AU2015238296B2 - 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 - Google Patents

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 Download PDF

Info

Publication number
AU2015238296B2
AU2015238296B2 AU2015238296A AU2015238296A AU2015238296B2 AU 2015238296 B2 AU2015238296 B2 AU 2015238296B2 AU 2015238296 A AU2015238296 A AU 2015238296A AU 2015238296 A AU2015238296 A AU 2015238296A AU 2015238296 B2 AU2015238296 B2 AU 2015238296B2
Authority
AU
Australia
Prior art keywords
substituted
6alkyl
hydrogen
formula
cyano
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
AU2015238296A
Other languages
English (en)
Other versions
AU2015238296A1 (en
Inventor
Sophie Descamps
Matthieu Ludovic Jeanty
Thierry Francois Alain Jean Jousseaume
Lieven Meerpoel
Guillaume Jean Maurice Mercey
Laurence Anne Mevellec
Elisabeth Therese Jeanne Pasquier
Jorge Eduardo Vialard
Berthold Wroblowski
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Janssen Pharmaceutica NV
Original Assignee
Janssen Pharmaceutica NV
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Janssen Pharmaceutica NV filed Critical Janssen Pharmaceutica NV
Publication of AU2015238296A1 publication Critical patent/AU2015238296A1/en
Application granted granted Critical
Publication of AU2015238296B2 publication Critical patent/AU2015238296B2/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • C07D487/04Ortho-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
    • C07D487/02Heterocyclic 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

Landscapes

  • 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)
AU2015238296A 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 Active AU2015238296B2 (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
AU2015238296A1 AU2015238296A1 (en) 2016-09-08
AU2015238296B2 true AU2015238296B2 (en) 2018-10-18

Family

ID=50389872

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2015238296A Active AU2015238296B2 (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

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)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004058176A2 (en) * 2002-12-20 2004-07-15 Pharmacia Corporation Acyclic pyrazole compounds

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
US9345476B2 (en) 2009-05-28 2016-05-24 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
MX2014001354A (es) 2011-08-02 2014-10-14 Pfizer Crizotinib para uso en el tratamiento de 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

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004058176A2 (en) * 2002-12-20 2004-07-15 Pharmacia Corporation Acyclic pyrazole compounds

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
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

Similar Documents

Publication Publication Date Title
AU2015238296B2 (en) 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
EP3472147B1 (en) Azabenzimidazole derivatives as pi3k beta inhibitors
CA3157361A1 (en) Bicyclic heterocycles as fgfr inhibitors
AU2015239098B2 (en) Macrocylic pyrimidine derivatives
AU2015238298B2 (en) Substituted 4,5,6,7-tetrahydro-pyrazolo[1,5-a]pyrimidine derivatives and 2,3-dihydro-1H-imidazo[1,2-b]pyrazole derivatives as ROS1 inhibitors
JP2017508779A5 (enExample)
CN109311846B (zh) 作为nik抑制剂的新的6元杂芳族取代的氰基吲哚衍生物
TW202110848A (zh) 取代的稠合雙環類衍生物、其製備方法及其在醫藥上的應用
EP3233862B1 (en) Imidazopyridazine derivatives as pi3kbeta inhibitors
KR102662373B1 (ko) Nik 억제제로서의 신규 치환 아자인돌린 유도체
KR20220137002A (ko) 헤테로고리 화합물 및 그의 약제학적 조성물, 제조 방법, 중간체 및 용도
US20240368139A1 (en) Novel modulators of ehmt1 and ehmt2 and therapeutic use thereof
TW202045487A (zh) Pd-l1拮抗劑化合物
CN107108633B (zh) 作为PI3Kβ抑制剂的杂环基连接的咪唑并哒嗪衍生物
EP3472160B1 (en) Bicyclic pyridine, pyrazine, and pyrimidine derivatives as pi3k beta inhibitors
WO2025193878A1 (en) Kras inhibitors

Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)