Abstract: The application relates to a compound of Formula (I) which modulate the amount of STK4, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease or disorder associated with the modulation of STK4.

Abstract: The disclosed embodiments detail improved methods for the synthesis of diketopiperazines from amino acids. In particular improved methods for the cyclocondensation and purification of N-protected 3,6-(aminoalkyl)-2,5-diketopiperazines from N-protected amino acids. Disclosed embodiments describe methods for the synthesis of 3,6-bis-[N-protected aminoalkyl]-2,5-diketopiperazine comprising heating a mixture of an amino acid in the presence of a catalyst in an organic solvent. The catalyst is selected from the group comprising sulfuric acid, phosphoric acid, p-toluenesulfonic acid, 1-propylphosphonic acid cyclic anhydride, tributyl phosphate, phenyl phosphonic acid and phosphorous pentoxide among others. The solvent is selected from the group comprising: dimethylacetamide, N-methyl-2-pyrrolidone, diglyme, ethyl glyme, proglyme, ethyldiglyme, m-cresol, p-cresol, o-cresol, xylenes, ethylene glycol and phenol among others.

Abstract: The present invention provides a compound having a dihydropyran structure, a method of producing a compound having a dihydropyran structure, a method of producing Pre-SMTP, a method of producing a group of SMTPs, and a pharmaceutical composition. The compound having a dihydropyran structure can be a useful intermediate in the chemically producing a group of Pre-SMTP and SMTP. Specifically, the compound having a dihydropyran structure is represented by the following formula (1), wherein: R3Si is a silyl group selected from TMS: trimethylsilyl, TES: triethysilyl, TBS (TBDMS): tert-butyldimethylsil, TIPS: triisopropylsilyl, TBDPS: tert-butyldiphenylsilyl, X is selected from COOH, CHO, and —CH?C(CH3)—(CH2)2—CH?C(CH3)2.

Abstract: The present invention relates to a novel method for producing a triazolopyridine compound or a salt thereof having a PHD inhibitory action and useful for treating or preventing diseases caused by decreased production of EPO, or the like. The present invention provides a method for producing 2-({[7-hydroxy-5-(2-phenylethyl)-[1,2,4]triazolo[1,5-a]pyridin-8-yl]carbonyl}amino)acetic acid comprising a step of reacting Compound [VI]: wherein R61, R62 and R111 are as defined in the specification, or a salt thereof.

Abstract: Identification and evaluation of a set of first-in-class potent inhibitors targeting a new cancer target, Grb2-associated binder-1 (GAB1), which integrates signals from different signaling pathways and is frequently over-expressed in cancer cells. Intensive computational modeling is utilized to understand the structure of the GAB1 pleckstrin homology (PH) domain and screened five million compounds. Upon biological evaluation, several inhibitors were found that induced large conformational changes of the target structure exhibited strong selective binding to GAB1 PH domain. Particularly, these inhibitors demonstrated potent and tumor-specific cytotoxicity in breast cancer cells. This targeting GAB1 signaling may be used for cancer therapy, especially for triple negative breast cancer patients.

Abstract: A borate compound serving as a proteasome inhibitor, a preparation method for the borate compound and uses thereof.

Abstract: The present disclosure relates to substituted thiophene carboxamides and analogues thereof of formula (I) that may be used for protecting plants from bacterial diseases, in particular from bacterial diseases caused by bacteria belonging to the genus Xanthomonas.

Abstract: A heterocyclic compound that exhibits superior control effects against harmful arthropods is provided. In particular, a heterocyclic compound of formula (I) is provided, wherein the variable groups are as defined in the specification. Also provided is a composition containing the heterocyclic compound of formula (I) and one or more types of components selected from the components described in the specification.

Abstract: A pyranoglucose-substituted pyrazole compound, used as a pharmaceutical intermediate, having the structural formula represented by formula (9c). The present invention further relates to an intermediate compound represented by formula (10c) or a salt thereof. The present invention further relates to a preparation method of the aforementioned intermediate compound and a method of using the same to prepare an SGLT inhibitor. By means of the novel key intermediate, the preparation technique of an SGLT inhibitor is greatly simplified. In addition, because the intermediate can be precipitated in the form of a salt and is easy to purify, the purity of the SGLT inhibitor is significantly increased, compared with the original preparation pathway (crude product purity can reach 99% or more).

Abstract: Provided are a fluorescent dye and a preparation process and use thereof. The fluorescent dye is able to emit a long wavelength, is sensitive and specific to viscosity, and is used for a wide range of purposes, such as viscosity testing, fluorescent labeling, quantification or detection of proteins, enzymes or nucleic acids. In addition, it can be used as a fluorescent-activated probe.

Abstract: The present disclosure provides compounds, for example, a compound of Formula (I), that modulate a protein function and/or restore protein homeostasis. The disclosure provides a method of modulating a protein-mediated disease, disorder, condition, or response. Compositions, including in combination with other therapeutic agents, are provided.

Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, Ra, Rb, Q1, and Q2 are defined in the specification. The invention also comprises a method of treating or ameliorating a ROR-?-t mediated syndrome, disorder or disease, including wherein the syndrome, disorder or disease is selected from the group consisting of rheumatoid arthritis, psoriatic arthritis, and psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.

Abstract: The present disclosure provides methods and formulations for reducing ammonia and carbon dioxide emissions from a bovine using lubabegron, or a physiologically acceptable salt thereof. The present disclosure also provides bovine feed additives and bovine feed compositions.

Abstract: Provided herein are thiophene compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.

Abstract: Methods for inhibiting cell growth, inhibiting DNA polymerase activity, and inhibiting DNA replication and repair are provided. In a method of inhibiting cell growth, a cell, such as a cancer cell, is contacted with zelpolib or a derivative or pharmaceutically acceptable salt thereof. The cell growth can be inhibited in vivo, and in certain embodiments, the cell growth is inhibited in vitro. In a method for inhibiting DNA polymerase activity, a DNA polymerase is contacted with zelpolib or a derivative or pharmaceutically acceptable salt thereof. In certain embodiments, the DNA polymerase is Pol ?. In a method for inhibiting DNA replication and repair, a cell, such as a cancer cell, is contacted with zelpolib or a derivative or pharmaceutically acceptable salt thereof. The DNA replication and repair can be inhibited in vivo, and in certain embodiments, the DNA replication and repair is inhibited in vitro.

Abstract: The present disclosure relates generally to modulators of Cot (cancer Osaka thyroid) and methods of use and manufacture thereof.

Abstract: Use of imeglimin for the prevention and/or treatment of hepatocellular carcinoma.

Abstract: The present invention describes the combination of a 6-propylamino-4,5,6,7-tetrahydro-1,3-benzothiazole-2-amine or of a pharmaceutically acceptable salt or solvate thereof with fluoxetine or a pharmaceutically acceptable salt or solvate thereof, for use for treating a synucleinopathy such as Parkinson's disease, Lewy body disease, mutations in the glucocerebrosidase gene, or multiple system atrophy.

Abstract: The present invention is directed to heteroarylpiperidine ether compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

Abstract: A 7H-azulene [1,2,3-i,j] isoquinolin-7-one compound, a single crystal and a use thereof are provided. The compound has a structure as shown in a formula (I). The present invention obtains a crude extract of Acorus calamus L., then extracts with different polar solvents in sequence and separates column chromatography to obtain a novel alkaloid compound, which is expected to be developed into a novel class of drug exerting neuroprotective effects, so as to prevent and treat senile dementia, stroke and epilepsy diseases.