Abstract: The present invention is directed to a compound of Formula I or Formula III or a pharmaceutically acceptable ester, amide, solvate, or salt thereof, or a salt of such an ester or amide or a solvate of such an ester amide or salt: wherein the definitions R1-R13 and L1-L4 are provided in the disclosure, and wherein R14 is a peptide. The compounds of Formula I may be covalently bonded to a peptide via a linker to provide a compound of Formula III and thereby extend the half-life of the therapeutic compound. The invention is also directed to pharmaceutical compositions of the disclosed compounds, as well as their use in the diagnosis or treatment of diseases.

Abstract: Indoline and tetrahydroquinoline sulfonyl compounds that can inhibit DapE and/or bacterial metallo-62 -lactamases (“MBLs”), such as NDM-1 are disclosed. Also disclosed are methods of treating an individual suffering from a bacterial infection using the compounds disclosed herein.

Abstract: Provided is a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises the following formula: wherein X1, X2, X3, X4, and X5 may be the same or different and each is independently selected from C, N and O; each atom having a dotted line may independently have a double bond or a single bond, provided that valencies at each atom arc maintained; each R1, R2, R3, R4, and R7 may be present or absent and may be the same or different and is selected from H and a substituted or unsubstituted organic group, provided that the number of such R groups present is such that the valencies of X1, X2, X3, X4, and X5 are maintained; one or two R6 groups may be present and are selected from H and a substituted or unsubstituted organic group, provided that the number of R6 groups present is such that the valency of the carbon atom to which they are attached is maintained, and provided that at least one R6 is an organic group comprising an atom doub

Abstract: The present specification provides a compound of formula (I): or a pharmaceutically acceptable salt thereof; a process for preparing such a compound; and to the use of such a compound in the treatment of an ROR? and/or ROR?t mediated disease state.

Abstract: A polymorph III of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N?-[4-(2-methylpropoxy)phenylmethyl]urea tartrate, a preparation method therefor, and a medicinal use. Compared to the existing crystalline forms, the new crystalline form has clear advantages with respect to solubility, stability and the preparation process.

Abstract: The invention relates to compounds of formula (I), wherein R1, R2, R3, R4, R5, and R6 are as defined in the claims. The invention further provides compositions which comprise these compounds and to their use in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi.

Abstract: Lactam compounds of Formula I and their use for the treatment of neurological and psychiatric disorders including schizophrenia, bipolar disorder, anxiety disorder and insomnia is disclosed.

Abstract: The present invention relates to a novel serotonin reuptake inhibitor which also exhibits 5-HT2C antagonistic action (antidepressive and anxiolytic effects), in particular, 5-HT2C inverse agonistic action comprising Compound (1): or a pharmaceutically acceptable salt thereof wherein R1, R2, R3 and R4 are independently hydrogen or C1-6 alkyl etc.; R5 is C4-7 alkyl or —(CR8R9)r-E; R6, R7, R8 and R9 are independently hydrogen, fluorine or C1-6 alkyl; A is C6-10 aryl or heteroaryl etc.; r is 1, 2, 3 or 4; E is C3-8 cycloalkyl or C6-10 aryl etc.; L is oxygen, sulfur or —NR10—; n is 1, 2 or 3; R10 is hydrogen or C1-6 alkyl etc.; and X is hydrogen or halogen etc.

Abstract: Novel compounds having a formula embodiments of a method of making the same, and of a composition comprising them are disclosed herein. Also disclosed are embodiments of a method of treating or preventing a metabolic disorder in a subject, comprising administering to a subject (e.g., via the gastrointestinal tract) a therapeutically effective amount of one or more of the disclosed compounds, thereby activating FXR receptors in the intestines, and treating or preventing a metabolic disorder in the subject. Additionally disclosed are embodiments of a method of treating or preventing inflammation in an intestinal region of a subject, comprising administering to the subject (e.g., via the gastrointestinal tract) a therapeutically effective amount of one or more of the disclosed compounds, thereby activating FXR receptors in the intestines, and thereby treating or preventing inflammation in the intestinal region of the subject.

Abstract: Disclosed are benzamide derivatives useful in slowing the expansion of cancer cells.

Abstract: The invention provides compounds of Formula I, and methods of treating or preventing a bacterial infection in a subject using a compound of Formula I. The invention also provides the use of a compound of Formula I in the manufacture of a medicament for the treatment of a bacterial infection in a subject. The invention further provides a medical device when used in a method of treating or preventing a bacterial infection in a subject and to a medical device comprising the composition of the invention.

Abstract: The disclosure provides processes of preparing compounds of Formula (I) and Formula (IV), their salts, and intermediates thereof, wherein R1? R2? R3, and R7 are defined as set forth in the specification.

Abstract: This invention provides compounds of the formula I: and their pharmaceutically acceptable salts, useful as sodium channel blockers, compositions containing the same, therapeutic methods and uses for the same and processes for preparing the same.

Abstract: The present invention provides methods of inducing proliferation of and/or differentiating cells comprising contacting cells with compounds witin the methods of the invention. The present invention further provides cells obtainable by the methods of the invention.

Abstract: The present invention provides methods and uses of inhibitors of histone deacetylase 11 (HDAC11) in the treatment of diseases and/or disorders, such as, for example, cell proliferative diseases.

Abstract: The present invention provides methods and uses of inhibitors of histone deacetylase 11 (HDAC11) in the treatment of diseases and/or disorders, such as, for example, cell proliferative diseases.

Abstract: Compounds that activate a sphingosine-1-phosphate receptor of the subtype 1 are provided. Certain compounds selectively activate the receptor subtype 1 in relation to the sphinogosine-1-phosphate receptor subtype 3. Uses and methods of inventive compounds for treatment of malconditions wherein activation, agonism, inhibition or antagonism of the S1P1 is medically indicated are provided.

Abstract: Methods of synthesizing 2?(1?H-indole-3?-carbonyl)-thiazole-4-carboxylic acid methyl ester (ITE) and structural analogs thereof. The methods include condensation reactions or condensation and oxidation reactions to form the thiazoline or thiazole moiety of ITE or its structural analogs.

Abstract: The present invention provides a compound having the structure: or a pharmaceutically acceptable salt or ester thereof.

Abstract: Oxathiazin-like compounds, processes for making new oxathiazin-like compounds, compounds useful for making oxathiazin-like compounds, and their uses are disclosed. Processes for efficient and safe manufacture of compounds useful for making oxathiazin-like compounds useful for treating patients suffering from cancers, bacterial infections, fungal infections and/or viral infections by administering oxathiazin-like compounds are also disclosed.

Abstract: Biomass feedstocks (e.g., plant biomass, animal biomass, and municipal waste biomass) are processed to produce useful products, such as fuels. For example, systems are described that can convert feedstock materials to a sugar solution, especially, xylose, which can then be chemically converted to furfural and furfural-derived products.

Abstract: Disclosed herein are processes for producing 2,5-furandicarboxylic acid dialkyl ester. In one embodiment, the process comprises a) contacting 2,5-furan dicarboxylic acid, excess alcohol, and optionally, a catalyst in a reactor at a temperature in the range of from 50° C. to 325° C. and a pressure in the range of between 1 bar to 140 bar to form a liquid phase composition comprising an ester of 2,5-furan dicarboxylic acid, the alcohol and water; b) lowering the temperature of the liquid phase composition to form a crude crystallized ester of 2,5-furan dicarboxylic acid; c) separating the product of step b) to form a solids phase comprising a purified ester of 2,5-furan dicarboxylic acid and a mother liquor comprising alcohol and water; and d) removing at least a portion of the water from the mother liquor. In one embodiment, the 2,5-furan dicarboxylic acid is contacted with an alcohol source and optionally, a catalyst.

Abstract: A method for synthesizing a dicarboxylate containing an aromatic heterocycle is provided. A carboxylic acid containing a heterocycle is provided. A CO32? salt is provided to form a mixture, which converts the carboxylic acid containing an aromatic heterocycle to a carboxylate containing an aromatic heterocycle. CO2 gas is provided to the mixture. The mixture is heated to a temperature to at least partially melt the carboxylate containing an aromatic heterocycle.

Abstract: A compound of formula (I) wherein Z is a group of formula (II) and Core is selected from groups of formula (IIIa) or (IIIb) wherein X is S or O; R1 is a substituent; n is 0 or a positive integer; Ar1 independently in each occurrence is an arylene group; R2 is a substituent; R3 is a substituent; R4 is an arylene or heteroarylene group; Y is C or Si; a is 1, 2 or 3; b is 0 or a positive integer; and c is 0 or a positive integer. The compound of formula (I) may be used as a host for a light-emitting dopant in an organic light-emitting device.

Abstract: The present invention provides compounds represented by formula (1A), or pharmaceutically acceptable salts. Compounds represented by formula (1A), or pharmaceutically acceptable salts thereof, wherein A1 and A2 are identical or different, and each independently —C(?O)B, —C(?O)CR3AR3BB, —CO2B, —C(?S)OB, —CONR3CB, —C(?S)NR3CB, a hydrogen atom, or the like, wherein A1 and A2 are not both hydrogen atoms, wherein B is an optionally substituted 3- to 12-membered monocyclic or polycyclic heterocyclic group, an optionally substituted 3- to 12-membered cyclic amino group, or a group represented by the following formula (B), wherein the 3- to 12-membered monocyclic or polycyclic heterocyclic group and the 3- to 12-membered cyclic amino group have at least one or more secondary nitrogen atoms in the ring; R1 is a hydrogen atom or the like; R2A, R2B, R2C, and R2D are identical or different, and each independently a hydrogen atom or the like; and R8 is alkyl. wherein * denotes a bonding position.

Abstract: Disclosed herein are novel compounds and uses thereof. The present compounds may suppress the activity of farnesyl transferase and thus, may act as modulators of immune cells; therefor, they are useful for the development of a medicament for treating diseases that are associated with or caused by excessive levels of farnesyl transferase or immune response. Also disclosed herein are pharmaceutical compositions containing the present compounds.

Abstract: Provided are a 4-sulfur pentafluoride phenol compound and a preparation method therefor, and a preparation method for a sulfur pentafluoride substituted benzopyran compound. According to the present invention, sulfur pentafluoride salicylaldehyde with multiple substituent groups is synthesized through a plurality of steps by using sulfur pentafluoride phenol as a raw material, and then the sulfur pentafluoride substituted benzopyran compound is synthesized on this basis. The method is simple and convenient, and low in cost; overcomes the defects that, at present, the number of types of sulfur pentafluoride phenols is small, and the synthesis of various sulfur pentafluoride substituted benzopyran compounds cannot be met; and has wide industrial application prospects.

Abstract: Provided herein are compounds I, II or III and compositions useful in increasing PPAR8 activity. The compounds and compositions provided herein are useful for the treatment of PPAR8 related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).

Abstract: The invention relates to new heteroaryl derivatives of the formula wherein X is selected from the group consisting of: N and CH; X is selected from the group consisting of: N and CF; (whith the proviso that at least one of X1 and X2 is N), and A is as defined in the description and claims, to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Abstract: The present invention provides a compound represented by formula (I), or a pharmaceutically acceptable salt, a solvate, an ester, an acid, a metabolite or a prodrug thereof. The compound itself in the present invention or in combination with at least one therapeutic agent can be used for preventing or treating diseases, disorders or symptoms caused by the adjustment of the activity of tyrosine kinase C-KIT, or affected by the activity of the tyrosine kinase C-KIT or involving in the activity of the tyrosine kinase C-KIT, especially cancers or other cell proliferation diseases.

Abstract: A compound having the following formula: or a pharmaceutically acceptable salt thereof. A medicament or pharmaceutical composition contains the compound. A method of treating a respiratory tract disease includes administering to a patient an effective amount of a compound or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof in which q, R11, R12, R13 and R14 are as defined in the specification, for use in therapy.

Abstract: The present disclosure relates to pharmaceutically acceptable salts, cocrystals, and crystalline forms thereof, of a compound which is N—((S)-1-(3-(4-chloro-3-(methylsulfonamido)-1-(2,2,2-trifluoroethyl)-1H-indazol-7-yl)-6-(3-methyl-3-(methylsulfonyl)but-1-yn-1 -yl)pyridin-2-yl)-2-(3,5-difluorophenypethyl)-2- ((3bS,4aR)-5,5-difluoro-3-(trifluoromethyl)-3b,4,4a,5-tetrahydro-1H-cyclopropa[3,4]cyclopenta[1,2-c]pyrazol-1-yl)acetamide, which is useful in the treatment of a Retroviridae viral infection including an infection caused by the HIV virus.

Abstract: Compounds useful as labels with properties comparable to known fluorescent compounds. The compounds are conjugated to proteins and nucleic acids for biological imaging and analysis. Synthesis of the compounds, formation and use of the conjugated compounds, and specific non-limiting examples of each are provided.

Abstract: The present invention relates to lipid compounds and uses thereof. In particular, the compounds include a class of cationic lipids having an amine moiety, such as an amino-amine or an amino-amide moiety. The lipid compounds are useful for in vivo or in vitro delivery of one or more agents (e.g., a polyanionic payload or an antisense payload, such as an RNAi agent).

Abstract: The invention provides methods of synthesizing a viral protease inhibitor in high yield, without using expensive catalysts or challenging reaction conditions.

Abstract: The present invention describes carbazolyl compounds substituted by electron-deficient heteroaryl groups, especially for use as triplet matrix materials in organic electroluminescent devices. The invention further relates to a process for preparing the compounds of the invention and to electronic devices comprising these.

Abstract: Disclosed herein, in part, are fumagillol compounds and methods of use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making fumagillol compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.

Abstract: Disclosed herein, in part, are fumagillol compounds and methods of use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making fumagillol compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.

Abstract: Disclosed herein plant propagation materials, methods of manufacturing, formulations and uses thereof. The plant propagation materials disclosed herein may comprise a strigolactone obtained by a biosynthetic process. The plant propagation material may comprise a chemical mimic of a strigolactone. The strigolactone may be 5-deoxystrigol. Methods of manufacturing the plant propagation materials may comprise a chemical process. Alternatively, methods of manufacturing the plant propagation material may comprise a biosynthetic process. The methods may comprise use of one or more polynucleotides. The polynucleotides may encode a metabolite. The polynucleotides may comprise one or more genes encoding one or more components of a strigolactone pathway.

Abstract: The invention provides improved methods of synthesizing oltipraz, which result in higher overall yield and better purity of the desired product.

Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein Q, Z, R2, R3 and m are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention.

Abstract: Premature termination codon readthrough prodrug compounds, compositions thereof, and methods of making and using the same are provided. In certain embodiments, the compounds are of Formula Ia or a pharmaceutically acceptable salt, solvate, polymorph, hydrate, ester, isomer, stereoisomer, or tautomer thereof, wherein R, A and W are as described herein.

Abstract: The present invention comprises compounds of Formula I and their use in the inhibition of cell proliferation in therapeutic treatments. Pharmaceutical compositions comprising at least one compound of Formula I and at least one pharmaceutical excipient are disclosed, as well as methods of using compounds of Formula I and pharmaceutical compositions thereof for treatment of hyper-proliferative diseases and other disorders.

Abstract: The present disclosure relates generally to compounds of formula (I) or a pharmaceutically acceptable salt, prodrug, deuterated analog, tautomer, stereoisomer, or mixture of stereoisomers thereof and their use as LRRK2 inhibitors.

Abstract: Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.

Abstract: Provided herein are tricyclic small molecule inhibitors of maternal embryonic leucine zipper kinase (MELK). The compounds are useful for treating cancer and other conditions or diseases associated with aberrant MELK expression. Also provided herein are pharmaceutical compositions comprising a tricyclic compound of the invention and a pharmaceutically acceptable carrier. The invention also provides methods of treating cancers associated with over-expression of MELK.

Abstract: Methods of preparing substantially pure SNS-595 substance are disclosed. Also provided are compositions comprising SNS-595 substance that are substantially pure and essentially free of visible particles.

Abstract: The present invention relates to highly soluble, non-fluorescent and photostable myosin inhibitors; especially, for in vivo inhibition of the ATPase activity of neuronal non-muscle myosin 2 of formula (II): wherein Q1, Q2, Q3, Q4, R1, R2, R4 and R5 are as defined in claim 1. The invention also relates to pharmaceutical compositions or medicaments comprising the compounds of the invention and processes for manufacturing these compounds and their intermediates.

Abstract: This disclosure relates amide-sulfamide compounds disclosed herein and uses related to CXCR4 inhibition. In certain embodiments, the compounds have formula I, salts, derivatives, and prodrugs thereof wherein, A is a bridging aryl or heterocyclyl and R1 and R2 are further disclosed herein. In certain embodiments, the disclosure contemplates pharmaceutical compositions comprising compounds disclosed herein. In certain embodiments, the disclosure relates to methods of treating or preventing CXCR4 related diseases or conditions by administering an effective amount of a compound disclosed herein to a subject in need thereof.