TWI849114B - 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
TWI849114B
TWI849114B TW109113538A TW109113538A TWI849114B TW I849114 B TWI849114 B TW I849114B TW 109113538 A TW109113538 A TW 109113538A TW 109113538 A TW109113538 A TW 109113538A TW I849114 B TWI849114 B TW I849114B
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Taiwan
Prior art keywords
pyridin
pyrrolo
tetrahydro
methoxy
chloro
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TW109113538A
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English (en)
Chinese (zh)
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TW202106683A (zh
Inventor
史蒂芬 史基爾
弗蘭齊斯卡 史基爾
沃克 舒爾
馬克斯 柏格
凱斯 格雷漢姆
德特樂芙 蘇爾茲樂
爾芙 巴馬爾
丹尼爾 柯爾
詹斯 施勒德
爾蘇拉 摩尼
麥克爾 尼霍斯
馬修 邁伊爾森
海蒂 格羅伊奇
貝瑟尼 卡普蘭
Original Assignee
德商拜耳廠股份有限公司
美商博德研究所有限公司
美商達納 法伯癌症協會
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Publication of TW202106683A publication Critical patent/TW202106683A/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)
TW109113538A 2019-04-24 2020-04-22 4H-吡咯并[3,2-c]吡啶-4-酮化合物 TWI849114B (zh)

Applications Claiming Priority (4)

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

Publications (2)

Publication Number Publication Date
TW202106683A TW202106683A (zh) 2021-02-16
TWI849114B true TWI849114B (zh) 2024-07-21

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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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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
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
BR112021019998B1 (pt) 2024-01-16

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