43 results about "Prostaglandin analogue" patented technology

A dosage unit for treating constipation in a human patient is described. The dosage unit of the invention comprises a halogenated prostaglandin analog and a pharmaceutically suitable excipient. The dosage unit relieves constipation without substantial side effects.

A method of stimulating melanogenesis in a skin surface of a patient, by treating the skin surface with a topical formulation comprising an effective amount of 17-phenyl-18,19,20-trinor-PGF2α ethyl amide in a dermatologically acceptable carrier. The topical formulation may be a cream, a gel, a lotion, a spray, an ointment, an aqueous solution, a nonaqueous solution, or a transdermal patch. The dermatologically acceptable carrier may contain an oily carrier or an aqueous carrier.

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.

Provided are a crystal form A of a compound having the structure as represented by formula I, and preparation method and use thereof. The X-ray powder diffraction (XRPD) chart of the crystal form A has characteristic peaks at the following diffraction angles: 2.9±0.2°, 13.6±0.2°, 17.3±0.2° and 18.6±0.2°.

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.

Provided are a crystal form B of a compound having the structure as represented by formula I, and preparation method and use thereof. The X-ray powder diffraction (XRPD) chart of the crystal form B has characteristic peaks at the following diffraction angles: 2.9±0.2°, 6.5±0.2°, 12.6±0.2°, 13.1±0.2° and 20.6±0.2°.

The invention is based upon the discovery that red blood cells contain phosphodiesterase 3B (PDE3B), and that inhibition of that phosphodiesterase allows for an enhanced accumulation of cAMP and subsequent release of ATP. It was further discovered that RBCs treated with insulin accumulate significantly less cAMP and release significantly less ATP than normal RBCs. Likewise, RBCs of patients suffering from type 2 diabetes (hyperinsulinemia) accumulate significantly less cAMP and release significantly less ATP than normal RBCs. It was further discovered that prostaglandin analogues synergistically work with phosphodiesterase 3B inhibitors to improve or increase cAMP accumulation and ATP release by RBCs. Thus the invention is directed to compositions and methods for improving ATP release by RBCs, via administering PDE3B inhibitor or a combination of PDE3B inhibitor and prostaglandin analogue.

The present invention relates in general to polymer-drug conjugates. In particular, the invention relates to polymer-drug conjugates wherein the conjugated drugs are selected from prostaglandins and substituted prostaglandins, to a method of delivering such prostaglandin drugs to a subject, to a sustained drug delivery system comprising the polymer-drug conjugates, to a method of preparing the polymer-drug conjugates, and to an implant comprising the polymer-drug conjugates. The polymer-drug conjugates may be useful for delivering prostaglandins and substituted prostaglandins for the treatment of glaucoma.

The present invention relates in general to polymer-bioactive agent conjugates for delivering a bioactive agent to a subject. The polymer-bioactive agent conjugates contain triazole moieties in the polymer backbone and a bioactive moiety comprising prostaglandin analogues. The present invention also relates to methods for preparing the polymer conjugates using click chemical reactions, to monomer-bioactive agent conjugates suitable for preparing the polymer conjugates, and to pharmaceutical products comprising the polymer conjugates for the treatment of glaucoma.

A method for preparing a prostaglandin F analogue represented by the following formula (I) is disclosed,wherein R1, and are as defined in the specification.

A dosage unit for treating constipation in a human patient is described. The dosage unit of the invention comprises a halogenated prostaglandin analog and a pharmaceutically suitable excipient. The dosage unit relieves constipation without substantial side effects.

The presentinvention relates in general to polymer-bioactive agent conjugates for delivering a bioactive agent to a subject. The polymer-bioactive agent conjugates contain triazole moieties in the polymer backbone and a bioactive moiety selected from prostaglandin analogues, β-blockers and mixtures thereof. The present invention also relates to methods for preparing the polymer conjugates using click chemical reactions, to monomer-bioactive agent conjugates suitable for preparing the polymer conjugates, and to pharmaceutical products comprising the polymer conjugates for the treatment of glaucoma.

The invention relates to a novel method for synthetizing prostaglandin analogues, and an important intermediate compound related to the novel method. The method comprises the steps of (a), just protecting 15-site hydroxyl of the compound of a formula 2 by utilizing a hydroxyl protection group under an alkaline condition; (b) restoring a lactone ketone group from DIBAL (diisobutylaluminium hydride) to obtain the intermediate of a formula 4; (c) carrying out Wittig reaction on the intermediate of the formula 4 by utilizing 4-carboxy butyl-triphenylphosphine bromide, carrying out esterification or amidation after connecting an alpha chain; (d) removing 15-site hydroxyl protection group to obtain the prostaglandin analogue of the formula 1. The method is less in side reaction, easy to monitor, and convenient to separate due to the fact that the difference between a crude product and the polarity of a process material is large.

The invention discloses a preparation method of a prostaglandin analogue, the prostaglandin analogue is a compound shown as a formula 9, the specific synthetic route is as follows: reagents and raw materials used in the invention are available on the market, and the preparation method has the advantages of mild reaction conditions, simple operation, low energy consumption and cost, and high yield,and is suitable for industrial production.

The invention relates to a composition comprising 2% to 5% minoxidil, 0.01% to 15% finasteride and 0.01% to 15% of a prostaglandin analogue. In one embodiment, the prostaglandin analogue is latanoprost. In a preferred embodiment, the composition comprises 5% minoxidil, 0.1% finasteride and 0.03% latanoprost. The invention also relates to the use of the said composition to reduce hair loss and / or increase regrowth of hair in a human subject.

A compound of formula (I): (I) wherein Y is, Z is OR10, NR11R11 SR11, S(0)R11 S02R11, R10 is H, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, CO—R11, or a protecting group, and R11 is optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, or alkoxyl; a process for making a compound of formula (I); and a process for making a prostaglandin or a prostaglandin analogue using a compound of formula (I).whereinY is

An eye drop composition for treating glaucoma is disclosed. The eye drop composition includes a prostaglandin analogue, a thickening agent, and a solubilizing agent, wherein the thickening agent is carboxymethylcellulose or a salt thereof, and the solubilizing agent is tyloxapol.

The invention relates to a prostacyclin analogue sustained release preparation, which belongs to a trace sustained release preparation technology. The prostacyclin analogue sustained release preparation contains a prostaglandin analogue, a sustained release material, a lubricating agent and other pharmaceutically accepted additives. A process comprises various simple and convenient granulation processes, including wet granulation, and the sustained release preparation which contains uniform content of main drugs and is released sustainably and stably in vitro is obtained by controlling critical process parameters. According to the prostacyclin analogue sustained release preparation, no organic solvent is used from the composition of the formula to the whole process preparation process; therefore, the prostacyclin analogue sustained release preparation is more environment-friendly and is suitable for wider crowds. Meanwhile, according to the prostacyclin analogue sustained release preparation, the problem that the physicochemical property of the main drugs is extremely unstable is solved, so that a patient can use the preparation more safely and more reliably.

Provided is intraocular drug delivery systems. The invention refers to biodegradable implants sized and suitable for implantation in an ocular region or site and methods for treating ocular conditions. The implants provide an extended release of an active agent at a therapeutically effective amount for a period of time between 10 days and one year or longer. The active agents are selected from estradiol such as 2-methoxyl estradiol or alpha 2-adrenergic agonist such as brimonidine or derivatives thereof or prostaglandin analogues.

The invention discloses a preparation method of prostaglandin analogue midbody Corey aldehyde for treating glaucoma. The preparation method comprises the following steps: by taking Corey lactones and 2-iodoxybenzoic acid as basic raw materials, adding the raw materials and a solvent to a reaction container in sequence, heating for a reflux reaction, and after reaction, and cooling to a room temperature for filtration; and sequentially filtering and drying obtained filtrate, after drying, filtering, and removing the solvent from the filtrate by adopting conventional reduced pressure distillation, thus obtaining the product Corey aldehyde. The preparation method is used for preparing the midbody Corey aldehyde and has the characteristics that the operation is simple, the cost is relatively low, an adopted oxidizing agent is mild in property, stable in air, easy to store and the like; the whole operation process is relatively simple and convenient, and the purity and the yield of product are high.

The present invention provides a cocrystal composite composed of resveratrol and a prostaglandin analog and a pharmaceutical composition comprising the same. The cocrystal composite and the composition are characterized in that the prostaglandin analog is one selected from the latanoprost, travoprost, bimatoprost, tafluprost and Latanoprostene Bunod. The cocrystal composite can generate synergistic inhibit effects (with CI being less than 1) on cell proliferation of various cells of cancer such as lung cancer and gastric cancer.

The present invention provides a combination therapy for use in treating hair loss comprising: (a) a topical composition comprising a prostaglandin analogue and progesterone; and (b) an enteric composition comprising a vasodilator. Cosmetic methods for treating hair loss are also provided.

The invention is based upon the discovery that red blood cells contain phosphodiesterase 3B (PDE3B), and that inhibition of that phosphodiesterase allows for an enhanced accumulation of cAMP and subsequent release of ATP. It was further discovered that RBCs treated with insulin accumulate significantly less cAMP and release significantly less ATP than normal RBCs. Likewise, RBCs of patients suffering from type 2 diabetes (hyperinsulinemia) accumulate significantly less cAMP and release significantly less ATP than normal RBCs. It was further discovered that prostaglandin analogues synergistically work with phosphodiesterase 3B inhibitors to improve or increase cAMP accumulation and ATP release by RBCs. Thus the invention is directed to compositions and methods for improving ATP release by RBCs, via administering PDE3B inhibitor or a combination of PDE3B inhibitor and prostaglandin analogue.

A convergent synthesis of the prostaglandin F2α analogues, travoprost and bimatoprost, was developed employing Julia-Lythgoe olefination of the structurally advanced phenylsulfone with an enantiomerically pure aldehyde ω-chain synthon. The novel convergent strategy allows the synthesis of a whole series of prostaglandin analogues of high purity from a common and structurally advanced prostaglandin intermediate.

The invention provides an ophthalmic bigeminy and trigeminy compound pharmaceutical composition for treating glaucoma and ocular hypertension, the stability of the pharmaceutical composition is obviously improved through a salt modification technology, and the bigeminy compound pharmaceutical composition is prepared from netardil free alkali or pharmaceutically acceptable salt thereof and an epinephrine beta receptor blocker; the triplet compound pharmaceutical composition is prepared from netardil free alkali or pharmaceutically acceptable salt thereof, an epinephrine beta receptor blocker and a prostaglandin analogue, and has excellent stability when the pH value is 4.5-5.4; according to the present invention, the effective dose of the pharmaceutical composition is applied to the eyes of the patient requiring the intraocular pressure at the sleeping time or at the time close to the sleeping time once a day, such that the intraocular pressure can be efficiently and rapidly reduced so as to maintain the intraocular pressure in the physiological range for a long time, the side effect is small, and the patient compliance is high.