Abstract: The invention relates to compound of the formula (I) or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.

Abstract: Compounds of formula (I) can modulate the activity of autotaxin (ATX).

Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, for example as modulators of the growth hormone secretagogue receptor (also referred to as the ghrelin receptor or GHSRla receptor) and/or for the treatment and/or prophylaxis of a disorder mediated by the ghrelin receptor.

Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including mutant EGFR and mutant HER2 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including mutant EGFR and mutant HER2 activity, are described herein.

Abstract: A process for preparation of (2S, 5R)-7-oxo-6-sulphooxy-2-[((3R)-piperidine-3-carbonyl)-hydrazino carbonyl]-1,6-diaza-bicyclo[3.2.1]octane is disclosed.

Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.

Abstract: The present invention relates to imidazopyridazine derivatives. More particularly, it relates to 4-(biphenyl-3-yl)-7H-imidazo[4,5-c]pyridazine derivatives of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5 and R6 are as defined in the description. The imidazopyridazine derivatives of the present invention modulate the activity of the GABAA receptor.

Abstract: The invention provides compounds represented by the structural formula (1): wherein R1, R2, R3 and R4 are as defined in the claims. The compounds are inhibitors of nucleases, and are useful in particular in a method of treatment and/or prevention of proliferative diseases, neurodegenerative diseases, and other genomic instability associated diseases.

Abstract: The present invention provides compounds and compositions which are positive allosteric modulators of GABA-A receptors that selectively target the peripheral nervous system and organs of the body, and which do not pass through the blood-brain barrier. The compounds and compositions of the present invention are useful for treatment of diseases or disorders which are mediated by GABA-A neuronal activity, such as, for example, visceral pain, gut motility, irritable bowel syndrome, functional abdominal pain, functional idiopathic diarrhea, inflammatory bowel diseases, drug induced pain, bile salt malabsorption, lactase or other carbohydrate intolerance.

Abstract: The present invention provides small-molecule inhibitors of BMP signaling and compositions and methods for inhibiting BMP signaling. These compounds and compositions may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation. These compounds and compositions may also be used to reduce circulating levels of ApoB-100 or LDL and treat or prevent acquired or congenital hypercholesterolemia or hyperlipoproteinemia; diseases, disorders, or syndromes associated with defects in lipid absorption or metabolism; or diseases, disorders, or syndromes caused by hyperlipidemia.

Abstract: The present invention provides compounds of formula (I) wherein A, X1, X2, R1, R2, R3, R4 and R5 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments.

Abstract: The invention relates to 3-((hetero-)aryl)-8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.

Abstract: The invention relates to 3-(carboxymethyl)-8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.

Abstract: The present invention relates to a benzodiazepine compound, processes for its preparation, pharmaceutical compositions containing such a compound and to its use in therapy.

Abstract: Compounds that modulate the oxidoreductase enzyme indoleamine 2,3-dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided.

Abstract: Provided are PDE1 inhibitors of Formula I, processes for their production, their use as pharmaceuticals, and pharmaceutical compositions comprising them. Previous publication WO 2009/075784 disclosed, among others, (6aR,9aS)-2-(4-(6-fluoropyridin-2-yl) benzyl)-5-methyl-3-(phenylamino)-5,6a,7,8,9,9a-hexahydrocyclopenta[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(2H)-one as an inhibito of PDE1. This compound undergoes significant metabolism at several positions including the aniline ring and the cyclopentane ring. The current invention provides for Compounds of Formula I wherein such metabolism is attenuated by the substitution of hydrogen atoms for deuterium atoms at key locations discovered by the inventors.

Abstract: The present disclosure provides acetate salts of buprenorphine, and its anhydrates, solvates, hydrates, and crystalline forms thereof, where the acetate salts of buprenorphine are essentially free of impurities. The disclosure further provides method of preparing the acetate salts, buprenorphine free base prepared from the acetate salts, other salts prepared from the free base, and pharmaceutical compositions thereof essentially free of impurities.

Abstract: A compound of formula I, (I) or a pharmaceutically-acceptable salt thereof. The compound is useful in the treatment of cancer.

Abstract: This invention relates to novel diarylamino compounds that bind to the sigma-2 receptor, to pharmaceutical compositions comprising such compounds, and to methods for inhibiting or restoring synapse loss in neuronal cells, modulating a membrane trafficking change in neuronal cells, and treating cognitive decline and neurodegenerative diseases and disorders therewith.

Abstract: The present invention relates to novel retinoid-related orphan receptor gamma (ROR?) modulators and their use in the treatment of diseases mediated by ROR?.

Abstract: The present invention relates to substituted benzothiadiazolamine compounds of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyperproliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.

Abstract: Docusate salts of N-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl}phenyl)-N?-(3-fluorophenyl)urea are suitable pharmaceutical ingredients for pharmaceutical compositions useful in the treatment of disease, for example, cancer.

Abstract: The present invention provides N-benzyl-3-sulfonamidopyrrolidines and related compounds, as well as pharmaceutical compositions and sanitizing compositions containing the same. The compounds and compositions are useful as antibiotic agents. Methods for making and using the compounds and compositions are also described.

Abstract: Disclosed is a compound of formula (I), wherein R1, R2, R3, R4, R5, R6, R7 and R8 are as defined in the present application.

Abstract: An object of the present invention is to provide a compound having a superior CH24H inhibitory action, which is useful as an agent for the prophylaxis or treatment of epilepsy, neurodegenerative disease and the like. The present invention relates to a compound represented by the formula: wherein each symbol is as defined in the specification, or a salt thereof.

Abstract: The present invention relates to compounds having dual pharmacological activity towards both the sigma (?) receptor, and the ?-opiod receptor and more particularly to diazaspiro undecane compounds having this pharmacological activity, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain. wherein Y is n is 1 or 2; q is 1, 2, 3, 4, 5 or 6; X is a bond, —C(O)O—, —C(O)NR8—, —C(O)—, —O— or —C(R4R4?)—; R1 is C(O)R5 or S(O)2R5.

Abstract: The present Invention relates to sodium (2R,5S,13aR)-7,9-dioxo-10 ((2,4,6-trifluorobenzyl)carbamoyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1?,2?:4,5] pyrazino[2,1-b][1,3]oxazepin-8-olate Form I.

Abstract: Disclosed is a dihydropyrimido fused ring derivative as a HBV inhibitor, and in particular relates to a compound shown as formula (I) or a pharmaceutically acceptable salt thereof.

Abstract: Certain embodiments are directed to fullerene derivatives tetrahydro-1H—C60-fulleropyrrolo[1,2-c][1,3]thiazine salts (Formula I) or tetrahydro-1H—C70-fulleropyrrolo[1,2-c][1,3]thiazine salts (Formula II). Certain further embodiments are directed to ?, ?, ?, and/or ? isomer of tetrahydro-1H—C70-fulleropyrrolo[1,2-c][1,3]thiazine salt.

Abstract: The instant invention describes macrocyclic compounds having therapeutic activity, and methods of treating disorders such as cancer, tumors and cell proliferation related disorders.

Abstract: The present invention provides compounds of Formula (I) and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.

Abstract: The present invention provides compounds of formula (I) wherein A, R1, R2 and R3 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments.

Abstract: Disclosed are compounds of Formula G1: where “RG3”. “Rd1” to “Rd4”, “n”, “m”, “p”, “W”, “X”, “Y”, and “Z” are defined herein, which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2A receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.

Abstract: The present invention relates to a 4,5-diarylimidazole derivative of formulae (I), (II) or (III): or a pharmaceutically acceptable salt thereof, wherein the 4,5-diarylimidazole derivative has a hydroxamic acid residue at a first aryl ring and a residue R1 at a second aryl ring; and wherein R1 is hydrogen, a halogen atom or an unsubstituted or substituted alkoxy group; R2 is independently selected from an unsubstituted or substituted alkyl, alkoxy or alkene group; M is a metal atom; L is a halogen atom, an unsubstituted or substituted phosphane, sulfane, arene or alkene group or a 4,5-diarylimidazole-derivative of formula (I); and n is an integer of from 1 to 5.

Abstract: A compound of formula (I) useful as a photosensitizer in photodynamic therapy is provided. There is also provided a photosensitizing composition for use in photodynamic therapy comprising this compound. Finally, there are provided a method of killing cells under oxidative stress conditions and a method for the selective delivery of singlet oxygen (1O2) to cells having an increased reactive oxygen species (ROS) concentration, these methods comprising the steps of contacting such cells with a compound of formula (I), and exposing the cells to light.

Abstract: The instant disclosure relates to liquid salts such as but not limiting to ionic liquids; and method for recovering liquid salts including ionic liquids. Ionic liquids get deactivated due to presence of various contaminants or impurities. The present disclosure deals with recovery and regeneration of ionic liquids using compounds containing at least one coordinating agent to form adduct with metal compounds. The instant disclosure also includes an assembly for carrying out the recovery and regeneration of the ionic liquids.

Abstract: A process for the preparation of 3-methacryloxypropyldimethylchlorosilane by reaction of allylmethacrylate with dimethylchlorosilane in the presence of a hydrosilylation catalyst, characterized in that the reaction is carried out in the absence of a peroxide is provided. The process includes providing a first stream containing allylmethacrylate. A a second stream containing dimethylchlorosilane is provided. The streams contact in a continuous flow reactor in the presence of the hydrosilylation catalyst, thereby producing 3-methacryloxypropyldimethylchlorosilane. A product stream is continuously removed from the continuous flow reactor.

Abstract: The invention provides compounds that inhibit cholinesterases, such as acetylcholinesterase and butyrylcholinesterase. Such compounds are useful to prevent or treat exposure of a patient (e.g., a human) to an organophosphoric nerve agent (e.g., sarin and VX) or to treat a patient suffering from a neurodegenerative disorder such as Alzheimer's Disease or Lewy Body Dementia. The compounds are further useful as diagnostic tools for use in medical or research radiography (e.g., positron emission tomography) when synthesized with a radionuclide (e.g., [18F]. Synthetic schemes to produce such compounds are also provided.

Abstract: Monomeric and dimeric gold(I) complexes as anticancer agents. The gold(I) complexes are coordinated to mixed ligands: one phosphine-based ligand that may be monodentate or bidentate and at least one dithiocarbamate-based ligand that is monodentate. Pharmaceutical compositions incorporating the gold(I) complexes, methods of synthesis, methods of treating cancer and methods of inhibiting cancer cell proliferation and inducing cancer cell apoptosis are also provided.

Abstract: The present invention relates to a phosphazene compound comprising cyano group having a molecular structure of Formula (I); wherein, Y and Y? are independently selected from organic groups; M1 and M2 are independently selected from phosphazene groups, and M1 contains m1 phosphorus atoms, and M2 contains m2 phosphorus atoms; X1, X1?, X2, X3 and X4 are independently selected from any one of the sixth main-group elements; R and R? are independently selected from divalent organic groups; a is an integer greater than or equal to 0; b is an integer greater than or equal to 1; and c is an integer greater than or equal to 0; and a+b=2m1, d+2=2m2. The present invention achieves a synergistic effect with P and N of phosphazene group by introducing cyano group to the phosphazene group, and thus improves thermal stability and flame retardancy of the phosphazene compound, and the compatibility thereof with other components is excellent.

Abstract: A method for production of potassium antimony tartrate by utilizing one or more residues bearing antimony includes the step of leaching of the one or more residues bearing antimony for a first pre-determined time interval in each of one or more jacketed reactors. In addition, the method includes filtering obtained slurry from a leached solution of the one or more residues products bearing antimony to obtain an aqueous solution and a solid residue. The method also includes crystallizing the obtained aqueous solution to form one or more crystals of the potassium antimony tartrate in a jacketed crystallizer. The antimony contained in the one or more residues is in an oxidic form and the oxidic form of the antimony is more than 20%. The solid residue is a leached cake.

Abstract: The present invention relates to a process for preparing hydridocarbonyltris(triphenylphosphine)rhodium(I), RhH(CO)(PPh3)3, also referred to hereinafter as “Rh-hydrido.” An alcoholic suspension of triphenylphosphine is stirred with an Rh(III) chloride precursor at elevated temperature. The Rh(III) chloride precursor used may be rhodium(III) chloride hydrate RhCl3*xH2O or rhodium(III) chloride solution H3[RhCl6]*(H2O)n. After cooling, alcoholic alkali metal hydroxide solution is added, and the mixture is stirred for a few hours. Finally, sparging is effected with CO gas and the Rh-hydrido formed is removed. Rh-hydrido can be prepared by this process on the industrial scale with high yields and at very good quality.

Abstract: Provided are a heterostructured nickel compound including a nickel amidinate ligand and an aliphatic alkoxy group and a method of forming a thin film including the heterostructured nickel compound. The method includes forming a nickel-containing layer on a substrate by using the heterostructured nickel compound including the nickel amidinate ligand and the aliphatic alkoxy group.

Abstract: Provided herein is a highly pure carbohydrate composition, and a method of making a highly pure carbohydrate composition. The method includes passing an aqueous carbohydrate solution through an anion exchange chromatography column including a polyethyleneimine (PEI) chromatographic media to obtain a purified solution, and isolating a highly pure carbohydrate composition from the purified solution.

Abstract: Provided herein include methods and compositions for synthesis of Lipid IVA and derivatives thereof, using a defined set of pathway enzyme, which may be isolated and used to reconstitute all or part of the pathway in a cell-free reaction.

Abstract: The present invention relates to novel semi-synthetic meningococcal conjugate vaccine comprising novel synthetic oligosaccharide conjugated to a carrier protein. The present invention also relates to novel synthetic meningococcal oligosaccharide and a process for its preparation.

Abstract: Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 2?-dichloro or 2?-fluoro-2?-chloro nucleoside analogue compounds which display remarkable efficacy and bioavailability for the treatment of, for example, HCV infection in a human. In certain embodiments, the compounds are of Formula (I): or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof; wherein each of RA and RB is independently Cl or F, wherein at least one of RA and RB is Cl; and Base, PD and Z are as described herein.

Abstract: Described herein are compounds of Formula (I)-(XIII), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.

Abstract: The present disclosure relates to immunoglobulins and immunoglobulin conjugates with reduced oligomerization and efficient labeling and compositions, methods of generating such immunoglobulins and immunoglobulin conjugates and methods of using such immunoglobulin conjugates particularly in the treatment and prevention of disease.

Abstract: The present disclosure provides compositions and methods for purifying a protein such as DNase using a chromatographic process. The methods include a single chromatographic step and the use of high concentration salt buffers.