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 (https=) | 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 (https=) |
| EP (2) | EP2854787A4 (https=) |
| JP (2) | JP2015517579A (https=) |
| KR (1) | KR20150059638A (https=) |
| CN (2) | CN107243078A (https=) |
| AR (1) | AR091171A1 (https=) |
| AU (2) | AU2013266087A1 (https=) |
| BR (1) | BR112014029245A2 (https=) |
| CA (1) | CA2874244A1 (https=) |
| HK (1) | HK1243075A1 (https=) |
| IL (2) | IL235862A0 (https=) |
| MX (1) | MX2014014062A (https=) |
| NZ (1) | NZ702093A (https=) |
| TW (1) | TW201400442A (https=) |
| WO (1) | WO2013177536A2 (https=) |
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 |
| CA2772618C (en) | 2009-09-01 | 2018-08-21 | Catabasis Pharmaceuticals, Inc. | Fatty acid niacin conjugates and their uses |
| PL3395836T3 (pl) | 2011-01-28 | 2021-12-13 | Sanofi Biotechnology | Ludzkie przeciwciała przeciwko pcsk9 do zastosowania w sposobach leczenia konkretnych grup osobników |
| AR087305A1 (es) | 2011-07-28 | 2014-03-12 | Regeneron Pharma | Formulaciones estabilizadas que contienen anticuerpos anti-pcsk9, metodo de preparacion y kit |
| ES2992345T3 (es) | 2011-09-16 | 2024-12-11 | Regeneron Pharma | Métodos para reducir los niveles de lipoproteína(a) mediante la administración de un inhibidor de la proproteína convertasa subtilisina kexina-9 (PCSK9) |
| US9255154B2 (en) | 2012-05-08 | 2016-02-09 | Alderbio Holdings, Llc | Anti-PCSK9 antibodies and use thereof |
| US20150352094A1 (en) * | 2013-01-07 | 2015-12-10 | 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 |
| WO2014150395A1 (en) * | 2013-03-15 | 2014-09-25 | Shifa Biomedical Corporation | Anti-pcsk9 compounds and methods for the treatment and/or prevention of cardiovascular diseases |
| MX2016006226A (es) | 2013-11-12 | 2016-09-07 | Sanofi Biotechnology | Regimenes de dosificacion para uso con inhibidores de pcsk9. |
| CN106029096A (zh) * | 2014-02-14 | 2016-10-12 | 瑞泽恩制药公司 | 用于治疗具有未被中等剂量他汀疗法充分控制的高胆固醇血症的患者的方法 |
| 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 |
| EP3973958A3 (en) | 2015-03-20 | 2022-06-22 | Aarhus Universitet | Inhibitors of pcsk9 for treatment of lipoprotein metabolism disorders |
| JP2018523684A (ja) | 2015-08-18 | 2018-08-23 | リジェネロン・ファーマシューティカルズ・インコーポレイテッドＲｅｇｅｎｅｒｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． | リポタンパク質アフェレーシスを受けている高脂血症の患者を治療するための抗ｐｃｓｋ９阻害抗体 |
| US10821106B2 (en) | 2015-08-21 | 2020-11-03 | Srx Cardio, Llc | Composition and methods of use of novel phenylalanine small organic compounds to directly modulate PCSK9 protein activity |
| US10865185B2 (en) | 2015-08-21 | 2020-12-15 | Srx Cardio, Llc | Composition and methods of use of tetrahydroisoquinoline small molecules to bind and modulate PCSK9 protein activity |
| HK1257102A1 (zh) | 2015-08-21 | 2019-10-11 | Portola Pharmaceuticals, Inc. | 苯基哌嗪前蛋白转化酶枯草杆菌蛋白酶/kexin9型(pcsk9)调节剂及其应用 |
| US20190119236A1 (en) | 2016-02-23 | 2019-04-25 | Portola Pharmaceuticals, Inc. | Compounds for binding proprotein convertase subtilisin/kexin type 9 (pcsk9) |
| CN109475521B (zh) | 2016-06-21 | 2022-11-15 | 实发生物医学公司 | 抗前蛋白转化酶枯草杆菌蛋白酶Kexin 9型(抗PCSK9)化合物及其用于治疗和/或预防心血管疾病的方法 |
| BR112018076242A2 (pt) | 2016-06-24 | 2019-03-26 | Hoffmann La Roche | inibidores de pcsk9, pcsk9 inibido, composição farmacêutica, métodos para modular a atividade de pcsk9, para inibir a ligação de pcsk9 a ldlr, para aumentar a disponibilidade de ldlr, para reduzir um nível de ldl-c, para reduzir o nível sérico de ldl-c, para o tratamento de um distúrbio relacionado com colesterol, métodos para o tratamento de um distúrbio associado a um nível anormal de ldl-c, de uma condição associada a um nível elevado de ldl-c, de dislipidemia, de hipercolesterolemia, usos de um inibidor de pcsk9 e método para identificar um composto candidato como um inibidor de pcsk9 que liga um epítopo da seq id nº 1 |
| CA3035875A1 (en) | 2016-09-20 | 2018-03-29 | Aarhus Universitet | Compounds for treatment of lipoprotein metabolism disorders |
| 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 |
| SG11202107614PA (en) | 2019-01-18 | 2021-08-30 | Astrazeneca Ab | Pcsk9 inhibitors and methods of use thereof |
| AU2020209216A1 (en) | 2019-01-18 | 2021-08-26 | Astrazeneca Ab | 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 |
| EP2315740B1 (en) | 2008-07-08 | 2017-10-25 | Catabasis Pharmaceuticals, Inc. | Fatty acid acetylated salicylates and their uses |
| WO2011006000A1 (en) * | 2009-07-08 | 2011-01-13 | Haiyan Liu | Berberine derivatives useful for modulating lipid levels and their methods of synthesis |
| CA2772618C (en) * | 2009-09-01 | 2018-08-21 | Catabasis Pharmaceuticals, Inc. | Fatty acid niacin conjugates and their uses |
| JP5771627B2 (ja) * | 2010-01-08 | 2015-09-02 | カタバシス ファーマシューティカルズ，インコーポレイテッド | 脂肪酸フマル酸塩誘導体およびそれらの使用 |
| 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 |
| US20150352094A1 (en) * | 2013-01-07 | 2015-12-10 | Catabasis Pharmaceuticals, Inc. | Use of fatty acid niacin conjugates for treating diseases |
| CN105916378A (zh) * | 2013-11-15 | 2016-08-31 | 克塔巴西斯制药有限公司 | 脂肪酸烟酸缀合物 |
-
2013
- 2013-05-24 CA CA2874244A patent/CA2874244A1/en not_active Abandoned
- 2013-05-24 JP JP2015514228A patent/JP2015517579A/ja 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 CN CN201710061317.XA patent/CN107243078A/zh active Pending
- 2013-05-24 KR KR1020147035929A patent/KR20150059638A/ko not_active Withdrawn
- 2013-05-24 NZ NZ702093A patent/NZ702093A/en not_active IP Right Cessation
- 2013-05-24 AU AU2013266087A patent/AU2013266087A1/en not_active Abandoned
- 2013-05-24 MX MX2014014062A patent/MX2014014062A/es unknown
- 2013-05-24 WO PCT/US2013/042693 patent/WO2013177536A2/en not_active Ceased
- 2013-05-24 CN CN201380027530.9A patent/CN104487060A/zh active Pending
- 2013-05-24 EP EP16201768.5A patent/EP3210972A1/en not_active Withdrawn
- 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
- 2013-05-27 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
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