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)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (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)

Application Number Title Priority Date Filing Date
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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WO2017038650A1 (ja) * 2015-08-28 2017-03-09 積水メディカル株式会社 ベンジル化合物
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
TW202016113A (zh) * 2018-06-08 2020-05-01 大陸商貝達藥業股份有限公司 Erk抑制劑及其應用
KR20210114001A (ko) * 2019-01-11 2021-09-17 시오노기 앤드 컴파니, 리미티드 Mgat2 저해 활성을 갖는 다이하이드로피라졸로피라지논 유도체
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
AU2020242287A1 (en) 2019-03-21 2021-09-02 INSERM (Institut National de la Santé et de la Recherche Médicale) A Dbait molecule in combination with kinase inhibitor for the treatment of cancer
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
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
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
CN116744926A (zh) * 2020-12-15 2023-09-12 北京原基华毅生物科技有限公司 作为酪蛋白激酶抑制剂的化合物
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
KR20040097375A (ko) 2002-04-23 2004-11-17 시오노기 앤드 컴파니, 리미티드 피라졸로[1, 5-에이]피리미딘 유도체 및 이를 함유한엔에이디(피)에이취 산화효소 저해제
CA2494700C (en) 2002-08-26 2011-06-28 Takeda Pharmaceutical Company Limited Calcium receptor modulating compound and use thereof
AU2003301226A1 (en) * 2002-12-20 2004-07-22 Pharmacia Corp Acyclic pyrazole compounds for the inhibition of mitogen activated protein kinase-activated protein kinase-2
JP2005343889A (ja) 2004-05-06 2005-12-15 Taisho Pharmaceut Co Ltd イミダゾピリジン誘導体
ES2398677T3 (es) * 2007-12-12 2013-03-20 E. I. Du Pont De Nemours And Company Pirazoles bicíclicos fungicidas
AU2008345687A1 (en) 2007-12-21 2009-07-09 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
CN102056925A (zh) * 2008-04-07 2011-05-11 Irm责任有限公司 作为激酶抑制剂的化合物和组合物
CA2720946C (en) 2008-04-07 2013-05-28 Irm Llc Compounds and compositions as protein kinase inhibitors
JP5492194B2 (ja) * 2008-05-13 2014-05-14 アイアールエム・リミテッド・ライアビリティ・カンパニー キナーゼ阻害剤としての縮合窒素含有ヘテロ環およびその組成物
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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
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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

Also Published As

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

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