KR20260047300A - Tlr7/8 안타고니스트 및 이의 용도 - Google Patents

Tlr7/8 안타고니스트 및 이의 용도

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Publication number
KR20260047300A
KR20260047300A KR1020267009849A KR20267009849A KR20260047300A KR 20260047300 A KR20260047300 A KR 20260047300A KR 1020267009849 A KR1020267009849 A KR 1020267009849A KR 20267009849 A KR20267009849 A KR 20267009849A KR 20260047300 A KR20260047300 A KR 20260047300A
Authority
KR
South Korea
Prior art keywords
compound
methyl
trifluoromethyl
pharmaceutically acceptable
piperidine
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
KR1020267009849A
Other languages
English (en)
Korean (ko)
Inventor
브라이언 셰러
록시 랜
나디아 브루거
샤오링 첸
모마르 뚜레
에스더 클리어리
리즈베스 셀레스트 데셀름
왕얀핑
Original Assignee
메르크 파텐트 게엠베하
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 메르크 파텐트 게엠베하 filed Critical 메르크 파텐트 게엠베하
Publication of KR20260047300A publication Critical patent/KR20260047300A/ko
Pending legal-status Critical Current

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    • 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
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non 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
    • 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • 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
    • A61K31/498Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • 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
    • 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
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic 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
    • 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
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic 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
    • C07D495/10Spiro-condensed systems
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against 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)
KR1020267009849A 2018-07-31 2019-07-29 Tlr7/8 안타고니스트 및 이의 용도 Pending KR20260047300A (ko)

Applications Claiming Priority (4)

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
KR1020217005440A KR102947440B1 (ko) 2018-07-31 2019-07-29 Tlr7/8 안타고니스트 및 이의 용도

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
KR1020217005440A Division KR102947440B1 (ko) 2018-07-31 2019-07-29 Tlr7/8 안타고니스트 및 이의 용도

Publications (1)

Publication Number Publication Date
KR20260047300A true KR20260047300A (ko) 2026-04-07

Family

ID=67660056

Family Applications (2)

Application Number Title Priority Date Filing Date
KR1020267009849A Pending KR20260047300A (ko) 2018-07-31 2019-07-29 Tlr7/8 안타고니스트 및 이의 용도
KR1020217005440A Active KR102947440B1 (ko) 2018-07-31 2019-07-29 Tlr7/8 안타고니스트 및 이의 용도

Family Applications After (1)

Application Number Title Priority Date Filing Date
KR1020217005440A Active KR102947440B1 (ko) 2018-07-31 2019-07-29 Tlr7/8 안타고니스트 및 이의 용도

Country Status (13)

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

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

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI529171B (zh) * 2013-07-29 2016-04-11 赫孚孟拉羅股份公司 1,7-萘啶衍生物
ES2670550T3 (es) 2013-10-14 2018-05-30 Eisai R&D Management Co., Ltd. Derivados de quinolina selectivamente sustituidos
CN104557913B (zh) * 2013-10-28 2017-02-08 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
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.
CN108290855A (zh) * 2015-07-01 2018-07-17 西北大学 被取代的喹唑啉化合物及其调节葡糖脑苷脂酶活性的用途
WO2017031427A1 (en) * 2015-08-19 2017-02-23 3-V Biosciences, Inc. COMPOUNDS AND METHODS FOR INHIBITING mTOR
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
CN106632089B (zh) * 2016-11-04 2019-06-18 中山大学 一类喹唑啉类化合物及其制备方法与应用
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

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
AU2019313441B2 (en) 2024-05-23
WO2020025517A1 (en) 2020-02-06
KR20210040085A (ko) 2021-04-12
US20210300940A1 (en) 2021-09-30
MX2021000093A (es) 2021-03-25
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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