Abstract: The invention relates to a process for preparing a carboxylic ester by reacting an aldehyde in the presence of an aluminum alkoxide, wherein the aluminum alkoxide is obtained either by reacting an aluminum hydride with an aldehyde or by reacting a different aluminum alkoxide with a carboxylic ester.

Abstract: A composition comprising a) a quaternary trialkylalkanolamine hydroxide and b) at least one diamine as component b), which is selected from the group consisting of 1-amino-4-methylpiperazine, 1,2-diaminopropane and mixtures thereof.

Abstract: A solid form of RAD1901-2HCl having an X-ray powder diffraction pattern comprising a peak, in terms of 2-theta, at 11.53 degrees 2?±0.2 degrees 2?, and compositions, methods, and processes thereof.

Abstract: High purity 2-naphthylacetonitrile with fewer impurities can be used as a starting material or intermediate for synthesizing various pharmaceutical products, agricultural chemicals, and chemical products, and a production method thereof. A high purity 2-naphthylacetonitrile having an HPLC purity of 2-naphthylacetonitrile of not less than 95 area %, and containing naphthalene compounds represented by the formulas (a)-(j) at a content of a predetermined area % or below. A method for producing high purity 2-naphthylacetonitrile, may include: subjecting 2?-acetonaphthone to a Willgerodt reaction in the presence of an additive where necessary, and hydrolyzing the obtained amide compound to give 2-naphthylacetic acid; and reacting the 2-naphthylacetic acid obtained in the subjecting, a halogenating agent and sulfamide in the presence of a catalyst as necessary in an organic solvent to give 2-naphthylacetonitrile.

Abstract: A process for synthesis of urea from ammonia and carbon dioxide comprising the synthesis of urea in parallel in a first urea reactor (1) at a first urea synthesis pressure and in a second urea reactor (2) at a second and lower urea synthesis pressure; a stripping step of the reaction effluent of the first reactor, which is performed in a stripper (4) operating at a stripping pressure lower than the first urea synthesis pressure; the reaction effluent (21) of the second reactor (2) and the stripper liquid effluent (11) are sent to a recovery section (13) where a carbamate-containing recycle solution (17) is produced, and said recycle solution (17) is sent partly to said first reactor and partly to said second reactor.

Abstract: Disclosed herein, inter alia, are inhibitors of alpha 2 beta 1 integrin and methods of using the same.

Abstract: A method for producing a maleimide compound having a group represented by the formula (a1), the method including condensing a primary amino group in a raw material compound having the primary amino group and dicarboxylic anhydride represented by the formula (a2) to generate a group represented by the formula (a3); and heating a compound having the group represented by the formula (a3), and converting the group represented by the formula (a3) into the group represented by the formula (a1).

Abstract: Syntheses of compounds of Formula III from compounds of Formula I via compounds of Formula II are described, as well as particular compounds of Formula III, or pharmaceutically acceptable salts thereof, compositions comprising such compounds, and uses thereof. For example, certain of these compounds and compositions of Formula III have uses in the treatment of psychiatric or neurological disorders.

Abstract: Provided herein are compounds of Formula (I), or pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R8, R9, X, Y, Z, W, and m are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) or pharmaceutically acceptable salt thereof and a pharmaceutically acceptable excipient.

Abstract: The present application relates to compounds which are integrin antagonists. Methods of preparing the integrin antagonists and methods of treating diseases and disorders associated with abnormal levels and/or expression of one or more integrins are also provided.

Abstract: The present disclosure is concerned with small molecule modulators of KLF15 signaling useful for treating various disorders such as, for example, kidney disease (e.g., chronic kidney disease), heart disease, obesity, or a neurodegenerative disorder (e.g., amyotrophic lateral sclerosis (ALS), Alzheimer's disease, Parkinson's disease, spinal muscular atrophy, traumatic brain injury, vascular dementia, Huntington's disease, mental retardation, and attention deficit and hyperactivity disorder (ADHD)). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: One embodiment of the invention relates to the treatment of diseases associated with increased butyrylcholinesterase (BuChE) enzyme activity such Alzheimer's Disease (AD), involving administering an effective amount of a compound selected from a group of new N, N?-disubstituted benzylamine derivatives (1-8) of 4-aminoantipyrine (ampyrone). The kinetic studies of two potent compounds 4-(Bis(4-iodobenzyl) amino)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one (5) (IC50=2.43±0.4 and Ki=5.67±0.5 ?M) and 4-(Bis(2-bromobenzyl) amino)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one (6) (IC50=0.7±0.2 and Ki=2.4±0.4 ?M), revealed them as a competitive and a non-competitive inhibitor of BuChE, respectively. Galantamine Hydrobromide was used as standard inhibitor with IC50=40.83±0.4 and Ki=21.5±0.7 ?M (Mixed type Inhibitor). The metabolite of aminophenazone, 4-aminoantipyrine (A) is also being reported here as an inhibitor of BuChE for the first time.

Abstract: Disclosed herein are compounds that are inhibitors of BDR4 and their use in the treatment of cancer. Methods of screening for selective inhibitors of BDR4 are also disclosed. In certain aspects, disclosed are compounds of Formula I through IV.

Abstract: The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

Abstract: A metallic salt including at least one anion having a heterocyclic aromatic structure represented by one of Formulae 1 to 3; and a metallic cation: wherein, in Formulae 1 to 3, each X is independently N, P, or As, one of A1 and A2 is an electron-donating group, and the other one is an electron-withdrawing group, ring Ar1 and ring Ar2 are as defined herein, L is a linker group as defined herein, m is an integer from 1 to 5, and n is an integer from 0 to 5.

Abstract: Methods are provided for modulating MRGPR X4 generally, or for treating a MRGPR X4 dependent condition more specifically, by contacting the MRGPR X4 or administering to a subject in need thereof, respectively, an effective amount of a compound having the structure of Formula (I): or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein n, x, A, Q1, Q2, Z, R, R1, R2, R3, R4 and R5 are as defined herein. Pharmaceutical compositions containing such compounds, as well as to compounds themselves, are also provided.

Abstract: The present disclosure generally relates to compounds and pharmaceutical compositions that may be used in methods of treating cancer.

Abstract: The invention relates to crystalline forms of a 3-substituted 1,2,4-oxadiazole compound, including an anhydrous crystalline form, methods of their preparation, and related pharmaceutical preparations thereof. The invention also relates to preparations suitable for pharmaceutical, veterinary, and agriculturally-relevant uses.

Abstract: Various aspects of this disclosure relate to gas phase methods to decarboxylate cannabinoid carboxylic acids.

Abstract: Disclosed are novel compounds of Chemical Formula 1, optical isomers of the compounds, and pharmaceutically acceptable salts of the compounds or the optical isomers. The compounds, isomers, and salts exhibit excellent activity as GLP-1 receptor agonists. In particular, they, as GLP-1 receptor agonists, exhibit excellent glucose tolerance, thus having a great potential to be used as therapeutic agents for metabolic diseases. Moreover, they exhibit excellent pharmacological safety for cardiovascular systems.

Abstract: The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof: The compounds, compositions, methods and kits of the invention are useful for the treatment of pain, itch, and neurogenic inflammation.

Abstract: The invention discloses compounds for treatment or prevention of liver diseases. The compounds are compounds represented by a formula (I) or (II), optical isomers or pharmaceutically acceptable salts of the compounds. The compounds and optical isomers or pharmaceutically acceptable salts of the compounds can be applied to preparation of drugs for treatment or prevention of liver diseases.

Abstract: Benzoxazine compounds, methods of making them, polymers made therefrom and methods of polymerizing the benzoxazines. These renewable benzoxazine monomers and polymers that utilize the variety of building blocks found in renewable plant biomass, demonstrate excellent processability and large temperature windows for processing of resin systems.

Abstract: The present invention relates to indane compounds, methods of making them, pharmaceutical compositions containing them and their use as NRF2 activators.

Abstract: This invention relates to compounds. More specifically, the invention relates to compounds useful as inhibitors of the Wnt signalling pathway. Specifically, inhibitors of Porcupine (Porcn) are contemplated by the invention. In addition the invention contemplates processes to prepare the compounds and uses of the compounds. The compounds of the invention may therefore be used in treating conditions mediated by the Wnt signalling pathway, for example treating cancer, sarcoma, melanoma, skin cancer, haematological tumors, lymphoma, carcinoma, and leukemia; or enhancing the effectiveness of an anti-cancer treatment.

Abstract: Provided herein is a bulk composition comprising the trihydrate form of (3S, 4R, 3?R)-6-[4-(4-amino-5-chloro-2-methoxy-benzoylamino)-3-methoxy-piperidin-1-yl]-hexanoic acid 1-azabicyclo[2.2.2]oct-3?-yl ester di-hydrochloride salt. Provided are also pharmaceutical compositions and dosage forms comprising the trihydrate form, and methods and uses for treating a gastrointestinal disorder in a subject with the trihydrate form. In some embodiments, the gastrointestinal disorder is gastroesophageal reflux disease (GERD), dyspepsia (such as functional dyspepsia or functional motility disorder), gastroparesis, paralytic ileus, post-operative ileus, emesis, nausea, heartburn, intestinal pseudo-obstruction, irritable bowel syndrome (IBS), constipation, enteral feeding intolerance (EFI), or esophagitis. In some embodiments, the gastrointestinal disorder is post-operative ileus, chronic grass sickness, constipation, megacolon, gastritis, gastrointestinal stasis, or abomasal emptying defect.

Abstract: The invention relates to new bicyclic heterocycle compounds, to pharmaceutical compositions comprising the compounds and to the use of the compounds in the treatment of diseases, e.g. cancer.

Abstract: A morphinan derivative represented by the following general formula (I): wherein R1 represents hydrogen, C1-10 alkyl, cycloalkylalkyl where the cycloalkyl moiety has 3 to 6 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms, etc.; R2 represents heterocyclic ring containing 1 to 4 heteroatoms selected from N, O and S and at least one carbon atom as ring-constituting atoms, containing at least one set of adjacent ring-constituting atoms bound by a double bond, and further substituted with at least one oxo group; Y binds to a carbon atom as a ring-constituting atom of R2; R3, R4, and R5 represent hydrogen, hydroxy, etc.; R6a and R6b represent hydrogen, etc.; R7 and R8 represent hydrogen, etc.; R9 and R10, which are the same or different, represent hydrogen, etc.; X represents O or CH2; and Y represents C(?O)); a tautomer or stereoisomer of the compound, or a pharmaceutically acceptable salt thereof, or a solvate thereof is used as an anxiolytic drug, antidepressant, etc.

Abstract: Described herein are compounds of Formula I: and their pharmaceutically acceptable salts, wherein R1, R2, R3, X1, Y1, Y2, Y3, Y4 and Y5 are defined herein; their use as MC4R antagonists; pharmaceutical compositions containing such compounds and salts; the use of such compounds and salts to treat, for example, cachexia, anorexia, or anorexia nervosa; and intermediates and processes for preparing such compounds and salts.

Abstract: The invention relates to N2,N6-disubstituted-9-(2-oxacycloalkyl)-9H-purine-2, 6-diamine derivatives and their use as drugs and cosmetics. The compounds of the present invention exhibit a number of biological activities associated with oxidative stress inhibition, especially anti-aging, anti-inflammatory and anti-neurodegenerative biological activities. The invention also relates to cosmetic and pharmaceutical compositions containing such derivatives as active agents.

Abstract: The present invention relates to compounds of formula (1). The compounds are suitable for use in electronic devices, in particular organic electroluminescent devices, comprising these compounds. In some embodiments, the compounds are used as matrix materials for phosphorescent or fluorescent emitters as well as a hole-blocking or electron-transport.

Abstract: Rabeximod compounds selected from HCl salts, methane sulphonic acid salts and malonic acid salts of Rabeximod. Also, a pharmaceutical composition including a Rabeximod compound, and optionally a pharmaceutically acceptable additive. Further, a method for treatment of a mammal, such as a human subject, suffering from or diagnosed with rheumatoid arthritis, preferably moderate rheumatoid arthritis, severe rheumatoid arthritis or moderate to severe rheumatoid arthritis. The method includes administering to the mammal subject an amount of a Rabeximod compound effective to treat the rheumatoid arthritis.

Abstract: This invention is in the area of cell cycle inhibiting compounds for the treatment of disorders involving abnormal cellular proliferation, and include selective CDK2 inhibitors for medical therapy and their pharmaceutically acceptable salts and compositions.

Abstract: The present invention provides a compound having a Pim-1 inhibitory activity. The present invention provides a compound of Formula [I] or a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing the same, and a pharmaceutical use thereof, and the like. wherein each symbol is as defined in the description.

Abstract: The invention provides methods for the synthesis of eribulin or a pharmaceutically acceptable salt thereof (e.g., eribulin mesylate) through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Homer-Wadsworth-Emmons olefination), Dieckmann reaction, catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic intermediate. The invention also provides compounds useful as intermediates in the synthesis of eribulin or a pharmaceutically acceptable salt thereof and methods for preparing the same.

Abstract: The invention relates to the compounds or its pharmaceutical acceptable polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, formula II, formula III, formula IV and formula V and the methods for the treatment of xerostomia may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, lozenge, spray, intravenous, oral solution, buccal mucosal layer tablet, parenteral administration, syrup, or injection. Such compositions may be used to treatment of oral mucosal inflammatory, dry mouth or oral dry mouth mediated infectious diseases.

Abstract: The present invention provides compounds and pharmaceutical compositions including the compounds for the treatment of a skin disease associated with proteolytic activity of one or more KLK proteases, wherein the compounds are according to formula (I): wherein R is as described herein.

Abstract: The present disclosure provides for methods for preparing tricyclic PI3K inhibitor compounds in high yield and purity in aqueous solvent systems.

Abstract: Disclosed herein are methods of purifying compounds useful for the deposition of high purity tin oxide and high purity compounds purified by those methods. Such compounds are those of the Formula as follows Rx—Sn-A4-x, wherein: A is selected from the group consisting of (YaR?z) and a 3- to 7-membered N-containing heterocyclic group; each R group is independently selected from the group consisting of an alkyl or aryl group having from 1 to 10 carbon atoms; each R? group is independently selected from the group consisting of an alkyl, acyl or aryl group having from 1 to 10 carbon atoms; x is an integer from 0 to 4; a is an integer from 0 to 1; Y is selected from the group consisting of N, O, S, and P; and z is 1 when Y is O, S or when Y is absent and z is 2 when Y is N or P.

Abstract: The subject invention provides catalytical compounds/complexes, compositions comprising such compound/complex, synthesis of the compounds/complexes, and methods of using such compounds/complexes as catalysts in, for example, RCM reactions. Specifically, the subject invention provides the synthesis of the first catalytically active V oxo alkylidene, VO(CHSiMe3)(PEt3)2Cl, which exhibits superior performance compared to other analogs.

Abstract: The present invention includes compound having the following structural formula:

Abstract: The invention relates to compounds in accordance with the general formula [Ru(arene)(Ra—N?CR1—CR3?N—Rb)] or [Ru(arene)((Rc,Rd)N—N?CRH1—CRH3?N—N(Re,Rf))]. In this case, arene is selected from the group consisting of mononuclear and polynuclear arenes and heteroarenes. R1, R3, RH1, RH3 and Ra-Rf are independently selected from the group consisting of H, an alkyl radical (C1-C10) and an aryl radical. It further relates to methods for the production of these compounds, compounds obtainable according to these methods, their use and a substrate having on a surface thereof a ruthenium layer or a layer containing ruthenium. In addition, the invention relates to a method for producing compounds [Ru(arene)X2]2, wherein arene is selected from the group consisting of mononuclear and polynuclear arenes and X=halogen, compounds of this type obtainable according to this method, and their use.

Abstract: A hypergolic metal organic framework material for producing a hypergol when combined with an oxidizer, comprising a general structure M1-L-M2, wherein L is an aromatic organic linker comprising one or more unsaturated substituents, and wherein M1 and M2 are same or different metal cations.

Abstract: A complex of formula (I): (I?) M is Hf; each X is a sigma ligand; L is a bridge of formula -(ER82)y—; y is 1 or 2; E is C or Si; each R8 is independently a C1-C20-hydrocarbyl, tri(C1-C20-alkyl)silyl, C6-C20-aryl, C7-C20-arylalkyl or C7-C20-alkylaryl or L is an alkylene group such as methylene or ethylene; Ar and Ar? are each independently an aryl or heteroaryl group optionally substituted by 1 to 3 groups R1 or R1? respectively; R1 and R1? are each independently the same or can be different and are a linear or branched C1-C6-alkyl group, C7-20 arylalkyl, C7-20 alkylaryl group or C6-20 aryl group with the proviso that if there are four or more R1 and R1? groups present in total, one or more of R1 and R1? is other than tert butyl; R2 and R2? are the same or are different and are a CH2—R9 group, with R9 being H or linear or branched C1-C6-alkyl group, C3-8 cycloalkyl group, C6-10 aryl group; each R is a —CH2—, —CHRx- or C(Rx)2- group wherein Rx is C1-4 alkyl and where m is 2-6; R5 is a linear or branched C1-C6-a

Abstract: The present invention relates to a novel therapeutic drug for a neurodegenerative disease and an application thereof. Provided is a novel compound of formula (I). The compound can effectively facilitate the proliferation of neural stem cells in both in vitro and in vivo experiments and can be used as a treatment approach for facilitating neuroregeneration to fight against cognitive decline associated with aging or a neurodegenerative disease.

Abstract: Described herein are compositions and methods for the treatment of ocular surface disorders including meibomian gland dysfunction, blepharitis, dry eye disease and other inflammatory/infections disease of the anterior surface of the eye. Said compositions and methods comprise keratolytic conjugate which demonstrate keratolytic activity, and anti-inflammatory or other desirable activities. Topical administration of said compositions to the eye, ocular surface or surrounding areas provides therapeutic benefit to patients suffering from ocular surface disorders.

Abstract: There is provided with a porphyrin compound represented by Formula (I) or a salt thereof; where A is a linking group represented as —X—NHCO— where X is a C1 to C6 alkylene group, each of R1, R2, R4, R5, R7, R8, R10, and R11 is a hydrogen atom, each of R3, R6, and R9 is a substituent of Formula; R12 is selected from a group of substituents represented by Formulae, R13 is a sulfo group, Ra, Rb, and Rc are substituents independently selected from C1 to C6 alkyl groups, and Rd is a hydrogen atom or a C1 to C6 alkyl group, and Rx is a substituent represented by General Formula. The porphyrin compound is useful as a cancer therapeutic agent, photosensitizer and fluorescent probe.

Abstract: Disclosed herein is the use of a hyaluronan conjugate for treating pulmonary inflammation, including acute and chronic pulmonary inflammation. Also disclosed herein is the use of a hyaluronan conjugate for treating virus infection. The hyaluronan conjugate is a hyaluronic acid (HA)-nimesulide conjugate.

Abstract: A nucleoside derivative represented below, or a salt thereof. (In (1), R1 represents a hydrogen atom, a hydroxyl group or a protected group, and in (2), X represent a halogen atom. In (1) and (2), R2 and R4 each represent a hydrogen atom, a hydroxyl protecting, phosphate, or protected phosphate group, or —P(?O)nR5R6 (n is 0 or 1, R5 and R6 each representing a hydrogen atom, hydroxyl, protected hydroxyl, mercapto, protected mercapto, lower alkoxy, cyano lower alkoxy, amino or substituted amino group, when n is 1, R5 and R6 are not both hydrogen atoms), R3 represents NHR7 (R7 represents a hydrogen atom, alkyl, alkenyl or protecting group for an amino group), an azide, amidino or guanidino group, each having a linking group (when R7 is hydrogen atom, the linking group is an alkylene group), and B represents any of a purine-9-yl, 2-oxo-pyrimidin-1-yl, substituted purine-9-yl or substituted 2-oxo-pyrimidin-1-yl group).

Abstract: The invention relates to the development and optimization of PCR and RT-PCR systems used to detect nucleic acids, including the diagnosis of genetic, viral, and other diseases. The essence of the proposed method is that neutral derivatives of oligonucleotides, namely phosphoryl guanidines containing one or more phosphate groups in which guanidine or substituted guanidine residue is introduced on the phosphorus atom, are used as primers for the template-based amplification, including polymerase chain reaction (PCR) and PCR combined with reverse transcription (RT-PCR). The invention allows to obtain more reliable, specific and selective results in the process of PCR, in particular, to increase the sensitivity of PCR by reducing the yield of by-products of DNA amplification and/or to control the yield of the PCR product, including intentionally suppressing, by using different combinations of the location and number of modified phosphate groups in the oligonucleotide primers.