CN114127064B - 4H-吡咯并[3,2-c]吡啶-4-酮化合物 - Google Patents

4H-吡咯并[3,2-c]吡啶-4-酮化合物 Download PDF

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Publication number
CN114127064B
CN114127064B CN202080031189.4A CN202080031189A CN114127064B CN 114127064 B CN114127064 B CN 114127064B CN 202080031189 A CN202080031189 A CN 202080031189A CN 114127064 B CN114127064 B CN 114127064B
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Prior art keywords
pyridin
pyrrolo
tetrahydro
methoxy
chloro
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CN202080031189.4A
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English (en)
Chinese (zh)
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CN114127064A (zh
Inventor
S.西格尔
F.西格尔
V.舒尔茨
M.伯格
K.格雷厄姆
D.苏尔兹勒
U.伯默
D.科尔
J.施罗德
U.蒙宁
M.尼休斯
M.迈耶森
H.格罗伊利希
B.卡普兰
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Bayer AG
Dana Farber Cancer Institute Inc
Broad Institute Inc
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Bayer AG
Dana Farber Cancer Institute Inc
Broad Institute Inc
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Priority to CN202311716707.8A priority Critical patent/CN117986251A/zh
Priority to CN202311714944.0A priority patent/CN117946100A/zh
Publication of CN114127064A publication Critical patent/CN114127064A/zh
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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)
CN202080031189.4A 2019-04-24 2020-04-22 4H-吡咯并[3,2-c]吡啶-4-酮化合物 Active CN114127064B (zh)

Priority Applications (2)

Application Number Priority Date Filing Date Title
CN202311716707.8A CN117986251A (zh) 2019-04-24 2020-04-22 4H-吡咯并[3,2-c]吡啶-4-酮化合物
CN202311714944.0A CN117946100A (zh) 2019-04-24 2020-04-22 4H-吡咯并[3,2-c]吡啶-4-酮化合物

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

Related Child Applications (2)

Application Number Title Priority Date Filing Date
CN202311716707.8A Division CN117986251A (zh) 2019-04-24 2020-04-22 4H-吡咯并[3,2-c]吡啶-4-酮化合物
CN202311714944.0A Division CN117946100A (zh) 2019-04-24 2020-04-22 4H-吡咯并[3,2-c]吡啶-4-酮化合物

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CN114127064A CN114127064A (zh) 2022-03-01
CN114127064B true CN114127064B (zh) 2023-12-26

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CN202080031189.4A Active CN114127064B (zh) 2019-04-24 2020-04-22 4H-吡咯并[3,2-c]吡啶-4-酮化合物
CN202311716707.8A Pending CN117986251A (zh) 2019-04-24 2020-04-22 4H-吡咯并[3,2-c]吡啶-4-酮化合物
CN202311714944.0A Pending CN117946100A (zh) 2019-04-24 2020-04-22 4H-吡咯并[3,2-c]吡啶-4-酮化合物

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CN202311716707.8A Pending CN117986251A (zh) 2019-04-24 2020-04-22 4H-吡咯并[3,2-c]吡啶-4-酮化合物
CN202311714944.0A Pending CN117946100A (zh) 2019-04-24 2020-04-22 4H-吡咯并[3,2-c]吡啶-4-酮化合物

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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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CN107406417A (zh) * 2015-01-28 2017-11-28 拜耳制药股份公司 4H‑吡咯并[3,2‑c]吡啶‑4‑酮衍生物

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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
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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