KR20220004102A - Plk4 억제제 (1r,2s)-(e)-2-(3-(4-((시스-2,6-디메틸모르폴리노)메틸)스티릴)-1h-이미다졸-6-일)-5'-메톡시스피로[시클로프로판-1,3'-인돌린]-2'-온 푸마레이트의 결정 형태 s4 - Google Patents

Plk4 억제제 (1r,2s)-(e)-2-(3-(4-((시스-2,6-디메틸모르폴리노)메틸)스티릴)-1h-이미다졸-6-일)-5'-메톡시스피로[시클로프로판-1,3'-인돌린]-2'-온 푸마레이트의 결정 형태 s4 Download PDF

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Publication number
KR20220004102A
KR20220004102A KR1020217037777A KR20217037777A KR20220004102A KR 20220004102 A KR20220004102 A KR 20220004102A KR 1020217037777 A KR1020217037777 A KR 1020217037777A KR 20217037777 A KR20217037777 A KR 20217037777A KR 20220004102 A KR20220004102 A KR 20220004102A
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South Korea
Prior art keywords
cancer
compound
fumarate salt
crystalline form
fumaric acid
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KR1020217037777A
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English (en)
Korean (ko)
Inventor
스쩌-완 리
마크 로버트 브레이
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유니버시티 헬스 네트워크
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Publication of KR20220004102A publication Critical patent/KR20220004102A/ko
Ceased legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
KR1020217037777A 2019-04-24 2020-04-23 Plk4 억제제 (1r,2s)-(e)-2-(3-(4-((시스-2,6-디메틸모르폴리노)메틸)스티릴)-1h-이미다졸-6-일)-5'-메톡시스피로[시클로프로판-1,3'-인돌린]-2'-온 푸마레이트의 결정 형태 s4 Ceased KR20220004102A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962837858P 2019-04-24 2019-04-24
US62/837,858 2019-04-24
PCT/CA2020/050535 WO2020215155A1 (en) 2019-04-24 2020-04-23 Crystal form s4 of the plk4 inhibitor (lr,2s)-(e)-2-(3-(4-((cis-2,6-dimethylmorpholino)methyl)styryl)- 1 h-imidazol-6- yl)-5'-methoxyspiro[cyclopropane-l,3'-indolin]-2'-one fumarate

Publications (1)

Publication Number Publication Date
KR20220004102A true KR20220004102A (ko) 2022-01-11

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KR1020217037777A Ceased KR20220004102A (ko) 2019-04-24 2020-04-23 Plk4 억제제 (1r,2s)-(e)-2-(3-(4-((시스-2,6-디메틸모르폴리노)메틸)스티릴)-1h-이미다졸-6-일)-5'-메톡시스피로[시클로프로판-1,3'-인돌린]-2'-온 푸마레이트의 결정 형태 s4

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US (1) US12325700B2 (enExample)
EP (1) EP3959209A4 (enExample)
JP (1) JP7705351B2 (enExample)
KR (1) KR20220004102A (enExample)
CN (1) CN113966330B (enExample)
AU (1) AU2020264143B2 (enExample)
BR (1) BR112021021106A2 (enExample)
CA (1) CA3137191A1 (enExample)
EA (1) EA202192903A1 (enExample)
IL (1) IL287394A (enExample)
MA (1) MA55767A (enExample)
MX (1) MX2021012993A (enExample)
SA (1) SA521430647B1 (enExample)
SG (1) SG11202111003UA (enExample)
TW (1) TWI862582B (enExample)
WO (1) WO2020215155A1 (enExample)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20220124177A (ko) 2019-12-06 2022-09-13 유니버시티 헬스 네트워크 급성 골수성 백혈병 또는 골수형성이상증후군의 치료방법
TWI926033B (zh) 2021-05-11 2026-05-21 美商歐瑞克製藥公司 類ｐｏｌｏ激酶４抑制劑

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7205328B2 (en) 2002-10-21 2007-04-17 Irm Llc Oxindoles with anti-HIV activity
DE102005005395A1 (de) 2005-02-03 2006-08-10 Schering Aktiengesellschaft Thiazolidinone, deren Herstellung und Verwendung als Arzneimittel
GB0606234D0 (en) 2006-03-29 2006-05-10 Pliva Istrazivanje I Razvoj D Pharmaceutically acceptable salts and polymorphic forms
BRPI0817315A2 (pt) 2007-09-25 2015-03-17 Takeda Pharmaceutical Inibidores de quinase do tipo polo
EP2235004A4 (en) 2007-12-21 2011-05-04 Univ Health Network INDAZOLYL, BENZIMIDAZOLYL, BENZOTRIAZOLYL-SUBSTITUTED INDOLUND DERIVATIVES AS A KINASE-HEMMER FOR CANCER TREATMENT
WO2010115279A1 (en) 2009-04-06 2010-10-14 University Health Network Kinase inhibitors and method of treating cancer with same
WO2010125004A1 (en) 2009-04-29 2010-11-04 Nerviano Medical Sciences S.R.L. Cdk inhibitor salts
TWI516262B (zh) 2010-04-06 2016-01-11 健康網路大學 激酶抑制劑及以其治療癌症的方法
CA2803446C (en) 2010-07-02 2019-06-04 University Health Network Use of plk4 antagonists for treating pten mutant diseases
WO2012048411A1 (en) 2010-10-13 2012-04-19 University Health Network Plk-4 inhibitors and method of treating cancer with same
JP5808818B2 (ja) 2010-11-25 2015-11-10 ラツィオファーム・ゲーエムベーハー アファチニブの新規塩及び多形形態
EP2766352B1 (en) 2011-10-12 2018-06-06 University Health Network (UHN) Indazole compounds as kinase inhibitors and method of treating cancer with same
TR201902875T4 (tr) * 2013-10-18 2019-03-21 Univ Health Network Plk-4 inhibitörünün tuz ve kristal formları.
EA030089B1 (ru) 2013-10-18 2018-06-29 Юниверсити Хелс Нетуорк Лечение рака поджелудочной железы

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Publication number Publication date
AU2020264143B2 (en) 2026-05-21
SA521430647B1 (ar) 2024-01-27
CN113966330B (zh) 2024-09-13
MX2021012993A (es) 2021-12-10
TW202104216A (zh) 2021-02-01
JP7705351B2 (ja) 2025-07-09
CN113966330A (zh) 2022-01-21
WO2020215155A8 (en) 2020-11-26
EA202192903A1 (ru) 2022-02-09
EP3959209A4 (en) 2022-12-28
JP2022530028A (ja) 2022-06-27
AU2020264143A1 (en) 2021-10-28
CA3137191A1 (en) 2020-10-29
EP3959209A1 (en) 2022-03-02
SG11202111003UA (en) 2021-11-29
MA55767A (fr) 2022-03-02
TWI862582B (zh) 2024-11-21
US20220204494A1 (en) 2022-06-30
WO2020215155A1 (en) 2020-10-29
US12325700B2 (en) 2025-06-10
BR112021021106A2 (pt) 2021-12-14
IL287394A (en) 2021-12-01

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