CN103732594A - 替诺福韦艾拉酚胺(tenofovir alafenamide)半反丁烯二酸盐 - Google Patents

替诺福韦艾拉酚胺(tenofovir alafenamide)半反丁烯二酸盐 Download PDF

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CN103732594A
CN103732594A CN201280039891.0A CN201280039891A CN103732594A CN 103732594 A CN103732594 A CN 103732594A CN 201280039891 A CN201280039891 A CN 201280039891A CN 103732594 A CN103732594 A CN 103732594A
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hemifumarate
tenofovir alafenamide
hiv
infection
composition
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刘大展
施冰
王芳
理查德·洪秋·于
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Gillian Science
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Gillian Science
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    • C07—ORGANIC CHEMISTRY
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    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
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    • A61K31/00—Medicinal preparations containing organic active ingredients
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/683—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
    • A61K31/685—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P31/12—Antivirals
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine

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  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
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CN201280039891.0A 2011-08-16 2012-08-15 替诺福韦艾拉酚胺(tenofovir alafenamide)半反丁烯二酸盐 Pending CN103732594A (zh)

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CN201910647566.6A CN110343135A (zh) 2011-08-16 2012-08-15 替诺福韦艾拉酚胺(tenofovir alafenamide)半反丁烯二酸盐

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US201161524224P 2011-08-16 2011-08-16
US61/524,224 2011-08-16
PCT/US2012/050920 WO2013025788A1 (en) 2011-08-16 2012-08-15 Tenofovir alafenamide hemifumarate

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CN201910647566.6A Pending CN110343135A (zh) 2011-08-16 2012-08-15 替诺福韦艾拉酚胺(tenofovir alafenamide)半反丁烯二酸盐

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CN104558036A (zh) * 2014-12-11 2015-04-29 杭州和泽医药科技有限公司 一种替诺福韦艾拉酚胺半反丁烯二酸盐晶型及其制备方法
CN105237571A (zh) * 2014-11-28 2016-01-13 成都苑东药业有限公司 9-[(r)-2-[[(s)-[[(s)-1-(异丙氧基羰基)乙基]氨基]苯氧基氧膦基]甲氧基]丙基]腺嘌呤的盐
CN105669751A (zh) * 2015-03-05 2016-06-15 洛阳聚慧医药科技有限公司 非环核苷酸磷酰胺类化合物及其盐的制备以及在抗病毒方面的应用
CN106414466A (zh) * 2014-05-20 2017-02-15 四川海思科制药有限公司 替诺福韦艾拉酚胺复合物及其制备方法和用途
CN106699812A (zh) * 2015-11-12 2017-05-24 江苏豪森药业集团有限公司 替诺福韦前药的制备和纯化方法
CN107226826A (zh) * 2016-03-25 2017-10-03 江苏奥赛康药业股份有限公司 替诺福韦艾拉酚胺富马酸盐化合物及其药物组合物
CN107445994A (zh) * 2017-05-31 2017-12-08 北京阜康仁生物制药科技有限公司 替诺福韦艾拉酚胺半富马酸盐新晶型
WO2017211325A1 (zh) * 2016-06-05 2017-12-14 上海诚妙医药科技有限公司 富马酸替诺福韦艾拉酚胺盐的新晶型、制备方法及其用途
CN107793451A (zh) * 2016-08-30 2018-03-13 江苏奥赛康药业股份有限公司 替诺福韦艾拉酚胺半富马酸盐化合物及其药物组合物
CN107865874A (zh) * 2017-10-23 2018-04-03 上海博悦生物科技有限公司 一种替诺福韦艾拉酚胺的药物组合物及其制备方法
CN108070003A (zh) * 2016-12-02 2018-05-25 上海博志研新药物技术有限公司 替诺福韦艾拉酚胺半反丁烯二酸盐晶型及制备方法和应用
CN108117570A (zh) * 2016-11-28 2018-06-05 正大天晴药业集团股份有限公司 一种替诺福韦艾拉酚胺半富马酸盐的结晶及其制备方法
CN108148094A (zh) * 2014-11-12 2018-06-12 四川海思科制药有限公司 一种替诺福韦艾拉酚胺富马酸盐晶型c及其制备方法和用途
CN108440596A (zh) * 2018-03-22 2018-08-24 山东科兴生物制品有限公司 一种半富马酸替诺福韦艾拉酚胺的新型制备工艺
CN108794530A (zh) * 2017-04-26 2018-11-13 上海医药工业研究院 一种替诺福韦丙酚酰胺盐晶型及其制备方法和用途
CN110234655A (zh) * 2017-01-31 2019-09-13 吉利德科学公司 替诺福韦艾拉酚胺的结晶形式
CN110452268A (zh) * 2019-08-21 2019-11-15 天地恒一制药股份有限公司 一种丙酚替诺福韦半富马酸单晶的制备方法

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