Abstract: Provided herein are polyol estolide compounds. Polyol estolides may be prepared by contacting a polyol with an estolide compound. Also provided are compositions containing polyol estolides and methods of making the same.

Abstract: The invention provides compounds and monomers having a carbonate linkage. The monomers can be used to form homopolymers or can be coupled with other monomers to provide a wide variety of non-homopolymers. The invention further provides a wide variety of compositions comprising the compounds, monomers, and polymers. In the exemplary structures below, Q, A, R, and n are as described herein.

Abstract: Aqueous solution containing in the range of from 60.5 to 75% by weight of a mixture of trialkalimetal salts of the L- and D-enantiomers of methyl glycine diacetic acid (MGDA), said mixture containing predominantly the respective L-isomer with an enantiomeric excess (ee) in the range of from 3 to 97%, wherein said trialkali metal salts have the general formula (I) [CH3—CH(COO)—N(CH2—COO)2]K3-xNax (I) wherein x is in the range of from zero to 2.9.

Abstract: The invention relates to solid pharmaceutical compositions comprising (Z)-2-cyano-3-hydroxy-but-2-enoic acid-(4?-trifluoromethylphenyl)-amide, as well as a process for the preparation of the same, methods of using such compositions to treat subjects suffering from autoimmune diseases in particular systemic lupus erythematosus or chronic graft-versus-host disease, multiple sclerosis or rheumatoid arthritis.

Abstract: The present invention relates to a novel amino-phenyl-sulfonyl-acetate derivative or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition for preventing or treating diabetes comprising the same as an active ingredient.

Abstract: The application discloses pharmaceutical compounds of formula I useful for treating CNS diseases wherein m, s, R1 R5, R6 and R7 are as defined herein.

Abstract: The present invention provides a polythiol composition containing, as the main component, a polythiol compound (a) having two or more mercapto groups, and containing 0.5% by mass or less of a nitrogen-containing compound (b) in which at least one mercapto group in the polythiol compound (a) is substituted with a group represented by formula (1).

Abstract: A salt having a group represented by the formula (aa): wherein Xa and Xb independently each represent an oxygen atom or a sulfur atom, the ring W represents a C3-C36 heterocyclic ring which has an ester bond or a thioester bond, said heterocyclic ring optionally further having an oxygen atom, a sulfur atom, a carbonyl group or a sulfonyl group each by which a methylene group has been replaced, and said heterocycilic ring optionally having a hydroxyl group, a cyano group, a carboxyl group, a C1-C12 alkyl group, a C1-C12 alkoxy group, a C2-C13 alkoxycarbonyl group, a C2-C13 acyl group, a C2-C13 acyloxy group, a C3-C12 alicyclic hydrocarbon group, a C6-C10 aromatic hydrocarbon group or any combination of these groups each by which a hydrogen atom has been replaced, and * represents a binding position.

Abstract: The present invention relates to ligation agents and their use in making an amide ligation product. Methods of making the ligation agents are also disclosed.

Abstract: Provided herein are compounds that bind to androgen receptors and/or modulate activity of androgen receptors. Also provided are methods for making and using such compounds. Also provided are compositions including such compounds and methods for making and using such compositions.

Abstract: The present disclosure provides pyrrolidine carboxamide compounds having Formula I and the pharmaceutically acceptable salts and solvates thereof, wherein A, B, X, Y, and Z are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of SMYD proteins such as SMYD3 or SMYD2. Compounds of the present disclosure are especially useful for treating cancer.

Abstract: The present invention provides Octahydrocyclopentapyrrole compounds having the structure: (structurally represented) wherein psi is absent or present, and when present is a bond; R1, R2, R3, R4, and R5 are each independently H, halogen, CF, or C1-C4 alkyl; R6 is absent or present, and when present is H, OH, or halogen; A is absent or present, and when present is C(O) or C(O)NH; B is substituted or unsubstituted monocycle, bicycle, heteromonocycle, heterobicycle, benzyl, CO2H or (C1-C4 alkyl)-CO2H, wherein when B is CO2H, then A is present and is C(O); and when psi is present, then R6 is absent and when psi is absent, then R6 is present, or a pharmaceutically acceptable salt thereof, for treatment of diseases characterized by excessive lipofuscin accumulation in the retina.

Abstract: The present invention relates to an improved process for the preparation of [[2(S)-[[4(R)-(3-hydroxyphenyl)-3(R),4-dimethyl-1-piperidinyl]methyl]-1-oxo-3-phenylpropyl]amino]acetic acid dihydrate, represented by the following structural formula (I).

Abstract: Compounds of Formula I which are derivatives of 3-Hydroxypyridin-4-ones. The compounds may be used in treatment of a medical condition related to a toxic concentration of iron. The compounds may be used for preparation of a medicament for treatment of a medical condition related to a toxic concentration of iron. The medical condition related to a toxic concentration of iron may be selected from the group consisting of: cancer, pulmonary disease, progressive kidney disease and Friedreich's ataxia.

Abstract: 4-Alkoxy-3-hydroxypicolinic acids may be conveniently prepared from 2-hydroxypicolinonitrile in a series of chemical steps selected from chlorination, chloro substitution, nitrile hydrolysis and chloro reduction.

Abstract: The present invention relates to a process for the preparation of 4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluophenoxy]-N-methylpyridine-2-carboxamide compound of formula-I, its amorphous form and its crystalline polymorph-I which is represented by the following structural formula: (I)

Abstract: Provided herein are a quinolinone compound, pharmaceutical composition thereof, and use of the compound or the pharmaceutical composition in drug preparation, the drug being used to prevent, manage, treat or relieve diseases related to HIF and/or EPO of a patient, including anemia, vascular disease, myocardial ischemia, dysmetabolism, or for wound healing.

Abstract: Backfunctionalized imidazolinium salts and methods of synthesizing the same and NHC carbene-metal complexes therefrom. For backfunctionalized imidazolinium salts of the formula: Wherein R1 is selected from the group consisting of an ester group, an amide group, and an aromatic group; R2 is selected from the group consisting of hydrogen, an ester group, an amide group, and an aromatic group; R3 and R4 are each an aliphatic group; and X is an anion; the method comprises cyclization of a halogenated acrylate with Hünig's base in a solvent.

Abstract: A novel imidazole compound that yields a surface treatment liquid that is very effective at suppressing migration and oxidation of a wiring surface; a metal surface treatment liquid that contains the imidazole compound; a metal surface treatment method that uses the metal surface treatment liquid; and a laminate production method that uses the surface treatment liquid. A metal is surface-treated using the surface treatment liquid which includes a saturated fatty acid or a saturated fatty acid ester of a specific structure, in which a prescribed position is substituted by an aromatic group of a prescribed structure and an imidazolyl group that may have a substituent group.

Abstract: The present invention concerns compounds belonging to the family of fluorinated pyridazin-3-ones, for the use thereof in the treatment of broncho-pulmonary conditions. In compounds having a formula, or a pharmaceutically acceptable salt of the compound, the formula includes R1 representing H, an alkyl, an aryl or a heteroaryl; either E2 and E3 representing, separately from each other, H, an alkyl, an aryl or a heteroaryl, or R2 and R3 being bridged within a same cycle or via several cycles; and F representing CF3, (CF2)nCF3 or CF2H, with n representing an integer of between 1 and 7.

Abstract: The present invention concerns compounds of Formula I that inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.

Abstract: The invention provides processes for preparing a compound of formula I and salts thereof, wherein R1 is defined herein, and compounds and intermediates of said formula.

Abstract: The present disclosure relates to processes for preparing (cyclopentyl[d]pyrimidin-4-yl)piperazine compounds, and more particularly relates to processes for preparing (R)-4-(5-methyl-7-oxo-6,7-dihydro-5H-cyclopenta[d] pyrimidin-4-yl)piperazine and N-protected derivatives thereof, which may be used as an intermediate in the synthesis of Ipatasertib (i.e., (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)-propan-1-one). The present disclosure additionally relates to various compounds that are intermediates employed in these processes.

Abstract: Disclosed are a quinazoline derivative, a preparation method therefor, and a pharmaceutical composition and an application thereof. The present invention provides a compound represented by general formula I, a stereoisomer thereof and a pharmaceutical acceptable salt or a solvate thereof. The quinazoline derivative of the present invention has a unique chemical structure, is characterized by irreversibly inhibiting EGFR tyrosine kinase, has high biological activity, apparently improves the inhibiting effect on the EGFR tyrosine kinase, has quite strong tumor inhibiting effect on tumor cells and a transplantation tumor pathological model of animal tumors, and has good market developing prospects.

Abstract: Herein are provided, inter alia, compounds capable of modulating the level of activity of low molecular weight protein tyrosine phosphatase (LMPTP) and methods of using the same. In embodiments, the compound has a structure according to Formula (I-A).

Abstract: The invention provides compounds which inhibit or modulate the activity of Chk-1 kinase and which are useful in the treatment of cancer.

Abstract: An object is to provide a novel production method suitable for industrial production of a 3,3-dimethyl-3,4-dihydro-1H-quinoxalin-2-one derivative and a synthetic intermediate for the method.

Abstract: The present invention provides compounds of Formula (I): wherein A, X and Y are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are myeloperoxidase (MPO) inhibitors and/or eosinophil peroxidase (EPX) inhibitors, which may be used as medicaments.

Abstract: The present invention relates to a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof, wherein: R1 is alkyl, Cl, F or Br; R2 is H or F; R3 is selected from H and alkyl; R4 is selected from H and C(O)R6; R5 is H; or R4 and R5 are linked to form a heterocyclic group which is optionally substituted with one or more R10 groups; R6 is selected from R7, OR7 and NR8R9; R7, R8 and R9 are each independently selected from alkyl, cycloalkyl, aralkyl, cycloalkenyl, heterocyclyl and aryl, each of which is optionally substituted with one or more R10 groups; each R10 is independently selected from halogen, OH, CN, NO2, COO-alkyl, aralkyl, SO2-alkyl, SO2-aryl, COOH, CO-alkyl, CO-aryl, NH2, NH-alkyl, N(alkyl)2, CF3, alkyl and alkoxy; X and Z are each independently CR11, and Y is selected from CR11 and N; and R11 is H or F; for use in treating a disorder associated with protein misfolding stress and in particular associated with accumulation of misfolded proteins.

Abstract: The present invention relates to a novel process for preparing dihydroisoxazole derivatives.

Abstract: The invention relates to tetrahydrofuran derivatives of the formula (I) in which the radical R1 has the definition (CH2?CH—CO—O—(CHR3—CH2—O)m—CH2)— and the radical R2 has the definition (CH2?CH—CO—O—(CHR4—CH2—O)n—CH2)—, in which the radicals R3 and R4 independently of one another are hydrogen or methyl, and with the proviso that the sum of the indices m and n is a number in the range from 0 to 20. The compounds (I) are suitable for coating the surfaces of solid substrates, more particularly for coating plastics.

Abstract: The present invention relates to a process for preparing an ester having formula R—COO—R? (I), wherein R represents a group selected from: (i) a linear or branched alkyl, containing from 1 to 20 carbon atoms, (ii) an aryl containing from 6 to 12 carbon atoms, (iii) a heterocycle with 4 to 12 carbon atoms containing at least one heteroatom selected from O, N, P and S, R? represents a linear or branched alkyl containing from 1 to 12 carbon atoms, said process comprising at least a phase of reacting a reaction mixture comprising at least one aldehyde having formula R—CHO (II), wherein R has the meanings defined above, and at least one alcohol having general formula R?—OH (III), wherein R? has the meanings defined above, in the presence of at least one solid basic catalyst, at a temperature within the range of 120° C.-300° C., obtaining said ester having formula (I).

Abstract: Methods for providing effective, efficient and convenient ways of producing 2-5-furandicarboxylic acid are presented. In addition, compositions of 2-5-furandicarboxylic acid including 2-5-furandicarboxylic acid, and at toast one byproduct are preserved, in some aspects, 4-deoxy-S-dehydroglucaric acid is dehydrated to obtain the 2-5-furandicarboxylic acid, A solvents catalyst, and/or reactant may be combined with the 4-deoxy-S-dehydroglucaric acid to produce a reaction product including the 2-5-furandicarboxylic acid. In some arrangements, the reaction product may additionally include water and/or byproducts.

Abstract: The present invention discloses a process for synthesis of chiral 2,4-disubstituted-tetrahydropyran-4-ol and its derivatives having a general formula (I) comprising of asymmetric reaction of an aliphatic aldehyde and a homoallylic alcohol in the presence of a chiral organocatalyst, and a fragrance and cosmetic composition containing chirally enriched molecules of the said general formula (I) prepared by the aforesaid process.

Abstract: Methods for recovering monomers from polymers, such as polyurethanes (including thermoset polyurethanes) include heating the polymer to depolymerize the polymer and release the monomer. The monomer may be directly recovered. The polymer may include a poly(?-methyl-?-valerolactone) (PMVL) block and the monomer recovered may be ?-methyl-?-valerolactone (MVL).

Abstract: According to the present invention, it is possible to provide an optical material composition that contains an episulfide compound represented by formula (1) and an episulfide compound represented by formula (2). According to this optical material composition, it is possible to suppress a reduction in the yield rate caused by molding defects, and possible to obtain an optical material having excellent dyeability. (In formula (1), m and p are each an integer between 0 and 4, and n and q are each an integer between 0 and 2.) (In formula (2), m is an integer between 0 and 4 and n is an integer between 0 and 2.

Abstract: A method for preparing Alectinib (Alectinib, I), comprising the preparation steps: subjecting 6-cyano-1H-indole-3-carboxylate and 4-ethyl-3-(4-morpholine-4-yl-piperidine-1-yl)-?,?-dimethylbenzyl alcohol to condensation, hydrolyzing and cyclization reaction so as to prepare Alectinib (I). The preparation method has easily available raw materials and a simple process, and is economical and environmentally friendly and suitable for industrial production.

Abstract: Compounds having formula (I) are described. Also described, are methods of using these compounds to treat diseases, conditions, and disorders.

Abstract: A crystal form of rimsulfuron is provided that exhibits improved solubility and decreased viscosity. Furthermore, a process for its preparation is provided. The novel crystal form is particularly suitable for use in herbicidal compositions and in the control of unwanted plant growth.

Abstract: The present invention is directed to compounds having the Formulae (Ia-Ie), (II), (IIIa-IIId), (IVa-IVc), (Va-Vb), (VIa-VIe), (VII), (VIIIa-VIIIc), and (IX), pharmaceutically acceptable salts, prodrugs and solvates thereof, compositions of any of thereof and methods for the treatment of a condition associated with a dysfunction in proteostasis comprising an effective amount of these compounds.

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: The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including Respiratory and Gastro-Intestinal diseases.

Abstract: Provided are novel compounds of Formula (I): pharmaceutically acceptable salts thereof, and pharmaceutical composition thereof, which are useful as dual Hsp90/TRAP1 inhibitors. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I) and their use in treating one or more cancers.

Abstract: A process for the preparation of canagliflozin. The process may be effectively implemented on an industrial scale. Several compounds useful as intermediates for the synthesis of canagliflozin (Formula 4, Formula 4a, Formula 4b and Formula 5) are also disclosed. The process involves the reduction of the compound of formula 3 in the presence of a metal hydride and an organic solvent to obtain the compound of formula 4, converting this into a compound of formula 5 which in turn is converted into canagliflozin.

Abstract: The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula I: as defined in the specification. The invention is also directed to compositions containing and uses of the compounds of formula I.

Abstract: The present invention relates to processes for the preparation of thietane derivatives of the formula IA and thietane derivatives of the formula IB wherein R1, R2, A1, A2, A3, A4, B, and n are as defined in the claims. The invention also relates to intermediates useful in the processes, as well as the compounds of formula IA and IB and their use as pesticides.

Abstract: The present invention provides: a novel compound which is characterized by being capable of increasing the number of heart beats or a blood pressure mildly to improve hemodynamics, and which is useful as a therapeutic or prophylactic agent for atrial fibrillation and heart failure; and a pharmaceutical composition which contains the compound. The present invention relates to: an optical isomer of a 1,4-benzothiazepine-1-oxide derivative represented by general formula [II] (wherein R represents a hydrogen atom or a hydroxy group; and * indicates the presence of an optical isomer) or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition which contains the optical isomer or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides compounds having the general structural formula (I) (I) and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis and proliferation, and where anti-fibrotic or anti-proliferative activity is beneficial.

Abstract: There are provided: 4-methyl-2-[4-(2-methylpropoxy)-3-(1H-1,2,3,4-tetrazol-1-yl)phenyl]-1,3-thiazole-5-carboxylic acid, a sodium salt thereof and crystals of these, useful as a therapeutic agent and a prophylactic agent for gout, hyperuricemia and the like, and a method for producing the same.

Abstract: The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase L1 (UCHL1). The invention further relates to the use of DUB inhibitors in the treatment of cancer and other indications. Compounds of the invention include compounds having the formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 to R8 are as defined herein.