JP7424639B2 - ３－（５－フルオロベンゾフラン－３－イル）－４－（５－メチル－５Ｈ－［１，３］ジオキソロ［４，５－ｆ］インドール－７－イル）ピロール－２，５－ジオンの固体形態 - Google Patents

３－（５－フルオロベンゾフラン－３－イル）－４－（５－メチル－５Ｈ－［１，３］ジオキソロ［４，５－ｆ］インドール－７－イル）ピロール－２，５－ジオンの固体形態 Download PDF

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JP7424639B2
JP7424639B2 JP2020530441A JP2020530441A JP7424639B2 JP 7424639 B2 JP7424639 B2 JP 7424639B2 JP 2020530441 A JP2020530441 A JP 2020530441A JP 2020530441 A JP2020530441 A JP 2020530441A JP 7424639 B2 JP7424639 B2 JP 7424639B2
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solvate
cancer
mixture
ethyl acetate
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JP2020530497A (ja
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チャン、ヤミン
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アクチュエイト セラピューティクス インク．
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/056—Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Medicinal Preparation (AREA)
JP2020530441A 2017-08-11 2018-08-10 ３－（５－フルオロベンゾフラン－３－イル）－４－（５－メチル－５Ｈ－［１，３］ジオキソロ［４，５－ｆ］インドール－７－イル）ピロール－２，５－ジオンの固体形態 Active JP7424639B2 (ja)

Priority Applications (2)

Application Number Priority Date Filing Date Title
JP2023123302A JP7778750B2 (ja) 2017-08-11 2023-07-28 ３－（５－フルオロベンゾフラン－３－イル）－４－（５－メチル－５Ｈ－［１，３］ジオキソロ［４，５－ｆ］インドール－７－イル）ピロール－２，５－ジオンの固体形態
JP2025168516A JP2026012715A (ja) 2017-08-11 2025-10-06 ３－（５－フルオロベンゾフラン－３－イル）－４－（５－メチル－５Ｈ－［１，３］ジオキソロ［４，５－ｆ］インドール－７－イル）ピロール－２，５－ジオンの固体形態

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762544277P 2017-08-11 2017-08-11
US62/544,277 2017-08-11
PCT/US2018/046203 WO2019032958A1 (en) 2017-08-11 2018-08-10 SOLID FORMS OF 3- (5-FLUOROBENZOFURAN-3-YL) -4- (5-METHYL-5H [1,3] DIOXOLO [4,5-F] INDOL-7-YL) PYRROLE-2,5-DIONE

Related Child Applications (1)

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JP2023123302A Division JP7778750B2 (ja) 2017-08-11 2023-07-28 ３－（５－フルオロベンゾフラン－３－イル）－４－（５－メチル－５Ｈ－［１，３］ジオキソロ［４，５－ｆ］インドール－７－イル）ピロール－２，５－ジオンの固体形態

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JP2020530497A JP2020530497A (ja) 2020-10-22
JP2020530497A5 JP2020530497A5 (https=) 2021-09-09
JP7424639B2 true JP7424639B2 (ja) 2024-01-30

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JP2020530441A Active JP7424639B2 (ja) 2017-08-11 2018-08-10 ３－（５－フルオロベンゾフラン－３－イル）－４－（５－メチル－５Ｈ－［１，３］ジオキソロ［４，５－ｆ］インドール－７－イル）ピロール－２，５－ジオンの固体形態
JP2023123302A Active JP7778750B2 (ja) 2017-08-11 2023-07-28 ３－（５－フルオロベンゾフラン－３－イル）－４－（５－メチル－５Ｈ－［１，３］ジオキソロ［４，５－ｆ］インドール－７－イル）ピロール－２，５－ジオンの固体形態
JP2025168516A Pending JP2026012715A (ja) 2017-08-11 2025-10-06 ３－（５－フルオロベンゾフラン－３－イル）－４－（５－メチル－５Ｈ－［１，３］ジオキソロ［４，５－ｆ］インドール－７－イル）ピロール－２，５－ジオンの固体形態

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Application Number Title Priority Date Filing Date
JP2023123302A Active JP7778750B2 (ja) 2017-08-11 2023-07-28 ３－（５－フルオロベンゾフラン－３－イル）－４－（５－メチル－５Ｈ－［１，３］ジオキソロ［４，５－ｆ］インドール－７－イル）ピロール－２，５－ジオンの固体形態
JP2025168516A Pending JP2026012715A (ja) 2017-08-11 2025-10-06 ３－（５－フルオロベンゾフラン－３－イル）－４－（５－メチル－５Ｈ－［１，３］ジオキソロ［４，５－ｆ］インドール－７－イル）ピロール－２，５－ジオンの固体形態

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US (3) US11136334B2 (https=)
EP (1) EP3665176B1 (https=)
JP (3) JP7424639B2 (https=)
KR (3) KR102700883B1 (https=)
CN (2) CN117362305A (https=)
AU (3) AU2018313259B2 (https=)
BR (1) BR112020002892A2 (https=)
CA (1) CA3072240A1 (https=)
DK (1) DK3665176T3 (https=)
ES (1) ES2974328T3 (https=)
FI (1) FI3665176T3 (https=)
IL (2) IL272556B2 (https=)
MX (3) MX2020001547A (https=)
PL (1) PL3665176T3 (https=)
PT (1) PT3665176T (https=)
WO (1) WO2019032958A1 (https=)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL3697794T3 (pl) 2017-10-16 2026-04-07 Actuate Therapeutics Inc. Stałe postacie 3-(5-fluorobenzofuran-3-ylo)-4-(5-metylo-5h-[1,3]dioksolo[4,5-f]indol-7-ilo)pirolo-2,5-dionu
WO2019222483A1 (en) * 2018-05-17 2019-11-21 Board Of Regents, The University Of Texas System Treatment of idiopathic pulmonary fibrosis with glycogen synthase kinase 3 form beta inhibitors
US20250325517A1 (en) * 2022-06-27 2025-10-23 Actuate Therapeutics, Inc. Oral dosage forms of elraglusib

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008077138A1 (en) 2006-12-19 2008-06-26 The Board Of Trustees Of The University Of Illinois 3-benzofuranyl-4-indolyl maleimides as potent gsk3 inhibitors for neurogenerative disorders
JP2013515737A (ja) 2009-12-23 2013-05-09 アークル インコーポレイテッド 精製されたピロロキノリニル−ピロリジン−２，５−ジオン組成物ならびにその調製方法および使用方法

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008077138A1 (en) 2006-12-19 2008-06-26 The Board Of Trustees Of The University Of Illinois 3-benzofuranyl-4-indolyl maleimides as potent gsk3 inhibitors for neurogenerative disorders
JP2013515737A (ja) 2009-12-23 2013-05-09 アークル インコーポレイテッド 精製されたピロロキノリニル−ピロリジン−２，５−ジオン組成物ならびにその調製方法および使用方法

Non-Patent Citations (6)

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Title
IRINA N GAISINA; ET AL，FROM A NATURAL PRODUCT LEAD TO THE IDENTIFICATION OF POTENT AND SELECTIVE BENZOFURAN-，JOURNAL OF MEDICINAL CHEMISTRY，AMERICAN CHEMICAL SOCIETY，2009年04月09日，VOL:52, NR:7，PAGE(S):1853 - 1863，http://dx.doi.org/10.1021/jm801317h，3-YL-(INDOL-3-YL)MALEIMIDES AS GLYCOGEN SYNTHASE KINASE 3β INHIBITORS THAT SUPPRESS
IRINA N GAISINA; ET AL，FROM A NATURAL PRODUCT LEAD TO THE IDENTIFICATION OF POTENT AND SELECTIVE BENZOFURAN-以下備考，JOURNAL OF MEDICINAL CHEMISTRY，AMERICAN CHEMICAL SOCIETY，2009年04月09日，VOL:52, NR:7，PAGE(S):1853 - 1863，http://dx.doi.org/10.1021/jm801317h，3-YL-(INDOL-3-YL)MALEIMIDES AS GLYCOGEN SYNTHASE KINASE 3β INHIBITORS THAT SUPPRESS 以下省略
PAL K; ET AL，INHIBITION OF GSK-3 INDUCES DIFFERENTIATION AND IMPAIRED GLUCOSE METABOLISM IN RENAL CANCER，MOLECULAR CANCER THERAPEUTICS，米国，AMERICAN ASSOCIATION FOR CANCER RESEARCH，2013年12月10日，VOL:13, NR:2，PAGE(S):285 - 296，http://dx.doi.org/10.1158/1535-7163.MCT-13-0681
PHARM TECH JAPAN，2002年，Vol.18, No.10，pp.1629-1644
平山令明，有機化合物結晶作製ハンドブック，2008年，p.17-23,37-40,45-51,57-65
杉本功、高橋嘉輝，溶媒和物、非晶質固体と医薬品製剤，紛体工学会誌，1985年，22(2)，p.85-97

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CN117362305A (zh) 2024-01-09
MX2020001547A (es) 2020-08-03
ES2974328T3 (es) 2024-06-26
PL3665176T3 (pl) 2024-06-17
JP7778750B2 (ja) 2025-12-02
IL313800A (en) 2024-08-01
BR112020002892A2 (pt) 2020-08-04
KR102700883B1 (ko) 2024-09-02
JP2023156372A (ja) 2023-10-24
KR20240063198A (ko) 2024-05-09
KR20250070131A (ko) 2025-05-20
AU2025202936A1 (en) 2025-05-15
CN111247153B (zh) 2024-04-02
US20220009939A1 (en) 2022-01-13
MX2024003249A (es) 2024-04-04
IL272556B1 (en) 2024-09-01
AU2023201059A1 (en) 2023-03-23
EP3665176A1 (en) 2020-06-17
DK3665176T3 (da) 2024-03-25
JP2020530497A (ja) 2020-10-22
US20250115616A1 (en) 2025-04-10
US20200223861A1 (en) 2020-07-16
WO2019032958A1 (en) 2019-02-14
US11136334B2 (en) 2021-10-05
AU2018313259B2 (en) 2022-11-24
CA3072240A1 (en) 2019-02-14
AU2023201059B2 (en) 2025-04-03
PT3665176T (pt) 2024-03-13
AU2018313259A1 (en) 2020-02-27
EP3665176B1 (en) 2024-01-24
US12145943B2 (en) 2024-11-19
KR20200040799A (ko) 2020-04-20
FI3665176T3 (fi) 2024-03-20
IL272556A (en) 2020-03-31
MX2023005875A (es) 2023-06-05
CN111247153A (zh) 2020-06-05
JP2026012715A (ja) 2026-01-27
IL272556B2 (en) 2025-01-01

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