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103 results about "Nitrosylation" patented technology

Nitrosylation is the general term for covalent incorporation of a nitric oxide "nitrosyl" moiety into another (usually organic) molecule. There are multiple chemical mechanisms by which this can be achieved; including biological enzymes and industrial processes. The biological functions of nitrosylation are particularly important as S-nitrosylation, the conjugation of NO to cysteine thiols in proteins, is an important part of cell signalling. Coordination of NO to transition metals to give metal nitrosyl complexes, is also referred to as nitrosylation.

Polymers for delivering nitric oxide in vivo

InactiveUS6875840B2Reducing platelet depositionReduce restenosisOrganic active ingredientsBiocideS-NitrosylationIn vivo
Disclosed are novel polymers derivatized with at least one —NOx group per 1200 atomic mass unit of the polymer. X is one or two. In one embodiment, the polymer is an S-nitrosylated polymer and is prepared by reacting a polythiolated polymer with a nitrosylating agent under conditions suitable for nitrosylating free thiol groups. The polymers of the present invention can be used to coat medical devices to deliver nitric oxide in vivo to treatment sites.
Owner:DUKE UNIV

Nitrosated and/or nitrosylated compounds, compositions and methods of use

The invention describes novel nitrosated and / or nitrosylated compounds of the invention and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and / or nitrosylated compound of the invention, and, optionally, at least one nitric oxide donor and / or at least one therapeutic agent. The invention also provides novel compositions comprising at least one compound of the invention, and at least one nitric oxide donor and / or at least one therapeutic agent. The invention also provides novel kits comprising at least one compound of the invention, that is optionally nitrosated and / or nitrosylated, and, optionally, at least one nitric oxide donor and / or at least one therapeutic agent. The invention also provides methods for (a) treating bacterial infections; (b) treating viral infections; (c) treating fungal infections; and (d) treating lesions. The nitrosated and / or nitrosylated compounds of the invention are preferably nitrosated and / or nitrosylated antimicrobial compounds, nitrosated and / or nitrosylated adenosine antagonists, nitrosated and / or nitrosylated LTB4 antagonists, nitrosated and / or nitrosylated mucoregulators and nitrosated and / or nitrosylated purine agonists. The methods of the invention are preferably for the treatment of bacterial infections associated with pulmonary diseases such as cystic fibrosis.
Owner:NICOX SA

C-nitroso compounds and use thereof

A C-nitroso compound having a molecular weight ranging from about 225 to about 1,000 (from about 225 to about 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less than about 25, is useful as an NO donor. In another case, the C-nitroso compound contains the moiety—C—N(O)X—where X is S, O or NR. One embodiment is directed to COX-2 inhibitors where a tertiary carbon atom and / or an oxygen atom and / or a sulfur atom is nitrosylated.
Owner:DUKE UNIV

Nitrosated and nitrosylated diuretic compounds, compositions and methods of use

InactiveUS20050059655A1Improve propertiesBiocideSenses disorderRenovascular diseaseNitric oxide
The invention describes novel nitrosated and / or nitrosylated diuretic compounds or pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and / or nitrosylated diuretic compound, and, optionally, at least one nitric oxide donor and / or at least one therapeutic agent. The invention also provides novel compositions and kits comprising at least one diuretic compound of the invention, that is optionally nitrosated and / or nitrosylated, and, optionally, at least one nitric oxide donor compound and / or at least one therapeutic agent. The invention also provides methods for (a) treating conditions resulting from excessive water and / or electrolyte retention; (b) treating cardiovascular diseases; (c) treating renovascular diseases; (d) treating diabetes; (e) treating diseases resulting from oxidative stress; (f) treating endothelial dysfunctions; (g) treating diseases caused by endothelial dysfunctions; (h) treating cirrhosis; (j) treating pre-eclampsia; (k) treating osteoporosis; and (l) treating nephropathy.
Owner:NICOX SA

C-nitroso compounds and use thereof

A C-nitroso compound having a molecular weight ranging from 225 to 1,000 (from 225 to 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less than about 25, is useful as an NO donor. When the compound is obtained from a carbon acid with a pKa less than about 10, it provides vascular relaxing effect when used at micromolar concentrations and this activity is potentiated by glutathione to be obtained at nanomolar concentrations. When the compound is obtained from a carbon acid with a pKa ranging from about 15 to about 20, vascular relaxing effect is obtained at nanomolar concentrations without glutathione. In another embodiment, a biocompatible polymer incorporates a C-nitroso moiety.
Owner:DUKE UNIV

C-nitroso compounds and use thereof

A C-nitroso compound having a molecular weight ranging from 225 to 1,000 (from 225 to 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less than about 25, is useful as an NO donor. When the compound is obtained from a carbon acid with a pKa less than about 10, it provides vascular relaxing effect when used at micromolar concentrations and this activity is potentiated by glutathione to be obtained at nanomolar concentrations. When the compound is obtained from a carbon acid with a pKa ranging from about 15 to 20, vascular relaxing effect is obtained at nanomolar concentrations without glutathione. In another embodiment, a biocompatible polymer incorporates a C-nitroso moiety.
Owner:DUKE UNIV

Nitrosated and nitrosylated rapamycin compounds, compositions and methods of use

The invention describes novel nitrosated and / or nitrosylated rapamycin compounds, and novel compositions comprising at least one nitrosated and / or nitrosylated rapamycin compound, and, optionally, at least one nitric oxide donor compound. The invention also provides novel compositions comprising at least one rapamycin compound and at least one nitric oxide donor compound and / or at least one therapeutic agent. The compounds and compositions of the invention can also be bound to a matrix. The invention also provides methods for treating and / or preventing cardiovascular diseases, for the prevention of platelet aggregation and platelet adhesion caused by the exposure of blood to a medical device, for treating and / or preventing pathological conditions resulting from abnormal cell proliferation; transplantation rejections; autoimmune, inflammatory, proliferative, hyperproliferative or vascular diseases; for reducing scar tissue or for inhibiting wound contraction, particularly the prophylactic and / or therapeutic treatment of restenosis by administering nitrosated and / or nitrosylated rapamycin compounds or rapamycin compounds in combination with nitric oxide donors that are capable of releasing nitric oxide or indirectly delivering or transferring nitric oxide to targeted sites under physiological conditions.
Owner:NICOX SA

Nitrosated and nitrosylated compounds, compositions and methods use

The invention describes novel nitrosated and / or nitrosylated compounds of the invention, and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and / or nitrosylated compound of the invention, and, optionally, at least one nitric oxide donor compound and / or at least one therapeutic agent. The invention also provides novel compositions comprising at least one compound of the invention, that is optionally nitrosated and / or nitrosylated, and at least one nitric oxide donor compound and / or at least one therapeutic agent. The compounds and compositions of the invention can also be bound to a matrix. The invention also provides methods for treating cardiovascular diseases, for inhibiting platelet aggregation and platelet adhesion caused by the exposure of blood to a medical device, for treating pathological conditions resulting from abnormal cell proliferation; transplantation rejections, autoimmune, inflammatory, proliferative, hyperproliferative or vascular diseases; for reducing scar tissue or for inhibiting wound contraction, particularly the prophylactic and / or therapeutic treatment of restenosis by administering at least one compound of the invention that is optionally nitrosated and / or nitrosylated, in combination with nitric oxide donors that are capable of releasing nitric oxide or indirectly delivering or transferring nitric oxide to targeted sites under physiological conditions. The compounds of the invention are preferably estradiol compounds, troglitazone compounds, tranilast compounds, retinoic acid compounds, resveratol compounds, myophenolic acid compounds, acid compounds, anthracenone compounds and trapidil compounds.
Owner:NICOX SA

Nitrosated and nitrosylated alpha-adrenergic receptor antagonist compounds

The present invention describes novel nitrosated and / or nitrosylated α-adrenergic receptor antagonists, and novel compositions containing at least one nitrosated and / or nitrosylated α-adrenergic receptor antagonist, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or are a substrate for nitric oxide synthase, and / or one or more vasoactive agents. The present invention also provides novel compositions containing at least one α-adrenergic receptor antagonist, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and / or one or more vasoactive agents. The present invention also provides methods for treating or preventing sexual dysfunctions in males and females, for enhancing sexual responses in males and females, and for treating or preventing benign prostatic hyperplasia, hypertension, congestive heart failure, variant (Printzmetal) angina, glaucoma, neurodegenerative disorders, vasospastic diseases, cognitive disorders, urge incontinence, or overactive bladder, and for reversing the state of anesthesia.
Owner:NITROMED

Methods of chemical synthesis and purification of diaminophenothiazinium compounds including methylthioninium chloride (MTC)

This invention pertains generally to the field of chemical synthesis and purification, and more specifically to methods of synthesizing and purifying certain 3,7-diaminophenothiazin-5-ium compounds (referred to herein as “diaminophenothiazinium compounds”) including Methythioninium Chloride (MTC) (also known as Methylene Blue). In one embodiment, the method comprises the steps of, in order: nitrosylation (NOS); nitrosyl reduction (NR); thiosulfonic acid formation (TSAF); oxidative coupling (OC); Cr(VI) reduction (CR); isolation and purification of zwitterionic intermediate (IAPOZI); ring closure (RC); chloride salt formation (CSF); one of: sulphide treatment (ST); dimethyldithiocarbamate treatment (DT); carbonate treatment (CT); ethylenediaminetetraacetic acid treatment (EDTAT); organic extraction (OE); and recrystallisation (RX). The present invention also pertains to the resulting (high purity) compounds, compositions comprising them (e.g., tablets, capsules), and their use in methods of inactivating pathogens, and methods of medical treatment and diagnosis, etc., for example, for tauopathies, Alzheimer's disease (AD), skin cancer, melanoma, viral diseases, bacterial diseases, or protozoal diseases.
Owner:WISTA LAB LTD

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

Nitrosated and nitrosylated potassium channel activators, compositions and methods of use

The present invention describes novel nitrosated and / or nitrosylated potassium channel activators, and novel compositions comprising at least one nitrosated and / or nitrosylated potassium channel activator, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and / or at least one vasoactive agent. The present invention also provides novel compositions comprising at least one potassium channel activator, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and / or at least one vasoactive agent. The present invention also provides methods for treating or preventing sexual dysfunctions in males and females, for enhancing sexual responses in males and females, and for treating or preventing cardiovascular disorders, cerebrovascular disorders, hypertension, asthma, baldness, urinary incontinence, epilepsy, sleep disorders, gastrointestinal disorders, migraines, irritable bowel syndrome and sensitive skin.
Owner:GARVEY DAVID S +1

Nitrosated and nitrosylated compounds and compositions and their use for treating respiratory disorders

Disclosed are (i) compounds of a steroid, a β-agonist, an anticholinergic, a mast cell stabilizer and a phosphodiesterase (PDE) inhibitor directly or indirectly linked to a NO or NO2 group or a group which stimulates endogenous production of NO or EDRF in vivo; (ii) compositions of steroids, β-agonists, anticholinergics, mast cell stabilizers and PDE inhibitors, which can optionally be substituted with at least one NO or NO2 moiety or a group which stimulates endogenous production of NO or EDRF in vivo, and a compound that donates, transfers or releases nitric oxide as a charged species, i.e., nitrosonium (NO+) or nitroxyl (NO−), or as the neutral species, nitric oxide (NO.) or that stimulates endogenous production of NO or EDRF in vivo; and (iii) uses for them in preventing and / or treating respiratory disorders.
Owner:ARBOR PHARMA LLC

Nitrosated and nitrosylated nebivolol and its metabolites, compositions and methods of use

InactiveUS7138430B2Prevention of platelet aggregation and platelet adhesionAntibacterial agentsBiocideMetaboliteAntioxidant
The invention describes novel nitrosated and / or nitrosylated nebivolol, novel nitrosated and / or nitrosylated metabolites of nebivolol and novel compositions comprising at least one nitrosated and / or nitrosylated nebivolol and / or at least one nitrosated and / or nitrosylated metabolite of nebivolol, and, optionally, at least one nitric oxide donor and / or at least one antioxidant or a pharmaceutically acceptable salt thereof, and / or at least one compound used to treat cardiovascular diseases or a pharmaceutically acceptable salt thereof, and / or at least one nitrosated compound used to treat cardiovascular diseases. The invention also provides novel compositions comprising nebivolol and / or at least one metabolite of nebivolol and at least one nitric oxide donor, and, optionally, at least one antioxidant or a pharmaceutically acceptable salt thereof, and / or at least one compound used to treat cardiovascular diseases or a pharmaceutically acceptable salt thereof, and / or at least one nitrosated compound used to treat cardiovascular diseases. The compounds and compositions of the invention can also be bound to a matrix. The nitric oxide donor is a compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and may preferably be isosorbide dinitrate and / or isosorbide mononitrate. The antioxidant may preferably be a hydralazine compound or a pharmaceutically acceptable salt thereof. The invention also provides methods for treating and / or preventing vascular diseases characterized by nitric oxide insufficiency; and for treating and / or preventing Raynaud's syndrome; and for treating and / or preventing cardiovascular diseases or disorders.
Owner:NICOX SA

Nitrosated and nitrosylated rapamycin compounds, compositions and methods of use

InactiveUS20050209266A1Treating and preventing restenosisTreating and preventing and atherosclerosisBiocideOrganic chemistryPercent Diameter StenosisTherapeutic treatment
The invention describes novel nitrosated and / or nitrosylated rapamycin compounds, and novel compositions comprising at least one nitrosated and / or nitrosylated rapamycin compound, and, optionally, at least one nitric oxide donor compound. The invention also provides novel compositions comprising at least one rapamycin compound and at least one nitric oxide donor compound and / or at least one therapeutic agent. The compounds and compositions of the invention can also be bound to a matrix. The invention also provides methods for treating and / or preventing cardiovascular diseases, for the prevention of platelet aggregation and platelet adhesion caused by the exposure of blood to a medical device, for treating and / or preventing pathological conditions resulting from abnormal cell proliferation; transplantation rejections; autoimmune, inflammatory, proliferative, hyperproliferative or vascular diseases; for reducing scar tissue or for inhibiting wound contraction, particularly the prophylactic and / or therapeutic treatment of restenosis by administering nitrosated and / or nitrosylated rapamycin compounds or rapamycin compounds in combination with nitric oxide donors that are capable of releasing nitric oxide or indirectly delivering or transferring nitric oxide to targeted sites under physiological conditions.
Owner:NICOX SA

Methods of screening for a candidate modulator of glucokinase

The present invention relates to providing novel therapeutics for treating diabetes other glycemic disorders. Such therapeutics involve the signaling pathways that contribute to regulation of glucose-stimulated insulin secretion. Of particular interest are modulators of a key component in the glucokinase pathway. Thus, the present provides methods of screening for modulators of glucokinase activity, expression, translocation, conformation, nitrosylation and interaction with other molecules as useful target for pharmacological manipulation in the treatment of diabetes and other glycemic disorders.
Owner:VANDERBILT UNIV

Methods of chemical synthesis and purification of diaminophenothiazinium compounds including methylthioninium chloride (MTC)

This invention pertains generally to the field of chemical synthesis and purification, and more specifically to methods of synthesizing and purifying certain 3,7 diamino-phenothiazin-5-ium compounds (referred to herein as “diaminophenothiazinium compounds”) including Methylthioninium Chloride (MTC) (also known as Methylene Blue). In one embodiment, the method comprises the steps of, in order: nitrosylation (NOS); nitrosyl reduction (NR); thiosulfonic acid formation (TSAF); oxidative coupling (OC); Cr(VI) reduction (CR); isolation and purification of zwitterionic intermediate (IAPOZI); ring closure (RC); chloride salt formation (CSF); one of: sulphide treatment (ST); dimethyldithiocarbamate treatment (DT); carbonate treatment (CT); ethylenediaminetetraacetic acid treatment (EDTAT); organic extraction (OE); and recrystallisation (RX). The present invention also pertains to the resulting (high purity) compounds, compositions comprising them (e.g., tablets, capsules), and their use in methods of inactivating pathogens, and methods of medical treatment and diagnosis, etc., for example, for tauopathies, Alzheimer's disease (AD), skin cancer, melanoma, viral diseases, bacterial diseases, or protozoal diseases. Wherein: each of R1 and R9 is independently selected from: —H; C1-4 alkenyl; and halogenated C1-4alkyl; each of R3NA and R3NB is independently selected from: C1-4 alkyl; C2-4alkenyl; and halogenated C4-1 alkyl; each of R7NA and R7NB is independently selected from: C1-4 alkyl; C2-4alkenyl; and halogenated C1-4 alkyl; and X is one or more anionic counter ions to achieve electrical neutrality.
Owner:WISTA LAB LTD

Nitrosated and nitrosylated alpha-adrenergic receptor antagonist compounds, compositions and their uses

The invention is directed to nitrosated or nitrosylated alpha-adrenergic receptor antagonists, compositions comprising alpha-adrenergic receptor antagonists that are optionally substituted with at least one NO or NO2 moiety and compounds that donate, transfer or release nitric oxide or elevate levels of endogenous endothelium-derived relaxing factor, and methods for treating sexual dysfunctions in males and females. The invention also provides methods for treating female sexual dysfunctions by administering S-nitrosothiol compounds.
Owner:NITROMED

Oxime and/or hydrozone containing nitrosated and/or nitrosylated cyclooxygenase-2 selective inhibitors, compositions and methods of use

InactiveUS7211598B2Unexpected potential for facilitating wound healingImproving cardiovascular profile of COX-BiocideSenses disorderDiseaseCyclooxygenase
The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors having at least one oxime group or hydrazone group and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor having at least one oxime group or hydrazone group, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and / or at least one therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor having at least one oxime group or hydrazone group, optionally nitrosated and / or nitrosylated, and, optionally, at least one nitric oxide donor, and / or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention having at least one oxime group or hydrazone group can be optionally nitrosated and / or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and / or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and / or preventing renal and / or respiratory toxicity; for treating and / or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.
Owner:NICOX SA

Nitrosylation of protein SH groups and amino acid residues as a therapeutic modality

InactiveUS20060198831A1Inhibiting platelet functionPeptide/protein ingredientsSerum albuminVascular smooth muscle relaxationPlatelet inhibition
Nitrosylation of proteins and amino acid groups enables selective regulation of protein function, and also endows the proteins and amino acids with additional smooth muscle relaxant and platelet inhibitory capabilities. Thus, the invention relates to novel compounds achieved by nitrosylation of protein thiols. Such compounds include: S-nitroso-t-PA, S-nitroso-cathepsin; S-nitroso-lipoprotein; and S-nitroso-immunoglobulin. The invention also relates to therapeutic use of S-nitroso-protein compounds for regulating protein function, cellular metabolism and effecting vasodilation, platelet inhibition, relaxation of non-vascular smooth muscle, and increasing blood oxygen transport by hemoglobin and myoglobin. The compounds are also used to deliver nitric oxide in its most bioactive form in order to achieve the effects described above, or for in vitro nitrosylation of molecules present in the body. The invention also relates to the nitrosylation of oxygen, carbon and nitrogen moieties present on proteins and amino acids, and the use thereof to achieve the above physiological effects.
Owner:THE BRIGHAM & WOMEN S HOSPITAL INC

Albumin having enhanced antimicrobial activity

InactiveUS20050222026A1Sufficient antimicrobial propertyEfficiently nitrosylating albuminAntibacterial agentsBiocideMicroorganismAlbumin
The present invention provides a nitrosylated albumin variant wherein one or more amino acid residues of constituent amino acid sequences are substituted, or a different amino acid residue is inserted into a part of the constituent amino acid sequences. The albumin variant has sufficient antimicrobial property and permits application as various useful pharmaceutical compositions.
Owner:NIPRO CORP

Oxime and/or hydrazone containing nitrosated and/or nitrosylated cyclooxygenase-2 selective inhibitors, compositions and methods of use

InactiveUS20070155734A1Unexpected potential for facilitating wound healingImproved profileBiocideSenses disorderDiseaseCyclooxygenase
The invention provides novel cyclooxygenase 2 (COX-2) selective inhibitors having at least one oxime group or hydrazone group and novel compositions and kits comprising at least one COX-2 selective inhibitor having at least one oxime group or hydrazone group, optionally nitrosated and / or nitrosylated, and, optionally, at least one nitric oxide donor, and / or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention having at least one oxime group or hydrazone group can be optionally nitrosated and / or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and / or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and / or preventing renal and / or respiratory toxicity; for treating and / or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.
Owner:NICOX SA

Nitrosated and nitrosylated phosphodiesterase inhibitors, compositions and methods of use

The present invention describes novel nitrosated and / or nitrosylated phosphodiesterase inhibitors, and novel compositions containing at least one nitrosated and / or nitrosylated phosphodiesterase inhibitor, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and / or one or more vasoactive agents. The present invention also provides novel compositions containing at least one phosphodiesterase inhibitor, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and / or one or more vasoactive agents. The present invention also provides methods for treating or preventing sexual dysfunctions in males and females, for enhancing sexual responses in males and females, and for treating or preventing diseases induced by the increased metabolism of cyclic guanosine 3′,5′-monophosphate (cGMP), such as hypertension, pulmonary hypertension, congestive heart failure, renal failure, myocardial infraction, stable, unstable and variant (Prinzmetal) angina, atherosclerosis, cardiac edema, renal insufficiency, nephrotic edema, hepatic edema, stroke, asthma, bronchitis, chronic obstructive pulmonary disease (COPD), cystic fibrosis, dementia, immunodeficiency, premature labor, dysmenorrhoea, benign prostatic hyperplasis (BPH), bladder outlet obstruction, incontinence, conditions of reduced blood vessel patency, e.g., postpercutaneous transluminal coronary angioplasty (post-PTCA), peripheral vascular disease, allergic rhinitis, glucoma, and diseases characterized by disorders of gut motility, e.g., irritable bowel syndrome (IBS).
Owner:NITROMED

Cyclooxygenase 2 selective inhibitors, compositions and methods of use

InactiveUS7087630B2Unexpected potential for facilitating wound healingImproving cardiovascular profile of COX-BiocideSenses disorderWound healingDisease
The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and / or at least one therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, optionally nitrosated and / or nitrosylated, and, optionally, at least one nitric oxide donor, and / or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and / or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and / or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and / or preventing renal and / or respiratory toxicity; for treating and / or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.
Owner:NICOX SA

Keratin biomacromolecular nitric oxide donor and synthesis and application thereof

The invention discloses a keratin biomacromolecular nitric oxide donor. The keratin biomacromolecular nitric oxide donor contains reduced keratin obtained through reduction treatment on keratin, and SNO groups are formed on the sulfydryl groups of the reduced keratin. The keratin biomacromolecular nitric oxide donor is an S-nitrosated keratin and is synthesized and prepared through reaction between the reduced kertin and tert-butyl nitrite or sodium nitrite. The keratin biomacromolecular nitric oxide donor is high in molecular weight, stable in storage and capable of releasing nitric oxide under certain conditions. The keratin biomacromolecular nitric oxide donor can directly serve as a nitric oxide donor as well as be compounded with other polymers to prepare nitric oxide releasing materials to give play to a controllable nitric oxide releasing function, thereby being applicable to preparing materials such as artificial blood vessels, intravascular stent and wound dressings.
Owner:NANJING NORMAL UNIVERSITY

New method for treating nitrogen oxide waste gas

The invention relates to a new method for treating nitrogen oxide waste gas. The new method for treating the nitrogen oxide waste gas comprises three key links, namely efficient absorption of an organic solvent, catalytic oxidation and subsequent water extraction, wherein the organic solvent is a mixed organic solvent mainly comprising one or more esters, alcohols and ketones; nitrogen monoxide and oxygen which are absorbed by the organic solvent are oxidized into nitrogen dioxide and dinitrogen trioxide under the catalytic action of a rare earth complex, and then water extraction is carried out, so as to obtain an aqueous solution of dinitrogen trioxide, nitrous acid and nitric acid; the aqueous solution can be applied to a nitration and nitrosylation reaction or be recycled as an oxidizing agent, and the organic solvent can be recycled and applied to absorption of nitrogen monoxide; the rare earth complex has the catalytic oxidation function and is formed by rare earth and a phenolic ester compound, and complexing capacity of the rare earth complex is approximate to that of rare earth and nitrogen oxide. The new method for treating the nitrogen oxide waste gas is applicable to absorption, conversion and utilization of low-concentration nitrogen oxide, and harm to the environment owning to emission of waste gas is eliminated.
Owner:NANCHANG UNIV

Detection of nitrosylated proteins

InactiveUS20050238734A1Electrolysis componentsInorganic active ingredientsThiolS-Nitrosylation
The present invention, in some aspects, relates to systems and methods for determining oxidized proteins, including nitrosylated proteins such as S-nitrosylated proteins. The systems and methods of the invention can be used in vitro (e.g., in cell or tissue culture) or in vivo. For instance, in some cases, the invention can be used to spatially determine the location and / or concentration of oxidized proteins within cells and / or tissues (e.g., through visual detection). In one set of embodiments, a nitrosylated or otherwise oxidized moiety on a protein may be reacted with a detection entity, which may be, for example, fluorescent, radioactive, electron-dense, able to bind to a signaling entity or a binding partner in order to produce a signal, etc. As a specific example, a nitrosothiol moiety on a nitrosylated protein may be reacted with an alkylating agent to form an alkylthio moiety; the alkylthio moiety may include a detection entity or otherwise be able to interact with a signaling entity. In some embodiments, other moieties on the protein may be altered or blocked before reaction of the protein with the detection entity. Such moieties on the protein may be, for instance, non-oxidized or non-nitrosylated moieties able to react with the detection entity. As a particular example, in a protein containing nitrosothiol and (non-nitrosylated) thiol moieties, the thiol moieties may first be altered or blocked prior to reaction of the protein with the detection entity. Also provided in certain aspects of the present invention are kits for determining oxidized proteins, which may include components such as detection entities, alkylating agents, blocking agents, reducing agents, signaling entities, binding partners, antibodies, instructions, and the like.
Owner:UNIVERSITY OF VERMONT

Small peptide TAT-AVPY for treating ischemic brain damage, and application thereof

The invention discloses a small peptide TAT-AVPY for treating ischemic brain damage, and an application thereof. The complete sequence of the small peptide TAT-AVPY is H-YGRKKRRQRRR-AVPY-OH, represented by SEQ ID NO:1. With the small peptide TAT-AVPY provided by the invention, the binding of XIAP and proaspase-9 (Casp 9) can be reduced; nitrosylation of XIAP and proaspase-9 (Casp 9) can be alleviated; and proaspase-9 activation can be alleviated. Therefore, cell apoptosis induced by cerebral ischemia can be alleviated. Also, TAT can directly bring fused small peptide into cells, such that a problem of the approach for the drug to enter cells is solved, and medication is convenient. The small peptide TAT-AVPY has no immunogenicity, and does not cause an immune response of a body. Therefore, side effects are reduced, and the effectiveness of secondary medication or more is ensured.
Owner:许铁
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