KR102915019B1 - 4H-피롤로[3,2-c]피리딘-4-온 화합물 - Google Patents

4H-피롤로[3,2-c]피리딘-4-온 화합물

Info

Publication number
KR102915019B1
KR102915019B1 KR1020217037778A KR20217037778A KR102915019B1 KR 102915019 B1 KR102915019 B1 KR 102915019B1 KR 1020217037778 A KR1020217037778 A KR 1020217037778A KR 20217037778 A KR20217037778 A KR 20217037778A KR 102915019 B1 KR102915019 B1 KR 102915019B1
Authority
KR
South Korea
Prior art keywords
pyridin
pyrrolo
tetrahydro
methoxy
chloro
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
KR1020217037778A
Other languages
English (en)
Korean (ko)
Other versions
KR20220004103A (ko
Inventor
스테판 지겔
프란치스카 지겔
볼커 슐체
마르쿠스 베르거
키이쓰 그레이엄
데틀레프 쥘츨레
울프 뵈머
다니엘 코어
옌스 슈뢰더
우르줄라 뫼닝
미카엘 니휘스
매튜 마이어슨
하이디 그로일리히
베타니 카플란
Original Assignee
바이엘 악티엔게젤샤프트
더 브로드 인스티튜트, 인코퍼레이티드
다나-파버 캔서 인스티튜트 인크.
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 바이엘 악티엔게젤샤프트, 더 브로드 인스티튜트, 인코퍼레이티드, 다나-파버 캔서 인스티튜트 인크. filed Critical 바이엘 악티엔게젤샤프트
Publication of KR20220004103A publication Critical patent/KR20220004103A/ko
Application granted granted Critical
Publication of KR102915019B1 publication Critical patent/KR102915019B1/ko
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/4353—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
KR1020217037778A 2019-04-24 2020-04-22 4H-피롤로[3,2-c]피리딘-4-온 화합물 Active KR102915019B1 (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201962838051P 2019-04-24 2019-04-24
US62/838,051 2019-04-24
US201962940036P 2019-11-25 2019-11-25
US62/940,036 2019-11-25
PCT/EP2020/061176 WO2020216781A1 (en) 2019-04-24 2020-04-22 4h-pyrrolo[3,2-c]pyridin-4-one compounds

Publications (2)

Publication Number Publication Date
KR20220004103A KR20220004103A (ko) 2022-01-11
KR102915019B1 true KR102915019B1 (ko) 2026-01-21

Family

ID=70456765

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020217037778A Active KR102915019B1 (ko) 2019-04-24 2020-04-22 4H-피롤로[3,2-c]피리딘-4-온 화합물

Country Status (26)

Country Link
US (2) US20220298157A1 (https=)
EP (1) EP3959211B1 (https=)
JP (1) JP7641913B2 (https=)
KR (1) KR102915019B1 (https=)
CN (3) CN114127064B (https=)
AU (1) AU2020262221B2 (https=)
BR (1) BR112021019998B1 (https=)
CA (1) CA3137218A1 (https=)
CL (1) CL2021002770A1 (https=)
CO (1) CO2021014022A2 (https=)
CR (1) CR20210530A (https=)
DK (1) DK3959211T3 (https=)
DO (1) DOP2021000216A (https=)
EC (1) ECSP21077614A (https=)
FI (1) FI3959211T3 (https=)
GE (2) GEP20247648B (https=)
IL (1) IL287390B2 (https=)
JO (1) JOP20210285A1 (https=)
MA (1) MA55751A (https=)
MX (1) MX2021012987A (https=)
PE (1) PE20220254A1 (https=)
PH (1) PH12021552693A1 (https=)
SG (1) SG11202111304UA (https=)
TW (1) TWI849114B (https=)
UA (1) UA130453C2 (https=)
WO (1) WO2020216781A1 (https=)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3700904B1 (en) 2017-10-24 2023-07-19 Bayer AG 4h-pyrrolo[3,2-c]pyridin-4-one derivatives
US12403135B2 (en) 2019-04-24 2025-09-02 Bayer Aktiengesellschaft 4H-pyrrolo[3,2-c]pyridin-4-one derivatives
CN115836070B (zh) * 2020-08-10 2024-08-09 上海和誉生物医药科技有限公司 作为egfr抑制剂的稠环化合物及其制备方法和应用
KR20230094197A (ko) * 2020-09-23 2023-06-27 스코르피온 테라퓨틱스, 인코퍼레이티드 암 치료에 유용한 피롤로[3,2-c]피리딘-4-온 유도체들
WO2022094271A1 (en) * 2020-10-30 2022-05-05 Scorpion Therapeutics, Inc. Methods for treating cancer
WO2022098992A1 (en) * 2020-11-05 2022-05-12 Scorpion Therapeutics, Inc. Use of macrocyclic compounds in methods of treating cancer
EP4244225A1 (en) * 2020-11-11 2023-09-20 Bayer Aktiengesellschaft N-[2-({4-[3-(anilino)-4-oxo-4,5,6,7-tetrahydro-1h-pyrrolo[3,2-c]pyridin-2-yl]pyridin-3-yl)oxy)ethyl]prop-2-enamide derivatives and similar compounds as egfr inhibitors for the treatment of cancer
TW202309022A (zh) 2021-04-13 2023-03-01 美商努法倫特公司 用於治療具egfr突變之癌症之胺基取代雜環
CN118019534A (zh) * 2021-05-06 2024-05-10 细胞基因公司 使用n-((r)-1-(3-氯吡啶-2-基)-2,2,2-三氟乙基)-2-((s)-2,6-二氧代哌啶-3-基)-1-氧代异吲哚啉-5-甲酰胺的治疗方法
CA3246654A1 (en) * 2022-03-24 2023-09-28 Antares Therapeutics, Inc. METHODS FOR SYNTHESIZING EGFR INHIBITORS
US20250282795A1 (en) * 2022-04-20 2025-09-11 Celyn Therapeutics, Inc. EGFR Inhibitors in cancer treatment
WO2026047022A1 (en) 2024-08-28 2026-03-05 Bayer Aktiengesellschaft Stable solid pharmaceutical dosage form comprising crystalline form of her2/mutegfr inhibitor and process for its preparation
WO2026047020A1 (en) 2024-08-28 2026-03-05 Bayer Aktiengesellschaft Crystalline forms of her2/mutegfr inhibitors and process for their preparation
CN119264091B (zh) * 2024-09-04 2025-05-27 康龙化成手性医药技术(宁波)有限公司 一种1,5-双取代-3-氧杂双环[3.1.1]庚烷的合成方法

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015175632A1 (en) 2014-05-13 2015-11-19 Ariad Pharmaceuticals, Inc. Heteroaryl compounds for kinase inhibition
WO2016120196A1 (en) 2015-01-28 2016-08-04 Bayer Pharma Aktiengesellschaft 4h-pyrrolo[3,2-c]pyridin-4-one derivatives

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3966781A (en) 1970-12-17 1976-06-29 Merck Sharp & Dohme (I.A.) Corporation Deuteration of functional group-containing hydrocarbons
US5011472A (en) 1988-09-06 1991-04-30 Brown University Research Foundation Implantable delivery system for biological factors
US6673908B1 (en) * 1999-02-22 2004-01-06 Nuvelo, Inc. Tumor necrosis factor receptor 2
US8299108B2 (en) 2002-03-29 2012-10-30 Novartis Ag Substituted benzazoles and methods of their use as inhibitors of raf kinase
US7211573B2 (en) 2004-12-08 2007-05-01 Hoffmann-La Roche Inc. Malonamide derivatives
DE102006033140A1 (de) 2006-07-18 2008-01-24 Merck Patent Gmbh Aminoindazolharnstoffderivate
BRPI0810498A2 (pt) 2007-04-27 2014-10-14 Sumitomo Chemical Compay Ltd Composto amida e seu uso
ES2424977T3 (es) 2007-08-08 2013-10-10 Glaxosmithkline Intellectual Property Development Limited Derivados de 2-[(2-{fenilamino}-1H-pirrolo[2,3-D]pirimidin-4-il)amino]benzamida como inhibidores de IGF-1R para el tratamiento del cáncer
TWI491610B (zh) 2008-10-09 2015-07-11 必治妥美雅史谷比公司 作為激酶抑制劑之咪唑并嗒腈
US8546413B2 (en) * 2009-06-15 2013-10-01 Nerviano Medical Sciences S.R.L. Substituted pyrimidinylpyrrolopyridinone derivatives, process for their preparation and their use as kinase inhibitors
US8791162B2 (en) 2011-02-14 2014-07-29 Merck Sharp & Dohme Corp. Cathepsin cysteine protease inhibitors
EP3033342A1 (en) 2013-08-13 2016-06-22 Grünenthal GmbH Annelated pyrroles and their use as crac inhibitors
EP3157914B1 (en) 2014-06-17 2018-09-26 Bayer Pharma Aktiengesellschaft 3-amino-1,5,6,7-tetrahydro-4h-indol-4-ones
CA2969771A1 (en) 2014-12-08 2016-06-16 Bayer Pharma Aktiengesellschaft Novel aryl-cyanoguanidine compounds
US10301306B2 (en) 2014-12-15 2019-05-28 Bristol-Myers Squibb Company Substituted dihydro-1H-pyrrolo[3,2-c]pyridin-4(5H)-ones as RIPK3 inhibitors
EP3700904B1 (en) * 2017-10-24 2023-07-19 Bayer AG 4h-pyrrolo[3,2-c]pyridin-4-one derivatives

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015175632A1 (en) 2014-05-13 2015-11-19 Ariad Pharmaceuticals, Inc. Heteroaryl compounds for kinase inhibition
WO2016120196A1 (en) 2015-01-28 2016-08-04 Bayer Pharma Aktiengesellschaft 4h-pyrrolo[3,2-c]pyridin-4-one derivatives

Also Published As

Publication number Publication date
EP3959211B1 (en) 2026-02-18
CA3137218A1 (en) 2020-10-29
KR20220004103A (ko) 2022-01-11
DOP2021000216A (es) 2022-05-15
IL287390A (en) 2021-12-01
SG11202111304UA (en) 2021-11-29
JP7641913B2 (ja) 2025-03-07
TWI849114B (zh) 2024-07-21
JOP20210285A1 (ar) 2023-01-30
CN117986251A (zh) 2024-05-07
GEP20247648B (en) 2024-07-25
PH12021552693A1 (en) 2022-03-21
CN114127064A (zh) 2022-03-01
TW202106683A (zh) 2021-02-16
IL287390B1 (en) 2025-07-01
AU2020262221B2 (en) 2025-11-20
GEAP202415804A (en) 2024-02-12
CR20210530A (es) 2021-12-23
US20220298157A1 (en) 2022-09-22
AU2020262221A1 (en) 2021-11-18
BR112021019998A2 (https=) 2021-12-07
WO2020216781A1 (en) 2020-10-29
MX2021012987A (es) 2022-04-01
ECSP21077614A (es) 2021-11-30
DK3959211T3 (da) 2026-04-27
CN114127064B (zh) 2023-12-26
MA55751A (fr) 2022-03-02
US20250136599A1 (en) 2025-05-01
JP2022532850A (ja) 2022-07-20
UA130453C2 (uk) 2026-02-25
IL287390B2 (en) 2025-11-01
FI3959211T3 (fi) 2026-04-01
CN117946100A (zh) 2024-04-30
CL2021002770A1 (es) 2022-05-27
EP3959211A1 (en) 2022-03-02
CO2021014022A2 (es) 2022-03-29
PE20220254A1 (es) 2022-02-16
BR112021019998B1 (pt) 2024-01-16

Similar Documents

Publication Publication Date Title
KR102915019B1 (ko) 4H-피롤로[3,2-c]피리딘-4-온 화합물
EP3700904B1 (en) 4h-pyrrolo[3,2-c]pyridin-4-one derivatives
US12403135B2 (en) 4H-pyrrolo[3,2-c]pyridin-4-one derivatives
US20240307362A1 (en) 4H-PYRROLO[3,2-c]PYRIDIN-4-ONE COMPOUNDS
US20230064983A1 (en) 3-(anilino)-2-[3-(3-alkoxy-pyridin-4-yl]-1,5,6,7-tetrahydro-4h-pyrrolo[3,2-c]pyridin-4-one derivatives as egfr inhibitors for the treatment of cancer
CA3201333A1 (en) N-[2-({4-[3-(anilino)-4-oxo-4,5,6,7-tetrahydro-1h-pyrrolo[3,2-c]pyridin-2-yl]pyridin-3-yl)oxy)ethyl]prop-2-enamide derivatives and similar compounds as egfr inhibitors for the treatment of cancer
EA046642B1 (ru) 4Н-ПИРРОЛО[3,2-с]ПИРИДИН-4-ОНОВЫЕ СОЕДИНЕНИЯ
WO2024028316A1 (en) 1h-pyrrolo[3,2-b]pyridine derivatives as irreversible inhibitors of mutant egfr for the treatment of cancer
HK40069903A (en) 4h-pyrrolo[3,2-c]pyridin-4-one compounds

Legal Events

Date Code Title Description
PA0105 International application

St.27 status event code: A-0-1-A10-A15-nap-PA0105

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

PA0201 Request for examination

St.27 status event code: A-1-2-D10-D11-exm-PA0201

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

St.27 status event code: A-1-2-D10-D21-exm-PE0902

E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

D22 Grant of ip right intended

Free format text: ST27 STATUS EVENT CODE: A-1-2-D10-D22-EXM-PE0701 (AS PROVIDED BY THE NATIONAL OFFICE)

PE0701 Decision of registration

St.27 status event code: A-1-2-D10-D22-exm-PE0701

F11 Ip right granted following substantive examination

Free format text: ST27 STATUS EVENT CODE: A-2-4-F10-F11-EXM-PR0701 (AS PROVIDED BY THE NATIONAL OFFICE)

PR0701 Registration of establishment

St.27 status event code: A-2-4-F10-F11-exm-PR0701

PR1002 Payment of registration fee

St.27 status event code: A-2-2-U10-U12-oth-PR1002

U12 Designation fee paid

Free format text: ST27 STATUS EVENT CODE: A-2-2-U10-U12-OTH-PR1002 (AS PROVIDED BY THE NATIONAL OFFICE)

PG1601 Publication of registration

St.27 status event code: A-4-4-Q10-Q13-nap-PG1601

Q13 Ip right document published

Free format text: ST27 STATUS EVENT CODE: A-4-4-Q10-Q13-NAP-PG1601 (AS PROVIDED BY THE NATIONAL OFFICE)