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231 results about "Phosphodiesterase inhibitor" patented technology

A phosphodiesterase inhibitor is a drug that blocks one or more of the five subtypes of the enzyme phosphodiesterase (PDE), thereby preventing the inactivation of the intracellular second messengers cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) by the respective PDE subtype(s). The ubiquitous presence of this enzyme means that non-specific inhibitors have a wide range of actions, the actions in the heart, and lungs being some of the first to find a therapeutic use.

Methods of using and compositions comprising (+) sibutramine optionally in combination with other pharmacologically active compounds

This invention encompasses methods for the treatment and prevention of disorders that include, but are not limited to, eating disorders; weight gain; obesity; irritable bowel syndrome; obsessive-compulsive disorders; platelet adhesion; apnea; affective disorders such as attention deficit disorders, depression, and anxiety; male and female sexual function disorders; restless leg syndrome; osteoarthritis; substance abuse including nicotine and cocaine addiction; narcolepsy; pain such as neuropathic pain, diabetic neuropathy, and chronic pain; migraines; cerebral function disorders; chronic disorders such as premenstrual syndrome; and incontinence. The invention further encompasses pharmaceutical compositions and dosage forms which comprise optically pure (+) sibutramine, optionally in combination with a phosphodiesterase inhibitor or a lipase inhibitor.
Owner:SEPACOR INC

Tetracyclic cyclic GMP-specific phosphodiesterase inhibitors, process of preparation and use

A compound of formula (I) and salts and solvates thereof, in which: R0 represents hydrogen, halogen, or C1-6alkyl; R1 represents hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, haloC1-6alkyl, C3-8cycloalkyl, C3-8cycloalkylC1-3alkyl, arylC1-3alkyl, or heteroarylC1-3alkyl; R2 represents an optionally substituted monocyclic aromatic ring selected from benzene, thiophene, furan, and pyridine, or an optionally substituted bicyclic ring (a) attached to the rest of the molecule via one of the benzene ring carbon atoms, and wherein the fused ring (A) is a 5- or 6-membered ring which may be saturated or partially or fully unsaturated, and comprises carbon atoms and optionally one or two heteroatoms selected from oxygen, sulphur, and nitrogen; and R3 represents hydrogen or C1-3alkyl, or R1 and R3 together represent a 3- or 4-membered alkyl or alkenyl chain. A compound of formula (I) is a potent and selective inhibitor of cyclic guanosine 3',5'-monophosphate specific phosphodiesterase (cGMP specific PDE) having a utility in a variety of therapeutic areas where such inhibition is beneficial, including the treatment of cardiovascular disorders and erectile dysfunction.
Owner:ICOS CORP

Compositions and Methods for the Treatment of Peripheral B-Cell Neoplasms

InactiveUS20080051379A1High level of apoptosisLevel of apoptosis inducedOrganic active ingredientsBiocidePDE4 InhibitorsAdenosine
The present invention is directed to the use of a PDE4 inhibitor and a glucocorticoid to treat peripheral B-cell neoplasms. In particular, the present invention provides a method of treating individuals (e.g. patients) diagnosed with peripheral B-cell leukemias by administering pharmaceutical compositions comprising Type 4 cyclic adenosine monophosphate phosphodiesterase inhibitors and a glucocorticoid. Preferably, the combination of the PDE4 inhibitor and the glucocorticoid has a synergistic effect on apoptosis such that the level of apoptosis induced is greater than the level that would be expected by simply adding a PDE4 inhibitor to a glucocorticoid.
Owner:BOSTON MEDICAL CENTER INC

Compounds and methods for the treatment of urogenital disorders

InactiveUS6987129B2Reduce painLess discomfortBiocidePeptide/protein ingredientsDiseaseFemale Sexual Arousal Disorder
The present invention provides methods for treating a variety of urogenital disorders, such as, for example, vaginismus, dyspareunia, vulvodynia (including vulvar vestibulitis), interstitial cystitis, nonspecific urethriris (i.e., nonspecific pain and / or burning of the urinary tract) and sexual dysfunctions, such as, for example, female sexual arousal disorders and female sexual orgasmic disorders, using a variety of compounds, including, but not limited to, NO donors, calcium channel blockers, cholinergic modulators, α-adrenergic receptor antagonists, β-adrenergic receptor agonists, phosphodiesterase inhibitors, cAMP-dependent protein kinase activators (e.g., cAMP mimetics), superoxide scavengers, potassium channel activators, estrogen-like compounds, testosterone-like compounds, benzodiazepines, adrenergic nerve inhibitors, antidiarrheal agents, HMG-CoA reductase inhibitors, smooth muscle relaxants, adenosine receptor modulators, adenylyl cyclase activators, endothelin receptor antagonists, bisphosphonates and cGMP-dependent protein kinase activators (e.g., cGMP mimetics).
Owner:STREHKEHN INT LTD

Methods of inducing ovulation using a non-polypeptide camp level modulator

The present invention relates to methods of inducing ovulation in a female host comprising the administration of a non-polypeptide cyclic adenosine monophosphate (cAMP) level modulator to female host. In another aspect, the invention provides for specific administration of the phosphodiesterase inhibitor prior to the luteal phase of the host's ovulatory cycle. Preferred non-polypeptide cAMP level modulator include phosphodiesterase inhibitors, particularly inhibitors of phosphodiesterase 4 isoforms.
Owner:MERCK SERONO SA

Tablets immediately disintegrating in the oral cavity

The present invention provides an intraoral quickly disintegrating tablet containing a phosphodiesterase inhibitor having an effect of improving the erectile dysfunction and a method for manufacturing the tablet. The present invention also provides an intraoral quickly disintegrating tablet containing a slightly soluble pharmaceutical agent having an improved solubility and a method for manufacturing the tablet. That is, it is an intraoral quickly disintegrating tablet containing a cyclic GMP phosphodiesterase inhibitor and a saccharide, and a method for manufacturing the tablet. Further, it is a method for manufacturing an intraoral quickly disintegrating tablet, which comprises dissolving a slightly soluble pharmaceutical agent in an organic solvent or an aqueous organic solvent together with a surfactant and / or a water-soluble polymer, coating the solution on a filler or granulating it with a filler to obtain molded products, mixing a saccharide with them, adding an organic solvent, water or an aqueous organic solvent thereto, followed by kneading, and subjecting it to a compression-molding.
Owner:EISIA R&D MANAGEMENT CO LTD

Pharmaceutical compositions comprising a multifunctional phosphodiesterase inhibitor and an adenosine uptake inhibitor

InactiveUS20050165030A1Increase antiplatelet effectIncrease vasodilationBiocideMuscular disorderDipyridamoleAdenosine
The present invention relates to pharmaceutical compositions comprising at least one multifunctional phosphodiesterase inhibitor (MPDEI) and at least one adenosine uptake inhibitor. The present invention also relates to compositions comprising cilostazol and dipyridamole and their use.
Owner:OTSUKA PHARM CO LTD

Combination antihistamine and steroid medication

InactiveUS20060228306A1BiocideSenses disorderTopical steroidPhosphodiesterase inhibitor
The invention provides a topical pharmaceutical composition for application to the nasal or ocular mucosa which comprises (1) a pharmaceutical excipient suitable for topical administration, (2) an antihistamine drug and (3) a mast cell stabilizer, a non-steroidal anti-inflammatory drug, a phosphodiesterase inhibitor, an anti-IgE agent, heparin, a topical steroid or a leukotriene blocker.
Owner:FAIRFIELD CLINICAL TRIALS

1-cycloalkyl-1,8-naphthyridin-4-one derivative as type IV phosphodiesterase inhibitor

A 1-cycloalkyl-1,8-naphthylidin-4-one derivative having the formula (I):wherein R1 indicates a substituted or unsubstituted cycloalkyl group or a substituted or unsubstituted heterocycloalkyl group,R2, R3, and R4 independently indicate a hydrogen atom, a substituted or unsubstituted lower alkyl group, or a halogen atom,X indicates a group NR5R6 or a group OR7, wherein R5 and R6 independently indicate a hydrogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted cycloalkyl group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted heteroaryl group, and R7 indicates a hydrogen atom, a substituted or unsubstituted lower alkyl group, or a substituted or unsubstituted cycloalkyl group or a pharmaceutically acceptable salt or solvate thereof and a type IV phosphodiesterase inhibitor containing the same as an effective component.
Owner:ASUBIO PHARMA

Derivatives of 1-phenyl-2-pyridynyl alkylene alcohols as phosphodiesterase inhibitors

The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridynyl alkylene alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.
Owner:CHIESI FARM SPA

1-phenyl-2-pyridinyl alkyl alcohol compounds as phosphodiesterase inhibitors

ActiveUS20100204256A1Good effectPreventing and/or treating of atopic dermatitisRespiratorsBiocideDiseaseAlcohol
1-Phenyl-2-pyridinyl alkyl alcohol compounds are effective as inhibitors of the phosphodiesterase 4 (PDE4) enzyme and may be used to prevent and / or treat certain diseases or conditions.
Owner:CHIESI FARM SPA

Nitrosated and nitrosylated phosphodiestrase inhibitor compounds, compositions and their uses

Disclosed are nitrosated and / or nitrosylated phosphodiesterase inhibitors having the formula NOn-PDE inhibitor where n is 1 or 2. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides a composition comprising a therapeutically effective amount of an phosphodiesterase inhibitor (PDE inhibitor), which can optionally be substituted with at least one NO or NO2 moiety, and one to ten fold molar excess of a compound that donates, transfers or releases nitrogen monoxide as a charged species, i.e., nitrosonium (NO+) or nitroxyl (NO-), or as the neutral species, nitric oxide (NO.) or which stimulates endogenous EDRF production. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides methods for treating sexual dysfunctions in males and females.
Owner:NITROMED

Therapeutic antisense phosphodiesterase inhibitors

This patent describes the invention of a series of novel therapeutic oligonucleotides targeted at inhibiting expression of genes coding for Phosphodiesterase 4. They are useful as analytical tools in the study of individual PDE isoforms and in the therapeutic treatment of depression, thrombosis, cystic fibrosis, gastric lesions, pulmonary hypertension, glaucoma, multiple sclerosis, atopic dermatitis, asthma and other allergic disorders as well as other illnesses in which an increase of cyclic AMP or a decrease in phosphodiesterase levels is useful.
Owner:LAKEWOOD AMEDEX

Reducing Side Effects of Tramadol

The invention provides methods of reducing the side effects of tramadol. Accordingly, in one embodiment, the invention provides a method of reducing the incidence of newly-discovered side effects related to sexual function in human males taking a tramadol material. The method comprises administering a phosphodiesterase inhibitor to a male taking the tramadol material. The invention also provides pharmaceutical compositions. In one embodiment, the composition comprises a tramadol material and a phosphodiesterase inhibitor. The invention further provides kits. In one embodiment, the kit comprises a tramadol material and a phosphodiesterase inhibitor.
Owner:AYTU BIOSCI

Treatment or prevention of vascular disorders with Cox-2 inhibitors in combination with cyclic AMP-specific phosphodiesterase inhibitors

InactiveUS20050187278A1Efficacious and safe and easy to administerBiocideAmide active ingredientsCOX-2 inhibitorPhosphodiesterase inhibitor
A method is described for the prevention and / or treatment of vascular disorders and vascular disorder-related complications in a subject, the method comprising administering to the subject a Cox-2 inhibitor in combination with a cAMP-specific PDE inhibitor. Also described are therapeutic and pharmaceutical compositions and kits that are useful in the present invention.
Owner:PHARMACIA CORP

Method of using and compositions comprising (-) sibutramine optionally in combination with other pharmacologically active compounds

This invention encompasses methods for the treatment and prevention of disorders that include, but are not limited to, eating disorders; weight gain; obesity; irritable bowel syndrome; obsessive-compulsive disorders; platelet adhesion; apnea; affective disorders such as attention deficit disorders, depression, and anxiety; male and female sexual function disorders; restless leg syndrome; osteoarthritis; substance abuse including nicotine and cocaine addiction; narcolepsy; pain such as neuropathic pain, diabetic neuropathy, and chronic pain; migraines; cerebral function disorders; chronic disorders such as premenstrual syndrome; and incontinence. The invention further encompasses pharmaceutical compositions and dosage forms which comprise optically pure (-) sibutramine, optionally in combination with a phosphodiesterase inhibitor or a lipase inhibitor.
Owner:SEPACOR INC

Methods for the collection and maturation of oocytes

The present invention relates to a method of producing an embryo from an oocyte by an assisted reproduction technology. The method includes (a) collecting an oocyte from an ovary of a subject in a collection medium comprising a first phosphodiesterase inhibitor and an agent that increases intracellular cAMP concentration in the oocyte, (b) culturing the oocyte in a maturation medium comprising a second phosphodiesterase inhibitor, and (c) producing an embryo from the oocyte by an assisted reproduction technology. The present invention also relates to methods of inducing oocyte maturation. For example a method of in vitro maturation of an oocyte is described which comprises steps (a) and (b) above. The present invention also relates to an oocyte maturation medium comprising a phosphodiesterase inhibitor and a ligand for inducing maturation of the oocyte. A combination product comprising an oocyte collection and maturation medium referred to above is also described.
Owner:GILCHRIST ROBERT BRUCE +2

Pharmaceutical formulation comprising a phosphodiesterase inhibitor

ActiveUS20120034172A1BiocideDispersion deliveryObstructive airway diseasePhosphodiesterase inhibitor
Pharmaceutical formulations to be administered by pressurized metered dose inhalers (pMDIs), comprising a compound of general formula (I) may be used for the treatment and / or prevention of inflammatory or obstructive airway diseases.
Owner:CHIESI FARM SPA

Derivatives of 1-phenyl-2-pyridynyl alkylene alcohols as phosphodiesterase inhibitors

The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridynyl alkylene alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.
Owner:CHIESI FARM SPA

Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols as phosphodiesterase inhibitors

The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.
Owner:CHIESI FARM SPA
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