JP2022537140A - プロタンパク質転換酵素サブチリシン／ケキシン９型（ｐｃｓｋ９）の調節のための化合物 - Google Patents

プロタンパク質転換酵素サブチリシン／ケキシン９型（ｐｃｓｋ９）の調節のための化合物 Download PDF

Info

Publication number
JP2022537140A
JP2022537140A JP2021573446A JP2021573446A JP2022537140A JP 2022537140 A JP2022537140 A JP 2022537140A JP 2021573446 A JP2021573446 A JP 2021573446A JP 2021573446 A JP2021573446 A JP 2021573446A JP 2022537140 A JP2022537140 A JP 2022537140A
Authority
JP
Japan
Prior art keywords
alkyl
cycloalkyl
optionally substituted
halo
haloalkyl
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
Application number
JP2021573446A
Other languages
English (en)
Japanese (ja)
Other versions
JP2022537140A5 (https=
JPWO2020252383A5 (https=
Inventor
シメオン バウアーズ，
マーク カーバーツ，
ジアン ジュー，
トーマス イー． バルタ，
ジョナサン ウィリアム ボーン，
アンジャリ パンディ，
Original Assignee
エスアールエックス カーディオ，エル エル シー
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by エスアールエックス カーディオ，エル エル シー filed Critical エスアールエックス カーディオ，エル エル シー
Publication of JP2022537140A publication Critical patent/JP2022537140A/ja
Publication of JP2022537140A5 publication Critical patent/JP2022537140A5/ja
Publication of JPWO2020252383A5 publication Critical patent/JPWO2020252383A5/ja
Pending legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/10—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
    • C07D211/14—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/38—Halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/40—Oxygen atoms
    • C07D211/42—Oxygen atoms attached in position 3 or 5
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/56—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/06—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to ring carbon atoms
    • C07D233/08—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to ring carbon atoms with alkyl radicals, containing more than four carbon atoms, directly attached to ring carbon atoms
    • C07D233/10—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to ring carbon atoms with alkyl radicals, containing more than four carbon atoms, directly attached to ring carbon atoms with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to ring nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/20—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D233/22—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2021573446A 2019-06-14 2020-06-12 プロタンパク質転換酵素サブチリシン／ケキシン９型（ｐｃｓｋ９）の調節のための化合物 Pending JP2022537140A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962861902P 2019-06-14 2019-06-14
US62/861,902 2019-06-14
PCT/US2020/037591 WO2020252383A2 (en) 2019-06-14 2020-06-12 Compounds for the modulation of proprotein convertase subtilisin/kexin type 9 (pcsk9)

Publications (3)

Publication Number Publication Date
JP2022537140A true JP2022537140A (ja) 2022-08-24
JP2022537140A5 JP2022537140A5 (https=) 2023-06-19
JPWO2020252383A5 JPWO2020252383A5 (https=) 2023-06-19

Family

ID=73780709

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2021573446A Pending JP2022537140A (ja) 2019-06-14 2020-06-12 プロタンパク質転換酵素サブチリシン／ケキシン９型（ｐｃｓｋ９）の調節のための化合物

Country Status (8)

Country Link
US (1) US20220267269A1 (https=)
EP (1) EP3983392A4 (https=)
JP (1) JP2022537140A (https=)
CN (1) CN114206843A (https=)
AU (1) AU2020291468A1 (https=)
CA (1) CA3142890A1 (https=)
IL (1) IL288848A (https=)
WO (1) WO2020252383A2 (https=)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
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
US20190119236A1 (en) 2016-02-23 2019-04-25 Portola Pharmaceuticals, Inc. Compounds for binding proprotein convertase subtilisin/kexin type 9 (pcsk9)
US12115154B2 (en) 2020-12-16 2024-10-15 Srx Cardio, Llc Compounds for the modulation of proprotein convertase subtilisin/kexin type 9 (PCSK9)
CN121443616A (zh) * 2023-07-27 2026-01-30 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
WO2025034510A1 (en) 2023-08-04 2025-02-13 University Of Rochester Adrenergic antagonists for use in a method for treating cerebral edema or a brain injury

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH10511084A (ja) * 1994-12-16 1998-10-27 ローヌ−プーラン ローラー ファーマシューティカルズ インコーポレイテッド ポリアリールカルバモイルアザ及びカルバモイルアルカン二酸
JP2003523941A (ja) * 1999-05-21 2003-08-12 ファイザー・プロダクツ・インク Ｎｏｓ阻害剤のための新規医薬組合せ
WO2005016910A1 (ja) * 2003-08-18 2005-02-24 Sankio Chemical Co., Ltd. ピリジルテトラヒドロピリジン類およびピリジルピペリジン類とそれらの製造方法
JP2009542732A (ja) * 2006-07-10 2009-12-03 ハー・ルンドベック・アクチエゼルスカベット ６，７−ジアルコキシキナゾリン、６，７−ジアルコキシフタラジンおよび６，７−ジアルコキシイソキノリンの（３−アリール−ピペラジン−１−イル）、（２−アリール−モルホリン−４−イル）および（２−アリール−チオモルホリン−４−イル）誘導体
CN106995413A (zh) * 2016-01-25 2017-08-01 中国科学院大连化学物理研究所 一种铱催化氢化不对称合成哌嗪衍生物的方法

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HN1997000027A (es) * 1996-12-06 1997-06-05 Pfizer Prod Inc Derivados de 6-fenil piridil - 2 amina
EP1957477B1 (en) * 2005-09-29 2011-12-07 Abbott Laboratories 1h-benzimidazole-4-carboxamides substituted with phenyl at the 2-position are potent parp inhibitors
US7834178B2 (en) * 2006-03-01 2010-11-16 Bristol-Myers Squibb Company Triazine 11-beta hydroxysteroid dehydrogenase type 1 inhibitors
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
WO2018165718A1 (en) * 2017-03-17 2018-09-20 Cardio Therapeutics Pty Ltd Heterocyclic inhibitors of pcsk9
CN110546149B (zh) * 2017-04-21 2022-11-11 深圳信立泰药业股份有限公司 作为pcsk9抑制剂的哌啶类化合物

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH10511084A (ja) * 1994-12-16 1998-10-27 ローヌ−プーラン ローラー ファーマシューティカルズ インコーポレイテッド ポリアリールカルバモイルアザ及びカルバモイルアルカン二酸
JP2003523941A (ja) * 1999-05-21 2003-08-12 ファイザー・プロダクツ・インク Ｎｏｓ阻害剤のための新規医薬組合せ
WO2005016910A1 (ja) * 2003-08-18 2005-02-24 Sankio Chemical Co., Ltd. ピリジルテトラヒドロピリジン類およびピリジルピペリジン類とそれらの製造方法
JP2009542732A (ja) * 2006-07-10 2009-12-03 ハー・ルンドベック・アクチエゼルスカベット ６，７−ジアルコキシキナゾリン、６，７−ジアルコキシフタラジンおよび６，７−ジアルコキシイソキノリンの（３−アリール−ピペラジン−１−イル）、（２−アリール−モルホリン−４−イル）および（２−アリール−チオモルホリン−４−イル）誘導体
CN106995413A (zh) * 2016-01-25 2017-08-01 中国科学院大连化学物理研究所 一种铱催化氢化不对称合成哌嗪衍生物的方法

Non-Patent Citations (9)

* Cited by examiner, † Cited by third party
Title
DATABASE REGISTRY, JPN7024002078, 2017, ISSN: 0005485502 *
DATABASE REGISTRY, JPN7024002080, 2015, ISSN: 0005331036 *
DATABASE REGISTRY, JPN7024002081, 2012, ISSN: 0005331037 *
DATABASE REGISTRY, JPN7024002082, 2012, ISSN: 0005331038 *
DATABASE REGISTRY, JPN7024002083, 2015, ISSN: 0005331039 *
DATABASE REGISTRY, JPN7024002084, 2015, ISSN: 0005331040 *
DATABASE REGISTRY, JPN7024002085, 2017, ISSN: 0005331041 *
J. AM. CHEM. SOC., vol. 70, no. 10, JPN7024002079, 1948, pages 3340 - 3342, ISSN: 0005331035 *
SYNTHETIC COMMUNICATIONS, vol. 35, JPN7024002086, 2005, pages 357 - 369, ISSN: 0005331034 *

Also Published As

Publication number Publication date
EP3983392A2 (en) 2022-04-20
CN114206843A (zh) 2022-03-18
WO2020252383A3 (en) 2021-03-18
WO2020252383A2 (en) 2020-12-17
IL288848A (en) 2022-02-01
AU2020291468A1 (en) 2022-01-06
US20220267269A1 (en) 2022-08-25
CA3142890A1 (en) 2020-12-17
EP3983392A4 (en) 2023-12-06

Similar Documents

Publication Publication Date Title
US11891369B2 (en) Compounds for binding proprotein convertase subtilisin/kexin type 9
JP2022537140A (ja) プロタンパク質転換酵素サブチリシン／ケキシン９型（ｐｃｓｋ９）の調節のための化合物
US12115154B2 (en) Compounds for the modulation of proprotein convertase subtilisin/kexin type 9 (PCSK9)
USRE48150E1 (en) Apoptosis signal-regulating kinase inhibitors
US8664399B2 (en) Substituted heterocyclic compounds as ion channel modulators
US8952007B2 (en) Fused heterocyclic compounds as ion channel modulators
US9458132B2 (en) Therapeutic compounds and compositions and their use as PKM2 modulators
US20130197001A1 (en) Substituted heterocyclic compounds
US8389500B2 (en) Fused heterocyclic compounds as ion channel modulators
TW202220961A (zh) Ｐｈｄ抑制劑化合物、組成物及使用方法
HK1184781B (en) Apoptosis signal-regulating kinase inhibitors
HK1224284B (en) Apoptosis signal-regulating kinase inhibitors
HK1224284A1 (en) Apoptosis signal-regulating kinase inhibitors

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20230609

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20230609

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20240523

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20240527

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20241217