CAS: 16106-20-0; [(3R,3Ar,6S,6As)-3-Hydroxy-2,3,3A,5,6,6A-Hexahydrofuro[3,2-B]Furan-6-Yl] Nitrate

上下游产品

D-sorbitol isosorbide 2-acetate-5-mononitrate isosorbide dinitrate isosorbide 2-O-butanoate(1S,2S,5S,6R)-6-(nitrooxy)-4,8-dioxabicyclo(3.3.0)°Ct-2-yl 2-(1-((4-chlorophenyl)carbonyl)-5-methoxy-2-methylindol-3-yl)acetate isosorbide-2-(2-chlorophenylcarbamate)-5-mononitrate isosorbide-2-phenylcarbamate-5-mononitrate isosorbide-2-(cyclohexylcarbamate)-5-mononitrate

📜硝酸异山梨酯置于ferrous Sulfate,水体系中,用 甲醇 用作溶剂,以69.65%的收率获得2-硝酸异山梨酯(Store Below +4 Degr C)
参考文献:发现"真正的"阿司匹林前药.
标题:发现"真正的"阿司匹林前药.
摘要:通过苯甲酸酯基团的衍生形成的阿司匹林前药非常难以获得,因为该肽原促进了邻近乙酰基团上血浆酯酶的水解速度,从而产生了水杨酸衍生物.通过追踪人血浆溶液中阿司匹林前药异山梨醇-2,5-二氢阿司匹林酸酯(isda)的水解模式,我们能够鉴定出代谢物异山梨醇-2-Aspirinate-5-Salicylate,该代谢物几乎完全转化为阿司匹林人血浆丁酰胆碱酯酶,使其成为迄今为止发现的最成功的阿司匹林前药.
Doi:10.1021/jm801094C

专利信息

专利号:WO-2022193577-A1
优先权日:2021-03-15
标题 :Synthesis method for isosorbide mononitrate and application thereof
发明人：XIAO HANWEN; FU YONGHONG; LIN FANGYU; Zheng Yuannv; LIN XIAOXUE; Tang Xiongzhao
权利人:CHINA MEHECO KANGLI PHARMA CO LTD
摘要:The present invention belongs to the field of pharmaceutical synthesis, and disclosed are a synthesis method for isosorbide mononitrate and the application thereof. The synthesis method for isosorbide mononitrate provided by the present invention involves using a one-pot method and comprises taking sorbitol, and adding the sorbitol to concentrated sulfuric acid; and after dehydration and ring closing, adding a nitrate to perform a nitration reaction, and then adding zinc powder to perform a reduction reaction to then obtain isosorbide mononitrate. The synthesis method has a simple process flow and high raw material utilization, and saves on production costs. The present invention is suitable for the synthesis of isosorbide mononitrate, and the obtained isosorbide mononitrate is used for the preparation of isosorbide mononitrate for injection.

专利号:WO-9614060-A1
优先权日:1994-11-04
标题 :Use of receptor agonists to stimulate superoxide dismutase activity
发明人：MARKLUND STEFAN L; STRAALIN PONTUS
权利人:MARKLUND STEFAN L; STRAALIN PONTUS
摘要:The present invention relates to the use of a substance for the manufacture of a composition for stimulating the release of EC-SOD from cells or stimulating the synthesis of EC-SOD in cells. In particular, the invention relates to the use of a substance for the manufacture of a composition for prophylaxis or treatment of a disease or disorder connected with the presence or formation of superoxide radicals and other toxic intermediates derived from the superoxide radical. Further, the invention relates to a method for determining the effect of a substance with respect to stimulating the release of EC-SOD from cells or stimulating the synthesis of EC-SOD in cells and to substances which have been selected by said method. Within the scope of the invention is a method of preventing, diminishing, controlling or inhibiting a disease or disorder connected with the presence or formation of superoxide radicals and other toxic intermediates derived from the superoxide radical in a patient who has been established to have a high risk of developing a such disease or disorder, or who has developed a such disease or disorder, the method comprising administering an effective amount of a substance which is capable of stimulating the release of EC-SOD from cells or stimulating the synthesis of EC-SOD in cells.

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.