66 results about "No synthase" patented technology

This invention provides a method for treating a condition of a subject, comprising identifying the subject as suffering from heart failure; treating the heart failure by applying a stimulating current to parasympathetic nervous tissue of the subject, and configuring the stimulating current to change a level of protein expression of at least one NO synthase of the subject selected from the group consisting of: NOS-1, NOS-2, and NOS-3; and thereafter, measuring the level of the protein expression of at least one NO synthase, and evaluating an effectiveness of the current application by assessing at least one change in the level of the protein expression of at least one NO synthase.

The present invention relates to trans-capsularly administering into a diseased joint a high specificity antagonist selected from the group consisting of: i) an inhibitor of a pro-inflammatory interleukin; ii) an inhibitor of TNF-α synthesis; iii) an inhibitor of membrane-bound TNF-α; iv) an inhibitor of a natural receptor of TNF-α; v) an inhibitor of NO synthase, vi) an inhibitor of PLA2 enzyme; vii) an anti-proliferative agent; viii) an anti-oxidant; ix) an apoptosis inhibitor selected from the group consisting of EPO mimetic peptides, EPO mimetibodies, IGF-I, IGF-II, and caspase inhibitors, and x) an inhibitor of MMPs; and xi) an inhibitor of p38 kinase.

A method is provided for the improvement of implantation rates and / or pregnancy rates in a female mammal, comprising administering to a female mammal in whom pregnancy is desired an effective amount of (a) a nitric oxide synthase substrate, a nitric oxide donor, or both, optionally in combination with (b) a progestin, and, (c) optionally, in further combination with an estrogen. A method is also provided for fertility control for a female mammal, comprising administering to a female mammal in whom pregnancy is not desired and at risk for becoming pregnant an effective amount of nitric oxide synthase inhibitor in combination with an antiprogestin. Pharmaceutical compositions are also provided.

A method is provided for the improvement of implantation rates and / or pregnancy rates in a female mammal, comprising administering to a female mammal in whom pregnancy is desired an effective amount of (a) a nitric oxide synthase substrate, a nitric oxide donor, or both, optionally in combination with (b) a progestin, and, (c) optionally, in further combination with an estrogen. A method is also provided for fertility control for a female mammal, comprising administering to a female mammal in whom pregnancy is not desired and at risk for becoming pregnant an effective amount of nitric oxide synthase inhibitor in combination with an antiprogestin. Pharmaceutical compositions are also provided.

A medicament based on antibodies contains an activated form of ultra-low doses of monoclonal, polyclonal, or natural antibodies to endothelial nitric oxide synthase (NO synthase), the activated form being prepared by multiple consecutive dilutions and exposure to external factors, preferably according to the homeopathic technology. A method of treating erectile dysfunctions and vegetative disturbances of male climax by regulating the level of cyclic guanosine monophosphate (cGMP) in the cavernous bodies on sexual stimulation, the method being characterized by the use of activated forms of ultra-low doses of antibodies to the entire molecule of the endothelial NO synthase or to its polypeptide fragments, activated forms being prepared by multiple consecutive dilutions and exposure to external factors.

Compositions and methods are provided for modulating the growth, development and repair of bone, cartilage or other connective tissue. Devices and stimulus waveforms are provided to differentially modulate the behavior of osteoblasts, chondrocytes and other connective tissue cells to promote proliferation, differentiation, matrix formation or mineralization for in vitro or in vivo applications. Continuous-mode and pulse-burst-mode stimulation of cells with charge-balanced signals may be used. Bone, cartilage and other connective tissue growth is stimulated in part by nitric oxide release through electrical stimulation and may be modulated through co-administration of NO donors and NO synthase inhibitors. Bone, cartilage and other connective tissue growth is stimulated in part by release of BMP-2 and BMP-7 in response to electrical stimulation to promote differentiation of cells. The methods and devices described are useful in promoting repair of bone fractures, cartilage and connective tissue repair as well as for engineering tissue for transplantation.

Compositions and methods are provided for modulating the growth, development and repair of cartilage, bone or other connective tissue. Devices and stimulus waveforms are provided to differentially modulate the behavior of chondrocytes, osteoblasts and other connective tissue cells to promote proliferation, differentiation, matrix formation or mineralization for in vitro or in vivo applications. Continuous-mode and pulse-burst-mode stimulation of cells with charge-balanced signals may be used. Cartilage, bone and other connective tissue growth is stimulated in part by nitric oxide release through electrical stimulation and may be modulated through co-administration of NO donors and NO synthase inhibitors. The methods and devices described are useful in promoting repair of bone fractures, cartilage and connective tissue repair as well as for engineering tissue for transplantation.

The present invention relates to heteroarylacrylamides of the formula I,in which Het, X, Ra, Rb, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.

The present invention relates to heteroarylacrylamides of the formula I,in which Het, X, Ra, Rb, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.

A medicament based on antibodies contains an activated form of ultra-low doses of monoclonal, polyclonal, or natural antibodies to endothelial nitric oxide synthase (NO synthase), the activated form being prepared by multiple consecutive dilutions and exposure to external factors, preferably according to the homeopathic technology. A method of treating erectile dysfunctions and vegetative disturbances of male climax by regulating the level of cyclic guanosine monophosphate (cGMP) in the cavernous bodies on sexual stimulation, the method being characterized by the use of activated forms of ultra-low doses of antibodies to the entire molecule of the endothelial NO synthase or to its polypeptide fragments, activated forms being prepared by multiple consecutive dilutions and exposure to external factors.

Compositions and methods are provided for modulating the growth, development and repair of bone, cartilage or other connective tissue. Devices and stimulus waveforms are provided to differentially modulate the behavior of osteoblasts, chondrocytes and other connective tissue cells to promote proliferation, differentiation, matrix formation or mineralization for in vitro or in vivo applications. Continuous-mode and pulse-burst-mode stimulation of cells with charge-balanced signals may be used. Bone, cartilage and other connective tissue growth is stimulated in part by nitric oxide release through electrical stimulation and may be modulated through co-administration of NO donors and NO synthase inhibitors. Bone, cartilage and other connective tissue growth is stimulated in part by release of BMP-2 and BMP-7 in response to electrical stimulation to promote differentiation of cells. The methods and devices described are useful in promoting repair of bone fractures, cartilage and connective tissue repair as well as for engineering tissue for transplantation.

Provided are 7-hydroxy-6-methoxy-1,2,3,4-tetrahydroisoquinoline derivatives and synthesis methods thereof. The compounds significantly inhibit the production of nitrogen monoxide (NO) and superoxide in an activated microglial cell and expressions of TNF-alpha, IL- 1beta inducive NO synthase and cyclooxygenase-2 genes. They also prevent NF-kB shift to a nucleus, decrease reactive oxygen species (ROS), inhibit expression of GTP cyclohydrolase I gene and over-production of tetrahydrobiopterin (BH 4 ), and protect dopaminergic neurons from injury due to activated microglial cells. Consequently, the compounds are effective in treating inflammatory and neurodegenerative diseases.

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).

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.

An expression regulatory sequence comprising a NF- kappa B recognition sequence, at least part of the 3'-untranslated region (3'-UTR) and at least part of the 3'-flanking region of human induced nitrogenmonoxide synthase (hiNOS) gene; and a method for screening a substance repressing the activation of NF- kappa B, comprising treating cells having the expression regulatory sequence and capable of detecting the activation of NF- kappa B with a subject substance, and observing a change in the expression amount of reporter genes.

The present invention relates to trans-capsularly administering into a diseased joint a high specificity antagonist selected from the group consisting of:i) an inhibitor of a pro-inflammatory interleukin;ii) an inhibitor of TNF-α synthesis;iii) an inhibitor of membrane-bound TNF-α;iv) an inhibitor of a natural receptor of TNF-α;v) an inhibitor of NO synthase,vi) an inhibitor of PLA2 enzyme;vii) an anti-proliferative agent;viii) an anti-oxidant;ix) an apoptosis inhibitor selected from the group consisting of EPO mimetic peptides, EPO mimetibodies, IGF-I, IGF-II, and caspase inhibitors, andx) an inhibitor of MMPs; andxi) an inhibitor of p38 kinase.

The present invention is directed to the use of an inhibitor of NO activity, such as a nitric oxide scavenger or an NO synthase inhibitor, as as an adjunct to treatment of inappropriate tissue vascularization disorders.

The present invention contains novel compounds useful as nitric oxide synthase inhibitors.

The present invention provides compositions and methods for modulating the growth, development, and repair of bone, cartilage, or other connective tissue. Also provided are devices and stimulation waveforms to differentially modulate the behavior of osteoblasts, chondrocytes, and other connective tissue cells to promote proliferation, differentiation, matrix formation, or mineralization for in vitro or in vivo applications. Continuous mode and pulsed segment mode of cell stimulation with charge-balanced signals can be used. Bone, cartilage, and other connective tissue growth is stimulated in part by the release of nitric oxide via electrical stimulation, and can be regulated by simultaneous supply of NO donors and NO synthase inhibitors. Bone, cartilage and other connective tissue growth is stimulated in part by the release of BMP-2 and BMP-7 in response to electrical stimulation that promotes cell differentiation. The methods and devices are useful for promoting bone fracture repair, cartilage and connective tissue repair, and for engineering tissue for transplantation.

Compositions for the treatment of uric acid deficiency are disclosed. The compositions generally comprise either a precursor or derivative of uric acid, which, when administered to a patient, will result in a raising of the uric acid levels in that patient. The compositions can optionally comprise one or more additional active ingredients such as antioxidants, glutathione precursors, or inhibitors of NO synthase or homocysteine. Methods for raising uric acid levels in a patient are also disclosed. These methods are useful for in the treatment of various illnesses, such as cancer, infectious disease, Alzheimer disease and neurodegenerative diseases. Use of improved solutions comprising the present compositions in organ preservation is also disclosed.

The invention relates to a method of determining the presence and / or amount of an asymmetric methylarginine in a sample, the method comprising:(a) contacting the sample with a nitric oxide synthase (NOS) polypeptide in the presence of a detectably labelled species under conditions which permit the asymmetric methylarginine and detectably labelled species to bind to the NOS polypeptide; and(b) determining the amount or presence of the detectably labelled species bound to the NOS polypeptide

Endothelial cells produce many factors that are involved in maintaining blood vessels. One of the best understood and most studied factor is nitric oxide (NO), which is produced by an endothelial enzyme called nitric oxide synthase (eNOS). The present invention provides a molecule designed to be delivered to the endothelium where it can reconstitute eNOS activity and restore NO production. Thus, the present invention provides methods of detecting, treating and preventing diseases or disorders associated with the vasculature and denoted by reduced levels of eNOS in the endothelium, as well as a concomitant reduction in the amount of NO that can be produced.

The invention provides nucleic acid segments, compositions and methods for the treatment of heart failure, vascular dysfunction, endothelial dysfunction, diabetes, [Ca2+]i regulation and NO synthase dysfunction. Adeno-associated and adenovirus are used as gene delivery vectors for the nucleic acid segments to product long term over-expression of S100A1, a small calcium sensing protein associated with the disclosed ailments and dysfunctions.

The present invention relates to N-alkylamides of the formula I,in which A, Het, X, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.

Methods for melanoma treatment and prevention with selective nitric oxide synthase inhibitor compounds and related pharmaceutical compositions, alone or in conjunction with one or more other melanoma therapies.

The invnetion relates to the field of a plant extract, and particularly to use of a young watermelon fruit and a young chiapao melon fruit in preparing a medical composition for gene controlling. Thecomposition which comprises a young watermelon fruit extract, a young chiapao melon fruit extract or combination thereof can promote keratinocyte metabolism and suppression interleukin-8 secretion through up-regulating expression amounts of nitricoxide synthase3 (NOS3) and von Willebrand factor (vWF) gene and down-regulating the expression amounts of interleukin-8 (IL-8), endothelin1 (EDN1), tissue-type plasminogenactivator (PALT), human coagulation factor (F3), serine protease inhibitor1 (SERPINE1) and intercellular adhesion molecule1 (ICAM1) gene, thereby finally realizing effects of anti-inflammation, anti-acne and reducing blood pressure and blood fat.

Use of the substance characterized by general structural formula (I)for the preparation of an agent inhibiting the enzymatic activity of NO-synthase, R1, R2, R3, R4 and / or R5 being hydrogen, an alkyl group, an aryl group or a heterocyclic group and n equals 2 or 3.

A novel, highly polymorphic DNA marker based on the pentanucleotide repeat (CCTTT / GGAAA)n has been identified in the human inducible nitric oxide synthase (iNOS) gene. Twelve different alleles, having between 7 and 18 repeats, have been identified. The repeat is highly polymorphic in the human population and so lends itself to use as a microsatellite marker with uses in, for example, forensic medicine, population studies, family linkage studies and disease diagnosis.

The present invention relates to a compound-laughing gas synthase inhibitor. Said invention also provides its general formula and its preparation method, and also discloses the medicine containing said compound and its application for curing the diseases of septic shock, enteritis, rheumatoid arthritis, diabetes mellitus, cerebral ischemic injury and presenile dementia, etc.

The invention relates to immunopotentiator proline-glycocoll cyclic tetrapeptide (C14H20N404). The compound is obtained by the fermentation and separation of microorganism Bacillussimplex DR-834. As shown by numerous tests, the compound can be used for preparing drugs for enhancing the immune function of animals such aquatic animal fish. A crude fermentation product of the Bacillussimplex DR-834 containing cyclic tetrapeptide can be used as feedstuff. By using the proline-glycocoll cyclic tetrapeptide, the mRNA (Messenger RNA) expression level of interleukin 1-beta gene and nitric oxide synthase in blood is obviously increased compared with contrast, and the immunity of aquatic animals can be obviously improved. The result of a virus attacking test indicates that the cyclic tetrapeptide is remarkable in immune protection. In test groups, the average death rate is 26.67%, and the rate of a contrast group is 73.33% and the relative immune protection rate of the contrast group is 63.63%.