Abstract: A systematic screening has revealed a family of compounds that exhibit inhibitory effects on 12/15-lipoxygenase. Accordingly, the present invention relates to the use of these compounds for the inhibition of 12/15-lipoxygenase and for the treatment of a condition involving 12/15-lipoxygenase. Exemplary conditions include, but are not limited to, stroke, periventricular leukomalacia, cardiac arrest with resuscitation, atherosclerosis, Parkinson's disease, Alzheimer's disease, and breast cancer.

Abstract: A novel processes for the preparation of suvorexant (formula I), its related compounds and its intermediates that are simple, economical and commercially viable.

Abstract: There is provided a morpholine derivative represented by General Formula [1A] or a salt thereof. (In the formula, a ring A represents a ring represented by General Formula [I]; * represents a bonding position; Z2 represents CH or the like; Z1 represents CR6 or the like; R6 represents a hydrogen atom or the like; X1 represents CHR7 or the like; R7 represents a hydrogen atom or the like; X2 represents CH2 or the like; R1 and R2 are the same as or different from each other, and each of R1 and R2 represents a hydrogen atom or the like; R3, R4, and R5 are the same as or different from each other, and each of R3, R4, and R5 represents a hydrogen atom, NRaRb, or the like; and each of Ra and Rb represents a hydrogen atom, a C1-8 alkyl group which may have a substituent, or the like.

Abstract: The invention relates to heterocyclic compounds and their use as antibiotics and/or as antibiotic potentiators. The compounds may act as colistin potentiators and SOS inhibitors.

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, W, X1, X2, X3, X4, Y, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and R12 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.

Abstract: The present invention primarily relates to salts of Dasatinib, wherein the salts are in amorphous form. The salts described herein preferably comprise a cation of a compound of formula 1 and an anion of a second compound selected from the group consisting of glutaric acid, nicotinic acid and saccharin. The invention is further related to pharmaceutical compositions comprising such a salt. Furthermore, the invention relates to processes for preparing said salts. The invention also relates to several aspects of using said salt or pharmaceutical composition to treat a disease.

Abstract: The present invention primarily relates to molecular crystalline substances, preferably salts of Dasatinib in crystalline form, comprising a compound of formula 1, preferably a cation of a compound of formula 1, and a second compound selected from the group consisting of glutaric acid, nicotinic acid and saccharin, preferably an anion thereof. The Invention is further related to pharmaceutical compositions comprising such a substance. Furthermore, the Invention relates to processes for preparing said substances. The invention also relates to several aspects of using said substances or pharmaceutical compositions to treat a disease.

Abstract: The present invention embraces compounds that modulate the activity of Epstein-Barr Nuclear Antigen 1 (EBNA1) protein and use thereof in methods for treating latent Epstein-Barr virus infection.

Abstract: The present invention relates to oxazolidin-2-one substituted pyrimidine compounds that act as PI3K (phosphatidylinositol-3-kinase) inhibitors, as well as pharmaceutical compositions thereof, methods for their manufacture and uses for the treatment of conditions, diseases and disorders dependent on PI3K.

Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.

Abstract: The present invention relates to deuterated compounds that are useful for inhibiting Janus kinases and processes and intermediates useful for preparing such compounds.

Abstract: The present invention relates to tricyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.

Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, 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: This invention concerns pyrrolo[3,2-d]pyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treatment and/or therapy of diseases.

Abstract: This invention generally relates to pyrazolo pyrimidine derivatives useful as, inter alia, inhibitors of short chain dehydrogenase/reductase (SDR) family of NAD(P)(H) dependent oxido-reductases. More specifically, the invention relates to pyrazolo pyrimidine derivatives, including derivatives and analogs of SDR inhibitors, pharmaceutical compositions containing derivatives and analogs of SDR inhibitors, methods of making derivatives and analogs of SDR inhibitors and methods of use thereof.

Abstract: An N-alkyl tryptanthrin derivative, a preparation method for same, and an application thereof are provided. The structure of the derivative is as represented by formula I. The N-alkyl tryptanthrin derivative can serve as a highly active IDO inhibitor, for use in preparing a medicament for prevention and/or treatment of a disease having a pathological characteristic of an IDO-mediated tryptophan metabolic pathway.

Abstract: The present invention is directed to novel crystalline forms of pemetrexed tromethamine salts and processes for preparation thereof.

Abstract: The present invention provides novel compounds of any one of Formulae (I) to (IV), and pharmaceutically compositions thereof. Compounds of any one of Formulae (I) to (IV) are believed to be inhibitors of bromodomain-containing proteins (e.g., bromo and extra terminal proteins (BETs)). Also provided are methods, uses, and kits using the inventive compounds and pharmaceutical compositions for inhibiting the activity of the bromodomain-containing proteins and for treating and/or preventing in a subject in need thereof diseases associated with bromodomain-containing proteins, such as proliferative diseases.

Abstract: Polymorphs of a bis-mesylate salt of a compound of Formula (I): or a hydrate thereof, are provided. The bis-mesylate salt may also be depicted as a compound of Formula (IA): Provided herein are also compositions thereof, methods for their preparation and methods for such polymorphs.

Abstract: The disclosure provides novel chemical compounds represented by Formula I or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof. The compounds can be used as an inhibitor of Trk and are useful in the treatment of pain, cancer, inflammation, neurodegenerative disease and certain infectious diseases.

Abstract: The present invention provides heterocyclic compounds for use as kinase inhibitors and in other applications. Also provided are pharmaceutical compositions and methods of treatments of diseases and conditions associated with P13 kinase activity.

Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.

Abstract: There is provided a novel process for the preparation of a compound of formula I, wherein R1, R2 and R3 are as described in the description, by conversion of a corresponding allylic alcohol.

Abstract: The presently described technology provides compositions comprising aryl carboxylic acids and, for example NSAIDs, chemically conjugated to oxycodone (4,5-?-epoxy-14-hydroxy-17-methylmorphinan-6-one) to form novel prodrugs/compositions of oxycodone, including benzoates, salicylates, propionates, fenamates, and acetates, which have a decreased potential for abuse of oxycodone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

Abstract: There is provided a method for producing with a high efficiency a heterocyclic compound that is useful as a raw material for pharamaceuticals. A novel production method for producing 2,2,7,9-tetramethyl-2H-pyrano[2,3-g]quinoline (compound (6)) that has a quinoline ring and a chromene ring using N-(3-acetyl-4-hydroxyphenyl)butylamide (compound (1?)) that is commercially available as a raw material for pharamaceuticals or the like as a starting raw material; and a method for purifying compound (6), characterized by purifying by subjecting it to conversion into a salt form.

Abstract: A chemical compound is provided having a structure that includes at least one donor moiety covalently bonded to at least one acceptor moiety. For example, the compound may include an indolocarbazole moiety covalently bonded to at least one furylpyridine moiety. The compound may exhibit thermally activated delayed fluorescence and an accompanying ?EST of no greater than about 0.25 eV. The compound finds use in OLED display technology.

Abstract: The present invention relates to a process for the manufacture of N-(2-((2R,12bS)-2?-oxo-1,3,4,6,7,12b-hexahydrospiro[benzofuro[2,3-a]quinolizine-2,4?-imida-zolidine]-3?-yl)ethyl)-methanesulfonamide, where in the process trimethylsilyl cyanide is used.

Abstract: This invention relates to thieno[3,2-d]pyrimidines derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.

Abstract: The present disclosure provides compounds of Formula (I-a), Formula (I), and Formula (II). The compounds described herein may be Myc modulators (e.g., Myc inhibitors) and may be useful in treating in a subject in need thereof diseases associated with Myc and proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including a compound described herein.

Abstract: The present invention relates to a process for obtaining rifaximin ? comprising the following steps: a) reacting rifamycin O with 2-amino-4-picoline in the presence of a solvent mixture comprising water and a solvent selected from methyl isobutylketone, ethylacetate and a water soluble solvent; b) obtaining a rifaximin solution by removing the aqueous phase; c) obtaining rifaximin ? from the rifaximin solution, wherein when the solvent is a water soluble solvent, either methyl isobutylketone or ethylacetate is further added in step a). In another aspect the process of the invention relates to a process for obtaining the crystalline form ? of rifaximin comprising the following steps: i) contacting rifaximin or a rifaximin solution with exclusively ethylacetate, ii) obtaining the rifaximin in crystalline form ? by removing ethylacetate.

Abstract: The present invention relates to a novel tricyclic benzoxaborole derivative, a preparation method thereof, and use of antibiotics pharmaceutical composition including the same as an active ingredient.

Abstract: The present invention is a process comprising contacting a compound of formula 6: or a pharmaceutically acceptable salt thereof; with a deprotecting reagent to form a compound of formula A: or a pharmaceutically acceptable salt thereof; where R is H or OR1; R1 and each R1? are protecting groups; R1? is H or OH, and n is 0, 1, 2, 3, 4, or 5.

Abstract: Organoaminosilanes, such as without limitation di-iso-propylaminosilane (DIPAS), are precursors for the deposition of silicon containing films such as silicon-oxide and silicon-nitride films. Described herein are methods to make organoaminosilane compounds, or other compounds such as organoaminodisilanes and organoaminocarbosilanes, via the catalytic hydrosilylation of an imine by a silicon source comprising a hydridosilane.

Abstract: The present invention is directed to a process for the preparation of heterocyclic ester derivatives of formula I wherein A1, SEM, and W1 are as defined herein. Such compounds are useful as intermediates in the synthesis of derivatives useful as protein tyrosine kinase inhibitors, more particularly inhibitors of c-fms kinase.

Abstract: Methods of preparing organosilica materials, which is a polymer comprising independent siloxane units of Formula [Z3Z4SiCH2]3 (I), wherein each Z3 represents a hydroxyl group, a C1-C4 alkoxy group or an oxygen atom bonded to a silicon atom of another siloxane unit and each Z4 represents a hydroxyl group, a C1-C4 alkoxy group, a C1-C4 alkyl group, or an oxygen atom bonded to a silicon atom of another siloxane, in the absence of a structure directing agent and/or porogen are provided herein. Processes of using the organosilica materials, e.g., for gas separation, etc., are also provided herein.

Abstract: Organosilica materials, which are a polymer of at least one independent monomer of Formula [Z1OZ2SiCH2]3 (I), wherein each Z1 represents a hydrogen atom, a C1-C4 alkyl group or a bond to a silicon atom of another monomer and each Z2 represents a hydroxyl group, a C1-C4 alkoxy group, a C1-C6 alkyl group or an oxygen atom bonded to a silicon atom of another monomer and at least one other monomer are provided herein. Processes of using the organosilica materials, e.g., gas separation, etc., are also provided herein.

Abstract: Provided herein are organosilica materials, which is a polymer of at least one monomer of Formula [Z1OZ2OSiCH2]3 (I), wherein each Z1 and Z2 independently represent a hydrogen atom, a C1-C4 alkyl group or a bond to a silicon atom of another monomer. Processes of using the organosilica materials, e.g., for gas separation, are also provided herein.

Abstract: Organosilica materials, which are a polymer of at least one independent monomer of Formula [Z1OZ2OSiCH2]3 (I), wherein Z1 and Z2 each independently represent a hydrogen atom, a C1-C4 alkyl group or a bond to a silicon atom of another monomer and at least one other monomer is provided herein. Methods of preparing and processes of using the organosilica materials, e.g., for gas separation, color removal etc., are also provided herein.

Abstract: The present invention relates to silylated polyisocyanates, to processes for preparing them, to their use, and to coating compositions comprising them.

Abstract: A compound represented by the formula (I) or a salt thereof: wherein a ring Z is a 5 to 6-membered heteroaromatic ring having one or two heteroatoms in the ring; X1 is a hydrogen atom, a hydroxy group, a hydroxy C1-6 alkyl group, —B(OH)2, a boronate ester group, a cyclic boronate ester group, a boranyl group, a cyclic boranyl group, —BF3Mn1, —Sn(R12)(R13)(R14), a leaving group, a carboxy group, a formyl group, or —NR16R17; and X2 is a hydrogen atom or —CO2R18.

Abstract: A photoinitiator mixture comprising the components (a) a compound of the formula (I) wherein Ar and Ar2 independently of each other are or naphthyl which is unsubstituted or substituted one or more times by R1, R2, R3 or R?; R1 and R3 in-dependently of each other are C1-C4alkyl, C1-C4alkoxy or halogen; R2 is hydrogen, C1-C4alkyl, halogen, C1-C4alkoxy or C2-C20alkoxy which is interrupted by one or more O; Q is C1-C4alkylene; R4 is methyl or ethyl; R? and R? independently of each other are hydrogen or PG-Y-R??—X—; PG is a polymerizable group or methyl or ethyl; Y is a direct bond, O or S; X is a direct bond, O or S; R?? is a direct bond, C1-C20alkylene or C2-C20alkylene which is interrupted by one or more O; (b) one or more compounds of the formula (II) wherein Ar1, Ar2 and Q are as defined above, and R5 is for example C3-C30alkyl which is unsubstituted or substituted and (c) optionally a compound of the formula (III) R5—OH ??(III), wherein R5 is as defined above; provides a l

Abstract: The present invention describes dual-modality probes. In particular, the present invention discloses hydroxyapatite specific multimeric bisphosphonate dual-modality MRI and optical probes.

Abstract: If a method for directly functionalizing cycloparaphenylene compounds is developed, such a method is expected to be applied to any cycloparaphenylene compound, thus theoretically enabling introduction of a functional group into all cycloparaphenylene compounds. Therefore, a primary object of the present invention is to provide a method for easily functionalizing cycloparaphenylene compounds directly. A cyclopolyarylene metal complex in which a metal tricarbonyl is coordinated to one benzene ring of a cyclopolyarylene compound is provided. The cyclopolyarylene metal complex is obtained by using a production method comprising the step of reacting a cyclopolyarylene compound with a metal compound represented by the following formula: M(CO)3Ym, wherein M is a metal atom; Y is the same or different, and each represents a ligand; and m is an integer of 1 to 3.

Abstract: N2-phosphinyl amidine compounds, N2-phosphinyl amidinates, N2-phosphinyl amidine metal salt complexes, N2-phosphinyl amidinate metal salt complexes are described. Methods for making N2-phosphinyl amidine compounds, N2-phosphinyl amidinates, N2-phosphinyl amidine metal salt complexes, and N2-phosphinyl amidinate metal salt complexes are also disclosed. Catalyst systems utilizing the N2-phosphinyl amidine metal salt complexes and N2-phosphinyl amidinate metal salt complexes are also disclosed along with the use of the N2-phosphinyl amidine compounds, N2-phosphinyl amidinates, N2-phosphinyl amidine metal salt complexes, and N2-phosphinyl amidinate metal salt complexes for the oligomerization and/or polymerization of olefins.

Abstract: Highly active, recoverable and recyclable transition metal-based metathesis catalysts and their organometallic complexes including dendrimeric complexes are disclosed, including a Ru complex bearing a 1,3-dimesityl-4,5-dihydroimidazol-2-ylidene and styrenyl ether ligand. The heterocyclic ligand significantly enhances the catalytic activity, and the styrenyl ether allows for the easy recovery of the Ru complex. Derivatized catalysts capable of being immobilized on substrate surfaces are also disclosed. The present catalysts can be used to catalyze ring-closing metathesis (RCM), ring-opening (ROM) and cross metatheses (CM) reactions, and promote the efficient formation of various trisubstituted olefins at ambient temperature in high yield.

Abstract: A method of preparing purified decitabine comprises mixing crude decitabine with solvent, such as dimethylacetamide, to form a solution or suspension and forming the purified decitabine from the solution or suspension. The forming step comprises adding an anti-solvent, such as ethanol, to the solution or suspension. The forming step may further comprise after adding ethanol to provide a mixture of dimethylacetamide and ethanol: cooling the mixture; isolating the solid decitabine present in the cooled mixture; and evaporating residual dimethylacetamide and ethanol from the solid decitabine to provide the purified decitabine. The mixture of dimethylacetamide and ethanol may be heated. The purification method preferably results in decitabine having a ratio of the ?-anomer of decitabine to the ?-anomer of decitabine of at least about 99.9:0.1.

Abstract: Described herein are compositions and methods for use in targeted drug delivery using cell receptor binding drug delivery conjugates containing hydrophilic spacer linkers for use in imaging, diagnosing, and/or treating diseases and disease states caused by pathogenic cell populations.

Abstract: The invention relates to methods of preparing nicotinamide riboside and derivatives thereof.

Abstract: A compound of Formula I, a pharmaceutically acceptable salt thereof, a prodrug thereof, or combinations thereof: wherein R1 is H, methyl, or benzyl; R2 is 2-cyanoethyl, 2-methoxycarbonylethyl, or 2-iodoethyl; X is N or S; wherein if X=S, R2=O; Y is C3 or C4; Z1 is O, S, N, or CH2; and Z2 is N or CR4, wherein R4 is a halogen, alkyl, aryl or a 5- or 6-membered heterocycle; and wherein said compound is selective for DOT1L Methyl Transferase.

Abstract: The application provides methods for treatment or prophylaxis of dengue virus mediated diseases with compounds of Formula I wherein R1, R2a, R2b, R3, R4, R5 R6, R8a, R9 and R10 are as defined herein. The application further discloses methods for treatment or prophylaxis of dengue virus mediated diseases with pharmaceutical compositions comprising compounds of Formula I.