JP2015517579A - 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 - Google Patents

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 Download PDF

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JP2015517579A
JP2015517579A JP2015514228A JP2015514228A JP2015517579A JP 2015517579 A JP2015517579 A JP 2015517579A JP 2015514228 A JP2015514228 A JP 2015514228A JP 2015514228 A JP2015514228 A JP 2015514228A JP 2015517579 A JP2015517579 A JP 2015517579A
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JP2015517579A5 (enExample
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シー． ミルン，ジル
シー． ミルン，ジル
アール． ジローセック，マイケル
アール． ジローセック，マイケル
ビー． ヴュ，チ
ビー． ヴュ，チ
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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
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
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Families Citing this family (32)

* Cited by examiner, † Cited by third party
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

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011028689A1 (en) * 2009-09-01 2011-03-10 Catabasis Pharmaceuticals, Inc. Fatty acid niacin conjugates and their uses
WO2011085211A1 (en) * 2010-01-08 2011-07-14 Catabasis Pharmaceuticals, Inc. Fatty acid fumarate derivatives and their uses

Family Cites Families (10)

* Cited by examiner, † Cited by third party
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
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

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011028689A1 (en) * 2009-09-01 2011-03-10 Catabasis Pharmaceuticals, Inc. Fatty acid niacin conjugates and their uses
WO2011085211A1 (en) * 2010-01-08 2011-07-14 Catabasis Pharmaceuticals, Inc. Fatty acid fumarate derivatives and their uses

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