EA201890142A1 - Замещенные пиримидиновые обратные ингибиторы bmi-1 - Google Patents

Замещенные пиримидиновые обратные ингибиторы bmi-1

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Publication number
EA201890142A1
EA201890142A1 EA201890142A EA201890142A EA201890142A1 EA 201890142 A1 EA201890142 A1 EA 201890142A1 EA 201890142 A EA201890142 A EA 201890142A EA 201890142 A EA201890142 A EA 201890142A EA 201890142 A1 EA201890142 A1 EA 201890142A1
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EA
Eurasian Patent Office
Prior art keywords
bmi
substituted pyrimidine
reduce
inhibit
function
Prior art date
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EA201890142A
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English (en)
Other versions
EA035349B1 (ru
Inventor
Чан-Сун Ли
Рамиль Байазитов
Лянсянь Цао
Томас У. Дэвис
У Ду
Жунган Лю
Йоунг-Чоон Моон
Стивен Д. Пэджет
Хунюй Жэнь
Надя Сидоренко
Ричард Джеральд Уайлде
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ПиТиСи ТЕРАПЬЮТИКС, ИНК.
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Publication of EA201890142A1 publication Critical patent/EA201890142A1/ru
Publication of EA035349B1 publication Critical patent/EA035349B1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • 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
    • C07D403/12Heterocyclic 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 chain containing hetero atoms as chain links
    • 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
    • A61NELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY
    • A61N5/00Radiation therapy
    • A61N5/10X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • 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
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pathology (AREA)
  • Radiology & Medical Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Hematology (AREA)
  • Oncology (AREA)

Abstract

В настоящей заявке описаны аминзамещенные обратные пиримидиновые соединения и их формы, которые ингибируют функцию и снижают уровень B-клеточного специфического сайта интеграции 1 вируса мышиного лейкоза Молони (Bmi-1), и способы их использования для ингибирования функции Bmi-1 и снижения уровня Bmi-1 для лечения рака, опосредованного Bmi-1.
EA201890142A 2012-11-21 2013-11-21 ЗАМЕЩЕННЫЕ ПИРИМИДИНОВЫЕ ОБРАТНЫЕ ИНГИБИТОРЫ Bmi-1 EA035349B1 (ru)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201261728907P 2012-11-21 2012-11-21

Publications (2)

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EA201890142A1 true EA201890142A1 (ru) 2018-06-29
EA035349B1 EA035349B1 (ru) 2020-05-29

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EA201890142A EA035349B1 (ru) 2012-11-21 2013-11-21 ЗАМЕЩЕННЫЕ ПИРИМИДИНОВЫЕ ОБРАТНЫЕ ИНГИБИТОРЫ Bmi-1
EA201590992A EA031405B1 (ru) 2012-11-21 2013-11-21 Замещенные пиримидиновые обратные ингибиторы bmi-1

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US (3) US10428050B2 (ru)
EP (1) EP2922828B1 (ru)
JP (3) JP6412503B2 (ru)
KR (4) KR20220143164A (ru)
CN (2) CN111423417B (ru)
AR (1) AR093579A1 (ru)
AU (1) AU2013348009C1 (ru)
BR (1) BR112015011760B1 (ru)
CA (1) CA2892045C (ru)
CL (1) CL2015001377A1 (ru)
CR (1) CR20150294A (ru)
CU (1) CU24387B1 (ru)
DK (1) DK2922828T3 (ru)
EA (2) EA035349B1 (ru)
EC (1) ECSP15019948A (ru)
ES (1) ES2821529T3 (ru)
HK (1) HK1215032A1 (ru)
IL (2) IL238871B (ru)
MA (1) MA38208B1 (ru)
MX (2) MX2015006469A (ru)
NI (1) NI201500072A (ru)
NZ (2) NZ746607A (ru)
PE (1) PE20151413A1 (ru)
PH (1) PH12015501130A1 (ru)
PL (1) PL2922828T3 (ru)
PT (1) PT2922828T (ru)
SA (1) SA517381847B1 (ru)
SG (2) SG11201503982XA (ru)
TW (1) TWI623531B (ru)
UA (1) UA118094C2 (ru)
WO (1) WO2014081906A2 (ru)
ZA (1) ZA201503642B (ru)

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