CN112513024A - Tlr7/8拮抗剂及其用途 - Google Patents

Tlr7/8拮抗剂及其用途 Download PDF

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Publication number
CN112513024A
CN112513024A CN201980051004.3A CN201980051004A CN112513024A CN 112513024 A CN112513024 A CN 112513024A CN 201980051004 A CN201980051004 A CN 201980051004A CN 112513024 A CN112513024 A CN 112513024A
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CN
China
Prior art keywords
compound
methyl
pharmaceutically acceptable
acceptable salt
piperidin
Prior art date
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Pending
Application number
CN201980051004.3A
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English (en)
Chinese (zh)
Inventor
B·舍雷尔
兰若曦
N·布鲁格
陈晓玲
M·图雷
E·克莱里
L·C·德塞尔姆
王艳平
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Merck Patent GmbH
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Merck Patent GmbH
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Publication date
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Publication of CN112513024A publication Critical patent/CN112513024A/zh
Pending legal-status Critical Current

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    • 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
    • C07D401/02—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
    • 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)
CN201980051004.3A 2018-07-31 2019-07-29 Tlr7/8拮抗剂及其用途 Pending CN112513024A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862712439P 2018-07-31 2018-07-31
US62/712439 2018-07-31
PCT/EP2019/070312 WO2020025517A1 (en) 2018-07-31 2019-07-29 Tlr7/8 antagonists and uses thereof

Publications (1)

Publication Number Publication Date
CN112513024A true CN112513024A (zh) 2021-03-16

Family

ID=67660056

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201980051004.3A Pending CN112513024A (zh) 2018-07-31 2019-07-29 Tlr7/8拮抗剂及其用途

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) TWI827641B (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
CA3005766A1 (en) 2015-12-17 2017-06-22 Merck Patent Gmbh Polycyclic tlr7/8 antagonists and use thereof in the treatment of immune disorders
JP7125385B2 (ja) 2016-08-08 2022-08-24 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｔｌｒ７／８アンタゴニストおよびそれらの使用
SG11202005547YA (en) * 2017-12-19 2020-07-29 Merck Patent Gmbh Tlr7/8 antagonists and uses thereof
JPWO2020203609A1 (https=) * 2019-03-29 2020-10-08
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
EP4031539A1 (en) * 2019-09-16 2022-07-27 F. Hoffmann-La Roche AG Piperidinyl amine compounds for the treatment of autoimmune disease
KR20220122637A (ko) 2019-11-28 2022-09-02 바이엘 악티엔게젤샤프트 면역 활성화를 위한 dgk알파 억제제로서의 치환된 아미노퀴놀론
JP7832124B2 (ja) * 2020-05-14 2026-03-17 メルク ヘルスケア コマンディトゲゼルシャフト アウフ アクティーン コロナウイルス感染症治療のためのｔｌｒ７／８拮抗薬
CN116745291A (zh) 2020-12-17 2023-09-12 阿斯利康(瑞典)有限公司 N-(2-(4-氰基噻唑烷-3-基)-2-氧代乙基)-喹啉-4-甲酰胺
CR20230478A (es) 2021-04-16 2023-11-30 Gilead Sciences Inc Compuestos de tienopirrol.
KR20240056747A (ko) 2021-09-10 2024-04-30 길리애드 사이언시즈, 인코포레이티드 티에노피롤 화합물
WO2024153063A1 (zh) * 2023-01-18 2024-07-25 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)

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Publication number Priority date Publication date Assignee Title
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
CN105636945A (zh) * 2013-10-14 2016-06-01 卫材R&D管理有限公司 选择性取代的喹啉化合物
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
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

Family Cites Families (5)

* 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
CA2929461A1 (en) 2013-11-12 2015-05-21 F. Hoffmann-La Roche Ag Pyrido[4,3-b]pyrazine-2-carboxamides as neurogenic agents for the treatment of neurodegenerative disorders
EP3655401B1 (en) 2017-07-18 2023-09-06 Merck Patent GmbH Tlr7/8 antagonists and uses thereof
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
SG11202005547YA (en) 2017-12-19 2020-07-29 Merck Patent Gmbh Tlr7/8 antagonists and uses thereof

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105636945A (zh) * 2013-10-14 2016-06-01 卫材R&D管理有限公司 选择性取代的喹啉化合物
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
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
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
MX2024013464A (es) 2024-12-06
KR20210040085A (ko) 2021-04-12
WO2020025517A1 (en) 2020-02-06
KR102947440B1 (ko) 2026-04-03
JP2024105611A (ja) 2024-08-06
TW202542153A (zh) 2025-11-01
AU2019313441B2 (en) 2024-05-23
KR20260047300A (ko) 2026-04-07
IL280479A (en) 2021-03-01
BR112021001618A2 (pt) 2021-04-27
TW202019899A (zh) 2020-06-01
US20210300940A1 (en) 2021-09-30
JP7491900B2 (ja) 2024-05-28
TW202423913A (zh) 2024-06-16
EP3830080A1 (en) 2021-06-09
AU2019313441A1 (en) 2021-03-18
CA3108099A1 (en) 2020-02-06
SG11202100818RA (en) 2021-02-25
JP2021533125A (ja) 2021-12-02
BR122023023308A2 (pt) 2024-02-20
TWI827641B (zh) 2024-01-01
AU2024203629A1 (en) 2024-06-20
TWI880472B (zh) 2025-04-11
MX2021000093A (es) 2021-03-25

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