JP7350061B2 - フューリンインヒビター - Google Patents

フューリンインヒビター Download PDF

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Publication number
JP7350061B2
JP7350061B2 JP2021513005A JP2021513005A JP7350061B2 JP 7350061 B2 JP7350061 B2 JP 7350061B2 JP 2021513005 A JP2021513005 A JP 2021513005A JP 2021513005 A JP2021513005 A JP 2021513005A JP 7350061 B2 JP7350061 B2 JP 7350061B2
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JP
Japan
Prior art keywords
methyl
oxy
pyridin
dichlorophenyl
piperidin
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JP2021513005A
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English (en)
Japanese (ja)
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JPWO2019215341A5 (https=
JP2021523941A (ja
JP2021523941A5 (https=
Inventor
マイケル アクステン,ジェフリー
チェン,ムイ
ピー. デマルチーノ,マイケル
アミー ガン,フイピン
フー,ヤン
ベイン ミラー,アーロン
クイン,ドンギ
ウー,チョンド
チャン,ジーリウ
リン,シャオジャン
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GlaxoSmithKline Intellectual Property Development Ltd
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GlaxoSmithKline Intellectual Property Development Ltd
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Publication of JP2021523941A publication Critical patent/JP2021523941A/ja
Publication of JPWO2019215341A5 publication Critical patent/JPWO2019215341A5/ja
Publication of JP2021523941A5 publication Critical patent/JP2021523941A5/ja
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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 chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic 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
    • C07D211/08Heterocyclic 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
    • C07D211/18Heterocyclic 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
    • C07D211/26Heterocyclic 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 with hydrocarbon radicals, substituted by nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72Nitrogen atoms
    • C07D213/76Nitrogen atoms to which a second hetero atom is attached
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Steroid Compounds (AREA)
JP2021513005A 2018-05-11 2019-05-10 フューリンインヒビター Active JP7350061B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862670050P 2018-05-11 2018-05-11
US62/670,050 2018-05-11
PCT/EP2019/062098 WO2019215341A1 (en) 2018-05-11 2019-05-10 Furin inhibitors

Publications (4)

Publication Number Publication Date
JP2021523941A JP2021523941A (ja) 2021-09-09
JPWO2019215341A5 JPWO2019215341A5 (https=) 2022-05-18
JP2021523941A5 JP2021523941A5 (https=) 2022-05-18
JP7350061B2 true JP7350061B2 (ja) 2023-10-02

Family

ID=66597541

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2021513005A Active JP7350061B2 (ja) 2018-05-11 2019-05-10 フューリンインヒビター

Country Status (12)

Country Link
US (1) US11773078B2 (https=)
EP (1) EP3790871B1 (https=)
JP (1) JP7350061B2 (https=)
KR (1) KR102823187B1 (https=)
CN (1) CN112384509B (https=)
AU (1) AU2019267166C1 (https=)
BR (1) BR112020022961A2 (https=)
CA (1) CA3099863A1 (https=)
IL (2) IL278642B2 (https=)
MX (1) MX2020012034A (https=)
SG (1) SG11202010914YA (https=)
WO (1) WO2019215341A1 (https=)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112384509B (zh) 2018-05-11 2024-04-30 葛兰素史密斯克莱知识产权发展有限公司 弗林蛋白酶抑制剂
WO2021097008A1 (en) * 2019-11-12 2021-05-20 Bp Asset V, Inc. Use of pyridyloxypyridines for treating infectious diseases
CA3157892A1 (en) * 2019-11-12 2021-05-20 Keith Wilcoxen Small molecule furin inhibitors for treating infectious diseases
WO2021097002A1 (en) * 2019-11-12 2021-05-20 Bp Asset V, Inc. Use of pyridyloxypyrimidines for treating infectious diseases
JP2023521032A (ja) * 2020-04-02 2023-05-23 ビーピー アセット ヴイ,インコーポレーテッド コロナウイルス感染症を処置するためのフーリンインヒビター
FR3110345B1 (fr) 2020-05-21 2024-03-29 Agence Francaise Pour Le Dev D’Al Ula Hydrolysat de protéines du tourteau des graines de Moringa peregrina pour son application en tant que médicament, son procédé d’obtention et compositions pharmaceutiques, dermatologiques et cosmétiques.
CN117222410A (zh) * 2021-02-03 2023-12-12 Bp资产V股份有限公司 用于吸入的弗林蛋白酶抑制剂的制剂
CN114853640A (zh) * 2022-05-12 2022-08-05 马鞍山昂扬新材料科技有限公司 2-溴乙基磺酸钠的制备方法
WO2024073576A1 (en) * 2022-09-29 2024-04-04 Bp Asset V, Inc. 4-((2-(3,5-dichlorophenyl)-6-((pyrimidin-5-yl)oxy)pyridin-4-yl)methyl)piperazine derivatives as furin inhibitors and uses thereof
DE102023126563A1 (de) * 2023-09-28 2025-04-03 Philipps-Universität Marburg, Körperschaft des öffentlichen Rechts Hemmstoffe der Proproteinkonvertase Furin, Verfahren zu deren Herstellung und Verwendung
CN119119096B (zh) * 2024-09-09 2025-09-16 郑州药领医药科技有限公司 一种4-((4,4,5,5-四甲基-1,3,2-二氧硼杂环戊烷-2-基)甲基)哌啶-1-甲酸叔丁酯的合成方法

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005047268A2 (en) 2003-11-10 2005-05-26 X-Ceptor Therapeutics, Inc. Substituted pyrimidine compositions and methods of use
WO2006031852A1 (en) 2004-09-13 2006-03-23 Amgen Inc. Vanilloid receptor ligands and their use in treatments
JP2006514118A (ja) 2002-11-21 2006-04-27 カイロン コーポレイション ホスホチジルイノシトール(pi)3−キナーゼインヒビターとしての2,4,6−三置換ピリミジン、および癌の処置におけるその使用
JP2011512380A (ja) 2008-02-22 2011-04-21 エフ.ホフマン−ラ ロシュ アーゲー アミロイドβの調節薬
WO2014031438A2 (en) 2012-08-20 2014-02-27 Merck Sharp & Dohme Corp. SUBSTITUTED PHENYL SPLEEN TYROSINE KINASE (Syk) INHIBITORS
JP2018510852A (ja) 2015-03-06 2018-04-19 ファーマケア,インク. リシルオキシダーゼ様2阻害剤とその使用

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1646160A (zh) 2002-03-13 2005-07-27 拜奥根Idec马萨诸塞公司 抗αvβ6抗体
CA2586086A1 (en) 2004-07-23 2006-01-23 Robert E.(Deceased) Smith Furin inhibitors
EP2155894A4 (en) 2007-05-09 2010-08-18 Burnham Inst Medical Research HOST PROTEINAS AS A TARGET FOR A THERAPEUTIC STRATEGY AGAINST VIRAL AND BACTERIAL DISEASES
CN107011359A (zh) 2010-10-18 2017-08-04 塞伦尼斯医疗控股有限公司 可用于胆固醇动员的化合物、组合物和方法
WO2013138666A1 (en) 2012-03-16 2013-09-19 Sanford-Burnham Medical Research Institute Inhibitors of furin and other pro-protein convertases
US9266828B2 (en) 2012-03-16 2016-02-23 Sanford-Burnham Medical Research Institute Inhibitors of Furin and other pro-protein convertases
WO2014152716A1 (en) 2013-03-15 2014-09-25 President And Fellows Of Harvard College Substituted heterocyclic compounds for treating or preventing viral infections
CN107441094B (zh) 2017-08-08 2020-05-22 南方医科大学 尼罗替尼作为治疗登革病毒感染的药物及其制药用途
CN112384509B (zh) 2018-05-11 2024-04-30 葛兰素史密斯克莱知识产权发展有限公司 弗林蛋白酶抑制剂
CA3157892A1 (en) 2019-11-12 2021-05-20 Keith Wilcoxen Small molecule furin inhibitors for treating infectious diseases

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006514118A (ja) 2002-11-21 2006-04-27 カイロン コーポレイション ホスホチジルイノシトール(pi)3−キナーゼインヒビターとしての2,4,6−三置換ピリミジン、および癌の処置におけるその使用
WO2005047268A2 (en) 2003-11-10 2005-05-26 X-Ceptor Therapeutics, Inc. Substituted pyrimidine compositions and methods of use
WO2006031852A1 (en) 2004-09-13 2006-03-23 Amgen Inc. Vanilloid receptor ligands and their use in treatments
JP2011512380A (ja) 2008-02-22 2011-04-21 エフ.ホフマン−ラ ロシュ アーゲー アミロイドβの調節薬
WO2014031438A2 (en) 2012-08-20 2014-02-27 Merck Sharp & Dohme Corp. SUBSTITUTED PHENYL SPLEEN TYROSINE KINASE (Syk) INHIBITORS
JP2018510852A (ja) 2015-03-06 2018-04-19 ファーマケア,インク. リシルオキシダーゼ様2阻害剤とその使用

Also Published As

Publication number Publication date
AU2019267166A1 (en) 2020-11-26
IL302997B1 (en) 2024-04-01
IL278642B2 (en) 2023-10-01
IL302997A (en) 2023-07-01
IL278642A (https=) 2020-12-31
IL278642B1 (en) 2023-06-01
BR112020022961A2 (pt) 2021-02-17
KR102823187B1 (ko) 2025-06-20
KR20210021298A (ko) 2021-02-25
CA3099863A1 (en) 2019-11-14
EP3790871A1 (en) 2021-03-17
EP3790871C0 (en) 2024-01-24
CN112384509A (zh) 2021-02-19
US11773078B2 (en) 2023-10-03
CN112384509B (zh) 2024-04-30
EP3790871B1 (en) 2024-01-24
MX2020012034A (es) 2021-04-12
SG11202010914YA (en) 2020-12-30
JP2021523941A (ja) 2021-09-09
AU2019267166B2 (en) 2023-06-15
AU2019267166C1 (en) 2023-11-30
WO2019215341A1 (en) 2019-11-14
US20220315556A1 (en) 2022-10-06
IL302997B2 (en) 2024-08-01

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