Abstract: Compounds for the inhibition of mammalian Ste20-like kinase 1 (MST1) are disclosed, along with compositions comprising them and methods of their use in the treatment, management or prevention of an inflammatory or autoimmune diseases or disorders.

Abstract: Substituted pyridines of the formula I in which the variables are defined according to the description, processes and intermediates for preparing the compounds of the formula I and their N-oxides, their agriculturally suitable salts, compositions comprising them and their use as herbicides, and also methods for controlling unwanted vegetation.

Abstract: Described is a method for the synthesis and/or purification of a high purity diaminophenothiazinium compound of the following formula: characterized by a purity of greater than 98% and less than 1% Azure B, 0.15% Azure A, 0.15% Azure C and 0.05% Methylene Violet Bernthsen (MVB), as impurities. Also described are related high purity compounds, compositions, and methods of using such compounds and compositions. The compounds and compositions are useful in the treatment of diseases caused by tau aggregation, such as Alzheimer's disease and other dementias, and infection.

Abstract: Disclosed is a compound represented by Formula (I): or a pharmaceutically acceptable salt, monohydrate, enantiomer or diastereomer thereof. Also disclosed are pharmaceutical compositions comprising the compound of Formula (I) or a pharmaceutically acceptable salt, monohydrate, enantiomer or diastereomer thereof and methods of inhibiting 11?-HSD1 activity comprising the step of administering to a mammal in need of such treatment an effective amount of a compound of Formula (I), or a pharmaceutically acceptable salt, monohydrate, enantiomer or diastereomer thereof. Values for the variables in Formula (I) are defined herein.

Abstract: The invention relates to novel substituted piperidines, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular diseases and tumour diseases.

Abstract: The present invention relates to substituted heterocyclic compounds of Formula I: or pharmaceutically acceptable salts or N-oxides or quaternary ammonium salts thereof wherein constituent members are provided hereinwith, as well as their compositions and methods of use, which are histamine H4 receptor inhibitors/antagonists useful in the treatment of histamine H4 receptor-associated conditions or diseases or disorders including, for example, inflammatory diseases or disorders, pruritus, and pain.

Abstract: The present invention provides arylpiperazine derivatives having Formula I which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder and depression.

Abstract: Provided are compounds and methods useful for the preparation of compounds useful as inhibitors of beta-site amyloid precursor protein (APP)-cleaving enzyme.

Abstract: The present invention is directed to a process for the preparation of Efavirenz, (4S)-6-chloro-4-(cyclopropylethynyl)-4-(trifluoromethyl)-1,4-dihydro-2H-3,1-benzoxazin-2-one, of formula (I) comprising reacting the intermediate of formula (II) [0045] as a free base or a salt thereof, with diphosgene (TCMCF, trichlormethylchloroformate) Cl3CO—COCl in an organic solvent or in a biphasic medium comprised of an organic solvent and water, preferably but not mandatorily in the presence of a weak base in an amount sufficient to neutralise the reaction mixture or in an up to 30% molar excess of such amount.

Abstract: The invention relates to a method for the preparation of 11-(4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl]dibenzo [b,f]-1,4-thiazepine and pharmaceutically acceptable salts thereof comprising the reaction of 1-[2-(hydroxyethoxy)-ethyl]piperazine with dibenzo[b,f][1,4]thiazepin-11-ylamine.

Abstract: The present invention is directed to tricyclic tetrahydroquinoline compounds of formula I, and pharmaceutically acceptable salts thereof wherein the variables R1, R2, R3, R4, R5, R20 and X are as described herein and to pharmaceutical compositions thereof, that exhibit useful antibacterial activity against a wide range of human and veterinary pathogens.

Abstract: Fused bicyclic compound having an affinity to mineral corticoid receptor (MR), of formula [I]: wherein ring A is benzene having a substituent R1, fused to an adjacent 6-membered heterocyclic ring and further optionally having a substituent(s) other than R1, R1 is alkylsulfonylamino, etc., R2 and R3 are (a) the same of different and are hydrogen, alkyl, or optionally substituted aryl, or (b) combined with each other to form an oxo group or (c) combined with each other at its terminal together with the adjacent carbon atom to form cycloalkyl, X is ?N—, ?C(R4)— or —CH(R4)—, R4 is (a) hydrogen, (b) cyano, (c) halogen, (d) alkyl, (e) alkenyl, (f) cycloalkyl, (g) alkanoyl, (h) carbamoyl, or (i) cycloalkenyl, Ar is an optionally substituted aromatic cyclic group and a dotted line means presence or absence of a double bond, or a pharmaceutically acceptable salt thereof, useful e.g. as an antihypertensive agent.

Abstract: The present invention relates to N-[3-(5-Amino-3,3a,7,7a-tetrahydro-1H-2,4-dioxa-6-aza-inden-7-yl)-phenyl]-amides of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.

Abstract: Disclosed are heterocyclic derivatives, and more particularly heterocyclic derivatives having the following Formula I which are useful for the preparation of medicaments for treating diseases related to uric acid: wherein R1, R2, R3, R4, R5, R6, R7, R8, X1, X2, X3, L and Y are the same as defined in the detailed description.

Abstract: This invention concerns a crystalline, enantiopure hydrochloride salt of N-(5-{2-[3-(4,4-diethyl-2-oxo-4H-benzo[d][1,3]oxazin-1-yl)-1,1-dimethyl-propylamino-1-hydroxy-ethyl}-2-hydroxy-phenyl)-methanesulfonamide, preferably of N-(5-{(R)-2-[3-(4,4-diethyl-2-oxo-4H-benzo[d][1,3]oxazin-1-yl)-1,1-dimethyl-propylamino-1-hydroxy-ethyl}-2-hydroxy-phenyl)-methanesulfonamide and its action as a long acting beta-agonist, alone or in combination with one or multiple other active ingredients for the treatment of respiratory diseases.

Abstract: The present invention relates to 2-Amino-5,5-difluoro-5,6-dihydro-4H-[1,3]oxazin-4-yl)-phenyl]-amides of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.

Abstract: The present disclosure provides biologically active 2,4-pyrimidinediamine compounds of formulae (I)-(III): and salts thereof, compositions comprising these compounds, and methods of using these compounds in a variety of applications.

Abstract: The invention is directed to novel crystalline forms of meloxicam. These novel crystalline forms of meloxicam have improved bioavailability, an enhanced rate of dissolution and shorter time to Cmax in blood, as compared to pure meloxicam.

Abstract: Provided herein are aminoquinolones and pharmaceutically acceptable derivatives thereof. In certain embodiments, provided herein are compounds, compositions and methods for treating, preventing or ameliorating GSK-3 mediated diseases.

Abstract: The present invention relates to a process for the preparation of crystalline non-hygroscopic form H1 of efavirenz, and pharmaceutical compositions containing it. In accordance with the present invention efavirenz was dissolved in acetone at 25° C.-30° C., the solution was slowly added to water at 0° C.-5° C., the separated solid was filtered, washed with mixture of acetone and water and dried at 25° C.-35° C. under below 65% relative humidity for 18 hours to give crystalline non-hygroscopic efavirenz form H1.