AU2020264143B2 - Crystal form S4 of the PLK4 inhibitor (1R,2S)-(E)-2-(3-(4-((cis-2,6-dimethylmorpholino)methyl)styryl)- 1 H-imidazol-6- yl)-5'-methoxyspiro(cyclopropane-1,3'-indolin)-2'-one fumarate - Google Patents

Crystal form S4 of the PLK4 inhibitor (1R,2S)-(E)-2-(3-(4-((cis-2,6-dimethylmorpholino)methyl)styryl)- 1 H-imidazol-6- yl)-5'-methoxyspiro(cyclopropane-1,3'-indolin)-2'-one fumarate

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Publication number
AU2020264143B2
AU2020264143B2 AU2020264143A AU2020264143A AU2020264143B2 AU 2020264143 B2 AU2020264143 B2 AU 2020264143B2 AU 2020264143 A AU2020264143 A AU 2020264143A AU 2020264143 A AU2020264143 A AU 2020264143A AU 2020264143 B2 AU2020264143 B2 AU 2020264143B2
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cancer
compound
fumarate salt
crystal form
fumaric acid
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AU2020264143A
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AU2020264143A1 (en
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Mark Robert Bray
Sze-Wan Li
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University Health Network
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University Health Network
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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)
AU2020264143A 2019-04-24 2020-04-23 Crystal form S4 of the PLK4 inhibitor (1R,2S)-(E)-2-(3-(4-((cis-2,6-dimethylmorpholino)methyl)styryl)- 1 H-imidazol-6- yl)-5'-methoxyspiro(cyclopropane-1,3'-indolin)-2'-one fumarate Active AU2020264143B2 (en)

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 (2)

Publication Number Publication Date
AU2020264143A1 AU2020264143A1 (en) 2021-10-28
AU2020264143B2 true AU2020264143B2 (en) 2026-05-21

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Family Applications (1)

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AU2020264143A Active AU2020264143B2 (en) 2019-04-24 2020-04-23 Crystal form S4 of the PLK4 inhibitor (1R,2S)-(E)-2-(3-(4-((cis-2,6-dimethylmorpholino)methyl)styryl)- 1 H-imidazol-6- yl)-5'-methoxyspiro(cyclopropane-1,3'-indolin)-2'-one fumarate

Country Status (16)

Country Link
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)

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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

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3057965A1 (en) * 2013-10-18 2016-08-24 University Health Network Salt and crystal forms of plk-4 inhibitor

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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
EA030089B1 (ru) 2013-10-18 2018-06-29 Юниверсити Хелс Нетуорк Лечение рака поджелудочной железы

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3057965A1 (en) * 2013-10-18 2016-08-24 University Health Network Salt and crystal forms of plk-4 inhibitor

Also Published As

Publication number Publication date
SA521430647B1 (ar) 2024-01-27
KR20220004102A (ko) 2022-01-11
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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