CN104114555B - 吡唑并嘧啶衍生物、其制备方法及其治疗用途 - Google Patents

吡唑并嘧啶衍生物、其制备方法及其治疗用途 Download PDF

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Publication number
CN104114555B
CN104114555B CN201280069679.9A CN201280069679A CN104114555B CN 104114555 B CN104114555 B CN 104114555B CN 201280069679 A CN201280069679 A CN 201280069679A CN 104114555 B CN104114555 B CN 104114555B
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Prior art keywords
pyrazolo
pyridin
phenyl
trifluoromethyl
pyridine
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Chinese (zh)
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CN104114555A (zh
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C·奥库弗
K·布杰加德
J·莫杰
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Sanofi Aventis France
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Sanofi Aventis France
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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
    • A61K31/535—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
    • A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic 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
    • A61K31/435—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
    • A61K31/435—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
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/535—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
    • A61K31/5355—Non-condensed oxazines 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
    • A61K31/535—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
    • A61K31/536—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 ortho- or peri-condensed with carbocyclic 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
    • A61N—ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY
    • A61N5/00—Radiation therapy
    • A61N5/10—X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Pathology (AREA)
  • Radiology & Medical Imaging (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201280069679.9A 2011-12-14 2012-12-13 吡唑并嘧啶衍生物、其制备方法及其治疗用途 Active CN104114555B (zh)

Priority Applications (1)

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CN201610708994.1A CN106317056B (zh) 2011-12-14 2012-12-13 吡唑并嘧啶衍生物、其制备方法及其治疗用途

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
FR1161589A FR2984325A1 (fr) 2011-12-14 2011-12-14 Derives de pyrazolopyridine, leur procede de preparation et leur application en therapeutique
FR1161589 2011-12-14
PCT/EP2012/075328 WO2013087744A1 (en) 2011-12-14 2012-12-13 Pyrazolopyridine derivatives, preparation process therefor and therapeutic use thereof

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CN104114555B true CN104114555B (zh) 2017-09-01

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US (2) US20140350006A1 (enExample)
EP (1) EP2791137B1 (enExample)
JP (2) JP6214551B2 (enExample)
KR (1) KR102012058B1 (enExample)
CN (2) CN106317056B (enExample)
AU (1) AU2012351712B2 (enExample)
BR (1) BR112014014452A2 (enExample)
CA (1) CA2857749A1 (enExample)
CL (1) CL2014001539A1 (enExample)
CO (1) CO7000778A2 (enExample)
DK (1) DK2791137T3 (enExample)
EA (1) EA027421B1 (enExample)
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MA (1) MA35841B1 (enExample)
MX (1) MX358422B (enExample)
PH (1) PH12014501258A1 (enExample)
PL (1) PL2791137T3 (enExample)
PT (1) PT2791137T (enExample)
SG (2) SG10201510204QA (enExample)
WO (1) WO2013087744A1 (enExample)

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FR2984325A1 (fr) * 2011-12-14 2013-06-21 Sanofi Sa Derives de pyrazolopyridine, leur procede de preparation et leur application en therapeutique
US10138235B2 (en) 2011-12-14 2018-11-27 Sanofi Pyrazolopyridine derivatives, preparation process therefor and therapeutic use thereof
CA2898415A1 (en) 2013-01-16 2014-07-24 Inserm (Institut National De La Sante Et De La Recherche Medicale) A soluble fibroblast growth factor receptor 3 (fgr3) polypeptide for use in the prevention or treatment of skeletal growth retardation disorders
AR094812A1 (es) 2013-02-20 2015-08-26 Eisai R&D Man Co Ltd Derivado de piridina monocíclico como inhibidor del fgfr
DK2970265T3 (en) 2013-03-15 2018-10-01 Plexxikon Inc HETEROCYCLIC COMPOUNDS AND APPLICATIONS THEREOF
US20140303121A1 (en) 2013-03-15 2014-10-09 Plexxikon Inc. Heterocyclic compounds and uses thereof
WO2014198942A1 (en) * 2013-06-14 2014-12-18 Sanofi Pyrazolopyridine derivatives for use in the treatment of bladder cancer
JP5925978B1 (ja) 2014-08-18 2016-05-25 エーザイ・アール・アンド・ディー・マネジメント株式会社 単環ピリジン誘導体の塩およびその結晶
CA2974937C (en) 2015-03-25 2023-09-05 National Cancer Center Therapeutic agent for bile duct cancer
US11059817B2 (en) 2015-09-23 2021-07-13 The Regents Of The University Of California Potent antiviral pyrazolopyridine compounds
KR102486722B1 (ko) 2015-12-17 2023-01-11 에자이 알앤드디 매니지먼트 가부시키가이샤 유방암 치료제
PL3481859T3 (pl) 2016-07-07 2022-07-11 Pfizer Inc. Rozpuszczalne polipeptydy receptora 3 czynnika wzrostu fibroblastów (sfgfr3) i ich zastosowania
EP3694855A1 (en) 2017-10-13 2020-08-19 Plexxikon Inc. Solid forms of a compound for modulating kinases
EP3752150A1 (en) * 2018-02-16 2020-12-23 UCB Biopharma SRL Pharmaceutical 6,5 heterobicyclic ring derivatives
US11219619B2 (en) 2018-03-28 2022-01-11 Eisai R&D Management Co., Ltd. Therapeutic agent for hepatocellular carcinoma
CN108774224B (zh) * 2018-04-23 2020-10-30 浙江大学 吡唑并[3,4-b]吡啶类化合物及其制备方法和应用
CN110833556A (zh) * 2018-08-15 2020-02-25 广西梧州制药（集团）股份有限公司 吡唑并嘧啶衍生物在治疗肝纤维化的用途
WO2020178316A1 (en) * 2019-03-05 2020-09-10 Aziende Chimiche Riunite Angelini Francesco - A.C.R.A.F. S.P.A. 5- or 7-azaindazoles as beta-lactamase inhibitors
CN118791483B (zh) * 2024-07-01 2025-10-21 郑州大学 一种1H-吡唑并[3,4-b]吡啶类衍生物及其制备方法和应用

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Also Published As

Publication number Publication date
FR2984325A1 (fr) 2013-06-21
CN106317056A (zh) 2017-01-11
IL232906A0 (en) 2014-08-03
EP2791137A1 (en) 2014-10-22
ES2719444T3 (es) 2019-07-10
SG11201402851TA (en) 2014-07-30
CO7000778A2 (es) 2014-07-21
JP6214551B2 (ja) 2017-10-18
KR102012058B1 (ko) 2019-08-19
JP2015500318A (ja) 2015-01-05
IL232906A (en) 2017-12-31
US20170231998A1 (en) 2017-08-17
MX2014007168A (es) 2015-02-10
SG10201510204QA (en) 2016-01-28
HK1198442A1 (en) 2015-04-24
EA201491149A1 (ru) 2014-11-28
MA35841B1 (fr) 2014-12-01
AU2012351712A1 (en) 2014-07-10
PT2791137T (pt) 2019-05-08
CA2857749A1 (en) 2013-06-20
US20140350006A1 (en) 2014-11-27
PH12014501258A1 (en) 2014-09-08
BR112014014452A2 (pt) 2017-06-13
WO2013087744A1 (en) 2013-06-20
PL2791137T3 (pl) 2019-07-31
AU2012351712B2 (en) 2017-08-31
EA027421B1 (ru) 2017-07-31
DK2791137T3 (en) 2019-04-23
KR20140105551A (ko) 2014-09-01
CN106317056B (zh) 2020-06-23
CL2014001539A1 (es) 2014-10-17
JP2017206544A (ja) 2017-11-24
CN104114555A (zh) 2014-10-22
MX358422B (es) 2018-08-20
EP2791137B1 (en) 2019-01-23

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