JP2015517579A5 - - Google Patents
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- Publication number
- JP2015517579A5 JP2015517579A5 JP2015514228A JP2015514228A JP2015517579A5 JP 2015517579 A5 JP2015517579 A5 JP 2015517579A5 JP 2015514228 A JP2015514228 A JP 2015514228A JP 2015514228 A JP2015514228 A JP 2015514228A JP 2015517579 A5 JP2015517579 A5 JP 2015517579A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- alkyl
- independently
- pharmaceutically acceptable
- pharmaceutical composition
- 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.)
- Pending
Links
- 150000001875 compounds Chemical class 0.000 claims 37
- 125000000217 alkyl group Chemical group 0.000 claims 20
- 239000008194 pharmaceutical composition Substances 0.000 claims 12
- 239000003937 drug carrier Substances 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 208000006575 hypertriglyceridemia Diseases 0.000 claims 5
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 5
- 208000030159 metabolic disease Diseases 0.000 claims 4
- 208000032928 Dyslipidaemia Diseases 0.000 claims 3
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 3
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 3
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 2
- 101001098868 Homo sapiens Proprotein convertase subtilisin/kexin type 9 Proteins 0.000 claims 2
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 2
- 102000004895 Lipoproteins Human genes 0.000 claims 2
- 108090001030 Lipoproteins Proteins 0.000 claims 2
- 102100038955 Proprotein convertase subtilisin/kexin type 9 Human genes 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
- 229910052805 deuterium Inorganic materials 0.000 claims 2
- 208000016097 disease of metabolism Diseases 0.000 claims 2
- 208000010706 fatty liver disease Diseases 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 1
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 1
- 208000000563 Hyperlipoproteinemia Type II Diseases 0.000 claims 1
- 102100024640 Low-density lipoprotein receptor Human genes 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 206010045261 Type IIa hyperlipidaemia Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 235000012000 cholesterol Nutrition 0.000 claims 1
- 208000029078 coronary artery disease Diseases 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 208000033679 diabetic kidney disease Diseases 0.000 claims 1
- 201000001386 familial hypercholesterolemia Diseases 0.000 claims 1
- 230000002068 genetic effect Effects 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000005549 heteroarylene group Chemical group 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 210000002966 serum Anatomy 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261651870P | 2012-05-25 | 2012-05-25 | |
| US61/651,870 | 2012-05-25 | ||
| US201261697104P | 2012-09-05 | 2012-09-05 | |
| US61/697,104 | 2012-09-05 | ||
| US201361780445P | 2013-03-13 | 2013-03-13 | |
| US61/780,445 | 2013-03-13 | ||
| PCT/US2013/042693 WO2013177536A2 (en) | 2012-05-25 | 2013-05-24 | Methods of lowering proprotein convertase subtilisin/kexin type 9 (pcsk9) |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018081025A Division JP2018127484A (ja) | 2012-05-25 | 2018-04-20 | プロタンパク質転換酵素スブチリシン／ケキシン９型（ｐｃｓｋ９）を低下させる方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2015517579A JP2015517579A (ja) | 2015-06-22 |
| JP2015517579A5 true JP2015517579A5 (enExample) | 2016-07-14 |
Family
ID=49624540
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015514228A Pending JP2015517579A (ja) | 2012-05-25 | 2013-05-24 | プロタンパク質転換酵素スブチリシン／ケキシン９型（ｐｃｓｋ９）を低下させる方法 |
| JP2018081025A Pending JP2018127484A (ja) | 2012-05-25 | 2018-04-20 | プロタンパク質転換酵素スブチリシン／ケキシン９型（ｐｃｓｋ９）を低下させる方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018081025A Pending JP2018127484A (ja) | 2012-05-25 | 2018-04-20 | プロタンパク質転換酵素スブチリシン／ケキシン９型（ｐｃｓｋ９）を低下させる方法 |
Country Status (15)
| Country | Link |
|---|---|
| US (3) | US20140093513A1 (enExample) |
| EP (2) | EP3210972A1 (enExample) |
| JP (2) | JP2015517579A (enExample) |
| KR (1) | KR20150059638A (enExample) |
| CN (2) | CN107243078A (enExample) |
| AR (1) | AR091171A1 (enExample) |
| AU (2) | AU2013266087A1 (enExample) |
| BR (1) | BR112014029245A2 (enExample) |
| CA (1) | CA2874244A1 (enExample) |
| HK (1) | HK1243075A1 (enExample) |
| IL (2) | IL235862A0 (enExample) |
| MX (1) | MX2014014062A (enExample) |
| NZ (1) | NZ702093A (enExample) |
| TW (1) | TW201400442A (enExample) |
| WO (1) | WO2013177536A2 (enExample) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JO3672B1 (ar) | 2008-12-15 | 2020-08-27 | Regeneron Pharma | أجسام مضادة بشرية عالية التفاعل الكيماوي بالنسبة لإنزيم سبتيليسين كنفرتيز بروبروتين / كيكسين نوع 9 (pcsk9). |
| USRE46608E1 (en) | 2009-09-01 | 2017-11-14 | Catabasis Pharmaceuticals, Inc. | Fatty acid niacin conjugates and their uses |
| DK2473045T3 (en) | 2009-09-01 | 2016-12-12 | Catabasis Pharmaceuticals Inc | Niacin-FATTY ACID CONJUGATES AND THEIR USES |
| CA2825778A1 (en) | 2011-01-28 | 2012-08-02 | Sanofi | Pharmaceutical compositions comprising human antibodies to pcsk9 |
| AR087305A1 (es) | 2011-07-28 | 2014-03-12 | Regeneron Pharma | Formulaciones estabilizadas que contienen anticuerpos anti-pcsk9, metodo de preparacion y kit |
| ES2773111T3 (es) | 2011-09-16 | 2020-07-09 | Regeneron Pharma | Inhibidor de la proproteína convertasa subtilisina/kexina 9 (PCSK9) para su uso en la reducción de los niveles de lipoproteína (a) |
| US9255154B2 (en) | 2012-05-08 | 2016-02-09 | Alderbio Holdings, Llc | Anti-PCSK9 antibodies and use thereof |
| AU2014203872A1 (en) * | 2013-01-07 | 2015-07-09 | Catabasis Pharmaceuticals, Inc. | Use of fatty acid niacin conjugates for treating diseases |
| US9682085B2 (en) | 2013-02-22 | 2017-06-20 | Shifa Biomedical Corporation | Anti-proprotein convertase subtilisin kexin type 9 (anti-PCSK9) compounds and methods of using the same in the treatment and/or prevention of cardiovascular diseases |
| EP2968318A4 (en) | 2013-03-15 | 2016-12-14 | Shifa Biomedical Corp | ANTI-PCSK9 COMPOUNDS AND METHODS FOR TREATING AND / OR PREVENTING CARDIOVASCULAR DISEASES |
| US10428157B2 (en) | 2013-11-12 | 2019-10-01 | Sanofi Biotechnology | Dosing regimens for use with PCSK9 inhibitors |
| EA201691320A1 (ru) * | 2014-02-14 | 2016-11-30 | Ридженерон Фармасьютикалз, Инк. | Способы лечения пациентов с гиперхолестеринемией, которая устойчива к терапии умеренными дозами статинов |
| MA41031A (fr) | 2014-11-26 | 2017-10-03 | Catabasis Pharmaceuticals Inc | Conjugués cystéamine-acide gras et leur utilisation comme activateurs de l'autophagie |
| WO2016130417A1 (en) * | 2015-02-11 | 2016-08-18 | Omthera Pharmaceuticals Inc | Omega-3 fatty acid prodrug compounds and uses thereof |
| EP3271405A1 (en) | 2015-03-20 | 2018-01-24 | Aarhus Universitet | Inhibitors of pcsk9 for treatment of lipoprotein metabolism disorders |
| EA201890519A1 (ru) | 2015-08-18 | 2018-07-31 | Ридженерон Фармасьютикалз, Инк. | Ингибирующие антитела против pcsk9 для лечения пациентов с гиперлипидемией, подвергающихся аферезу липопротеинов |
| WO2017034994A1 (en) | 2015-08-21 | 2017-03-02 | Portola Pharmaceuticals, Inc. | Composition and methods of use of novel phenylalanine small organic compounds to directly modulate pcsk9 protein activity |
| HK1260897A1 (zh) | 2015-08-21 | 2019-12-27 | Portola Pharmaceuticals, Inc. | 使用四氢异喹啉小分子来结合并调节pcsk9的蛋白活性的组合物和方法 |
| EP3337788A4 (en) | 2015-08-21 | 2019-03-27 | Portola Pharmaceuticals, Inc. | PHENYLPIPERAZINE PROPROTEIN CONVERTASE SUBTILISIN / -KEXIN TYPE 9 P (CSK9) MODULATORS AND THEIR USE |
| WO2017147328A1 (en) | 2016-02-23 | 2017-08-31 | Portola Pharmaceuticals, Inc. | Compounds for binding proprotein convertase subtilisin/kexin type 9 (pcsk9) |
| EP3471714B1 (en) | 2016-06-21 | 2025-06-11 | Shifa Biomedical Corporation | Anti-proprotein convertase subtilisin kexin type 9 (anti-pcsk9) compounds and methods of using the same in the treatment and/or prevention of cardiovascular diseases |
| AU2017281332A1 (en) | 2016-06-24 | 2018-12-20 | F. Hoffmann-La Roche Ag | Compositions and methods for treating cardiovascular disease |
| ES2871783T3 (es) | 2016-09-20 | 2021-11-02 | Univ Aarhus | Compuestos para el tratamiento de trastornos del metabolismo de las lipoproteínas |
| US20200017603A1 (en) * | 2016-12-01 | 2020-01-16 | Bhl Patent Holdings, Llc | Novel uses of pcsk9 inhibitors and related medications |
| TW201823222A (zh) * | 2016-12-23 | 2018-07-01 | 財團法人生物技術開發中心 | 化合物、醫藥組成物及其用途 |
| US10357476B1 (en) * | 2018-10-30 | 2019-07-23 | Anis Ahmad | Method for treating coronary artery disease |
| BR112021013924A2 (pt) | 2019-01-18 | 2021-09-21 | Astrazeneca Ab | Inibidores de pcsk9 e métodos de uso do mesmo |
| WO2020150473A2 (en) | 2019-01-18 | 2020-07-23 | Dogma Therapeutics, Inc. | Pcsk9 inhibitors and methods of use thereof |
| GB201905779D0 (en) * | 2019-04-25 | 2019-06-05 | Manchester Univ Nhs Foundation Trust | Pcsk9 inhibitors for neuropathy |
| CN112341395B (zh) * | 2020-11-08 | 2022-06-21 | 复旦大学 | 一种微反应系统及使用其连续制备2-甲基-4-氨基-5-氨基甲基嘧啶的方法 |
| US12115154B2 (en) | 2020-12-16 | 2024-10-15 | Srx Cardio, Llc | Compounds for the modulation of proprotein convertase subtilisin/kexin type 9 (PCSK9) |
| CN114380991B (zh) * | 2022-01-17 | 2023-05-26 | 河南大学 | 一种聚合物-脂质偶联物及其制备方法和应用 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5262564A (en) | 1992-10-30 | 1993-11-16 | Octamer, Inc. | Sulfinic acid adducts of organo nitroso compounds useful as retroviral inactivating agents anti-retroviral agents and anti-tumor agents |
| US20050267091A1 (en) * | 2004-05-25 | 2005-12-01 | Roger Berlin | Compositions containing policosanol and niacin and/or niacin derivatives and their pharmaceutical uses |
| US9085527B2 (en) * | 2008-07-08 | 2015-07-21 | Catabasis Pharmaceuticals, Inc. | Fatty acid acylated salicylates and their uses |
| DK2315740T3 (en) | 2008-07-08 | 2018-01-08 | Catabasis Pharmaceuticals Inc | Fatty Acid Acetylated Salicylates and Their Uses |
| US20110009628A1 (en) * | 2009-07-08 | 2011-01-13 | Haiyan Liu | Compounds and Compositions for Modulating Lipid Levels and Methods of Preparing Same |
| DK2473045T3 (en) * | 2009-09-01 | 2016-12-12 | Catabasis Pharmaceuticals Inc | Niacin-FATTY ACID CONJUGATES AND THEIR USES |
| AU2011204277B2 (en) * | 2010-01-08 | 2015-12-24 | Catabasis Pharmaceuticals, Inc. | Fatty Acid Fumarate Derivatives and their uses |
| US9216224B2 (en) * | 2010-03-05 | 2015-12-22 | Catabasis Pharmaceuticals, Inc. | Fatty acid COX inhibitor derivatives and their uses |
| US20130045939A1 (en) * | 2010-03-19 | 2013-02-21 | Catabasis Pharmaceuticals, Inc. | Fatty acid macrolide derivatives and their uses |
| CN102532114B (zh) * | 2011-12-19 | 2016-08-03 | 中山大学 | 烟酸衍生物,其制备方法及其药物组合物 |
| AU2014203872A1 (en) * | 2013-01-07 | 2015-07-09 | Catabasis Pharmaceuticals, Inc. | Use of fatty acid niacin conjugates for treating diseases |
| EP3068224A1 (en) * | 2013-11-15 | 2016-09-21 | Catabasis Pharmaceuticals, Inc. | Fatty acid niacin conjugates |
-
2013
- 2013-05-24 WO PCT/US2013/042693 patent/WO2013177536A2/en not_active Ceased
- 2013-05-24 CN CN201710061317.XA patent/CN107243078A/zh active Pending
- 2013-05-24 NZ NZ702093A patent/NZ702093A/en not_active IP Right Cessation
- 2013-05-24 EP EP16201768.5A patent/EP3210972A1/en not_active Withdrawn
- 2013-05-24 CA CA2874244A patent/CA2874244A1/en not_active Abandoned
- 2013-05-24 JP JP2015514228A patent/JP2015517579A/ja active Pending
- 2013-05-24 CN CN201380027530.9A patent/CN104487060A/zh active Pending
- 2013-05-24 EP EP13794508.5A patent/EP2854787A4/en not_active Withdrawn
- 2013-05-24 US US13/902,360 patent/US20140093513A1/en not_active Abandoned
- 2013-05-24 US US14/402,615 patent/US20150344430A1/en not_active Abandoned
- 2013-05-24 BR BR112014029245A patent/BR112014029245A2/pt not_active IP Right Cessation
- 2013-05-24 MX MX2014014062A patent/MX2014014062A/es unknown
- 2013-05-24 AU AU2013266087A patent/AU2013266087A1/en not_active Abandoned
- 2013-05-24 KR KR1020147035929A patent/KR20150059638A/ko not_active Withdrawn
- 2013-05-27 AR ARP130101843 patent/AR091171A1/es unknown
- 2013-05-27 TW TW102118590A patent/TW201400442A/zh unknown
-
2014
- 2014-11-23 IL IL235862A patent/IL235862A0/en unknown
-
2016
- 2016-06-13 US US15/180,906 patent/US20170144972A1/en not_active Abandoned
-
2018
- 2018-02-21 IL IL257665A patent/IL257665A/en unknown
- 2018-02-23 HK HK18102634.8A patent/HK1243075A1/en unknown
- 2018-03-14 AU AU2018201804A patent/AU2018201804A1/en not_active Abandoned
- 2018-04-20 JP JP2018081025A patent/JP2018127484A/ja active Pending