AU2019267166C1 - Furin inhibitors - Google Patents

Furin inhibitors Download PDF

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Publication number
AU2019267166C1
AU2019267166C1 AU2019267166A AU2019267166A AU2019267166C1 AU 2019267166 C1 AU2019267166 C1 AU 2019267166C1 AU 2019267166 A AU2019267166 A AU 2019267166A AU 2019267166 A AU2019267166 A AU 2019267166A AU 2019267166 C1 AU2019267166 C1 AU 2019267166C1
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AU
Australia
Prior art keywords
methyl
pyridin
oxy
dichlorophenyl
piperidin
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Active
Application number
AU2019267166A
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English (en)
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AU2019267166A1 (en
AU2019267166B2 (en
Inventor
Jeffrey Michael Axten
Mui Cheung
Michael P. Demartino
Huiping Amy Guan
Yan Hu
Xiaojuan Lin
Aaron Bayne Miller
Donghui Qin
Chengde Wu
Zhiliu Zhang
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
GlaxoSmithKline Intellectual Property Development Ltd
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GlaxoSmithKline Intellectual Property Development Ltd
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Publication of AU2019267166A1 publication Critical patent/AU2019267166A1/en
Publication of AU2019267166B2 publication Critical patent/AU2019267166B2/en
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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)
AU2019267166A 2018-05-11 2019-05-10 Furin inhibitors Active AU2019267166C1 (en)

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 (3)

Publication Number Publication Date
AU2019267166A1 AU2019267166A1 (en) 2020-11-26
AU2019267166B2 AU2019267166B2 (en) 2023-06-15
AU2019267166C1 true AU2019267166C1 (en) 2023-11-30

Family

ID=66597541

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2019267166A Active AU2019267166C1 (en) 2018-05-11 2019-05-10 Furin inhibitors

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 (1)

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WO2016144702A1 (en) * 2015-03-06 2016-09-15 Pharmakea, Inc. Lysyl oxidase-like 2 inhibitors and uses thereof

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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
MX2010008700A (es) 2008-02-22 2010-08-30 Hoffmann La Roche Moduladores de beta-amiloide.
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
EP2884982B1 (en) * 2012-08-20 2017-09-20 Merck Sharp & Dohme Corp. SUBSTITUTED PHENYL SPLEEN TYROSINE KINASE (Syk) INHIBITORS
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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

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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
JP7350061B2 (ja) 2023-10-02
JP2021523941A (ja) 2021-09-09
AU2019267166B2 (en) 2023-06-15
WO2019215341A1 (en) 2019-11-14
US20220315556A1 (en) 2022-10-06
IL302997B2 (en) 2024-08-01

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