Abstract: The present embodiments are related to the compound of Formula 1 or Formula 2 below and pharmaceutical formulations thereof as well as treatments for a wide variety of Central Nervous System disorders with the pharmaceutical formulations. Some embodiments include the use of a variety of the instant compounds which surprisingly and advantageously exhibit improved pharmacokinetic and therapeutic profiles in comparison to pivagabine.

Abstract: Pharmaceutical presentations or phenoxathiin-based MAO-A inhibitors are disclosed whereby the MAO receptors are capable of sustained release in the digestive tract. Particular phenoxathiin-based MAO-A inhibitors include those of the following formula: wherein n is 0, 1 or 2; R1 is a branched or straight chain C1-5 alkyl or C3-6 cycloalkyl optionally substituted with hydroxyl, or one or more halogens; and X1, X2, X3, X4, and X5 are either all hydrogens or one or two of X1, X2, X3, X4, and X5 are halogen and the remainder are hydrogens, with the proviso that when n is 0 or 1 and each X is hydrogen, R1 is not methyl. A wide variety or sustained release mechanisms can be utilized so as to provide gradual release of the active ingredient after ingestion as a pharmaceutical presentation, such as a tablet or capsule. Presentations include sustained release tablets, sustained release capsules, capsules containing sustained release beads.

Abstract: Pharmaceutical presentations of phenoxathiin-based MAO-A inhibitors are disclosed whereby the MAO receptors are protected from binding to active ingredient in the stomach. Particular phenoxathiin-based MAO-A inhibitors include those of the following formula: (I) wherein n is 0, 1 or 2; R1 is a branched or straight chain C1-5 alkyl or C3-6 cycloalkyl optionally substituted with hydroxyl, or one or more halogens; and X1, X2, X3, X4, and X5 are either all hydrogens or one or two of X1, X2, X3, X4, and X5 are halogen and the remainder are hydrogens, with the proviso that when n is 0 or 1 and each X is hydrogen, R1 is not methyl. A wide variety of enteric mechanisms may be utilized so as to provide release of the active ingredient essentially out of the environment of the stomach after ingestion as a pharmaceutical presentation, such as a tablet or capsule. Presentations include enteric coated tablets, enteric coated capsules, capsules containing enteric coated beads.

Abstract: The present embodiments are related to the compound of Formula 1 or Formula 2 below and pharmaceutical formulations thereof as well as treatments for a wide variety of Central Nervous System disorders with the pharmaceutical formulations. Some embodiments include the use of a variety of the instant compounds which surprisingly and advantageously exhibit improved pharmacokinetic and therapeutic profiles in comparison to pivagabine.

Abstract: Provided are methods for reducing the excipient load of pharmaceutical formulations containing 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathiin 10,10-dioxide as the active pharmaceutical ingredient, and compositions related thereto. In particular, provided is a pharmaceutical product comprising 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathiin 10,10-dioxide and a stabilizer admixed throughout a solid-form unilamellar matrix, wherein the ratio of 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathiin 10,10-dioxide to stabilizer ranges from about 2:3 to about 1:10, and related methods of forming the pharmaceutical product.

Abstract: Provided herein is a new form of 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathin 10,10-dioxide, which demonstrates higher stability relative to other forms of 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathiin-10,10-dioxide. In particular, this new form affords less dosage critical administration of 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathin 10,10-dioxide relative to other forms. The new solid form of 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathiin-10,10-dioxide has been determined and is provided herein. This new solid form of 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathiin-10,10-dioxide can be characterized by any of a number of its properties, including, but not limited to, melting point, differential scanning calorimetry, infrared spectroscopic spectrum or portions thereof, solubility, methods and conditions under which this form is prepared, and/or precipitated from solution, and, when in crystalline form, the crystalline form can be characterized according to the diffraction pattern or portions thereof.

Abstract: The present embodiments are related to the compound of Formula 1 or Formula 2 below and pharmaceutical formulations thereof as well as treatments for a wide variety of Central Nervous System disorders with the pharmaceutical formulations. Some embodiments include the use of a variety of the instant compounds which surprisingly and advantageously exhibit improved pharmacokinetic and therapeutic profiles in comparison to pivagabine.

Abstract: The present embodiments are related to the compound of Formula 1 or Formula 2 below and pharmaceutical formulations thereof as well as treatments for a wide variety of Central Nervous System disorders with the pharmaceutical formulations. Some embodiments include the use of a variety of the instant compounds which surprisingly and advantageously exhibit improved pharmacokinetic and therapeutic profiles in comparison to pivagabine.

Abstract: Provided herein is a new form of 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathin 10,10-dioxide, which demonstrates higher stability relative to other forms of 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathiin-10,10-dioxide. In particular, this new form affords less dosage critical administration of 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathin 10,10-dioxide relative to other forms. The new solid form of 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathiin-10,10-dioxide has been determined and is provided herein.