Abstract: The present invention relates to polymorphic forms of compound 1 or 1a and processes for preparing compound 1 and 1a polymorphs, which are useful as antifungal agents. In particular, the invention seeks to provide a new methodology for preparing polymorphs of compound 1 and substituted derivatives thereof.

Abstract: The invention relates to methods of reducing the level of 2-hydroxyglutarate in cells by administration of an inhibitor of mutant isocitrate dehydrogenase-1.

Abstract: A method of treating disorders associated with aberrant kinase activity, wherein the kinase is. Adaptor-associated protein kinase 1 (AAK1), Aurora Kinase A (AURKA), Aurora Kinase B (AURKB), Bruton's Tyrosine Kinase (BTK), Interleukin-1 receptor-associated kinase 3 (IRAK3), Protein tyrosine kinase 2 beta (PTK2B), Tyrosine-protein kinase Tec (TEC), Serine/threonine-protein kinase Wee1 (WEE1), Cyclin G-associated kinase (GAK), Large Tumour suppressor 1 Kinase (LATS1), Focal Adhesion Kinase (PTK2), Ribosomal protein S6 kinase alpha-1 (RPS6KA1) said method comprising degrading said kinase.

Abstract: The present invention relates to an alkynyl-substituted heterocyclic compound acting as an FGFR inhibitor, a preparation method therefor and a medical use thereof. In particular, the present invention relates to a compound as shown in general formula (I) and a pharmaceutically acceptable salt thereof; a pharmaceutical composition including the compound or a pharmaceutically acceptable salt thereof; a method for treating and/or preventing FGFR-associated diseases, particularly tumors, by using the compound or a pharmaceutically acceptable salt thereof; and a preparation method for the compound or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to the fields of medicinal chemistry and pharmacotherapy, and specifically relates to the chemical compound of formula (I), and its racemate, R-isomer, S-isomer, pharmaceutically acceptable salt, and mixtures thereof, as well as its method for preparation, a pharmaceutical composition containing said chemical compound, and use as a lysine-specific demethylase 1 (LSD 1) inhibitor. The cyclopropylamine chemical compound to which the present invention relates may be used in the treatment of cancer.

Abstract: Oral formulations of benzofuran compounds which modulate cannabinoid receptors are presented. Methods of using these formulations for treatment of cannabinoid receptor-mediated disease, including neuropathic pain and addition, are also described.

Abstract: The present invention provides compounds of Formulae (A), (B), (C), and (D), pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof, pharmaceutical compositions thereof, and kits thereof. The present invention further provides methods of using the compounds to treat or prevent neurological disorders, including Alzheimer's disease, Parkinson's disease, Huntington's disease, ALS (amyotrophic lateral sclerosis), traumatic brain injury, ischemic brain injury, stroke, frontal temporal dementia, Pick's disease, corticobasal degeneration, supra cerebral palsy, prion diseases (e.g., Creutzfeldt-Jakob disease, Gerstmann-Straussler-Scheinker syndrome, Fatal Familial Insomnia, and Kuru), Nieman Pick type C, spinal cerebellar ataxia, spinal muscular dystrophy, ataxia telangiectasia, hippocampal sclerosis, Cockayne syndrome, Werner syndrome, xeroderma pigmentosaum, and Bloom syndrome.

Abstract: Compounds that disrupt the interaction between PCSK9 and LDLR, compositions that include the compounds, and methods for making and using the compounds and compositions.

Abstract: The present invention relates to novel triazole derivatives, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators.

Abstract: The invention discloses 20,23-modified novel derivatives of 16-membered demycarosyltylonolide antibiotics, which are useful against bacterial and mycoplasmic pathogens in humans and animals. Also claimed are pharmaceutical compositions of such derivatives and their use in treating bacterial and mycoplasmic infections in humans and animals.

Abstract: This invention provides for flow and batch synthesis processes for the production of Lamivudine and Emtricitabine, including flow and batch synthesis processes wherein at least of the synthesis steps are conducted in a solvent free environment.

Abstract: The invention describes an aryl-2,2?-tandem bisthiazole compound and a preparation method and the use thereof. In particular, disclosed in the present invention are an aryl-2,2?-tandem bisthiazole compound with the structure as shown in general formula I and the preparation method thereof and use thereof as a histone deacetylase inhibitor in the preparation of antitumor drugs.

Abstract: Disclosed herein are aztreonam derivatives, therapeutic methods of using the aztreonam derivatives, particularly in combination with ?-lactamase inhibitors, and pharmaceutical compositions thereof. The aztreonam derivatives can be administered orally to provide orally bioavailable aztreonam.

Abstract: The invention provides various novel compositions of berberine in combination with pharmacologically active organic acids, and related methods of their use in treating various diseases or disorders. The invention further provides various novel compounds prepared from berberine and pharmacologically active organic acids and prepared from ursodeoxycholic acid and pharmacologically active organic bases, and pharmaceutical compositions thereof, and methods of their preparation and therapeutic use in treating and/or preventing various diseases or disorders.

Abstract: Solid state forms of Palbociclib dimesylate, processes for preparation thereof and use thereof for preparation of Palbociclib are disclosed.

Abstract: The invention disclosed herein relates to 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridinyl compounds and 4,5,6,7-tetrahydro-2H-pyrazolo[4,3-c]pyridinyl compounds of Formula (A), pharmaceutical compositions comprising such compounds and the use of such compounds in the treatment of autoimmune diseases.

Abstract: The present invention provides a pyrido five-element aromatic ring compound, and a preparation method therefor and a use thereof. The compound provided in the present invention has an inhibitory effect on wild-type and/or mutant EZH2, and is well positioned to become a novel anti-tumor drug or a drug for the treatment of autoimmune diseases.

Abstract: The invention relates to compounds of formula (II) for using in imaging and particularly for the diagnosis of neurodegenerative diseases

Abstract: The present invention relates to novel compounds that can be employed in the treatment, alleviation or prevention of a group of disorders and abnormalities associated with Tau (Tubulin associated unit) protein aggregates including, but not limited to, Neurofibrillary Tangles (NFTs), such as Alzheimer's disease (AD).

Abstract: Compounds of the formula (I), in which R1, R3, Het1 and HET have the meanings given in Claim 1, are ATM kinase inhibitors and can be employed, inter alia, for the treatment of cancer.

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

Abstract: Disclosed are solid state forms of lumateperone ditosylate, uses thereof, and pharmaceutical compositions thereof.

Abstract: This invention is directed to synthetic co-crystals of anhydrous guanine and at least one additional material, wherein the co-crystals have a high refraction index and therefore, provide products with pearlescence or whiteness with high coverage. The invention is further directed to a process for the preparation of anhydrous guanine and of the co crystals.

Abstract: Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.

Abstract: The present disclosure relates generally to the field of antimicrobial compounds and to methods of making and using them. These compounds are useful for treating, preventing, reducing the risk of, and delaying the onset of microbial infections in humans and animals. In some embodiments, the present disclosure provides a compound of Formula (I): or a tautomer thereof or a pharmaceutically acceptable salt of the compound or tautomer.

Abstract: The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders.

Abstract: The present invention relates to certain compounds (e.g., imidazopyrazine, imidazopyridine, imidazopyridazine and imidazpyrimidine compounds) that act as inhibitors of the MAP kinase interacting kinases MNK2a, MNK2b, MNK1a, and MNK1b. The present invention further relates to pharmaceutical compositions comprising these compounds, and to the use of the compounds for the preparation of a medicament for the prophylaxis and treatment of diseases (e.g., proliferative diseases (e.g., cancer), neurodegenerative diseases (e.g., Alzheimer's disease), metabolic diseases (e.g. diabetes), neurodevelopmental disorders (e.g. autism), or psychiatric disorders (e.g. schizophrenia or anxiety)) as well as methods of treating these diseases.

Abstract: Provided are a preparation method for a chiral pyrrolopyrimidine compound and a related intermediate. In the method, a compound of formula A and a compound of formula 6 or a salt thereof are reacted to obtain a compound of formula 7 or a compound of formula 14, and a compound of formula I is prepared from the compound of formula 7 or the compound of formula 14. Also provided are the intermediate used, a preparation method for the intermediate and a use of the intermediate in the preparation of the compound of formula I. The preparation method has characteristics such as brief steps, a high stereoselectivity, a high utilization ratio of atoms, mild reaction conditions and a convenient post-treatment. The method avoids using an expensive asymmetric reaction catalyst, and is suitable for industrial production.

Abstract: Provided herein are crystalline forms of a triazolopyrimidine compound, which is useful for treating a PRC2-mediated disease or disorder.

Abstract: Imidazopyrazinamine phenyl derivatives, pharmaceutically acceptable salts and hydrates thereof, or metabolites thereof formed by any form of metabolism, and uses thereof in the preparation of medicaments for preventing and/or treating indications/diseases associated with BTK functions are disclosed. The disclosed imidazopyrazinamine phenyl derivatives are ideal high-efficient BTK inhibitors for treating or preventing diseases such as rheumatoid arthritis, B cell lymphoma, leukemia, multiple myeloma, allergies, asthma, multiple sclerosis, type I diabetes and systemic lupus erythematosus.

Abstract: The present invention relates to salt forms and derivatives of 2-methylthio-6-nitro-1,2,4-triazoio[5,1-c]1,2,4-triazine -7-one, dehydrate and pharmaceutical compositions thereof. These salt forms and derivatives exhibit improved antiviral activity. The present invention also relates to processes for preparing the compounds, and intermediates used in their preparation.

Abstract: The invention relates to compounds which are suitable for the treatment of cancer, an immune disease, Parkinson's disease, Cardiac Hypertrophy or Type-2 diabetes and to pharmaceutical compositions containing such compounds. The invention further relates to a kit of parts comprising such compounds.

Abstract: Described herein are fused bicyclic compounds, compositions, and methods for their use for the treatment of disease.

Abstract: The present invention relates to nimbolide analogs useful as anti-cancer agents and preparation thereof. Particularly the present invention relates to nimbolide analogs of general formula I. wherein, ring M is any ring selected from the group consisting of substituted or unsubstituted aryl, heteroaryl, cycloalkyl and heterocyclic; A and B are selected from the group consisting of C, O, N, S and H; R1, R2, R3, R4, R5 and R6 are selected from the group consisting of C1-C6 alkyl, aryl, heteroaryl, C1-C7 cycloalkyl, heteroalkyl, hydrogen, hydroxy, alkoxy, nitro, halogen, amino, alkylamino, aryl amino and cyano; wherein each of these groups may be further substituted with one or more substituents selected from the group consisting of hydrogen, hydroxy, halogen, cyano, alkyl amino, aryl amino, alkoxy, amino, nitro, aldehyde, carboxylic acid and ester.

Abstract: Disclosed are methods, compositions and kits for treating or preventing heart failure. Methods of the invention treating heart failure in a mammal comprising administering to the mammal an effective amount of a thienopyrimidine compound.

Abstract: The field of invention relates to a novel process, suitable for industrial scale manufacture, for the preparation of high-purity 5-[2-cyclopropyl-1-(2-fluorophenyl)-2-oxoethyl]-4,5,6,7-tetrahydrothieno[3,2-c]pyridine-2-yl acetate, prasugrel, of Formula (I). Especially in large-scale production, one of the main causes of piling up the impurities is the use of ether solvents consequently in each step in this procedure ethers are excluded. Avoiding the ethers resulted new conditions for production of intermediates in the different steps of our procedure. Conditions were determined so that each step from the beginning contributes to minimizing the impurity content of the end-product.

Abstract: The present invention relates to thienopyrimidine compound, preparation method thereof, pharmaceutical composition and use thereof, and in particular to a type of compounds having ALK and/or c-Met selective inhibitory activity, a method for the preparation thereof, a pharmaceutical composition comprising the same, and use of these compounds in the manufacture of a medicament for preventing or treating a disease associated with anaplastic lymphoma kinase in vivo, and in the manufacture of a medicament for preventing or treating a disease associated with angiogenesis or cancer metastasis, in particular in the manufacture of a medicament for preventing or treating tumor growth and metastasis.

Abstract: Disclosed is a method for the photoinitiated transformation of a transformable reactive substrate. The method includes an initial step in which a protected ketone photoinitator species which is present in the suhstrate is deprotected to form the corresponding ketone photoinitiator species for use in a subsequent photoinitiated reaction in the method. The ketone group of the photoinitiator is protected by an unsubstituted 1,3 dioxolanc group. Also disclosed are a composition which may be used in the method, the use of the protected ketone photoinitiator in a photoinitiated reaction, as well as the protected ketone photoinitiators themselves.

Abstract: Provided is a pharmaceutical composition for preventing and treating tumors, the pharmaceutical composition including an imidazooxazole derivative compound, a solvate, a stereoisomer, or a pharmaceutically acceptable salt thereof as an active ingredient. The pharmaceutical composition is administered to an entity which has developed a tumor or is in danger of developing a tumor, and thus tumors can be prevented or treated.

Abstract: Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an aryl, heteroaryl or heterocycle (R32) are provided. The inhibitors of Factor D described herein reduce the excessive activation of complement.

Abstract: Disclosed herein, inter alia, are compositions and methods of using the same for the treatment of cancer.

Abstract: PDI derivatives useful as opto-electronically active materials or for the synthesis of such materials. Certain compounds herein function as efficient electron acceptors and are useful as electron active components of electronic devices.

Abstract: The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a mammal, and in particular to spiro bicyclic compounds, pharmaceutical composition comprising such compounds, and their use as menin/MLL protein/protein interaction inhibitors, useful for treating diseases such as cancer, myelodysplastic syndrome (MDS) and diabetes.

Abstract: Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents.

Abstract: Boron and nitrogen containing heterocyclic compounds are disclosed, which can be used as emitters, hosts, charge blocking materials, charge transporting materials, etc. in an electroluminescent device. These novel compounds can offer very narrow emissive spectrum, and obtain high saturated deep blue emission. Also disclosed are an organic light-emitting device and a formulation.

Abstract: A hydrocarbyloxydisilane according to formula (I) Si2(OR)xH6-x; ??(I) where x is 1-5 and R is hydrocarbyl having from 1 to 10 carbon atoms, with the proviso that when x is 1, R is not methyl and when x is 3, (I) does not represent 1,1,2-trimethoxydisilane, and a method of making an hydrocarbyloxydisilane, the method comprising: causing the reaction of i) an hydrocarbylaminodisilane, and ii) an alcohol according to formula (II) R2OH; ??(II) where R2 is hydrocarbyl having from 1 to 10 carbon atoms, to form a product mixture comprising the hydrocarbyloxydisilane.

Abstract: The present invention relates to chiral compounds with two optically active phosphorus atoms, chiral transition metal catalysts which comprise these compounds as ligands, a process for preparing the P-chiral compounds and processes for asymmetric synthesis using the chiral transition metal catalysts. The present invention specifically relates to a process for preparing an optically active carbonyl compound by asymmetric hydrogenation of a prochiral ?,?-unsaturated carbonyl compound with hydrogen in the presence of an optically active transition metal catalyst according to the invention. Yet more specifically, the present invention relates to a process for the asymmetric hydrogenation of citral, and also a process for preparing optically active menthol.

Abstract: Provided is a method for producing a halogen-crosslinked iridium dimer, including reacting an iridium compound represented by the general formula (1) with an aromatic bidentate ligand in a solvent to produce a halogen-crosslinked iridium dimer, the solvent having a boiling point of 50° C. or higher and lower than 350° C., the reaction being carried out at a reaction temperature of 50° C. or higher and lower than 300° C., and the aromatic bidentate ligand being added in an amount of 0.5 times or more and less than 10 times the molar amount of the iridium compound. The halogen-crosslinked iridium dimer is usable as a precursor of a cyclometalated iridium complex useful as a phosphorescent material.

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

Abstract: Compositions and methods comprising metal organic frameworks (MOFs) and related uses are generally provided. In some embodiments, a MOF comprises a plurality of metal ions, each coordinated with at least one ligand comprising at least two sets of ortho-diimine groups arranged about an organic core.