发明公开
- 专利标题: ALPHA 1a ADRENERGIC RECEPTOR ANTAGONIST
- 专利标题(中): ALFA 1A肾上腺素能受体拮抗剂
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申请号: EP98938234.6申请日: 1998-07-31
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公开(公告)号: EP1003734A2公开(公告)日: 2000-05-31
- 发明人: SIDLER, Daniel, R. , LARSEN, Robert, D. , CHARTRAIN, Michel , IKEMOTO, Norihiro , ROBERGE, Christopher, M. , TAYLOR, Colleen, S. , LI, Wenjie , BILLS, Gerald, F.
- 申请人: MERCK & CO., INC.
- 申请人地址: 126 East Lincoln Avenue Rahway, New Jersey 07065 US
- 专利权人: MERCK & CO., INC.
- 当前专利权人: MERCK & CO., INC.
- 当前专利权人地址: 126 East Lincoln Avenue Rahway, New Jersey 07065 US
- 代理机构: Horgan, James Michael Frederic
- 优先权: US54815P 19970805; US54902P 19970805; GB9719706 19970916; GB9719708 19970916; US122301 19980724
- 国际公布: WO9907695 19990218
- 主分类号: C07D401/00
- IPC分类号: C07D401/00
摘要:
This invention relates to crystalline pharmaceutically acceptable salts of an alpha 1a adrenergic receptor antagonist, Compound A, which are useful in the treatment of benign prostatic hyperplasia. Pharmaceutical compositions employing the crystalline salts, and processes for making and using the crystalline salts and pharmaceutical compositions of Compound A are also disclosed. This invention further relates to a process for obtaining enantiomerically pure intermediate useful for the synthesis of end product alpha 1a adrenergic receptor antagonists. The end product compounds are useful for the treatment of benign prostatic hyperplasia and for relaxing lower urinary tract tissue. The invention also relates to a process for preparing a class of dihydropyrimidinone compounds of which Compound A is a member, wherein the process involves deprotonating a dihydropyrimidinone compound and then coupling the deprotonated derivative with a primary amine.
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