CAS: 70024-40-7; (4-(4-Amino-6,7-Dimethoxyquinazolin-2-yl)Piperazin-1-yl)(Tetrahydrofuran-2-yl)Methanone Hydrochloride Dihydrate

该化合物是一种选择性的α1-Adnergic受体对立物,主要用于治疗良性先兆性高血压和高血压,其二氢酸盐形式增强了稳定性和溶性,确保了连贯一致的药用植物特性.该化合物对α1受体具有较高的生物利用率和选择性约束性,最大限度地减少离目标效果.其延长的半衰期允许每天服一次剂量,改善病人的合规性.Terazosin 盐酸二氢酸盐在严格的质量控制下合成,以达到药用标准,确保纯度和功效.二氢酸盐形式的晶体结构有助于改进处理和配制特性,使之适合制板.其记录良好的安全特征进一步支持其临床用途.

结构式图片

欧盟法规

ECHA物质C&L通报

上下游产品

isopropyl alcohol 2-chloro-6,7-dimethoxyquinazolin-4-amine N-(tetrahydro-2-furoyl)-piperazine

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    专利信息


    专利号:US-10925977-B2
    优先权日:2006-10-05
    标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
    发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
    权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
    摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

    专利号:US-6080860-A
    优先权日:1992-08-31
    标 题:Methods of making ureas and guanidines including, terazosin, prazosin, doxazosin, tiodazosin, trimazosin, quinazosin and bunazosin (exemplary of 2-substituted quinazoline compounds), and meobentine, and bethanidine and intermediates therefor
    发明人:KARIMIAN KHASHAYAR; MURTHY KESHAVA; HALL DARREN
    权利人:BRANTFORD CHEMICALSS INC
    摘要:Novel methods for the synthesis of substituted ureas and guanidines including Terazosin, Prazosin, Doxazosin, Tiodazosin, Trimazosin, Quinasin and Bunazosin (exemplary of 2-amino substituted Quinazolines), Meobentine and Bethanidine and novel intermediates suitable for use in such methods of synthesis are taught.

    专利号:US-6869973-B2
    优先权日:2000-06-22
    标题:Nitrosated and nitrosylated taxanes, compositions and methods of use
    发明人:GARVEY DAVID S; LETTS L GORDON; LIN CHIA-EN; RICHARDSON STEWART K; WANG TIANSHENG
    权利人:NITROMED INC
    摘要:The present invention describes novel nitrosated and/or nitrosylated taxanes, and novel compositions comprising at least one nitrosated and/or nitrosylated taxane, 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 therapeutic agent. The present invention also provides novel compositions comprising at least one taxane 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 compounds and compositions of the present invention can also be bound to a matrix. The present invention also provides methods for treating or preventing cardiovascular diseases and disorders, autoimmune diseases, pathological conditions resulting from abnormal cell proliferation, polycystic kidney disease, inflammatory disease, preserving organs and/or tissues or to inhibit wound contraction, particularly the prophylactic and/or therapeutic treatment of restenosis, by administering nitrosated and/or nitrosylated taxane or parent taxanes in combination with nitric oxide donors that are capable of releasing nitric oxide or indirectly delivering or transferring nitric oxide to targeted sites under physiological conditions.

    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-7384976-B2
    优先权日:2001-05-02
    标 题:Nebivolol and its metabolites in combination with nitric oxide donors, compositions and methods of use
    发明人:GARVEY DAVID S
    权利人:NITROMED INC
    摘要:The invention describes novel compositions comprising nebivolol and/or at least one metabolite of nebivolol and at least one nitric oxide donor, and, optionally, at least one antioxidant or a pharmaceutically acceptable salt thereof, and/or at least one compound used to treat cardiovascular diseases or a pharmaceutically acceptable salt thereof, and/or at least one nitrosated compound used to treat cardiovascular diseases. The compounds and compositions of the invention can also be bound to a matrix. The nitric oxide donor is a 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 may preferably be isosorbide dinitrate and/or isosorbide mononitrate. The antioxidant may preferably be a hydralazine compound or a pharmaceutically acceptable salt thereof. The invention also provides methods for treating and/or preventing vascular diseases characterized by nitric oxide insufficiency; and for treating and/or preventing Raynaud's syndrome; and for treating and/or preventing cardiovascular diseases or disorders.

    专利号:US-6387893-B1
    优先权日:1999-09-30
    标题 :Spirotricyclic substituted azacycloalkane derivatives and uses thereof
    发明人:EVANS BEN E; HOFFMAN JACOB M; GILBERT KEVIN F; RITTLE KENNETH E
    权利人:MERCK & CO INC
    摘要:Spirotricyclic azacycloalkyl compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds is also described. One application of these compounds, which are alpha 1a adrenergic receptor antagonists, is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
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    主要参考文献


    1: Wang J, Yan D, Liang K, Xu Z. A randomized controlled trial of levofloxacin, terazosin, and combination therapy in patients with category III chronic prostatitis/chronic pelvic pain syndrome. Int Urol Nephrol. 2016 Jan;48(1):13-8. doi: 10.1007/s11255-015-1147-1. Epub 2015 Nov 17. doi: 10.5867/medwave.2016.05.6480. English, Spanish. doi: 10.1097/WNF.0000000000000077. doi: 10.1590/S1677-5538.IBJU.2013.06.09. doi: 10.2116/analsci.32.763. doi: 10.3109/13651501.2012.687449. Epub 2012 Jun 26. doi: 10.1002/chir.22095. Epub 2012 Aug 9. doi: 10.1038/nchembio.1657. Epub 2014 Nov 10.
    9: Mitropoulos D, Patris E, Deliconstantinos G, Kyroudi-Voulgari A, Anastasiou I, Perea D. Terazosin-induced alterations in catalase expression and lipid peroxidation in the rat seminal vesicles. Andrologia. 2013 Apr;45(2):128-34. doi: 10.1111/j.1439-0272.2012.01324.x. Epub 2012 Jun 26. Epub 2013 May 1.

    合成参考文献


    摘要:Iyakuhin Kenkyu. Study of Medical Supplies., 18(505), 1987
    摘要:New Cardiovascular Drugs., 4(1), 1986
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