JP2020535142A5 - - Google Patents
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- Publication number
- JP2020535142A5 JP2020535142A5 JP2020516839A JP2020516839A JP2020535142A5 JP 2020535142 A5 JP2020535142 A5 JP 2020535142A5 JP 2020516839 A JP2020516839 A JP 2020516839A JP 2020516839 A JP2020516839 A JP 2020516839A JP 2020535142 A5 JP2020535142 A5 JP 2020535142A5
- Authority
- JP
- Japan
- Prior art keywords
- use according
- inhibitor
- cholesterol
- akr1a1
- aryl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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- 239000003112 inhibitor Substances 0.000 claims 14
- 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 11
- 102100026448 Aldo-keto reductase family 1 member A1 Human genes 0.000 claims 9
- 101000718007 Homo sapiens Aldo-keto reductase family 1 member A1 Proteins 0.000 claims 9
- 102100027265 Aldo-keto reductase family 1 member B1 Human genes 0.000 claims 7
- 101000836540 Homo sapiens Aldo-keto reductase family 1 member B1 Proteins 0.000 claims 7
- 238000008214 LDL Cholesterol Methods 0.000 claims 5
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 4
- 235000012000 cholesterol Nutrition 0.000 claims 4
- 210000002966 serum Anatomy 0.000 claims 4
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 claims 4
- 108010027006 Apolipoproteins B Proteins 0.000 claims 3
- 102000018616 Apolipoproteins B Human genes 0.000 claims 3
- 108010069201 VLDL Cholesterol Proteins 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- -1 carboxy, carboxylato, carbamoyl Chemical group 0.000 claims 3
- QCCHBHSAIQIQGO-UHFFFAOYSA-N 2,7-difluorospiro[fluorene-9,5'-imidazolidine]-2',4'-dione Chemical compound C12=CC(F)=CC=C2C2=CC=C(F)C=C2C21NC(=O)NC2=O QCCHBHSAIQIQGO-UHFFFAOYSA-N 0.000 claims 2
- 208000032928 Dyslipidaemia Diseases 0.000 claims 2
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 2
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 2
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims 2
- 125000004104 aryloxy group Chemical group 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 208000029078 coronary artery disease Diseases 0.000 claims 2
- 210000004185 liver Anatomy 0.000 claims 2
- 150000003904 phospholipids Chemical class 0.000 claims 2
- 125000006413 ring segment Chemical group 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- 208000004476 Acute Coronary Syndrome Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 206010014476 Elevated cholesterol Diseases 0.000 claims 1
- 208000004930 Fatty Liver Diseases 0.000 claims 1
- 206010019708 Hepatic steatosis Diseases 0.000 claims 1
- 101001098868 Homo sapiens Proprotein convertase subtilisin/kexin type 9 Proteins 0.000 claims 1
- 108010028554 LDL Cholesterol Proteins 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 208000018262 Peripheral vascular disease Diseases 0.000 claims 1
- 102100038955 Proprotein convertase subtilisin/kexin type 9 Human genes 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 125000004423 acyloxy group Chemical group 0.000 claims 1
- 230000001476 alcoholic effect Effects 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000003302 alkenyloxy group Chemical group 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 125000005115 alkyl carbamoyl group Chemical group 0.000 claims 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000005277 alkyl imino group Chemical group 0.000 claims 1
- 125000004644 alkyl sulfinyl group Chemical group 0.000 claims 1
- 125000004414 alkyl thio group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- 125000001769 aryl amino group Chemical group 0.000 claims 1
- 125000005116 aryl carbamoyl group Chemical group 0.000 claims 1
- 125000004467 aryl imino group Chemical group 0.000 claims 1
- 125000005161 aryl oxy carbonyl group Chemical group 0.000 claims 1
- 125000005163 aryl sulfanyl group Chemical group 0.000 claims 1
- 125000005135 aryl sulfinyl group Chemical group 0.000 claims 1
- 239000004202 carbamide Substances 0.000 claims 1
- 235000013877 carbamide Nutrition 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 208000010706 fatty liver disease Diseases 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 208000006454 hepatitis Diseases 0.000 claims 1
- 231100000283 hepatitis Toxicity 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 125000004366 heterocycloalkenyl group Chemical group 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 125000001841 imino group Chemical group [H]N=* 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 231100000240 steatosis hepatitis Toxicity 0.000 claims 1
- 125000000020 sulfo group Chemical group O=S(=O)([*])O[H] 0.000 claims 1
- 229940124530 sulfonamide Drugs 0.000 claims 1
- 150000003456 sulfonamides Chemical class 0.000 claims 1
- 125000001273 sulfonato group Chemical group [O-]S(*)(=O)=O 0.000 claims 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 1
- 125000003396 thiol group Chemical group [H]S* 0.000 claims 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2023173195A JP2024001162A (ja) | 2017-09-25 | 2023-10-04 | 血清コレステロールおよびｐｃｓｋ９を低減する組成物および方法 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762562784P | 2017-09-25 | 2017-09-25 | |
| US62/562,784 | 2017-09-25 | ||
| PCT/US2018/052214 WO2019060720A1 (en) | 2017-09-25 | 2018-09-21 | COMPOSITIONS AND METHODS FOR REDUCING SERUM CHOLESTEROL AND PCSK9 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023173195A Division JP2024001162A (ja) | 2017-09-25 | 2023-10-04 | 血清コレステロールおよびｐｃｓｋ９を低減する組成物および方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020535142A JP2020535142A (ja) | 2020-12-03 |
| JP2020535142A5 true JP2020535142A5 (enExample) | 2021-11-04 |
| JP7414712B2 JP7414712B2 (ja) | 2024-01-16 |
Family
ID=65810650
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020516839A Active JP7414712B2 (ja) | 2017-09-25 | 2018-09-21 | 血清コレステロールおよびｐｃｓｋ９を低減する組成物および方法 |
| JP2023173195A Pending JP2024001162A (ja) | 2017-09-25 | 2023-10-04 | 血清コレステロールおよびｐｃｓｋ９を低減する組成物および方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023173195A Pending JP2024001162A (ja) | 2017-09-25 | 2023-10-04 | 血清コレステロールおよびｐｃｓｋ９を低減する組成物および方法 |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US11576900B2 (enExample) |
| EP (1) | EP3688163A4 (enExample) |
| JP (2) | JP7414712B2 (enExample) |
| CN (2) | CN111356764B (enExample) |
| CA (1) | CA3076889A1 (enExample) |
| WO (1) | WO2019060720A1 (enExample) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA3076889A1 (en) * | 2017-09-25 | 2019-03-28 | Case Western Reserve University | Compositions and methods of reducing serum cholesterol and pcsk9 |
| CA3113790A1 (en) * | 2018-09-21 | 2020-03-26 | Case Western Reserve University | Aldoketo reductase inhibitors and uses thereof |
| CN113648427B (zh) * | 2021-08-20 | 2023-07-28 | 山东大学 | 透明质酸-es2-af肽偶联物及其制备方法和应用 |
| CN117427170A (zh) * | 2023-11-15 | 2024-01-23 | 首都医科大学附属北京安贞医院 | Krt18蛋白在制备降低胆固醇的药物中的用途 |
Family Cites Families (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2683718A (en) | 1952-01-11 | 1954-07-13 | Searle & Co | Spiro-[xanthene-9, 4'-imidazolidine]-2, 5-dione |
| JPS58140020A (ja) * | 1982-02-13 | 1983-08-19 | Nippon Zoki Pharmaceut Co Ltd | 脂質代謝改善剤 |
| US4436745A (en) | 1982-04-15 | 1984-03-13 | Alcon Laboratories, Inc. | Method of inhibiting aldose reductase activity |
| US5153211A (en) * | 1983-09-14 | 1992-10-06 | Alcon Laboratories, Inc. | Spiro-tricyclicaromatic succinimide derivatives as inhibitors of aldose reductase |
| CA2430415A1 (en) | 2000-12-15 | 2002-06-20 | Galileo Laboratories, Inc. | Use of tocopherol, metabolites or derivatives thereof or flavonoid metabolites or derivatives thereof in the manufacture of a medicament for the treatment of tissue ischemia |
| WO2002098510A1 (en) * | 2001-06-07 | 2002-12-12 | Wyeth | Combination of a ptpase inhibitor and an aldose reductase inhibitor |
| EP1431399A1 (en) | 2002-12-20 | 2004-06-23 | Clinigenetics | Methods and composition for identifying therapeutic agents of atherosclerotic plaque lesions |
| JP4544503B2 (ja) | 2003-04-15 | 2010-09-15 | 株式会社アミノアップ化学 | 雲南苦丁茶成分を含有する組成物 |
| US20050014697A1 (en) | 2003-06-04 | 2005-01-20 | Stamler Jonathan S. | Compositions and methods for modulating S-nitrosoglutathione reductase |
| JP2007015924A (ja) | 2003-06-12 | 2007-01-25 | Sanwa Kagaku Kenkyusho Co Ltd | 抗癌剤耐性を克服する薬剤及びそのスクリーニング方法 |
| US20100292178A1 (en) | 2003-07-21 | 2010-11-18 | Jeffrey Young | Method of treating non-insulin dependent diabetes mellitus and related complications |
| US9308206B2 (en) | 2004-08-23 | 2016-04-12 | The Board Of Regents Of The University Of Texas System | Compositions and methods for treating colon cancer |
| US20110092566A1 (en) | 2004-11-19 | 2011-04-21 | Srivastava Satish K | Treatment of cancer with aldose reductase inhibitors |
| FR2885904B1 (fr) | 2005-05-19 | 2007-07-06 | Aventis Pharma Sa | Nouveaux derives du fluorene, compositions les contenant et utilisation |
| CN101325952B (zh) | 2005-12-16 | 2012-02-08 | 株式会社三和化学研究所 | 用于急性肾衰竭的预防和治疗剂 |
| CA2642933A1 (en) | 2006-02-20 | 2007-08-30 | Sanwa Kagaku Kenkyusho Co., Ltd. | Prophylactic or therapeutic agent for cerebral ischemia or cerebral ischemic reperfusion injury in stroke |
| WO2008064311A2 (en) | 2006-11-21 | 2008-05-29 | Viamet Pharmaceuticals, Inc. | Metallo-oxidoreductase inhibitors using metal binding moieties in combination with targeting moieties |
| US8440617B2 (en) | 2007-03-22 | 2013-05-14 | The Trustees Of The University Of Pennsylvania | Hyperbaric treatment in wound healing |
| EP2405755A4 (en) | 2009-03-11 | 2012-11-28 | Xintria Pharmaceutical Corp Inc | METHOD AND COMPOSITIONS FOR TREATING METABOLISM AND CARDIOVASCULAR DISEASES |
| EP2295593A1 (en) | 2009-09-15 | 2011-03-16 | Philippe Marliere | Method for the enymatic production of 3-hydroxy-3-methylbutyric acid from acetone and acetyl-CoA |
| AR083169A1 (es) | 2010-09-24 | 2013-02-06 | Array Biopharma Inc | Compuestos para tratar enfermedades neurodegenerativas |
| US20150335615A1 (en) * | 2013-01-04 | 2015-11-26 | Toshihisa Kawai | Cholesterol-lowering compounds in combination with lipid metabolism-altering compounds of non-absorbable sugars, compounds that convert nh3 to nh4+, or hydrogen-generating compounds for the treatment of high cholesterol and inflammation |
| EP3179995B1 (en) | 2014-08-12 | 2018-11-07 | University of Pécs (Pécsi Tudományegyetem) | Methods and materials for reducing ischemia-reperfusion injury |
| WO2016090373A1 (en) | 2014-12-05 | 2016-06-09 | Case Western Reserve University | Compositions and methods of modulating s-nitrosylation |
| US10537557B2 (en) | 2016-01-27 | 2020-01-21 | Case Western Reserve University | Methods of treating respiratory disorders |
| CA3076889A1 (en) * | 2017-09-25 | 2019-03-28 | Case Western Reserve University | Compositions and methods of reducing serum cholesterol and pcsk9 |
| CA3113790A1 (en) * | 2018-09-21 | 2020-03-26 | Case Western Reserve University | Aldoketo reductase inhibitors and uses thereof |
| US12391703B2 (en) * | 2019-09-23 | 2025-08-19 | Case Western Reserve University | Aldoketo reductase inhibitors and uses thereof |
-
2018
- 2018-09-21 CA CA3076889A patent/CA3076889A1/en active Pending
- 2018-09-21 EP EP18858000.5A patent/EP3688163A4/en active Pending
- 2018-09-21 JP JP2020516839A patent/JP7414712B2/ja active Active
- 2018-09-21 WO PCT/US2018/052214 patent/WO2019060720A1/en not_active Ceased
- 2018-09-21 CN CN201880074862.5A patent/CN111356764B/zh active Active
- 2018-09-21 CN CN202410548659.4A patent/CN118512442A/zh active Pending
- 2018-09-21 US US16/648,737 patent/US11576900B2/en active Active
-
2023
- 2023-02-14 US US18/109,406 patent/US20230190710A1/en active Pending
- 2023-10-04 JP JP2023173195A patent/JP2024001162A/ja active Pending
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