IL247947B - 7,6,5,4-tetrahydro-pyrazolo[5,1-a]pyrazine compounds and 8,7,6,5-tetrahydro-h4-pyrazolo[5,1-a][4,1]diazepine compounds as ros1 inhibitors - Google Patents

7,6,5,4-tetrahydro-pyrazolo[5,1-a]pyrazine compounds and 8,7,6,5-tetrahydro-h4-pyrazolo[5,1-a][4,1]diazepine compounds as ros1 inhibitors

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Publication number
IL247947B
IL247947B IL247947A IL24794716A IL247947B IL 247947 B IL247947 B IL 247947B IL 247947 A IL247947 A IL 247947A IL 24794716 A IL24794716 A IL 24794716A IL 247947 B IL247947 B IL 247947B
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Israel
Prior art keywords
pyrazolo
tetrahydro
derivatives
substituted
diazepine
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IL247947A
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English (en)
Hebrew (he)
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Janssen Pharmaceutica Nv
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Publication of IL247947B publication Critical patent/IL247947B/en

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    • 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
    • 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
    • A61K31/495Heterocyclic 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002Heterocyclic compounds
    • 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
    • C07D487/10Spiro-condensed systems
    • 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
    • C07D487/12Heterocyclic 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 three hetero rings
    • C07D487/20Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled

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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)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
IL247947A 2014-03-27 2016-09-21 7,6,5,4-tetrahydro-pyrazolo[5,1-a]pyrazine compounds and 8,7,6,5-tetrahydro-h4-pyrazolo[5,1-a][4,1]diazepine compounds as ros1 inhibitors IL247947B (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP14161950 2014-03-27
PCT/EP2015/056498 WO2015144799A1 (en) 2014-03-27 2015-03-26 SUBSTITUTED 4,5,6,7-TETRAHYDRO-PYRAZOLO[1,5-a]PYRAZINE DERIVATIVES AND 5,6,7,8-TETRAHYDRO-4H-PYRAZOLO[1,5-a][1,4]DIAZEPINE DERIVATIVES AS ROS1 INHIBITORS

Publications (1)

Publication Number Publication Date
IL247947B true IL247947B (en) 2019-03-31

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Family Applications (1)

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IL247947A IL247947B (en) 2014-03-27 2016-09-21 7,6,5,4-tetrahydro-pyrazolo[5,1-a]pyrazine compounds and 8,7,6,5-tetrahydro-h4-pyrazolo[5,1-a][4,1]diazepine compounds as ros1 inhibitors

Country Status (13)

Country Link
US (1) US10280170B2 (enExample)
EP (1) EP3129376B1 (enExample)
JP (1) JP6522646B2 (enExample)
KR (1) KR102455519B1 (enExample)
CN (1) CN106164076B (enExample)
AU (1) AU2015238296B2 (enExample)
BR (1) BR112016022105B1 (enExample)
CA (1) CA2940918C (enExample)
EA (1) EA032255B1 (enExample)
ES (1) ES2715676T3 (enExample)
IL (1) IL247947B (enExample)
MX (1) MX367914B (enExample)
WO (1) WO2015144799A1 (enExample)

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EP3342777B1 (en) * 2015-08-28 2023-01-11 Sekisui Medical Co., Ltd. Benzyl compound
TWI782056B (zh) 2017-07-14 2022-11-01 日商鹽野義製藥股份有限公司 具有mgat2抑制活性的縮合環衍生物
CN112204027A (zh) * 2018-06-08 2021-01-08 贝达药业股份有限公司 Erk 抑制剂及其应用
MX2021008050A (es) * 2019-01-11 2021-08-05 Shionogi & Co Derivado de dihidropirazolopirazinona que tiene actividad inhibidora de monoacilglicerol aciltransferasa 2 (mgat2).
JP7068743B2 (ja) * 2019-01-11 2022-05-17 塩野義製薬株式会社 Mgat2阻害活性を有する縮合環誘導体を含有する医薬組成物
EA202192575A1 (ru) 2019-03-21 2022-01-14 Онксео Соединения dbait в сочетании с ингибиторами киназ для лечения рака
CN114761006A (zh) 2019-11-08 2022-07-15 Inserm(法国国家健康医学研究院) 对激酶抑制剂产生耐药性的癌症的治疗方法
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
TW202229282A (zh) * 2020-09-30 2022-08-01 美商史考皮恩治療有限公司 治療癌症之方法
CN114315866B (zh) * 2020-09-30 2023-10-31 烟台药物研究所 一种盐酸左旋咪唑的合成方法
US20250276972A1 (en) * 2020-12-15 2025-09-04 Gritscience Biopharmaceuticals Co.,Ltd. Compounds as casein kinase inhibitors
CN114957259A (zh) * 2021-02-25 2022-08-30 南京明德新药研发有限公司 氰基取代的芳香双环类化合物及其应用

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US5356897A (en) 1991-09-09 1994-10-18 Fujisawa Pharmaceutical Co., Ltd. 3-(heteroaryl)-pyrazololi[1,5-a]pyrimidines
US7662826B2 (en) 2002-04-23 2010-02-16 Shionogi & Co., Ltd. Pyrazolo [1,5-a] pyrimidine derivative and nad (p) h oxidase inhibitor containing the same
EP1572113B1 (en) 2002-08-26 2017-05-17 Takeda Pharmaceutical Company Limited Calcium receptor modulating compound and use thereof
ZA200504898B (en) * 2002-12-20 2006-11-29 Pharmacia Corp Acyclic pyrazole compounds
JP2005343889A (ja) 2004-05-06 2005-12-15 Taisho Pharmaceut Co Ltd イミダゾピリジン誘導体
PL2217600T3 (pl) * 2007-12-12 2013-04-30 Du Pont Grzybobójcze pirazole bicykliczne
US20100324073A1 (en) 2007-12-21 2010-12-23 Wyeth Llc Pyrazolo [1,5-A] Pyrimidine Compounds
US20100029657A1 (en) 2008-02-29 2010-02-04 Wyeth Bridged, Bicyclic Heterocyclic or Spiro Bicyclic Heterocyclic Derivatives of Pyrazolo[1, 5-A]Pyrimidines, Methods for Preparation and Uses Thereof
MX2010010968A (es) 2008-04-07 2010-10-26 Irm Llc Compuestos y composiciones como inhibidores de cinasa de proteina.
AU2009233963B2 (en) * 2008-04-07 2011-10-06 Irm Llc Compounds and compositions as kinase inhibitors
KR101324804B1 (ko) * 2008-05-13 2013-11-01 아이알엠 엘엘씨 키나제 억제제로서의 질소 함유 융합 헤테로사이클 및 그의 조성물
JP2012528175A (ja) * 2009-05-27 2012-11-12 アボット・ラボラトリーズ キナーゼ活性のピリミジン阻害剤
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WO2011153553A2 (en) * 2010-06-04 2011-12-08 The Regents Of The University Of California Methods and compositions for kinase inhibition
RU2014102935A (ru) * 2011-08-02 2015-09-10 Пфайзер Инк. Кризотиниб для применения в лечении рака
TWI585088B (zh) 2012-06-04 2017-06-01 第一三共股份有限公司 作爲激酶抑制劑之咪唑并[1,2-b]嗒衍生物

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Publication number Publication date
JP2017508779A (ja) 2017-03-30
BR112016022105A2 (enExample) 2017-08-15
EP3129376B1 (en) 2018-12-26
JP6522646B2 (ja) 2019-05-29
AU2015238296A1 (en) 2016-09-08
AU2015238296B2 (en) 2018-10-18
EP3129376A1 (en) 2017-02-15
CN106164076A (zh) 2016-11-23
EA032255B1 (ru) 2019-04-30
KR102455519B1 (ko) 2022-10-14
WO2015144799A1 (en) 2015-10-01
CA2940918A1 (en) 2015-10-01
MX367914B (es) 2019-09-11
CN106164076B (zh) 2019-03-26
BR112016022105B1 (pt) 2023-01-31
CA2940918C (en) 2023-10-24
MX2016012668A (es) 2016-12-14
US10280170B2 (en) 2019-05-07
KR20160137576A (ko) 2016-11-30
ES2715676T3 (es) 2019-06-05
US20170174690A1 (en) 2017-06-22
EA201691930A1 (ru) 2017-02-28

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