CAS: 78628-28-1; Roxatidine Acetate

该化合物是一种主要用作抗口炎和抗肺素剂的药物化合物,具有选择性的H2受体抗体对抗剂的作用,有助于减少胃酸分泌,在治疗胃溃疡和胃肠复发病等条件下有效.该化合物的特点是能够通过阻塞胃内衬内H2受体的异丙胺行动,提供抗酸性失调的症状缓解.该化合物一般是口服的,而且已知其行动时间相对较长,与其他H2对口服者相比,它的作用是很好的.该化合物的副作用可能包括某些病人头痛,眩晕或胃肠紊乱.该化合物的化学结构包括一个乙酸酯类,它有助于其药性.与任何药物一样,它对于在医疗监督下使用霉素乙酸盐以确保安全性和功效至关重要,特别是在那些有前健康状况的病人中,使用其他药物.

结构式图片

上下游产品

formaldehyd acetic acid propyl>amineN-3-3-(1-piperidinylmethyl)phenoxypropylamine potassium acetate

合成工艺路线路线简述

    N-3-[3-(1-哌啶甲基)-苯氧基]丙胺置于三乙胺体系中,用 二氯甲烷 作为反应溶剂,化学反应 7.0H,反应生成 醋酸罗沙替丁
    参考文献:在passerini反应中使用2-羟甲基苯甲酸作为有效的水替代物:直接获得α-羟酰胺
    标题:在passerini反应中使用2-羟甲基苯甲酸作为有效的水替代物:直接获得α-羟酰胺
    摘要:多年来,已经描述了用于合成α-羟基酰胺的数十种策略,但是它们在通用性和耐受性(尤其是对酸不稳定的功能性)方面具有共同的缺点.在这里,我们报告截短的passerini反应,适用于轻松温和地制备官能化的α-羟基酰胺.特别地,该方法耐受酸敏感性保护基,其在多组分反应期间保持完整.
    DOI:10.1016/j.Tetlet.2017.11.021

    海关参考信息

    专利信息


    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-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.

    专利号:US-8304409-B2
    优先权日:2002-07-03
    标 题:Nitrosated nonsteroidal antiinflammatory compounds, compositions and methods of use
    发明人:EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; KHANAPURE SUBHASH P; LETTS L GORDON; LIN CHIA-EN; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI
    权利人:EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; KHANAPURE SUBHASH P; LETTS L GORDON; LIN CHIA-EN; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI; NICOX SA
    摘要:The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, 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 NSAID, 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 NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating inflammation, pain and fever; for treating gastrointestinal disorders; for facilitating wound healing; for treating and/or preventing gastrointestinal, renal and/or respiratory toxicities resulting from the use of nonsteroidal antiinflammatory compounds; for treating inflammatory disease states and/or disorders; and for treating and/or preventing ophthalmic diseases and/or disorders.

    专利号:US-2002183366-A1
    优先权日:2001-03-23
    标题:Cyclooxygenase-2 inhibitors, compositions and methods of use
    发明人:GARVEY DAVID S; SCHROEDER JOSEPH D
    摘要:This invention describes novel compounds that are 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, optionally, at least one therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, 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 toxicity or other toxicities; 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.

    专利号:US-2003203915-A1
    优先权日:2002-04-05
    标题 :Nitric oxide donors, compositions and methods of use related applications
    发明人:FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; LIN CHIA-EN; RANATUNGA RAMANI R; RICHARDSON STEWART K; WANG TIANSHENG; WANG WEIHENG; WEY SHIOW-JYI
    权利人:FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; LIN CHIA-EN; RANATUNGA RAMANI R; RICHARDSON STEWART K; WANG TIANSHENG; WANG WEIHENG; WEY SHIOW-JYI
    摘要:The invention describes novel nitric oxide donors and novel compositions comprising at least one nitric oxide donor. The invention also provides novel compositions comprising at least one nitric oxide donor, and, optionally, 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 the inhibition of 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, vascular diseases; for reducing scar tissue or for inhibiting wound contraction, particularly the prophylactic and/or therapeutic treatment of restenosis by administering the nitric oxide donor optionally in combination with at least one therapeutic agent. The invention also provides methods for treating inflammation, pain, fever, gastrointestinal disorders, respiratory disorders and sexual dysfunctions. The nitric oxide donors donate, transfer or release nitric oxide, and/or elevate endogenous levels of endothelium-derived relaxing factor, and/or stimulate endogenous synthesis of nitric oxide and/or are substrates for nitric oxide synthase and are capable of releasing nitric oxide or indirectly delivering or transferring nitric oxide to targeted sites under physiological conditions. The therapeutic agent can optionally be substituted with at least one NO and/or NO 2 group (i.e., nitrosylated and/or nitrosated). The invention also provides novel compositions and kits comprising at least one nitric oxide donor and/or at least one therapeutic agent.

    专利号:US-7256205-B2
    优先权日:1998-11-17
    标题 :Nitrosated and nitrosylated H2 receptor antagonist compounds, compositions and methods of use
    发明人:GARVEY DAVID S; LETTS L GORDON; LIN CHIA-EN; WANG TIANSHENG
    权利人:NITROMED INC
    摘要:The invention describes novel nitrosated and/or nitrosylated H 2 receptor antagonist compounds, and novel compositions comprising at least one H 2 receptor antagonist compound that is optionally substituted with at least one NO and/or NO 2 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 nonsteroidal antiinflammatory drug, antacid, bismuth-containing reagent or anti-viral agent. The invention also describes methods for treating and/or preventing gastrointestinal disorders; improving gastroprotective properties of H 2 receptor antagonists; decreasing the recurrence of ulcers; facilitating ulcer healing; preventing and/or treating inflammations and microbial infections, ophthalmic diseases and disorders, multiple sclerosis, and viral infections; and decreasing or reducing the gastrointestinal toxicity associated with the use of nonsteroidal antiinflammatory compounds.
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    主要参考文献


    1: Nakamura H, Kawashima H, Azuma R, Sato I, Nagao K, Miyazawa K. Pharmacokinetics of the H(2) blocker roxatidine acetate hydrochloride in pediatric patients, in comparison with healthy adult volunteers. Drug Metab Pharmacokinet. 2012;27(4):422-9. Epub 2012 Jan 31. doi: 10.1016/j.carres.2011.07.003. Epub 2011 Jul 18. Review. Review. doi: 10.1002/jcb.23294. doi: 10.1631/jzus.B1100078.
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    合成参考文献


    参考文献:10.1007/s00109-011-0788-5
    摘要:Paulin R, Courboulin A, Barrier M, Bonnet S. From oncoproteins/tumor suppressors to microRNAs, the newest therapeutic targets for pulmonary arterial hypertension. J Mol Med (Berl). 2011 Nov;89(11):1089–101. doi: 10.1007/s00109-011-0788-5.
    参考文献:10.3164/jcbn.10-101
    摘要:Hirota K, Kudo M, Hashimoto H, Kushikata T. A marked increase in gastric fluid volume during cardiopulmonary bypass. J Clin Biochem Nutr. 2011 Jul;49(1):16–9.
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