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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Expired - Fee Related
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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
European Molecular Biology Laboratory
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Savira Pharmaceuticals GmbH
F Hoffmann La Roche AG
European Molecular Biology Laboratory
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    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/435—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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 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
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/535—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic 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
    • C07D513/02—Heterocyclic 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
    • C07D513/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Pulmonology (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

Publications (2)

Publication Number Publication Date
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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LT3418281T (lt) 2012-12-07 2021-01-11 Vertex Pharmaceuticals Inc. Pirazolo[1,5-a]pirimidinai, naudotini kaip atr kinazės inhibitoriai, skirti vėžinių ligų gydymui
RU2015143517A (ru) * 2013-03-13 2017-04-19 Дженентек, Инк. Пиразолсодержащие соединения и их применения
EP2970288A1 (en) 2013-03-15 2016-01-20 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2014143240A1 (en) 2013-03-15 2014-09-18 Vertex Pharmaceuticals Incorporated Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase
EP2970289A1 (en) 2013-03-15 2016-01-20 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
HUE046727T2 (hu) 2013-12-06 2020-03-30 Vertex Pharma Az ATR-kináz inhibitoraként használható vegyület, 2-amino-6-fluoro-N-[5-fluoro-piridin-3-IL]-pirazolo-[1,5-A]-pirimidin-3-karboxamid, ennek elõállítása, különbözõ szilárd formái és ezek radioaktív nyomjelzett származékai
ES2777608T3 (es) 2014-06-05 2020-08-05 Vertex Pharma Derivados radiomarcados de un compuesto de 2-amino-6-fluoro-N-[5-fluoro-piridin-3-il]-pirazolo[1,5-a]pirimidin-3-carboxamida útiles como inhibidores de ATR cinasa, la preparación de dicho compuesto y diferentes formas sólidas del mismo
US11179394B2 (en) 2014-06-17 2021-11-23 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of Chk1 and ATR inhibitors
AU2015284307A1 (en) 2014-07-01 2017-02-02 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
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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
US11464774B2 (en) 2015-09-30 2022-10-11 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of DNA damaging agents and ATR inhibitors
HK1254961A1 (en) 2015-12-15 2019-08-02 Shionogi & Co., Ltd. Medicine for treating influenza characterized by comprising combination of cap-dependent endonuclease inhibitor with anti-influenza drug
JP6957535B2 (ja) 2016-06-29 2021-11-02 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ ピリダジノンベースの広域スペクトル抗インフルエンザ阻害剤
US10759814B2 (en) 2016-08-10 2020-09-01 Shionogi & Co., Ltd. Pharmaceutical compositions containing substituted polycyclic pyridone derivatives and prodrug thereof
WO2018071282A1 (en) * 2016-10-12 2018-04-19 Merck Sharp & Dohme Corp. Kdm5 inhibitors
US10975084B2 (en) 2016-10-12 2021-04-13 Merck Sharp & Dohme Corp. KDM5 inhibitors
US10738056B2 (en) 2017-09-15 2020-08-11 Aduro Biotech Inc. Pyrazolopyrimidinone compounds and uses thereof
CA3087926A1 (en) * 2018-01-31 2019-08-08 Janssen Sciences Ireland Unlimited Company Cycloalkyl substituted pyrazolopyrimidines having activity against rsv
AR125966A1 (es) 2021-05-26 2023-08-30 Novartis Ag Nuevos compuestos bicíclicos y sus usos
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
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KR20150014506A (ko) 2015-02-06
BR112014029006A2 (pt) 2017-06-27
CA2874253A1 (en) 2013-11-28
CN104507481A (zh) 2015-04-08
HK1204987A1 (en) 2015-12-11
EP2861232A1 (en) 2015-04-22
US20160367557A1 (en) 2016-12-22
WO2013174931A1 (en) 2013-11-28
JP2015521189A (ja) 2015-07-27
RU2014146778A (ru) 2016-07-10
MX2014014109A (es) 2016-03-31
US20130317021A1 (en) 2013-11-28

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Inventor after: WOLKERSTORFER ANDREA

Inventor after: Harder Craig

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Inventor after: CLASSEN-HOUBEN DIRK

Inventor after: Helmut Buschmann

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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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