AU2019313441B2 - TLR7/8 antagonists and uses thereof - Google Patents

TLR7/8 antagonists and uses thereof Download PDF

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Publication number
AU2019313441B2
AU2019313441B2 AU2019313441A AU2019313441A AU2019313441B2 AU 2019313441 B2 AU2019313441 B2 AU 2019313441B2 AU 2019313441 A AU2019313441 A AU 2019313441A AU 2019313441 A AU2019313441 A AU 2019313441A AU 2019313441 B2 AU2019313441 B2 AU 2019313441B2
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methyl
piperidin
trifluoromethyl
mmol
compound
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AU2019313441A1 (en
Inventor
Nadia Brugger
Xiaoling Chen
Esther Cleary
Lizbeth Celeste DESELM
Ruoxi Lan
Brian Sherer
Momar TOURE
Yanping Wang
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Merck Patent GmbH
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Merck Patent GmbH
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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
    • C07D401/04—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
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/10—Spiro-condensed 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
    • A61K31/435—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
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • 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
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • A61K31/535—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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C07D405/14—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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
    • C07D413/14—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
    • C07D417/14—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 three or more hetero rings
    • 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
    • C07D471/02—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
    • C07D471/10—Spiro-condensed systems
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
AU2019313441A 2018-07-31 2019-07-29 TLR7/8 antagonists and uses thereof Active AU2019313441B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2024203629A AU2024203629A1 (en) 2018-07-31 2024-05-30 TLR7/8 antagonists and uses thereof

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862712439P 2018-07-31 2018-07-31
US62/712,439 2018-07-31
PCT/EP2019/070312 WO2020025517A1 (en) 2018-07-31 2019-07-29 Tlr7/8 antagonists and uses thereof

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2024203629A Division AU2024203629A1 (en) 2018-07-31 2024-05-30 TLR7/8 antagonists and uses thereof

Publications (2)

Publication Number Publication Date
AU2019313441A1 AU2019313441A1 (en) 2021-03-18
AU2019313441B2 true AU2019313441B2 (en) 2024-05-23

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AU2019313441A Active AU2019313441B2 (en) 2018-07-31 2019-07-29 TLR7/8 antagonists and uses thereof
AU2024203629A Pending AU2024203629A1 (en) 2018-07-31 2024-05-30 TLR7/8 antagonists and uses thereof

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Country Status (13)

Country Link
US (1) US20210300940A1 (enExample)
EP (1) EP3830080A1 (enExample)
JP (2) JP7491900B2 (enExample)
KR (2) KR20260047300A (enExample)
CN (1) CN112513024A (enExample)
AU (2) AU2019313441B2 (enExample)
BR (2) BR122023023308A2 (enExample)
CA (1) CA3108099A1 (enExample)
IL (1) IL280479A (enExample)
MX (2) MX2021000093A (enExample)
SG (1) SG11202100818RA (enExample)
TW (3) TW202542153A (enExample)
WO (1) WO2020025517A1 (enExample)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT3889145T (pt) * 2015-12-17 2024-04-02 Merck Patent Gmbh 8-ciano-5-piperidino-quinolinas como antagonistas de tlr7/8 e suas utilizações para tratamento de distúrbios imunitários
EP4198031A1 (en) 2016-08-08 2023-06-21 Merck Patent GmbH Tlr7/8 antagonists and uses thereof
CN111511729A (zh) * 2017-12-19 2020-08-07 默克专利股份公司 Tlr7/8拮抗剂及其用途
AU2020250468A1 (en) * 2019-03-29 2021-11-04 Kinki University Use of T-type calcium channel blocker for treating pruritus
JP2022081710A (ja) * 2019-03-29 2022-06-01 ユーティアイ リミテッド パートナーシップ 関節リウマチを治療するためのｔ型カルシウムチャネル阻害剤の使用
WO2021052892A1 (en) * 2019-09-16 2021-03-25 F. Hoffmann-La Roche Ag Piperidinyl amine compounds for the treatment of autoimmune disease
CR20220236A (es) 2019-11-28 2022-10-03 Bayer Pharma AG Aminoquinolonas sustituidas como inhibidores de dgk alfa para la activación inmune
TW202200139A (zh) * 2020-05-14 2022-01-01 德商馬克專利公司 用於治療冠狀病毒感染之tlr7/8拮抗劑
EP4263535A1 (en) 2020-12-17 2023-10-25 Astrazeneca AB N-(2-(4-cyanothiazolidin-3-yl)-2-oxoethyl)- quinoline-4-carboxamides
KR20230171469A (ko) 2021-04-16 2023-12-20 길리애드 사이언시즈, 인코포레이티드 티에노피롤 화합물
EP4398989A1 (en) 2021-09-10 2024-07-17 Gilead Sciences, Inc. Thienopyrrole compounds
CN120603821A (zh) * 2023-01-18 2025-09-05 苏州科睿思制药有限公司 Enpatoran的晶型及其制备方法和用途

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015057655A1 (en) * 2013-10-14 2015-04-23 Eisai R&D Management Co., Ltd. Selectively substituted quinoline compounds
CN104557913A (zh) * 2013-10-28 2015-04-29 上海汇伦生命科技有限公司 吡啶并嘧啶类化合物，其制备方法和用途
US20170001976A1 (en) * 2015-07-01 2017-01-05 Northwestern University Substituted quinazoline compounds and uses thereof for modulating glucocerebrosidase activity
WO2017031427A1 (en) * 2015-08-19 2017-02-23 3-V Biosciences, Inc. COMPOUNDS AND METHODS FOR INHIBITING mTOR
CN106632089A (zh) * 2016-11-04 2017-05-10 中山大学 一类喹唑啉类化合物及其制备方法与应用
WO2017106607A1 (en) * 2015-12-17 2017-06-22 Merck Patent Gmbh Polycyclic tlr7/8 antagonists and use thereof in the treatment of immune disorders

Family Cites Families (5)

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TWI529171B (zh) * 2013-07-29 2016-04-11 赫孚孟拉羅股份公司 １，７－萘啶衍生物
MX2016006052A (es) 2013-11-12 2016-07-18 Hoffmann La Roche Pirido[4,3-b]pirazin-2-carboxamidas como agentes neurogenicos para el tratamiento de trastornos neurodegenerativos.
ES2965044T3 (es) 2017-07-18 2024-04-10 Merck Patent Gmbh Antagonistas de TLR7/8 y sus usos
CN111801015B (zh) * 2017-12-12 2022-03-18 先正达参股股份有限公司 植物生长调节
CN111511729A (zh) 2017-12-19 2020-08-07 默克专利股份公司 Tlr7/8拮抗剂及其用途

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015057655A1 (en) * 2013-10-14 2015-04-23 Eisai R&D Management Co., Ltd. Selectively substituted quinoline compounds
CN104557913A (zh) * 2013-10-28 2015-04-29 上海汇伦生命科技有限公司 吡啶并嘧啶类化合物，其制备方法和用途
US20170001976A1 (en) * 2015-07-01 2017-01-05 Northwestern University Substituted quinazoline compounds and uses thereof for modulating glucocerebrosidase activity
WO2017031427A1 (en) * 2015-08-19 2017-02-23 3-V Biosciences, Inc. COMPOUNDS AND METHODS FOR INHIBITING mTOR
WO2017106607A1 (en) * 2015-12-17 2017-06-22 Merck Patent Gmbh Polycyclic tlr7/8 antagonists and use thereof in the treatment of immune disorders
CN106632089A (zh) * 2016-11-04 2017-05-10 中山大学 一类喹唑啉类化合物及其制备方法与应用

Also Published As

Publication number Publication date
AU2024203629A1 (en) 2024-06-20
JP2024105611A (ja) 2024-08-06
TWI880472B (zh) 2025-04-11
EP3830080A1 (en) 2021-06-09
TW202542153A (zh) 2025-11-01
JP7491900B2 (ja) 2024-05-28
TW202019899A (zh) 2020-06-01
IL280479A (en) 2021-03-01
BR122023023308A2 (pt) 2024-02-20
CN112513024A (zh) 2021-03-16
AU2019313441A1 (en) 2021-03-18
SG11202100818RA (en) 2021-02-25
TWI827641B (zh) 2024-01-01
BR112021001618A2 (pt) 2021-04-27
WO2020025517A1 (en) 2020-02-06
KR20210040085A (ko) 2021-04-12
US20210300940A1 (en) 2021-09-30
MX2021000093A (es) 2021-03-25
KR20260047300A (ko) 2026-04-07
JP2021533125A (ja) 2021-12-02
KR102947440B1 (ko) 2026-04-03
MX2024013464A (es) 2024-12-06
CA3108099A1 (en) 2020-02-06
TW202423913A (zh) 2024-06-16

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