CA2940918C - Substituted 4,5,6,7-tetrahydro-pyrazolo[1,5-.alpha.]pyrazine derivatives and 5,6,7,8-tetrahydro-4h-pyrazolo[1,5-.alpha.][1,4]diazepine derivatives as ros1 inhibitors - Google Patents

Substituted 4,5,6,7-tetrahydro-pyrazolo[1,5-.alpha.]pyrazine derivatives and 5,6,7,8-tetrahydro-4h-pyrazolo[1,5-.alpha.][1,4]diazepine derivatives as ros1 inhibitors Download PDF

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CA2940918C
CA2940918C CA2940918A CA2940918A CA2940918C CA 2940918 C CA2940918 C CA 2940918C CA 2940918 A CA2940918 A CA 2940918A CA 2940918 A CA2940918 A CA 2940918A CA 2940918 C CA2940918 C CA 2940918C
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substituted
6alkyl
hydrogen
formula
cyano
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CA2940918A1 (en
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Laurence Anne Mevellec
Elisabeth Therese Jeanne Pasquier
Sophie Descamps
Guillaume Jean Maurice Mercey
Berthold Wroblowski
Jorge Eduardo Vialard
Lieven Meerpoel
Matthieu Ludovic Jeanty
Thierry Francois Alain Jean Jousseaume
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Janssen Pharmaceutica NV
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Janssen Pharmaceutica NV
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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
    • A61K31/505Pyrimidines; 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
    • 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
    • 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)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CA2940918A 2014-03-27 2015-03-26 Substituted 4,5,6,7-tetrahydro-pyrazolo[1,5-.alpha.]pyrazine derivatives and 5,6,7,8-tetrahydro-4h-pyrazolo[1,5-.alpha.][1,4]diazepine derivatives as ros1 inhibitors Active CA2940918C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP14161950.2 2014-03-27
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 (2)

Publication Number Publication Date
CA2940918A1 CA2940918A1 (en) 2015-10-01
CA2940918C true CA2940918C (en) 2023-10-24

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CA2940918A Active CA2940918C (en) 2014-03-27 2015-03-26 Substituted 4,5,6,7-tetrahydro-pyrazolo[1,5-.alpha.]pyrazine derivatives and 5,6,7,8-tetrahydro-4h-pyrazolo[1,5-.alpha.][1,4]diazepine derivatives as ros1 inhibitors

Country Status (13)

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

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* Cited by examiner, † Cited by third party
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KR102630720B1 (ko) 2015-08-28 2024-01-29 세키스이 메디칼 가부시키가이샤 벤질 화합물
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
WO2019233456A1 (zh) * 2018-06-08 2019-12-12 贝达药业股份有限公司 Erk抑制剂及其应用
CA3126334A1 (en) * 2019-01-11 2020-07-16 Shionogi & Co., Ltd. Dihydropyrazolopyrazinone derivative having mgat2 inhibitory activity
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
US20220143049A1 (en) 2019-03-21 2022-05-12 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
EP4054579A1 (en) 2019-11-08 2022-09-14 Institut National de la Santé et de la Recherche Médicale (INSERM) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
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
WO2022127756A1 (en) * 2020-12-15 2022-06-23 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

Family Cites Families (16)

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US5356897A (en) 1991-09-09 1994-10-18 Fujisawa Pharmaceutical Co., Ltd. 3-(heteroaryl)-pyrazololi[1,5-a]pyrimidines
EP1505068A4 (en) 2002-04-23 2008-03-19 Shionogi & Co PYRAZOLO (1,5-a) PYRIMIDINE DERIVATIVE AND INHIBITOR OF NAD (P) H OXIDASE CONTAINING SAID DERIVATIVE
KR101050700B1 (ko) 2002-08-26 2011-07-20 다케다 야쿠힌 고교 가부시키가이샤 칼슘 수용체 조절 화합물 및 이의 용도
CN1747949A (zh) * 2002-12-20 2006-03-15 法马西亚公司 无环吡唑化合物
JP2005343889A (ja) * 2004-05-06 2005-12-15 Taisho Pharmaceut Co Ltd イミダゾピリジン誘導体
US8288375B2 (en) * 2007-12-12 2012-10-16 E.I. Du Pont De Nemours And Company Fungicidal bicyclic pyrazoles
CN101952293A (zh) 2007-12-21 2011-01-19 惠氏有限责任公司 吡唑并[1,5-a]嘧啶化合物
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
US8592432B2 (en) 2008-04-07 2013-11-26 Bei Chen Compounds and compositions as protein kinase inhibitors
KR20110002080A (ko) * 2008-04-07 2011-01-06 아이알엠 엘엘씨 키나제 억제제로서의 화합물 및 조성물
WO2009140128A2 (en) * 2008-05-13 2009-11-19 Irm Llc Compounds and compositions as kinase inhibitors
CN102459264A (zh) * 2009-05-27 2012-05-16 雅培制药有限公司 激酶活性的嘧啶抑制剂
AU2010254151B2 (en) 2009-05-28 2013-11-28 Cook Medical Technologies Llc Tacking device and methods of deployment
WO2011153553A2 (en) 2010-06-04 2011-12-08 The Regents Of The University Of California Methods and compositions for kinase inhibition
AU2012291744A1 (en) * 2011-08-02 2014-02-20 Pfizer Inc. Crizotinib for use in the treatment of cancer
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
AU2015238296A1 (en) 2016-09-08
EA032255B1 (ru) 2019-04-30
CN106164076B (zh) 2019-03-26
BR112016022105B1 (pt) 2023-01-31
EP3129376A1 (en) 2017-02-15
IL247947B (en) 2019-03-31
EA201691930A1 (ru) 2017-02-28
BR112016022105A2 (https=) 2017-08-15
CA2940918A1 (en) 2015-10-01
ES2715676T3 (es) 2019-06-05
CN106164076A (zh) 2016-11-23
AU2015238296B2 (en) 2018-10-18
MX367914B (es) 2019-09-11
EP3129376B1 (en) 2018-12-26
KR20160137576A (ko) 2016-11-30
JP6522646B2 (ja) 2019-05-29
MX2016012668A (es) 2016-12-14
US20170174690A1 (en) 2017-06-22
WO2015144799A1 (en) 2015-10-01
US10280170B2 (en) 2019-05-07
KR102455519B1 (ko) 2022-10-14
JP2017508779A (ja) 2017-03-30

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