BR112021019998B1 - 4h-pirrolo[3,2-c]piridin-4-ona, seus usos, composição farmacêutica, e kit de partes - Google Patents

4h-pirrolo[3,2-c]piridin-4-ona, seus usos, composição farmacêutica, e kit de partes Download PDF

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Publication number
BR112021019998B1
BR112021019998B1 BR112021019998-5A BR112021019998A BR112021019998B1 BR 112021019998 B1 BR112021019998 B1 BR 112021019998B1 BR 112021019998 A BR112021019998 A BR 112021019998A BR 112021019998 B1 BR112021019998 B1 BR 112021019998B1
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BR
Brazil
Prior art keywords
pyridin
pyrrolo
tetrahydro
methoxy
dioxan
Prior art date
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BR112021019998-5A
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English (en)
Portuguese (pt)
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BR112021019998A2 (https=
Inventor
Stephan Siegel
Franziska SIEGEL
Volker Schulze
Markus Berger
Keith Graham
Detlev Sülzle
Ulf Bömer
Daniel Korr
Jens Schröder
Ursula Mönning
Michael Niehues
Matthew Meyerson
Heidi Greulich
Bethany Kaplan
Original Assignee
The Broad Institute, Inc.
Dana-Farber Cancer Institute, Inc.
Bayer Aktiengesellschaft
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.)
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Publication date
Application filed by The Broad Institute, Inc., Dana-Farber Cancer Institute, Inc., Bayer Aktiengesellschaft filed Critical The Broad Institute, Inc.
Publication of BR112021019998A2 publication Critical patent/BR112021019998A2/pt
Publication of BR112021019998B1 publication Critical patent/BR112021019998B1/pt

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    • 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

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  • 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)
BR112021019998-5A 2019-04-24 2020-04-22 4h-pirrolo[3,2-c]piridin-4-ona, seus usos, composição farmacêutica, e kit de partes BR112021019998B1 (pt)

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
BR112021019998A2 BR112021019998A2 (https=) 2021-12-07
BR112021019998B1 true BR112021019998B1 (pt) 2024-01-16

Family

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Family Applications (1)

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BR112021019998-5A BR112021019998B1 (pt) 2019-04-24 2020-04-22 4h-pirrolo[3,2-c]piridin-4-ona, seus usos, composição farmacêutica, e kit de partes

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=)

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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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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
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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
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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
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

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Legal Events

Date Code Title Description
B06A Patent application procedure suspended [chapter 6.1 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 22/04/2020, OBSERVADAS AS CONDICOES LEGAIS