CAS: 74191-85-8; (4-(4-Amino-6,7-Dimethoxyquinazolin-2-yl)Piperazin-1-yl)(2,3-Dihydrobenzo[b][1,4]Dioxin-2-yl)Methanone

该化合物是一种主要用于治疗高血压和良性先质高血压和良性高血压的选择性甲型-1肾上抗激剂(BPH),其作用是将阿尔法-1受体屏蔽在血管滑动肌肉中,导致血管变异,随后血液压力下降.Doxazosin的特征是化学配方,包括一种quinazoline结构,通常看起来像白色的脱白晶粉.该物质在甲醇和乙醇等有机溶剂中溶解,但水溶性有限.其药用动力学涉及广泛的肝脏新陈代谢,其半衰期相对较长,允许每天一次服用.常见副作用可能包括眩晕,疲劳和或霍氏性低温.Doxazosin通常与改变生活方式和其他抗体剂相结合,以提高治疗功效.与任何药物一样,它对于监测潜在相互作用和反常变异性,特别是病人与心血管病史上的问题至关重要.

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CAS号23680-84-4 4-氨基-2-氯-6, 7-二氧基喹唑啉 | CAS号70918-00-2 2-(1-哌嗪羰基)-1,4-... | CAS号60547-97-9 2-(1-哌嗪基)-4-氨基-... | CAS号120-80-9 邻苯二酚 | CAS号4739-94-0 2,3-二氢-1,4-苯并二噁... | CAS号3663-80-7 1,4-苯并二烷-2-羧酸

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    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:WO-9900440-A1
    优先权日:1997-06-26
    标 题:Synthesis of a dendritic polyalcohol
    发明人:IHRE HENRIK; HULT ANDERS
    权利人:PERSTORP AB; IHRE HENRIK; HULT ANDERS
    摘要:A process for a double stage convergent synthesis of a polymeric polyalcohol substantially and preferably built up from polyester units and composed of a monomeric or polymeric core to which at least one hyperbranched dendritic branch (dendron) consisting of a number of branching generations is added. The branching generations comprise a polymeric or monomeric branching chain extender having three reactive functions of which two are hydroxyl groups and one is a carboxyl group. The two hydroxyl groups of the branching chain extender is in a first step ketal protected by reacting said two hydroxyl groups with a ketal. A second step includes protection of the carboxyl group of said branching chain extender. The ketal protected branching chain extender and the carboxyl protected chain extender are then employed for repeated addition in a number of step yielding a predetermined number of branching generations. The thus synthesized dendron is finally added to a core having reactive hydroxyl or epoxide groups and the ketal protected hydroxyl groups are optionally deprotected.

    专利号:US-10973847-B2
    优先权日:2017-06-30
    标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof
    发明人:JOHNSON JEREMIAH A; GOLDER MATTHEW R
    权利人:MASSACHUSETTS INST TECHNOLOGY
    摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.

    专利号:US-2015239796-A1
    优先权日:2014-02-19
    标题:One pot synthesis of 18f labeledtrifluoromethylated compounds with difluoro(iodo)methane
    发明人:RüHL THOMAS; RISS PATRICK; RAFIQUE WAQAS
    权利人:UNIV OSLO
    摘要:The present invention relates to compositions and methods for the synthesis of 18 F labeled compounds. In particular, the present invention relates to a copper (I) mediated one pot method for 18 F-trifluoromethylation of aromatic- or heteroaromatic halides with difluoro(iodo)methane (e.g., for use at PET imaging agents).

    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-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.
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    主要参考文献


    1: Paik YH. Reappraisal of Antihypertensive Medicine Doxazosin and Carvedilol as a Potential Therapeutic for Hepatic Fibrosis. Gut Liver. 2016 Jan 23;10(1):10-1. doi: 10.5009/gnl15576. doi: 10.5009/gnl14459. Spectrochim Acta A Mol Biomol Spectrosc. 2015 Dec 17;157:55-60. doi: 10.1016/j.saa.2015.12.012. [Epub ahead of print] doi: 10.1016/j.juro.2015.09.040. Epub 2015 Sep 21. Spironolactone versus placebo, bisoprolol, and doxazosin to determine the optimal treatment for drug-resistant hypertension (PATHWAY-2): a randomised, double-blind, crossover trial. Lancet. 2015 Nov 21;386(10008):2059-68. doi: 10.1016/S0140-6736(15)00257-3. Epub 2015 Sep 20.
    9: Kasacka I, Piotrowska Ż, Filipek A, Majewski M. Influence of doxazosin on biosynthesis of S100A6 and atrial natriuretic factor peptides in the heart of spontaneously hypertensive rats. Exp Biol Med (Maywood). 2015 Oct 28. pii: 1535370215611972. [Epub ahead of print] doi: 10.1002/chir.22483. Epub 2015 Jul 23. doi: 10.1016/j.ejps.2015.06.022. Epub 2015 Jun 25.
    14: Konca C, Tekin M, Turgut M. Doxazosin in the treatment of scorpion envenomation. Indian J Pediatr. 2015 Jun;82(6):499-503. doi: 10.1007/s12098-014-1423-6. Epub 2014 Apr 4. Chinese. doi: 10.1016/j.juro.2014.11.042. Epub 2014 Nov 15. doi: 10.3109/10641963.2014.913599. Epub 2014 May 27. doi: 10.1016/j.urology.2014.10.004. doi: 10.1016/j.ijbiomac.2014.08.028. Epub 2014 Aug 29. doi: 10.1016/j.saa.2014.06.095. Epub 2014 Jun 24.

    合成参考文献


    参考文献:10.1002/jemt.20828
    摘要:Delella FK, Felisbino SL. Doxazosin treatment alters stromal cell behavior and increases elastic system fibers deposition in rat prostate. Microsc Res Tech. 2010 Oct;73(11):1036–44. doi: 10.1002/jemt.20828.
    参考文献:10.4111/kju.2011.52.6.406
    摘要:Jang DG, Yoo C, Oh CY, Kim SJ, Kim SI, Kim CI, Kim HS, Park JY, Seong do H, Song YS, Yang WJ, Cho IR, Cho SY, Cheon SH, Im H, Cho JS. Current status of transurethral prostatectomy: a korean multicenter study. Korean J Urol. 2011 Jun;52(6):406–9.
    参考文献:10.2147/cia.s13803
    摘要:Yoshida M, Kudoh J, Homma Y, Kawabe K. Safety and efficacy of silodosin for the treatment of benign prostatic hyperplasia. Clin Interv Aging. 2011;6():161–72.
    参考文献:10.2147/tcrm.s13883
    摘要:Masumori N. Naftopidil for the treatment of urinary symptoms in patients with benign prostatic hyperplasia. Ther Clin Risk Manag. 2011;7():227–38.
    参考文献:10.1007/s00508-011-0030-z
    摘要:Struhal W, Hödl S, Mazhar S, Ransmayr G. Acute pandysautonomia--restitutio ad integrum by high prednisolone therapy. Wien Klin Wochenschr. 2011 Aug;123(15-16):508–11. doi: 10.1007/s00508-011-0030-z.
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