JP7237362B2 - 急性腎不全の治療における使用のためのアンブリセンタン - Google Patents
急性腎不全の治療における使用のためのアンブリセンタン Download PDFInfo
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- JP7237362B2 JP7237362B2 JP2019500021A JP2019500021A JP7237362B2 JP 7237362 B2 JP7237362 B2 JP 7237362B2 JP 2019500021 A JP2019500021 A JP 2019500021A JP 2019500021 A JP2019500021 A JP 2019500021A JP 7237362 B2 JP7237362 B2 JP 7237362B2
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| EP16166046.9A EP3235496A1 (en) | 2016-04-19 | 2016-04-19 | Treatment of acute renal failure |
| US201662437949P | 2016-12-22 | 2016-12-22 | |
| US62/437,949 | 2016-12-22 | ||
| PCT/EP2017/056476 WO2017158199A1 (en) | 2016-03-18 | 2017-03-20 | Ambrisentan for use in the treatment of acute renal failure |
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| EP4142731A1 (en) * | 2020-04-28 | 2023-03-08 | Noorik Biopharmaceuticals AG | Treatment of pulmonary complications of coronavirus infections |
| US20230165856A1 (en) * | 2020-04-29 | 2023-06-01 | Astrazeneca Ab | Dapagliflozin and ambrisentan for the prevention and treatment of covid-19 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013129549A1 (ja) | 2012-02-29 | 2013-09-06 | 東レ株式会社 | 体腔液貯留抑制剤 |
| WO2014138738A1 (en) | 2013-03-08 | 2014-09-12 | Abbive Inc. | Methods of treating acute kidney injury |
| WO2014176534A1 (en) | 2013-04-26 | 2014-10-30 | La Jolla Pharmaceutical Company | Compositions and methods for treating renal failure |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE19533023B4 (de) | 1994-10-14 | 2007-05-16 | Basf Ag | Neue Carbonsäurederivate, ihre Herstellung und Verwendung |
| EP2183223A2 (en) * | 2007-07-31 | 2010-05-12 | Gilead Colorado, Inc. | Metabolites and derivatives of ambrisentan |
| US9255931B2 (en) | 2010-06-24 | 2016-02-09 | Morehouse School Of Medicine | Method and compositions for the treatment and detection of endothelin-1 related kidney diseases |
| US20150125546A1 (en) * | 2013-11-06 | 2015-05-07 | Gilead Sciences, Inc. | Combination therapy for treating pulmonary hypertension |
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Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013129549A1 (ja) | 2012-02-29 | 2013-09-06 | 東レ株式会社 | 体腔液貯留抑制剤 |
| WO2014138738A1 (en) | 2013-03-08 | 2014-09-12 | Abbive Inc. | Methods of treating acute kidney injury |
| WO2014176534A1 (en) | 2013-04-26 | 2014-10-30 | La Jolla Pharmaceutical Company | Compositions and methods for treating renal failure |
Non-Patent Citations (2)
| Title |
|---|
| ARCH. INTERN. MED.,2002年,Vol.162,P.323-328 |
| 日本内科学会雑誌,2013年,第102巻/第7号,P.1807-1813 |
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| ZA201805562B (en) | 2019-06-26 |
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| EP3235496A1 (en) | 2017-10-25 |
| IL261457B (en) | 2021-09-30 |
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| AU2017235618A1 (en) | 2018-09-27 |
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