59 results about "Prostaglandin analog" patented technology

Compounds comprisingare disclosed, wherein Y, A, X, R, D, and n are as described.A compound comprising a prostaglandin EP2 selective agonist wherein the ω-chain comprises a substituted phenyl, wherein at least one substituent consists of hydrocarbyl or non-linear hydroxyhydrocarbyl is also disclosed herein.Methods, compositions, and medicaments related thereto are also disclosed.

The present invention relates to the formulation and delivery of prostaglandin analogs to treat epithelial-related condition. In some embodiments, the compositions of the invention are used to stimulate hair growth. In some embodiments, the compositions of the invention are used to restore hair color to depigmented hair.

A method for treating hair loss in mammals uses compositions containing prostaglandin F analogs. The compositions can be applied topically to the skin. The compositions can arrest hair loss, reverse hair loss, and promote hair growth.

Fused cyclopentane—4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A:wherein R represents an aryl group such as p-methoxyphenyl.This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required a-side chain and then the required ω-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.

An ophthalmic formulation for the treatment of glaucoma and intraocular pressure with a prostaglandin compound of the F-series (PGF), and particularly a prodrug form of a PGF2α analog, such as an ester, amide, or internal lactone, wherein preservative is an antimicrobial peptide, such as lactoferrin. In particularly preferred embodiments, the prostaglandin compound is a macrocyclic internal 1,15-lactone, such as the 16-aryloxy prostaglandin analogs, illustratively fluprostenol or cloprstenol.

A method for treating hair loss in mammals uses compositions containing prostaglandins analogs. The compositions can be applied topically to the skin. The compositions can arrest hair loss, reverse hair loss, and promote hair growth.

A safe and effective treatment for glaucoma for mammalian species comprises the steps of applying insulin and / or insulin like growth factors (IGF-1) to an eye. In addition to the insulin, another therapeutic agent may be applied to enhance the activity of the insulin. The therapeutic agent may be a pharmaceutical agent or a biochemical pharmaceutical agent. The therapeutic agents include prostaglandin analogs, topical beta-adrenergic receptor antagonists-β blockers, Alpha2-adrenergic agonists hair growth therapeutic agents, beta2-agonist action agents, parasympathomimetic miotic agents, carbonic anhydrase inhibitors, and Physostigmine. In another embodiment, a combination of at least two agents are applied to the eye. To enhance the effect of the insulin, uptake facilitators may be used. Additionally, an antibacterial agent may be applied to control bacterial infection.

Bimatoprost, a prostamide F2 alpha analog, used alone or in combination with other prostamides, or prostaglandin analogs, in a topical manner for the promotion of hair growth in mustache, beard, chest and other androgen dependent hair growth areas in humans and animals.

The described invention relates to the formulation and delivery of compositions to treat an epithelial-related condition selected from the group consisting of sparse hair growth, short hair growth, thin hair growth, alopecia and hair depigmentation and methods for their use. In some embodiments, the composition contains a first component and a second component wherein the first component is at least one prostaglandin analog and the second component is at least one imidazole analog, such that the at least one imidazole analog improves the efficacy of the at least one prostaglandin analog when delivered to a subject refractory to the effect of the prostaglandin analog alone.

Fused cyclopentane—4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A:wherein R represents an aryl group such as p-methoxyphenyl.This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required α-side chain and then the required ω-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.

Compounds comprising are disclosed, wherein Y, A, X, R, D, and n are as described. A compound comprising a prostaglandin EP2 selective agonist wherein the ω-chain comprises a substituted phenyl, wherein at least one substituent consists of hydrocarbyl or non-linear hydroxyhydrocarbyl is also disclosed herein. Methods, compositions, and medicaments related thereto are also disclosed.

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.

Fused cyclopentane—4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A:wherein R represents an aryl group such as p-methoxyphenyl.This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required α-side chain and then the required ω-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.

The present invention provides efficient, economical and environmental friendly methods for synthesis of prostaglandin analogs including tafluprost and intermediates thereof. The invention involves a selective oxidation using in situ boronate ester protection and a unique crystallization method to remove the undesired isomers of fluorinated intermediates.

The present invention relates to an improved process for the production of prostaglandins and prostaglandin analogs. In particular, this invention relates to the production of prostaglandins of the PGF2α-series, including latanoprost, travoprost, and bimatoprost, which are active pharmaceutical ingredients used for the reduction of elevated intra-ocular pressure in patients with glaucoma and ocular hypertension.

This invention provides a novel method for the preparation of 2,3-disubstituted-4-oxy-cyclopentan-1-one compounds that are useful for the synthesis of prostaglandins and prostaglandin analogs of industrial relevance. The method comprises the metal-catalyzed asymmetric 1,4-conjugate addition of vinylboron compounds to 2-substituted-4-oxy-cyclopent-2-en-1-ones. This method relies on the use of less toxic, easily-handled reagents, and can be performed under milder conditions than offered by some conventional methods, affording 2,3-disubstituted-4-oxy-cyclopentan-1-one compounds enantio- and diastereoselectively, which are precursors to the said prostaglandin and prostaglandin analogs, in high yield.

This invention provides a novel method for the preparation of 2,3-disubstituted -4-oxy-cyclopentan1-one compounds that are useful for the synthesis of prostaglandins and prostaglandin analogs of industrial relevance. The method comprises the metal-catalyzed asymmetric 1,4-conjugate addition of vinylboron compounds to 2-substituted -4-oxy-cyclopent-2-en-1-ones. This method relies on the use of less toxic, easily-handled reagents, and can be performed under milder conditions than offered by some conventional methods, affording 2,3-disubstituted-4-oxy-cyclopentan-1-one compounds enantio- and diastereoselectively, which are precursors to the said prostaglandin and prostaglandin analogs, in high yield.

The present invention relates to the formulation and delivery of prostaglandin analogs to treat epithelial-related condition. In some embodiments, the compositions of the invention are used to stimulate hair growth. In some embodiments, the compositions of the invention are used to restore hair color to depigmented hair.

The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of prostaglandins or prostaglandin analogs which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent prostaglandins or prostaglandin analogs after crossing the biological barrier and thus can render treatments for the conditions that the parent prostaglandins or prostaglandin analogs can. Additionally, the HPPs are capable of reaching areas that parent prostaglandins or prostaglandin analogs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof is disclosed herein. A, X, J, E, and Z are as described herein. These compounds are useful for treating diseases.

The invention provides a pharmaceutical composition, in particular relating to a pharmaceutical composition for the treatment of eye diseases, especially eye inflammation. The pharmaceutical composition for the treatment of eye diseases consists of active ingredients and one or a plurality of accessories that are pharmaceutically acceptable, and is characterized in that the active ingredients of the pharmaceutical composition are one or a plurality of prostaglandin analogs and one or a plurality of glucocorticoids.

A method of enhancing in vitro development of a mammalian embryo is disclosed which comprises supplementing the culture medium with a prostaglandin, or a prostaglandin analog, in an amount effective to promote complete hatching of the embryo (i.e., freeing of the embryo from the zona pellucida). The quality of human blastocysts is enhanced in vitro by culturing with a prostacyclin agonist, Iloprost. The in vivo implantation potential and live birth potential of an in vitro fertilization embryo is thereby enhanced and establishment of a viable pregnancy is facilitated.

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 selected from prostaglandin analogs, 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 present invention provides an enteric coated composition for oral administration of a chloride channel opener which can provide improved pharmaceutical activity with reduced adverse side effect such as nausea.

The present invention relates to an ophthalmic composition comprising at least two active pharmaceutical ingredients. In particular, the active pharmaceutical ingredients are selected from the group consisting of: an alpha 2 adrenergic receptor agonist; a beta-adrenergic receptor agonist; an immunosuppressant; a lymphocyte associated antigen antagonist; an anti-inflammatory; a beta-blocker; a prostaglandin analog; a histamine receptor antagonist; a carbonic anhydrase inhibitor; and an antibiotic. In some embodiments, the composition of the invention is a nanoemulsion formulation. In one particular embodiment, the first active pharmaceutical ingredient is an alpha 2 adrenergic receptor agonist. The present invention also provides a method for treating various clinical conditions associated with an eye disorder or eye disease using the composition of the invention.

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 a method for improving hair biology, e.g., hair growth. The method comprises administering to a subject a monoamine oxidase inhibitor and a vasodilator, a zinc salt of a carboxylic acid, a xanthine compound, pyrithione or a salt thereof, saponin, tritapene, crataegolic acid, celastrol, asiatic acid, an inhibitor of 5-alpha-reductase, 1,4-methyl-4-azasteroid, an androgen receptor antagonist, azelaic acid or a derivate thereof, cyclosporin, triiodothyronine, diazoxide, retinoic acid, a prostaglandin analog, aminexil, carnitine tartrate, apigenin, procapil, or adenosine, in an amount effective to achieve a desired effect. The invention further provides a method of reducing or delaying the appearance of an age-related skin imperfection. The method comprises administering to the subject a composition comprising an MAO inhibitor. A kit for improving hair growth also is provided.

The present application relates to amine salts of prostaglandin analogs and their uses for the preparation of substantially pure prostaglandin analogs. Specific embodiments relate to amine salts of tafluprost and their uses for the preparation of substantially pure tafluprost.

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.