WO2016085221A3 - 단백질 키나아제 저해제로 유용한 헤테로아릴아민 유도체 - Google Patents

단백질 키나아제 저해제로 유용한 헤테로아릴아민 유도체 Download PDF

Info

Publication number
WO2016085221A3
WO2016085221A3 PCT/KR2015/012610 KR2015012610W WO2016085221A3 WO 2016085221 A3 WO2016085221 A3 WO 2016085221A3 KR 2015012610 W KR2015012610 W KR 2015012610W WO 2016085221 A3 WO2016085221 A3 WO 2016085221A3
Authority
WO
WIPO (PCT)
Prior art keywords
protein kinase
heteroaryl amine
kinase inhibitor
amine derivative
fgfr
Prior art date
Application number
PCT/KR2015/012610
Other languages
English (en)
French (fr)
Other versions
WO2016085221A2 (ko
Inventor
심태보
윤호종
윤지혜
허우영
노은주
곽연의
Original Assignee
한국과학기술연구원
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 한국과학기술연구원 filed Critical 한국과학기술연구원
Publication of WO2016085221A2 publication Critical patent/WO2016085221A2/ko
Publication of WO2016085221A3 publication Critical patent/WO2016085221A3/ko

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-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
    • C07D487/02—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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10S428/00—Stock material or miscellaneous articles
    • Y10S428/917—Electroluminescent

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

본 발명은 단백질 키나아제 저해활성을 갖는 헤테로아릴아민 화합물, 이의 약학적으로 허용 가능한 염, 그리고 이 화합물을 유효성분으로 함유하는 비정상 세포 성장으로 유발되는 질환의 예방 및 치료용 약학적 조성물에 관한 것이다. 본 발명의 신규 화합물은 방광암, 자궁내막암 등의 주요 유발인자인 FGFR 및 그의 점 돌연변이 및 FGFR 이외에 신호 전달에 관여하는 다양한 단백질 키나아제에 대하여 우수한 억제 효과를 나타내므로, 이들 단백질 키나아제에 의해 유발되는 비정상 세포 성장 질환의 예방 및 치료제로서 유용하다.
PCT/KR2015/012610 2014-11-26 2015-11-24 단백질 키나아제 저해제로 유용한 헤테로아릴아민 유도체 WO2016085221A2 (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR10-2014-0166484 2014-11-26
KR1020140166484A KR101850282B1 (ko) 2014-11-26 2014-11-26 단백질 키나아제 저해제로 유용한 헤테로아릴아민 유도체

Publications (2)

Publication Number Publication Date
WO2016085221A2 WO2016085221A2 (ko) 2016-06-02
WO2016085221A3 true WO2016085221A3 (ko) 2016-09-15

Family

ID=56009522

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/KR2015/012610 WO2016085221A2 (ko) 2014-11-26 2015-11-24 단백질 키나아제 저해제로 유용한 헤테로아릴아민 유도체

Country Status (3)

Country Link
US (1) US9586936B2 (ko)
KR (1) KR101850282B1 (ko)
WO (1) WO2016085221A2 (ko)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201204384D0 (en) 2012-03-13 2012-04-25 Univ Dundee Anti-flammatory agents
AU2015292818B2 (en) * 2014-07-21 2020-01-16 Dana-Farber Cancer Institute, Inc. Imidazolyl kinase inhibitors and uses thereof
CA2954187C (en) 2014-07-21 2022-08-16 Dana-Farber Cancer Institute, Inc. Macrocyclic kinase inhibitors and uses thereof
AU2015300782B2 (en) 2014-08-08 2020-04-16 Dana-Farber Cancer Institute, Inc. Uses of salt-inducible kinase (SIK) inhibitors
US10954242B2 (en) 2016-07-05 2021-03-23 The Broad Institute, Inc. Bicyclic urea kinase inhibitors and uses thereof
US11241435B2 (en) 2016-09-16 2022-02-08 The General Hospital Corporation Uses of salt-inducible kinase (SIK) inhibitors for treating osteoporosis
CN106883235B (zh) * 2016-12-29 2019-04-30 天津国际生物医药联合研究院 恶二唑类化合物的制备和应用
AU2018226771B2 (en) 2017-02-28 2023-11-23 Dana-Farber Cancer Institute, Inc. Uses of pyrimidopyrimidinones as SIK inhibitors
WO2018228476A1 (zh) * 2017-06-15 2018-12-20 南京明德新药研发股份有限公司 苯并咪唑类化合物及其应用
CN112341344B (zh) * 2019-08-09 2021-10-26 上海喀露蓝科技有限公司 一种激酶抑制剂中间体的制备方法
KR102333854B1 (ko) 2019-10-24 2021-12-06 한국과학기술연구원 단백질 키나아제 저해 활성을 갖는 신규한 피리디닐트리아진 유도체 및 이를 포함하는 암의 예방, 개선 또는 치료용 약학 조성물

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20080015475A (ko) * 2005-07-01 2008-02-19 아이알엠 엘엘씨 단백질 키나제 억제제로서의 피리미딘-치환 벤즈이미다졸유도체
US20120165334A1 (en) * 2009-02-18 2012-06-28 Amgen Inc. Indole/Benzimidazole Compounds as mTOR Kinase Inhibitors

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR077823A1 (es) * 2009-08-11 2011-09-28 Sanofi Aventis Us Llc Proceso para preparar compuestos de benzimidazol sustituidos con 2-arilamino o heteroarilamino

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20080015475A (ko) * 2005-07-01 2008-02-19 아이알엠 엘엘씨 단백질 키나제 억제제로서의 피리미딘-치환 벤즈이미다졸유도체
US20120165334A1 (en) * 2009-02-18 2012-06-28 Amgen Inc. Indole/Benzimidazole Compounds as mTOR Kinase Inhibitors

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
PETERSON, E. A. ET AL.: "Discovery of Triazine-Benzimidazoles as Selective Inhibitors of mTOR", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 21, no. 7, 2011, pages 2064 - 2070, XP028162337 *
WU, F. ET AL.: "Exploring the Selectivity of PI3Kalpha and mTOR Inhibitors by 3D-QSAR, Molecular Dynamics Simulations and MM/GBSA Binding Free Energy Decomposition", MEDCHEMCOMMUN., vol. 4, 2013, pages 1482 - 1496, XP055309871 *
XIE, W. G. ET AL.: "3D-QSAR Studies and Molecular Design on a Novel Series of Pyrimidine Benzimidazoles as Lck Inhibitors", INTERNATIONAL JOURNAL OF QUANTUM CHEMISTRY, vol. 114, no. 9, 26 February 2014 (2014-02-26), pages 598 - 609, XP055309853 *
ZHANG, G. ET AL.: "Discovery of Pyrimidine Benzimidazoles as Lck Inhibitors: Part I", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 18, no. 20, 2008, pages 5618 - 5621, XP025562120 *
ZHANG, G. ET AL.: "Discovery of Pyrimidine Benzimidazoles as Src-Family Selective Lck Inhibitors. Part II", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 19, no. 23, 2009, pages 6691 - 6695, XP026736085 *

Also Published As

Publication number Publication date
US9586936B2 (en) 2017-03-07
US20160145240A1 (en) 2016-05-26
WO2016085221A2 (ko) 2016-06-02
KR20160063026A (ko) 2016-06-03
KR101850282B1 (ko) 2018-05-31

Similar Documents

Publication Publication Date Title
WO2016085221A3 (ko) 단백질 키나아제 저해제로 유용한 헤테로아릴아민 유도체
MX2021013110A (es) Compuestos heterociclicos como inhibidores de la cinasa ret.
SA518400547B1 (ar) مشتقات بيرازولو بيريميدين كمثبط كيناز
WO2017205536A3 (en) Heterocyclic inhibitors of cbp/ep300 and their use in the treatment of cancer
EP4104837A3 (en) Heterocyclic compounds as ret kinase inhibitors
WO2016172134A3 (en) Novel compounds
WO2015200680A8 (en) Prmt5 inhibitors and uses thereof
PH12016502382A1 (en) Substituted indazole compounds as irak4 inhibitors
EA201891917A1 (ru) Бициклические гетероциклические производные в качестве ингибиторов irak4
WO2015200677A3 (en) Prmt5 inhibitors and uses thereof
PH12018500360A1 (en) Heteroaryl derivatives as parp inhibitors
CA2983481A1 (en) Janus kinase inhibitor
TN2020000125A1 (en) Amino-fluoropiperidine derivative as kinase inhibitor
MD4800B1 (ro) Compuşi de aminopirimidinil ca inhibitori de JAK
WO2016172496A8 (en) Lsd1 inhibitors and uses thereof
SA520412335B1 (ar) مشتقات أوكسي فلورو ببريدين كمثبط كيناز
TN2017000075A1 (en) Compounds and compositions as raf kinase inhibitors
NZ745210A (en) Novel 2,3,5-substituted thiophene compound as protein kinase inhibitor
SA519401322B1 (ar) مركبات أريل كربوكساميد غير متجانسة كمثطبات لكيناز بروتين سيرين/ ثريونين متداخل مع المستقبل 2
MX2018008307A (es) Derivado de ascoclorina y uso del mismo como activador de proteina cinasa activada por adenosin monofosfato (ampk).
WO2015155680A3 (en) Pyrazole derivatives as dihydroorotate dehydrogenase (dhodh) inhibitors
SG11201903463PA (en) Quinolyl-substituted carboxylic acid compound or pharmaceutically acceptable salt thereof, pharmaceutical composition of the same, and use of the same
PH12019502046A1 (en) Pyrrolotriazine derivatives as kinase inhibitor
MX2019014438A (es) Derivados de acidos carboxilicos eficaces como inhibidores de la proteina quinasa.
MX2019014436A (es) Derivados de piridoquinazolina eficaces como inhibidores de proteina quinasa.

Legal Events

Date Code Title Description
121 Ep: the epo has been informed by wipo that ep was designated in this application

Ref document number: 15862389

Country of ref document: EP

Kind code of ref document: A2

NENP Non-entry into the national phase

Ref country code: DE

122 Ep: pct application non-entry in european phase

Ref document number: 15862389

Country of ref document: EP

Kind code of ref document: A2