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 PDF

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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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pcsk9
group
lower alkyl
aryl
heteroaryl
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シェリン・サラヘルディン・アブデル−メグイド
ナビル・エルシュウバジー
ハロルド・マイヤーズ
シェイカー・エイ・ムーサ
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Shifa Biomedical Corp
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    • A—HUMAN NECESSITIES
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    • 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
    • A—HUMAN NECESSITIES
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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
    • A—HUMAN NECESSITIES
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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
    • A—HUMAN NECESSITIES
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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
    • A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • A—HUMAN NECESSITIES
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4196—1,2,4-Triazoles
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/433—Thidiazoles
    • A—HUMAN NECESSITIES
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    • 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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    • A61K31/395—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
    • A61K31/445—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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JP2016501110A 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 Pending JP2016512825A (ja)

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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

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JP2016512825A true JP2016512825A (ja) 2016-05-09
JP2016512825A5 JP2016512825A5 (https=) 2017-04-13

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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

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US (1) US20160256467A1 (https=)
EP (1) EP2968266B1 (https=)
JP (2) JP2016512825A (https=)
CN (1) CN105228616B (https=)
AU (1) AU2014237312B2 (https=)
BR (1) BR112015023294A2 (https=)
CA (1) CA2904660C (https=)
WO (1) WO2014150326A1 (https=)

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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
JP7855670B2 (ja) 2018-06-21 2026-05-08 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

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JP2017526706A (ja) * 2014-09-10 2017-09-14 エピザイム，インコーポレイティド イソオキサゾールカルボキサミド化合物
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JP7110124B2 (ja) 2016-06-24 2022-08-01 エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト 心血管疾患を治療するための組成物及び方法
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WO2018093576A1 (en) 2016-11-16 2018-05-24 Amgen Inc. Alkyl substituted triazole compounds as agonists of the apj receptor
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WO2018093577A1 (en) 2016-11-16 2018-05-24 Amgen Inc. Cycloalkyl substituted triazole compounds as agonists of the apj receptor
WO2018093579A1 (en) 2016-11-16 2018-05-24 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
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
WO2018165718A1 (en) 2017-03-17 2018-09-20 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
MA50509A (fr) 2017-11-03 2021-06-02 Amgen Inc Agonistes de triazole fusionnés du récepteur apj
US11724997B2 (en) 2018-03-01 2023-08-15 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
US11807624B2 (en) 2018-05-01 2023-11-07 Amgen Inc. Substituted pyrimidinones as agonists of the APJ receptor
EP3810177B1 (en) 2018-06-21 2024-12-04 Ra Pharmaceuticals, Inc. Cyclic polypeptides for pcsk9 inhibition
WO2019246386A1 (en) 2018-06-21 2019-12-26 Ra Pharmaceuticals Inc. Cyclic polypeptides for pcsk9 inhibition
EP3877359A4 (en) 2018-11-05 2022-09-07 Shifa Biomedical Corporation Anti-proprotein convertase subtilisin kexin type 9 (anti-pcsk9) nano-formulation of compounds and methods of using the same
BR112021013807A2 (pt) 2019-01-18 2021-11-30 Astrazeneca Ab Inibidores de pcsk9 e seus métodos de uso
EP4076492A4 (en) 2019-12-20 2024-01-17 Merck Sharp & Dohme LLC PCSK9 ANTAGONIST COMPOUNDS
EP4347568A1 (en) * 2021-05-27 2024-04-10 Protego Biopharma, Inc. Heteroaryl diamide ire1/xbp1s activators
CN120019043B (zh) * 2022-10-14 2026-04-03 上海翰森生物医药科技有限公司 含氮杂环类衍生物抑制剂、其制备方法和应用
EP4626865A1 (en) * 2022-11-30 2025-10-08 Protego Biopharma, Inc. Cyclic pyrazole diamide ire1/xbp1s activators
CN119264042A (zh) 2023-07-04 2025-01-07 上海翰森生物医药科技有限公司 含环戊烷类衍生物抑制剂、其制备方法和应用
TW202506682A (zh) * 2023-07-27 2025-02-16 大陸商上海拓界生物醫藥科技有限公司 二胺基環戊基取代的雜芳基衍生物及其用途和製備方法

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