JP6214551B2 - ピラゾロピリミジン誘導体、これらの調製方法およびこれらの治療的使用 - Google Patents

ピラゾロピリミジン誘導体、これらの調製方法およびこれらの治療的使用 Download PDF

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JP6214551B2
JP6214551B2 JP2014546500A JP2014546500A JP6214551B2 JP 6214551 B2 JP6214551 B2 JP 6214551B2 JP 2014546500 A JP2014546500 A JP 2014546500A JP 2014546500 A JP2014546500 A JP 2014546500A JP 6214551 B2 JP6214551 B2 JP 6214551B2
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pyrazolo
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phenyl
pyridin
trifluoromethyl
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JP2015500318A (ja
JP2015500318A5 (enExample
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アルクフ,シャンタル
ビエルガルデ,カーステン
モージェ,ジャック
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Sanofi SA
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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
    • A61K31/535Heterocyclic 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
    • A61K31/5381,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic 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
    • A61K31/435Heterocyclic 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
    • A61K31/435Heterocyclic 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
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/5355Non-condensed oxazines 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
    • A61K31/535Heterocyclic 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
    • A61K31/536Heterocyclic 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
    • 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
    • A61NELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY
    • A61N5/00Radiation therapy
    • A61N5/10X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (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)
JP2014546500A 2011-12-14 2012-12-13 ピラゾロピリミジン誘導体、これらの調製方法およびこれらの治療的使用 Active JP6214551B2 (ja)

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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JP2017133321A Division JP2017206544A (ja) 2011-12-14 2017-07-07 ピラゾロピリミジン誘導体、これらの調製方法およびこれらの治療的使用

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JP2015500318A5 JP2015500318A5 (enExample) 2016-01-14
JP6214551B2 true JP6214551B2 (ja) 2017-10-18

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JP2017133321A Withdrawn JP2017206544A (ja) 2011-12-14 2017-07-07 ピラゾロピリミジン誘導体、これらの調製方法およびこれらの治療的使用

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US (2) US20140350006A1 (enExample)
EP (1) EP2791137B1 (enExample)
JP (2) JP6214551B2 (enExample)
KR (1) KR102012058B1 (enExample)
CN (2) CN104114555B (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)
ES (1) ES2719444T3 (enExample)
FR (1) FR2984325A1 (enExample)
HK (1) HK1198442A1 (enExample)
IL (1) IL232906A (enExample)
MA (1) MA35841B1 (enExample)
MX (1) MX358422B (enExample)
PH (1) PH12014501258A1 (enExample)
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PT (1) PT2791137T (enExample)
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Cited By (1)

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JP2017206544A (ja) * 2011-12-14 2017-11-24 サノフイ ピラゾロピリミジン誘導体、これらの調製方法およびこれらの治療的使用

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US10138235B2 (en) 2011-12-14 2018-11-27 Sanofi Pyrazolopyridine derivatives, preparation process therefor and therapeutic use thereof
EA201591324A1 (ru) 2013-01-16 2016-01-29 Инсерм (Энститю Насьональ Де Ля Сантэ Э Де Ля Решерш Медикаль) Полипептид растворимого рецептора 3 фактора роста фибробластов (fgr3) для применения с целью предотвращения или лечения нарушений, связанных с замедлением роста скелета
AR094812A1 (es) 2013-02-20 2015-08-26 Eisai R&D Man Co Ltd Derivado de piridina monocíclico como inhibidor del fgfr
US20140303121A1 (en) 2013-03-15 2014-10-09 Plexxikon Inc. Heterocyclic compounds and uses thereof
RU2680100C9 (ru) 2013-03-15 2019-04-18 Плексксикон Инк. Гетероциклические соединения и их применения
PL3007694T3 (pl) * 2013-06-14 2018-12-31 Sanofi Pochodne pirazolopirydynowe do zastosowania w leczeniu nowotworu pęcherza moczowego
ES2914072T3 (es) 2014-08-18 2022-06-07 Eisai R&D Man Co Ltd Sal de derivado de piridina monocíclico y su cristal
EP3275442B1 (en) 2015-03-25 2021-07-28 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
RU2730503C2 (ru) 2015-12-17 2020-08-24 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Терапевтическое средство для лечения рака молочной железы
RU2751483C2 (ru) 2016-07-07 2021-07-14 Пфайзер Инк. Полипептиды, являющиеся растворимыми рецепторами 3 фактора роста фибробластов (sfgfr3), и пути их применения
US10717735B2 (en) 2017-10-13 2020-07-21 Plexxikon Inc. Solid forms of a compound for modulating kinases
CN112105357A (zh) * 2018-02-16 2020-12-18 Ucb生物制药有限责任公司 药用6,5杂双环衍生物
EP3777860A4 (en) 2018-03-28 2021-12-15 Eisai R&D Management Co., Ltd. THERAPEUTIC 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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PL1896470T3 (pl) * 2005-05-16 2011-03-31 Irm Llc Pochodne pirolopirydynowe jako inhibitory kinazy białkowej
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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017206544A (ja) * 2011-12-14 2017-11-24 サノフイ ピラゾロピリミジン誘導体、これらの調製方法およびこれらの治療的使用

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SG11201402851TA (en) 2014-07-30
FR2984325A1 (fr) 2013-06-21
CN106317056A (zh) 2017-01-11
AU2012351712B2 (en) 2017-08-31
PT2791137T (pt) 2019-05-08
DK2791137T3 (en) 2019-04-23
CN104114555B (zh) 2017-09-01
MX358422B (es) 2018-08-20
CA2857749A1 (en) 2013-06-20
ES2719444T3 (es) 2019-07-10
KR102012058B1 (ko) 2019-08-19
US20170231998A1 (en) 2017-08-17
CN104114555A (zh) 2014-10-22
HK1198442A1 (en) 2015-04-24
EA027421B1 (ru) 2017-07-31
PL2791137T3 (pl) 2019-07-31
JP2017206544A (ja) 2017-11-24
AU2012351712A1 (en) 2014-07-10
IL232906A0 (en) 2014-08-03
IL232906A (en) 2017-12-31
WO2013087744A1 (en) 2013-06-20
CO7000778A2 (es) 2014-07-21
SG10201510204QA (en) 2016-01-28
CL2014001539A1 (es) 2014-10-17
BR112014014452A2 (pt) 2017-06-13
EP2791137A1 (en) 2014-10-22
US20140350006A1 (en) 2014-11-27
JP2015500318A (ja) 2015-01-05
EA201491149A1 (ru) 2014-11-28
MX2014007168A (es) 2015-02-10
PH12014501258A1 (en) 2014-09-08
KR20140105551A (ko) 2014-09-01
MA35841B1 (fr) 2014-12-01
CN106317056B (zh) 2020-06-23
EP2791137B1 (en) 2019-01-23

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