JP2016512825A - 抗プロタンパク質転換酵素サブチリシン/ケキシン9型(抗pcsk9)化合物および心血管疾患の治療および/または予防におけるその使用方法 - Google Patents
抗プロタンパク質転換酵素サブチリシン/ケキシン9型(抗pcsk9)化合物および心血管疾患の治療および/または予防におけるその使用方法 Download PDFInfo
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- JP2016512825A JP2016512825A JP2016501110A JP2016501110A JP2016512825A JP 2016512825 A JP2016512825 A JP 2016512825A JP 2016501110 A JP2016501110 A JP 2016501110A JP 2016501110 A JP2016501110 A JP 2016501110A JP 2016512825 A JP2016512825 A JP 2016512825A
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- Prior art keywords
- pcsk9
- group
- lower alkyl
- aryl
- heteroaryl
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- 0 B*(*C)*(C)C(NC(CC(C)(*)C1)*(C)CC(C)(*)CC1C([*+])=*)=* Chemical compound B*(*C)*(C)C(NC(CC(C)(*)C1)*(C)CC(C)(*)CC1C([*+])=*)=* 0.000 description 3
- XDTMQSROBMDMFD-UHFFFAOYSA-N C1CCCCC1 Chemical compound C1CCCCC1 XDTMQSROBMDMFD-UHFFFAOYSA-N 0.000 description 1
- SQQVCWYREDTFTJ-UHFFFAOYSA-N CC1SC=C(C)N1 Chemical compound CC1SC=C(C)N1 SQQVCWYREDTFTJ-UHFFFAOYSA-N 0.000 description 1
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- 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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- A61K31/40—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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- A61K31/403—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
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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
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- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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- 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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- Pharmacology & Pharmacy (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (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 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018190991A Division JP6691948B2 (ja) | 2013-03-15 | 2018-10-09 | 抗プロタンパク質転換酵素サブチリシン/ケキシン9型(抗pcsk9)化合物および心血管疾患の治療および/または予防におけるその使用方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016512825A true JP2016512825A (ja) | 2016-05-09 |
| JP2016512825A5 JP2016512825A5 (enExample) | 2017-04-13 |
Family
ID=51580740
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016501110A Pending JP2016512825A (ja) | 2013-03-15 | 2014-03-11 | 抗プロタンパク質転換酵素サブチリシン/ケキシン9型(抗pcsk9)化合物および心血管疾患の治療および/または予防におけるその使用方法 |
| JP2018190991A Expired - Fee Related JP6691948B2 (ja) | 2013-03-15 | 2018-10-09 | 抗プロタンパク質転換酵素サブチリシン/ケキシン9型(抗pcsk9)化合物および心血管疾患の治療および/または予防におけるその使用方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018190991A Expired - Fee Related JP6691948B2 (ja) | 2013-03-15 | 2018-10-09 | 抗プロタンパク質転換酵素サブチリシン/ケキシン9型(抗pcsk9)化合物および心血管疾患の治療および/または予防におけるその使用方法 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US20160256467A1 (enExample) |
| EP (1) | EP2968266B1 (enExample) |
| JP (2) | JP2016512825A (enExample) |
| CN (1) | CN105228616B (enExample) |
| AU (1) | AU2014237312B2 (enExample) |
| BR (1) | BR112015023294A2 (enExample) |
| CA (1) | CA2904660C (enExample) |
| WO (1) | WO2014150326A1 (enExample) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2017528448A (ja) * | 2014-08-21 | 2017-09-28 | エスアールエックス カーディオ,エル エル シー | プロタンパク質コンバターゼであるスブチリシン/ケキシンタイプ9(pcsk9)のタンパク質活性のモジュレーションのための、結合リガンドとしての小分子の組成物およびその使用方法 |
| JP2019523781A (ja) * | 2016-06-21 | 2019-08-29 | 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 |
| JP2021522311A (ja) * | 2018-06-21 | 2021-08-30 | メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. | Pcsk9アンタゴニスト化合物 |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20170290806A1 (en) * | 2014-09-08 | 2017-10-12 | Temple University-Of The Commonwealth System Of Higher Education | PCSK9 Inhibitors and Methods of Use Thereof |
| US10428029B2 (en) * | 2014-09-10 | 2019-10-01 | Epizyme, Inc. | Isoxazole carboxamide compounds |
| GB201504763D0 (en) | 2015-03-20 | 2015-05-06 | Mironid Ltd | Compounds and uses |
| TN2017000483A1 (en) | 2015-05-20 | 2019-04-12 | Amgen Inc | Triazole agonists of the apj receptor. |
| JP2018531924A (ja) | 2015-09-24 | 2018-11-01 | ファイザー・インク | テトラヒドロピラノ[3,4−d][1,3]オキサジン誘導体、およびbace阻害剤としてのその使用 |
| 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 |
| 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 |
| WO2018093580A1 (en) | 2016-11-16 | 2018-05-24 | Amgen Inc. | Triazole pyridyl compounds as agonists of the apj receptor |
| US10906890B2 (en) | 2016-11-16 | 2021-02-02 | Amgen Inc. | Triazole phenyl compounds as agonists of the APJ receptor |
| US11191762B2 (en) | 2016-11-16 | 2021-12-07 | Amgen Inc. | Alkyl substituted triazole 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 |
| WO2018097945A1 (en) | 2016-11-16 | 2018-05-31 | Amgen Inc. | Heteroaryl-substituted triazoles as apj receptor agonists |
| EP3541792B1 (en) | 2016-11-16 | 2020-12-23 | Amgen Inc. | Triazole furan compounds as agonists of the apj receptor |
| 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 |
| WO2019089335A1 (en) | 2017-11-03 | 2019-05-09 | Amgen Inc. | Fused triazole agonists of the apj receptor |
| WO2019169193A1 (en) | 2018-03-01 | 2019-09-06 | Annapurna Bio Inc. | Compounds and compositions for treating conditions associated with apj receptor activity |
| 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 |
| WO2019246386A1 (en) | 2018-06-21 | 2019-12-26 | Ra Pharmaceuticals Inc. | Cyclic polypeptides for pcsk9 inhibition |
| EP3810177B1 (en) | 2018-06-21 | 2024-12-04 | Ra Pharmaceuticals, Inc. | Cyclic polypeptides for pcsk9 inhibition |
| CN112969684B (zh) * | 2018-11-05 | 2023-11-10 | 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)纳米制剂化合物及使用其的方法 |
| CN119060040A (zh) | 2019-01-18 | 2024-12-03 | 阿斯利康(瑞典)有限公司 | Pcsk9抑制剂及其使用方法 |
| WO2022251533A1 (en) * | 2021-05-27 | 2022-12-01 | Protego Biopharma, Inc. | Heteroaryl diamide ire1/xbp1s activators |
| TW202423430A (zh) * | 2022-10-14 | 2024-06-16 | 大陸商上海翰森生物醫藥科技有限公司 | 含氮雜環類衍生物抑制劑、其製備方法和應用 |
| EP4626865A1 (en) * | 2022-11-30 | 2025-10-08 | 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 |
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| 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 |
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| DE3021590A1 (de) * | 1980-06-09 | 1981-12-17 | Hoechst Ag, 6000 Frankfurt | 4-halogen-5-(halogenmethyl-phenyl)-oxazol-derivate, ein verfahren zu ihrer herstellung und sie enthaltenden strahlungsempfindliche massen |
| US20030130343A1 (en) * | 2001-08-10 | 2003-07-10 | Adipogenix, Inc. | Fat accumulation-modulating compounds |
| RU2004109818A (ru) * | 2001-10-03 | 2005-05-10 | Юсиби, С.А. (Be) | Производные пирролидинона |
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- 2014-03-11 AU AU2014237312A patent/AU2014237312B2/en not_active Ceased
- 2014-03-11 CA CA2904660A patent/CA2904660C/en active Active
- 2014-03-11 BR BR112015023294A patent/BR112015023294A2/pt not_active IP Right Cessation
- 2014-03-11 CN CN201480016193.8A patent/CN105228616B/zh not_active Expired - Fee Related
- 2014-03-11 JP JP2016501110A patent/JP2016512825A/ja active Pending
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Cited By (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2017528448A (ja) * | 2014-08-21 | 2017-09-28 | エスアールエックス カーディオ,エル エル シー | プロタンパク質コンバターゼであるスブチリシン/ケキシンタイプ9(pcsk9)のタンパク質活性のモジュレーションのための、結合リガンドとしての小分子の組成物およびその使用方法 |
| US11026957B2 (en) | 2014-08-21 | 2021-06-08 | Srx Cardio, Llc | Method to treat lipid dysregulation by modulation of proprotein convertase subtilisin/kexin type 9 (PCSK9) protein activity with small molecule ligands |
| US11771710B2 (en) | 2014-08-21 | 2023-10-03 | Srx Cardio, Llc | Method to treat lipid dysregulation by modulation of proprotein convertase subtilisin/kexin type 9 (PCSK9) protein activity with small molecule ligands |
| JP2019523781A (ja) * | 2016-06-21 | 2019-08-29 | 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 |
| 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 |
| JP2021522311A (ja) * | 2018-06-21 | 2021-08-30 | メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. | Pcsk9アンタゴニスト化合物 |
| JP7112531B2 (ja) | 2018-06-21 | 2022-08-03 | メルク・シャープ・アンド・ドーム・コーポレーション | Pcsk9アンタゴニスト化合物 |
| JP2022141879A (ja) * | 2018-06-21 | 2022-09-29 | メルク・シャープ・アンド・ドーム・コーポレーション | Pcsk9アンタゴニスト化合物 |
| JP7607615B2 (ja) | 2018-06-21 | 2024-12-27 | メルク・シャープ・アンド・ドーム・エルエルシー | Pcsk9アンタゴニスト化合物 |
Also Published As
| Publication number | Publication date |
|---|---|
| CN105228616B (zh) | 2019-05-03 |
| EP2968266A1 (en) | 2016-01-20 |
| CN105228616A (zh) | 2016-01-06 |
| EP2968266B1 (en) | 2019-05-01 |
| AU2014237312A1 (en) | 2015-11-05 |
| JP6691948B2 (ja) | 2020-05-13 |
| EP2968266A4 (en) | 2016-09-07 |
| CA2904660A1 (en) | 2014-09-25 |
| BR112015023294A2 (pt) | 2017-07-18 |
| CA2904660C (en) | 2021-04-06 |
| AU2014237312B2 (en) | 2019-03-28 |
| JP2019031522A (ja) | 2019-02-28 |
| WO2014150326A1 (en) | 2014-09-25 |
| US20160256467A1 (en) | 2016-09-08 |
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