GEP20247648B - 4h-pyrrolo[3,2-c]pyridin-4-one compounds - Google Patents

4h-pyrrolo[3,2-c]pyridin-4-one compounds

Info

Publication number
GEP20247648B
GEP20247648B GEAP202015804A GEAP2020015804A GEP20247648B GE P20247648 B GEP20247648 B GE P20247648B GE AP202015804 A GEAP202015804 A GE AP202015804A GE AP2020015804 A GEAP2020015804 A GE AP2020015804A GE P20247648 B GEP20247648 B GE P20247648B
Authority
GE
Georgia
Prior art keywords
compounds
pyrrolo
pyridin
deseases
hyperproliferative
Prior art date
Application number
GEAP202015804A
Other languages
English (en)
Inventor
Ursula Mönning
Michael Niehues
Franziska Siegel
Keith Graham
Stephan Siegel
Matthew Meyerson
Heidi Greulich
Jens SCHRÖDER
Volker Schulze
Daniel Korr
Bethany Kaplan
Ulf Bömer
Markus Berger
Detlev Sülzle
Original Assignee
Bayer Ag
Dana Farber Cancer Inst Inc
Broad Inst Inc
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 Bayer Ag, Dana Farber Cancer Inst Inc, Broad Inst Inc filed Critical Bayer Ag
Publication of GEP20247648B publication Critical patent/GEP20247648B/en

Links

Classifications

    • 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
    • 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • 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
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • 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
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs 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)
GEAP202015804A 2019-04-24 2020-04-22 4h-pyrrolo[3,2-c]pyridin-4-one compounds GEP20247648B (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962838051P 2019-04-24 2019-04-24
US201962940036P 2019-11-25 2019-11-25

Publications (1)

Publication Number Publication Date
GEP20247648B true GEP20247648B (en) 2024-07-25

Family

ID=70456765

Family Applications (2)

Application Number Title Priority Date Filing Date
GEAP202015804A GEP20247648B (en) 2019-04-24 2020-04-22 4h-pyrrolo[3,2-c]pyridin-4-one compounds
GEAP202415804A GEAP202415804A (en) 2019-04-24 2020-04-22 4h-pyrrolo[3,2-c]pyridin-4-one compounds

Family Applications After (1)

Application Number Title Priority Date Filing Date
GEAP202415804A GEAP202415804A (en) 2019-04-24 2020-04-22 4h-pyrrolo[3,2-c]pyridin-4-one compounds

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

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US3966781A (en) 1970-12-17 1976-06-29 Merck Sharp & Dohme (I.A.) Corporation Deuteration of functional group-containing hydrocarbons
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US8299108B2 (en) 2002-03-29 2012-10-30 Novartis Ag Substituted benzazoles and methods of their use as inhibitors of raf kinase
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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
JP6468611B2 (ja) * 2014-05-13 2019-02-13 アリアド ファーマシューティカルズ, インコーポレイテッド キナーゼ阻害のためのヘテロアリール化合物
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
TN2017000329A1 (en) * 2015-01-28 2019-01-16 Bayer Pharma AG 4h-pyrrolo[3,2-c]pyridin-4-one derivatives
EP3700904B1 (en) * 2017-10-24 2023-07-19 Bayer AG 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
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
KR102915019B1 (ko) 2026-01-21
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

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