EA023173B1 - Ингибиторы киназы и способ лечения злокачественной опухоли с их помощью - Google Patents

Ингибиторы киназы и способ лечения злокачественной опухоли с их помощью Download PDF

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Publication number
EA023173B1
EA023173B1 EA201270752A EA201270752A EA023173B1 EA 023173 B1 EA023173 B1 EA 023173B1 EA 201270752 A EA201270752 A EA 201270752A EA 201270752 A EA201270752 A EA 201270752A EA 023173 B1 EA023173 B1 EA 023173B1
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EA
Eurasian Patent Office
Prior art keywords
mmol
title compound
indazol
indoline
cyclopropan
Prior art date
Application number
EA201270752A
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English (en)
Russian (ru)
Other versions
EA201270752A1 (ru
Inventor
Питер Брент Сампсон
Юн Лю
Сцзе-Вань Ли
Брайан Т. Форрест
Хайнц В. Паулс
Луис Г. Эдвардс
Миклос Фехер
Нарендра Кумар Б. Пател
Радослав Лауфер
Гуохуа Пан
Original Assignee
Юниверсити Хелс Нетворк
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Priority claimed from PCT/CA2010/000518 external-priority patent/WO2010115279A1/en
Application filed by Юниверсити Хелс Нетворк filed Critical Юниверсити Хелс Нетворк
Publication of EA201270752A1 publication Critical patent/EA201270752A1/ru
Publication of EA023173B1 publication Critical patent/EA023173B1/ru

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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
    • C07D403/10—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 linked by a carbon chain containing aromatic 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
    • A61K31/40—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
    • A61K31/403—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 carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • 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
    • 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
    • C07D403/14—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 three or more hetero rings
    • 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
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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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)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Indole Compounds (AREA)
EA201270752A 2010-04-06 2011-04-06 Ингибиторы киназы и способ лечения злокачественной опухоли с их помощью EA023173B1 (ru)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US32133210P 2010-04-06 2010-04-06
US32132910P 2010-04-06 2010-04-06
PCT/CA2010/000518 WO2010115279A1 (en) 2009-04-06 2010-04-06 Kinase inhibitors and method of treating cancer with same
PCT/CA2011/000386 WO2011123946A1 (en) 2010-04-06 2011-04-06 Kinase inhibitors and method of treating cancer with same

Publications (2)

Publication Number Publication Date
EA201270752A1 EA201270752A1 (ru) 2013-04-30
EA023173B1 true EA023173B1 (ru) 2016-04-29

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US (9) US8263596B2 (enExample)
EP (2) EP2556071B1 (enExample)
JP (1) JP5442906B2 (enExample)
KR (1) KR101782668B1 (enExample)
CN (1) CN102892766B (enExample)
AU (1) AU2011238384B2 (enExample)
BR (1) BR112012025496B1 (enExample)
CY (1) CY1118610T1 (enExample)
DK (1) DK2556071T3 (enExample)
EA (1) EA023173B1 (enExample)
ES (2) ES2603613T3 (enExample)
HR (1) HRP20161498T1 (enExample)
HU (1) HUE030651T2 (enExample)
IL (1) IL221556A (enExample)
LT (1) LT2556071T (enExample)
ME (1) ME02545B (enExample)
MX (1) MX2012011516A (enExample)
NZ (1) NZ602350A (enExample)
PL (1) PL2556071T3 (enExample)
PT (1) PT2556071T (enExample)
SG (1) SG183875A1 (enExample)
SI (1) SI2556071T1 (enExample)
SM (1) SMT201600430B (enExample)
TW (1) TWI516262B (enExample)
WO (2) WO2011123947A1 (enExample)

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MX357763B (es) 2013-10-18 2018-07-23 Univ Health Network Tratamiento para cancer pancreatico.
CN104130175A (zh) * 2014-06-13 2014-11-05 天津科技大学 不同位置取代吲哚酮类衍生物及其应用
WO2018145525A1 (zh) 2017-02-08 2018-08-16 中国医药研究开发中心有限公司 吡咯并芳杂环类化合物及其制备方法和医药用途
CN108947961B (zh) * 2017-05-18 2021-06-04 四川大学 吲唑类衍生物及其制备方法和用途
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CN115397429A (zh) * 2019-12-06 2022-11-25 大学健康网络 急性髓性白血病或骨髓增生异常综合征治疗
CA3181537A1 (en) 2020-05-06 2021-11-11 Ajax Therapeutics, Inc. 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors
CN112250614B (zh) * 2020-10-20 2022-02-01 苏州大学 3-螺三元环吲哚酮衍生物的合成方法
WO2022140527A1 (en) 2020-12-23 2022-06-30 Ajax Therapeutics, Inc. 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors
TW202300485A (zh) * 2021-03-02 2023-01-01 大陸商上海齊魯製藥研究中心有限公司 Plk4抑制劑及其用途
WO2022240876A1 (en) 2021-05-11 2022-11-17 Oric Pharmaceuticals, Inc. Polo like kinase 4 inhibitors
CN115677682B (zh) * 2021-07-30 2023-07-18 上海齐鲁制药研究中心有限公司 螺环类plk4抑制剂及其用途
TW202325289A (zh) 2021-11-09 2023-07-01 美商雅捷可斯治療公司 Ｊａｋ２抑制劑之形式及組合物
CA3234638A1 (en) 2021-11-09 2023-05-19 Ajax Therapeutics, Inc. 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors
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US8921545B2 (en) 2014-12-30
CN102892766B (zh) 2015-05-20
TWI516262B (zh) 2016-01-11
SI2556071T1 (sl) 2016-12-30
BR112012025496B1 (pt) 2021-02-23
SG183875A1 (en) 2012-10-30
EP2556071A4 (en) 2013-09-04
CN102892766A (zh) 2013-01-23
US8481533B2 (en) 2013-07-09
US9796703B2 (en) 2017-10-24
NZ602350A (en) 2014-05-30
PT2556071T (pt) 2016-11-22
US8263596B2 (en) 2012-09-11
EP2556070A4 (en) 2013-10-23
JP5442906B2 (ja) 2014-03-19
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