CN1986553A - 无环核苷膦酸的前体药物 - Google Patents
无环核苷膦酸的前体药物 Download PDFInfo
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- CN1986553A CN1986553A CN 200510134731 CN200510134731A CN1986553A CN 1986553 A CN1986553 A CN 1986553A CN 200510134731 CN200510134731 CN 200510134731 CN 200510134731 A CN200510134731 A CN 200510134731A CN 1986553 A CN1986553 A CN 1986553A
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- China
- Prior art keywords
- propyl group
- phosphonium mesitoyl
- mesitoyl methoxy
- propyl
- vitamin
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- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
Compound | IC50(μM) | CC50(μM) |
(R)-(POM)2-PMPA | 0.29 | 46 |
(R)-(POC)2-PMPA | 0.15 | >100 |
I1 | 0.12 | >100 |
I2 | 1.41 | >100 |
I4 | 0.09 | >100 |
I5 | 1.58 | 85 |
I6 | 1.22 | >100 |
I7 | 0.26 | >100 |
I8 | 0.94 | >100 |
I10 | 0.08 | >100 |
I11 | 0.27 | >100 |
I13 | 0.06 | >100 |
I14 | 0.18 | 39 |
I15 | 0.90 | >100 |
I16 | 1.53 | 87 |
I17 | 2.49 | >100 |
化合物 | 生物利用度(%) |
(R)-(POM)2-PMPA | 27.6 |
(R)-(POC)2-PMPA | 18.5 |
I1 | 35.0 |
I2 | 26.2 |
I4 | 24.8 |
I5 | 24.7 |
I6 | 22.4 |
I7 | 26.8 |
I8 | 29.3 |
I10 | 23.9 |
I11 | 28.1 |
I13 | 26.7 |
I14 | 21.0 |
I15 | 15.2 |
I16 | 13.6 |
Claims (5)
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CNB2005101347316A CN100567315C (zh) | 2005-12-19 | 2005-12-19 | 无环核苷膦酸的前体药物 |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CNB2005101347316A CN100567315C (zh) | 2005-12-19 | 2005-12-19 | 无环核苷膦酸的前体药物 |
Publications (2)
Publication Number | Publication Date |
---|---|
CN1986553A true CN1986553A (zh) | 2007-06-27 |
CN100567315C CN100567315C (zh) | 2009-12-09 |
Family
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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CNB2005101347316A Active CN100567315C (zh) | 2005-12-19 | 2005-12-19 | 无环核苷膦酸的前体药物 |
Country Status (1)
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CN (1) | CN100567315C (zh) |
Cited By (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN101357930B (zh) * | 2008-09-09 | 2011-06-29 | 珠海联邦制药股份有限公司 | 一种阿德福韦酯的制备方法 |
CN101418017B (zh) * | 2008-11-12 | 2011-07-20 | 上海奥锐特国际贸易有限公司 | (r)-9-(2-磷酸甲氧基丙基)腺嘌呤的合成方法 |
CN102219805A (zh) * | 2011-03-10 | 2011-10-19 | 苏州腾龙生物医药技术有限公司 | 一种新型的泰诺福韦生产工艺 |
WO2012016506A1 (zh) * | 2010-08-01 | 2012-02-09 | 江苏正大天晴药业股份有限公司 | 泰诺福韦双特戊酯富马酸盐的晶体 |
CN102977146A (zh) * | 2012-11-20 | 2013-03-20 | 广东肇庆星湖生物科技股份有限公司 | 一种腺嘌呤衍生物及其包合物 |
JP2013513552A (ja) * | 2009-12-10 | 2013-04-22 | インスティチュート オブ ファーマコロジー アンド トクシコロジー アカデミー オブ ミリタリー メディカル サイエンス、 ピー.エル.エー.チャイナ | 非環式ヌクレオシドホスホネート誘導体とその医療用途 |
JP2014514352A (ja) * | 2011-05-10 | 2014-06-19 | オカピ サイエンシーズ エン ヴェー | ネコレトロウイルス感染症の治療に使用するための化合物 |
CN104230987A (zh) * | 2014-08-15 | 2014-12-24 | 上海科一生物医药有限公司 | 一种[1-卤代-(2-丙氧基)]-甲基膦酸类化合物及其制备和应用 |
WO2015096697A1 (zh) * | 2013-12-23 | 2015-07-02 | 四川海思科制药有限公司 | 非环核苷磷酸酯类衍生物及其制备方法与在医学上的应用 |
US9908908B2 (en) | 2012-08-30 | 2018-03-06 | Jiangsu Hansoh Pharmaceutical Co., Ltd. | Tenofovir prodrug and pharmaceutical uses thereof |
-
2005
- 2005-12-19 CN CNB2005101347316A patent/CN100567315C/zh active Active
Cited By (16)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN101357930B (zh) * | 2008-09-09 | 2011-06-29 | 珠海联邦制药股份有限公司 | 一种阿德福韦酯的制备方法 |
CN101418017B (zh) * | 2008-11-12 | 2011-07-20 | 上海奥锐特国际贸易有限公司 | (r)-9-(2-磷酸甲氧基丙基)腺嘌呤的合成方法 |
JP2013513552A (ja) * | 2009-12-10 | 2013-04-22 | インスティチュート オブ ファーマコロジー アンド トクシコロジー アカデミー オブ ミリタリー メディカル サイエンス、 ピー.エル.エー.チャイナ | 非環式ヌクレオシドホスホネート誘導体とその医療用途 |
US9187507B2 (en) | 2009-12-10 | 2015-11-17 | Institute Of Pharmacology And Toxicology Academy Of Military Medical Sciences P.L.A. China | Acyclic nucleoside phosphonate derivatives and medical uses thereof |
WO2012016506A1 (zh) * | 2010-08-01 | 2012-02-09 | 江苏正大天晴药业股份有限公司 | 泰诺福韦双特戊酯富马酸盐的晶体 |
US9187508B2 (en) | 2010-08-01 | 2015-11-17 | Jiangsu Chiatai Tianqing Pharmaceutical Co., Ltd. | Crystalline forms of tenofovir dipivoxil fumarate |
CN102219805A (zh) * | 2011-03-10 | 2011-10-19 | 苏州腾龙生物医药技术有限公司 | 一种新型的泰诺福韦生产工艺 |
JP2014514352A (ja) * | 2011-05-10 | 2014-06-19 | オカピ サイエンシーズ エン ヴェー | ネコレトロウイルス感染症の治療に使用するための化合物 |
US9908908B2 (en) | 2012-08-30 | 2018-03-06 | Jiangsu Hansoh Pharmaceutical Co., Ltd. | Tenofovir prodrug and pharmaceutical uses thereof |
CN102977146B (zh) * | 2012-11-20 | 2016-04-20 | 广东肇庆星湖生物科技股份有限公司 | 一种腺嘌呤衍生物的合成方法 |
CN102977146A (zh) * | 2012-11-20 | 2013-03-20 | 广东肇庆星湖生物科技股份有限公司 | 一种腺嘌呤衍生物及其包合物 |
WO2015096697A1 (zh) * | 2013-12-23 | 2015-07-02 | 四川海思科制药有限公司 | 非环核苷磷酸酯类衍生物及其制备方法与在医学上的应用 |
CN105705508A (zh) * | 2013-12-23 | 2016-06-22 | 四川海思科制药有限公司 | 非环核苷磷酸酯类衍生物及其制备方法与在医学上的应用 |
CN105705508B (zh) * | 2013-12-23 | 2017-09-01 | 四川海思科制药有限公司 | 非环核苷磷酸酯类衍生物及其制备方法与在医学上的应用 |
CN104230987B (zh) * | 2014-08-15 | 2016-09-21 | 上海科一生物医药有限公司 | 一种[1-卤代-(2-丙氧基)]-甲基膦酸类化合物及其制备和应用 |
CN104230987A (zh) * | 2014-08-15 | 2014-12-24 | 上海科一生物医药有限公司 | 一种[1-卤代-(2-丙氧基)]-甲基膦酸类化合物及其制备和应用 |
Also Published As
Publication number | Publication date |
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CN100567315C (zh) | 2009-12-09 |
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Address after: 510075 Guangdong city of Guangzhou province Yuexiu District Shuiyin Road No. 119 star Ying king 2405A room Patentee after: Guangdong Beijing Hao Biological Pharmaceutical Co., Ltd. Address before: No. 13, Yan Garden Road, Guangzhou, Tianhe District, No. 8 Patentee before: GUANGDONG KINGHO PHARMACEUTICAL RANDD CO.,LTD |