CN112384509B - 弗林蛋白酶抑制剂 - Google Patents

弗林蛋白酶抑制剂 Download PDF

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Publication number
CN112384509B
CN112384509B CN201980046497.1A CN201980046497A CN112384509B CN 112384509 B CN112384509 B CN 112384509B CN 201980046497 A CN201980046497 A CN 201980046497A CN 112384509 B CN112384509 B CN 112384509B
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CN
China
Prior art keywords
methyl
pyridin
oxy
dichlorophenyl
piperidin
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CN201980046497.1A
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English (en)
Chinese (zh)
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CN112384509A (zh
Inventor
J.M.阿克斯坦
M.张
M.P.德马蒂诺
H.A.关
Y.胡
A.B.米勒
D.秦
C.吴
Z.张
X.林
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GlaxoSmithKline Intellectual Property Development Ltd
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GlaxoSmithKline Intellectual Property Development Ltd
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    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • 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
    • 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
    • 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
    • A61K31/435—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
    • 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
    • A61K31/435—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
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D211/26—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 with hydrocarbon radicals, substituted by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic 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
    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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
    • C07D213/72—Nitrogen atoms
    • C07D213/76—Nitrogen atoms to which a second hetero atom is attached
    • 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
    • C07D413/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/08—Bridged 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)
CN201980046497.1A 2018-05-11 2019-05-10 弗林蛋白酶抑制剂 Active CN112384509B (zh)

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 (2)

Publication Number Publication Date
CN112384509A CN112384509A (zh) 2021-02-19
CN112384509B true CN112384509B (zh) 2024-04-30

Family

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CN201980046497.1A Active CN112384509B (zh) 2018-05-11 2019-05-10 弗林蛋白酶抑制剂

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 (2)

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CN101952275A (zh) * 2008-02-22 2011-01-19 弗·哈夫曼-拉罗切有限公司 β-淀粉样蛋白的调节剂
CN107624110A (zh) * 2015-03-06 2018-01-23 法玛克亚公司 赖氨酰氧化酶样2抑制剂及其用途

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CN1646160A (zh) 2002-03-13 2005-07-27 拜奥根Idec马萨诸塞公司 抗αvβ6抗体
US7423148B2 (en) 2002-11-21 2008-09-09 Chiron Corporation Small molecule PI 3-kinase inhibitors and methods of their use
WO2005047268A2 (en) 2003-11-10 2005-05-26 X-Ceptor Therapeutics, Inc. Substituted pyrimidine compositions and methods of use
CA2586086A1 (en) 2004-07-23 2006-01-23 Robert E.(Deceased) Smith Furin inhibitors
EP1789413A1 (en) * 2004-09-13 2007-05-30 Amgen Inc. Vanilloid receptor ligands and their use in treatments
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
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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 (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101952275A (zh) * 2008-02-22 2011-01-19 弗·哈夫曼-拉罗切有限公司 β-淀粉样蛋白的调节剂
CN107624110A (zh) * 2015-03-06 2018-01-23 法玛克亚公司 赖氨酰氧化酶样2抑制剂及其用途

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
EP3790871B1 (en) 2024-01-24
MX2020012034A (es) 2021-04-12
SG11202010914YA (en) 2020-12-30
JP7350061B2 (ja) 2023-10-02
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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