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-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.
专利号:US-6130218-A 优先权日:1996-12-20 标 题 :Polymorphic form of doxazosin mesylate (Form I) 发明人:MOERSDORF JOHANN PETER; GRAFE INGOMAR 权利人:HEUMANN PHARMA GMBH & CO 摘要:A new crystalline and anhydrous form of doxazosin mesylate is described. The new form is crystalline and anhydrous and is characterized in its X-ray spectrum by the following reflex positions of high and medium intensity: 15.40°, 16.85°, 18.06°, 24.15° and 25.81°. Owing to its crystalline properties, the new form of doxazosin mesylate according to the invention has surprising advantages both with regard to its synthesis and for pharmaceutical processing into solid dosage forms. A process for preparing the new form of doxazosin mesylate and pharmaceutical compositions comprising the new form of doxazosin mesylate are also described.
专利号:US-6133269-A 优先权日:1996-12-20 标题:Polymorphic form of doxazosin mesylate (form II) 发明人:MOERSDORF JOHANN PETER; GRAFE INGOMAR 权利人:HEUMANN PHARMA GMBH & CO 摘要:A new crystalline and anhydrous form of doxazosin mesylate is described. The new form is crystalline and anhydrous and is characterized in its X-ray spectrum by the following reflex positions of high and medium intensity: 10.68°, 14.45°, 17.37°, 23.45°, 23.82° and 24.30 °. Owing to its crystalline properties, the new form of doxazosin mesylate according to the invention has surprising advantages both with regard to its synthesis and for pharmaceutical processing into solid dosage forms. A process for preparing the new form of doxazosin mesylate and pharmaceutical compositions comprising the new form of doxazosin mesylate are also described.
专利号:US-6232318-B1 优先权日:1998-11-12 标 题:Pyrimidinedione derivatives useful as alpha 1A adrenoceptor antagonists 发明人:NERENBERG JENNIE B; BOCK MARK G 权利人:MERCK & CO LTD 摘要:Novel pyrimidinedione compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds 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.
专利号:US-6326372-B1 优先权日:1999-09-30 标 题:Lactam and cyclic urea derivatives useful as alpha 1a adrenoceptor antagonists 发明人:EVANS BEN E; GILBERT KEVIN F 权利人:MERCK & CO INC 摘要:Lactam and cyclic urea derivatives and their pharmaceutically acceptable salts are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are typically 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.
1: Ansari E, Honarvar B, Sajadian SA, Arab Aboosadi Z, Azizi M. Utilization of RESOLV with polymer to produce prazosin hydrochloride nanoparticles and optimization of the process parameters. Sci Rep. 2024 Aug 7;14(1):18346. doi: 10.1038/s41598-024-69128-6. 2: Sudaki H, Fujimoto K, Wada K, Sugano K. Phosphate buffer interferes dissolution of prazosin hydrochloride in compendial dissolution testing. Drug Metab Pharmacokinet. 2023 Aug;51:100519. doi: 10.1016/j.dmpk.2023.100519. Epub 2023 Jun 10. 11(47):29441-29452. doi: 10.1039/d1ra04758b. 4: Mazeh AC, Angus JA, Wright CE. Pharmacological characterisation of the CB1 receptor antagonist activity of cannabidiol in the rat vas deferens bioassay. Eur J Pharmacol. 2021 Oct 15;909:174433. doi: 10.1016/j.ejphar.2021.174433. Epub 2021 Aug 17.
合成参考文献
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