JP2015503588A5 - - Google Patents
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- JP2015503588A5 JP2015503588A5 JP2014551345A JP2014551345A JP2015503588A5 JP 2015503588 A5 JP2015503588 A5 JP 2015503588A5 JP 2014551345 A JP2014551345 A JP 2014551345A JP 2014551345 A JP2014551345 A JP 2014551345A JP 2015503588 A5 JP2015503588 A5 JP 2015503588A5
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- Prior art keywords
- pharmaceutical composition
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- compound
- heart disease
- Prior art date
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- 239000008194 pharmaceutical composition Substances 0.000 claims 17
- 150000001875 compounds Chemical class 0.000 claims 8
- 208000004981 Coronary Disease Diseases 0.000 claims 6
- 201000008739 coronary artery disease Diseases 0.000 claims 6
- HVYWMOMLDIMFJA-DPAQBDIFSA-N (3β)-Cholest-5-en-3-ol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims 4
- 239000003112 inhibitor Substances 0.000 claims 4
- 230000002401 inhibitory effect Effects 0.000 claims 4
- 230000000271 cardiovascular Effects 0.000 claims 3
- 229940107161 Cholesterol Drugs 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 150000002148 esters Chemical class 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000011780 sodium chloride Substances 0.000 claims 2
- FJLGEFLZQAZZCD-JUFISIKESA-N (3S,5R)-fluvastatin Chemical compound C12=CC=CC=C2N(C(C)C)C(\C=C\[C@H](O)C[C@H](O)CC(O)=O)=C1C1=CC=C(F)C=C1 FJLGEFLZQAZZCD-JUFISIKESA-N 0.000 claims 1
- 101700065507 APOB Proteins 0.000 claims 1
- 210000004369 Blood Anatomy 0.000 claims 1
- 229920001268 Cholestyramine Polymers 0.000 claims 1
- 206010012601 Diabetes mellitus Diseases 0.000 claims 1
- OLNTVTPDXPETLC-XPWALMASSA-N Ezetimibe Chemical compound N1([C@@H]([C@H](C1=O)CC[C@H](O)C=1C=CC(F)=CC=1)C=1C=CC(O)=CC=1)C1=CC=C(F)C=C1 OLNTVTPDXPETLC-XPWALMASSA-N 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- PCZOHLXUXFIOCF-BXMDZJJMSA-N Lovastatin Chemical compound C([C@H]1[C@@H](C)C=CC2=C[C@H](C)C[C@@H]([C@H]12)OC(=O)[C@@H](C)CC)C[C@@H]1C[C@@H](O)CC(=O)O1 PCZOHLXUXFIOCF-BXMDZJJMSA-N 0.000 claims 1
- 102100019305 MTTP Human genes 0.000 claims 1
- 102100005352 PCSK9 Human genes 0.000 claims 1
- 101700000651 PCSK9 Proteins 0.000 claims 1
- VGYFMXBACGZSIL-MCBHFWOFSA-N Pitavastatin Chemical compound OC(=O)C[C@H](O)C[C@H](O)\C=C\C1=C(C2CC2)N=C2C=CC=CC2=C1C1=CC=C(F)C=C1 VGYFMXBACGZSIL-MCBHFWOFSA-N 0.000 claims 1
- 229960002965 Pravastatin Drugs 0.000 claims 1
- TUZYXOIXSAXUGO-PZAWKZKUSA-N Pravastatin Chemical compound C1=C[C@H](C)[C@H](CC[C@@H](O)C[C@@H](O)CC(O)=O)[C@H]2[C@@H](OC(=O)[C@@H](C)CC)C[C@H](O)C=C21 TUZYXOIXSAXUGO-PZAWKZKUSA-N 0.000 claims 1
- BPRHUIZQVSMCRT-VEUZHWNKSA-N Rosuvastatin Chemical compound CC(C)C1=NC(N(C)S(C)(=O)=O)=NC(C=2C=CC(F)=CC=2)=C1\C=C\[C@@H](O)C[C@@H](O)CC(O)=O BPRHUIZQVSMCRT-VEUZHWNKSA-N 0.000 claims 1
- RYMZZMVNJRMUDD-HGQWONQESA-N Simvastatin Chemical compound C([C@H]1[C@@H](C)C=CC2=C[C@H](C)C[C@@H]([C@H]12)OC(=O)C(C)(C)CC)C[C@@H]1C[C@@H](O)CC(=O)O1 RYMZZMVNJRMUDD-HGQWONQESA-N 0.000 claims 1
- HGMSJMJPXGGEBP-UHFFFAOYSA-N [4-[3-(4-ethylphenyl)butyl]phenyl]-trimethylazanium Chemical compound C1=CC(CC)=CC=C1C(C)CCC1=CC=C([N+](C)(C)C)C=C1 HGMSJMJPXGGEBP-UHFFFAOYSA-N 0.000 claims 1
- 230000003276 anti-hypertensive Effects 0.000 claims 1
- 239000003529 anticholesteremic agent Substances 0.000 claims 1
- 229960005370 atorvastatin Drugs 0.000 claims 1
- XUKUURHRXDUEBC-KAYWLYCHSA-N atorvastatin Chemical compound C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CC[C@@H](O)C[C@@H](O)CC(O)=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 XUKUURHRXDUEBC-KAYWLYCHSA-N 0.000 claims 1
- 239000003613 bile acid Substances 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- OYPRJOBELJOOCE-UHFFFAOYSA-N calcium Chemical class [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims 1
- 159000000007 calcium salts Chemical class 0.000 claims 1
- 230000001906 cholesterol absorption Effects 0.000 claims 1
- 239000003354 cholesterol ester transfer protein inhibitor Substances 0.000 claims 1
- 229940079593 drugs Drugs 0.000 claims 1
- 229960000815 ezetimibe Drugs 0.000 claims 1
- 229960003765 fluvastatin Drugs 0.000 claims 1
- 230000036571 hydration Effects 0.000 claims 1
- 238000006703 hydration reaction Methods 0.000 claims 1
- 229960004844 lovastatin Drugs 0.000 claims 1
- 108010038232 microsomal triglyceride transfer protein Proteins 0.000 claims 1
- 229960002797 pitavastatin Drugs 0.000 claims 1
- 230000002028 premature Effects 0.000 claims 1
- 239000012268 protein inhibitor Substances 0.000 claims 1
- 229940121649 protein inhibitors Drugs 0.000 claims 1
- 239000002516 radical scavenger Substances 0.000 claims 1
- 230000000306 recurrent Effects 0.000 claims 1
- 229960000672 rosuvastatin Drugs 0.000 claims 1
- 229960002855 simvastatin Drugs 0.000 claims 1
- 230000000391 smoking Effects 0.000 claims 1
- 239000004059 squalene synthase inhibitor Substances 0.000 claims 1
- 238000003786 synthesis reaction Methods 0.000 claims 1
- 230000002194 synthesizing Effects 0.000 claims 1
- 230000001225 therapeutic Effects 0.000 claims 1
- 150000003626 triacylglycerols Chemical class 0.000 claims 1
Claims (16)
- 前記患者は治療目標より高いLDL−Cレベルを有する、請求項1または2に記載の医薬組成物。
- 前記患者は、冠動脈心疾患を有し、または冠動脈性心臓病と同等のリスクを有し、または以前に一次的心血管イベントもしくは脳血管イベントを有したことがある、請求項1または2に記載の医薬組成物。
- 前記患者は、喫煙、高血圧、降圧薬物療法による治療、40mg/dL未満のHDLコレステロールレベル、早発性冠動脈心疾患の家族歴、45歳以上の男性、および55歳以上の女性からなる群より選ばれる1つ以上の危険因子を有する、請求項1または2に記載の医薬組成物。
- 前記患者は、冠動脈心疾患の10年間リスクが10%以上である、請求項1または2に記載の医薬組成物。
- 前記患者は、冠動脈心疾患の10年間リスクが20%以上である、請求項1または2に記載の医薬組成物。
- 前記患者のフラミンガムリスクスコアが1点以上減少する、請求項1または2に記載の医薬組成物。
- 前記患者は糖尿病を有する、請求項1または2に記載の医薬組成物。
- 前記患者のHDLコレステロールレベルは40mg/dL未満であり、血中トリグリセリドレベルは150mg/dL以上である、請求項1または2に記載の医薬組成物。
- 前記患者は、コレステロール吸収阻害剤、胆汁酸捕捉剤、コレステリルエステル転送タンパク質阻害剤、ミクロソームトリグリセリド転送タンパク質阻害剤、PCSK9阻害剤、マイクロRNA−33阻害剤、スクアレン合成酵素阻害剤、およびapoB合成阻害剤から独立して選ばれる1つ以上の追加のコレステロール低下薬を投与される、請求項1または2に記載の医薬組成物。
- 前記追加のコレステロール低下薬はエゼチミブ、コレスチラミン(cholestryamine)、またはバイトリンである、請求項11に記載の医薬組成物。
- 前記スタチンはアトルバスタチン、ロバスタチン、シンバスタチン、プラバスタチン、ロスバスタチン、フルバスタチン、またはピタバスタチンである、請求項1、2または12に記載の医薬組成物。
- 前記化合物は式(I)の化合物である、請求項1、2または12に記載の医薬組成物。
- 前記化合物は式(I)の化合物のカルシウム塩である、請求項1、2または12に記載の医薬組成物。
- 前記化合物は式(I)の化合物の一カルシウム塩である、請求項15に記載の医薬組成物。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201261584002P | 2012-01-06 | 2012-01-06 | |
US61/584,002 | 2012-01-06 | ||
PCT/US2013/020317 WO2013103842A1 (en) | 2012-01-06 | 2013-01-04 | Methods of reducing risk of cardiovascular disease |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2018026939A Division JP2018104452A (ja) | 2012-01-06 | 2018-02-19 | 心血管疾患のリスクを低減する方法 |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2015503588A JP2015503588A (ja) | 2015-02-02 |
JP2015503588A5 true JP2015503588A5 (ja) | 2016-02-18 |
JP6295205B2 JP6295205B2 (ja) | 2018-03-14 |
Family
ID=48745439
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2014551345A Active JP6295205B2 (ja) | 2012-01-06 | 2013-01-04 | 心血管疾患のリスクを低減する方法 |
JP2018026939A Pending JP2018104452A (ja) | 2012-01-06 | 2018-02-19 | 心血管疾患のリスクを低減する方法 |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2018026939A Pending JP2018104452A (ja) | 2012-01-06 | 2018-02-19 | 心血管疾患のリスクを低減する方法 |
Country Status (9)
Country | Link |
---|---|
US (2) | US10028926B2 (ja) |
EP (2) | EP2800564B1 (ja) |
JP (2) | JP6295205B2 (ja) |
CN (2) | CN110025608A (ja) |
AU (1) | AU2013207423B2 (ja) |
CA (1) | CA2861643C (ja) |
HK (1) | HK1201452A1 (ja) |
MX (1) | MX367352B (ja) |
WO (1) | WO2013103842A1 (ja) |
Families Citing this family (27)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2012019168A2 (en) | 2010-08-06 | 2012-02-09 | Moderna Therapeutics, Inc. | Engineered nucleic acids and methods of use thereof |
EP2622064B1 (en) | 2010-10-01 | 2019-05-29 | Modernatx, Inc. | Modified nucleosides, nucleotides, and nucleic acids, and uses thereof |
US8710200B2 (en) | 2011-03-31 | 2014-04-29 | Moderna Therapeutics, Inc. | Engineered nucleic acids encoding a modified erythropoietin and their expression |
US9464124B2 (en) | 2011-09-12 | 2016-10-11 | Moderna Therapeutics, Inc. | Engineered nucleic acids and methods of use thereof |
HRP20220250T1 (hr) | 2011-10-03 | 2022-04-29 | Modernatx, Inc. | Modificirani nukleozidi, nukleotidi i nukleinske kiseline, te njihove uporabe |
EP2791160B1 (en) | 2011-12-16 | 2022-03-02 | ModernaTX, Inc. | Modified mrna compositions |
US9440754B2 (en) | 2012-03-29 | 2016-09-13 | R.P. Scherer Technologies, Llc | Three circuit fill system for blow fill seal containers |
US9572897B2 (en) | 2012-04-02 | 2017-02-21 | Modernatx, Inc. | Modified polynucleotides for the production of cytoplasmic and cytoskeletal proteins |
EP2834259A4 (en) | 2012-04-02 | 2016-08-24 | Moderna Therapeutics Inc | MODIFIED POLYNUCLEOTIDES |
US9878056B2 (en) | 2012-04-02 | 2018-01-30 | Modernatx, Inc. | Modified polynucleotides for the production of cosmetic proteins and peptides |
US9283287B2 (en) | 2012-04-02 | 2016-03-15 | Moderna Therapeutics, Inc. | Modified polynucleotides for the production of nuclear proteins |
US9255154B2 (en) | 2012-05-08 | 2016-02-09 | Alderbio Holdings, Llc | Anti-PCSK9 antibodies and use thereof |
ES2921623T3 (es) | 2012-11-26 | 2022-08-30 | Modernatx Inc | ARN modificado terminalmente |
US8980864B2 (en) | 2013-03-15 | 2015-03-17 | Moderna Therapeutics, Inc. | Compositions and methods of altering cholesterol levels |
AU2014255381A1 (en) | 2013-04-17 | 2015-10-08 | Pfizer Inc. | N-piperidin-3-ylbenzamide derivatives for treating cardiovascular diseases |
EP3052521A1 (en) | 2013-10-03 | 2016-08-10 | Moderna Therapeutics, Inc. | Polynucleotides encoding low density lipoprotein receptor |
SG10201912713YA (en) | 2014-11-14 | 2020-02-27 | Gemphire Therapeutics Inc | PROCESSES AND INTERMEDIATES FOR PREPARING α,ω-DICARBOXYLIC ACID-TERMINATED DIALKANE ETHERS |
UA123355C2 (uk) | 2015-03-13 | 2021-03-24 | Есперіон Терапеутікс, Інк. | Фіксовані комбінації й склади, які містять etc-1002 й езетиміб, і способи лікування або зменшення ризику розвитку серцево-судинного захворювання |
MA41793A (fr) * | 2015-03-16 | 2018-01-23 | Esperion Therapeutics Inc | Associations de doses fixes comprenant du etc1002 et une ou plusieurs statines permettant de traiter ou de réduire un risque cardiovasculaire |
CA3000016A1 (en) * | 2015-11-06 | 2017-05-11 | Gemphire Therapeutics Inc. | Gemcabene combinations for the treatment of cardiovascular disease |
AU2017224230A1 (en) * | 2016-02-26 | 2018-08-30 | Gemphire Therapeutics Inc. | Treatment of patients with homozygous familial hypercholesterolemia on lipid lowering therapy |
MX2019009418A (es) * | 2017-02-08 | 2019-10-02 | Esperion Therapeutics Inc | Formulaciones de combinacion del triplete y metodos para tratar o reducir el riesgo de enfermedad cardiovascular. |
EP3612171A4 (en) * | 2017-04-18 | 2020-10-21 | Gemphire Therapeutics Inc. | GEMCABED, PHARMACEUTICAL SALT THEREOF, COMPOSITIONS THEREOF, AND METHOD OF USE THEREOF |
WO2018209257A1 (en) * | 2017-05-11 | 2018-11-15 | Gemphire Therapeutics Inc. | Gemcabene compositions and methods of use thereof |
CN109666727B (zh) * | 2018-12-29 | 2020-11-06 | 中国药科大学 | 一种高活性抑制pcsk9表达的微小rna的用途 |
BR112021025964A2 (pt) | 2019-06-21 | 2022-05-24 | Esperion Therapeutics Inc | Formas de sal de ácido bempedoico e métodos para uso das mesmas |
CN113134086B (zh) * | 2020-01-20 | 2024-05-24 | 深圳市长卿医学研究院 | 一种降血脂的药物组合物 |
Family Cites Families (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5648387A (en) * | 1995-03-24 | 1997-07-15 | Warner-Lambert Company | Carboxyalkylethers, formulations, and treatment of vascular diseases |
US6861555B2 (en) | 2000-01-25 | 2005-03-01 | Warner-Lambert Company | Calcium dicarboxylate ethers, methods of making same, and treatment of vascular disease and diabetes therewith |
NZ503982A (en) | 1997-12-12 | 2002-03-28 | Warner Lambert Co | Statin-carboxyalkylether combinations useful for treating vascular disorders and diabetes mellitus |
US20020103252A1 (en) | 1997-12-12 | 2002-08-01 | Bisgaier Charles Larry | Statin-carboxyalkylether combinations |
CN1329359C (zh) | 1999-04-01 | 2007-08-01 | 埃斯佩里安医疗公司 | 醚化合物,及其组合物和用途 |
CA2425121A1 (en) | 2000-10-11 | 2002-04-18 | Esperion Therapeutics, Inc. | Ether compounds and compositions for cholesterol management and related uses |
US6645170B2 (en) | 2001-03-05 | 2003-11-11 | Bioject Medical Technologies, Inc. | Simplified disposable needle-free injection apparatus and method |
US20040229954A1 (en) * | 2003-05-16 | 2004-11-18 | Macdougall Diane Elaine | Selective manipulation of triglyceride, HDL and LDL parameters with 6-(5-carboxy-5-methyl-hexyloxy)-2,2-dimethylhexanoic acid monocalcium salt |
US7345190B2 (en) | 2003-11-12 | 2008-03-18 | Ssv Therapeutics, Inc. | Carnitine conjugates as dual prodrugs and uses thereof |
US7579504B2 (en) | 2005-12-07 | 2009-08-25 | Gilead Sciences, Inc. | ABCA1 elevating compounds |
BRPI0714793A2 (pt) * | 2006-08-03 | 2015-06-16 | Tufts College | Análogos de niacina não enrubecedores e método de uso dos mesmos. |
-
2013
- 2013-01-04 CN CN201910123564.7A patent/CN110025608A/zh active Pending
- 2013-01-04 US US14/370,722 patent/US10028926B2/en not_active Expired - Fee Related
- 2013-01-04 CA CA2861643A patent/CA2861643C/en active Active
- 2013-01-04 AU AU2013207423A patent/AU2013207423B2/en not_active Ceased
- 2013-01-04 MX MX2014008180A patent/MX367352B/es active IP Right Grant
- 2013-01-04 EP EP13733913.1A patent/EP2800564B1/en active Active
- 2013-01-04 CN CN201380004642.2A patent/CN104136023A/zh active Pending
- 2013-01-04 WO PCT/US2013/020317 patent/WO2013103842A1/en active Application Filing
- 2013-01-04 EP EP20166700.3A patent/EP3735967A1/en not_active Withdrawn
- 2013-01-04 JP JP2014551345A patent/JP6295205B2/ja active Active
-
2015
- 2015-02-27 HK HK15101958.1A patent/HK1201452A1/xx unknown
-
2018
- 2018-02-19 JP JP2018026939A patent/JP2018104452A/ja active Pending
- 2018-06-29 US US16/024,288 patent/US10709678B2/en active Active
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