TWI748541B - ｅＩＦ４Ｅ抑制性化合物與方法 - Google Patents

ｅＩＦ４Ｅ抑制性化合物與方法 Download PDF

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Publication number
TWI748541B
TWI748541B TW109122116A TW109122116A TWI748541B TW I748541 B TWI748541 B TW I748541B TW 109122116 A TW109122116 A TW 109122116A TW 109122116 A TW109122116 A TW 109122116A TW I748541 B TWI748541 B TW I748541B
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Taiwan
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cancer
mmol
alkyl
compound
reaction mixture
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TW109122116A
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English (en)
Chinese (zh)
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TW202115058A (zh
Inventor
山繆爾 史派瑞
新 向
賈斯汀 恩斯特
席格菲 瑞奇
保羅 史倫格勒
麥克 夏赫菲
帝歐 米榭爾斯
克利斯汀 奈爾維斯基
金 崔倫
格瑞克 派卡德
艾倫 格普斯
卡維里 烏卡蘭
向山貴祐
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美商ｅＦＦＥＣＴＯＲ醫療公司
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Publication of TW202115058A publication Critical patent/TW202115058A/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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
TW109122116A 2019-07-02 2020-06-30 ｅＩＦ４Ｅ抑制性化合物與方法 TWI748541B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962869662P 2019-07-02 2019-07-02
US62/869,662 2019-07-02

Publications (2)

Publication Number Publication Date
TW202115058A TW202115058A (zh) 2021-04-16
TWI748541B true TWI748541B (zh) 2021-12-01

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TW109122116A TWI748541B (zh) 2019-07-02 2020-06-30 ｅＩＦ４Ｅ抑制性化合物與方法

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US (2) US11286268B1 (https=)
EP (1) EP3994139A1 (https=)
JP (1) JP7595055B2 (https=)
KR (1) KR20220061945A (https=)
CN (1) CN114269756B (https=)
AR (1) AR119339A1 (https=)
AU (1) AU2020299362B2 (https=)
BR (1) BR112021026682A2 (https=)
CA (2) CA3085255A1 (https=)
CL (1) CL2021003573A1 (https=)
IL (1) IL289456A (https=)
PY (1) PY2031844A (https=)
TW (1) TWI748541B (https=)
UY (1) UY38773A (https=)
WO (1) WO2021003157A1 (https=)

Families Citing this family (9)

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Publication number Priority date Publication date Assignee Title
US20220378821A1 (en) * 2019-07-02 2022-12-01 Effector Therapeutics, Inc. Methods of treating braf-mutated cancer cells
EP4076438A4 (en) * 2019-12-18 2023-11-29 Merck Sharp & Dohme LLC BICYCLIC HETEROCYCLIC COMPOUNDS AND THEIR USE FOR THE TREATMENT OF HERPES VIRUSES
WO2021240337A1 (en) * 2020-05-27 2021-12-02 Effector Therapeutics, Inc. Covalent modifiers of eif4e inhibiting compounds
JP2023554521A (ja) 2020-12-22 2023-12-27 ファイザー・インク Ｅｉｆ４ｅ阻害剤の固体形態
JP2025539263A (ja) * 2022-11-10 2025-12-04 リボメトリックス，インコーポレイティド ｅＩＦ４Ｅ阻害剤としての化合物及び組成物、ならびにそれらの使用
TW202428278A (zh) * 2022-12-23 2024-07-16 大陸商南京聖和藥業股份有限公司 作為ｅＩＦ４Ｅ抑制劑的化合物及其應用
IL326137A (en) 2023-07-28 2026-03-01 Cogent Biosciences Inc PI3K inhibitors
WO2025101516A1 (en) * 2023-11-06 2025-05-15 Ribometrix, Inc. Methods of using eif4e inhibitors for treating cancer
WO2025120599A1 (en) * 2023-12-08 2025-06-12 Ribometrix, Inc. METHODS OF USING eIF4E INHIBITORS FOR TREATING CANCER

Citations (1)

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WO2014179237A1 (en) * 2013-04-29 2014-11-06 Vanderbilt University Substituted 3-benzylquinoxalin-4(3h)-one analogs as positive allosteric modulators of muscarinic acetycholine receptor m1

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Publication number Priority date Publication date Assignee Title
US20080255161A1 (en) * 2007-04-11 2008-10-16 Dmitry Koltun 3-HYDROQUINAZOLIN-4-ONE DERIVATIVES FOR USE AS STEAROYL CoA DESATURASE INHIBITORS
US20110065671A1 (en) * 2008-05-19 2011-03-17 Harris Joel M Bicyclic heterocycle derivatives and use thereof as gpr119 modulators
TW201412740A (zh) 2012-09-20 2014-04-01 Bayer Pharma AG 經取代之吡咯并嘧啶胺基苯并噻唑酮
WO2015120350A2 (en) 2014-02-07 2015-08-13 Effector Therapeutics, Inc. Compositions and methods for treating fibrotic disease
TWI713455B (zh) 2014-06-25 2020-12-21 美商伊凡克特治療公司 ＭｎＫ抑制劑及其相關方法

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014179237A1 (en) * 2013-04-29 2014-11-06 Vanderbilt University Substituted 3-benzylquinoxalin-4(3h)-one analogs as positive allosteric modulators of muscarinic acetycholine receptor m1

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Giri RS, et al. "Synthesis and evaluation of quinazolinone derivatives as inhibitors of NF-kappaB, AP-1 mediated transcription and eIF-4E mediated translational activation: inhibitors of multi-phathways involve in cancer" European Journal of Medicinal Chemistry 2010;45(9):3558-3563 *

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Publication number Publication date
CN114269756A (zh) 2022-04-01
CA3188446A1 (en) 2021-01-07
AU2020299362A1 (en) 2022-02-24
PY2031844A (es) 2021-04-19
JP7595055B2 (ja) 2024-12-05
CA3085255A1 (en) 2021-01-02
WO2021003157A1 (en) 2021-01-07
IL289456A (en) 2022-02-01
JP2022539256A (ja) 2022-09-07
KR20220061945A (ko) 2022-05-13
AR119339A1 (es) 2021-12-09
UY38773A (es) 2021-01-29
BR112021026682A2 (pt) 2022-03-15
CL2021003573A1 (es) 2022-08-12
US11286268B1 (en) 2022-03-29
TW202115058A (zh) 2021-04-16
CN114269756B (zh) 2024-05-14
EP3994139A1 (en) 2022-05-11
US20230108594A1 (en) 2023-04-06
AU2020299362B2 (en) 2026-02-26

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