Abstract: Compounds and compositions are provided as inhibitors of the Wnt/?-catenin pathway for the treatment of diseases that implicate the same.

Abstract: Disclosed herein are Notch transcriptional activation complex kinase (“NACK”) inhibitors, and methods for their use in treating or preventing diseases, such as cancer. The inhibitors described herein include compounds of Formula (la) and pharmaceutically acceptable salts thereof: wherein the substituents are as described.

Abstract: The invention features dosing regimens and pharmaceutical formulations for oral administration of palovarotene. The dosing regimens can reduce heterotopic ossification, reduce the number of flare-ups, and/or reduce the severity of flare-ups in subjects suffering from fibrodysplasia ossificans progressiva.

Abstract: Synergistic compositions comprising: one component (A), consisting of the compound having formula (I) 3-difluoromethyl-N-(7-fluoro-1,1,3-trimethyl-4-indanyl)-1-methyl-4-pyrazolecarboxamide one or more components (B) having a fungicidal or insecticidal activity, and their use for the control of of harmful insects in agrarian crops.

Abstract: A series of substituted spirocyclic indane derivatives of Formula (I), and analogues thereof, being potent modulators of human IL-17 activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including inflammatory and autoimmune disorders.

Abstract: Methods of reducing blood brain barrier dysfunction involve inhibiting 5-LOX and COX-2.

Abstract: The present disclosure provides compounds suitable for inhibiting CaMKK2. Also provided are compositions and methods of treating diseases associated with CaMKK2.

Abstract: The present invention provides a therapeutic agent or a prophylactic agent of dementia containing xanthine oxidase inhibitor such as a compound represented in formula (I), (II), (III) or (IV), or a pharmaceutically acceptable salt thereof as an active ingredient.

Abstract: Disclosed are compounds useful, for example, in methods of treating hyperproliferative disorders such as cancer, methods of arresting the cell cycle in cancer cells, methods of inhibiting glutathione synthesis in cancer cells, and associated compounds for use and uses in medicaments. In certain embodiments, the methods, uses and compounds are provided with reference to compounds of the structural formulae (Ia), (Ib), (Ic), (Id) and (Ie), in which R1, L1, L2, Q, L3, R3, L4, R4, L5, and R5 are as described herein. In certain embodiments, compounds disclosed herein are especially active against cancers having a mutant KRAS gene.

Abstract: Herein is described the design and synthesis of resorcylate aminopyrazole compounds. These compounds show broad, potent and fungal-selective Hsp90 inhibitory activity. These compounds also find use in treating Hsp90 related diseases.

Abstract: The present invention relates to certain pyrazole derivatives of Formula (I) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor and their uses for the treatment and prophylaxis of visual hallucinations associated with Lewy Body dementia.

Abstract: Disclosed are compounds of Formula (I), methods of using the compounds for inhibiting HPK1 activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer.

Abstract: Provided are methods of regulating proliferation and/or differentiation of keratinocytes and immune cells, more specifically to methods of treating pathologies characterized by hyperproliferative keratinocytes or inflammatory skin diseases by administration of FABP4-inhibitor.

Abstract: An anesthetic pharmaceutical composition, system and method is provided. The anesthetic pharmaceutical composition comprises an intraoperative local injection and one or more postoperative medications. The intraoperative local injection is long-acting and comprises at least one local anesthetic agent, such as ropivacaine; ketorolac; and at least one steroid, such as dexamethasone. The one or more postoperative medications comprise an atypical opioid agonist, such as tramadol; a non-steroidal anti-inflammatory drug, such as a cyclooxygenase-2 inhibitor; a gamma-aminobutyric acid analogue, such as pregabalin; and acetaminophen. The method comprises the steps of commencing a surgical procedure involving one or more incision sites; injecting an intraoperative local injection at the one or more incision sites; performing and completing the surgical procedure; and administering one or more postoperative medications.

Abstract: Disclosed are compounds useful, for example, in methods of treating hyperproliferative disorders such as cancer, methods of arresting the cell cycle in cancer cells, methods of inhibiting glutathione synthesis in cancer cells, and associated compounds for use and uses in medicaments. In certain embodiments, the methods, uses and compounds are provided with reference to compounds of the structural formulae (Ia), (Ib), (Ic), (Id) and (Ie), in which R1, L1, L2, Q, L3, R3, L4, R4, L5, and R5 are as described herein. In certain embodiments, compounds disclosed herein are especially active against cancers having a mutant KRAS gene.

Abstract: The invention provides compounds of the formula (I): wherein R1 and R2 are defined in the specification, to pharmaceutical compositions comprising the compounds and the compounds for use as medicaments. The compounds potentiate AMPA receptor function and are expected to be useful in the treatment of central nervous system disorders, for example in the treatment of depressive disorders, mood disorders and cognitive dysfunction associated with neuropsychiatric disorders such as schizophrenia.

Abstract: Adrenergic receptor modulating compounds and methods of using the same are provided. Also provided are methods of treating a subject for a disease or condition associated with an adrenergic receptor including administering a therapeutically effective amount of the subject compound. Aspects of the disclosure include a method of modulating an inflammatory pathway in a cell, such as the production of TNF-alpha in the cell. The method can include contacting a cell with ?1-selective adrenergic receptor modulating compound to selectively activate a cAMP pathway over a beta-arrestin pathway in the cell. Pharmaceutical compositions and kits which include the subject compounds are provided.

Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds which are prodrugs of ALOX-15 inhibitors. Also described herein are methods for using such compounds in the treatment of disease.

Abstract: This invention relates to, in part, methods and compositions that are useful for the diagnosis, treatment, or prevention of a blinding eye disease, including in the discovery of drugs that are efficacious against these diseases. Diseases include, for example, age related macular degeneration and reticular pseudodrusen disease, and the methods described herein include, for example, the method named delayed near infrared analysis (DNIRA).

Abstract: The present invention relates to pharmaceutical compositions comprising a combination of a therapeutically-effective amount of the antiviral compound valaciclovir and a therapeutically-effective amount of the COX-2 inhibitor celecoxib. The invention is further related to methods of treating functional somatic syndromes by administering a therapeutically-effective combination of valaciclovir and celecoxib.

Abstract: Use of a glucagon receptor antagonist in combination with a cholesterol absorption inhibitor for the treatment of diabetes and related conditions is disclosed.

Abstract: Described herein are methods for treating transthyretin (TTR) amyloidosis in a subject. The methods include specific dosing regimens that have great efficacy in treating the subjects and that are well tolerated in subjects.

Abstract: The invention provides novel regimens of farnesoid X receptor (FXR) agonist and methods for modulating the activity of farnesoid X receptors (FXRs) using novel regimes of specific FXR agonists, in particular for treating or preventing fibrotic or cirrhotic diseases or disorders, such as liver diseases.

Abstract: Disclosed are compounds of formulae: and pharmaceutically acceptable salts thereof, wherein the variables, R1, R2, R3, R4, R5, R6, R7, R11, R12, R13, R14, R15, R16, R17, n, and m are defined herein. These compounds are useful for treating Gram-negative bacteria infections. Also disclosed are methods of making these compounds.

Abstract: Provided herein are compounds of the formula I: as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment or prevention of mGluR5 mediated disorders, such as acute and/or chronic neurological disorders, cognitive disorders and memory deficits, as well as acute and chronic pain.

Abstract: The present invention relates to nitro-vinyl-pyrazole compounds of formula (B) wherein ring A, RB2 and RB3 are as defined in claim 1, as well as the manufacture of such compounds and their subsequent use in the production of agrochemicals and/or pharmaceuticals.

Abstract: The present disclosure provides solid forms of (E)-3-[2-(2-thienyl)vinyl]-1H-pyrazole, compositions thereof, and methods of making and using the same.

Abstract: Provided are a condensed cyclic compound and an organic light-emitting device including the same. The material is represented by the formula A2-(A1)n1, wherein A2 may be selected from groups represented by Formula 2, A1 may be selected from groups represented by Formulae 2-1 to 2-4, and n1 may be an integer selected from 1 to 5: Organic light-emitting devices manufactured using this material were found to have lower driving voltages, higher brightness values, higher efficiencies, and longer half-lifespans.

Abstract: The present invention relates to a stable oral liquid pharmaceutical composition of celecoxib or its pharmaceutically acceptable salts thereof. The celecoxib present in the compositions as described herein do not show any precipitation when subjected in Fasted-State Simulated Gastric Fluid (FaSSGF) at pH 2.0, temperature of 37° C.±0.5° C. and under stirring at a speed of 50 rpm at least for 60 minutes. It also relates to the process of preparing and method of using said composition of celecoxib.

Abstract: Semiconductor packages with electromagnetic interference supported stacked die and a method of manufacture therefor is disclosed. The semiconductor packages may house a stack of dies in a system in a package (SiP) implementation, where one or more of the dies may be wire bonded to a semiconductor package substrate. The dies may be stacked in a partially overlapping, and staggered manner, such that portions of some dies may protrude out over an edge of a die that is below it. This dies stacking may define a cavity, and in some cases, wire bonds may be made to the protruding portions of the die. Underfill material may be provided in the cavity and cured to form an underfill support. Wire bonding of the bond pads overlying the cavity formed by the staggered stacking of the dies may be performed after the formation of the underfill support.

Abstract: Compounds having activity as PKM2 activators are disclosed. The compounds have the following structure (I): including stereoisomers, tautomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4, R5 and R6 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: In certain embodiments the present invention provides methods useful in the treatment of glioma, such as glioblastoma, such methods comprising administering to a subject in need thereof a CSF-IR inhibitor together with one or more additional active agents such as IGF-IR inhibitors, PI3K inhibitors, IL4 inhibitors, NFAT inhibitors, and/or Stat6 inhibitors. In certain embodiments the present invention provides pharmaceutical compositions comprising a CSF-IR inhibitor together with one or more of such additional active agents.

Abstract: This invention provides a pharmaceutical composition for treating or preventing synucleinopathy comprising a compound represented by formula (I), or a pharmaceutically acceptable salt thereof.

Abstract: Compounds discovered through a high-throughput screen, along with methods of use of the compounds, are provided. The compounds can be used to strongly inhibit key drug targets found in protozoan parasites, e.g., the target Trypanosoma cruzi glucokinase. Compounds include derivatives of N-phenylbenzenesulfonamide, barbituric acid, (R)-3-(piperidin-2-yl)pyridine, 3-nitro-2-phenyl-2H-chromene, 6-amino-3-methyl-4-phenyl-1,4-dihydropryranole[2,3-c]pyrazole-5-carbonitrile, and gossypol (2,2?-Bis(formyl-1,6,7-trihydroxy-5-isopropyl-3-methylnaphthalene).

Abstract: The present invention provides methods and kits a) for preventing and/or treating cancer (e.g., colorectal cancer, neuroblastoma) that is linked, in part, to high levels of ODC activity and increased cellular polyamine content, b) for predicting cancer patient survival, especially cancer patient's whose cancer is linked, in part, to high levels of ODC activity and increased cellular polyamine contents, and c) for selecting the corresponding treatment options for such patients based on the allelic nucleotide sequence or SNP at positions +263 and/or +316 of the ODC1 gene as well as cancer treatment methods, in each case, which include the determination of the ODC1 genotype at the +263 and/or +316 positions, as a means to guide treatment selection.

Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer.

Abstract: Disclosed in the present invention are a new thiazole compound, particularly a compound represented by formula (I), a pharmaceutical composition thereof and applications thereof in the preparation of drugs for the treatment of diseases related to herpes simplex viruses.

Abstract: A process for preparation of 4-aminoindane derivatives of a first formula, salts and enantiomers thereof comprising the steps of: a) hydrogenating a 1,2-dihydroquinoline of a second formula to give a corresponding tetrahydroquinoline of a third formula; b) acylating the tetrahydroquinoline of the third formula with a carboxylic acid derivative of a fourth formula to obtain a corresponding acyl derivative compound of a fifth formula; c) rearranging the acyl derivative compound of the fifth formula under acidic conditions so as to give an acyl indane compound of a sixth formula; and d) hydrolysing the acyl group of the acyl indane compound of the sixth formula so as to obtain the 4-aminoindane derivatives of the first formula.

Abstract: Described herein are methods and compositions for the treatment of conditions, diseases, or disorders associated with autotaxin activity. The methods and compositions disclosed herein include the use of at least one autotaxin inhibitor compound.

Abstract: It was found that finafloxacin has a high solubility in the presence of Tris. Such solubility is significantly higher than in the presence of other compounds typically used as buffers (e.g. phosphate buffer). The observed significant increase in solubility of finafloxacin in compositions comprising Tris is further advantageously accompanied by a long term stability of such solutions. Tris is therefore to be regarded as a specific tool to considerably enhance the solubility of finafloxacin in solutions. By preparing compositions comprising Tris it is possible to dissolve finafloxacin in such an amount therein that these compositions can effectively be used as parenteral compositions for the treatment of bacterial infections.

Abstract: The invention provides methods and compositions for treating cancer and for enhancing immune function in an individual having cancer. The methods comprise administering a PD-1 axis binding antagonist and a taxane.

Abstract: The present invention relates to a novel process for converting the unwanted S enantiomer form to its useful raceme with respect to a 4-aminoindane derivative.

Abstract: A crystal form of 2-(3,5-dimethyl-1H-pyrazol-1-yl)-5-methylphenol which is stable and has high purity for preservation, industrial manufacturing, and circulation, and process for providing the same by using a boron compound.

Abstract: The present invention is directed to processes and intermediates useful for the preparation of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea (Compound I), crystalline forms and solvate forms thereof; and compositions comprising 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea, crystalline forms and solvate forms thereof prepared by processes as described herein.

Abstract: The present invention provides compounds and a method for the targeted delivery of Mitochondrial Angiotensin Receptor Blockers (MARBs) to the Mitochondrial Angiotensin System (MAS) for the treatment of diseases caused by angiotensin-related mitochondrial dysfunction. The compounds include a mitochondrial targeting signal, a residue of a drug molecule, a functional moiety, and a scaffold moiety.

Abstract: The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.

Abstract: Provided herein are improved processes for the preparation of a compound of Formula IX (AG-10). Also provided herein are pharmaceutically acceptable salts of Formula I and Formula Ib as well as crystalline types of Formula IX (AG-10). The processes described herein provide improved yields and efficiency, while the pharmaceutically acceptable salts and crystalline forms provide unexpected pharmacokinetic properties. Other features and aspects of the present disclosure will be apparent to a person of skill in the art upon reading the remainder of the specification.

Abstract: A solid composition comprising sofosbuvir and at least one pharmaceutically acceptable matrix compound wherein at least 99 weight-% of the sofosbuvir comprised in the composition are present in amorphous form, at least 99 weight-% of the solid composition consist of the sofosbuvir and the at least one matrix compound, and wherein the solid composition contains the sofosbuvir in an amount of at least 55 weight-% based on the combined weight of the sofosbuvir and the at least one matrix compound.

Abstract: Combinations of certain analgesics with COX-II inhibitors, related pharmaceutical compositions, including advantageous galenical forms containing these combinations, and the use of such combinations in methods of treatment, in particular for the treatment of pain.

Abstract: Compounds having activity as PKM2 activators are disclosed. The compounds have the following structure (I): including stereoisomers, tautomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4, R5 and R6 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.