Abstract: A method for manufacturing amidomagnesium halogenides and admixtures thereof with alkali metal salts in aparotic, organic solvents, compounds obtained according to the method and use thereof in synthesis chemistry, for example for deprotonizing enolizable systems, functionalized aromatics and heteroaromatics.

Abstract: The present invention relates to new arylaminoalcohol derivatives of formula (I), and to a method for the preparation of such compounds: I The invention also relates to the use of these compounds as medicaments, and in particular for the prevention and/or the treatment of parasitic diseases caused by apicomplexan parasites such as malaria and toxoplasmosis. Finally, the invention relates to pharmaceutical compositions containing such compounds of formula (I) as active principles.

Abstract: Objects of the present invention are to provide a compound which is highly active against pests, to provide a pest control agent comprising the compound, and to provide a method for controlling a pest by applying the compound. The present invention provides a 4-(arylethynyl)pyridine or a salt thereof, a pest control agent which comprises the 4-(arylethynyl)pyridine or salt thereof as an active ingredient, and a method for controlling a pest by applying the 4-(arylethynyl)pyridine or salt thereof in an effective amount.

Abstract: Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of treatment of cancer are described.

Abstract: The present application relates to novel 5-amino-5,6,7,8-tetrahydroquinoline-2-carboxylic acids, to processes for their preparation, to their use for the treatment and/or prevention of diseases, and to their use for producing medicaments for the treatment and/or prevention of diseases, especially for the treatment and/or prevention of cardiovascular and cardiopulmonary disorders.

Abstract: Disclosed are novel benzamide compounds and the uses thereof for treating diseases and disorders in a patient in need thereof by increasing cellular levels of A3G and/or other members of the A3 family of proteins in the patient. The disclosed compounds include 3-benzamide compounds that may be administered treat an HIV-1 infection or cancer in a patient.

Abstract: Provided are compounds, including those of Formula I; and pharmaceutically acceptable salts and solvates thereof. The compounds described herein relate to and/or have application(s) in (among others) the fields of drug discovery, pharmacotherapy, physiology, organic chemistry and polymer chemistry.

Abstract: Disclosed are solid forms of 4-(2-bromo-4-fluorophenyl)-N-(2-chloro-6-fluorophenyl)-1,3-dimethyl-1H-pyrazol-5-amine (Compound 1). Methods for the preparation of solid forms of Compound 1 and for the conversion of one solid form of Compound 1 into another are disclosed. Disclosed are compositions for protecting a plant or plant seed from diseases caused by fungal pathogens comprising a biologically effective amount of a solid form of Compound 1 and at least one additional component selected from the group consisting of surfactants, solid diluents and liquid carriers. Compositions comprising a mixture of a solid form of Compound 1 and at least one other nematocide, insecticide and/or fungicide are also disclosed. Also disclosed are methods for protecting a plant or plant seed from diseases caused by fungal pathogens comprising applying to a plant or seed, or to the environment of the plant or seed, a biologically effective amount of a solid form of Compound 1.

Abstract: There is provided a compound of formula (I): or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.

Abstract: The invention relates to a process for preparing an asymmetrical imidazolium salt of formula (1A), in which R1 is an aromatic group, R2 is chosen from a cyclic secondary aliphatic alkyl group and a heteroalkyl group, R3 and R4 are chosen, independently of one another, from the group consisting of hydrogen, a halide and an alkyl group, and A? is an anion. The process comprises a first substep of forming a reaction mixture by bringing one equivalent of an aniline into contact with one equivalent of a compound bearing an amine group, in the presence of at least four point five equivalents of a Brønsted acid. The process also comprises a second substep of forming a solution comprising one equivalent of a dicarbonyl, one equivalent of formaldehyde, and at least four point five equivalents of the Brønsted acid, and adding thereto the reaction mixture formed in the first substep. The mixture is left to stir for a predetermined time at a predetermined temperature.

Abstract: Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR40 receptor. Such compounds are represented by Formula (I) as follows: wherein R1, G, and R2 are defined herein.

Abstract: The present invention provides a novel P2X3 and/or P2X2/3 receptor antagonist. A compound represented by the formula (I): wherein Ra, Rb and Rc are, (a) Ra and Rb are taken together ?Z; and Rc is a group represented by R1c; or (b) Rb and Rc are taken together to form a bond; and Ra is a group represented by —Y—R1a; R1a and R1c are each independently hydrogen, substituted or unsubstituted alkyl, etc.; R2 and R3 are each independently substituted or unsubstituted aryl, etc.; R4a and R4b are each independently hydrogen, substituted or unsubstituted alkyl, etc.; X is —N(R5)—, etc.; R5 is hydrogen, substituted or unsubstituted lower alkyl, etc.; —Y— is —O—, etc.; ?Z is ?O, etc.; and n is an integer of 0 to 4.

Abstract: The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for substituents at positions 4a, 5, 5a, and 12a of the tetracycline ring system.

Abstract: The invention relates to compounds of the formula (I) which are inhibitors of activated thrombin-activable fibrinolysis inhibitor. The compounds of the formula I are suitable for producing medicaments for prophylaxis, secondary prevention and treatment of one or more disorders associated with thromboses, embolisms, hypercoagulability or fibrotic changes.

Abstract: A process for producing N-methyl or N,N-dimethyl amines, which comprises using amine compound, nitro-containing compound or nitrile compound as a starting material, carbon dioxide as a methylating agent and hydrogen gas as a reducing agent, and allowing them to react in a sealed reactor for 6 to 48 h in a reaction medium at a reaction temperature of 80 to 180 ° C. in the presence of a composite catalyst, so as to provide N-methyl or N,N-dimethyl amines. The process of the present invention is simple and under relative mild reaction conditions. By means of the process of the invention, the target products can be prepared at low cost with a high yield. The catalysts used have a high catalytic activity and can be separated from the reaction system simply and reused. Furthermore, the whole process of the present invention is environmental-friendly and facilitates the cycling use of carbon dioxide.

Abstract: Direct epoxidation of propene is carried out on electrochemically tuned mixed oxide catalyst surfaces in a single chamber reactor with mixed reaction gas of hydrocarbon and oxygen. Yield and selectivity improvement compared to platinum- or silver-based noble metal catalysts have been demonstrated for the same reactor set up. Increase in propylene oxide yield has been demonstrated when a cell voltage is applied.

Abstract: A continuous process for the preparation of propylene oxide, comprising (i) providing a liquid feed stream comprising propene, hydrogen peroxide, acetonitrile, water, dissolved potassium dihydrogen phosphate, and optionally propane; (ii) passing the liquid feed stream provided in (i) into an epoxidation reactor comprising a catalyst comprising a titanium zeolite of structure type MWW, and subjecting the liquid feed stream to epoxidation reaction conditions; (iii) removing an effluent stream from the epoxidation reactor; wherein the concentration of the dissolved potassium dihydrogen phosphate in the liquid feed stream is at least 10% of the solubility limit of the potassium dihydrogen phosphate in the liquid feed stream.

Abstract: A perfluoropolyether thiol compound comprises a perfluoropolyether segment, at least one mercapto group (—SH), and at least one intervening divalent carbonylimino moiety (—C(?O)—NR—, wherein R is hydrogen or alkyl). The compound can be produced, for example, by a ring-opening reaction of thiolactones with perfluoropolyether-substituted, primary or secondary amines. The compound can be used, for example, as a polymerization chain transfer agent, as an intermediate for the preparation of functional group-containing fluorochemical derivatives such as disulfides, and as a fluorinated surface treatment.

Abstract: The invention relates to a method for producing 2-substituted 4-hydroxy-4-methyltetrahydropyrans.

Abstract: The invention relates to novel therapeutic compounds, more in particular to biologically active analogs and uses thereof as medicament, for instance for the treatment of atrial fibrillation. Provided is a compound of the general formula (formula I) wherein R1 is H or a saturated or unsaturated aliphatic moiety comprising 1 to 8 C-atoms; and X is selected from the group consisting of moieties X1, X2, X3, X4, X5 and X6. Exemplary uses include the prevention or therapeutic treatment of a HSF1-mediated disease.

Abstract: Disclosed are methods for treating catmint oil. The process allows the separation of sulfur-containing compounds from the catmint oil. The treated catmint oil can be used for the production of hydrogenated catmint oil, which is enriched in the insect repellent, dihydronepetalactone.

Abstract: This invention relates generally to the discovery of a method of inhibiting, preventing or treating bacterial infections. The invention also relates to a method of inhibiting bacterial capsule biogenesis.

Abstract: The present invention is directed to indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK2 kinase is involved.

Abstract: Disclosed are processes and intermediates for the preparation of compound (X), which is currently being investigated for the treatment of prostate cancer.

Abstract: The present invention provides compounds of Formula (I): a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a polymorph, a solvate thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.

Abstract: The present invention relates to a process for preparation of Dabigatran etexilate or pharmaceutically acceptable salt thereof. The present invention relates to novel compounds, in particular Ethyl-3-{[(2-formyl-1-methyl-1H-benzimidazole-5-yl)carbonyl]-(2-pyridinyl) amino}propanoate and Ethyl-3-{[(2-dichloromethyl-1-methyl-1H-benzimidazole-5-yl)carbonyl]-(2-pyridinyl)amino}propanoate and process for preparation thereof. The present invention further relates to the use of these novel compounds in the preparation of Dabigatran etexilate or pharmaceutically acceptable salt thereof.

Abstract: An efficient process for increasing the optical purity of the active pharmaceutical ingredient Esomeprazole, by means of a substantially quantitative and selective precipitation and removal of Omeprazole is provided.

Abstract: The invention provides novel chemical compounds useful for treating various hematologic malignancies, or a related disease or disorder thereof, and pharmaceutical composition and methods of preparation and use thereof.

Abstract: The disclosures herein relate to novel compounds of formula wherein Ar1 and R1 are as defined herein, and their use in treating, preventing, ameliorating, controlling or reducing cerebrovascular or vascular disorders associated with CGRP receptor function.

Abstract: The present invention relates to substituted pyrrole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular Jak family kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them.

Abstract: The present invention relates to N-(2,3-dihydro-1H-pyrrolo[2,3-b]pyridin-5-yl)-4-quinazolinamine and N-(2,3-dihydro-1H-indol-5-yl)-4-quinazolinamine derivatives of Formula (I) wherein R1, R2, R3, R4, R5, R6 and A have the meaning defined in the claims. The compounds according to the present invention are useful as inhibitors of PERK. The invention further relates to processes for preparing such compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

Abstract: The invention provides reagents, methods, and compositions for studying protein-protein interactions. The inventive system and methods allow the analysis of protein-protein interactions in vivo and in vitro. Advantages offered by various embodiments of the inventive system and methods compared to existing photocrosslinking approaches include, for example, (i) novel reversible crosslinking reagents that allow easy isolation, purification, and enrichment of the crosslinked products; (ii) trifiuoromethyl phenyldiazirine- or perfluorinaled phenylazide-based photocrosslinking reagents that provide high specific labeling, no side product, and higher photocrosslinking efficiency; (iii) versatile spacer groups that allow systematic contact site mapping; (iv) novel methods for isolating, purifying, and detecting crosslinked products based on the reversible-link chemistry; and (v) the ability to study the interaction sites in vitro, in situ, or in vivo.

Abstract: 4-(2,2-Difluoro-benzo[1,3]dioxol-5-ylmethyl)-piperazine-1-carboxylic acid (4-chloro-pyridin-3-yl)-amide is described, which is useful as a FAAH modulator. 4-(2,2-Difluoro-benzo[1,3]dioxol-5-ylmethyl)-piperazine-1-carboxylic acid (4-chloro-pyridin-3-yl)-amide may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis). A method of synthesizing 4-(2,2-difluoro-benzo[1,3]dioxol-5-ylmethyl)-piperazine-1-carboxylic acid (4-chloro-pyridin-3-yl)-amide is also disclosed.

Abstract: The present invention relates to methods of treating cancer by administering the EZH2 inhibitor compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.

Abstract: The present disclosure relates to novel crystalline salt forms of lamivudine, methods for the preparation thereof, pharmaceutical compositions thereof, and their use in the treatment of viruses such as Human Immunodeficiency Virus (HIV) infection.

Abstract: The present invention relates to a method of treating acne or psoriasis by topically administering Tazarotene substantially free of dimer impurity of formula 4,4-dimethyl-6-[4-(4,4-dimethylthiochroman-6-yl)-buta-1,3-diynyl]-thiochroman.

Abstract: The invention relates to inhibitors of Sphingosine Kinase enzymatic activity, and methods of treating diseases and disorders by administering inhibitors of Sphingosine Kinase enzymatic activity.

Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, agonists and partial agonists for the mGluR5 receptor and may be useful for the treatment of various disorders of the central nervous system.

Abstract: The present invention provides a medicament for treating a disease involving Nav 1.7 such as neuropathic pain, nociceptive pain, inflammatory pain, small-fiber neuropathy, erythromelalgia, paroxysmal extreme pain disorder, dysuria, and multiple sclerosis, which comprises a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1a, R1b, R1c and R1d are hydrogen, halogen, cyano, C1-4 alkyl, C1-4 alkoxy, or the like, provided that at least one of R1a, R1b, R1c and R1d is C6-10 aryl, C6-10 aryloxy, or the like, R2 and R3 are hydrogen, C1-6 alkyl, C3-10 cycloalkyl, or the like, R4 is hydrogen, C1-6 alkyl, C3-7 cycloalkyl, or the like, m is 1, 2 or 3, L is CR7R8, and R7 and R8 are hydrogen, hydroxyl, C1-4 alkyl, C1-4 alkoxy, or the like.

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 invention is directed to a formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2a, R2b and R3-R7 are herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.

Abstract: The invention provides compounds that bind to deoxycytidine kinase (dCK) and compositions including pharmaceutically acceptable compositions containing the compounds. The compounds are useful in treating diseases and disorders where dCK activity is implicated such as cancer and immune disorders. The compounds also find use in clinical methodologies including positron emission tomography (PET) imaging.

Abstract: This invention provides a medicament for the treatment of cancer, which cause a reduction of cancer. This invention relates to use of a compound which has inhibitory activities against prostaglandin E2 receptor (EP4 receptor) and is represented by the following general formula (I), (II), (III), or (IV), or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt for the manufacture of a medicament for the treatment of cancer. The invention relates to a method for treatment of cancer comprising administering the compound or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt to humans or animals. The compound or a pharmaceutically acceptable salt thereof, or the pharmaceutical composition may be used in combination with one or more second active agents.

Abstract: The present invention relates to compounds of general formula I wherein R1, R2, R3 and R4 are as defined herein which may be used for the treatment of schizophrenia, obsessive-compulsive personality disorder, major depression, bipolar disorders, anxiety disorders, normal aging, epilepsy, retinal degeneration, traumatic brain injury, spinal cord injury, post-traumatic stress disorder, panic disorder, Parkinson's disease, dementia, Alzheimer's disease, cognitive impairment, chemotherapy-induced cognitive dysfunction (“chemobrain”), Down syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, stroke, and disturbances due to radiation therapy, chronic stress, optic neuropathy or macular degeneration, or abuse of neuro-active drugs, selected from alcohol, opiates, methamphetamine, phencyclidine and cocaine.

Abstract: The present disclosure provides compounds that are tyrosine kinase inhibitors, in particular Bruton tyrosine kinase (“BTK”) inhibitors, and are therefore useful for the treatment of diseases treatable by inhibition of BTK such as cancer, autoimmune, inflammatory, and thromboembolic diseases. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Abstract: A process for preparation of a compound of Formula (I) is disclosed.

Abstract: The present invention relates to novel substituted oxindole derivatives of the formula I wherein A is a ring selected from phenyl and 6-membered hetaryl containing 1 or 2 nitrogen atoms as ring members, where ring A carries one substituent R6 and optionally one substituent R7; B is a ring selected from phenyl and a monocyclic or bicyclic heteroaromatic ring containing 1, 2 or 3 heteroatoms selected from O, N and S as ring members, where ring B may carry 1, 2 or 3 substituents R8; X1, X2, X3 and X4, independently of each other, are selected from —CH2—, —O—, —S(O)c—, —NH—, —C(O)—, —CH2CH2—, —CH2O—, —OCH2—, —S(O)cCH2—, —CH2S(O)c—, CH2NH—, —NHCH2—, —CH2C(O)— and C(O)CH2—; X5 is NH, CH2 or O; and wherein c, R1, R2, (R3)a, (R4)b, R5, R6, R7, and R8 are as defined in the claims. The present invention also relates to pharmaceutical compositions comprising the novel substituted oxindole derivatives of the formula I, and to their use for the treatment of vasopressin-related disorders.

Abstract: This disclosure relates, at least in part, to a method of treatment. In one embodiment, the method of treatment comprises administering to a subject in need of such treatment a first therapeutic agent including compound (1): (structurally represented) or a pharmaceutically acceptable salt thereof in combination with a second therapeutic agent, wherein the first therapeutic agent and the second therapeutic agent are administered either simultaneously or sequentially.

Abstract: Compounds and compositions useful for treating disorders related to Kit are described herein.

Abstract: The present application relates to the use of known and novel heterocyclic compounds for controlling animal pests, to novel heterocyclic compounds, to processes for preparation thereof and to the use thereof for controlling animal pests.