Abstract: This invention relates to antagonists of G3BP2, G3BP1, and ZEB1. Pharmaceutical compositions comprising G3BP2 inhibitors, methods of inhibiting G3BP2, G3BP1, and ZEB1, methods of treating cancer and inflammation, and methods of identifying an inhibitor of cancer stems cells are also provided.

Abstract: The present invention is relates to an improved process for the preparation of pazopanib or a pharmaceutically acceptable salts thereof. The present invention also relates to novel polymorphic Forms of pazopanib hydrochloride, and its intermediates thereof.

Abstract: Compounds of formula (I) wherein, R1, R2, R3, R4a, R4b and R5 are described herein, or a stereoisomer, enantiomer or tautomer thereof or mixtures thereof, or a pharmaceutically acceptable salt or solvate thereof, are described herein, as well as other compounds. These compounds are useful in treating inflammation and/or pain. Compositions comprising a compound of the invention are also disclosed, as are methods of using the compounds to treat inflammation and/or pain.

Abstract: The invention relates to novel methods for preparing indolinobenzodiazepine dimer compounds and their synthetic precursors.

Abstract: The present invention relates to the technical field of chemical synthesis of pharmaceutical chemicals, and provides a 6H-imidazo[4,5,1-ij]quinolone, a synthesis method and use thereof. 6H-imidazo[4,5,1-ij]quinolone derivatives provided by the present invention are a novel group of active quinolone derivatives, which have tumor cell inhibition activity and exhibit IC50 values equivalent to anti-lung cancer drug osimertinib; these quinolone derivatives have a broad application prospect in the preparation of antitumor drugs. The 6H-imidazo[4,5,1-ij]quinolone provided by the present invention is of high research and application value and has potential application prospects in fields of pharmaceutical chemicals, materials, dyes, etc. The present invention uses thioquinolinamide as a raw material to synthesize 6H-imidazo[4,5,1-ij]quinolones, featuring simple operation, excellent selectivity, high yield, mild reaction conditions, and easy product separation.

Abstract: The present invention relates to novel heterocyclic compounds. The invention is also directed to compounds which are modulators of the metabotropic glutamate receptors (m Glu R), preferably of the metabotropic glutamate receptor subtype 7 (“m Glu R7”). The present invention also relates to pharmaceutical composition comprising such compounds and their use for the treatment or prevention of disorders associated with glutamate dysfunction or in which metabotropic glutamate receptor, preferably m Glu R7 subtype of metabotropic glutamate receptors, is involved.

Abstract: Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.

Abstract: The invention provides novel methods for preparing indolinobenzodiazepine dimer compounds and their synthetic precursors.

Abstract: Lysosomal acid lipase (LAL) substrates, assays for lysosomal acid lipase using the substrates, and methods for diagnosing diseases and conditions attributable to lysosomal acid lipase deficiency.

Abstract: The present invention provides a cured product obtained by curing a curable composition including a compound represented by General Formula 1, in which a birefringence ?n (587 nm) is 0.00??n (587 nm)?0.01. Pol1-Sp1-L1-Ar-L2-Sp2-Pol2??(General Formula 1) In the formula, Ar represents a divalent group containing a ring structure selected from the group consisting of a quinoxaline ring and a quinazoline ring; L1 and L2 each represent a single bond, —O—, —OC(?O)—, —OC(?O)O—, —OC(?O)NH—, and the like; Sp1 and Sp2 each represent a single bond or a divalent linking group; Pol1 and Pol2 each represent a hydrogen atom or a polymerizable group; and the compound represented by General Formula 1 has at least one polymerizable group. The cured product of the present invention has a small Abbe number (?d) and a large partial dispersion ratio (?g, F), and is therefore useful for production of optical members.

Abstract: A process is provided to prepare propylene amines of the formula NH2—(A-NH—)pR, wherein R is a hydrogen atom or an alkyl group, p is at least 1 when R is an alkyl group, and at least 2 when R is a hydrogen atom, or derivatives or precursors thereof wherein one or more units —NH-A-NH— may be present as a cyclic urea unit or a cyclic unit or between two units —NH-A-NH— a carbonyl bond is present, each unit -A- can be independently an alkylene unit and at least one unit -A- is a —C3H6— unit, wherein each —C3H6— unit can be linear or branched. The process includes reacting (i) at least one of a hydroxy-functional compound chosen from the alkanolamine-functional compounds, and dihydroxyalkylene compounds, with (ii) an amine-functional compound, in the presence of (iii) a carbon oxide delivering agent, wherein at least one of the alkanolamine-functional compound, the amine-functional compound and/or the carbon oxide delivering agent contains at least one alkylene unit (A) that is a propylene unit.

Abstract: Provided herein are novel polymorphic forms of metopimazine mesylate. These polymorphic forms are useful in methods, compositions, and kits for the treatment of an enteric nervous system disorder.

Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit Respiratory Syncytial Virus (RSV). The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from RSV infection. The invention also relates to methods of treating an RSV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Abstract: The invention provides novel methods for preparing indolinobenzodiazepine dimer compounds and their synthetic precursors.

Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

Abstract: The invention relates to a method for producing cyclododecanone (CDON). During the production, contaminated cyclododecane (CDAN) is produced. This can be separated from CDON by distillation (CDAN-containing fraction). The separation of CDAN and impurities such as 13-oxabicyclo [7.3.1]tridecane occurs by crystallizing out CDAN from the CDAN-containing fraction.

Abstract: Provided is an additive for imparting ultraviolet absorbency, or an additive for imparting a high refractive index, which has satisfactory compatibility with a resin serving as a matrix and can maintain high transparency even if added in high concentrations. Also provided is an additive with which the function of imparting both ultraviolet absorbency and a high refractive index can be realized by means of one kind of additive. This additive is represented by the following Formula (I): wherein at least one of R1a to R9a is a monovalent sulfur-containing group represented by the following Formula (i-1) or Formula (i-2): R10amSH??(i-1) R11anSR12a—SpR13a??(i-2) wherein R10a to R12a each represent a divalent hydrocarbon group or the like; and R13a represents a monovalent hydrocarbon group or the like.

Abstract: The disclosure discloses a sulfur-containing polycyclic-hydroxypyridone carboxamide analog against HIV and an application thereof. The sulfur-containing polycyclic-hydroxypyridone carboxamide analog has a compound represented by the following formula (I) or a stereoisomer thereof or a pharmaceutically acceptable salt thereof. The sulfur-containing polycyclic-hydroxypyridone carboxamide analogs provided by the disclosure have good anti-HIV activity, and in particularly, compound 2, compound 18, compound 34 and compound 66 have strong inhibitory effects on HIV-1 replication in vitro, and the therapeutic index thereof against HIV is hundreds of times greater than that of the existing drugs TDF and Dolutegravir. The development of such the compounds is of great significance for the development of AIDS drugs and will bright good news to AIDS patients.

Abstract: The invention relates to compounds for treating and/or preventing obesity and obesity-related disorders. Particularly, the invention provides chromanone derivatives used as ATF3 inducer and for treating and/or preventing obesity and obesity-related disorders such as heart disease, hypertension, hyperlipidemia and diabetes.

Abstract: The present invention relates to a method for preparing an intermediate (Formula IV) of sodium elagolix. The intermediate is prepared by the following route. The method has advantages of simple and safe operation, high yield, less environmental pollution, good economic effect and suitability for industrial production, wherein R represents C1-C4 substituted or unsubstituted benzyl or allyl.