CN106573920B - 用于在流感病毒感染中使用的吲哚 - Google Patents

用于在流感病毒感染中使用的吲哚 Download PDF

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Publication number
CN106573920B
CN106573920B CN201580042406.9A CN201580042406A CN106573920B CN 106573920 B CN106573920 B CN 106573920B CN 201580042406 A CN201580042406 A CN 201580042406A CN 106573920 B CN106573920 B CN 106573920B
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mmol
amino
methyl
mixture
fluoro
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Expired - Fee Related
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CN201580042406.9A
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Chinese (zh)
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CN106573920A (zh
Inventor
T.H.M.琼克斯
P.J-M.B.拉伯瓦森
J.E.G.圭莱蒙
D.C.麦克戈万
W.C.J.恩布雷希茨
L.P.库伊曼斯
A.B.米绍
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Janssen R&D Ireland ULC
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Janssen R&D Ireland ULC
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Pulmonology (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
CN201580042406.9A 2014-08-08 2015-08-07 用于在流感病毒感染中使用的吲哚 Expired - Fee Related CN106573920B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP14180331.2 2014-08-08
EP14180331 2014-08-08
PCT/EP2015/068257 WO2016020526A1 (en) 2014-08-08 2015-08-07 Indoles for use in influenza virus infection

Publications (2)

Publication Number Publication Date
CN106573920A CN106573920A (zh) 2017-04-19
CN106573920B true CN106573920B (zh) 2020-11-10

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CN201580042406.9A Expired - Fee Related CN106573920B (zh) 2014-08-08 2015-08-07 用于在流感病毒感染中使用的吲哚

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Country Link
US (1) US10597390B2 (enExample)
EP (1) EP3177609A1 (enExample)
JP (1) JP6577570B2 (enExample)
KR (1) KR102488479B1 (enExample)
CN (1) CN106573920B (enExample)
AU (1) AU2015298876B2 (enExample)
BR (1) BR112017002370B1 (enExample)
CA (1) CA2954751C (enExample)
CL (1) CL2017000309A1 (enExample)
EA (1) EA201790266A1 (enExample)
IL (1) IL250408B (enExample)
MA (1) MA40547A (enExample)
MX (1) MX381488B (enExample)
PH (1) PH12017500207B1 (enExample)
SG (1) SG11201700956VA (enExample)
UA (1) UA124609C2 (enExample)
WO (1) WO2016020526A1 (enExample)
ZA (1) ZA201700952B (enExample)

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GEAP202213376A (en) 2009-06-17 2022-02-25 Vertex Pharmaceuticals Incorporated Us Inhibitors of influenza viruses replication
UA118010C2 (uk) 2011-08-01 2018-11-12 Вертекс Фармасьютікалз Інкорпорейтед Інгібітори реплікації вірусів грипу
MA40547A (fr) 2014-08-08 2017-06-14 Janssen Sciences Ireland Uc Indoles pouvant être utilisés dans l'infection par le virus influenza
WO2016183116A1 (en) 2015-05-13 2016-11-17 Vertex Pharmaceuticals Incorporated Methods of preparing inhibitors of influenza viruses replication
JP6857617B2 (ja) 2015-05-13 2021-04-14 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ インフルエンザウイルスの複製の阻害剤
JP6952695B2 (ja) 2015-12-09 2021-10-20 サンシャイン・レイク・ファーマ・カンパニー・リミテッドＳｕｎｓｈｉｎｅ Ｌａｋｅ Ｐｈａｒｍａ Ｃｏ．，Ｌｔｄ． インフルエンザウイルス複製の阻害剤、その適用方法および使用
KR20180099839A (ko) * 2016-01-07 2018-09-05 얀센 사이언시즈 아일랜드 유씨 인플루엔자 바이러스 감염에서 사용하기 위한 작용화된 펜탄산
WO2017133670A1 (en) * 2016-02-05 2017-08-10 Savira Pharmaceuticals Gmbh Pyridine and pyrimidine derivatives and their use in treatment, amelioration or prevention of influenza
WO2018033082A1 (en) * 2016-08-16 2018-02-22 Sunshine Lake Pharma Co., Ltd. Inhibitors of influenza virus replication, application methods and uses thereof
WO2018041091A1 (en) * 2016-08-30 2018-03-08 Sunshine Lake Pharma Co., Ltd. Inhibitors of influenza virus replication, application methods and uses thereof
KR102312088B1 (ko) * 2016-09-05 2021-10-14 광둥 레이노벤트 바이오테크 컴퍼니 리미티드 항인플루엔자 바이러스 피리미딘 유도체
EP3555095B1 (en) 2016-12-15 2023-04-12 Sunshine Lake Pharma Co., Ltd. Inhibitors of influenza virus replication and uses thereof
CA3047404A1 (en) * 2016-12-23 2018-06-28 Aquinnah Pharmaceuticals, Inc. Compounds, compositions and methods of use
WO2018127096A1 (en) 2017-01-05 2018-07-12 Sunshine Lake Pharma Co., Ltd. Inhibitors of influenza virus replication and uses thereof
US10927118B2 (en) 2017-03-02 2021-02-23 Sunshine Lake Pharma Co., Ltd. Inhibitors of influenza virus replication and uses thereof
CN108727369B (zh) * 2017-04-25 2023-06-09 广东东阳光药业有限公司 流感病毒复制抑制剂及其用途
CA3092315C (en) 2018-03-05 2023-08-29 Jian Xiong Crystal form and salt form of pyridopyrazole compound and preparation method therefor
EP3992192B1 (en) 2019-07-22 2026-02-18 Guangdong Raynovent Biotech Co., Ltd. Dominant salt forms of pyrimidine derivatives, and crystal forms thereof
CN113045475A (zh) * 2019-12-27 2021-06-29 上海泓博智源医药股份有限公司 一种5-溴-7-甲基吲哚的制备方法
AU2021313150A1 (en) * 2020-07-20 2023-03-16 Nido Biosciences, Inc. Indole compounds as androgen receptor modulators
US20240010643A1 (en) * 2020-09-18 2024-01-11 Sunshine Lake Pharma Co., Ltd. Preparation method of substituted pyrimidine piperazine compounds
AU2023361174A1 (en) * 2022-10-12 2025-05-01 Maze Therapeutics, Inc. Inhibitors of solute carrier family 6a member 19 (slc6a19) and methods of use thereof

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010148197A1 (en) * 2009-06-17 2010-12-23 Vertex Pharmaceuticals Incorporated Inhibitors of influenza viruses replication
WO2012032065A1 (en) * 2010-09-08 2012-03-15 Glaxo Group Limited Indazole derivatives for use in the treatment of influenza virus infection
CN103562205A (zh) * 2010-12-16 2014-02-05 沃泰克斯药物股份有限公司 流感病毒复制的抑制剂
CN103764654A (zh) * 2011-08-01 2014-04-30 沃泰克斯药物股份有限公司 流感病毒复制抑制剂

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NZ584499A (en) 2004-03-30 2011-08-26 Vertex Pharma Azaindoles Useful as Inhibitors of Jak and Other Protein Kinases
AR060316A1 (es) 2006-01-17 2008-06-11 Vertex Pharma Azaindoles de utilidad como inhibidores de janus quinasas
CN103492381A (zh) * 2010-12-16 2014-01-01 沃泰克斯药物股份有限公司 流感病毒复制的抑制剂
EP2763990B1 (en) 2011-09-01 2017-02-22 F. Hoffmann-La Roche AG Pyrrolopyrazine kinase inhibitors
EP2858984A1 (en) * 2012-06-08 2015-04-15 Vertex Pharmaceuticals Inc. Inhibitors of influenza viruses replication
LT3068776T (lt) 2013-11-13 2019-08-12 Vertex Pharmaceuticals Incorporated Gripo virusų replikacijos inhibitoriai
MA40547A (fr) 2014-08-08 2017-06-14 Janssen Sciences Ireland Uc Indoles pouvant être utilisés dans l'infection par le virus influenza
UY36249A (es) 2014-08-08 2016-01-29 Bayer Cropscience Ag Compuestos sustituidos con halógeno novedosos
AR101448A1 (es) 2014-08-08 2016-12-21 Bayer Cropscience Ag Compuestos sustituidos por halógeno
CN104592038A (zh) 2015-01-12 2015-05-06 烟台万润精细化工股份有限公司 一种5,5-二甲基-1,3-环己二胺的制备方法

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010148197A1 (en) * 2009-06-17 2010-12-23 Vertex Pharmaceuticals Incorporated Inhibitors of influenza viruses replication
WO2012032065A1 (en) * 2010-09-08 2012-03-15 Glaxo Group Limited Indazole derivatives for use in the treatment of influenza virus infection
CN103562205A (zh) * 2010-12-16 2014-02-05 沃泰克斯药物股份有限公司 流感病毒复制的抑制剂
CN103764654A (zh) * 2011-08-01 2014-04-30 沃泰克斯药物股份有限公司 流感病毒复制抑制剂

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PH12017500207A1 (en) 2017-07-10
CA2954751C (en) 2023-01-17
KR102488479B1 (ko) 2023-01-12
ZA201700952B (en) 2018-12-19
SG11201700956VA (en) 2017-03-30
IL250408A0 (en) 2017-03-30
MX381488B (es) 2025-03-12
WO2016020526A1 (en) 2016-02-11
IL250408B (en) 2020-08-31
JP2017523225A (ja) 2017-08-17
CN106573920A (zh) 2017-04-19
AU2015298876B2 (en) 2020-02-13
EA201790266A1 (ru) 2017-06-30
CA2954751A1 (en) 2016-02-11
UA124609C2 (uk) 2021-10-20
EP3177609A1 (en) 2017-06-14
KR20170039275A (ko) 2017-04-10
AU2015298876A1 (en) 2017-02-02
JP6577570B2 (ja) 2019-09-18
US20170226102A1 (en) 2017-08-10
CL2017000309A1 (es) 2017-08-18
MX2017001752A (es) 2018-02-08
US10597390B2 (en) 2020-03-24
PH12017500207B1 (en) 2017-07-10
BR112017002370B1 (pt) 2022-11-22
MA40547A (fr) 2017-06-14
BR112017002370A2 (pt) 2017-12-05

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