172 results about "No donors" patented technology

Compositions and methods of the topical treatment of equine laminitis are disclosed. In particular, combinations of a fast acting nitric oxide (NO) donor, a sustained acting NO donor and an NSAID mixed in a lipid-based carrier are described. The application of such combinations to the affected areas, e.g., the hoofs and surrounding tissues, of an equine afflicted with laminitis provides relief from the debilitating effects of this painful, often life-threatening condition.

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).

Patients needing NO donor therapy or inhibition of pathologically proliferating cells or increased NO bioactivity are treated with a therapeutically effective amount of an inhibitor of glutathione-dependent formaldehyde dehydrogenase.

The invention belongs to the technical field of the pharmaceutical chemistry, and concretely discloses benzimidazole derivatives, and a preparation method and a medicinal use thereof. The benzimidazole derivatives comprise ligustrazine and NO donor derivatives, and the benzimidazole derivatives can rapidly release ligustrazine or NO in vivo, so there is an effective synergistic effect between the benzimidazole derivatives and azilsartan, thereby the benzimidazole derivatives enhances the antihypertension effect, reduces untoward effects, has an ideal protection effect on the liver and kidney of a patient, and fills a gap in the prior art.

The present invention relates to nanofibers that produce therapeutic amounts of nitric oxide after a delay period, which allows time to install or implant the device into a patient. The nitric oxide release is thus localized to the area of the organism where NO dosing is indicated. The delay time is achieved by cospinning the NO-producing fiber with a fiber that tends to sequester the former's NO-producing functional groups. Fibers of the present invention may be incorporated into medical devices such as stents or other implantable medical devices to prevent the formation of adhesions or scarring in the area of the implant.

The present invention relates to multifunctional steroid compounds combining a steroid component with SOD mimic component and optionally also with NO donor component, and to their use in treating and preventing disorders associated with oxidative stress and free radical injury, or disorders in which treatment with steroids is indicated, whereas such combination increases the efficacy of treatment and reduces side effects associated with steroid treatment. The invention further relates to methods and devices for administering the compounds.

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.

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.

The invention discloses a preparation method of a copper ion mediated anticoagulant coating with function of in situ catalysis of NO release. The method includes steps of preparing an acidic buffer solution, and adding a compound with pyrogallol structure and certain concentration, a compound with amino or thiol, and copper ion soluble salt. The method of the invention has the advantages of simple operation, mild reaction conditions and easiness. The prepared coating has the advantages of controllable content of the units containing multiple amino or thiol compounds, and easily controlled loading amount of copper ion. The modified coating prepared by the method has excellent adhesion with a base material, and through act of the copper ions in the coating with the blood, the coating can conduct in situ catalyze the NO donor molecules in blood to continuously decompose and release NO molecules, thus realizing the inhibition of platelet activation and aggregation, inhibiting smooth muscle cell proliferation and migration, and protecting vascular endothelial layer function.

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.

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.

Compositions and methods for the treatment of anorectal disorders are provided in which certain combinations of NO donors, PDE inhibitors, superoxide (O2−) scavengers, β-adrenergic agonists, cAMP-dependent protein kinase activators, α1-adrenergic antagonists, L-type Ca2+ channel blockers, estrogens, ATP-sensitive K+ channel activators and smooth muscle relaxants are used.

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).

The invention relates to the field of natural medicines and medicinal chemistry and particularly relates to derivatives with modified 13-N of evodiamine. The invention discloses a preparation method of the 13-N furazan NO donor substituted evodiamine derivatives and evaluation of the anti-tumor activity. The structure of the compounds is shown in the specification, wherein R1 and R2 are (CH2)n or (CH2)n1O(CH2)n2, and n, n1 and n2 are integers between 1 and 8.

The invention discloses a preparation method of an anticoagulant material with function of inducing and catalyzing release of endogenous NO. The method comprises the steps of: configuring an alkaline Tris-buffer buffer solution, and adding a compound with certain concentration and pyrogallol structure and a compound with disulfide bond or diselenium bond and containing amino or thiol at two ends; and placing the substrate materials in a reaction solution, controlling the reaction temperature, reacting for 1-24 h, removing the substrate, and cleaning and drying to obtain the objective material. The invention has the advantages of simple operation, mild reaction conditions and easy operation. The component unit of the compound with disulfide bond or diselenium bond and containing amino or thiol at two ends has controllable content; the modified coating prepared by the method has excellent adhesion, and catalyzes the blood NO donors to continuously release NO molecules through in situ catalysis, inhibits activation and aggregation of platelets, inhibits proliferation of smooth muscle cells, and protects vascular endothelium.

The invention discloses a method for constructing an anti-blood coagulation blood vessel scaffold material by utilizing an endogenous NO donor. The method comprises the steps that organic selenium polycation high polymer and polyanion high polymer are alternately coated on the surface of the blood vessel scaffold material in sequence through a layer-by-layer self-assembled method to form a blood vessel scaffold material surface decorated by a multilayer bimolecular film, thus catalyzing the endogenous NO carries such as S-nitroso glutathione (GSNO) existing in the body, realizing sustained and partial release of NO, effectively regulating and controlling the release rate of NO by regulating and controlling the number of layers of the layer-by-layer self-assembled bimolecular film, and further improving blood coagulation resistance of the blood vessel scaffold material. The method of the invention can be used for metal blood vessel scaffolds or organic polymer artificial blood vessel scaffolds or cell-free artificial blood vessel scaffolds, and also can be used for other medical appliances contacting with blood.

A topical dermal delivery device, such as a patch, for topical delivery of nitric oxide (NO) to treatment sites of mammals is disclosed. In an embodiment the patch has three layers; a backing with an activation window, a absorbent core as a reservoir and an NO permeable membrane with an adhesive layer towards the skin. The NO donor is applied into the device as a solution prior to application through the activation window. The window is closed after activation and the lid and backing is non-permeable for NO in order to increase the partial pressure of NO and thus the concentration of dissolved NO. The patch is fixated on the area to be treated with an adhesive layer that also assures sufficient contact throughout the treatment. The generated NO moves within the patch and can escape through the NO permeable membrane towards the area to be treated. Depending on therapy needed, the patch release curve differs and is chosen accordingly.

Provided here are nitric oxide-releasing compounds that include at least two different NO donor functional groups of the same class. In some embodiments, such nitric oxide-releasing compounds are macromolecules such as dendrimer and co-condensed silica. Pharmaceutical compositions, wound dressings, kits and methods of treatments are also provided herein.

The invention discloses a nitric oxide (NO) donor-type farnesyl thiosalicylic acid (FTA) derivative, and pharmaceutically acceptable salt, a preparation method and medical application thereof. The FTA derivative is a compound obtained by carrying out heterozygosis on a NO donor furazan nitrogen oxide and Ras protein inhibitor FTA by an ester bond or an amido bond. Pharmacological test results show that the FTA derivative can reserve the Ras protein inhibiting activity of FTA and simultaneously releases high-concertration NO to induce cancer cell apoptosis and enhance the inhibiting action on cancer cell proliferation; compared with the FTA, the FTA derivative has more excellent anti-tumor activity, and therefore, the compound can be suitable for treating various clinical malignant tumours.

The present invention is directed to methods, pharmaceutical compositions and kits for modulating skeletal muscle precursor cell activation. Modulation is effected through the use of nitric oxide (NO), donors of NO, inhibitors of NO activity (NO inhibitor) or regulators of NO production, either locally or systemically. The invention further teaches the use of NO, an NO donor, an NO inhibitor or a regulator of NO production to modulate the effects of steroid hormone on skeletal muscle. The invention further provides a method for identifying a compound which effects a change in activation state of muscle precursor cells. A number of advantages is evident. By allowing skeletal muscle precursor cells to be manipulated directly, the invention enables specific treatments to regenerate and repair muscle.

The invention relates to the field of medical chemistry and pharmacotherapeutics, and particularly relates to an NO donor type matrine derivative and a preparation method thereof and application in pharmacy. The compounds have an anti-tumor effect and can be used for preparing anti-tumor medicines. The invention also relates to a preparation method of the compounds.

The invention provides a preparation method for a multifunctional nanometer medicine system with the functions of fluorescence tracing, targeting conveying and intracellular light-operated release of nitric oxide. The nanometer system takes titanium dioxide nanoparticle, carbon quantum dot, graphene quantum dot or the like as a carrier, takes metal ruthenium and manganese nitrosyl compounds as exogenous NO donors, and takes folic acid, galactose molecules and the like as targeting guiding groups. The nitric oxide release nanometer system has good biological compatibility and stability, has fluorescence tracing function, is capable of performing nitric oxide selective light-operated release on specific cancer cells, and has potential application prospect and commercial business in the fields of treatment, photodynamic therapy (PDT) and the like on diseases caused by lack of NO in body.

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.

Patients needing NO donor therapy or inhibition of pathologically proliferating cells or increased NO bioactivity are treated with a therapeutically effective amount of an inhibitor of glutathione-dependent formaldehyde dehydrogenase.

The invention relates to the field of medicinal chemistry, and relates to derivatives obtained by modification on 7-site of brefeldin A. Particularly, the invention relates to 7-site furazan NO donor substituted brefeldin A derivatives, and a preparation method of the derivatives and uses of the derivatives in preparing antineoplastic drugs. The brefeldin A derivatives are as shown by a general formula I or II, shown in the description, wherein m and n are respectively integers within the range of 1 to 8.

The invention belongs to the technical field of pharmaceutical chemistry and particularly discloses a benzimidazole derivative and a preparation method and medical application thereof. The benzimidazole derivative comprises a ligustrazine and an NO donor derivative and rapidly releases the ligustrazine or NO in vivo, accordingly the benzimidazole derivative and azilsartan produce effective synergistic effect, the anti-hypertensive treating effect is improved, the untoward effect is reduced, and the benzimidazole derivative has fairly ideal production effect on the liver and kidney of a patient and fills the blank in the prior art.

A nucleophilic NO donor is prepared from chitosan through modifying by amino acid to increase its nucleophilic sites (NH groups), and reacting on NO. It has different NO releasing speeds and half-life, low cytotoxicity and generation of cancergenic ammonium nitrite.

The invention discloses a rooting-promoting, disease-resistant and plant-strengthening agent for cotton and a water, fertilizer and pesticide integrated application method. The rooting-promoting, disease-resistant and plant-strengthening agent is mainly prepared from a growth regulator, a microelement, a signal molecule donor and an elicitor capable of improving the disease resistance of the cotton, wherein the growth regulator is prepared from indolebutyric acid, sodium nitrophenolate, naphthylacetic acid and diethyl aminoethyl hexanoate through compounding, the microelement is prepared from zinc sulfate, ferrous sulfate, ammonium molybdate, amino acid powder and ammonium hydrogen phosphate through compounding, the signal molecule donor is NO donor sodium nitroprusside, and the elicitor is a penicillium dry mycelium extracting solution. The problems that a drip irrigation technology does no good to root development and severe diseases are caused by successive cropping to the cotton are solved, the growth regulator accelerates growth of root systems, the physiological function time of the root systems is prolonged, the disease-resistant elicitor enhances the resistance of cotton plants, growth of lateral roots is further promoted in combination of the signal molecule donor, and the disease-resistant response of the cotton plant is promoted. The rooting-promoting, disease-resistant and plant-strengthening agent can promote growth of roots and resist diseases in multiple angles; the agent can be injected into irrigation water through a fertilizer pump, integrated application of water, fertilizer and pesticides in the drip irrigation cotton field of the northwest inland is realized, and the agent can promote growth of roots, resist diseases and strengthen seedlings and has remarkable disease resisting and yield increasing effects.

The present invention is synthesis of quaternary ammonium salt modified nucleophilic chitosan NO donor, and belongs to the field of medicine engineering technology. The synthesis includes the following steps: 1. reacting chitosan to quaternary aminate its NH2 radical and obtain ammonium salt modified chitosan molecule; and 2. reacting the ammonium salt modified chitosan molecule with NO gas molecule at high pressure in methanol solution of sodium methoxide to produce [N(O)NO] radical; washing the product with methanol and ether for several times, separating to purify, re-crystallizing, vacuum drying at room temperature and storing in a drier at -20 deg.c. The quaternary ammonium salt modified nucleophilic chitosan NO donor of the present invention has stable chemical property and relatively long release half life, and may be applied widely in treating cardiac vascular diseases and hypertensive lung, promoting wound healing, etc.