CAS: 57564-91-7; (S)-2-Amino-5-(((R)-1-((Carboxymethyl)Amino)-3-(Nitrosothio)-1-Oxopropan-2-yl)Amino)-5-Oxopentanoic Acid

上下游产品

Glutathion 70-18-8
谷胱甘肽 Glutathione 70-18-8

📜谷胱甘肽置于二乙烯三胺五醋酸,L-苯丙氨酸,1-Nitrosopyrrolidine-2-Thiocarboxamide体系中,用98%的收率获得产物n-(N-L-γ-谷氨酰基-S-亚硝基-L-半胱氨酰----甘氨酸
参考文献:含硫原子的脂环族n-亚硝胺的反硝化
标题:含硫原子的脂环族n-亚硝胺的反硝化
摘要:已知芳香族和脂肪族亚硝胺可将亚硝鎓离子转移至另一种胺上.脂环族n-亚硝基化合物的反硝化产生s-亚硝基硫醇,S-亚硝基硫醇是体内潜在的一氧化氮供体.在这项研究中,基于非诱变的n-亚硝基脯氨酸或n-亚硝基硫代脯氨酸合成了某些脂环族n-亚硝基化合物,并在酸性条件下定量了s-亚硝基谷胱甘肽(gsno)的形成.然后,我们研究了硫原子作为取代基和环组分对gsno形成的影响.在酸性条件下存在硫脲的情况下,由n形成gsno.-亚硝基脯氨酸和谷胱甘肽以及含有硫原子和谷胱甘肽的n-亚硝基化合物可制得不含硫脲的gsno.由含硫原子的n-亚硝胺与谷胱甘肽反应得到的gsno含量高于由n-亚硝基脯氨酸与谷胱甘肽加硫脲反应得到的gsno含量.在环上或作为取代基包含硫原子的类似物中,噻唑烷类化合物产生的gsno量略高于具有硫酰胺基的类似物.在脂环族n中,在环中和作为取代基均含有硫原子的化合物对gsno的形成具有最高的活性
DOI:10.1016/j.Bmc.2013.10.008

专利信息

专利号:US-2009311292-A1
优先权日:2006-09-14
标题:Process for synthesis and incorporation of nitric oxide donors in macromolecular compositions
发明人：PACHECO OGARI; MOREIRA ROBERTO; SEABRA AMEDEA; SOUZA GABRIELA; OLIVEIRA MARCELO
权利人:CRISTALIA PROD QUIMICOS FARM; UNIV ESTADUAL DE CAMPINASUNICA
摘要:The present invention describes a process for the synthesis of S-nitrosothiols and the subsequent incorporation of these compounds in hydrophilic macromolecular compositions. By the process described herein, the S-nitrosothiols are synthesized in a device (FIG. 2 ) in a first step from the S-nitrosation reaction of their respective precursor thiols (A), promoted by a mechanical action that puts the thiols in contact with the nitrous acid formed from nitrite anions in acidic medium (B), and in a second mechanical operation, the freshly formed S-nitrosothiols are incorporated in an application vehicle (C) based on hydrophilic macromolecular compositions that increases their thermal stability. Therefore, the process under consideration combine the pre-application synthesis of S-nitrosothiols with their subsequent incorporation in delivery vehicles, with provide a relative stabilization of the S-nitrosothiols for sufficient periods so that the formulations prepared by this process may be stored in a domestic refrigerator during its time of use in its several possible applications.

专利号:WO-2008031182-A1
优先权日:2006-09-14
标 题 :Process for synthesis and incorporation of nitric oxide donors in macromolecular compositions
发明人：PACHECO OGARI; MOREIRA ROBERTO; SEABRA AMEDEA; SOUZA GABRIELA; OLIVEIRA MARCELO
权利人:CRISTALIA PROD QUIMICOS FARM; UNICAMP; PACHECO OGARI; MOREIRA ROBERTO; SEABRA AMEDEA; SOUZA GABRIELA; OLIVEIRA MARCELO
摘要:The present invention describes a device and a process for extemporaneous synthesis and incorporation of a s-nitrosothiol in a hydrophilic macromolecular composition resulting in a. topical S-nitrosothiol pharmaceutical composition, said, device constituted by a reaction compartment (5) or (12) containing an acid aqueous solution; a storage compartment [(1)+ (3)] and. [(2) + (4)] or (11) containing a nitrosable thiol, or an acid salt of the nitrosable thiol, and a nitrite salt, both in the solid form, separated from each other or in a mixture; and a formulation compartment (6) or (13) containing a hydrophilic macramolecular composition, which may be either coupled to or uncoupled from the reaction compartment, and said device being used in a process that combine the extemporaneous synthesis of a S-nitrosothiol with the incorporation of the extemporaneously synthesized S- nitrosothiol in a hydrophilic macromolecular composition immediately prior to the topical application of the resulting composition to a patient.

专利号:US-2003050305-A1
优先权日:2000-05-22
标题:Thromboxane inhibitors, compositions and methods of use
发明人：TEJADA INIGO SAENZ DE
摘要:The present invention describes methods for treating or preventing sexual dysfunctions in males and females, and for enhancing sexual responses in males and females by administering a therapeutically effective amount of at least one thromboxane inhibitor, 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 male or female may preferably be diabetic. The present invention also provides novel compositions comprising at least one thromboxane inhibitor, 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, optionally, at least one therapeutic agent, such as, vasoactive agents, nonsteroidal antiinflanmmatory compounds (NSAIDs), selective cyclooxygenase-2 (COX-2) inhibitors, anticoagulants, angiotensin converting enzymes (ACE) inhibitors, angiotensin II receptor antagonists, renin inhibitors, and mixtures thereof. The present invention also provides methods for treating or preventing ischemic heart disorders, myocardial infarction, angina pectoris, stroke, migraine, cerebral hemorrhage, cardiac fatalities, transient ischaemic attacks, complications following organ transplants, coronary artery bypasses, angioplasty, endarterectomy, atherosclerosis, pulmonary embolism, bronchial asthma, bronchitis, pneumonia, circulatory shock of various organs, nephritis, graft rejection, cancerous metastases, pregnancy-induced hypertension, preeclampsia, eclampsia, thrombotic and thromboembolic disorders, intrauterine growth, gastrointestinal disorders, renal diseases and disorders, disorders resulting from elevated uric acid levels and dysmenorrhea, and for inhibiting platelet aggregation or platelet adhesion or relaxing smooth muscles.

专利号:US-7211590-B2
优先权日:2002-08-01
标 题:Nitrosated proton pump inhibitors, compositions and methods of use
发明人：FANG XINQIN; GARVEY DAVID S; LETTS L GORDON
权利人:NITROMED INC
摘要:The invention describes novel nitrosated proton pump inhibitor compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated proton pump inhibitor compound, 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 compositions comprising at least one nitrosated proton pump inhibitor compound, 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 therapeutic agent. The invention also provides novel kits comprising at least one nitrosated proton pump inhibitor compound, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating gastrointestinal disorders; facilitating ulcer healing; decreasing the recurrence of ulcers; improving gastroprotective properties, anti-Helicobacter pylori properties or antacid properties of proton pump inhibitors; decreasing or reducing the gastrointestinal toxicity associated with the use of nonsteroidal antiinflammatory compounds; treating bacterial infections and/or viral infections.

专利号:US-6469065-B1
优先权日:1996-02-02
标 题:Nitrosated and nitrosylated α-adrenergic receptor antagonist, compositions and methods of use
发明人：GARVEY DAVID S; SCHROEDER JOSEPH D; DE TEJADA INIGO SAENEZ; GASTON RICKY D; SHELEKHIN TATIANA E; WANG TIANSHENG
权利人:NITROMED INC
摘要: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.

专利号:US-2008287407-A1
优先权日:2003-12-10
标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use
发明人：GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI
权利人:NITROMED INC
摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, 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 compositions comprising at least one pyruvate compound 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 therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, 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 treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.