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MD4531B1 - Derivaţi ai benzimidazolonei în calitate de inhibitori ai bromodomeniului - Google Patents

Derivaţi ai benzimidazolonei în calitate de inhibitori ai bromodomeniului Download PDF

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Publication number
MD4531B1
MD4531B1 MDA20150104A MD20150104A MD4531B1 MD 4531 B1 MD4531 B1 MD 4531B1 MD A20150104 A MDA20150104 A MD A20150104A MD 20150104 A MD20150104 A MD 20150104A MD 4531 B1 MD4531 B1 MD 4531B1
Authority
MD
Moldova
Prior art keywords
bromodomain inhibitors
compounds
benzimidazolone derivatives
bromodomain
inhibitors
Prior art date
Application number
MDA20150104A
Other languages
English (en)
Russian (ru)
Other versions
MD4531C1 (ro
MD20150104A2 (ro
Inventor
Евангелос АКТОУДИАНАКИС
Грегори ЧИНЬ
Бриттон Кеннет Корки
Цзиньфа Ду
Кристина Элбел
Роберт Х. Цзян
Тецуя Кобаяси
Рубен Мартинес
Сэмюель Е. МЕТОБО
Майкл Миш
Софи Шевик
Дэвид Сперандио
Х Ян
Джефф ЗАБЛОКИ
Original Assignee
Gilead Sciences, Inc.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Gilead Sciences, Inc. filed Critical Gilead Sciences, Inc.
Publication of MD20150104A2 publication Critical patent/MD20150104A2/ro
Publication of MD4531B1 publication Critical patent/MD4531B1/ro
Publication of MD4531C1 publication Critical patent/MD4531C1/ro

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    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Epidemiology (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Invenţia se referă la compuşi chimici care pot acţiona ca inhibitori sau care în alt mod pot modula activitatea unei proteine conţinând un domeniu bromic, inclusiv a proteinei conţinând domeniul bromic 4 (BRD4), la compoziţii şi formulări ce conţin astfel de compuşi, precum şi la utilizarea unor astfel de compuşi. Compuşii sunt prezentaţi de formula (I)(I),în care semnificaţiile R1a, R1b, R2a, R2b, R3 şi X sunt dezvăluite în descriere şi revendicări.
MDA20150104A 2013-03-28 2014-03-27 Derivaţi ai benzimidazolonei în calitate de inhibitori ai bromodomeniului MD4531C1 (ro)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361805995P 2013-03-28 2013-03-28
US201361860230P 2013-07-30 2013-07-30
PCT/US2014/032031 WO2014160873A1 (en) 2013-03-28 2014-03-27 Benzimidazolone derivatives as bromodomain inhibitors

Publications (3)

Publication Number Publication Date
MD20150104A2 MD20150104A2 (ro) 2016-02-29
MD4531B1 true MD4531B1 (ro) 2017-11-30
MD4531C1 MD4531C1 (ro) 2018-06-30

Family

ID=50897885

Family Applications (1)

Application Number Title Priority Date Filing Date
MDA20150104A MD4531C1 (ro) 2013-03-28 2014-03-27 Derivaţi ai benzimidazolonei în calitate de inhibitori ai bromodomeniului

Country Status (35)

Country Link
US (2) US20160031868A1 (ro)
EP (1) EP2978759B1 (ro)
JP (1) JP6339175B2 (ro)
KR (1) KR101847698B1 (ro)
CN (1) CN105102453B (ro)
AP (1) AP2015008741A0 (ro)
AU (1) AU2014241152B2 (ro)
BR (1) BR112015024078A2 (ro)
CA (1) CA2907502C (ro)
CL (1) CL2015002871A1 (ro)
CR (1) CR20150515A (ro)
CY (1) CY1119165T1 (ro)
DK (1) DK2978759T3 (ro)
EA (1) EA029497B1 (ro)
ES (1) ES2626397T3 (ro)
HR (1) HRP20170750T1 (ro)
HU (1) HUE034772T2 (ro)
IL (1) IL241186A0 (ro)
LT (1) LT2978759T (ro)
MD (1) MD4531C1 (ro)
MX (1) MX2015013798A (ro)
MY (1) MY176634A (ro)
NZ (1) NZ711586A (ro)
PE (1) PE20151982A1 (ro)
PH (1) PH12015502246A1 (ro)
PL (1) PL2978759T3 (ro)
PT (1) PT2978759T (ro)
RS (1) RS56050B1 (ro)
SG (1) SG11201507926RA (ro)
SI (1) SI2978759T1 (ro)
SM (1) SMT201700249T1 (ro)
TW (1) TWI530499B (ro)
UY (1) UY35516A (ro)
WO (1) WO2014160873A1 (ro)
ZA (1) ZA201506356B (ro)

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US10292968B2 (en) 2014-12-11 2019-05-21 Zenith Epigenetics Ltd. Substituted heterocycles as bromodomain inhibitors
EP3233846A4 (en) 2014-12-17 2018-07-18 Zenith Epigenetics Ltd. Inhibitors of bromodomains
KR102662814B1 (ko) 2015-03-13 2024-05-03 리스버로직스 코퍼레이션 보체 관련 질환을 치료하기 위한 조성물 및 치료 방법
GB201504694D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Covalent conjugates
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AR106520A1 (es) 2015-10-29 2018-01-24 Incyte Corp Forma sólida amorfa de un inhibidor de proteína bet
WO2017114843A1 (en) 2015-12-29 2017-07-06 INSERM (Institut National de la Santé et de la Recherche Médicale) Xanthine derivative inhibitors of bet proteins
CN114366748A (zh) 2016-06-20 2022-04-19 因赛特公司 Bet抑制剂的结晶固体形式
US20180179191A1 (en) * 2016-11-22 2018-06-28 Gilead Sciences, Inc. Synthesis of a compound that modulates the activity of bromodomain-containing proteins
US11180510B2 (en) 2017-11-06 2021-11-23 Centre National De La Recherche Scientifique Xanthine derivatives and uses thereof as inhibitors of bromodomains of BET proteins
IL275478B2 (en) 2017-12-20 2024-06-01 Betta Pharmaceuticals Co Ltd A preparation that functions as a bromodomain protein inhibitor, and the composition
CN113365699B (zh) * 2019-02-02 2024-06-14 石药集团中奇制药技术（石家庄）有限公司 靶向泛素化降解brd4蛋白化合物及其制备方法和应用
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Also Published As

Publication number Publication date
PH12015502246A1 (en) 2016-02-01
MY176634A (en) 2020-08-19
JP6339175B2 (ja) 2018-06-06
SI2978759T1 (sl) 2017-05-31
JP2016515584A (ja) 2016-05-30
WO2014160873A1 (en) 2014-10-02
MD4531C1 (ro) 2018-06-30
EA029497B1 (ru) 2018-04-30
SMT201700249T1 (it) 2017-07-18
AU2014241152B2 (en) 2016-11-03
EP2978759B1 (en) 2017-03-15
DK2978759T3 (da) 2017-06-19
EA201591455A1 (ru) 2016-01-29
AP2015008741A0 (en) 2015-09-30
PT2978759T (pt) 2017-05-31
PE20151982A1 (es) 2016-01-28
PL2978759T3 (pl) 2017-08-31
RS56050B1 (sr) 2017-09-29
CN105102453A (zh) 2015-11-25
US20160031868A1 (en) 2016-02-04
US20140296246A1 (en) 2014-10-02
TWI530499B (zh) 2016-04-21
IL241186A0 (en) 2015-11-30
CR20150515A (es) 2015-12-01
KR101847698B1 (ko) 2018-04-10
CA2907502A1 (en) 2014-10-02
BR112015024078A2 (pt) 2017-07-18
HUE034772T2 (en) 2018-02-28
LT2978759T (lt) 2017-05-25
CA2907502C (en) 2018-02-27
CL2015002871A1 (es) 2016-05-13
TW201504233A (zh) 2015-02-01
AU2014241152A1 (en) 2015-09-17
ES2626397T3 (es) 2017-07-24
US9255089B2 (en) 2016-02-09
MX2015013798A (es) 2016-02-16
SG11201507926RA (en) 2015-10-29
ZA201506356B (en) 2017-08-30
MD20150104A2 (ro) 2016-02-29
EP2978759A1 (en) 2016-02-03
HRP20170750T1 (hr) 2017-07-28
HK1220692A1 (en) 2017-05-12
CN105102453B (zh) 2018-04-06
CY1119165T1 (el) 2018-02-14
NZ711586A (en) 2016-09-30
KR20150135476A (ko) 2015-12-02
UY35516A (es) 2014-09-30

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