Abstract: Compounds having a structure according to formula (I) or (II) where R1, R2, R3, R4, Ar and X1 are as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.

Abstract: Methods to produce substantially closed cell foams with densities less than 0.75 g/cm3, and more preferably less than 0.5 g/cm3, without substantial loss of the polymer's weight average molecular weight, have been developed. The closed cells foams have an open cell content of generally less than 50%, and more preferably an open cell content of less than 20%, and the cells have a maximum diameter of less than 5 mm. The foam may include poly-4-hydroxybutyrate or a copolymer thereof. Preferably, the foam is derived by heating a foam polymer formula to a temperature above the melt temperature of the polymer to form a melt polymer system, adding a blowing agent to produce a foamable melt, extruding the foamable melt through a die to a lower pressure to cause foaming, cooling of the foam, and solidification of the foam. These foam structures can be used for fabrication of medical products.

Abstract: Described is a composition comprising (a) a population of particles of an aripiprazole prodrug having a volume based particle size (Dv50) of less than 1000 nm and (b) at least one surface stabilizer comprising an adsorbed component which is adsorbed on the surface of the aripiprazole prodrug particles and a free component available for solubilisation of the aripiprazole prodrug. The surface stabilizer to prodrug ratio provides the optimal quantity of free surface stabilizer for the purposes of producing a lead-in formulation. Also described are methods of treatment using the aforementioned composition.

Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, ester, stereoisomer, tautomer, solvate, hydrate, or combination thereof: which inhibit the Apoptosis signal-regulating kinase 1 (ASK-1), which associated with autoimmune disorders, neurodegenerative disorders, inflammatory diseases, chronic kidney disease, cardiovascular disease. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from ASK-1 related disease. The invention also relates to methods of treating an ASK-1 related disease in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention specifically relates to methods of treating ASK-1 associated with hepatic steatosis, including non-alcoholic fatty liver disease (NAFLD) and non-alcohol steatohepatitis disease (NASH).

Abstract: The present invention relates to novel compounds or pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions and treatment methods or uses as antibacterials for bacterial infections.

Abstract: The present invention relates generally to therapeutics targeting the bacterium Porphyromonas gingivalis, including its protease Lysine gingipain (Kgp), and their use for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I, as described herein, and pharmaceutically acceptable salts thereof.

Abstract: The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein A, L, D, R1-R15, w, x, y, and z are defined herein. The novel cycloalkyl-linked diheterocycle derivatives that are useful in the treatment of abnormal cell growth, such as cancer, in mammals. The present invention also relates to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.

Abstract: 2-(5-{1-[2-(Difluoromethoxy)-6-fluorobenzyl]-2-methyl-1H-benzimidazol-6-yl}pyrimidin-2-yl)propan-2-ol, or a pharmaceutically acceptable salt 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: The present invention provides compounds of Formula (I): wherein all variables are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are APJ agonists which may be used as medicaments, in particular for treating cardiovascular disorders.

Abstract: The present invention relates to novel anthracycline derivatives comprising two oxazolidine cycles and the preparation of said anthracycline derivatives. Furthermore, antibody-drug conjugates (ADCs) comprising the novel anthracycline derivatives and the use of such ADCs in the prevention and treatment of cancer are disclosed.

Abstract: A one-pot synthesis for preparing an aqueous reactive black mixture includes a) dissolving 2-[(4-aminophenyl)sulfonyl]ethanesulfonic acid (vinyl sulphone parabase ester) in water; b) diazotizing the dissolved vinyl sulphone parabase ester using excess nitrous acid or using excess nitrite and an acid, resulting in a diazonium salt and remaining nitrous acid; c) quenching the remaining nitrous acid with sulfamic acid; d) coupling the diazonium salt of step c) with 4-amino-5-hydroxy-2,7-naphthalenedisulfonic acid (H-acid) until the reaction is complete, resulting in Reactive Black 5 (RB 5) and remaining diazonium salt, e) coupling the remaining diazonium salt with 7-acetamido-4-hydroxy-2-naphthalenesulfonic acid (acetyl-J-acid) until the reaction is complete resulting in Reactive Orange 78 (RO 78); and f) obtaining the aqueous reactive black mixture.

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: 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 the formula (I): wherein the substituents are as defined in claim 1, useful as pesticides, and especially fungicides.

Abstract: The invention provides 1,4-dihydropyridine derivatives of formula (I) wherein R1 is optionally substituted C6-24aryl group or 5 to 6 membered heteroaryl group comprising 1 to 3 nitrogen atoms or other heteroatoms like oxygen and sulphur, and combinations thereof; R2 and R3 are independently hydrogen or C1-6alkyl group; R4 and R5 are independently hydrogen, C1-6alkyl group optionally substituted with amino, mono- or di(C1-6alkyl)amino, or with 5 to 24 membered optionally fused heterocyclic ring attached by nitrogen and optionally comprising additional 1 to 3 N, O, S heteroatoms and optionally substituted with C1-6alkyl group or C1-6 alkoxy group; R6 is C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-6alkyl or arylC1-6alkyl group; and stereoisomers including enantiomers, diastereomers, racemic mixtures, mixture of enantiomers and combination thereof, as well as polymorphs, pharmaceutically acceptable salts, solvates, esters and prodrugs thereof for use in the therapeutic or prophylactic treatment of a disorder medi

Abstract: Thin molecules, compounds producible by cleaving bilirubin at its methylene site in the center of the molecule, methods of making the same, and methods of using the same, are described.

Abstract: Described herein, inter alia, are compositions and methods for treating or preventing obesity and using the same.

Abstract: The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives.

Abstract: Described herein are polymorphic forms of 1,6-dibromo-1,6-dideoxy-dulcitol (dibromo dulcitol or DBD), which is a known antitumor agent. Also described are methods of making these new crystalline polymorphic forms as well as methods of using these polymorphic forms to treat cancer.

Abstract: The present invention relates to water-dispersible microcapsules that include an oil phase, e.g. a perfume, containing a photolabile compound capable of generating a gas upon exposure to light. The gas is able to cause an extension or the breaking of the microcapsule allowing the release of the oil phase and thus increasing the long-lastingness of the odor perception. The present invention concerns also the use of such microcapsules in perfumery as well as the perfuming compositions or perfumed articles that include such microcapsules therein to provide a prolonged release of fragrant molecules.