CN104507481B - 用于治疗、改善或预防病毒疾病的7‑氧代‑4,7‑二氢‑吡唑并[1,5‑a]嘧啶衍生物 - Google Patents

用于治疗、改善或预防病毒疾病的7‑氧代‑4,7‑二氢‑吡唑并[1,5‑a]嘧啶衍生物 Download PDF

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Publication number
CN104507481B
CN104507481B CN201380025121.5A CN201380025121A CN104507481B CN 104507481 B CN104507481 B CN 104507481B CN 201380025121 A CN201380025121 A CN 201380025121A CN 104507481 B CN104507481 B CN 104507481B
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alkyl
optionally substituted
compound
oxo
cycloalkyl
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CN201380025121.5A
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Chinese (zh)
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CN104507481A (zh
Inventor
A·沃尔克斯托弗
O·索拉尔
N·汉德勒
S·丘萨克
T·索维特
C·米绍-西蒙
C·莫里斯
B·吉特兰
T·朗格
M·史密斯
S-S·苏
D·克拉森-霍本
H·布施曼
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Savira Pharmaceuticals GmbH
F Hoffmann La Roche AG
Europaisches Laboratorium fuer Molekularbiologie EMBL
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Savira Pharmaceuticals GmbH
F Hoffmann La Roche AG
Europaisches Laboratorium fuer Molekularbiologie EMBL
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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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/535Heterocyclic 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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/16Antivirals for RNA viruses for influenza or rhinoviruses
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pulmonology (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201380025121.5A 2012-05-23 2013-05-23 用于治疗、改善或预防病毒疾病的7‑氧代‑4,7‑二氢‑吡唑并[1,5‑a]嘧啶衍生物 Expired - Fee Related CN104507481B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261650725P 2012-05-23 2012-05-23
US61/650,725 2012-05-23
PCT/EP2013/060634 WO2013174931A1 (en) 2012-05-23 2013-05-23 7-oxo-4,7 -dihydro- pyrazolo [1, 5 -a] pyrimidine derivatives which are useful in the treatment, amelioration or prevention of a viral disease

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CN104507481A CN104507481A (zh) 2015-04-08
CN104507481B true CN104507481B (zh) 2017-08-04

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CN201380025121.5A Expired - Fee Related CN104507481B (zh) 2012-05-23 2013-05-23 用于治疗、改善或预防病毒疾病的7‑氧代‑4,7‑二氢‑吡唑并[1,5‑a]嘧啶衍生物

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US (2) US20130317021A1 (enExample)
EP (1) EP2861232A1 (enExample)
JP (1) JP2015521189A (enExample)
KR (1) KR20150014506A (enExample)
CN (1) CN104507481B (enExample)
BR (1) BR112014029006A2 (enExample)
CA (1) CA2874253A1 (enExample)
HK (1) HK1204987A1 (enExample)
MX (1) MX2014014109A (enExample)
RU (1) RU2014146778A (enExample)
WO (1) WO2013174931A1 (enExample)

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WO2014089379A1 (en) 2012-12-07 2014-06-12 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2970307B1 (en) * 2013-03-13 2020-03-11 Genentech, Inc. Pyrazolo compounds and uses thereof
EP2970289A1 (en) 2013-03-15 2016-01-20 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
US9663519B2 (en) 2013-03-15 2017-05-30 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
EP2970288A1 (en) 2013-03-15 2016-01-20 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2015085132A1 (en) 2013-12-06 2015-06-11 Vertex Pharmaceuticals Incorporated 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, its preparation, different solid forms and radiolabelled derivatives thereof
HRP20200186T1 (hr) 2014-06-05 2020-05-29 Vertex Pharmaceuticals Inc. Radioaktivno obilježeni derivati 2-amino-6-fluoro-n-[5-fluoro-piridin-3-il]-pirazolo[1,5-a]pirimidin-3-karboksamid spojeva koji se koriste kao inhibitori atr kinaze, priprava navedenih spojeva i njihovi različiti čvrsti oblici
JP6936007B2 (ja) 2014-06-17 2021-09-15 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 Chk1阻害剤とatr阻害剤との組み合わせを使用してがんを処置する方法
EA201692301A1 (ru) 2014-07-01 2017-06-30 Ремпекс Фармасьютикалз, Инк. Производные бороновой кислоты и их терапевтическое применение
CN107074880A (zh) 2014-07-07 2017-08-18 萨维拉制药有限公司 二氢吡啶并吡嗪‑1,8‑二酮和它们在治疗、改善或预防病毒疾病中的用途
HRP20241039T1 (hr) 2015-04-28 2024-11-08 Shionogi & Co., Ltd Supstituirani derivat policikličkog piridona i njegov predlijek
US20170081331A1 (en) * 2015-09-18 2017-03-23 F. Hoffmann-La Roche Ag Pyrazolopyrazines and their use in the treatment, amelioration or prevention of a viral disease
EP3355926B1 (en) 2015-09-30 2025-12-24 Vertex Pharmaceuticals Inc. Combination of dna damaging agents and atr inhibitors for use in a method for treating cancer using
SG10201911957QA (en) 2015-12-15 2020-02-27 Shionogi & Co Medicine for treating influenza characterized by comprising combination of cap-dependent endonuclease inhibitor with anti-influenza drug
CN109415345B (zh) 2016-06-29 2022-01-11 豪夫迈·罗氏有限公司 基于哒嗪酮的广谱抗流感抑制剂
UA125218C2 (uk) 2016-08-10 2022-02-02 Сіоногі Енд Ко., Лтд. Фармацевтичні композиції, що містять заміщені поліциклічні піридонові похідні та їх проліки
US20200048259A1 (en) * 2016-10-12 2020-02-13 Merck Sharp & Dohme Corp. Kdm5 inhibitors
US10975084B2 (en) 2016-10-12 2021-04-13 Merck Sharp & Dohme Corp. KDM5 inhibitors
MX2020002869A (es) 2017-09-15 2020-07-24 Aduro Biotech Inc Compuestos de pirazolopirimidinona y usos de los mismos.
AU2019216260B2 (en) * 2018-01-31 2023-03-02 Janssen Sciences Ireland Unlimited Company Cycloalkyl substituted pyrazolopyrimidines having activity against RSV
CN113620977B (zh) * 2021-08-24 2024-02-02 江苏弘和药物研发有限公司 一种噻唑烷并嘧啶酮乙酸的合成方法
CN117304133B (zh) * 2023-09-26 2026-03-17 华南农业大学 一种具有噻唑侧链的截短侧耳素衍生物及其制备方法和应用

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US20160367557A1 (en) 2016-12-22
RU2014146778A (ru) 2016-07-10
HK1204987A1 (en) 2015-12-11
BR112014029006A2 (pt) 2017-06-27
CA2874253A1 (en) 2013-11-28
US20130317021A1 (en) 2013-11-28
KR20150014506A (ko) 2015-02-06
JP2015521189A (ja) 2015-07-27
CN104507481A (zh) 2015-04-08
MX2014014109A (es) 2016-03-31
EP2861232A1 (en) 2015-04-22
WO2013174931A1 (en) 2013-11-28

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Free format text: CORRECT: INVENTOR; FROM: WOLKERSTORFER ANDREA SZOLAR OLIVER? HANDLER NORBERT CUSACK STEPHEN SAUVAITRE THIBAULT SIMON CELINE MORICE CHRISTOPHE GIETHLEN BRUNO T LANG SMITH MARTIN SO SUNG-SAU CLASSEN-HOUBEN DIRK BUSCHMANN HELMUT TO: WOLKERSTORFER ANDREA SZOLAR OLIVER? HANDLER NORBERT CUSACK STEPHEN SAUVAITRE THIBAULT MICHAUD-SIMON CELINE MORICE CHRISTOPHE GIETHLEN BRUNO T LANG SMITH MARTIN SO SUNG-SAU CLASSEN-HOUBEN DIRK BUSCHMANN HELMUT

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