Abstract: The present disclosure provides treprostinil derivatives that can act as prodrugs of treprostinil. The treprostinil derivatives can be used to treat any conditions responsive to treatment with treprostinil, including pulmonary hypertension, such as pulmonary arterial hypertension.

Abstract: A composition for restorative vaginal lubrication and a method of use thereof facilitates enhances the overall vaginal health. The composition includes a quantity of water, a quantity of glycerin, a quantity of cetearyl alcohol, a quantity of glyceryl stearate, a quantity of avocado oil, a quantity of squalene oil, a quantity of lecithin, a quantity of benzoin oil, a quantity of xanthan gum, a quantity of citric acid, a quantity of potassium sorbate, a quantity of Dehydroepiandrosterone (DHEA), a quantity of elderberry extract, a quantity of damiana extract, a quantity of progesterone, a quantity of pomegranate oil, and a quantity of sodium benzoate. The composition is homogeneously mixed into a vaginal salve that may be both externally and internally applied with the vaginal area in order to moisturize the vaginal area and enhance sexual pleasure during sexual activity. The vaginal salve also promotes blood circulation for the vaginal area.

Abstract: Compositions and methods for the treatment of vasospasm are provided comprising applying an amount of a semi-solid vasoactive prostaglandin composition to the affected tissue. Also provided are methods of improving microcirculation in a replanted body part.

Abstract: A method of reducing mortality in a human patient with pulmonary inflammation due to coronavirus or other pathogen, the method including administering an oral dose of a prostacyclin analog drug to the patient within a therapeutic window. The prostacyclin analog drug includes oral iloprost or iloprost betadex clathrate.

Abstract: The invention is a pharmaceutical composition of human insulin or insulin analog that includes citrate, treprostinil and stabilizing agents, that has faster pharmacokinetic and/or pharmacodynamic action than commercial formulations of existing insulin analog products and that is stable for commercial use.

Abstract: Described herein are compositions comprising a prostaglandin FP receptor agonist (PFPRA) compound and a fatty acid ester (e.g., isopropyl myristate), optionally comprising an ointment base such as a hydrocarbon base (e.g., petroleum jelly) and/or an organic alcohol (e.g., propylene glycol), that, when topically applied to the skin, locally delivers a therapeutically effective amount of the PFPRA compound to subcutaneous fat under the skin, and methods of preparation. The therapeutic effect is, for example, reduction of the subcutaneous fat under the skin. Further provided are methods of reducing body fat in a subject comprising topically administering the composition to the subject.

Abstract: The present disclosure provides treprostinil derivatives that can act as prodrugs of treprostinil. The treprostinil derivatives can be used to treat any conditions responsive to treatment with treprostinil, including pulmonary hypertension, such as pulmonary arterial hypertension.

Abstract: The present invention relates to a novel process for preparing Lubiprostone and novel intermediates prepared from the process. The process of the present invention does not generate hydrogenated by-products that are difficult to be removed, and thus enables the production of Lubiprostone in an efficient and economical way.

Abstract: This disclosure relates to a method of treating Prader-Willi Syndrome. The method includes administering to a patient in need thereof an effective amount of a composition containing a selective oxytocin receptor agonist or a pharmaceutically acceptable salt thereof.

Abstract: Disclosed are methods and devices for obtaining patent hemostasis of the radial artery by compressing the uninstrumented ulnar artery to increase radial artery flow. The device comprises a band having an inflatable bladder for applying blunt pressure to the ulnar artery. The method comprises applying a pressure to the homolateral ulnar artery and applying a pressure to the radial artery at the access site to obtain hemostasis at the access site. The method further comprises administering an anticoagulant to a patient at a dose ranging from about 20 units per kg of body weight to about 30 units per kg of body weight.

Abstract: Provided are methods, compositions, systems, and kits for treating metabolic syndrome or a disorder associated with metabolic syndrome, e.g., obesity, dyslipidemia, and/or a diabetic condition, comprising administering systemically to a subject one or more compounds of the Formula (I) and/or (II): or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, polymorph, tautomer, isotopically enriched derivative, or prodrug thereof, wherein , L, R1, R2, Z, X, A and B are defined herein.

Abstract: Methods, pharmaceutical compositions, and kits are provided for treating a subject with an effective amount of an oxytocin receptor (OXTR) agonist and an effective amount of an ALK5 antagonist. In certain aspects, the OXTR agonist may be oxytocin or an oxytocin analog (e.g., a small molecule). The ALK 5 antagonist may be a small molecule, such as 2-(3-(6-Methyl-pyridin-2-yl)-1H-pyrazol-4-yl)-1,5-naphthyridine, LY2157299, A 83-01, D 4476, GW 788388, LY 364947, Rep Sox, SB 431542, SB 505124, SB 525334, or SD 208. In certain aspects, the amounts of the OXTR agonist and ALK5 antagonist may be sufficient to induce muscle regeneration and/or neural cell regeneration in the subject.

Abstract: A composition for topical application to a mucosal body site contains a combination of L-arginine, niacin, and a cooling compound. In one embodiment the composition contains from about 2% to about 7% by weight of a nitric oxide releasing substance selected from the group consisting of L-arginine, L-arginine salts and L-arginine derivatives. The composition also contains from about 0.05% to about 0.5% by weight niacin, and from about 0.1% to about 1% by weight of at least one compound capable of providing a sensation of cooling to the body site of application.

Abstract: The invention is a composition of human insulin or insulin analog that includes treprostinil and that has faster pharmacokinetic action than commercial formulations of existing insulin analog products.

Abstract: Methods and apparatus for diagnosing cardiovascular health in a patient by monitoring changes in skin redness levels, which is associated with perfusion and ability of circulatory system to adapt to physical exertion. Color detectors including colorimeters and spectrophotometers may be used to monitor and quantify skin color. Wet run solutions such as acetylcholine solutions may be applied to the skin area being monitored. Skin redness can be monitored during the course of exercise or a stress test, as well as during recovery. Wearable color detector devices can be worn by patients during exercise.

Abstract: The present invention provides compositions comprising a prostacyclin or prostacyclin analog, or a pharmaceutically acceptable salt thereof for use in preventing or treating cystic fibrosis. The invention also provides the use of a kit comprising a prostacyclin or prostacyclin analog for treating or preventing a condition associated with cystic fibrosis in a subject.

Abstract: The invention provides novel pharmaceutical compositions for the treatment of increased intraocular pressure based on semifluorinated alkanes which are useful as carriers for a broad range of active ingredients. Preferred active ingredients include poorly water-soluble prostaglandin analogues. The compositions can be administered topically into the eye. The invention further provides kits comprising such compositions.

Abstract: Disclosed are methods and devices for obtaining patent hemostasis of the radial artery by compressing the uninstrumented ulnar artery to increase radial artery flow. The device comprises a band having an inflatable bladder for applying blunt pressure to the ulnar artery. The method comprises applying a pressure to the homolateral ulnar artery and applying a pressure to the radial artery at the access site to obtain hemostasis at the access site. The method further comprises administering an anticoagulant to a patient at a dose ranging from about 20 units per kg of body weight to about 30 units per kg of body weight.

Abstract: Dry powder formulations for inhalation and their use in the treatment diseases and conditions. The formulation contains a uniform blend of a first spray-dried powder and a second spray-dried powder. The first spray-dried powder contains spray-dried particles of a therapeutically active ingredient dispersed in a pharmaceutically acceptable hydrophobic excipient. The second spray-dried powder contains spray-dried particles formed from a pharmaceutically acceptable hydrophobic excipient but are substantially free of any therapeutically active ingredient. The active ingredient in the first spray-dried powder is loaded sufficiently high to compensate for the second spray-dried powder being substantially free of any active ingredient. A process for preparing such formulations is also described.

Abstract: Tetrahydrothiophene and related heterocyclic analogs and related methods for GABA aminotransferase inactivation.

Abstract: Described herein are compositions comprising a prostaglandin FP receptor agonist (PFPRA) compound and a fatty acid ester (e.g., isopropyl myristate), optionally comprising an ointment base such as a hydrocarbon base (e.g., petroleum jelly) and/or an organic alcohol (e.g., propylene glycol), that, when topically applied to the skin, locally delivers a therapeutically effective amount of the PFPRA compound to subcutaneous fat under the skin, and methods of preparation. The therapeutic effect is, for example, reduction of the subcutaneous fat under the skin. Further provided are methods of reducing body fat in a subject comprising topically administering the composition to the subject.

Abstract: Cyclopentene carboxylic acid-related compounds as GABA-AT inhibitors for treatment of various addictions, disorders and disease states.

Abstract: The present invention relates to a pharmaceutical composition suitable for ophthalmic use comprising one or more prostaglandin derivatives or salts, a stabilizing amount of polyethylene glycol hydroxystearate and pharmaceutically acceptable vehicle.

Abstract: A therapeutic or prophylactic agent for diabetes includes a thiazolidine derivative as a PPAR-? agonist as an effective component which exhibits a reduced side effect of the PPAR-? agonist. The therapeutic or prophylactic agent for diabetes includes a particular IP agonist such as beraprost sodium (BPS), and a thiazolidine derivative such as pioglitazone or a pharmaceutically acceptable salt thereof. Since the therapeutic or prophylactic agent exhibits a sufficiently effective hypoglycemic action without being accompanied by side effects characteristic to PPAR-? agonists, the agent is useful as a highly safe and effective therapeutic or prophylactic agent for diabetes.

Abstract: The present invention relates to novel methods, compositions and kits useful for the treatment of pulmonary diseases such as pulmonary arterial hypertension. In particular, aerosolisable compositions of iloprost are provided which are for use in inhalation therapy. The administration is by inhalation over a short period of time, which is patient-friendly, effective, and well tolerated. Inhalation may, for example, be achieved using an efficient nebulizer based on the vibrating mesh technology.

Abstract: The invention provides a latanoprost-containing aqueous pharmaceutical composition filled in a filter-equipped container, with the adsorption of latanoprost by the filter being prevented. In the latanoprost-containing aqueous pharmaceutical composition filled in the filter-equipped container, a nonionic surfactant is contained in the composition and the filter is made from at least one material selected from the group consisting of polyether sulfone, polyvinylidene fluoride, polycarbonate, and polytetrafluoroethylene.

Abstract: The present invention is directed to a method of screening for a therapeutic agent useful for treating pulmonary hypertension comprising: contacting an erythrocyte with a candidate therapeutic agent; and detecting a presence or absence of erythrocyte-derived adenosine triphosphate, wherein a greater erythrocyte-derived adenosine triphosphate level indicates the candidate therapeutic agent has greater activity in treating pulmonary hypertension. Additionally, the present invention is directed to methods of treating pulmonary arterial hypertension by stimulating ATP release from erythrocytes through co-administration to a subject in need thereof an amount of a PDE5 inhibitor compound, and an amount of a prostacyclin compound.

Abstract: The subject of the invention is process the preparation of travoprost of formula (I) characterized by that the free acid of formula (II) is a.) activated with 2-chloro-1,3-dimethyl-imidazolinium chloride (DMC) and the resulting activated carboxylic acid intermediate is reacted with isopropyl alcohol, or b.) reacted with alkyl haloformate and the resulting mixed anhydride is reacted with isopropyl alcohol, or c.) activated with a straight or branched C1-8 dialkyl dicarbonate and reacted with isopropanol in the presence of water-free magnesium salt.

Abstract: The present embodiments provide for methods of treating elevated intraocular pressure or glaucoma using a sustained release medicament consisting of prostaglandin in benzyl benzoate that is injected intraocularly no more frequently than once every two months.

Abstract: The present invention relates to a process for preparing a prostaglandin derivative and an intermediate therefor. In accordance with the present invention, the prostaglandin F (PGF) derivative can be efficiently prepared with high purity by removing the protecting group of a protected prostaglandin E (PGE) derivative obtained from conjugate addition and then stereoselectively reducing the ketone group on the cyclopentanone ring of the PGE derivative.

Abstract: Provided are methods, compositions, systems, and kits for treating metabolic syndrome or a disorder associated with metabolic syndrome, e.g., obesity, dyslipidemia, and/or a diabetic condition, comprising administering systemically to a subject one or more compounds of the Formula (I) and/or (II): or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, polymorph, tautomer, isotopically enriched derivative, or prodrug thereof, wherein, L, R1; R2, Z, X, A and B are defined herein.

Abstract: Compositions and methods for the treatment of premature ejaculation are provided wherein a composition comprising a topical anesthetic, a shear-thinning polymeric thickener, a lipophilic component that is selected from the group consisting of an aliphatic C1 to C8 alcohol, an aliphatic C8 to C30 ester, a liquid polyol and a mixture thereof, water and a buffer system that provides a buffered pH value for the composition in the range of about 3 to about 7.4 is administered to the penile meatus.

Abstract: Compositions and methods for the treatment of premature ejaculation are provided wherein a composition comprising a vasoactive prostaglandin, a topical anesthetic, a shear-thinning polymeric thickener, a lipophilic component that is selected from the group consisting of an aliphatic C1 to C8 alcohol, an aliphatic C8 to C30 ester, a liquid polyol and a mixture thereof, water and a buffer system that provides a buffered pH value for the composition in the range of about 3 to about 7.4 is administered to the penile meatus.

Abstract: Compositions and methods for the treatment of premature ejaculation are provided wherein a composition comprising a vasoactive prostaglandin, a topical anesthetic, a shear-thinning polymeric thickener, a lipophilic component that is selected from the group consisting of an aliphatic C1 to C8 alcohol, an aliphatic C8 to C30 ester, a liquid polyol and a mixture thereof, water and a buffer system that provides a buffered pH value for the composition in the range of about 3 to about 7.4 is administered to the penile meatus.

Abstract: Described herein are compositions comprising a prostaglandin FP receptor agonist (PFPRA) compound and a fatty acid ester (e.g., isopropyl myristate), optionally comprising an ointment base such as a hydrocarbon base (e.g., petroleum jelly) and/or an organic alcohol (e.g., propylene glycol), that, when topically applied to the skin, locally delivers a therapeutically effective amount of the PFPRA compound to subcutaneous fat under the skin, and methods of preparation. The therapeutic effect is, for example, reduction of the subcutaneous fat under the skin. Further provided are methods of reducing body fat in a subject comprising topically administering the composition to the subject.

Abstract: Provided is a pharmaceutical composition including an 11-deoxy-prostaglandin compound represented by formula (I): and a fatty acid ester. By mixing the compound of formula (I) and a fatty acid ester, the compound of formula (I) will be stabilized.

Abstract: The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient.

Abstract: The specification discloses compositions and methods for treating a soft tissue defect of an individual.

Abstract: The present invention relates to novel uses of compounds that protect the endothelium, particularly prostacyclin and variants and derivatives thereof in the treatment or prevention of acute traumatic coagulopathy (ATC) and of patients resuscitating from cardiac arrest. The invention also relates to a method of identifying individuals at risk of developing ATC.

Abstract: The present invention relates to combined use of (a) a specific prostaglandin (PG) compound and (b) a H+,K+-ATPase inhibitor for the treatment of gastrointestinal disorders.

Abstract: A method of treating melanoma in a subject comprising administering an amount of SOX9 sufficient to treat melanoma is disclosed. A method of treating a hyperpigmentary condition in a subject comprising administering an amount of inhibitor of SOX9 activity sufficient to treat the condition is disclosed. A method of treating melanoma in a subject comprising administering an amount of SOX9 sufficient to treat melanoma is disclosed. A method of treating melanoma in a subject comprising increasing the amounts of retinoic acid and SOX9 in the subject by amounts sufficient to treat melanoma. A method of treating melanoma in a subject comprising administering an amount of prostaglandin D2 and retinoic acid sufficient to treat cancer is disclosed. A method of sensitizing a melanoma cell to RA comprising administering an amount of SOX9 sufficient to decrease PRAME expression is disclosed.

Abstract: The present invention is directed to HIF inhibitors and methods of preventing cell proliferation, reducing inflammation, and treating an angiogenic disease or disorders.

Abstract: Formulations and methods for growing hone in a site specific location using an osteogenic molecule such as a prostaglandin, and a delivery vehicle which is preferably a polymer matrix.

Abstract: Disclosed herein is a method comprising administering a compound to a mammal suffering from an inflammatory bowel disease for the treatment of said disease, said compound having a structure according to Formula I wherein X, Y, B, R2, R3, R4, R5, R6 and n have the meanings found herein.

Abstract: A composition comprising from 0.005% to 0.02% bimatoprost by weight and from 100 ppm to 250 ppm benzalkonium chloride, wherein said composition is an aqueous liquid which is formulated for ophthalmic administration is disclosed herein. A method which is useful in treating glaucoma or ocular hypertension related thereto is also disclosed herein.

Abstract: Compositions and methods for the treatment of premature ejaculation are provided wherein a composition comprising a topical anesthetic, a shear-thinning polymeric thickener, a lipophilic component that is selected from the group consisting of an aliphatic C1 to C8 alcohol, an aliphatic C8 to C30 ester, a liquid polyol and a mixture thereof, water and a buffer system that provides a buffered pH value for the composition in the range of about 3 to about 7.4 is administered to the penile meatus.

Abstract: Compositions and methods for the treatment of premature ejaculation are provided wherein a composition comprising a topical anesthetic, a shear-thinning polymeric thickener, a lipophilic component that is selected from the group consisting of an aliphatic C1 to C8 alcohol, an aliphatic C8 to C30 ester, a liquid polyol and a mixture thereof, water and a buffer system that provides a buffered pH value for the composition in the range of about 3 to about 7.4 is administered to the penile meatus.

Abstract: The specification discloses compositions and methods for treating a soft tissue defect of an individual.

Abstract: The invention concerns the use of a preparation based on prostaglandin E1 (PGE1) as active ingredient in a carrier suitable for administration on the skin or on the mucous membranes, for the treatment by the transdermal or transmucosal route of acute or chronic ophthalmic pathologies of an ischemic nature, and in general for the treatment of ophthalmic pathologies involving at least in part an ischemic mechanism of the ocular district. By applying PGE1 on the skin, particularly in the form of a cream, it is possible to avoid the drawbacks of the intravenous administration of the drug, while still maintaining a comparable level of absorption of the drug in the ocular district. By suitably modulating the dosage, it is possible to obtain in the eye, by the cutaneous administration of PGE1, the same clinical results that can be obtained by intravenous administration.

Abstract: Drug-containing nanoparticles are provided that enable effective targeting and sustained-release of a water-soluble, non-peptide, low-molecular weight drug and cause reduced accumulation of the drug in the liver. The nanoparticles containing a water-soluble, non-peptide, low-molecular weight drug are obtained by hydrophobicizing the water-soluble, non-peptide, low-molecular weight drug by a metal ion, and reacting the hydrophobicized drug with a poly(lactic acid)-polyethylene glycol block copolymer or a poly(lactic-co-glycolic acid)-polyethylene glycol block copolymer. The nanoparticles have favorable targeting and sustained-release properties and cause reduced accumulation of the drug in the liver.