AU2019384136B2 - Bis-octahydrophenanthrene carboxamide derivatives and protein conjugates thereof for use as LXR agonists - Google Patents
Bis-octahydrophenanthrene carboxamide derivatives and protein conjugates thereof for use as LXR agonists Download PDFInfo
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- AU2019384136B2 AU2019384136B2 AU2019384136A AU2019384136A AU2019384136B2 AU 2019384136 B2 AU2019384136 B2 AU 2019384136B2 AU 2019384136 A AU2019384136 A AU 2019384136A AU 2019384136 A AU2019384136 A AU 2019384136A AU 2019384136 B2 AU2019384136 B2 AU 2019384136B2
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- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08L—COMPOSITIONS OF MACROMOLECULAR COMPOUNDS
- C08L5/00—Compositions of polysaccharides or of their derivatives not provided for in groups C08L1/00 or C08L3/00
- C08L5/16—Cyclodextrin; Derivatives thereof
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
- C07C237/52—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the nitrogen atom of at least one of the carboxamide groups further acylated
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
- A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6835—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
- A61K47/6849—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a receptor, a cell surface antigen or a cell surface determinant
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6835—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
- A61K47/6883—Polymer-drug antibody conjugates, e.g. mitomycin-dextran-Ab; DNA-polylysine-antibody complex or conjugate used for therapy
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- A—HUMAN NECESSITIES
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- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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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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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D225/00—Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom
- C07D225/04—Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
- C07D225/08—Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems condensed with two six-membered rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/16—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
- C07H17/02—Heterocyclic radicals containing only nitrogen as ring hetero atoms
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- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08B—POLYSACCHARIDES; DERIVATIVES THEREOF
- C08B37/00—Preparation of polysaccharides not provided for in groups C08B1/00 - C08B35/00; Derivatives thereof
- C08B37/0006—Homoglycans, i.e. polysaccharides having a main chain consisting of one single sugar, e.g. colominic acid
- C08B37/0009—Homoglycans, i.e. polysaccharides having a main chain consisting of one single sugar, e.g. colominic acid alpha-D-Glucans, e.g. polydextrose, alternan, glycogen; (alpha-1,4)(alpha-1,6)-D-Glucans; (alpha-1,3)(alpha-1,4)-D-Glucans, e.g. isolichenan or nigeran; (alpha-1,4)-D-Glucans; (alpha-1,3)-D-Glucans, e.g. pseudonigeran; Derivatives thereof
- C08B37/0012—Cyclodextrin [CD], e.g. cycle with 6 units (alpha), with 7 units (beta) and with 8 units (gamma), large-ring cyclodextrin or cycloamylose with 9 units or more; Derivatives thereof
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2603/00—Systems containing at least three condensed rings
- C07C2603/02—Ortho- or ortho- and peri-condensed systems
- C07C2603/04—Ortho- or ortho- and peri-condensed systems containing three rings
- C07C2603/22—Ortho- or ortho- and peri-condensed systems containing three rings containing only six-membered rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2603/00—Systems containing at least three condensed rings
- C07C2603/02—Ortho- or ortho- and peri-condensed systems
- C07C2603/04—Ortho- or ortho- and peri-condensed systems containing three rings
- C07C2603/22—Ortho- or ortho- and peri-condensed systems containing three rings containing only six-membered rings
- C07C2603/26—Phenanthrenes; Hydrogenated phenanthrenes
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biotechnology (AREA)
- Biomedical Technology (AREA)
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- Diabetes (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Genetics & Genomics (AREA)
- Materials Engineering (AREA)
- Peptides Or Proteins (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862769946P | 2018-11-20 | 2018-11-20 | |
| US62/769,946 | 2018-11-20 | ||
| PCT/US2019/062302 WO2020106780A1 (en) | 2018-11-20 | 2019-11-19 | Bis-octahydrophenanthrene carboxamide derivatives and protein conjugates thereof for use as lxr agonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2019384136A1 AU2019384136A1 (en) | 2021-06-10 |
| AU2019384136B2 true AU2019384136B2 (en) | 2024-06-06 |
Family
ID=69005818
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2019384136A Active AU2019384136B2 (en) | 2018-11-20 | 2019-11-19 | Bis-octahydrophenanthrene carboxamide derivatives and protein conjugates thereof for use as LXR agonists |
Country Status (20)
| Country | Link |
|---|---|
| US (2) | US12209180B2 (https=) |
| EP (2) | EP4428142A3 (https=) |
| JP (2) | JP7702866B2 (https=) |
| KR (1) | KR20210094568A (https=) |
| CN (1) | CN113382985A (https=) |
| AU (1) | AU2019384136B2 (https=) |
| BR (1) | BR112021009673A2 (https=) |
| CA (1) | CA3120528A1 (https=) |
| CL (1) | CL2021001308A1 (https=) |
| CO (1) | CO2021007581A2 (https=) |
| EA (1) | EA202191430A1 (https=) |
| ES (1) | ES2984190T3 (https=) |
| IL (1) | IL283313B2 (https=) |
| MA (1) | MA53455B1 (https=) |
| MX (1) | MX2021005822A (https=) |
| MY (1) | MY206542A (https=) |
| PH (1) | PH12021551153A1 (https=) |
| SG (1) | SG11202105175WA (https=) |
| WO (1) | WO2020106780A1 (https=) |
| ZA (1) | ZA202103431B (https=) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20250114431A (ko) | 2016-11-08 | 2025-07-29 | 리제너론 파마슈티칼스 인코포레이티드 | 스테로이드 및 이의 단백질-접합체 |
| KR20250008984A (ko) | 2017-05-18 | 2025-01-16 | 리제너론 파마슈티칼스 인코포레이티드 | 사이클로덱스트린 단백질 약물 접합체 |
| CN112533951A (zh) | 2018-05-09 | 2021-03-19 | 里珍纳龙药品有限公司 | 抗msr1抗体及其使用方法 |
| MA53455B1 (fr) * | 2018-11-20 | 2022-11-30 | Regeneron Pharma | Dérivés de bis-octahydrophénanthrène carboxamide et leurs conjugués protéiques destinés à être utilisés en tant qu'agonistes de lxr |
| KR20240038138A (ko) * | 2020-07-13 | 2024-03-22 | 리제너론 파마슈티칼스 인코포레이티드 | 단백질에서 글루타민 잔기에 접합된 캄토테신 유사체 및 그의 용도 |
| CA3198294A1 (en) | 2020-11-10 | 2022-05-19 | Thomas Nittoli | Selenium antibody conjugates |
| US11806405B1 (en) | 2021-07-19 | 2023-11-07 | Zeno Management, Inc. | Immunoconjugates and methods |
| TW202320858A (zh) | 2021-07-19 | 2023-06-01 | 美商薩諾管理公司 | 免疫接合物及方法 |
| US20240408226A1 (en) * | 2021-11-02 | 2024-12-12 | Mabplex International Co., Ltd. | Antibody drug conjugate intermediate containing sn38 and its preparation method |
| CN115594766A (zh) * | 2021-12-30 | 2023-01-13 | 辽宁键凯科技有限公司(Cn) | 一种缀合物及用其制备的抗体偶联药物 |
| CN115505028A (zh) * | 2022-09-16 | 2022-12-23 | 辽宁键凯科技有限公司 | 一种分支型聚乙二醇连接子及其用途 |
Citations (1)
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|---|---|---|---|---|
| US20030125357A1 (en) * | 2001-06-11 | 2003-07-03 | Adams Alan D. | Therapeutic compounds for treating dyslipidemic conditions |
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| US5714586A (en) | 1995-06-07 | 1998-02-03 | American Cyanamid Company | Methods for the preparation of monomeric calicheamicin derivative/carrier conjugates |
| WO2001041704A2 (en) * | 1999-12-13 | 2001-06-14 | Merck & Co., Inc. | Method for the prevention and/or treatment of atherosclerosis |
| US20070258987A1 (en) | 2000-11-28 | 2007-11-08 | Seattle Genetics, Inc. | Recombinant Anti-Cd30 Antibodies and Uses Thereof |
| EP1398032A1 (en) | 2002-09-10 | 2004-03-17 | PheneX Pharmaceuticals AG | 4-Oxo-quinazolines as LXR nuclear receptor binding compounds |
| AR048098A1 (es) | 2004-03-15 | 2006-03-29 | Wyeth Corp | Conjugados de caliqueamicina |
| EP1758651A2 (en) | 2004-06-24 | 2007-03-07 | Galapagos N.V. | Lxr agonists to promote bone homeostasis |
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| KR20090094125A (ko) * | 2006-12-08 | 2009-09-03 | 엑셀리시스, 인코포레이티드 | Lxr 및 fxr 조절자 |
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| JP2010528285A (ja) | 2007-05-23 | 2010-08-19 | ベンタナ・メデイカル・システムズ・インコーポレーテツド | 免疫組織化学およびinsituハイブリダーゼーションのためのポリマー担体 |
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| KR20250114431A (ko) | 2016-11-08 | 2025-07-29 | 리제너론 파마슈티칼스 인코포레이티드 | 스테로이드 및 이의 단백질-접합체 |
| WO2018213082A1 (en) | 2017-05-18 | 2018-11-22 | Regeneron Pharmaceuticals, Inc. | Bis-octahydrophenanthrene carboxamides and protein conjugates thereof |
| CN112533951A (zh) | 2018-05-09 | 2021-03-19 | 里珍纳龙药品有限公司 | 抗msr1抗体及其使用方法 |
| MA53455B1 (fr) * | 2018-11-20 | 2022-11-30 | Regeneron Pharma | Dérivés de bis-octahydrophénanthrène carboxamide et leurs conjugués protéiques destinés à être utilisés en tant qu'agonistes de lxr |
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2019
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
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| US20030125357A1 (en) * | 2001-06-11 | 2003-07-03 | Adams Alan D. | Therapeutic compounds for treating dyslipidemic conditions |
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| BR112021009673A2 (pt) | 2021-12-14 |
| MA53455B1 (fr) | 2022-11-30 |
| WO2020106780A1 (en) | 2020-05-28 |
| JP2022507781A (ja) | 2022-01-18 |
| KR20210094568A (ko) | 2021-07-29 |
| CA3120528A1 (en) | 2020-05-28 |
| ZA202103431B (en) | 2024-09-25 |
| EP3883926B1 (en) | 2024-07-10 |
| ES2984190T3 (es) | 2024-10-29 |
| EP4428142A2 (en) | 2024-09-11 |
| IL283313B2 (en) | 2025-08-01 |
| CO2021007581A2 (es) | 2021-06-21 |
| AU2019384136A1 (en) | 2021-06-10 |
| MX2021005822A (es) | 2021-07-15 |
| IL283313B1 (en) | 2025-04-01 |
| JP2025138724A (ja) | 2025-09-25 |
| US20220080052A1 (en) | 2022-03-17 |
| IL283313A (en) | 2021-07-29 |
| JP7702866B2 (ja) | 2025-07-04 |
| EP3883926A1 (en) | 2021-09-29 |
| US12209180B2 (en) | 2025-01-28 |
| PH12021551153A1 (en) | 2021-11-03 |
| MA53455A1 (fr) | 2021-12-31 |
| CN113382985A (zh) | 2021-09-10 |
| EA202191430A1 (ru) | 2021-11-29 |
| SG11202105175WA (en) | 2021-06-29 |
| CL2021001308A1 (es) | 2022-03-11 |
| MY206542A (en) | 2024-12-20 |
| US20250171622A1 (en) | 2025-05-29 |
| EP4428142A3 (en) | 2024-11-20 |
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