Provided herein are multicyclic compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.

Provided is an orally disintegrating tablet comprising brexpiprazole or a salt thereof that rapidly disintegrates in the oral cavity while having hardness suitable for practical use.

More specifically, provided is an orally disintegrating tablet comprising (A) brexpiprazole or a salt thereof, (B) D-mannitol, (C) partially pregelatinized starch, and (D) a lubricant.

An object of the present invention is to provide a compound having an anti-inflammatory activity or a pharmacologically acceptable salt thereof. The solution of the present invention is a compound of general formula (1) or a pharmacologically acceptable salt thereof. ##STR00001##
wherein the symbols in the formula are defined below:
A: e.g., Benzene, E: e.g., —CH.sub.2—, G: e.g., a 5-membered aromatic heterocyclic ring, X: e.g., cyclohexane, J: e.g., a 5-membered aromatic heterocyclic ring, Y: e.g., a phenyl group, R.sup.1, R.sup.2, R.sup.3: e.g., a halogen atom, R.sup.4: e.g., a C1-C6 alkyl group, R.sup.5: e.g., a hydrogen atom, R.sup.6a, R.sup.6b, R.sup.6c, R.sup.6d: e.g., a hydrogen atom, R.sup.7: e.g., a hydrogen atom, R.sup.8: e.g., a hydrogen atom, n.sup.1, n.sup.2, n.sup.3: e.g., 1.

The present technology is directed to compositions comprising d-threo-methylphenidate conjugates and/or unconjugated methylphenidate. The present technology also relates to compositions and oral formulations comprising d-threo-methylphenidate conjugated to nicotinoyl-L-serine, and/or a pharmaceutically acceptable salt thereof, and unconjugated methylphenidate and/or a pharmaceutically acceptable salt thereof. The present technology additionally relates to a pharmaceutical kit containing the composition comprising d-threo-methylphenidate conjugated to nicotinoyl-L-serine, and/or a pharmaceutically acceptable salt thereof, and unconjugated methylphenidate and/or a pharmaceutically acceptable salt thereof.

The subject invention concerns materials and methods for treating and/or preventing diseases associated with accumulation of Aβ peptide in neural tissue. The subject invention also concerns materials and methods for treating and/or preventing stress disorders, such as post-traumatic stress disorder (PTSD). In one embodiment, a method of the invention comprises administering a therapeutically effective amount of cotinine, or a pharmaceutically acceptable salt thereof, to a person or animal in need of treatment. The methods of the invention can be used to prevent and/or treat Alzheimer's disease, Parkinson's disease, and/or Down's syndrome. The subject invention also concerns compositions that comprise cotinine, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, diluent or adjuvant. The subject invention concerns materials and methods for detecting and diagnosing conditions associated with accumulation of Aβ peptide in neural tissue, such as Alzheimer's disease and Parkinson's disease, using the chemical cotinine. In one embodiment, the method comprises administering cotinine labeled with a detectable label to a person or animal. The presence of labeled cotinine in neural tissue is then determined. The level and/or location of cotinine can be analyzed and a diagnosis made. The subject invention also concerns cotinine labeled with a detectable label. In one embodiment, the cotinine is labeled with a radioisotope that can be detected by Positron Emission Tomography (PET) or single photon emission computed tomography (SPECT).

Described herein are compositions comprising (a) methyl 3 -((methyl sulfonyl)amino)-2-(((4-phenylcyclohexyl)oxy)methyl)piperidine- 1 -carboxylate or a salt thereof; and (b) an agent for reducing metabolism of (a) and uses thereof.

The disclosed compositions methods relate to a dietary supplement for subjects with slow caffeine metabolism and comprises paraxanthine and optionally other compounds that modulate the effects of paraxanthine. Uses for the paraxanthine-containing supplements contain improvement of at least one of endurance performance, mood, vigor, lipolysis, energy expenditure, exercise performance, and/or decreased appetite in a slow caffeine metabolizer subject.

The present invention relates to a medicament for treating or preventing a disease related to orexin receptor, especially orexin type 2 receptor, comprising a new compound having a urea structure or a pharmaceutically acceptable salt thereof as an active ingredient. In more detail, the present invention relates to a medicament for treating or preventing narcolepsy, idiopathic hypersomnia, hypersomnia, sleep apnea syndrome, etc.

The present invention relates to a medicament for treating or preventing a disease related to orexin receptor, especially orexin type 2 receptor, comprising a new compound having a urea structure or a pharmaceutically acceptable salt thereof as an active ingredient. In more detail, the present invention relates to a medicament for treating or preventing narcolepsy, idiopathic hypersomnia, hypersomnia, sleep apnea syndrome, etc.

A method for treating narcolepsy type 1 in a subject in need thereof is disclosed, comprising administering to the subject an effective amount of methyl 3-((methylsulfonyl)anhino)-2-(((4-phenylcyclohexyl)oxy)methyl)piperidine-1-carboxylate (Compound (I)), or a salt thereof, wherein plasma concentration for Compound (I) is about 5.04 ng/mL or more for about 1 hour or more. Compositions for treating narcolepsy type 1 comprising Compound (I) are also disclosed.