Abstract: A compound having the structure wherein Y is selected from the group consisting of —C(O)OR2, —C(O)NHR8, —C(CH2)1-2OR3, OH, and or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.

Abstract: The present invention provides cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl compounds, which may be substituted in the 1-position with amino, amido, ether or ester groups, e.g., a 1-OH cyclopentane heptanoic acid, 2-(cycloalkyl or arylalkyl) compound. The cyclopentane heptanoic acid, 2-(cycloalkyl or arylalkyl) compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma. Moreover, the cyclopentane heptanoic, 2-(cycloalkyl or arylalkyl) compounds of this invention are smooth muscle relaxants with broad application in systemic hypertensive and pulmonary diseases; smooth muscle relaxants with application in gastrointestinal disease, reproduction, fertility, incontinence, shock, etc.

Abstract: The present invention relates to methods of treating HIV-1 infection in a subject. These methods involve administering to the subject with HIV-1 infection a therapeutically effective amount of a conjugated or immunoconjugated betulinol derivative compound, or a pharmaceutically acceptable salt or derivative thereof, under conditions effective to treat the subject for HIV-1 infection. Also disclosed are methods inhibiting HIV-1 activity in a cell. These methods involve providing a cell infected with HIV-1 and contacting the cell with a conjugated or immunoconjugated betulinol derivative compound, or a pharmaceutically acceptable salt or derivative thereof, under conditions effective to inhibit HIV-1 activity in the cell.

Abstract: Biodegradable polymeric microparticle compositions containing one or more active agents, especially those useful for treating or preventing or one or more diseases or disorders of the eye, and methods of making and using thereof, are described. The microsphere compositions release an effective amount of the one or more active agents for a period greater than 14 days in vivo, preferably greater than 60 days in vivo, more preferably up to 73 days in vivo, more preferably greater than 90 days in vivo, even more preferably over 100 days in vivo, and most preferably greater than 107 days in vivo. In a preferred embodiment, the microparticle compositions contain one or more active agents such as AG1478 to induce nerve regeneration, specifically regeneration of the optic nerve useful for managing elevated intraocular pressure (TOP) in the eye.

Abstract: Described herein are intracameral implants including at least one therapeutic agent for treatment of at least one ocular condition. The implants described herein are not anchored to the ocular tissue, but rather are held in place by currents and gravity present in the anterior chamber of an eye. The implants are preferably polymeric, biodegradable and provide sustained release of at least one therapeutic agent to both the trabecular meshwork and associated ocular tissue and the fluids within the anterior chamber of an eye.

Abstract: The present invention is directed to a pulsatile ophthalmic peri-corneal drug delivery device. The device includes an annular body and a mechanism for releasing multiple separate and distinct doses of a therapeutic composition over an extended period of time.

Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-phenyl-sulfonamido-cycloalkyl compounds of the following formula (collectively referred to herein as “APSAC compounds”).

Abstract: The present invention is directed to a combination or a kit comprising a prostaglandin analog and an adenosine receptor A1 agonist and to a method of reducing intraocular pressure (IOP) in a subject using such combination or kit. The invention is particularly directed to a combination of latanoprost marketed under the brand Xalatan™ and Compound A.

Abstract: A new class of neuramidase inhibitor prodrugs is provided characterized by a prodrug moiety of a carboxyl group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide or a carbonyl ethoxy tripeptide, a guanidine group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide, a carbonyl ethoxy tripeptide; a primary alcohol modified to form an esterified single amino acid, dipeptide or tripeptide of zanavimir of the unaltered therapeutic agent. Exemplary therapeutic agents so modified to form prodrugs include zanavimir, oseltamivir and peramivir. The prodrug has increased oral bioavailability relative to the unaltered neuraminidase inhibitor and is effective in the inhibition of viral infections involving neuraminidase in the viral reproductive cycle.

Abstract: A topical pharmacological preparation in the form of cream, suppositories or drops delivered topically to the vagina in order to contract the smooth muscle of the vaginal wall. The preparation contains a smooth muscle contracting agent such as oxytocin capable of constrict the vaginal tube reducing its overall diameter for a more pleasurable sexual experience for the female subject and his partner alike. The smooth muscle contracting agent can be associated with a systemic absorption retardant such as a mixture of Benzyl Alcohol, Acetone and Isopropanol. Such a formulation achieves high local tissue concentration of the smooth muscle contraction substance such as oxytocin in vicinity to the site of application, via minimization of systemic absorption of the smooth muscle contraction inducing substance and at the same time via promotion of its submucosal absorption across the mucosal barrier.

Abstract: The present invention relates to an ophthalmic aqueous composition containing PGF2? analogues for treating ocular hypertension and glaucoma, to a method for treating ocular hypertension and glaucoma by administering said composition to a subject in need of such treatment, and to a method for increasing aqueous solubility and stability of PGF2? analogues in an aqueous composition.

Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.

Abstract: Prostaglandin nitroderivatives having improved pharmacological activity and enhanced tolerability are described. They can be employed for the treatment of glaucoma and ocular hypertension.

Abstract: Agrochemical compositions comprising (a) one or more branched alkyl polyglycosides, and (b) one or more biocides are disclosed. The compositions display improved solubility in water, and reduced foam generation.

Abstract: A method of forming an ocular delivery device includes exposing a solid, shaped cellulose polymer to a solution including an active pharmaceutical ingredient (API) and a solvent capable of solubilizing the API, wherein the polymer absorbs at least a portion of the solution, including the API and solvent. The method may further include removing at least a portion of the absorbed solvent from the polymer by allowing the absorbed solvent to evaporate from the polymer or by drying the polymer. A variety of cellulose polymers may be used, including hydroxypropyl cellulose. A variety of APIs may be used, including Cyclosporine, Tobramycin and Vancomycin. Ocular delivery devices prepared by the methods may be used to treat a variety of eye disorders.

Abstract: This invention pertains generally to prostacyclin analogs and methods for their use in promoting vasodilation, inhibiting platelet aggregation and thrombus formation, stimulating thrombolysis, inhibiting cell proliferation (including vascular remodeling), providing cytoprotection, preventing atherogenesis and inducing angiogenesis. Generally, the compounds and methods of the present invention increase the oral bioavailability and circulating concentrations of treprostinil when administered orally.

Abstract: A composition for use in treating corneal and conjunctival lesions, includes a prostaglandin F2alpha or analogue, in a therapeutic amount, the composition being in a form suitable for topical application on the ocular surface and is free of deleterious preservative. A method for treating surface ocular conditions in a patient in need thereof, includes administering an effective amount of the composition.

Abstract: A method of stabilizing latanoprost in an ophthalmic solution containing 0.005% (W/V) of latanoprost to be stored to be stored at room temperature (i) by adding 0.1 to 2% (W/V) of ?-aminocaproic acid to the solution or (ii) by adding 0.1 to 2% (W/V) of ?-aminocaproic acid and adjusting the pH of the solution to 5.0 to 6.25.

Abstract: The present specification provides drug delivery platforms useful for the controlled release of a compound over time in an individual.

Abstract: The present disclosure relates to methods and compositions for the topical sustained delivery of therapeutic agents. Topical application of compositions containing a muscle fasciculating agent result in the sustained release of any therapeutic agent contained within the composition. More particularly, topical application of such compositions to the outer surface of the eyelid of a patient results in increased absorption and sustained release of the therapeutic agent into the eyes or systemically.

Abstract: A method of solubilizing an analog active agent of the prostaglandin F2?, such as latanoprost, is described and a method of preparing an ophthalmic solution of the solubilized latanoprost for the treatment of distinct ocular ailments. This invention also refers to an ophthalmic aqueous solution resulting from the aforementioned method, which is characterized by its chemical stability at room temperature, its safety, and innocuousness and efficiency in the treatment of the patient. The new ophthalmic aqueous solution is distinguished because its pharmaceutical value is found in the handling of a vehicle of easy access that not only permits the solubility of latanoprost, but also promotes its chemical stability and a greater tolerance of the patient with its ophthalmic application for the treatment of the patient's ailment.

Abstract: A method of solubilizing an analog active agent of the prostaglandin F2?, such as latanoprost, is described and a method of preparing an ophthalmic solution of the solubilized latanoprost for the treatment of distinct ocular ailments. This invention also refers to an ophthalmic aqueous solution resulting from the aforementioned method, which is characterized by its chemical stability at room temperature, its safety, and innocuousness and efficiency in the treatment of the patient. The new ophthalmic aqueous solution is distinguished because its pharmaceutical value is found in the handling of a vehicle of easy access that not only permits the solubility of latanoprost, but also promotes its chemical stability and, a greater tolerance of the patient with its ophthalmic application for the treatment of the patient's ailment.

Abstract: A method of solubilizing an analog active agent of the prostaglandin F2?, such as latanoprost, is described and a method of preparing an ophthalmic solution of the solubilized latanoprost for the treatment of distinct ocular ailments. This invention also refers to an ophthalmic aqueous solution resulting from the aforementioned method, which is characterized by its chemical stability at room temperature, its safety, and innocuousness and efficiency in the treatment of the patient. The new ophthalmic aqueous solution is distinguished because its pharmaceutical value is found in the handling of a vehicle of easy access that not only permits the solubility of latanoprost, but also promotes its chemical stability and a greater tolerance of the patient with its ophthalmic application for the treatment of the patient's ailment.

Abstract: A pharmaceutical controlled release composition in solid dosage form is provided which comprises (I) a water-swellable linear polymer obtainable by reacting together: (a) a dried polyethylene oxide; (b) a dried C5 to C20 diol; and (c) a Bifunctional diisocyanate; and (II) a releasable pharmaceutically active agent.

Abstract: A cosmetic process for treating dry skin and/or a dry scalp of non-inflammatory origin, for example, in a menopausal woman, comprising topically applying to the skin and/or the scalp a composition comprising, in a physiologically acceptable medium, at least one (dihydro)jasmonic acid derivative; novel (dihydro)jasmonic acid derivatives and to the compositions, for example, suitable for topical application to the skin, comprising them.

Abstract: The disclosure relates to novel compounds of the formula (I) R1NH—CH(R2)CH2—S—S—CH2—C(R3)(R4)—CONH—C(R5)(R6)—COOR7, in which R1 is a (acyloxy)alkyl carbamate-C(O)—O—C(R8)(R9)—OC(O)—R10 group; R2 is a hydrocarbon chain, a methylene radical substituted by a heterocycle, R4 is a hydrogen atom and R3 is a phenyl or benzyl radical, a heteroaryl, a methylene group substituted by a heterocycle or R3 and R4 form together a saturated cycle; R5 and R6 are hydrogen, a hydrocarbon chain, a phenyl or benzyl radical or R5 and R6 form together a saturated cycle; R7 is hydrogen, a phenyl or benzyl radical, a group of the formula CR12(R13)C(O)OR14 or OCR12(R13)OC(O)R14 or OCR12(R13)OC(O)OR14. The disclosure also relates to the use of these compounds as a drug, and to a pharmaceutical composition containing said compounds and a pharmaceutically acceptable carrier.

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: Compounds comprising formula (I) or a pharmaceutically acceptable salt thereof, a dashed line represent the presence or absence of a double bond, are disclosed, wherein J1, J2, U1, B, Y, and A are as described in claims 1-12. Methods, compositions, and medicaments related thereto are also disclosed, for treating glaucoma, inflammatory bowel disease and baldness.

Abstract: The present specification provides drug delivery platforms useful for the controlled release of a compound over time in an individual.

Abstract: The present patent application relates to novel surface-active cationic compounds, to their use, in particular as hair conditioning agent, to a cosmetic treatment method, in particular for the hair, employing the said compounds, and to the cosmetic or pharmaceutical compositions, in particular hair compositions, comprising the said surfactants.

Abstract: A method is disclosed herein comprising administering a compound and a second drug to an eye of a mammal for the treatment of glaucoma or the reduction of intraocular pressure, said compound represented by the general formula I; wherein A, B, D, X, Y, Z, R1, R3 and R4 are as defined in the specification.

Abstract: Novel ester derivatives of ascorbic acid and 2-keto-acid saccharides are provided wherein the ester is introduced by ester bond formation between at least one hydroxy-functionality on the ascorbic acid or 2-keto-acid saccharide and a carboxy-functional organosiloxane, or between a 2-keto-gulonic acid and a hydroxy-functional organosiloxane, as well as methods for their synthesis. Treatment, cosmetic, and personal care formulations comprising the novel esters are also provided, including controlled release forms thereof.

Abstract: A clear ophthalmic solution containing latanoprost having a concentration of 0.005% (W/V), 0.003 to 0.01% (W/V) benzalkonium chloride and at least one agent selected from the group consisting of glycerin, polyethylene glycol, propylene glycol and trehalose, wherein the agent is in a concentration to make the solution isotonic. A method of preventing white turbidity in an ophthalmic solution containing latanoprost having a concentration of 0.005% (W/V) and 0.003 to 0.01% (W/V) benzalkonium chloride, the method involving adding to the solution at least one agent selected from the group consisting of glycerin, polyethylene glycol, propylene glycol and trehalose, wherein the agent is in a concentration to make the solution isotonic.

Abstract: The present invention relates to a delivery system for ophthalmic drugs, and more particularly, to a non aqueous oil delivery system. Low concentrations of ophthalmic drugs suspended in an oil vehicle delivery system are as therapeutically effective in man and animals as the corresponding higher concentrations of ophthalmic drugs that are commercially used in aqueous solutions. Eye drops that utilize this nonaqueous oil delivery system, when used in man, are comfortable to use and produce little ocular irritation, have a longer shelf-life, low systemic toxic potential, and only short term blurring of vision. Using this nonaqueous oil delivery system, a single drop of ophthalmic drug with a concentration that is 10 times less than the same drug used in commercially available aqueous eye drops is as effective as the commercially available aqueous ophthalmic eye drops that require many applications to be effective.

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: Covalent conjugates of an ?,?-disubstituted glycine ester and a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid and the ?,?-disubstituted glycine ester is conjugated to the modulator at a position remote from the binding interface between the inhibitor and the target enzyme or receptor pass into cells and the active acid hydrolysis product accumulates within the cells.

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: A PLG copolymer material, termed a PLG(p) copolymer material, adapted for use in a controlled release formulation for a bioactive material is provided, wherein the formulation exhibits a reduced “initial burst” effect when introduced into the tissue of a patient in need thereof. A method of preparation of the PLG copolymer material is also provided, as are methods of use.

Abstract: Novel ligand compounds having the general formula (I): and pharmaceutical/cosmetic compositions comprised thereof are useful in human and veterinary medicine or, alternatively, in cosmetics.

Abstract: The present application refers to pharmaceutical preparations comprising an active ingredient and a carrier wherein the carrier comprises an aqueous electrochemically activated salt solution.

Abstract: The present invention provides compositions and methods for treating an ischemic episode using PGE2 EP2 agonists and/or PGE2 EP4 agonists alone or in combination with anti-thrombotic agents.

Abstract: It is intended to provide medicines having a higher ocular tension-lowering effect on ocular hypertension and glaucoma. Because of showing an excellent effect of lowering ocular tension, medicines comprising a combination of a prostaglandin compound with an NO-donating compound are useful in treating ocular hypertension and glaucoma.

Abstract: The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR modulators to treat or inhibit the progression of, for example, dyslipidemia.

Abstract: Novel ligand compounds having the general formula (I): and pharmaceutical/cosmetic compositions comprised thereof are useful in human and veterinary medicine or, alternatively, in cosmetics.

Abstract: A method for treating skin, reducing oxidative damage to a skin cell, reducing lipoxygenase (LO) activity in a skin cell, reducing cyclooxygenase (COX) activity in a skin cell, reducing tumor necrosis factor alpha (TNF-?) in a skin cell, or reduction matrix metalloproteinase enzyme activity in a skin cell comprising contacting skin or a skin cell with an aromatic skin-active ingredient.

Abstract: It is intended to provide a bicyclic ?-amino acid derivative having excellent activity as an ?2? ligand. The present invention provides a compound represented by the general formula (I): wherein R1, R2, R2?, R4, R5, R6, R7, R8, and R8? are a hydrogen atom or the like; and R3 is a hydrogen atom, a halogen atom, a C1-C6 alkyl group, or the like.

Abstract: Biocompatible, bioerodible sustained release implants and microspheres for intracameral or anterior vitreal placement include an anti-hypertensive agent and a biodegradable polymer effective to treat an ocular hypertensive condition (such as glaucoma) by relapsing therapeutic amount of the anti-hypertensive agent over a period of time between 10 days and 1 year.

Abstract: The present invention relates to Compounds of general formula (I), wherein R is hydrogen and R1 is hydroxy or acyloxy, or R is acyl and R1 is hydroxy or acyloxy, X is sulphur, oxygen or NR10, wherein R10 is hydrogen or (C1-4)alkyl; Y is sulphur or oxygen; R2 is hydrogen or one or more substituents, e.g. including substituents such as conventional in organic, e.g. (pleuro)mutilin, chemistry; R4 is hydrogen or (C1-4)alkyl; R5 is hydrogen or (C1-4)alkyl; R3 and R3? are hydrogen, deuterium, or halogen; R6, R7 and R8 are hydrogen, halogen or deuterium; m is a number selected from 0 to 4, n is a number selected from 0 to 10, and p is a number selected from 0 to 10; with the proviso that n plus p are at least 1. These Compounds are usefül as pharmaceuticals, particularly as antimicrobials.

Abstract: A prostaglandin composition comprising prostaglandin and a low-density polyethylene container are disclosed. The prostaglandin compositions are stable in polyethylene containers over longer period of time.

Abstract: The present invention provides an ophthalmic solution without an antimicrobial preservative. The solution includes as an active substance at least one prostaglandin and as a solubilizing agent, a surfactant, where the solubilizing agent is polyoxyl-15-hydroxystearate.