RU2017136295A - Фиксированные комбинации и составы, содержащие етс1002 и один или более статинов, и способы лечения или уменьшения риска развития сердечно-сосудистого заболевания - Google Patents
Фиксированные комбинации и составы, содержащие етс1002 и один или более статинов, и способы лечения или уменьшения риска развития сердечно-сосудистого заболевания Download PDFInfo
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- statins
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- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 title claims 15
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 title claims 13
- 238000000034 method Methods 0.000 title claims 13
- 239000000203 mixture Substances 0.000 title claims 6
- 208000024172 Cardiovascular disease Diseases 0.000 title claims 4
- HYHMLYSLQUKXKP-UHFFFAOYSA-N bempedoic acid Chemical compound OC(=O)C(C)(C)CCCCCC(O)CCCCCC(C)(C)C(O)=O HYHMLYSLQUKXKP-UHFFFAOYSA-N 0.000 claims 15
- 229940068196 placebo Drugs 0.000 claims 6
- 239000000902 placebo Substances 0.000 claims 6
- FJLGEFLZQAZZCD-MCBHFWOFSA-N (3R,5S)-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-MCBHFWOFSA-N 0.000 claims 4
- 229960003765 fluvastatin Drugs 0.000 claims 4
- 102000005666 Apolipoprotein A-I Human genes 0.000 claims 3
- 108010059886 Apolipoprotein A-I Proteins 0.000 claims 3
- 101710095342 Apolipoprotein B Proteins 0.000 claims 3
- 102100040202 Apolipoprotein B-100 Human genes 0.000 claims 3
- 102000007330 LDL Lipoproteins Human genes 0.000 claims 3
- 108010007622 LDL Lipoproteins Proteins 0.000 claims 3
- PCZOHLXUXFIOCF-UHFFFAOYSA-N Monacolin X Natural products C12C(OC(=O)C(C)CC)CC(C)C=C2C=CC(C)C1CCC1CC(O)CC(=O)O1 PCZOHLXUXFIOCF-UHFFFAOYSA-N 0.000 claims 2
- TUZYXOIXSAXUGO-UHFFFAOYSA-N Pravastatin Natural products C1=CC(C)C(CCC(O)CC(O)CC(O)=O)C2C(OC(=O)C(C)CC)CC(O)C=C21 TUZYXOIXSAXUGO-UHFFFAOYSA-N 0.000 claims 2
- RYMZZMVNJRMUDD-UHFFFAOYSA-N SJ000286063 Natural products C12C(OC(=O)C(C)(C)CC)CC(C)C=C2C=CC(C)C1CCC1CC(O)CC(=O)O1 RYMZZMVNJRMUDD-UHFFFAOYSA-N 0.000 claims 2
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol 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 2
- 229960004844 lovastatin Drugs 0.000 claims 2
- 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 2
- QLJODMDSTUBWDW-UHFFFAOYSA-N lovastatin hydroxy acid Natural products C1=CC(C)C(CCC(O)CC(O)CC(O)=O)C2C(OC(=O)C(C)CC)CC(C)C=C21 QLJODMDSTUBWDW-UHFFFAOYSA-N 0.000 claims 2
- 229960002797 pitavastatin Drugs 0.000 claims 2
- 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 2
- 229960002965 pravastatin Drugs 0.000 claims 2
- 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 2
- 229960000672 rosuvastatin Drugs 0.000 claims 2
- 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 2
- 229960002855 simvastatin Drugs 0.000 claims 2
- 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 2
- 230000001225 therapeutic effect Effects 0.000 claims 2
- 101150102415 Apob gene Proteins 0.000 claims 1
- 108010023302 HDL Cholesterol Proteins 0.000 claims 1
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 1
- 235000012000 cholesterol Nutrition 0.000 claims 1
- 239000002245 particle Substances 0.000 claims 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/20—Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
-
- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/194—Carboxylic acids, e.g. valproic acid having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
- A61K31/225—Polycarboxylic acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/365—Lactones
- A61K31/366—Lactones having six-membered rings, e.g. delta-lactones
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
- A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
-
- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- 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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Claims (16)
1. Способ лечения сердечно-сосудистого заболевания или снижения риска развития сердечно-сосудистого заболевания у субъекта, включающий введение нуждающемуся в том субъекту фиксированной комбинации с фиксированной дозой ETC-1002 или ее аналога и фиксированной дозой одного или более статинов или его аналога, причем необязательно ETC-1002 вводят в фиксированной дозе 120 мг или в фиксированной дозе 180 мг, а каждый из одного более статинов вводят в фиксированной дозе от 2 до 80 мг, и причем необязательно способ приводит к излечению или снижению риска развития сердечно-сосудистого заболевания у субъекта.
2. Способ по п. 1, причем уровень общего холестерина и non-HDL-C у субъекта ниже, чем у контрольного субъекта, получающего плацебо, фиксированную дозу 120 мг ETC-1002, фиксированную дозу 180 мг ETC-1002 или фиксированную дозу 2-80 мг каждого из одного или более статинов.
3. Способ по п. 1, причем уровень липопротеинов низкой плотности (LDL) у субъекта ниже, чем у контрольного субъекта, получающего плацебо, фиксированную дозу 120 мг ETC-1002, фиксированную дозу 180 мг ETC-1002 или фиксированную дозу 2-80 мг каждого из одного или более статинов.
4. Способ по п. 1, причем количество частиц LDL у субъекта ниже, чем у контрольного субъекта, получающего плацебо, фиксированную дозу 120 мг ETC-1002, фиксированную дозу 180 мг ETC-1002 или фиксированную дозу 2-80 мг каждого из одного или более статинов.
5. Способ по п. 1, причем уровень аполипопротеина В (ароВ) у субъекта меньше, чем у контрольного субъекта, получающего плацебо, фиксированную дозу 120 мг ETC-1002, фиксированную дозу 180 мг ETC-1002 или фиксированную дозу 2-80 мг каждого из одного или более статинов.
6. Способ по п. 1, причем уровень аполипопротеина А-1 (ApoA1) у субъекта меньше, чем у контрольного субъекта, получающего плацебо, фиксированную дозу 120 мг ETC-1002, фиксированную дозу 180 мг ETC-1002 или фиксированную дозу 2-80 мг каждого из одного или более статинов.
7. Способ по п. 1, причем соотношение аполипопротеина В (АроВ) к аполипопротеину А-1 (ApoAl) у субъекта ниже, чем у контрольного субъекта, получающего плацебо, фиксированную дозу 120 мг ETC-1002, фиксированную дозу 180 мг ETC-1002 или фиксированную дозу 2-80 мг каждого из одного или более статинов.
8. Способ по п. 1, причем один или более статинов выбраны из группы, состоящей из розувастатина, симвастатина, правастатина, ловастатина, флувастатина, флувастатина и питавастатина.
9. Способ по п. 1, причем у субъекта есть гиперхолестеринемия.
10. Способ по п. 1, причем субъектом является животное.
11. Способ по п. 1, причем субъектом является человек.
12. Терапевтическая композиция, содержащая терапевтическое количество фиксированной дозы ETC-1002 и фиксированной дозы каждого из одного или более статинов.
13. Композиция по п. 12, причем доза составляет от 2 до 80 мг одного статина.
14. Композиция по п. 12, причем количество представляет собой дозу 120 или 180 мг ETC-1002 и фиксированную дозу 2-80 мг каждого из одного или более статинов.
15. Композиция по п. 12, причем доза составляет от 40 до 80 мг одного статина.
16. Композиция по п. 12, причем один или более статинов выбраны из группы, состоящей из розувастатина, симвастатина, правастатина, ловастатина, флувастатина, флувастатина и питавастатина.
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201562133739P | 2015-03-16 | 2015-03-16 | |
US62/133,739 | 2015-03-16 | ||
US201662277403P | 2016-01-11 | 2016-01-11 | |
US62/277,403 | 2016-01-11 | ||
PCT/US2016/022694 WO2016149405A1 (en) | 2015-03-16 | 2016-03-16 | Fixed dose combinations comprising etc1002 and one or more statins for treating or reducing cardiovascular risk |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
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RU2022101523A Division RU2022101523A (ru) | 2015-03-16 | 2016-03-16 | Фиксированные комбинации и составы, содержащие etc-1002 и один или более статинов, и способы лечения или уменьшения риска развития сердечно-сосудистого заболевания |
Publications (3)
Publication Number | Publication Date |
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RU2017136295A true RU2017136295A (ru) | 2019-04-16 |
RU2017136295A3 RU2017136295A3 (ru) | 2019-07-17 |
RU2765218C2 RU2765218C2 (ru) | 2022-01-26 |
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RU2017136295A RU2765218C2 (ru) | 2015-03-16 | 2016-03-16 | Фиксированные комбинации и составы, содержащие етс1002 и один или более статинов, и способы лечения или уменьшения риска развития сердечно-сосудистого заболевания |
Country Status (24)
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US (3) | US11116739B2 (ru) |
EP (2) | EP4327887A3 (ru) |
JP (3) | JP7296190B2 (ru) |
CN (3) | CN116832164A (ru) |
AU (2) | AU2016233257B2 (ru) |
BR (1) | BR112017019728A2 (ru) |
CA (1) | CA2978180A1 (ru) |
CL (1) | CL2017002334A1 (ru) |
DK (1) | DK3270909T3 (ru) |
FI (1) | FI3270909T3 (ru) |
HK (1) | HK1245643A1 (ru) |
HR (1) | HRP20240098T1 (ru) |
IL (2) | IL292829A (ru) |
LT (1) | LT3270909T (ru) |
MA (1) | MA41793A (ru) |
MX (2) | MX2017011500A (ru) |
PH (1) | PH12017501659A1 (ru) |
PT (1) | PT3270909T (ru) |
RU (1) | RU2765218C2 (ru) |
SG (2) | SG11201707579RA (ru) |
SI (1) | SI3270909T1 (ru) |
UA (1) | UA125371C2 (ru) |
WO (1) | WO2016149405A1 (ru) |
ZA (1) | ZA201706945B (ru) |
Families Citing this family (9)
Publication number | Priority date | Publication date | Assignee | Title |
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EP3267989A4 (en) | 2015-03-13 | 2018-11-07 | Esperion Therapeutics, Inc. | Fixed dose combinations and formulations comprising etc1002 and ezetimibe and methods of treating or reducing the risk of cardiovascular disease |
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 |
CN110536684A (zh) * | 2017-02-08 | 2019-12-03 | 艾斯柏伦治疗公司 | 三联组合制剂以及治疗心血管疾病或降低心血管疾病风险的方法 |
BR112020016494A2 (pt) * | 2018-02-16 | 2020-12-15 | Esperion Therapeutics, Inc. | Formulações de liberação prolongada de ácido bempedoico |
WO2019179494A1 (zh) * | 2018-03-23 | 2019-09-26 | 深圳市塔吉瑞生物医药有限公司 | 取代的十五烷二酸化合物及药物组合物及其用途 |
WO2020041799A1 (en) * | 2018-08-24 | 2020-02-27 | Esperion Therapeutics, Inc. | Methods for reducing the risk of diabetes in patients being treated for high cholesterol-related illnesses |
US20210322375A1 (en) * | 2018-08-27 | 2021-10-21 | Esperion Therapeutics, Inc. | Combination drug formulations for treating patients with cardiovascular disease and associated conditions |
JP2022536979A (ja) | 2019-06-21 | 2022-08-22 | エスペリオン・セラピューティクス・インコーポレイテッド | 塩形態のベンペド酸及びそれを使用する方法 |
CN113134086A (zh) * | 2020-01-20 | 2021-07-20 | 深圳市长卿医学研究院 | 一种降血脂的药物组合物 |
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