Abstract: A method for the treatment and/or prevention of pain which comprises administering to a subject in need of such treatment a therapeutically effective amount of 1-(3-4(((1R,3S,5S)-adamantan-1-yl)(phenyl)methyl)propyl)-4-methylpiperazine and pharmaceutically acceptable salts thereof (“AV1066”), with reference to visceral and neuropathic pain.

Abstract: This disclosure pertains to compounds, the preparation thereof, and the use of these compounds in the treatment of prostate cancer, including metastatic and/or castrate-resistant prostate cancer, in subjects in need thereof.

Abstract: This invention is directed to a pharmaceutical composition for drinking water administration comprising isoxazoline compounds of formula (I) and a polysorbate surfactant and diethylene glycol monoethyl ether (transcutol); and the use of the composition to treat or prevent parasite infestations of animals.

Abstract: The invention relates to the use of mavoglurant, or a pharmaceutically acceptable salt thereof: in the reduction of cocaine use by a cocaine use disorder patient; in preventing relapse into cocaine use by a cocaine use disorder patient; in the promotion of cocaine abstinence by a cocaine use disorder patient; in in the treatment of the symptoms of depression or anxiety associated with cocaine use disorder.

Abstract: Methods of treating presbyopia or cataract in a subject in need thereof are provided. The methods require administering to the subject an effective amount of a composition comprising a compound that inhibits the formation of high molecular weight aggregates of human ?-A-crystallin. Compositions containing certain compounds are believed to be also effective in the treatment of transthyretin (TTR)-associated amyloidosis and Parkinson's disease.

Abstract: The present invention relates to the use of selective aquaporin inhibitors, e.g., of aquaporin-4 or aquaporin-2, e.g., certain phenylbenzamide compounds, for the prophylaxis, treatment and control of aquaporin-mediated conditions, e.g., diseases of water imbalance, for example edema (particularly edema of the brain and spinal cord, e.g., following trauma or ischemic stroke, as well as the edema associated with glioma, meningitis, acute mountain sickness, epileptic seizures, infections, metabolic disorders, hypoxia, water intoxication, hepatic failure, hepatic encephalopathy, diabetic ketoacidosis, abscess, eclampsia, Creutzfeldt-Jakob disease, and lupus cerebritis, as well as edema consequent to microgravity and/or radiation exposure, as well as edema consequent to invasive central nervous system procedures, e.g.

Abstract: The present disclosure relates to the field of synthesizing substantially pure varenicline and its intermediates. It also relates to the pharmaceutical compositions comprising varenicline and the method of use of these pharmaceutical compositions for smoking cessation.

Abstract: The present invention relates to carbamoyl phenylalaninol compounds and methods of using the same to treat disorders. The invention further relates to the development of methods for treating excessive sleepiness in a subject, e.g., due to narcolepsy or obstructive sleep apnea, with the surprising outcome that “normal” levels of wakefulness are achieved based on standard objective and subjective sleepiness tests.

Abstract: This invention provides compounds that inhibit p38 mitogen-activated protein kinase. Moreover, the invention provides methods for testing a candidate compound for a p38 mitogen-activated protein kinase modifying activity by calculating the level of relocalization of an SMN complex component from the cytoplasm to the nucleus of a cell. Additionally, the invention provides a kit and a system for calculating the same.

Abstract: The invention provides two crystalline freebase forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester. The invention also provides pharmaceutical compositions comprising the crystalline freebase or prepared using the crystalline freebases; processes and intermediates for preparing the crystalline freebases; and methods of using the crystalline freebases to treat a pulmonary disorder.

Abstract: The present invention is directed to methods and uses of a series of compounds and compositions comprising the same for treating diseases, disorders and/or conditions related to fertility and preserving same and conditions related to same. In some aspects, the compounds and or compositions as herein described promote, improve, recover or restore fertility in a subject in need thereof, including in male and/or female subjects. Such methods/uses include promoting, enhancing or improving fertility-associated cell or tissue yield as part of an in vitro fertilization protocol.

Abstract: The present invention is directed to new bifunctional compounds and methods for treating HIV infections. The bifunctional small molecules, generally referred to as ARM-HI's, function through orthogonal pathways, by inhibiting the gp120-CD4 interaction, and by recruiting anti-DNP antibodies to gp120-expressing cells, thereby preventing cell infection and spread of HIV. It has been shown that ARM-HI's bind to gp120 and gp-120 expressing cells competitively with CD4, thereby decreasing viral infectivity as shown by an MT-2 cell assay, the binding leading to formation of a ternary complex by recruiting anti-DNP antibodies to bind thereto, the antibodies present in the ternary complex promoting the complement-dependent destruction of the gp120-expressing cells. Compounds and methods are described herein.

Abstract: Disclosed herein are pharmacologically acceptable and ophthalmologically suitable compositions and methods of their use in treating ophthalmic diseases or related conditions. In aspects, the invention provides compositions comprising effective amounts of carbonic anhydrase inhibitor(s) and alpha-2-adrenergic agonist(s). In facets, compositions comprise a penetration enhancer component comprising one or more penetration enhancer compound(s)/molecule(s). In aspects, the invention provides compositions comprising effective amounts of brimonidine compound(s) and brinzolamide compound(s) capable of being administered once or twice daily for the treatment of elevated intraocular pressure, but which provide similar efficacy to a similar or substantially identical reference product requiring administration three times per day.

Abstract: The object of the present invention is to provide a formulation with the effect of effectively suppressing or inhibiting amyloid fibril formation by the dissolution, elimination (discharge), etc. of amyloid fibril formation in vivo. If an agent for suppressing or inhibiting an amyloid fibril formation comprising tranilast or a pharmacologically acceptable salt thereof as an active ingredient is administered by a method such as oral administration, amyloid fibril formation can be effectively suppressed or inhibited in vivo as a result of effects such as amyloid fibril dissolution or elimination (discharge). Therefore, it is possible to prevent or treat amyloid plaques, in which amyloid fibrils formed by the aggregation of amyloid protein have been deposited, and to prevent or treat diseases arising from amyloid fibril deposition, that is, diseases arising from the deposited amyloid fibrils themselves and diseases that cause dysfunction of organs or tissues as a result of amyloid fibril deposition.

Abstract: Embodiments of the invention are directed to formulations that provide a solution to the problem of small molecule (e.g., diazepam) precipitation at the injection site when administered as a highly-concentrated formulation. In certain aspects the formulations include at least one surfactant in a non-aqueous formulation, which prevents small molecule precipitation and improves the bioavailability of the drug by enhancing absorption into the systemic circulation.

Abstract: Disclosed herein are methods of inhibiting tumor growth or producing tumor regression in a subject having a drug-resistant estrogen receptor alpha positive cancer or a mutant estrogen receptor alpha positive cancer. The methods entail administering to the subject a therapeutically effective amount of RAD1901 having the structure: or a salt or solvate thereof.

Abstract: The disclosure is directed to glucocorticoids for the treatment of epithelial microbial infections in fluid-containing organ having a natural exterior orifice in mammals; this new therapeutic use finds particular interest in the treatment of epithelial microbial infections of ear (such as otitis externa), udder (such as mastitis), and uterus (such as endometritis).

Abstract: Problem: to provide an activator for activating intracellular ATP production. Solution: use of a pyridodipyrimidine compound represented by the following formula (II): wherein, R1 and R3 each represent a hydrogen atom, an alkyl group, a halogen-substituted alkyl group, a carboxy-substituted alkyl group, a phenyl group, a phenyl group substituted by one of a halogen atom, a lower alkyl group, or a lower alkoxy group, or a lower alkyl disubstituted phenyl group and R2 represents an alkyl group, a cycloalkyl group, a phenyl-substituted lower alkyl group, a phenyl group, a phenyl group substituted by one of a halogen atom, a lower alkyl group, or a lower alkoxy group, or a lower alkyl disubstituted phenyl group for activating intracellular ATP production, the use comprising introducing said pyridodipyrimidine compound to a human-derived neuron cells, wherein said pyridodipyrimidine compound is used as a coenzyme factor effective for activating intracellular ATP production.

Abstract: The application describes creatine or its derivatives, compositions comprising the same, and uses thereof for topical or systemic administration to treat pain, itch, or eczema, or inflammation associated with a cosmetic or medical condition, disorder or disease in a human subject, wherein the inflammation causes the pain, itch, or eczema. In addition, the application describes clinical use of these compounds and compositions which can reduce or eliminate erythema, edema and tissue distortions associated with inflammation.

Abstract: Problem: to provide an activator for activating intracellular ATP production. Solution: use of deazaflavino-testosterone compound represented by the following formula (III): wherein, R1 represents a hydrogen atom, an alkyl group, a halogen-substituted alkyl group, a carboxy-substituted alkyl group, a phenyl group, or a phenyl group substituted by one of a halogen atom, a lower alkyl group, or a lower alkoxy group and R2 represents an alkyl group, a cycloalkyl group, a phenyl-substituted lower alkyl group, a phenyl group, a phenyl group substituted by one of a halogen atom, a lower alkyl group, or a lower alkoxy group, or a lower alkyl disubstituted phenyl group for activating intracellular ATP production, the use comprising introducing said deazaflavino-testosterone compound to a human-derived neuron cells, wherein said deazaflavino-testosterone compound is used as a coenzyme factor effective for activating intracellular ATP production.