Abstract: The present invention relates to crystalline polymorph forms of (S)-2-((2-((S)-4-(difluoromethyl)-2-oxooxazolidin-3-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)amino)propanamide (GDC-0077), having the structure, Formula I: or stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, and processes of preparing the polymorph forms.

Abstract: The present invention provides a prophylactic or therapeutic agent for hypoxic injury, ischemia-reperfusion injury or inflammation, an agent for protecting cells for transplantation, and an agent for preserving organism. A prophylactic or therapeutic agent for hypoxic injury, ischemia-reperfusion injury or inflammation, an agent for protecting cells for transplantation, or an agent for preserving organism, containing, as an active ingredient, at least one kind selected from a heterocyclic compound represented by the formula (I) wherein each symbol is as described in the DESCRIPTION, or a salt thereof; an isothiocyanate compound represented by the formula S?C?N—R5 (II) wherein the symbol is as described in the DESCRIPTION; and a TRPA1 agonist.

Abstract: The present invention provides compounds of Formula I: pharmaceutical compositions comprising these compounds and methods of using these compounds to treat or prevent a disease or disorder mediated by FXR and/or TGR5.

Abstract: The present invention concerns a PTGDR-1 antagonist, a PTGDR-2 antagonist, a dual PTGDR-1/PTGDR-1 antagonist, or a combination of PTGDR-1 antagonist and PTGDR-2 antagonist, and pharmaceutical compositions containing them, for use for preventing and/or treating SLE.

Abstract: Compounds of Formula (I), methods of using said compounds singly or in combination with additional agents and compositions of said compounds for the treatment of cancer are disclosed.

Abstract: Provided herein are spirolactone compounds of Formula I that are useful as inhibitors of ACC1 and/or ACC2. The spirolactone compounds described herein can be used for treating a disease or disorder associated with aberrant ACC1 and/or ACC2 activities, for example, non-alcoholic steatohepatitis (NASH), acne, obesity, diabetes, and cancer. Also provided herein are pharmaceutical compositions comprising the spirolactone compound of Formula I, or pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to a composition for injectable formulation, the composition comprising: —An aqueous solution of ibuprofen and arginine with a molar ratio of ibuprofen:arginine comprised between 1:1.1 and 1:2.1; —An aqueous solution of a diuretic compound comprising between 3.9% and 4.35% w/v of the diuretic compound. The present invention also concerns a pharmaceutical composition comprising said composition and the use of said composition and said pharmaceutical composition.

Abstract: It is provided a pharmaceutical composition comprising 3-beta-hydroxy-5-alpha-pregnan-20-one, at least one sterol or an ester thereof and a mixture of acylglycerols with a solid fat content of less than 25% at 25° C. and 0% at 37° C. In addition it is provided a method for preparing the pharmaceutical composition.

Abstract: The present invention provides methods and composition suitable for stabilizing cell-containing samples such as blood samples. The stabilizers used are primary or secondary carboxylic acid amides.

Abstract: A drug product and method for treating a parasitic disease in a host is described. The drug product comprises: a carrier matrix; and a drug substance having the formula: wherein: R1 is selected from the group consisting of H, aliphatic of 1 to 100 carbons and arene comprising up to 100 carbons; each R3 is independently selected from the group consisting of H, aliphatic of 1 to 100 carbons and arene comprising up to 100 carbons; Y represents those elements necessary to form a 5 or 6 membered ring; X is selected from the group consisting of B, O, N, S, Se and P; and n is 1-4 as necessary to complete the valence of X.

Abstract: Neuropeptide FF receptor modulators based on a proline scaffold are provided which offer NPFF receptor potencies in the nanomolar range and antagonistic selectivity for the NPFF1 receptor. Methods, compounds and compositions for modulating the function of neuropeptide FF receptors are provided for pharmacotherapies capable of influencing conditions or disorders affected by the neuropeptide FF receptors.

Abstract: The present invention discloses a composition comprising 70%-80% w/w tetrahydrocurcuminoids, 10%-20% w/w hexahydrocurcuminoids and 5%-10% w/w octahydrocurcuminoids and its therapeutic application. More specifically, the present invention discloses the use of a composition comprising 70%-80% w/w tetrahydrocurcuminoids, 10%-20% w/w hexahydrocurcuminoids and 5%-10% w/w octahydrocurcuminoids in the therapeutic management of interstitial lung disease or lung fibrosis.

Abstract: Provided herein are novel isotretinoin formulations that provide an enhanced targeted dermal delivery system for the drug isotretinoin with improved thermodynamic activity using no to a small level of ethanol relative to existing isotretinoin gel products, and methods for treatment of ichthyosis and other skin conditions using the same.

Abstract: In some embodiments, methods of inhibiting, ameliorating, reducing the severity of, treating, reducing the likelihood of, or preventing social isolation stress or symptoms thereof in a subject in need thereof are described. In some embodiments, methods of determining a risk of social isolation stress in a subject are described.

Abstract: The present invention relates to a composition for preventing, alleviating or treating inflammatory diseases, comprising, as an active ingredient, an acylhydrazone derivative compound, a stereoisomer thereof or a pharmaceutically acceptable salt thereof. an acylhydrazone derivative compound, a stereoisomer thereof or a pharmaceutically acceptable salt thereof, of the present invention, effectively inhibits inflammatory cytokines and inflammatory signaling pathways, thereby effectively alleviating symptoms of inflammatory diseases such as dermatitis. Therefore, the composition according to the present invention may be effectively used for the prevention, alleviation or treatment of inflammatory diseases.

Abstract: The present invention relates to a method of treating PIK3CA-Related Overgrowth Spectrum (PROS) more particularly, Congenital, Lipomatous, Overgrowth, Vascular Malformations, Epidermal Nevi and Spinal/Skeletal Anomalies and/or Scoliosis (CLOVES) 10 syndrome. To date, there are no specific treatments for patients and no animal models of PROS to better understand the physiopathology of the disorder. Inventors developed a genetic mouse model of PROS that recapitulates the human disease and demonstrated the efficacy of BYL719. Based on these results they treated two patients, one adult and one child, with severe CLOVES syndrome using BYL719. The drug had a robust efficiency on disease in the 15 two patients inducing quick recovery of all affected organs. Thus, the invention relates to a method of treating PROS in a subject in need thereof comprising the step of administrating the subject with a therapeutically effective amount of BYL719.

Abstract: The invention provides compounds which are selective PDE2 inhibitors for use in the treatment of tachycardia or tachyarrhythmia Such compounds are particularly suitable for use in the treatment of any of the following conditions: atrial tachycardia, atrial fibrillation, atrial flutter, paroxysmal supraventricular tachycardia, premature ventricular contractions (PVCs), ventricular fibrillation and ventricular tachycardia, and may be used alone or in combination therapy with other conventional cardiovascular drugs, e.g. beta-blockers. In particular, the invention provides compounds which are selective PDE2 inhibitors for use in the treatment of ventricular tachycardia in patients who are suffering from, or who are at risk of suffering from heart failure, CPVT or long QT syndrome.

Abstract: The present disclosure provides methods and compositions for reducing the risk of pathological effects of traumatic brain injury.

Abstract: The present invention is directed to methods of treating multiple myeloma by administering a compound of Formula (I) or pharmaceutically acceptable salt thereof.

Abstract: Co-crystals comprising the Nuclear receptor related 1 protein-ligand binding domain (Nurr1-LBD) and a cyclopentenone prostaglandin are provided. Also provided are methods of identifying or designing Nurr1-modulating ligands and compounds based on the crystal structures described herein as well as the applications of said ligands and compounds as Nurr1 modulators or medicaments.