发明授权
- 专利标题: Phosphonic acid based prodrugs of PMEA and its analogues
- 专利标题(中): 基于磷酸的前药PMEA及其类似物
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申请号: US10436922申请日: 2003-05-12
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公开(公告)号: US07214668B2公开(公告)日: 2007-05-08
- 发明人: K. Raja Reddy , Mark D. Erion , Michael C. Matelich , Joseph J. Kopcho
- 申请人: K. Raja Reddy , Mark D. Erion , Michael C. Matelich , Joseph J. Kopcho
- 申请人地址: US CA La Jolla
- 专利权人: Metabasis Therapeutics, Inc.
- 当前专利权人: Metabasis Therapeutics, Inc.
- 当前专利权人地址: US CA La Jolla
- 代理机构: Sterne, Kessler, Goldstein & Fox P.L.L.C.
- 主分类号: C07F9/6574
- IPC分类号: C07F9/6574 ; A61K31/675 ; A61P31/20 ; A61P31/14 ; A61P35/00
摘要:
Prodrugs of Formula I, their uses, their intermediates, and their method of manufacture are described: wherein: M and V are cis to one another and MPO3H2 is a phosphonic acid selected from the group consisting of 9-(2-phosphonylmethoxyethyl)adenine, (R)-9-(2-phosphonylmethoxy propyl)adenine, 9-(2-phosphonylmethoxyethyl)guanine, 9-(2-phosphonylmethoxy ethyloxy)adenine, 9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine, (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine, (S)-9-(3-hydroxy-2-phosphonylmethoxypropyl)adenine, 9-(3-hydroxy-2-phosphonylmethoxypropyl)guanine, and (S)-9-(3-fluoro-2-phosphonyl methoxypropyl)adenine; V is selected from a group consisting of phenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-furanyl, 3-furanyl, 2-thienyl, and 3-thienyl, all optionally substituted with 1-3 substituents selected from a group consisting of F, Cl, Br, C1-C3 alkyl, CF3 and OR6; R6 is selected from the group consisting of C1-C3 alkyl, and CF3; and pharmaceutically acceptable salts thereof.
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