CN105228616B - 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 - Google Patents
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 Download PDFInfo
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- CN105228616B CN105228616B CN201480016193.8A CN201480016193A CN105228616B CN 105228616 B CN105228616 B CN 105228616B CN 201480016193 A CN201480016193 A CN 201480016193A CN 105228616 B CN105228616 B CN 105228616B
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- pcsk9
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/4015—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
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- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
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- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
- A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
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- A61K31/4164—1,3-Diazoles
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- Health & Medical Sciences (AREA)
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- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
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- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361788061P | 2013-03-15 | 2013-03-15 | |
| US61/788,061 | 2013-03-15 | ||
| PCT/US2014/022957 WO2014150326A1 (en) | 2013-03-15 | 2014-03-11 | 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 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN105228616A CN105228616A (zh) | 2016-01-06 |
| CN105228616B true CN105228616B (zh) | 2019-05-03 |
Family
ID=51580740
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201480016193.8A Expired - Fee Related CN105228616B (zh) | 2013-03-15 | 2014-03-11 | 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 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US20160256467A1 (OSRAM) |
| EP (1) | EP2968266B1 (OSRAM) |
| JP (2) | JP2016512825A (OSRAM) |
| CN (1) | CN105228616B (OSRAM) |
| AU (1) | AU2014237312B2 (OSRAM) |
| BR (1) | BR112015023294A2 (OSRAM) |
| CA (1) | CA2904660C (OSRAM) |
| WO (1) | WO2014150326A1 (OSRAM) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
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| US10034892B2 (en) | 2014-08-21 | 2018-07-31 | Srx Cardio, Llc | Composition and methods of use of small molecules as binding ligands for the modulation of proprotein convertase subtilisin/kexin type 9(PCSK9) protein activity |
| WO2016040305A1 (en) * | 2014-09-08 | 2016-03-17 | Temple University-Of The Commonwealth System Of Higher Education | Pcsk9 inhibitors and methods of use thereof |
| EP3193603A4 (en) * | 2014-09-10 | 2018-02-28 | Epizyme, Inc. | Isoxazole carboxamide compounds |
| GB201504763D0 (en) | 2015-03-20 | 2015-05-06 | Mironid Ltd | Compounds and uses |
| JP6356364B1 (ja) | 2015-05-20 | 2018-07-11 | アムジエン・インコーポレーテツド | Apj受容体のトリアゾールアゴニスト |
| WO2017051303A1 (en) | 2015-09-24 | 2017-03-30 | Pfizer Inc. | Tetrahydropyrano[3,4-d][1,3]oxazin derivatives and their use as bace inhibitors |
| CN105214087B (zh) | 2015-10-29 | 2017-12-26 | 陈敏 | Pcsk9单克隆抗体在制备治疗炎症免疫性疾病药物中的应用 |
| WO2017192485A1 (en) | 2016-05-03 | 2017-11-09 | Amgen Inc. | Heterocyclic triazole compounds as agonists of the apj receptor |
| JP7097828B2 (ja) * | 2016-06-21 | 2022-07-08 | シファ バイオメディカル コーポレーション | 抗プロタンパク質変換酵素サブチリシン ケキシン タイプ9(Subtilisin Kexin Type 9)(抗PCSK9)化合物および心血管疾患の治療および/または予防にこれを使用する方法 |
| AU2017281332A1 (en) | 2016-06-24 | 2018-12-20 | F. Hoffmann-La Roche Ag | Compositions and methods for treating cardiovascular disease |
| GB201616439D0 (en) | 2016-09-28 | 2016-11-09 | Mironid Limited | Compounds and uses |
| MA46824A (fr) | 2016-11-16 | 2019-09-25 | Amgen Inc | Composés de triazole substitués par alkyle en tant qu'agonistes du récepteur apj |
| EP3541810B1 (en) | 2016-11-16 | 2020-12-23 | Amgen Inc. | Triazole phenyl compounds as agonists of the apj receptor |
| EP3541803B1 (en) | 2016-11-16 | 2020-12-23 | Amgen Inc. | Triazole pyridyl compounds as agonists of the apj receptor |
| US10736883B2 (en) | 2016-11-16 | 2020-08-11 | Amgen Inc. | Triazole furan compounds as agonists of the APJ receptor |
| MA46827A (fr) | 2016-11-16 | 2019-09-25 | Amgen Inc | Composés de triazole à substitution cycloalkyle en tant qu'agonistes du récepteur apj |
| US11046680B1 (en) | 2016-11-16 | 2021-06-29 | Amgen Inc. | Heteroaryl-substituted triazoles as APJ receptor agonists |
| 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 |
| US11091466B2 (en) | 2017-03-17 | 2021-08-17 | Cardio Therapeutics Pty Ltd | Heterocyclic inhibitors of PCSK9 |
| CN107596373A (zh) * | 2017-09-28 | 2018-01-19 | 韩庆亮 | 一种用于治疗心血管疾病的方法 |
| US11149040B2 (en) | 2017-11-03 | 2021-10-19 | Amgen Inc. | Fused triazole agonists of the APJ receptor |
| CN112055713A (zh) | 2018-03-01 | 2020-12-08 | 安娜普尔纳生物股份有限公司 | 用于治疗与apj受体活性有关的疾病的化合物和组合物 |
| GB201805527D0 (en) | 2018-04-04 | 2018-05-16 | Mironid Ltd | Compounds and their use as pde4 activators |
| WO2019213006A1 (en) | 2018-05-01 | 2019-11-07 | Amgen Inc. | Substituted pyrimidinones as agonists of the apj receptor |
| JOP20190150A1 (ar) | 2018-06-21 | 2019-12-21 | Merck Sharp & Dohme | مركبات مناهضة لـ pcsk9 |
| ES3013570T3 (en) | 2018-06-21 | 2025-04-14 | Ucb Holdings Inc | Cyclic polypeptides for pcsk9 inhibition |
| US11814445B2 (en) | 2018-06-21 | 2023-11-14 | Ra Pharmaceuticals, Inc. | Cyclic polypeptides for PCSK9 inhibition |
| KR20210090642A (ko) | 2018-11-05 | 2021-07-20 | 시파 바이오메디칼 코포레이션 | 항-프로단백질 전환효소 서브틸리신 켁신 유형 9(항-pcsk9) 화합물의 나노제형 및 이의 사용 방법 |
| CR20210441A (es) | 2019-01-18 | 2022-03-11 | Astrazeneca Ab | Inhibidores de la pcsk9 y métodos de uso de los mismos |
| WO2022251533A1 (en) * | 2021-05-27 | 2022-12-01 | Protego Biopharma, Inc. | Heteroaryl diamide ire1/xbp1s activators |
| EP4588914A1 (en) | 2022-10-14 | 2025-07-23 | Shanghai Hansoh Biomedical Co., Ltd. | Nitrogen-containing heterocyclic derivative inhibitor, preparation method therefor and use thereof |
| WO2024118810A1 (en) * | 2022-11-30 | 2024-06-06 | Protego Biopharma, Inc. | Cyclic pyrazole diamide ire1/xbp1s activators |
| WO2025021188A1 (zh) * | 2023-07-27 | 2025-01-30 | 上海拓界生物医药科技有限公司 | 二氨基环戊基取代的杂芳基衍生物及其用途和制备方法 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
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| US4017313A (en) * | 1974-09-30 | 1977-04-12 | E. I. Du Pont De Nemours And Company | Photosensitive composition containing a leuco dye, a photosensitizer, an aromatic aldehyde and a secondary or tertiary amine and the use thereof in a direct-print process |
| US4371607A (en) * | 1980-06-09 | 1983-02-01 | Hoechst Aktiengesellschaft | 4-Halogeno-5-(halogenomethyl-phenyl)-oxazole derivatives, a process for the preparation thereof, and radiation-sensitive compositions containing these derivatives |
| US8003654B2 (en) * | 2006-04-11 | 2011-08-23 | Actelion Pharmaceuticals Ltd. | N-glycinsulfonamide derivatives and uses as orexin receptor antagonists |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003013516A1 (en) * | 2001-08-10 | 2003-02-20 | Adipogenix, Inc. | Fat accumulation-modulating compounds |
| CZ2004442A3 (cs) * | 2001-10-03 | 2005-03-16 | Ucb, S.A. | Pyrrolidinonové deriváty |
| JP2006522750A (ja) * | 2003-04-11 | 2006-10-05 | ノボ ノルディスク アクティーゼルスカブ | 代謝性症候群ならびに関連の疾患および障害を治療するために、11β−ヒドロキシステロイドデヒドロゲナーゼ1型阻害剤および抗高血圧剤を使用する併用療法 |
| US20050288340A1 (en) * | 2004-06-29 | 2005-12-29 | Pfizer Inc | Substituted heteroaryl- and phenylsulfamoyl compounds |
| US20090275053A1 (en) * | 2008-04-30 | 2009-11-05 | Board Of Regents, The University Of Texas System | Cell-based pcsk9 screening assay |
| GB201205653D0 (en) * | 2012-03-30 | 2012-05-16 | Jaguar Cars | Wade sensing display control system |
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2014
- 2014-03-11 BR BR112015023294A patent/BR112015023294A2/pt not_active IP Right Cessation
- 2014-03-11 JP JP2016501110A patent/JP2016512825A/ja active Pending
- 2014-03-11 WO PCT/US2014/022957 patent/WO2014150326A1/en not_active Ceased
- 2014-03-11 CN CN201480016193.8A patent/CN105228616B/zh not_active Expired - Fee Related
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- 2014-03-11 EP EP14770138.7A patent/EP2968266B1/en active Active
- 2014-03-11 AU AU2014237312A patent/AU2014237312B2/en not_active Ceased
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2016
- 2016-05-12 US US15/152,703 patent/US20160256467A1/en not_active Abandoned
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2018
- 2018-10-09 JP JP2018190991A patent/JP6691948B2/ja not_active Expired - Fee Related
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4017313A (en) * | 1974-09-30 | 1977-04-12 | E. I. Du Pont De Nemours And Company | Photosensitive composition containing a leuco dye, a photosensitizer, an aromatic aldehyde and a secondary or tertiary amine and the use thereof in a direct-print process |
| US4371607A (en) * | 1980-06-09 | 1983-02-01 | Hoechst Aktiengesellschaft | 4-Halogeno-5-(halogenomethyl-phenyl)-oxazole derivatives, a process for the preparation thereof, and radiation-sensitive compositions containing these derivatives |
| US8003654B2 (en) * | 2006-04-11 | 2011-08-23 | Actelion Pharmaceuticals Ltd. | N-glycinsulfonamide derivatives and uses as orexin receptor antagonists |
Also Published As
| Publication number | Publication date |
|---|---|
| CA2904660C (en) | 2021-04-06 |
| JP2016512825A (ja) | 2016-05-09 |
| JP6691948B2 (ja) | 2020-05-13 |
| WO2014150326A1 (en) | 2014-09-25 |
| CA2904660A1 (en) | 2014-09-25 |
| BR112015023294A2 (pt) | 2017-07-18 |
| EP2968266B1 (en) | 2019-05-01 |
| JP2019031522A (ja) | 2019-02-28 |
| AU2014237312B2 (en) | 2019-03-28 |
| AU2014237312A1 (en) | 2015-11-05 |
| EP2968266A1 (en) | 2016-01-20 |
| US20160256467A1 (en) | 2016-09-08 |
| CN105228616A (zh) | 2016-01-06 |
| EP2968266A4 (en) | 2016-09-07 |
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