EA038028B1 - Производные дигидроимидазопиразинона, применимые в лечении рака - Google Patents

Производные дигидроимидазопиразинона, применимые в лечении рака Download PDF

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EA038028B1
EA038028B1 EA201891063A EA201891063A EA038028B1 EA 038028 B1 EA038028 B1 EA 038028B1 EA 201891063 A EA201891063 A EA 201891063A EA 201891063 A EA201891063 A EA 201891063A EA 038028 B1 EA038028 B1 EA 038028B1
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Prior art keywords
methyl
compound
dihydroimidazo
amino
formula
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EA201891063A
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Russian (ru)
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EA201891063A1 (ru
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Ричард Эндрью Уорд
Клиффорд Дэвид Джонс
Стивен Суоллоу
Марк Эндрю Грэм
Эндрю Хорнби Добсон
Джеймс Фрэнсис Маккэйб
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Астразенека Аб
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/4151,2-Diazoles
    • A61K31/4161,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
EA201891063A 2015-11-09 2016-11-08 Производные дигидроимидазопиразинона, применимые в лечении рака EA038028B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562252726P 2015-11-09 2015-11-09
US201662401351P 2016-09-29 2016-09-29
PCT/EP2016/076932 WO2017080979A1 (en) 2015-11-09 2016-11-08 Dihydroimidazopyrazinone derivatives useful in the treatment of cancer

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EA201891063A1 EA201891063A1 (ru) 2018-12-28
EA038028B1 true EA038028B1 (ru) 2021-06-24

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US (2) US9902731B2 (OSRAM)
EP (1) EP3374359B1 (OSRAM)
JP (1) JP6877423B2 (OSRAM)
KR (1) KR20180074788A (OSRAM)
CN (1) CN108349983B (OSRAM)
AU (1) AU2016351813B2 (OSRAM)
BR (1) BR112018008397B1 (OSRAM)
CA (1) CA3003549A1 (OSRAM)
CL (1) CL2018001226A1 (OSRAM)
CO (1) CO2018004857A2 (OSRAM)
CR (1) CR20180316A (OSRAM)
CY (1) CY1123627T1 (OSRAM)
DK (1) DK3374359T3 (OSRAM)
EA (1) EA038028B1 (OSRAM)
ES (1) ES2780650T3 (OSRAM)
HR (1) HRP20200342T1 (OSRAM)
IL (1) IL258953A (OSRAM)
LT (1) LT3374359T (OSRAM)
ME (1) ME03770B (OSRAM)
MX (1) MX376639B (OSRAM)
MY (1) MY197626A (OSRAM)
NI (1) NI201800058A (OSRAM)
PE (1) PE20181288A1 (OSRAM)
PH (1) PH12018500987A1 (OSRAM)
PL (1) PL3374359T3 (OSRAM)
PT (1) PT3374359T (OSRAM)
RS (1) RS60155B1 (OSRAM)
SG (1) SG11201803066VA (OSRAM)
SI (1) SI3374359T1 (OSRAM)
SM (1) SMT202000152T1 (OSRAM)
SV (1) SV2018005687A (OSRAM)
TN (1) TN2018000119A1 (OSRAM)
TW (1) TWI730012B (OSRAM)
WO (1) WO2017080979A1 (OSRAM)
ZA (1) ZA201803742B (OSRAM)

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EP3978498A1 (en) 2019-05-24 2022-04-06 Jiangsu Hengrui Medicine Co., Ltd. Substituted fused bicyclic derivative, preparation method therefor, and application thereof in medicines
AU2020288273B2 (en) * 2019-06-06 2025-11-13 Hutchison Medipharma Limited Tricyclic compounds and their use
EP4069687B1 (en) * 2019-12-05 2024-01-31 Astrazeneca AB Process and intermediates for the production of formula (i)
WO2021110169A1 (zh) * 2019-12-06 2021-06-10 南京明德新药研发有限公司 作为erk抑制剂的噻唑并内酰胺类化合物及其应用
TW202221001A (zh) 2020-09-29 2022-06-01 大陸商江蘇恒瑞醫藥股份有限公司 吡咯並雜環類衍生物的晶型及其製備方法
WO2022262797A1 (en) * 2021-06-18 2022-12-22 Shanghai Antengene Corporation Limited Combination of an erk inhibitor and a kras inhibitor and uses thereof
WO2022268065A1 (en) * 2021-06-22 2022-12-29 Fochon Biosciences, Ltd. Compounds as erk inhibitors
JPWO2023008462A1 (OSRAM) 2021-07-27 2023-02-02
US20250101034A1 (en) 2021-11-04 2025-03-27 Skyhawk Therapeutics, Inc. Compositions useful for modulating splicing
US20250340571A1 (en) 2022-04-27 2025-11-06 Skyhawk Therapeutics, Inc. Compositions useful for modulating splicing
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EP3374359A1 (en) 2018-09-19
HRP20200342T1 (hr) 2020-06-12
PE20181288A1 (es) 2018-08-07
CN108349983B (zh) 2021-02-26
US20180237443A1 (en) 2018-08-23
LT3374359T (lt) 2020-03-25
DK3374359T3 (da) 2020-03-30
RS60155B1 (sr) 2020-05-29
CL2018001226A1 (es) 2018-10-05
CY1123627T1 (el) 2022-03-24
SI3374359T1 (sl) 2020-04-30
AU2016351813B2 (en) 2019-05-30
MX376639B (es) 2025-03-07
CR20180316A (es) 2018-10-05
WO2017080979A1 (en) 2017-05-18
EP3374359B1 (en) 2020-01-08
SV2018005687A (es) 2018-07-20
SG11201803066VA (en) 2018-05-30
BR112018008397A2 (pt) 2018-10-23
AU2016351813A1 (en) 2018-06-21
EA201891063A1 (ru) 2018-12-28
CA3003549A1 (en) 2017-05-18
MY197626A (en) 2023-06-29
IL258953A (en) 2018-06-28
JP6877423B2 (ja) 2021-05-26
ZA201803742B (en) 2020-08-26
TWI730012B (zh) 2021-06-11
KR20180074788A (ko) 2018-07-03
ES2780650T3 (es) 2020-08-26
TW201728586A (zh) 2017-08-16
CO2018004857A2 (es) 2018-07-19
PH12018500987A1 (en) 2019-01-28
PL3374359T3 (pl) 2020-06-29
US20170204100A1 (en) 2017-07-20
HK1256283A1 (en) 2019-09-20
BR112018008397B1 (pt) 2023-12-12
US9902731B2 (en) 2018-02-27
SMT202000152T1 (it) 2020-05-08
PT3374359T (pt) 2020-03-27
NI201800058A (es) 2018-10-18
JP2019503337A (ja) 2019-02-07
CN108349983A (zh) 2018-07-31
ME03770B (me) 2021-04-20
US10202391B2 (en) 2019-02-12
MX2018005725A (es) 2018-08-14
TN2018000119A1 (en) 2019-10-04

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