KR102455518B1 - ROS1 저해제로서 치환된 4,5,6,7-테트라히드로피라졸로[1,5-a]피리미딘 유도체 및 2,3-디히드로-1H-이미다조[1,2-b]피라졸 유도체 - Google Patents

ROS1 저해제로서 치환된 4,5,6,7-테트라히드로피라졸로[1,5-a]피리미딘 유도체 및 2,3-디히드로-1H-이미다조[1,2-b]피라졸 유도체 Download PDF

Info

Publication number
KR102455518B1
KR102455518B1 KR1020167027337A KR20167027337A KR102455518B1 KR 102455518 B1 KR102455518 B1 KR 102455518B1 KR 1020167027337 A KR1020167027337 A KR 1020167027337A KR 20167027337 A KR20167027337 A KR 20167027337A KR 102455518 B1 KR102455518 B1 KR 102455518B1
Authority
KR
South Korea
Prior art keywords
alkyl
substituted
hydrogen
alkyloxy
formula
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
KR1020167027337A
Other languages
English (en)
Korean (ko)
Other versions
KR20160137566A (ko
Inventor
라우렌스 앤 메벨렉
마태우 루도빅 진티
티에리 프란체스코 알랭 쟌 주젬무
Original Assignee
얀센 파마슈티카 엔.브이.
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 얀센 파마슈티카 엔.브이. filed Critical 얀센 파마슈티카 엔.브이.
Publication of KR20160137566A publication Critical patent/KR20160137566A/ko
Application granted granted Critical
Publication of KR102455518B1 publication Critical patent/KR102455518B1/ko
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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/41621,2-Diazoles 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41881,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4409Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-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
    • C07D487/04Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
KR1020167027337A 2014-03-27 2015-03-26 ROS1 저해제로서 치환된 4,5,6,7-테트라히드로피라졸로[1,5-a]피리미딘 유도체 및 2,3-디히드로-1H-이미다조[1,2-b]피라졸 유도체 Active KR102455518B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP14161959.3 2014-03-27
EP14161959 2014-03-27
PCT/EP2015/056501 WO2015144801A1 (en) 2014-03-27 2015-03-26 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

Publications (2)

Publication Number Publication Date
KR20160137566A KR20160137566A (ko) 2016-11-30
KR102455518B1 true KR102455518B1 (ko) 2022-10-14

Family

ID=50389875

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020167027337A Active KR102455518B1 (ko) 2014-03-27 2015-03-26 ROS1 저해제로서 치환된 4,5,6,7-테트라히드로피라졸로[1,5-a]피리미딘 유도체 및 2,3-디히드로-1H-이미다조[1,2-b]피라졸 유도체

Country Status (13)

Country Link
US (1) US10342795B2 (enExample)
EP (1) EP3126366B1 (enExample)
JP (1) JP6527167B2 (enExample)
KR (1) KR102455518B1 (enExample)
CN (1) CN106132967B (enExample)
AU (1) AU2015238298B2 (enExample)
BR (1) BR112016021507B1 (enExample)
CA (1) CA2941206C (enExample)
EA (1) EA031639B1 (enExample)
ES (1) ES2686747T3 (enExample)
IL (1) IL247948B (enExample)
MX (1) MX367913B (enExample)
WO (1) WO2015144801A1 (enExample)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106580982B (zh) * 2016-11-26 2017-09-22 王玉美 一种治疗药物流产后子宫出血的药物
CN106866536A (zh) * 2017-04-12 2017-06-20 中国农业大学 一种制备4‑卤代‑5‑氨基吡唑的方法
WO2019033330A1 (en) * 2017-08-17 2019-02-21 Xw Laboratories, Inc. PREPARATION AND USES OF DERIVATIVES TRACERS OF OXYGEN REACTIVE SPECIES
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
CN111087398A (zh) * 2019-12-24 2020-05-01 上海万巷制药有限公司 一种制备拉罗替尼中间体的清洁工艺
US20230067461A1 (en) 2020-01-13 2023-03-02 Aptabio Therapeutics Inc. Novel pyrazole derivative
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN113416140B (zh) * 2021-06-03 2023-01-13 万华化学集团股份有限公司 一种制备2-甲基戊二胺的方法
US20250145628A1 (en) * 2022-02-15 2025-05-08 Novo Nordisk A/S Pyrazolopyrimidines, compositions comprising them and uses thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006502165A (ja) 2002-09-06 2006-01-19 バイオジェン・アイデック・エムエイ・インコーポレイテッド ピラゾロピリジンならびにその作製および使用方法
WO2009108838A1 (en) 2008-02-29 2009-09-03 Wyeth Bridged, bicyclic heterocyclic or spiro bicyclic heterocyclic derivatives of pyrazolo[1,5-a]pyrimidines, methods for preparation and uses thereof
WO2011153553A2 (en) 2010-06-04 2011-12-08 The Regents Of The University Of California Methods and compositions for kinase inhibition

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9204464D0 (en) * 1992-03-02 1992-04-15 Fujisawa Pharmaceutical Co New heterocyclic derivatives
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
AU2008345687A1 (en) 2007-12-21 2009-07-09 Wyeth Llc Pyrazolo [1,5-a] pyrimidine compounds
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
JO3407B1 (ar) * 2012-05-31 2019-10-20 Eisai R&D Man Co Ltd مركبات رباعي هيدرو بيرازولو بيريميدين
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 (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006502165A (ja) 2002-09-06 2006-01-19 バイオジェン・アイデック・エムエイ・インコーポレイテッド ピラゾロピリジンならびにその作製および使用方法
WO2009108838A1 (en) 2008-02-29 2009-09-03 Wyeth Bridged, bicyclic heterocyclic or spiro bicyclic heterocyclic derivatives of pyrazolo[1,5-a]pyrimidines, methods for preparation and uses thereof
JP2011513334A (ja) 2008-02-29 2011-04-28 ワイス・エルエルシー ピラゾロ[1,5−a]ピリミジンの架橋二環式複素環式またはスピロ二環式複素環式誘導体、その調製方法および使用
WO2011153553A2 (en) 2010-06-04 2011-12-08 The Regents Of The University Of California Methods and compositions for kinase inhibition

Also Published As

Publication number Publication date
CN106132967B (zh) 2019-05-28
AU2015238298A1 (en) 2016-09-15
BR112016021507B1 (pt) 2022-10-18
AU2015238298B2 (en) 2019-04-18
US10342795B2 (en) 2019-07-09
BR112016021507A2 (enExample) 2017-08-15
CN106132967A (zh) 2016-11-16
CA2941206C (en) 2022-09-20
MX367913B (es) 2019-09-11
MX2016012669A (es) 2016-12-14
US20170173014A1 (en) 2017-06-22
EP3126366B1 (en) 2018-06-06
JP2017508777A (ja) 2017-03-30
EP3126366A1 (en) 2017-02-08
EA031639B1 (ru) 2019-01-31
ES2686747T3 (es) 2018-10-19
WO2015144801A1 (en) 2015-10-01
KR20160137566A (ko) 2016-11-30
CA2941206A1 (en) 2015-10-01
JP6527167B2 (ja) 2019-06-05
IL247948B (en) 2019-03-31
EA201691934A1 (ru) 2017-01-30

Similar Documents

Publication Publication Date Title
KR102455518B1 (ko) ROS1 저해제로서 치환된 4,5,6,7-테트라히드로피라졸로[1,5-a]피리미딘 유도체 및 2,3-디히드로-1H-이미다조[1,2-b]피라졸 유도체
KR102390276B1 (ko) 마크로사이클릭 피리미딘 유도체
KR102455519B1 (ko) ROS1 저해제로서의 치환된 4,5,6,7-테트라히드로피라졸로[1,5-a]피라진 유도체 및 5,6,7,8-테트라히드로-4H-피라졸로[1,5-a][1,4]디아제핀 유도체
KR102472198B1 (ko) Pi3k 베타 저해제로서의 아자벤즈이미다졸 유도체
EP3768671B1 (en) Substituted imidazolidin-2-one derivatives as prmt5 inhibitors
JP2017508777A5 (enExample)
KR20160140739A (ko) 마크로사이클릭 피리미딘 유도체
EP4161927B9 (en) Spiro compounds as melanocortin 4 receptor antagonists and uses thereof
JP2019504067A (ja) Nik阻害剤としての新たな置換されたシアノインドリン誘導体
JP2017508779A5 (enExample)
KR102274755B1 (ko) Perk 저해제로서의 신규한 n―(2,3―디히드로―1h―피롤로[2,3―b]피리딘―5―일)―4―퀴나졸린아민 및 n―(2,3―디히드로―1h―인돌―5―일)―4―퀴나졸린아민 유도체
JP7213193B2 (ja) Nik阻害剤としての新規の置換アザインドリン誘導体
JP6586463B2 (ja) PI3Kβ阻害剤としての複素環連結イミダゾピリダジン誘導体
KR102472453B1 (ko) Pi3k 베타 저해제로서의 이환식 피리딘, 피라진, 및 피리미딘 유도체
KR20190133729A (ko) Pi3k-베타 억제제로서 퀴녹살린 및 피리도피라진 유도체
WO2023203374A1 (en) [1,2]selenazolo[2,3-a]pyridin-8-ium inhibitors of pyruvate kinase isoform m2
DE19608631A1 (de) 4-Amino-pyrimidin-Derivate, diese Verbindungen enthaltende Arnzeimittel, deren Verwendung und Verfahren zu ihrer Herstellung
KR20250073137A (ko) Egfr 억제제 및 그의 용도

Legal Events

Date Code Title Description
PA0105 International application

Patent event date: 20160930

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application
A201 Request for examination
PA0201 Request for examination

Patent event code: PA02012R01D

Patent event date: 20200323

Comment text: Request for Examination of Application

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

Comment text: Notification of reason for refusal

Patent event date: 20210908

Patent event code: PE09021S01D

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

Patent event code: PE07011S01D

Comment text: Decision to Grant Registration

Patent event date: 20220721

GRNT Written decision to grant
PR0701 Registration of establishment

Comment text: Registration of Establishment

Patent event date: 20221012

Patent event code: PR07011E01D

PR1002 Payment of registration fee

Payment date: 20221012

End annual number: 3

Start annual number: 1

PG1601 Publication of registration