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
Inventor
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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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/495—Heterocyclic 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic 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
    • C07D487/20—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically 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)
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 2014-03-27
EP14161950.2 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 (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
CA2763631A1 (en) * 2009-05-27 2010-12-02 Abbott Laboratories Pyrimidine inhibitors of kinase activity
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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
MX2014001354A (es) 2011-08-02 2014-10-14 Pfizer Crizotinib para uso en el tratamiento de cancer.
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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
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
IL247947B (en) 2019-03-31
JP2017508779A (ja) 2017-03-30
MX2016012668A (es) 2016-12-14
BR112016022105B1 (pt) 2023-01-31

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