Abstract: The invention relates to substituted pyrimidine compounds with the following formula: or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof. These compounds selectively target the hemopexin domain of matrix metalloproteinase 9 (MMP-9) and do not inhibit the protease's catalytic functions. The invention also relates to methods of treating cancer in a patient in need thereof with the compounds.

Abstract: This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from post-traumatic stress disorder comprising administering a disclosed compound or composition.

Abstract: ZnCl2 co-crystal of racemic-(±)-blarcamesine hydrochloride of formula 2a, ZnCl2 co-crystal of (S)-(?)-blarcamesine hydrochloride of formula 2b and ZnCl2 co-crystal of (R)-(+)-blarcamesine hydrochloride of formula 2c, processes for preparation thereof and pharmaceutical preparation thereof and methods of treating neurodegenerative, neurodevelopmental diseases such as Alzheimer's disease, Parkinson's disease dementia and/or Rett syndrome.

Abstract: The present invention is directed to methods for the preparation of eremophila-1(10)-11(13)-dien-12,8?-olide (EPD) and analogues thereof.

Abstract: An object is to provide a method for producing a compound which is useful as a synthetic intermediate for an active pharmaceutical ingredient of an antidiabetic drug or the like in an industrially inexpensive and efficient manner, and the present invention can achieve the object by reducing a compound (2) represented by the following formula (2): wherein R1, Ar, n and X are as mentioned herein in the presence of a titanium compound by using a reducing agent to produce a compound (1) represented by the following formula (1): wherein R1, Ar and n are the same as defined above.

Abstract: Described herein are amorphous and crystalline forms of the androgen receptor modulator 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide. Also described are pharmaceutical compositions suitable for administration to a mammal that include the androgen receptor modulator, and methods of using the androgen receptor modulator, alone and in combination with other compounds, for treating diseases or conditions that are associated with androgen receptor activity.

Abstract: Disclosed herein are aldehyde dehydrogenase (ALDH-2) inhibitor compounds, such as a compounds of Formula (I) or Formula (II), pharmaceutical compositions comprising these inhibitor compounds, and uses of these compounds and compositions, such as in the methods for safely treating chemical dependency on a substance or condition of addiction, such as alcohol, nicotine, cocaine, opiates, amphetamines, and compulsive eating disorder, and/or anxiety disorder, each individually or concurrent.

Abstract: The present invention relates to a novel method for preparing efinaconazole using an ionic liquid as a medium. The method includes subjecting 1-[[(2R,3S)-2-(2,4-difluorophenyl)-3-methyloxiranyl]methyl]-1H-1,2,4-triazole to a coupling reaction with 4-methylenepiperidine or an organic chemically acceptable salt thereof in the presence of a base and an ionic liquid compound. The base makes the 4-methylenepiperidine or organic chemically acceptable salt thereof anionic. The use of the ionic liquid in the method of the present invention prevents the formation of related substances, shortens the reaction time, and enables easy preparation of the final compound efinaconazole in high purity and yield on a large scale, compared to the use of organic solvents in conventional methods.

Abstract: The present invention relates to macrocyclic compounds of any one of Formula (I), or a pharmaceutically acceptable form thereof, pharmaceutical compositions comprising the same, methods of preparing the same, and methods of treating cancer dependent on a farnesylated protein, using the same.

Abstract: Provided herein are arylcyclopropyl amino-isoquinoline amide compounds. In particular, the disclosure provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds of the disclosure are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, diseases characterized by abnormal growth, such as cancers, and inflammatory diseases. The disclosure further provides compositions containing isoquinoline amide compounds.

Abstract: A pyrrole-substituted indolone derivative or pharmaceutically acceptable salts thereof, and a preparation method therefor and application thereof. The pyrrole-substituted indolone derivative or pharmaceutically acceptable salts thereof is simple to synthesize, easy to prepare, rich in raw materials for synthesis, and has an inhibitory effect on a plurality of tyrosine kinases, especially has higher selective inhibitory activity against KDR (VEGFR2), and FLT3 and its mutants, and can avoid toxic side effects caused by inhibiting KDR.

Abstract: The present disclosure related to compounds that can be useful as inhibitors of PD-1, PD-L1 or the PD-1/PD-L1 interaction. Also disclosed herein are pharmaceutical compositions of that can include a compound of Formula (I), or a pharmaceutically acceptable salt thereof, and uses of or methods of using a compound of Formula (I), or a pharmaceutically acceptable salt thereof, for the treatment of PD-L1 related diseases including but not limited to liver diseases, cancer, hepatocellular carcinoma, viral diseases, or hepatitis B.

Abstract: Compounds of formula (A) are provided which are useful in the treatment of diseases or conditions modulated at least in part by CCR6:

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: Provided are a pregabalin lactam methylene dimer and a preparation method therefor. The method comprises the following steps: dissolving pregabalin in a reaction solvent, reacting same with an aldehyde in an acidic system and isolating the obtained target product pregabalin lactam methylene dimer. The preparation method for pregabalin lactam methylene dimer provided by the present application has a simple operation, a high product yield, a good purity and a low cost.

Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

Abstract: The present application relates to crystalline forms of 1-[(3R,4S)-4-cyanotetrahydropyran-3-yl]-3-[(2-fluoro-6-methoxy-4-pyridyl) amino]pyrazole-4-carboxamide and processes for the preparation thereof. The compound is useful for the treatment of JAK-mediated diseases or conditions such as atopic dermatitis.

Abstract: Thiophene derivatives of formula (I) and a pharmaceutically acceptable salt thereof are provided. These compounds have utility for the treatment or prevention of disorders caused by IgE, such as allergy, type 1 hypersensitivity or familiar sinus inflammation.

Abstract: The present specification relates to a heterocyclic compound represented by Chemical Formula 1, an organic light emitting device comprising the same, a composition for an organic material layer of an organic light emitting device, and a method for manufacturing an organic light emitting device.

Abstract: The present invention relates to certain substituted heterocondensed pyridone analogues of formula (I) which modulate the activity of Isocitrate Dehydrogenase (IDH). The compounds of this invention are therefore useful in treating diseases caused by mutated IDH1 and/or mutated IDH2 enzyme and/or IDH1 wild type enzyme, in particular cancer, cell proliferative disorders and immune-related disorders. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.

Abstract: The invention relates to compounds of Formula I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for method for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of cryptosporidiosis by administering such a compound.

Abstract: Provided herein are integrin inhibitors, compositions thereof, and methods of their uses. Crystalline forms of salts of the inhibitors are also described, along with methods of preparing the crystalline forms. X-ray powder diffraction data, thermogravimetric analysis, and differential scanning calorimetry data are provided for the crystalline forms. The integrin inhibitors are useful for treatment of, inter alia, fibrotic diseases.

Abstract: Novel pyrido[4,3-e] [1,2,3]triazolo[1,5-a]pyrimidine compounds, a method of synthesizing said compounds, a pharmaceutical composition comprising said compounds and a suitable carrier, and a method of using the compounds. The pyrido[4,3-e] [1,2,3]triazolo[1,5-a]pyrimidine compounds, identified as CK2 inhibitors, are useful as anticancer and/or antitumor agents, and as agents for treating other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and other types of diseases such as diabetes, viral infection, neurodegenerative diseases.

Abstract: Disclosed are a class of macrocyclic derivatives, a preparation method therefor, a pharmaceutical composition containing the derivatives, and the use thereof as therapeutic agents, particularly as XIa factor inhibitors and in the preparation of a drug for treating and preventing thromboembolisms and other diseases. Particularly disclosed are compounds shown by formula (I), an isomer thereof and a pharmaceutically acceptable salt thereof.

Abstract: Novel 5-substituted aminopyrazino[2?,1?:2,3]imidazo[4,5-c][2,7]naphthyridine compounds, a method of synthesizing said compounds, a pharmaceutical composition comprising said compounds and a suitable carrier, and a method of using the compounds. The 5-substituted aminopyrazino[2?,1?:2,3]imidazo[4,5-c][2,7]naphthyridine compounds, identified as CK2 inhibitors, are useful as anticancer and/or antitumor agents, and as agents for treating other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and other types of diseases such as diabetes, viral infection, neurodegenerative diseases.

Abstract: The disclosure relates to compounds of Formula (I), or pharmaceutically acceptable salts thereof, wherein X1 and X5 is each selected from CR1 or N; X2, X3 and X4 is each selected from CR1, CR2 or N, provided at least one of X2, X3 and X4 is CR2 and provided only one of X1, X2, X3, X4 and X5 can be N. R1, R2, R3, R4, R5, L1, L2 and L3 are as defined herein. Compounds according to Formula (I) are pharmacologically effective as lysyl oxidase (LOX) inhibitors and are believed to be useful in the treatment of, for instance, cancer.

Abstract: The invention relates to inhibitors of USP7 inhibitors useful in the treatment of cancers, neurodegenerative diseases, immunological disorders, inflammatory disorders, cardiovascular diseases, ischemic diseases, viral infections and diseases, and bacterial infections and diseases, having the Formula: where m, n, X1, X2, R1-R5, R5? and R6 are described herein.

Abstract: The present invention relates to a manufacturing process and intermediates for preparing a crystalline or non-crystalline form of N-((1S,3S)-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)cyclobutyl)propane-1-sulfonamide. The present invention also relates to salt forms and pharmaceutical compositions comprising the crystalline form, and to methods for use of the compound prepared from a crystalline form in the treatment of various diseases.

Abstract: Described herein is N-[4-[4-(4-morpholinyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]phenyl]-4-[[3(R)-[(1-oxo-2-propen-1-yl)amino]-1-piperidinyl]methyl]-2-pyridinecarboxamide (I) including crystalline forms, solvates, and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions that include compound (I), as well as methods of using compound (I), alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.

Abstract: Provided herein are inhibitors of protein arginine deiminases (PADs), pharmaceutical compositions comprising the compounds, and methods for using the compounds for the treatment of diseases.

Abstract: Semisynthetic methods of preparing neosaxitoxin from cultures of the dinoflagellates Alexandrium pacificum and Gymnodinium catenatum are described. The scalable method includes the reductive desulfonation of an unresolved mixture of gonyautoxin 1 (GTX1) and gonyautoxin 4 (GTX4) using dithiol in a buffered reaction solvent at a pH of about 7.5.

Abstract: Provided are organoiridium compounds that are useful as emitters in OLEDs. The compounds have Formula I L1L2Ir-L-Ir-L3L4, where: L is a bis-bidentate ligand including two or more aromatic rings; one of the two or more aromatic rings is bonded to the two Ir atoms at the same time; and each of L1, L2, L3, and L4 is independently a bidentate N-heterocyclic carbene ligand or a substituted or unsubstituted acetylacetonate ligand with L1, L2, L3, and L4 each being the same or different. Also provided are formulations including these organoiridium compounds. Further provided are OLEDs and related consumer products that utilize these organoiridium compounds.

Abstract: Provided are transition metal compounds having 5-membered carbocyclic or heterocyclic ring in a unique configuration of fused rings per Formula I The compounds show improved phosphorescent emission in red to near IR region and are useful as emitter materials in organic electroluminescence device.

Abstract: An organometallic compound represented by Formula 1: wherein, in Formula 1, groups and variables are the same as described in the specification.

Abstract: The present invention provides a main group metal complex, or pharmaceutically acceptable salt, solvate, non-covalent bond compound or prodrug thereof, which is composed of planar tetradentate Schiff base ligands and p-block main group metal ions. The main group metal complex can be conveniently prepared, and shows high cytotoxicity to a variety of cancer cell lines and has selective killing effect. The pharmaceutical compositions or pharmaceutical preparations prepared from the main group metal complex according to the present invention can be used for treatment of tumors. The main group metal complex also has fluorescent properties and can be used for fluorescent labeling.

Abstract: The present disclosure relates to a boron compound useful in an organic light-emitting diode and an organic light-emitting diode comprising same and, more particularly, to a boron compound represented by [Chemical Formula A], wherein [Chemical Formula A] and [Chemical Formula C] are as defined in the description.

Abstract: Organoamino-functionalized cyclic oligosiloxanes, which have at least two silicon and two oxygen atoms as well as an organoamino group and methods for making the organoamino-functionalized cyclic oligosiloxanes are disclosed. Methods for depositing silicon and oxygen containing films using the organoamino-functionalized cyclic oligosiloxanes are also disclosed.

Abstract: A metal tin cyclized perylene diimide derivative, having a structure formula of: where R1 and R2 are each independently selected from a hydrogen atom or a group containing or not containing a substituent. The group containing or not containing a substituent is an alkyl having between 1 and 60 carbon atoms, an alkoxy having between 1 and 60 carbon atoms, a cycloalkyl having between 3 and 60 carbon atoms, an aryl having between 5 and 60 atoms, an alkylaryl having between 1 and 60 carbon atoms, an alkylheteroaryl having between 1 and 60 carbon atoms, an alkylheterocyclyl having between 1 and 60 carbon atoms, an alkyleneoxyalkyl having between 1 and 60 carbon atoms, an alkyleneoxyaryl having between 1 and 60 carbon atoms, an alkyleneoxyheteroaryl having between 1 and 60 carbon atoms, or an alkyleneoxyheterocyclyl having between 1 and 60 carbon atoms.

Abstract: Described herein are CD73 inhibitors and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of cancer, infections, and neurodegenerative diseases.

Abstract: Methods for purifying RNA from a sample, comprising one or more steps of tangential flow filtration, hydroxyapatite chromatography, core bead flow-through chromatography, or any combinations thereof. These techniques are useful individually, but show very high efficiency when used in combination, or when performed in particular orders. The methods can purify RNA in a highly efficient manner without unduly compromising potency or stability, to provide compositions in which RNA is substantially cleared of contaminants. Moreover, they can be performed without the need for organic solvents.

Abstract: Disclosed are compounds suitable for enhancing cancer treatment, for example, a compound of formula (I): (I) wherein R1 is as defined herein. Also disclosed is a method of enhancing the response of cancer cells in a mammal to treatment with an apoptosis inducing ligand, a method of inducing apoptosis in cancer cells in a mammal, and a method of treating prostate cancer in mammal in need thereof comprising administration of a compound described herein.

Abstract: The present invention relates to improved methods in the separation recombinant polypeptides with post-translational modifications from complex mixtures through the use of a cation exchange medium.

Abstract: Provided is a method of preparing an N-acetyl dipeptide and an N-acetyl amino acid, the method including producing the N-acetyl dipeptide and the N-acetyl amino acid by reaction of an amino acid with acetic anhydride or acetyl chloride.

Abstract: Cyclic depsipeptide compounds of formula (I) and compositions comprising the compounds are provided that are effective against parasites that harm animals, including humans. The compounds and compositions may be used for combating parasites in or on animals including mammals and birds. Also provided are improved methods for eradicating, controlling and preventing parasite infestation in animals, including birds and mammals.

Abstract: Provided herein are agents, compositions, and methods useful for animal health, e.g., for altering the level, activity, or metabolism of one or more microorganisms resident in a host insect (e.g., arthropod, e.g., insect, e.g., pathogen vector), the alteration resulting in a decrease in the fitness of the host. The invention features a composition that includes an agent (e.g., phage, peptide, small molecule, antibiotic, or combinations thereof) that can alter the host's microbiota in a manner that is detrimental to the host. By disrupting microbial levels, microbial activity, microbial metabolism, or microbial diversity, the agents described herein may be used to decrease the fitness of a variety of insects that carry vector-borne pathogens that cause disease in animals.

Abstract: This disclosure relates to variant AAVrh 10 particles engineered to escape host neutralizing antibodies but retain or improve transduction efficiency, and their use as gene delivery vehicles.

Abstract: Recombinant paramyxoviruses including a viral genome encoding a heterologous gene are provided. In several embodiments, the recombinant paramyxovirus is a recombinant parainfluenza virus, such as a recombinant PIV3 including a viral genome encoding a heterologous respiratory syncytial virus F ectodomain linked to the transmembrane domain and the cytoplasmic tail of the F protein from the PIV3. Nucleic acid molecules including the genome of a recombinant paramyxoviruses are also provided. The recombinant viruses may advantageously be used in vaccine formulations, such as for vaccines against parainfluenza virus and respiratory syncytial virus.

Abstract: The present disclosure relates to compositions, methods, mixtures, and kits for detecting the presence of, and for removing, a virus from a product produced in an insect cell. The disclosure also relates to proteins, peptides, polypeptides, drug substances, biological products, vaccine antigens, and virus-like particles that are produced in an insect cell and that are free or substantially free of a virus. The disclosure also relates to compositions, methods, assays, and kits for detecting a rhabdovirus in a sample.

Abstract: The disclosure relates to a polypeptide suitable for detecting antibodies against a flavivirus in an isolated biological sample having a flavivirus NS1 wing domain specific amino acid sequence, wherein no amino acid sequences from the NS1 ?-ladder domain of said flavivirus are present in the polypeptide. In an embodiment, the flavivirus is selected from Zika virus (ZIKV), West-Nile virus (WNV), Dengue virus types 1-4 (DENV1-4), tick-borne encephalitis virus (TBEV), yellow fever virus (YFV) and Japanese encephalitis virus (JEV). Also disclosed is a method for producing said flaviviral NS1 wing domain specific polypeptides, a method for detecting antibodies specific for a first flavivirus species, the use of said flaviviral NS1 wing domain specific polypeptides for detecting antibodies as well as a reagent kit for detecting said flavivirus antibodies that has a flavivirus NS1 wing domain polypeptide.

Abstract: The present invention relates to an immunogenic polypeptide, a nucleic acid encoding the same, a pharmaceutical composition comprising the same and the immunogenic polypeptide, nucleic acid or pharmaceutical composition for use as a medicament, particularly a vaccine, or for use in a method of treating or preventing a Borrelia infection.