Abstract: Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, fibrotic disease, cardiovascular disease, infectious disease, inflammatory disorder, graft rejection, or graft-versus-host disease.

Abstract: The present invention relates to stable crystalline Form I of lorcaserin hydrochloride of Formula (IA) and processes for its preparation. The invention also relates to processes for the preparation of lorcaserin and pharmaceutically acceptable salts, solvates and hydrates thereof.

Abstract: The invention provides compounds represented by the general formula I wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder.

Abstract: The present invention is related to a compound represented by formula (I) wherein —X— is —NH— or —S—; —Z— is —O— or —S—; R3, R5 and R6 are each independently a hydrogen atom, substituted or unsubstituted alkyl, or the like; R7 is a cyano, substituted or unsubstituted amino, or the like; R7? is each independently a halogen; b is 0 or 1; or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising thereof.

Abstract: Compounds which are tricyclopyrazole derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.

Abstract: Compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like.

Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Y, Z, n, R1 and R3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.

Abstract: The present disclosure provides dibenzazepine derivatives having Formula I or I(A): and the pharmaceutically acceptable salts and solvates thereof, wherein R3a, R3b, R6, V1, V2, Z1, Z2, Z3, and G are defined as set forth in the specification. The present disclosure is also directed to the use of the compounds of Formula I or I(A), and the pharmaceutically acceptable salts or solvates thereof, to treat a disorder responsive to the blockade of one or more sodium channels. In one embodiment, the compounds of the present disclosure are useful for treating pain.

Abstract: This invention relates to novel substituted triazolobenzodiazepines of the Formula (I), wherein each of the variables are defined herein and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering I-BET762.

Abstract: Provided are novel compounds which are capable of inhibiting an activity of RNA polymerase I, and uses thereof in treating diseases or disorders modulated by RNA polymerase I, preferably autoimmune diseases such as multiple sclerosis and proliferative diseases.

Abstract: An object of the present invention is to provide a method for producing an optically active amino acid in high yield and in a highly enantioselective manner, which method has fewer restrictions on the material that can be used as the substrate, and to provide, among others, a compound useful as a chiral auxiliary for the method.

Abstract: The present invention relates to a process for the synthesis of compounds of formula (I), wherein the meaning of R is dimethylamino or acetyl group, using the compound of formula (III) or (IV), wherein the meaning of R? is dimethylamino or 2-methyl-1,3-dioxan-2-yl group, as starting material and methoxymethyl lithium as reagent.

Abstract: The invention relates to new and improved processes for the preparation of Alcaftadine and pharmaceutically acceptable salts thereof as well as an intermediate for the preparation of Alcaftadine. The new process saves a number of steps compared to the known process and results in a higher yield.

Abstract: The present invention relates to a novel process for the synthesis of abiraterone and in particular abiraterone acetate, a compound of formula (I) reported below: having pharmacological activity suitable for slowing down the progression of advanced stage prostate cancer. The process is characterized by the fact that the intermediate triflation step is carried out on prasterone (DHEA) or its 3-acetate using Ar—N(OTf)2 as the triflation reagent, but where Ar is not phenyl, and by the fact that the base used in this step is an alkali metal alcoholate.

Abstract: The present invention in one embodiment provides a compound of Formula I: (I), or a pharmaceutically acceptable salt thereof, wherein Y1, Y2 and Y3 are each independently selected from hydrogen and deuterium; R1, R2, and R3 are each methyl and are independently substituted with 0 to 3 deuterium; and R4 is t-butyl and is substituted with 0 to 9 deuterium; provided that if R1, R2 and R3 are each —CH3, and R4 is —C(CH3)3, then at least one of Y1 and Y2 is deuterium.

Abstract: The present invention relates to a new process for the synthesis of compounds of formula (I) (wherein the meaning of R is dimethylamino or acetyl group) using the compound of formula (II) (wherein the meaning of R is dimethylamino or 2-methyl-1,3-dioxolan-2-yl group) as starting material, as well as to the intermediate of the process.

Abstract: The present invention relates to new substituted glycinamides of general formula (I) wherein D, M, R3, R4 and R5 are defined as in the specification, the tautomers, enantiomers, diastereomers, mixtures and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.

Abstract: The present invention relates to BET-protein-inhibitory, in particular BRD4-inhibitory 5-aryltriazoloazepines of the general formula (I) in which R1, R2, R3 and R4 have the meanings given for the general formula (I), to pharmaceutical compositions comprising the compounds according to the invention, and to the prophylactic and therapeutic use thereof for hyperproliferative disorders, especially for neoplastic disorders. The present invention further relates to the use of BET protein inhibitors in viral infections, in neurodegenerative disorders, in inflammatory diseases, in atherosclerotic disorders and in male fertility control.

Abstract: Novel solanidine-derived compounds, the synthesis method thereof and the uses of same in the fields of phytosanitary protection and health. In particular, the novel compounds have toxic and/or repellent properties in relation to aphids, as well as other properties.

Abstract: A method for preparing abiraterone acetate.