Abstract: This invention provides certain piperidine compounds as AT2R antagonists, e.g., compounds of formula (I): or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, and X are as defined herein, pharmaceutical compositions thereof, and methods of using the same to treat pain associated with AT2R activity.

Abstract: The present invention generally relates to sensitizer compounds and their use to sensitize cancer and/or pre-cancerous cells of certain cancers to treatment with certain resistance-prone therapeutics used in cancer therapy. In embodiments, the conjugates of particular esters or amides of Near Infrared Dyes, are used as sensitizers to avoid or overcome therapeutic resistance once formed. In embodiments, the sensitizers include conjugates with Cisplatin, Simvastatin, Artemisinin, platin-based compounds or statins. In embodiments, the resistance prone cancer therapeutics include cisplatin, gemcitabine, doxorubicin, paclitaxel, docetaxel, and platin-based compounds. These may be administered in combination with the sensitizer, or the sensitizer itself may comprise an therapeutic-derived moiety conjugated to the sensitizer, for example as is the case for dye-CIS conjugated sensitizers. Alternatively, the sensitizer may be co-administered with one or more therapeutic.

Abstract: K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer.

Abstract: The invention relates to 3-phenoxyazetidin-1-yl-heteroaryl pyrrolidine derivatives of general formula (I) which are agonists of GPR52, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to the 3-phenoxyazetidin-1-yl-heteroaryl pyrrolidine derivatives of general formula (I) for use as a medicament, pharmaceutical compositions comprising at least a compound of general formula (I) and processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.

Abstract: The present invention relates to deuterated 1-piperazino-3-phenyl-indanes and salts thereof with activity at dopamine receptors D1 and D2 as well as the 5HT2 receptors in the central nervous system, to medicaments comprising such compounds as active ingredients, to the use of such compounds in the treatment of diseases in the central nervous system, and to methods of treatment comprising administration of such compounds.

Abstract: Provided are certain methods useful in the treatment of cancer comprising administering a compound of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor;

Abstract: A system includes: a liquid formulation comprising an antipsychotic agent and an implantable infusion device. The implantable infusion device includes a reservoir, an outlet in communication with the reservoir, a drive mechanism configured to cause liquid formulation in the reservoir to be delivered to the outlet, and control electronics coupled to the drive mechanism. The control electronics are programmed with instructions that cause the liquid formulation to be delivered from the reservoir to the outlet at a flow rate of less than 500 microliters per hour for a period of time sufficient to reach a therapeutically effective steady state concentration in a subject's cerebrospinal fluid (CSF) if the liquid is delivered to a CSF-containing space of a subject.

Abstract: Embodiments relate to a tablet comprising celecoxib and ciprofloxacin or a pharmaceutically acceptable salt thereof, and low viscosity hydroxypropyl methylcellulose having a viscosity of less than 150 cP, when measured as a 2% solution in water at 20° C.

Abstract: The present invention relates to a pharmaceutical combination for use in the treatment, prevention and/or stabilization of age-related diseases and/or degenerative diseases. In particular, said pharmaceutical combination comprises a biguanide and an acetylcholinesterase inhibitor and/or an N-oxide, a hydrate, a pharmaceutically acceptable salt or solvate thereof. The invention is further also directed to the use of said pharmaceutical combination for prevention, stabilization and/or reduction of age-related complaints and/or degenerative complaints; and for improving a measure of life span and/or health span.

Abstract: The specification relates to a crystalline Latrepirdine dihydrochloride, Form DMB-I, method of its preparation, pharmaceutical composition containing it and its uses.

Abstract: This disclosure relates to novel catalysts for Suzuki-Miyaura cross-coupling reactions, the use thereof, and the methods of making the same.

Abstract: The present invention generally relates to a process for selective and direct activation and subsequent amidation of aliphatic and aromatic carboxylic acids to afford an amide R3CONR1R2. That the process is capable of delivering gaseous or low-boiling point amines provides a major advantage over existing methodologies, which involves an intermediate of triacyloxyborane-amine complex [(R3CO2)3—B—NHR1R2]. This procedure readily produces primary, secondary, and tertiary amides, and is compatible with the chirality of the acid and amine involved. The preparation of known pharmaceutical molecules and intermediates has also been demonstrated.

Abstract: Decarboxylated cannabis compositions and methods of making and using the same are provided. The methods produce a decarboxylated product that has more terpenes and cannabidiol preserved and less oxidation of tetrahydrocannabinol to cannabinol, compared to a decarboxylated product made by a traditional decarboxylation process.

Abstract: The present invention relates to the technical field of chiral synthesis, and specifically provides the synthesis and use of a new type of oxa-spirodiphosphine ligands. The bisphosphine ligand is prepared with oxa-spirobisphenol as a starting material after triflation, palladium catalyzed coupling with diaryl phosphine oxide, reduction of trichlorosilane, further palladium catalyzed coupling with diaryl phosphine oxide, and further reduction of trichlorosilane. The oxa-spiro compound has central chirality, and thus includes L-oxa-spirodiphosphine ligand and R-oxa-spirodiphosphine ligand. The racemic spirodiphosphine ligand is capable of being synthesized from racemic oxa-spirobisphenol as a raw material. The present invention can be used as a chiral ligand in the asymmetric hydrogenation of unsaturated carboxylic acids. The complex of the ligand with ruthenium can achieve an enantioselectivity of greater than 99% in the asymmetric hydrogenation of methyl-cinnamic acid.

Abstract: Stable Phytonadione compositions for parenteral administration are provided which comprise (E) isomer of phytonadione at or greater than 97% w/w as the active ingredient, and is substantially free of (Z) isomer. Said compositions are stable, sterile, and particulate-free. Further, said compositions reduce or avoid allergic reactions to benzyl alcohol and polysorbate. In some aspects, the compositions are free or substantially free of benzyl alcohol and/or reduced amounts of polysorbate. Methods of manufacture and methods of administration also provided.

Abstract: The present invention relates to a novel selenophenochromene hydroxamic acids as angiogenesis inhibitors, as well as methods of their manufacturing and use in different pharmaceutical compositions for the treatment or prevention of various diseases and disorders by administration of such substances.

Abstract: This invention is benzothiophene-based estrogen receptor downregulators and their compositions and uses to treat estrogen-related medical disorders.

Abstract: The present disclosure provides novel synthetic intermediates useful in the synthesis of MK2 kinase inhibitors.

Abstract: A compound represented by the general formula (V) wherein all the symbols are as defined in the specification, has an improved balance of the agonist activity against the S1P5 receptor relative to the S1P1 receptor, and can thus serve as a therapeutic agent for S1P5-mediated diseases such as schizophrenia and Binswanger's disease and other neurodegenerative diseases.

Abstract: Disclosed are a compound with near-infrared fluorescence that selectively binds to tau aggregates, a method for preparing the same, a tau-targeting near-infrared fluorescent probe including the compound, a composition for detecting a tau fiber protein containing the near-infrared fluorescent probe as an active ingredient, and the use of the composition for the diagnosis of tauopathy. In particular, the compound does not bind to an amyloid beta protein and has high selectivity to a tau aggregate, specifically reported as an etiology of the initial state of tauopathy, thus being useful as a near-infrared fluorescent detector for detecting a tau fiber protein for early diagnosis of a tauopathy including Alzheimer's disease.