Abstract: The present invention relates to diphenyloxyalkylamine derivatives and aryloxyalkylamine derivatives that are structurally analogous to mexiletine, said derivatives having important biological activity and not causing the undesired side effects observed with the prototype, as well as with other drugs from the same therapeutic class as the prototype. The derivatives of the present invention have formulas II and III and are used for treating, preventing or inhibiting pulmonary inflammatory diseases, for example, asthma and chronic obstructive pulmonary disease (COPD).

Abstract: Described herein are processes for the preparation of nepafenac and related intermediates, particularly wherein 2-aminobenzophenone is treated with a 2-(alkylthio)acetamide in the presence of sulfuryl chloride to afford a 2-(2-amino-3-benzoyl-phenyl)-2-(alkylthio)acetamide, which upon reduction affords nepafenac. Described herein are also processes for the purification of nepafenac, particularly for the removal of structurally similar impurities.

Abstract: A stock solution comprising a compound of formula (I) Wherein R1 together with the carbonyl group to which it is attached is a residue of a carboxylic acid, and NR2R3, in which R3 is H or together with R2 and the N-atom to which they are attached, a 5-membered ring, is a residue of an amino acid, in particular a proteinogenic amino acid, ornithine, gamma-aminobutyric acid or beta alanine, or a 1-amino cycloalkyl carboxylic acid.

Abstract: Process for preparing 4-[[(benzoyl)amino]sulphonyl]benzoyl chlorides of the formula (II).

Abstract: The present invention relates to novel compounds of polyfunctionalized polyethylene and polypropylene glycols, their synthesis and their use, in particular as tracers in applications related to oil and gas production, and especially as specific markers of various target fluids.

Abstract: There is provided as a biocide zinc or copper (II) salt having the general formula CH2?C(R1)COO-M-OCOC6H3R2R4, wherein M is Zn or Cu, R1 is selected from the group comprising hydrogen and methyl, R2 is selected from the group comprising hydrogen and OH, R4 is selected from the group comprising hydrogen, alkyl and SO2OH group.

Abstract: An alkyl phenyl sulfide derivative represented by the general formula [I] or an agriculturally acceptable salt thereof, and a pest control agent containing the derivative or the salt as an active ingredient. [in the above formula, R1 is, for example, a C1˜C6 alkyl group which is mono- or poly-substituted with halogen atom; R2 is, for example, a halogen atom or a C1˜C6 alkyl group; R3 is, for example, a hydrogen atom or a halogen atom; and R4 is, for example, a hydrogen atom or a C1˜C12 alkyl group.] The derivative or the salt has an excellent pest control effect.

Abstract: A family of amine mining collectors that uses alkoxylates allows for the easy adjustment of solubility and molecular weight useful because anionic and cationic mineral collectors require such varying degrees of solubility and molecular weight. The family of the present invention allows for the optimization of both parameters and an increase in collector efficiency.

Abstract: The present application, among other things, provides compounds that are capable of inhibiting the activity of anti-apoptotic Bcl-2 family proteins, for example, myeloid cell leukemia-1 (Mcl-1) protein. The present invention also provides pharmaceutical compositions as well as methods for using provided compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein. In some embodiments, a provided compound has the structure of formula I. In some embodiments, a provided compound has the structure of formula II.

Abstract: Described herein are compounds that are autotaxin inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with autotaxin activity.

Abstract: The present invention concerns in vivo imaging and in particular in vivo imaging of translocator protein (TSPO, formerly known as the peripheral benzodiazepine receptor). An indole-based in vivo imaging agent is provided that overcomes problems relating to known TSPO-binding radiotracers. The present invention also provides a precursor compound useful in the synthesis of the in vivo imaging agent of the invention, as well as a method for synthesis of said precursor compound. Other aspects of the invention include a method for the synthesis of the in vivo imaging agent of the invention comprising use of the precursor compound of the invention, a kit for carrying out said method, and a cassette for carrying out an automated version of said method. In addition, the invention provides a radiopharmaceutical composition comprising the in vivo imaging agent of the invention, as well as methods for the use of said in vivo imaging agent.

Abstract: An N-substituted triacetonediamine compound is prepared by reacting 4-amino-2,2,6,6-tetramethylpiperidine or a derivative thereof with a carbonyl compound in a reductive amination, wherein reductive conditions are established by conducting the reaction in the presence of hydrogen and in the presence of a supported catalyst, wherein the supported catalyst includes at least one metal M, wherein the metal M is selected from the group consisting of V, Cr, Mo, Mn, Ni, Pd, Pt, Fe, Ru, Os, Co, Rh, Ir, and Cu.

Abstract: Metallotriangle-based nanomolecules are formed by a one-step self-assembly of specifically chosen shaped poly-ligand monomers, the poly-ligand monomers coordinating with metal ions through coordinating ligands. The poly-ligand monomers are defined by vertex groups having arms extending therefrom and ending in coordinating ligands. Based on the desired metallotriangle-based nanomolecule structure to be assembled, specifically shaped poly-ligand monomers and metal ions are chosen and mixed in appropriate ratios so that coordinating ligands bind to metal ions and the poly-ligand monomers thus spontaneously self-assemble into the desired metallotriangle-based nanomolecule structure.

Abstract: Provided herein are solid forms comprising 2-(5-(3-fluorophenyl)-3-hydroxypicolinamido)acetic acid, methods of making the solid forms, methods of their use for the treatment of various diseases and/or disorders and pharmaceutical compositions comprising the solid forms.

Abstract: Described are negative allosteric modulators of metabotropic glutamate receptor 2 (mGlu2), pharmaceutical compositions including the compounds, and methods of using the compounds and compositions for treating depression, anxiety, obsessive-compulsive disorder, cognitive disorders, Alzheimer's disease, or autism spectrum disorders in a subject.

Abstract: Compounds For Inhibition Of Unregulated Cell Growth The present invention relates to compounds of Formula I for inhibition or eradication of unregulated cell growth.

Abstract: The invention relates to a heteroaryl compound according to formula (I) and to the use thereof in electronic devices.

Abstract: Described herein are liver X receptor (LXR) modulators and methods of utilizing LXR modulators in the treatment of dermal diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.

Abstract: Compounds having activity as inhibitors of ALK2 kinase and/or JAK2 kinase are disclosed. The compounds have the following structure (I): [FORMULA SHOULD BE INSERTED HERE] including stereoisomers, tautomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, X, z and A are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: The present invention relates to compounds which are of use in the field of agriculture as herbicides. The invention also relates to compositions comprising said compounds and methods of using said compounds.

Abstract: A copper catalyzed click chemistry ligation process is employed to bind azides and terminal acetylenes to provide 1,4-disubstituted 1,2,3-triazole triazoles. The process comprises contacting a solution of an organic azide and a terminal alkyne with a source of catalytic Ru ion to form a 1,4-disubstituted 1,2,3-triazole.

Abstract: Described herein are certain processes for the synthesis of compounds of Formula (I):

Abstract: The present invention relates to novel compounds for use as a medicament. In particular, the present invention relates to a medicament, preferably in the treatment and/or prevention of systemic diseases, autoimmune diseases, inflammatory diseases, for example multiple sclerosis and psoriasis.

Abstract: The present invention relates to an amorphous vortioxetine and salts thereof. In particular, the invention relates to a process for the preparation of an amorphous vortioxetine hydrobromide. Further, the invention also relates to a process for preparation of amorphous vortioxetine free base. The invention also relates to pharmaceutical compositions comprising an amorphous vortioxetine or hydrobromide salt thereof for oral administration for treatment of major depressive disorder (MDD) and generalized anxiety disorder (GAD).

Abstract: The present invention relates to the novel vortioxetine salts, solvates and crystalline forms thereof, specifically, vortioxetine hemihydrobromide and a crystalline form thereof, and isopropanol solvate of vortioxetine hydrobromide and a crystalline form thereof. Compared to the known vortioxetine hydrobromide, the vortioxetine salts, solvates and crystalline forms of the present invention have improved features in stability, hygroscopicity and purity. The present invention also relates to preparation methods of the vortioxetine salts, solvates and crystalline forms, pharmaceutical compositions thereof and their uses in the manufacture of antidepressant drugs.

Abstract: Provided herein are small molecule Epstein-Barr virus-induced G-protein coupled receptor 2 (EBI2) modulator compounds, compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds. EBI2 is a therapeutic target for the treatment of a variety of diseases or conditions. In some embodiments, EBI2 is a therapeutic target for the treatment of diseases or conditions such as, but not limited to, autoimmune diseases or conditions, cancer, and cardiovascular disease.

Abstract: The disclosed process relates to an improved process for manufacturing THF from a reaction mixture comprising BDO in the presence of an acid catalyst in a reaction vessel comprising a distillation reaction zone, wherein the acid catalyst is suspended in a vapor-rich region in the distillation reaction zone.

Abstract: The present invention provides an improved process for the preparation of dapagliflozin.of Formula (II) wherein the process comprises the step of hydrolyzing the compound of Formula (III) in the presence of an amine base.

Abstract: The present disclosure relates to salts of the compound (I), polymorphic forms thereof, methods for preparation and use thereof, and pharmaceutical compositions thereof.

Abstract: The present disclosure relates to carbon monoxide releasing molecules (“CORMs”), and methods of synthesizing and applying the molecules. More specifically, this disclosure relates to structurally tunable CORMS, compounds containing CORMS (and salts thereof).

Abstract: The invention relates to activators of soluble guanylate cyclase and their use in pharmaceutical compositions, primarily topically administered ophthalmic compositions. The pharmaceutical compositions are useful for reducing intraocular pressure in animals of the mammalian species.

Abstract: Solid forms comprising 3-(5-amino-2-methyl-4-oxo-4H-quinazolin-3-yl)-piperidine-2,6-dione, compositions comprising the solid forms, methods of making the solid forms and methods of their uses are disclosed

Abstract: The present invention relates to certain 2,4-disubstituted quinoline derivatives, to their therapy, as well as to pharmaceutical compositions comprising said compounds. More specifically the invention relates to certain 2,4-disubstituted quinoline derivatives or pharmaceutical compositions comprising said compounds for the treatment of cancers characterized by overactive Ras and/or Rac or signalling pathway.

Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.

Abstract: The present invention is directed to 2-pyridyloxy-4-ester compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-4-ester compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

Abstract: The present invention relates to novel pharmaceutically acceptable substituted aryl acrylic acid addition salts of Crizotinib (I) or its hydrate or solvate thereof. The present invention further relates to processes for preparation of the said substituted aryl acrylic acid addition salts of Crizotinib (I). The present application also provides pharmaceutically acceptable substituted aryl acrylic acid addition salts of Crizotinib (I) or its hydrate or solvate useful as active pharmaceutical ingredient in pharmaceutical composition comprising thereof, possessing anti-cancer activity.

Abstract: An N-methyl-substituted triacetonamine compound is prepared by reacting at least one triacetonamine compound (I) with formaldehyde under reductive conditions, in the presence of hydrogen and in the presence of a supported catalyst, wherein the supported catalyst contains at least one metal M, wherein the metal M is selected from the group consisting of V, Cr, Mo, Mn, Ni, Pd, Pt, Fe, Ru, Os, Co, Rh, Ir, and Cu.

Abstract: The disclosure includes compounds of Formula (I) wherein R0, R1, R2, R3, R4, R5, and L are defined herein. Also disclosed is a method for treating a neoplastic disease, autoimmune disease, and inflammatory disorder with these compounds.

Abstract: The present invention relates to a quinazoline derivative shown in formula (I) and a preparation method therefor, a pharmaceutical composition comprising the compound shown in formula (I), and an application of the compound in preparing drugs for curing and preventing tumors.

Abstract: The present invention relates to oligooxopiperazines and their use. Methods for preparing oligooxopiperazines are also disclosed.

Abstract: Disclosed are oxime ester compounds which have specific benzo (unsaturated 5-membered ring)-carbonyl group and their use as photoinitiators in photopolymerizable compositions, in particular in photoresist formulations for display applications, e.g. liquid crystal display (LCD), organic light emitting diode (OLED) and touch panel.

Abstract: An AdipoR activator for activating both AdipoR1 and AdipoR2 is provided. A compound represented by the following formula (1), wherein A is a substituted or unsubstituted aryl group or the like, Y1 is (CHR2)a— or the like, X is CH or N, R1 is a C1-7 alkyl group, m is an integer of 0-4, Y2 is *—O—CH2—CONH—, *—CONH—(CH2)b—CO— or the like, Z is a cyclic group, B may be a substituent of the cyclic group represented by Z, and n is an integer of 0-3.

Abstract: The present disclosure relates to compound of structural Formula I and a method for preparing said compounds. The disclosure further relates to a method of employing the Formula I compounds for modulation of Janus kinase-Signal Transducer and Activator of Transcription (JAK-STAT) pathway in cancer cells, and the corresponding use of compound of Formula I as anti-cancer agents.

Abstract: Disclosed are new small molecules and the uses thereof for inhibiting superoxide dismutase (SOD) expression. Also disclosed are pharmaceutical compositions comprising the small molecule inhibitors which may be administered in methods of treating diseases or disorders associated with elevated SOD expression or activity, including neurological diseases and disorders such as amyotrophic lateral sclerosis (ALS).

Abstract: Bis(difluoromethyl)pyrazole derivatives of the formula (I) in which the symbols R1, X and G are each as defined in the description, and agrochemically active salts, metal complexes and N-oxides thereof, and use thereof for controlling phytopathogenic harmful fungi, and also processes for preparing compounds of the formula (I).

Abstract: The present invention provides compounds of Formula (Ia), and pharmaceutically acceptable salts thereof. The compounds are useful as inhibitors of voltage-gated sodium channels, in particular Nav 1.7. as described in the specification. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention, as well as intermediates and processes useful for making the compounds.

Abstract: The present invention relates to bifunctional compounds, which find utility to degrade and (inhibit) Androgen Receptor. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds Androgen Receptor such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of Androgen Receptor.

Abstract: The present invention provides compounds having store overload-induced Ca2+ release (SOICR) inhibitory activity and methods for producing and using the same. In particular, compounds of the invention is of the formula: R1—X1-L-X2—R2, wherein R1, X1, L, X2, and R2 are those defined herein.

Abstract: A compound of formula I, (I), wherein A, Q, R1, and R2, are as defined in claim 1. Furthermore, the present invention relates to intermediates used to prepare compounds of formula (I), to methods of using them to combat and control insect, acarine, nematode and mollusc pests and to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising them.

Abstract: The invention relates to novel heteroaryl carboxamides, a process for their preparation, and pharmaceutical compositions containing them. These materials are useful for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning and/or memory.