Abstract: 2-Acylindazole compounds of formula I or formula II are disclosed: These compounds inhibit Coagulation Factor XIIa. They are useful to treat autoimmune diseases.

Abstract: The present invention features crystalline polymorphs of dimethyl (2S,2?S)-1,1,-((2S,2?S)-2,2,-(4,4,-((2S,5S)-1-(4-tert-butylphenyl) pyrrolidine-2,5-diyl) bis (4,1-phenylene)) bis (azanediyl) bis (oxomethylene) bis (pyrrolidine-2,1-diyl)) bis (3-methyl-1-oxobutane-2,1-diyl) dicarbamate i.e. ombitasvir, compound (I), which is a potent HCV NS5A inhibitor. In one embodiment, a crystalline form of Compound (I) has characteristic peaks in the PXRD pattern as shown in one of FIGS. 1-11.

Abstract: A process for preparing a compound of formula (I): or a pharmaceutically acceptable salt thereof includes reacting a compound of formula (6): (wherein R is H) with 2-aminocyclohexanol or a salt thereof.

Abstract: The present invention relates to processes for the preparation of empagliflozin. In particular, the present invention relates to the preparation of empagliflozin and intermediates thereof. The present invention also relates to co-crystal of empagliflozin and amino acid and amorphous form of empagliflozin.

Abstract: [Problem] To provide a compound useful as an MC4 receptor agonist. [Means for Solution] The present inventors studied MC4 receptor agonists, and have found that a piperazine derivative has an MC4 receptor agonistic action, thereby completing the present invention. The piperazine derivative of the present invention has an MC4 receptor agonistic action, and can be used as an agent for preventing or treating bladder and/or urinary tract diseases, in particular, underactive bladder, hypotonic bladder, acontractile bladder, detrusor underactivity, neurogenic bladder, urethral relaxation failure, detrusor-external urethral sphincter dyssynergia, and voiding dysfunctions in benign prostatic hyperplasia.

Abstract: The present invention relates to processes and intermediates for preparing compounds of formula (IA), wherein R1, R4, R5, R6, and L1 are as defined herein. Compounds of formula (IA) have been found useful as EP4 receptor agonists useful in the treatment of glaucoma, osteoporosis, neuropathic pain, and related disorders.

Abstract: The present invention relates to a compound for treating a degenerative disease of central nervous system or a brain tumor, a composition and a use thereof, wherein the compound has the structure of Formula I. These compounds can be used as SGK1 and JNK dual inhibitors with antioxidant effect, which can be formulated into suitable formulations for treating a degenerative disease of central nervous system or a brain tumor.

Abstract: The present invention relates to processes and intermediates for preparing compounds useful as inhibitors of ATR kinase, such as aminopyrazine-isoxazole derivatives and related molecules. The present invention also relates to compounds useful as inhibitors of ATR protein kinase. The invention relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and solid forms of the compounds of this invention. The compounds of this invention have formula I or II: wherein the variables are as defined herein.

Abstract: Indazole sulfonamide derivatives of formula (I), the pharmaceutically acceptable addition salts thereof, the hydrates and/or solvates thereof, and the use of same as inverse agonists of retinoid-related orphan receptor gamma ROR?t are described. Pharmaceutical compositions including such compounds, as well as the use thereof for the topical and/or oral treatment of ROR?t receptor-mediated inflammatory diseases, in particular acne, psoriasis and/or atopic dermatitis are also described.

Abstract: The present invention relates to a process for producing an organic fluoro compound containing [18F]fluorine. The method of the present invention for producing the organic fluoro compound is not only advantageous for producing the organic fluoro compound with high yield by using the solvent represented by formula 1 for nucleophilic fluorination reaction but also suitable for automatic synthesis of 18F-labeled radiopharmaceuticals due to the excellent solubility of the precursor compound in the solvent.

Abstract: Provided herein are compounds, compositions including them, and methods of modulating GPR120 activity and treating diseases mediated by GPR120 by administering such compounds and compositions.

Abstract: Compounds of Formula (I) and (II), or a stereoisomer, tautomer, solvate, prodrug or salt thereof, and methods of use as Janus kinase inhibitors are described herein.

Abstract: The present invention provides for compounds of formula (I) wherein R1, R2, R3, R4, R5, and R6 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions mediated and modulated by CFTR, including cystic fibrosis, Sjögren's syndrome, pancreatic insufficiency, chronic obstructive lung disease, and chronic obstructive airway disease. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).

Abstract: Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.

Abstract: A novel class of fluorinated derivatives of Formula I have been prepared and found to be useful in the treatment of cancers and other disorders related mediated by Bromodomain-Containing Proteins.

Abstract: This disclosure relates to phosphoinositide 3-kinases (PI3Ks) inhibitors such as N-(5-(imidazo[1,2-a]pyridin-6-yl)pyridin-3-yl)sulfonamide derivatives and uses related thereto. In certain embodiments, the disclosure relates to methods of treating PI3K associated diseases or conditions comprising administering an effective amount of a compound disclosed herein to a subject in need thereof. In certain embodiments, the subject is at risk of, exhibiting symptoms of, suffering from, or diagnosed with cancer or a hematological malignancy.

Abstract: A fluorine-containing triazolopyridine represented by formula (I) and a racemate, R-stereoisomer, S-stereoisomer, pharmaceutically acceptable salt, or mixture thereof are described. The triazolopyridine can be used as a positive allosteric modulator of an mGluR2, and is highly selective in activating the mGluR2, exerting no activation or very limited activation of other homologous metabotropic glutamate receptor. The triazolopyridine can thus be used to prepare a product for treating an mGluR2-related disease, such as a central nervous system disease or neurological disease.

Abstract: A compound of Formula (IA), or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for treating a PRC2-mediated disease or disorder: wherein A, R6, R7 and R8 are as defined herein.

Abstract: The present invention relates to a process for preparing halogenated pyridine derivatives of the formula (II) proceeding from compounds of the structure Q-H via intermediates of the formula (IIIa) or (IIIb) in which Q is a structural element where the symbol # indicates the bond to the rest of the molecule and A, Q1, Q2, Q3, Q4, Q5 and Q6 have the definitions given in the description, W is halogen, Y is halogen, CO2R1 or NO2, where R1 is (C1-C6)-alkyl or (C1-C6)-haloalkyl, and R2 is halogen or —O-pivaloyl.

Abstract: The present invention is directed to inhibitors of the interaction of menin with MLL and MLL fusion proteins, pharmaceutical compositions containing the same, and their use in the treatment of cancer and other diseases mediated by the menin-MLL interaction.

Abstract: A process for producing crystals of a compound represented by the following formula (I): by crystallizing the compound from an aqueous solution containing the compound and an inorganic salt, such as sodium chloride. Such crystals can be subjected to lyophilization to provide a lyophilized composition having a desirable storage stability.

Abstract: The present invention is directed to compounds which are beta-lactamase inhibitors. The compounds and their pharmaceutically acceptable salts are useful in combination with beta-lactam antibiotics, for the treatment of bacterial infections, including infections caused by drug resistant organisms, including multi-drug resistant organisms. The present invention includes compounds according to Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of R1, R2, R3, R4, R5 and R6 are described herein.

Abstract: The present invention relates to methods for treating and/or preventing SIRS and/or sepsis comprising the administration of an effective amount of a certain DPP-4 inhibitor, as well as to the use of a certain DPP-4 inhibitor for treating and/or preventing a metabolic disease in a patient with or at risk of SIRS and/or sepsis.

Abstract: The present disclosure provides a Baricitinib intermediate, a method for preparing the Baricitinib intermediate, and a method for preparing Baricitinib or a pharmaceutically acceptable salt thereof using the Baricitinib intermediate. The method for preparing the Baricitinib intermediate involves the use of a divalent palladium catalyst or a nickel catalyst and provides the Baricitinib intermediate in high yield.

Abstract: Provided are isotopologues of isoquinolinone and quinazolinone compounds of formula (AB?) that modulate PI3 kinase activity, processes for the preparation of the compounds, pharmaceutical compositions comprising the compounds, and methods of treatment of diseases and disorders using the compounds or pharmaceutical compositions.

Abstract: The present invention relates to a selective dual delta (?) and gamma (?) PI3K protein kinase modulator (S)—N-(5-(4-amino-1-(1-(5-fluoro-3-(3-fluorophenyl)-4-oxo-4H-chromen-2-yl)ethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-2-methoxyphenyl) methane sulfonamide, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of PI3K kinase mediated diseases or disorders with them.

Abstract: The invention relates to a novel process for preparing spiroketal-substituted cyclic ketoenols which can be used as insecticides, acaricides or herbicides. The present invention also relates to novel intermediates for the preparation of spiroketal-substituted cyclic ketoenols.

Abstract: Disclosed are a class of fused cyclic compounds against the HCMV virus, and use thereof in the preparation of a drugs for treating diseases associated with the HCMV virus. In particular, disclosed is the compound shown in formula (II) and pharmaceutically acceptable salts thereof.

Abstract: Provided herein are novel maytansinoid compounds of general formula I. Also provided herein are conjugates comprising the compounds linked to a binding protein via a linker, and conjugating reagents comprising the compounds attached via a linker to at least one functional group capable of reacting with a binding protein. Also provided herein are pharmaceutical compositions comprising the compounds and conjugates, therapeutic methods and uses involving the compounds and conjugates, for example in cancer therapy, and novel synthetic processes.

Abstract: The present invention relates to salt forms of the phosphoinositide 3-kinase (PI3K) inhibitor (S)-7-(1-(9H-purin-6-ylamino)ethyl)-6-(3-fluorophenyl)-3-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one, pharmaceutical compositions comprising the same, and methods of using the salts and compositions for the treatment of PI3K-associated diseases such as cancer.

Abstract: There is provided a 5,6-dihydro-4H-benzo[b]thieno-[2,3-d]azepine derivative which is useful in the treatment of respiratory syncytial virus (RSV) infection and for the prevention of disease associated with RSV infection. (Formula (I)).

Abstract: Described are precursor compounds and methods for atomic layer deposition of films containing scandium(III) oxide or scandium(III) sulfide. Such films may be utilized as dielectric layers in semiconductor manufacturing processes, particular for depositing dielectric films and the use of such films in various electronic devices.

Abstract: The present invention discloses novel silicon incorporated cyclic compounds of formula I, Wherein Ar1 and Ar2 are individually selected from any aryl group which can be optionally substituted; X is selected from any inorganic anion such as halide, carbonate, sulfate, nitrate or any organic anion selected from acetate, tartarate, citrate, carbonate or organosulfonates such as tosylate, mesylate, triflate; R1 and R2 are individually selected from C1-C8 alkyl, cycloalkyl, aryl, heteroaryl, aralkyl, alkoxyalkyl, aminoalkyl, thioalkyl, haloalkyl or hydroxyalkyl. R1 and R2 together may form a ring which optionally may be substituted or may contain heteroatoms; a pharmaceutical composition comprising a therapeutically effective amount of compounds of general formula I, including geometrical isomers and/or salts thereof along with a drug and optionally along with a carrier or diluent or pharmaceutically acceptable excipient for treating malaria and toxoplasmosis.

Abstract: The invention relates to silane compounds having the general formula (I): SiR1n(R2)4-n (I), as defined herein, to a method for preparing the silane compounds and use thereof as crosslinker or as adhesion promoter and to a curable composition comprising a reaction product of the at least one silane compound, at least one polyorganosiloxane, and at least one catalyst, and use thereof.

Abstract: An integrated circuit (IC) package comprising a substrate having a dielectric, a first structure over at least a portion of the dielectric, the first structure comprising a molecular compound having a ligand coordinating moiety and a second structure over at least a portion of the first structure, the second structure comprising a metal, wherein the first structure is chemically bonded to the dielectric.

Abstract: Large scale (bulk) compositions comprising high-purity stannsoporfin are disclosed, as well as methods of synthesizing such compositions.

Abstract: The present disclosure relates to a novel Group 5 metal compound, a method for preparing the Group 5 metal compound, a precursor composition for depositing a Group 5 metal-containing layer containing the Group 5 metal compound, and a method for depositing a Group 5 metal-containing layer using the precursor composition for depositing a Group 5 metal-containing layer.

Abstract: The present invention relates to a compound comprising at least one phosphepine ring and having the phosphorus atom of the phosphepine ring substituted with at least one monovalent substituent R, a semiconducting material comprising the compound, and electronic device comprising the semiconducting material.

Abstract: The invention relates to a method for preparing substituted thiolactones of formula (I), new substituted thiolactones of formula (I?) that can be obtained by carrying out said method, and the use of substituted thiolactones of formula (I) or (I?) for synthesizing polymers or functionalizing surfaces or polymers.

Abstract: A phosphorescent compound of formula (I): (Formula (I)) wherein: M is a transition metal; L in each occurrence is ON independently a mono- or poly-dentate ligand; R1 is a C4-20 alkyl comprising at least one tertiary carbon atom; R2 is a linear, branched or cyclic C1-20 alkyl group; R3 is a linear, branched or cyclic C1-20 alkyl group or a group of formula —(Ar1)p wherein Ar1 in each occurrence is an unsubstituted or substituted aryl or heteroaryl group and p is at least 1; R4 is a group of formula —(Ar2)q wherein Ar2 in is an unsubstituted or substituted aryl or heteroaryl group and q is at least 1; R5 is a substituent; w is 0 or a positive integer; x is at least 1; and y is 0 or a positive integer. The compound may be used as a blue light-emitting material in an organic light-emitting device.

Abstract: The present invention relates to bi- and trinuclear metal complexes and to electronic devices, in particular organic electroluminescent devices, containing these complexes.

Abstract: Provided herein are formulations, methods and substituted 2?-chloro aminopyrimidinone and pyrimidine dione compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of substituted 2?-chloro aminopyrimidinone and pyrimidine dione compounds.

Abstract: Methods and compounds are disclosed for irreversibly inhibiting a DNA repair enzyme that possesses lyase activity.

Abstract: Enantiomers of 1?,6?-isoneplanocin, including derivatives of the enantiomers of 1?,6?-isoneplanocin, are disclosed along with novel synthetic methods. In particular, a substituted cyclopentane epoxide is synthesized into the enantiomers of 1?,6?-isoneplanocin. Enantiomers of carbocyclic nucleoside analogs of 3-deazaneplanocin to provide D- and L-like 1?,6?-iso-3-deazaneplanocin are also disclosed. The small molecule chemotherapeutic compounds beneficially provide DNA and RNA antiviral activity, demonstrating activity towards, for example, human cytomegalovirus, measles, Ebola, norovirus, dengue, vaccinia and HBV. Compounds exhibiting reduced S-adenosylhomocysteine hydrolase inhibitory effects are disclosed and provide improved toxicity profiles in comparison to neplanocin. The invention provides improved prophylactic and/or therapeutic antiviral efficacy.

Abstract: Disclosed are polynucleotide constructs having a strand linked to a moiety carrying one or more auxiliary moieties. Also disclosed are polynucleotide constructs interrupted with a sugar analogue, and polynucleotide constructs with stereochemical{circumflex over (?)}enriched phosphorothioates. The polynucleotide constructs may be provided as hybridized polynucleotide constructs. Also featured are methods of delivery a polynucleotide construct to a cell and methods of reducing the expression of a protein in a cell by contacting the cell with the disclosed polynucleotide construct or hybridized polynucleotide construct.

Abstract: CRISPR proteins engineered to form covalent bonds with 5? phosphates in target nucleic acids and methods of using CRISPR systems comprising said engineered CRISPR proteins to covalently tag nucleic acids.

Abstract: The invention relates to a compound of Formula (I), or a pharmaceutically acceptable salt thereof: wherein R1 is C1-8 alkyl, C1-8 alkoxy, CN, NO2, amino, COOH, COOCH3, OH, N3, or halogen and R2 is H, OH, C1-8 alkyl, C1-8 alkoxy, C2-C6 alkenyl, halogen, Bn-O—, Bn- optionally substituted, or Ph- optionally substituted.

Abstract: This application is directed to the use of aminosteroid compounds for the selective inhibition of the enzyme PTP1B in a mammal for the treatment of diabetes.

Abstract: The present invention relates to a process for purification a protein comprising a semi-continuous chromatography step whereby the flow-through is collected and re-loaded onto the chromatography matrix.

Abstract: The present invention relates to a peptide having anticancer activity, and a pharmaceutical composition, health functional food composition and functional cosmetic composition for preventing and treating cancer including the same as an active ingredient, and more particularly, to a peptide set forth in SEQ ID NO: 1, wherein the peptide binds to a transcription factor CP2c and has prophylactic and therapeutic activities against cancer, and a pharmaceutical composition, a health functional food composition and a functional cosmetic composition for preventing and treating cancer including the same as an active ingredient.