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-2024390383-A1 优先权日:2021-09-28 标题 :Dioxazines and their use in treatment of gba-related diseases 发明人:NEVE SØREN; BROWN WILLIAM DALBY; THIRSTRUP KENNETH 权利人:ZEVRA DENMARK AS 摘要:The present invention relates to dioxazines, their synthesis, and their use for increasing GBA activity and/or levels as well as treatment of GBA-related diseases, such as Parkinson's disease.
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.
专利号:WO-0027817-A1 优先权日:1998-11-10 标 题:Oxazolidinones useful as alpha 1a adrenoceptor antagonists 发明人:NERENBERG JENNIE B; BOCK MARK G; PATANE MICHAEL A; SELNICK HAROLD G 权利人:MERCK & CO INC; NERENBERG JENNIE B; BOCK MARK G; PATANE MICHAEL A; SELNICK HAROLD G 摘要:Novel hydroxymethyl- and alkoxymethyl-oxazolidinone 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 uring 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:WO-0027827-A1 优先权日:1998-11-10 标题:Oxazolidinones useful as alpha 1a adrenoceptor antagonists 发明人:NERENBERG JENNIE B; BOCK MARK G; SELNICK HAROLD G; PAYNE LINDA 权利人:MERCK & CO INC; NERENBERG JENNIE B; BOCK MARK G; SELNICK HAROLD G; PAYNE LINDA 摘要:Novel oxazolidinone 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-6436962-B1 优先权日:1999-09-30 标题:Arylhydantoin derivatives and uses thereof 发明人:HOFFMAN JACOB M; BOCK MARK G; DIPARDO ROBERT M; PAYNE LINDA S; PATANE MICHAEL A 权利人:MERCK & CO INC 摘要:Arylhydantoin 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.
参考文献:10.1055/s-0029-1217818 摘要:Nishi T, Nakamura Y, Jojima T, Suzuki C, Miyazaki S. Efficient Synthesis of 5-Alkoxy-(3R)-hydroxy-2,3-dihydrospiro[indene-1,4′-piperidines]: A Novel Scaffold for Renin Inhibitors. Synlett. 2009 Aug 17;2009(15):2521–3. doi: 10.1055/s-0029-1217818. 参考文献:10.1007/s44371-025-00229-5 摘要:Nagalingaiah NK, Kameshwar VH, Nanjundappa SH, Ningegowda SK, Kempegowda M. Development of novel 3, 5-substituted-1,2,4-oxadiazole derivatives: a multidimensional approach with in vitro antibacterial, antioxidant, DFT insights, and molecular dynamics simulations. Discov. Chem. 2025 Jul 29;2(1). doi: 10.1007/s44371-025-00229-5.