrow, reducing or inhibiting adhesion of the cancer cells to endothelial cells including cells in bone marrow, and inhibiting thrombus formation.

Abstract: The present invention provides macrocyclic compounds useful as therapeutic agents of the formula: or a pharmaceutically acceptable salt, ester, N-oxide, or prodrug thereof, wherein T, R1, R2, R3, D, E, F, and G are as defined herein. More particularly, these compounds are useful as anti-infective, antiproliferative, anti-inflammatory and prokinetic agents.

Abstract: Provided herein are macrolide compounds of Formula (I) and (I-N) for the treatment of infectious diseases and inflammatory conditions. The 14-membered ketolides and 14-, 15-, and 16-membered azaketolides described herein comprise modified sugars which are desosamine or mycaminose analogs. Pharmaceutical compositions and methods of treating infection diseases and inflammatory conditions using the inventive macrolides are also provided. This disclosure additionally provides methods of preparing the macrolides by the coupling of an eastern and western half.

Abstract: The present invention is directed to n-alkylated synthetic nucleosides of high regiospecific purity and oligonucleotides that can be utilized for studies on reversal of cytotoxic and mutagenic DNA damage, and as diagnostic tools.

Abstract: Anti-inflammatory and antiallergic compounds of the glucocorticosteroid series, according to formula (I) according to formula (I) defined herein are useful for treating diseases of the respiratory tract characterized by airway obstruction.

Abstract: A method for producing a site-specifically modified protein based on new carbon-carbon bond formation is disclosed, including the following three steps (marking, activation, and coupling steps): (a) marking of the modification site by incorporating a specific amino acid into a selected position of a target protein; (b) activation of the marked site; and (c) coupling of various post-translational modification (PTM) moieties or other chemical groups onto the activated site to obtain a site-specifically modified protein. The method for producing a site-specifically modified protein can incorporate desired diverse chemical groups including post-translational modification (PTM) moieties into a designated site in a target protein through a new carbon-carbon bond. Furthermore, the modified protein having a site-specific PTM exhibits the same chemical and functional properties as that of a target protein present in cells.

Abstract: Systems and processes for performing solid phase peptide synthesis are generally described. Solid phase peptide synthesis is a known process in which amino acid residues are added to peptides that have been immobilized on a solid support. In certain embodiments, the inventive systems and methods can be used to perform solid phase peptide synthesis quickly while maintaining high yields. Certain embodiments relate to processes and systems that may be used to heat, transport, and/or mix reagents in ways that reduce the amount of time required to perform solid phase peptide synthesis.

Abstract: An improved method of coupling amino acids into peptides or peptidomimetics is disclosed in which the activation and coupling are carried out in the same vessel, in the presence of a carbodiimide in an amount greater than 1 equivalent as compared to the amino acid, in the presence of an activator additive, and at a temperature greater than 30° C.

Abstract: In accordance with the present subject matter there is provided peptide-based compounds. methods of making such compounds, gels comprising such compounds, methods of making gels, methods of using such compounds for the containing spill of a hydrocarbon, and methods for reclaiming solvent from gels comprising such compounds.

Abstract: The present invention generally relates to compounds that are useful for inhibiting one or more of hepatocyte growth factor activator, matriptase, hepsin, Factor Xa, or thrombin. The present invention also relates to various methods of using the inhibitor compounds including treating a malignancy, a pre-malignant condition, or cancer by administering an effective amount of the inhibitor to a subject in need thereof.

Abstract: Short tri- and tetrapeptides according to the following Formula I Ar(CH2)mX1—X2—CO—X3—X4—X5-(Trp)n-NX6R are potent, selective agonists of melanocortin 1 receptor (MC1R). Provided herein are pharmaceutical compositions including Formula I peptide agonists of MC1R and methods of treating skin diseases and disorders that include administering to an individual in need thereof a therapeutic amount of a Formula I peptide. The peptides, pharmaceutical compositions, and methods described herein are useful in the treatment of diseases and disorders that benefit from agonism of MC1R, including melanoma, basal cell carcinoma, squamous cell carcinoma, porphyria, polymorphous light eruption, vitiligo, and solar urticaria.

Abstract: A set of phosphorylated peptides are presented by HLA A*0101, A*0201, A*0301, B*4402, B*2705, B*1402, and B*0702 on the surface of melanoma cells. They have the potential to (a) stimulate an immune response to the cancer, (b) to function as immunotherapeutics in adoptive T-cell therapy or as a vaccine, (c) to facilitate antibody recognition of the tumor boundaries in surgical pathology samples, and (d) act as biomarkers for early detection of the disease. Phosphorylated peptides are also presented for other cancers.

Abstract: Conformationally-stable peptide analogs of the response selective C5a agonist EP67 having the formula Tyr-Ser-Phe-Lys-Asp-Met-Xaa-(Xaa2)-(D-Ala)-Arg (SEQ ID NO:1), wherein Xaa is a modified proline residue or a residue substitution for proline, and Xaa2 is leucine or N-methyl leucine. The conformationally-stable peptides selectively bind and activate APCs without directly engaging/binding C5a receptor-bearing cells involved in pro-inflammatory activities of natural C5a. Compositions and methods of using the peptide analogs are also described.

Abstract: A scorpion venom heat-resistant synthetic peptide (SVHRSP) contains an amino acid sequence of SEQ ID NO 1. One or more amino acids the amino acid sequence can be substituted or deleted. A pharmaceutical composition that contains the SVHRSP has numerous applications. The pharmaceutical composition can be used to protect neuronal cell against amyloid beta-induced toxic effects, or to inhibit the sodium channel current of a hippocampal neuronal cell, or to protect a neuronal cell against NMDA-induced injury. It may also promotes the formation of a pluripotent neural stem cell from a type II astrocyte, or treats a subject, such as a human, having epilepsy, Alzheimer's disease, or Parkinson's disease.