UA75614C2 - Спосіб лікування гетерозиготної родинної гіперхолестеринемії розувастатином (zd-4522) - Google Patents
Спосіб лікування гетерозиготної родинної гіперхолестеринемії розувастатином (zd-4522) Download PDFInfo
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- UA75614C2 UA75614C2 UA2003054394A UA2003054394A UA75614C2 UA 75614 C2 UA75614 C2 UA 75614C2 UA 2003054394 A UA2003054394 A UA 2003054394A UA 2003054394 A UA2003054394 A UA 2003054394A UA 75614 C2 UA75614 C2 UA 75614C2
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- density lipoprotein
- methylsulfonyl
- isopropyl
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Classifications
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
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- A61P9/00—Drugs for disorders of the cardiovascular system
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- Vascular Medicine (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0028429.9A GB0028429D0 (en) | 2000-11-22 | 2000-11-22 | Therapy |
| PCT/GB2001/005041 WO2002041895A1 (en) | 2000-11-22 | 2001-11-16 | Use of rosuvastatin (zd-4522) in the treatment of heterozygous familial hypercholesterolemia |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| UA75614C2 true UA75614C2 (uk) | 2006-05-15 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| UA2003054394A UA75614C2 (uk) | 2000-11-22 | 2001-11-16 | Спосіб лікування гетерозиготної родинної гіперхолестеринемії розувастатином (zd-4522) |
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Families Citing this family (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0003305D0 (en) * | 2000-02-15 | 2000-04-05 | Zeneca Ltd | Pyrimidine derivatives |
| US7407965B2 (en) * | 2003-04-25 | 2008-08-05 | Gilead Sciences, Inc. | Phosphonate analogs for treating metabolic diseases |
| US20050261237A1 (en) * | 2003-04-25 | 2005-11-24 | Boojamra Constantine G | Nucleoside phosphonate analogs |
| US7452901B2 (en) * | 2003-04-25 | 2008-11-18 | Gilead Sciences, Inc. | Anti-cancer phosphonate analogs |
| EP1628685B1 (en) | 2003-04-25 | 2010-12-08 | Gilead Sciences, Inc. | Antiviral phosphonate analogs |
| US7470724B2 (en) * | 2003-04-25 | 2008-12-30 | Gilead Sciences, Inc. | Phosphonate compounds having immuno-modulatory activity |
| US20090247488A1 (en) * | 2003-04-25 | 2009-10-01 | Carina Cannizzaro | Anti-inflammatory phosphonate compounds |
| MXPA05011296A (es) * | 2003-04-25 | 2006-01-24 | Gilead Sciences Inc | Conjugados de fosfonato inhibidores de la cinasa. |
| WO2005023778A2 (en) * | 2003-08-28 | 2005-03-17 | Teva Pharmaceutical Industries Ltd. | Process for preparation of rosuvastatin calcium |
| GB0322552D0 (en) | 2003-09-26 | 2003-10-29 | Astrazeneca Uk Ltd | Therapeutic treatment |
| US7432273B2 (en) * | 2003-10-24 | 2008-10-07 | Gilead Sciences, Inc. | Phosphonate analogs of antimetabolites |
| US7777034B2 (en) | 2003-11-24 | 2010-08-17 | Teva Pharmaceutical Industries Ltd. | Crystalline ammonium salts of rosuvastatin |
| EP1689723B1 (en) * | 2003-12-02 | 2011-04-27 | Teva Pharmaceutical Industries, Ltd. | Reference standard for characterization of rosuvastatin |
| US20070179166A1 (en) * | 2003-12-24 | 2007-08-02 | Valerie Niddam-Hildesheim | Process for preparation of statins with high syn to anti ratio |
| US7851624B2 (en) * | 2003-12-24 | 2010-12-14 | Teva Pharamaceutical Industries Ltd. | Triol form of rosuvastatin and synthesis of rosuvastatin |
| US20060013861A1 (en) * | 2004-05-26 | 2006-01-19 | Kgk Synergize Inc. | Functional foods comprising flavonoids and tocotrienols and methods thereof |
| EP1673351A1 (en) * | 2004-07-13 | 2006-06-28 | Teva Pharmaceutical Industries Ltd. | A process for the preparation of rosuvastatin involving a tempo-mediated oxidation step |
| WO2006110157A2 (en) | 2004-07-27 | 2006-10-19 | Gilead Sciences, Inc. | Nucleoside phosphonate conjugates as anti hiv agents |
| CA2591439C (en) * | 2005-02-22 | 2013-03-26 | Teva Pharmaceutical Industries Ltd. | Rosuvastatin and salts thereof free of rosuvastatin alkylether and a process for the preparation thereof |
| US20070037979A1 (en) * | 2005-02-22 | 2007-02-15 | Valerie Niddam-Hildesheim | Preparation of rosuvastatin |
| US20070167625A1 (en) * | 2005-02-22 | 2007-07-19 | Anna Balanov | Preparation of rosuvastatin |
| MX2007004427A (es) * | 2005-08-16 | 2007-06-14 | Teva Pharma | Intermedio de rosuvastatina cristalina. |
| US8383614B2 (en) * | 2008-01-31 | 2013-02-26 | The Trustees Of The University Of Pennsylvania | Hypercholestrolemia and tendinous injuries |
| US9427437B2 (en) | 2008-01-31 | 2016-08-30 | The Trustees Of The University Of Pennsylvania | Hypercholesterolemia and tendinous injuries |
| WO2009143776A1 (zh) | 2008-05-27 | 2009-12-03 | 常州制药厂有限公司 | 瑞舒伐他汀钙盐的制备方法及其中间体 |
| HRP20120700T1 (hr) | 2008-07-08 | 2012-09-30 | Gilead Sciences | SOLI SPOJEVA INHIBITORA HIV-a |
| AR092872A1 (es) | 2012-09-17 | 2015-05-06 | Madrigal Pharmaceuticals Inc | Metodo para sintetizar analogos de la hormona tiroidea y polimorfos de los mismos |
| US9132117B2 (en) | 2013-06-17 | 2015-09-15 | Kgk Synergize, Inc | Compositions and methods for glycemic control of subjects with impaired fasting glucose |
| US10600502B2 (en) | 2016-12-20 | 2020-03-24 | Astrazeneca Uk Ltd. | Systems and methods for dispensing a statin medication over the counter |
| ES2892402T3 (es) | 2017-08-01 | 2022-02-04 | Gilead Sciences Inc | Formas cristalinas de ((S)-((((2R,5R)-5-(6-amino-9H-purin-9-il)-4-fluoro-2,5-dihidrofuran-2-il)oxi)metil)(fenoxi)fosforil)-L-alaninato de etilo para tratar infecciones virales |
| PE20220164A1 (es) | 2019-05-27 | 2022-01-28 | Immatics Us Inc | Vectores viricos y uso de los mismos en terapias celulares adoptivas |
| DE102020111571A1 (de) | 2020-03-11 | 2021-09-16 | Immatics US, Inc. | Wpre-mutantenkonstrukte, zusammensetzungen und zugehörige verfahren |
| US20220008519A1 (en) | 2020-07-09 | 2022-01-13 | Costa Rican Social Security Fund / Caja Costarricense de Seguro Social (CCSS) | Treatment of severe acute respiratory syndrome-related coronavirus infection with klotho |
| WO2022040631A1 (en) | 2020-08-21 | 2022-02-24 | Immatics US, Inc. | Methods for isolating cd8+ selected t cells |
| JP2024506848A (ja) * | 2021-02-01 | 2024-02-15 | マドリガル ファーマシューティカルズ インコーポレイテッド | 肝障害又は脂質障害の治療のためのロスバスタチンとレスメチロムの治療的組み合わせ |
| US12377104B1 (en) | 2024-02-06 | 2025-08-05 | Madrigal Pharmaceuticals, Inc. | Methods for treating a fatty liver disease |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2051907C1 (ru) * | 1989-05-22 | 1996-01-10 | Сандос АГ | Способ получения 7-замещенной гептен-6-овой кислоты |
| JP2648897B2 (ja) * | 1991-07-01 | 1997-09-03 | 塩野義製薬株式会社 | ピリミジン誘導体 |
| US5631365A (en) * | 1993-09-21 | 1997-05-20 | Schering Corporation | Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents |
| US6369103B1 (en) * | 1994-01-18 | 2002-04-09 | Bristol-Myers Squibb Company | Method for preventing or reducing risk of onset of cardiovascular events employing an HMG CoA reductase inhibitor |
| GB0001621D0 (en) * | 2000-01-26 | 2000-03-15 | Astrazeneca Ab | Pharmaceutical compositions |
| AU6294501A (en) * | 2000-09-20 | 2002-04-02 | Rtp Pharma Inc | Spray drying process and compositions of fenofibrate |
-
2000
- 2000-11-22 GB GBGB0028429.9A patent/GB0028429D0/en not_active Ceased
-
2001
- 2001-11-16 CZ CZ20031406A patent/CZ301583B6/cs not_active IP Right Cessation
- 2001-11-16 JP JP2002544073A patent/JP5062940B2/ja not_active Expired - Lifetime
- 2001-11-16 NZ NZ525754A patent/NZ525754A/en not_active IP Right Cessation
- 2001-11-16 BR BR0115511-3A patent/BR0115511A/pt not_active Application Discontinuation
- 2001-11-16 PT PT01982623T patent/PT1339409E/pt unknown
- 2001-11-16 CA CA002429263A patent/CA2429263C/en not_active Expired - Fee Related
- 2001-11-16 MX MXPA03004336A patent/MXPA03004336A/es unknown
- 2001-11-16 EE EEP200300239A patent/EE05507B1/xx not_active IP Right Cessation
- 2001-11-16 PL PL01365386A patent/PL365386A1/xx not_active Application Discontinuation
- 2001-11-16 DK DK01982623T patent/DK1339409T3/da active
- 2001-11-16 SI SI200130839T patent/SI1339409T1/sl unknown
- 2001-11-16 AU AU2002214165A patent/AU2002214165B9/en not_active Revoked
- 2001-11-16 AT AT01982623T patent/ATE394103T1/de active
- 2001-11-16 EP EP01982623A patent/EP1339409B1/en not_active Revoked
- 2001-11-16 HU HU0301380A patent/HUP0301380A3/hu not_active Application Discontinuation
- 2001-11-16 IL IL15591901A patent/IL155919A0/xx unknown
- 2001-11-16 WO PCT/GB2001/005041 patent/WO2002041895A1/en not_active Ceased
- 2001-11-16 DE DE60133921T patent/DE60133921D1/de not_active Expired - Lifetime
- 2001-11-16 ES ES01982623T patent/ES2305118T3/es not_active Expired - Lifetime
- 2001-11-16 RU RU2003114300/15A patent/RU2294744C2/ru not_active IP Right Cessation
- 2001-11-16 UA UA2003054394A patent/UA75614C2/uk unknown
- 2001-11-16 KR KR1020037006791A patent/KR100815042B1/ko not_active Ceased
- 2001-11-16 SK SK621-2003A patent/SK6212003A3/sk not_active Application Discontinuation
- 2001-11-16 CN CNB018221599A patent/CN1268339C/zh not_active Expired - Lifetime
- 2001-11-16 AU AU1416502A patent/AU1416502A/xx active Pending
- 2001-11-16 US US10/432,402 patent/US6858618B2/en not_active Expired - Lifetime
- 2001-11-20 MY MYPI20015303A patent/MY134902A/en unknown
- 2001-11-21 TW TW090128858A patent/TWI238720B/zh not_active IP Right Cessation
- 2001-11-22 AR ARP010105452A patent/AR031766A1/es unknown
-
2003
- 2003-05-12 ZA ZA200303636A patent/ZA200303636B/en unknown
- 2003-05-13 BG BG107811A patent/BG66009B1/bg unknown
- 2003-05-14 IL IL155919A patent/IL155919A/en unknown
- 2003-05-19 IS IS6819A patent/IS6819A/is unknown
- 2003-05-21 NO NO20032292A patent/NO326245B1/no not_active IP Right Cessation
-
2008
- 2008-07-07 CY CY20081100703T patent/CY1110428T1/el unknown
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2009
- 2009-11-09 JP JP2009255813A patent/JP2010031047A/ja active Pending
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