Abstract: Compounds of Formula (I) are estrogen receptor alpha modulators, where the variables in Formula (I) are described in the disclosure. Such compounds, as well as pharmaceutically acceptable salts and compositions thereof, are useful for treating diseases or conditions that are estrogen receptor alpha dependent and/or estrogen receptor alpha mediated, including conditions characterized by excessive cellular proliferation, such as breast cancer.

Abstract: Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.

Abstract: The present invention includes substituted pyridinone-containing tricyclic compounds, and compositions comprising the same, that can be used to treat or prevent hepatitis B virus (HBV) infection in a patient. In certain embodiments, the compounds and compositions of the invention inhibit and/or reduce HBsAg secretion.

Abstract: Compositions for treatment of various nasal and/or sinus conditions, such as sinusitis, rhinitis, nasal drip, coughing, sneezing, cold, influenza, viral infections, and the like, along with related treatment methods. Certain compositions according to preferred embodiments of the invention may comprise one or more antihistamines, one or more corticosteroids, and xylitol. Some embodiments may further comprise aloe vera and/or various other optional ingredients, such as benzalkonium chloride and/or grapefruit seed extract.

Abstract: Provided are methods and compositions for treating cancers in patients carrying an IDH1 mutation or IDH2 mutation.

Abstract: Compositions, methods and formulation for the treatment and prophylactic management of an Antibacterial Formulation for Treating and Prophylactic use in Bacterial, and Fungal Urinary Bladder Infections include a solution comprising of Cetylpyridinium chloride and Sodium chloride in concentrations of Cetylpyridinium chloride, 0.01% to 5% and Sodium chloride, 1% to 10% at a pH of 4.5 to 8.5.

Abstract: Novel compounds of the structural formula I, and the pharmaceutically acceptable salts thereof, are inhibitors of TarO and may be useful in the prevention, treatment and suppression of diseases mediated by TarO, such as bacterial infections, including gram negative bacterial infections and gram positive bacterial infections such as MRSA and MRSE, alone or in combination with a ?-lactam antibiotic.

Abstract: The present invention relates to a pharmaceutical formulation which provides for extended release of an active pharmaceutical ingredient selected from N-[2-hydroxy-3-(1-piperidinyl)-propoxy]-pyridine-1-oxide-3-carboximidoyl chloride, its stereoisomers and the acid addition salts thereof.

Abstract: Provided herein are compounds, derivatives thereof, composition comprising one or more of said compounds and derivatives, and methods for prevention and/or treatment of microbial infections and/or related diseases or conditions. The present compounds and/or derivatives thereof can be represented by Formula (II): The present methods include administering to a subject an effective amount of one or more compounds of Formula (II). In one embodiment, said microbial infections are bacterial infections. More specifically, said bacterial infections are staphylococcal infections.

Abstract: An aqueous nicotine solution for use in an active mesh nebulizer as part of a smoking cessation program, or as a substitute for tobacco use, includes nicotine in water with a nicotine concentration ranging from about 1.0 milligram (mg) nicotine per milliliter (ml) of water (e.g., 0.01% nicotine), to about 0.005 mg nicotine per milliliter of water (about 0.0005% nicotine). The pH of the aqueous nicotine solution ranges from about 3.5 to about 12 because the plume of particles of aqueous nicotine solution produced by the active mesh nebulizer are entrained with the inhaled air and do not impact the walls of the throat or lungs. The aqueous nicotine solution is free from metals because it is delivered to a user at room temperature, without heating or boiling.

Abstract: This invention relates to the use of zinc(II) salts in combination with a zinc ionophore to resensitize a previously resistant pathogenic bacteria to an antibiotic. Methods of restoring the sensitivity of a resistant pathogenic bacterium to an antibiotic comprising administering a zinc ionophore in combination with a zinc(II) salt and methods of treating a bacterial infection comprising administering a zinc ionophore in combination with a zinc (II) salt concurrently and/or sequentially with administration of a therapeutically effective amount of an antibiotic is also described.

Abstract: Disclosed is the synthesis procedure for benzazolo[3,2-a]quinolinium chloride salts and the inclusion of chloro-substituent, amino-substituent, and nitro-substituent resulting in several compounds. The compounds are further used as markers due to their fluorescent properties including in hypoxic environments. This disclosure further describes anti-cancer screening of two BQS, namely, 7-benzyl-3-aminobenzimidazo[3,2-a]quinolinium chloride (ABQ-48: NSC D-763307) and the corresponding 7-benzyl-3-nitrobenzimidazo[3,2-a]quinolinium chloride (NBQ 48: NSC D-763303).

Abstract: Compounds of Formula I: pharmaceutically acceptable salts thereof, enantiomers thereof, metabolites thereof, derivatives thereof, prodrugs thereof, acid addition salts thereof, pharmaceutically acceptable salts thereof, or N-oxides thereof; or a combination thereof, processes and intermediates for preparation thereof, compositions thereof, and uses thereof, are provided. Pharmaceutical compositions comprising a compound of Formula I, or enantiomers thereof, metabolites thereof, derivatives thereof, prodrugs thereof, acid addition salts thereof, pharmaceutically acceptable salts thereof, or N-oxides thereof; or a combination thereof, wherein the compound is double and/or triple agent or ligand for CYP2D6, 5-HT2A, and/or 5HT2C receptors, and/or acetylcholinesterase; and methods comprising co-administering a compound of Formula I and an N-Methyl-d-Aspartate (NMDA) receptor antagonist to a subject in need thereof, and dosage forms, drug delivery systems, methods of treatment thereof.

Abstract: The invention relates to the surprising discovery that TMZ and pharmaceutical salts thereof are an effective pharmacological agent in the treatment of certain decompensating patients with an underlying chronic liver condition. In particular, TMZ or a pharmaceutical salt thereof is useful in treating cirrhosis patients having a Child Pugh score of at least 10, but not having a Child Pugh Score less than 10. In addition, TMZ or a pharmaceutical salt thereof is discovered to be useful in decompensating cirrhotics who are suffering from at least one organ system failure selected from the group consisting of hepatic, coagulation, renal, cerebral, circulatory and respiratory. Further to that, TMZ or a pharmaceutical salt thereof is useful in treating patients with acute-on-chronic liver.

Abstract: The present invention relates to a pharmaceutical combination comprising an FGFR4 inhibitor and a bile acid sequestrant, to the use of the pharmaceutical combination in the treatment of cancer, to the use of a bile acid sequestrant to reduce or mitigate side-effects associated with FGFR4 inhibition therapy.

Abstract: The present disclosure provides methods of reducing or eliminating HIV reservoirs in a human infected with HIV, comprising administering to the human a therapeutically effective amount of a Bcl-2 family inhibitor and one or more additional agents. Additional agents include a therapeutically effective amount of a latency reversing agent, a therapeutically effective vaccine which enhances CTL responses, an immunotherapy which enhances CTL responses, a therapeutically effective vaccine which enhances CD8+ T-cell responses, an immunotherapy which enhances CD8+ T-cell responses, a CTL, or a CD8+ T-cell.

Abstract: Pharmaceuticals compositions comprising the 2S, 4R, ketoconazole enantiomer or its pharmaceutically acceptable salts, hydrates, and solvates, that are substantially free of the 2R, 4S ketoconazole enantiomer are useful to reduce cortisol synthese and for the treatment of type 2 diabetes, hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other diseases and conditions, including but not limited to Cushing's Syndrome, depression, and glaucoma.

Abstract: Provided are compounds that target the lanthionine synthetase C-like protein 2 pathway. The compounds can be used to treat a number of conditions, including infectious disease, autoimmune disease, diabetes, and a chronic inflammatory disease.

Abstract: The present disclosure describes a method of treating pulmonary disorders, such as pulmonary arterial hypertension, using a combination of a PDGF receptor kinase inhibitor, PDEV inhibitor, and an endothelin receptor antagonist. The compounds can inhibit cell growth and proliferation and target the underlying pathology of PAH.

Abstract: Amorphous solid dispersions of nilotinib fumarate or nilotinib tartrate are provided, as well as pharmaceutical compositions thereof, wherein the compositions exhibit enhanced bioavailability in the fasted state. Preferably, the compositions may be orally administered to a patient in either the fed or fasted state, with a decrease or elimination of the food effect. Preferably, following oral administration of the pharmaceutical compositions, there is no substantial difference in the pharmacokinetic parameters (e.g., Cmax, AUC0-t and/or AUC0-infinity) of nilotinib, regardless of whether the pharmaceutical compositions are administered to a subject in the fed or fasted state.

Abstract: The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 (“mGluR2”). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved.

Abstract: The invention relates to oral pharmaceutical compositions comprising pimobendan pharmaceutically active compound. It also relates to a method for preparing the same uses thereof.

Abstract: Disclosed are a preparation method of an orexin receptor antagonist compound 5-3. Crystalline forms I-IV of an orexin receptor antagonist compound 5-3 are provided. Also provided are processes of preparing crystalline forms of the orexin receptor antagonist compound 5-3, as well as methods of using the crystalline forms I-IV for treating an orexin-related disease.

Abstract: Disclosed is a preparation method of an orexin receptor antagonist compound 5-3. Crystalline forms I-IV of an orexin receptor antagonist compound 5-3 are provided. Also provided are processes of preparing crystalline forms of the orexin receptor antagonist compound 5-3, as well as methods of using the crystalline forms I-IV for treating an orexin-related disease.

Abstract: A compound having the structure set forth in Formula (I) and Formula (II): wherein the substituents Y, Z, A, B, R1, R2, R3, R4 and R5 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.

Abstract: An epidermal growth factor receptor (EGFR) family tyrosine kinase inhibitor comprising a functional group that can bind to the serine S797 residue in EGFR having a C797S mutation or the serine S805 residue in HER2 having a C805S mutation.

Abstract: The present invention provides methods for treating ocular surface pain by administering 4-(7-hydroxy-2-isopropyl-4-oxo-4H-quinazolin-3-yl)-benzonitrile (compound I). The present invention also provides methods for treating dry eye disease and ocular hyperemia by administering 4-(7-hydroxy-2-isopropyl-4-oxo-4H-quinazolin-3-yl)-benzonitrile.

Abstract: The present invention provides formulations of 4-(7-hydroxy-2-isopropyl-4-oxo-4H-quinazolin-3-yl)-benzonitrile (compound I) and methods for treating ocular surface pain by administering such formulations. The present invention also provides methods for treating dry eye disease and ocular hyperemia by administering formulations of 4-(7-hydroxy-2-isopropyl-4-oxo-4H-quinazolin-3-yl)-benzonitrile.

Abstract: The present invention relates to a pharmaceutical composition with enhanced stability, containing pemetrexed or a salt thereof, and a preparation method therefor. The present invention provides an injection preparation in liquid form containing pemetrexed, capable of ensuring sufficient stability during circulation and storage by selection of an optimum material and setting of an optimum concentration range in order to secure the stability of pemetrexed. The present invention can provide a pemetrexed preparation which is readily commercially prepared, can prevent microbial contamination occurring during lyophilization or reconstitution, and has enhanced convenience of administration and stability.

Abstract: The present invention provides a compound represented by formula I, pharmaceutically acceptable salts, enantiomers, diastereomers or racemates thereof, the preparation method thereof, the pharmaceutical composition comprising the same, and the use thereof in the preparation of a medicament for treating a disease or condition mediated by EED and/or PRC2. The compound of the present invention can be used treating PRC2-mediated diseases or conditions.

Abstract: The invention relates to amorphous folate salt. The salt consists of a folate anion and an organic cation. The folate anion is selected from the group consisting of 5-formyl-(6S)-tetrahydrofolic acid, 10-formyl-(6R)-tetrahydrofolic acid, 5-methyl-(6S)-tetrahydrofolic acid, (6S)-tetrahydrofolic acid, 5,10-Methylene-(6R)-tetrahydrofolic acid, and its oxidized derivatives JK12A and Mefox, and the cation is an organic compound selected from the group arginine, choline, acetylcholine, 1,1-dimethyl-biguanidin and phenylethylbiguanidin. The cation is an organic compound with a complementary pharmacological activity.

Abstract: The present application relates to the use of fused heteroaromatic pyrrolidones for treatment and/or prophylaxis of allergic and/or inflammatory diseases in animals and to the use thereof for production of medicaments for treatment and/or prophylaxis of allergic and/or inflammatory diseases in animals, especially of atopic dermatitis and/or Flea Allergy Dermatitis, and especially in domestic animals, particularly in dogs.

Abstract: Provided herein are, inter alia, methods for treating cancer in subjects expressing elevated levels of adenosine A2A receptors, and optionally further expressing elevated levels of CD73 and/or PD-L1, by administering adenosine pathway inhibitors and PD-1 pathway inhibitors.

Abstract: The invention provides methods for treating a cancer selected from the group consisting of (i) a squamous cell carcinoma located in a patient's head and/or neck and (ii) a urothelial carcinoma using aryl dihydro-2H-benzo[b][1,4]oxazine sulfonamide compounds.

Abstract: Compounds of formula (1): wherein A1, A2, Ra, Rb, Rc, Rd, R3, R4, R5 and T are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.

Abstract: Disclosed are methods of synthesis and/or purification of certain 3,7-diamino-phenothiazin-5-ium compounds (“diaminophenothiazinium compounds”) including Methylthioninium Chloride (MTC) (Methylene Blue), and the resulting high purity characterized by a purity greater than 98%, and very low levels of heavy metals and organic impurities Azure A, B, C and MVB. Also disclosed are methods of treatment of a tauopathy or methemoglobinemia in a patient in need thereof, comprising administering to the patient a therapeutically effective amount of the high-purity diaminophenothiazinium compound.

Abstract: Disclosed herein are compositions comprising an NSAID such as meloxicam and/or rizatriptan in combination with a cyclodextrin and/or a carbonate or a bicarbonate. These compositions may be orally administered, for example, to improve the bioavailability or pharmacokinetics of the NSAID for the treatment of pain such as migraine, arthritis, and other conditions. Also disclosed herein are methods of treating pain, such as migraine, comprising administering meloxicam and rizatriptan to a human being suffering from pain, such as migraine. For migraine, these methods may be particularly useful when the meloxicam and rizatriptan are administered while the human being is suffering from an acute attack of migraine pain or migraine aura. In some embodiments, the combination of meloxicam and rizatriptan may be administered in a manner that results in a Tmax of meloxicam of 3 hours or less.

Abstract: Disclosed herein are compositions comprising an NSAID such as meloxicam and/or rizatriptan in combination with a cyclodextrin and/or a carbonate or a bicarbonate. These compositions may be orally administered, for example, to improve the bioavailability or pharmacokinetics of the NSAID for the treatment of pain such as migraine, arthritis, and other conditions. Also disclosed herein are methods of treating pain, such as migraine, comprising administering meloxicam and rizatriptan to a human being suffering from pain, such as migraine. For migraine, these methods may be particularly useful when the meloxicam and rizatriptan are administered while the human being is suffering from an acute attack of migraine pain or migraine aura. In some embodiments, the combination of meloxicam and rizatriptan may be administered in a manner that results in a Tmax of meloxicam of 3 hours or less.

Abstract: The present invention provides an extract of Dendrobii Caulis with eye care effect, wherein the extract of Dendrobii Caulis has an active ingredient comprising a picrotoxane-type sesquiterpene. The present invention further provides a pharmaceutical composition with eye care and a use of an extract of Dendrobii Caulis for preparing a pharmaceutical composition with eye care effect.

Abstract: Activators of mitofusins and their uses in treatment of diseases and disorders are disclosed.

Abstract: The present invention provides a method of treating a cancer in a subject comprising administering to the subject an effective amount of a CD33-targeted antibody-drug conjugate (ADC) and an effective amount of a poly-ADP ribose polymerase (PARP) inhibitor. Also provided are pharmaceutical compositions comprising an effective amount of a CD33-targeted ADC and an effective amount of a PARP inhibitor.

Abstract: The present invention provides a method for optimizing levels of mifepristone in a patient suffering from Cushing's syndrome. The method comprises the steps of treating the patient with seven or more daily doses of mifepristone over a period of seven or more days; testing the serum levels of the patient to determine whether the blood levels of mifepristone are greater than 1631 ng/mL; and adjusting the daily dose of the patient to achieve mifepristone blood levels greater than 1631 ng/mL.

Abstract: The invention provides liquid formulation compositions and medicament delivery devices, and methods for preparing and using the same. For example, the liquid formulation composition is an emulsion including a solvent and liquid particles, which includes surfactants and are dispersed in the solvent. The volume average particle size of the liquid particles is less than about 100 ?m; the surface tension of the liquid formulation composition is less than about 60 mN/m; and the absolute value of zeta potential is greater than about 15 mV. The containment vessel may be a sprayer or a dropping device. The invention also provides methods for preparation of the liquid formulation compositions and medicament delivery devices as well as methods for using the same in treatment of various diseases and condition, for example, otitis media, otitis externa, rhinitis, sinusitis, lower respiratory tract inflammation, xerostomia (dry mouth), xerophthalmia (dry eyes) and xeromycteria (dry nose).

Abstract: Compositions and methods for making a pharmaceutical dosage form include making a pharmaceutical composition that includes one or more active pharmaceutical ingredients (API) with one or more pharmaceutically acceptable excipients by thermokinetic compounding into a composite. Compositions and methods of preprocessing a composite comprising one or more APIs with one or more excipients include thermokinetic compounding, comprising thermokinetic processing the APIs with the excipients into a composite, wherein the composite can he further processed by conventional methods known in the art, such as hot melt extrusion, melt granulation, compression molding, tablet compression, capsule filling, film-coating, or injection molding.

Abstract: The invention provides unit dosage forms and methods that are effective to improve prostate function. Such unit dosage forms and methods are useful to decrease bladder discomfort and improve urinary flow in men.

Abstract: Described herein are methods and compositions for the treatment of pancreatic cancer in a subject in need thereof. The pancreatic cancer may be resistant to other therapeutic regimens. The methods may comprise administering ARDA compounds to the subject.

Abstract: The present invention is directed to provide antitumor agent including water-soluble sulfasalazine as an active ingredient. Antitumor agents were obtained with, as the water-soluble sulfasalazine, a PEG-modified sulfasalazine represented by the following formula: wherein an average value of n is 4 or larger and 1136 or smaller.

Abstract: The present discovery pertains generally to the field of therapeutic compounds. More specifically the present discovery pertains to a particular 1-di-alkyl-phosphinoyl-alkane, 1-(Diisopropyl-phosphinoyl)-nonane, referred to herein as “DIPA-1-9”. DIPA-1-9, is able to selectively treat (e.g., suppress) sensory discomfort arising from the airways without side effects. Compared to structurally similar compounds, DIPA-1-9 did not have the problems of excessive cold, stinging, or irritancy, or of adverse taste. To deliver the DIPA-1-9 to the upper airway it is formulated as a solution of DIPA-1-9 in water, a water-based solution, or syrup, at a concentration of 2 to 10 mg/mL and a delivery volume of less than 0.5 mL per unit dose. The drops of DIPA-1-9 are administered into the nasal cavity or onto the base of the tongue, next to the pillars of fauces. The DIPA-1-9 then reaches the nerve endings at the base of the epithelia and transduces signals of coolness and cold.

Abstract: The field of the present invention is that of fosfomycin formulations for parenteral administration, in particular for intravenous administration. Formulations of the prior art provide fosfomycin as a powder to be diluted directly prior to the administration. The aim of the invention is to provide a fosfomycin formulation for parenteral administration which is easier to produce and administer or which lowers the risk of puncture injuries for healthcare professionals and the health risks for the patients (for example due to contamination or incorrect dosages) by preventing additional processing steps. During the course of the invention, it was surprisingly shown that fosfomycin is much more stable in an aqueous solution than what is commonly assumed.

Abstract: An amorphous form of tenofovir alafenamide hemifumarate and process for the preparation of the same. A premix of amorphous tenofovir alafenamide hemifumarate with pharmaceutically acceptable excipients and process for the preparation of the same are also disclosed.