JP7491900B2 - Tlr7/8アンタゴニストおよびそれらの使用 - Google Patents

Tlr7/8アンタゴニストおよびそれらの使用 Download PDF

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JP7491900B2
JP7491900B2 JP2021505638A JP2021505638A JP7491900B2 JP 7491900 B2 JP7491900 B2 JP 7491900B2 JP 2021505638 A JP2021505638 A JP 2021505638A JP 2021505638 A JP2021505638 A JP 2021505638A JP 7491900 B2 JP7491900 B2 JP 7491900B2
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methyl
piperidin
mmol
trifluoromethyl
compound
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JP2021533125A5 (https=
JPWO2020025517A5 (https=
JP2021533125A (ja
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シェーラー,ブライアン
ラン,ルォックシ
ブルガー,ナディア
チェン,シアオリン
トウレ,モマール
クリアリー,エスター
セレステ デゼルム,リスベズ
ワン,イエンピン
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Merck Patent GmbH
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Merck Patent GmbH
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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
    • C07D401/02Heterocyclic 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
    • 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
    • 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
    • A61P35/00Antineoplastic agents
    • 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
    • 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)
JP2021505638A 2018-07-31 2019-07-29 Tlr7/8アンタゴニストおよびそれらの使用 Active JP7491900B2 (ja)

Priority Applications (1)

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JP2024080418A JP2024105611A (ja) 2018-07-31 2024-05-16 Tlr7/8アンタゴニストおよびそれらの使用

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

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Publications (4)

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JP2021533125A JP2021533125A (ja) 2021-12-02
JP2021533125A5 JP2021533125A5 (https=) 2022-08-08
JPWO2020025517A5 JPWO2020025517A5 (https=) 2022-08-08
JP7491900B2 true JP7491900B2 (ja) 2024-05-28

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JP2024080418A Pending JP2024105611A (ja) 2018-07-31 2024-05-16 Tlr7/8アンタゴニストおよびそれらの使用

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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=)

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* 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

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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
JP2016536320A (ja) 2013-11-12 2016-11-24 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft 神経変性疾患の処置用の神経新生薬としてのピリド[4,3−b]ピラジン−2−カルボキサミド
JP2016539079A (ja) 2013-10-14 2016-12-15 エーザイ・アール・アンド・ディー・マネジメント株式会社 選択的に置換されたキノリン化合物
WO2017004405A1 (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
JP2020527577A (ja) 2017-07-18 2020-09-10 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Merck Patent Gesellschaft mit beschraenkter Haftung Tlr7/8アンタゴニストおよびそれらの使用
JP2021506862A (ja) 2017-12-19 2021-02-22 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Merck Patent Gesellschaft mit beschraenkter Haftung Tlr7/8アンタゴニストおよびそれらの使用

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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
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

Patent Citations (9)

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Publication number Priority date Publication date Assignee Title
JP2016539079A (ja) 2013-10-14 2016-12-15 エーザイ・アール・アンド・ディー・マネジメント株式会社 選択的に置換されたキノリン化合物
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
JP2016536320A (ja) 2013-11-12 2016-11-24 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft 神経変性疾患の処置用の神経新生薬としてのピリド[4,3−b]ピラジン−2−カルボキサミド
WO2017004405A1 (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
JP2020527577A (ja) 2017-07-18 2020-09-10 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Merck Patent Gesellschaft mit beschraenkter Haftung Tlr7/8アンタゴニストおよびそれらの使用
JP2021506862A (ja) 2017-12-19 2021-02-22 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Merck Patent Gesellschaft mit beschraenkter Haftung Tlr7/8アンタゴニストおよびそれらの使用

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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
CN112513024A (zh) 2021-03-16
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
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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