KR20170092543A - 슈퍼-인핸서 부위에서 전사 조절을 표적화하는 방법 - Google Patents

슈퍼-인핸서 부위에서 전사 조절을 표적화하는 방법 Download PDF

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Publication number
KR20170092543A
KR20170092543A KR1020177013707A KR20177013707A KR20170092543A KR 20170092543 A KR20170092543 A KR 20170092543A KR 1020177013707 A KR1020177013707 A KR 1020177013707A KR 20177013707 A KR20177013707 A KR 20177013707A KR 20170092543 A KR20170092543 A KR 20170092543A
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South Korea
Prior art keywords
inhibitor
cyclin
dependent kinase
kinase inhibitor
super
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Ceased
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English (en)
Korean (ko)
Inventor
스티븐 엘. 워너
데이비드 제이. 베알스
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톨레로 파마수티컬스, 인크.
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Publication of KR20170092543A publication Critical patent/KR20170092543A/ko
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • 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
    • A61K31/40Heterocyclic 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
    • A61K31/403Heterocyclic 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
    • A61K31/404Indoles, e.g. pindolol
    • A61K31/4045Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/451Non condensed piperidines, e.g. piperocaine having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/453Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
    • 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/55131,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/55171,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7088Compounds having three or more nucleosides or nucleotides
    • A61K31/713Double-stranded nucleic acids or oligonucleotides
    • 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
    • A61P35/00Antineoplastic agents
    • 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

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (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)
  • Organic Chemistry (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
KR1020177013707A 2014-11-07 2015-11-06 슈퍼-인핸서 부위에서 전사 조절을 표적화하는 방법 Ceased KR20170092543A (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201462077042P 2014-11-07 2014-11-07
US62/077,042 2014-11-07
US201562150110P 2015-04-20 2015-04-20
US62/150,110 2015-04-20
PCT/US2015/059566 WO2016073913A1 (en) 2014-11-07 2015-11-06 Methods to target transcriptional control at super-enhancer regions

Publications (1)

Publication Number Publication Date
KR20170092543A true KR20170092543A (ko) 2017-08-11

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KR1020177013707A Ceased KR20170092543A (ko) 2014-11-07 2015-11-06 슈퍼-인핸서 부위에서 전사 조절을 표적화하는 방법

Country Status (12)

Country Link
US (2) US20180280407A1 (enExample)
EP (1) EP3215135B1 (enExample)
JP (1) JP6689841B2 (enExample)
KR (1) KR20170092543A (enExample)
CN (1) CN107205959B (enExample)
AU (1) AU2015342813B2 (enExample)
BR (1) BR112017009552A8 (enExample)
CA (1) CA2965690A1 (enExample)
IL (1) IL251816B (enExample)
MX (1) MX385762B (enExample)
RU (1) RU2737508C2 (enExample)
WO (1) WO2016073913A1 (enExample)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US12174198B2 (en) 2019-02-08 2024-12-24 Dewpoint Therapeutics, Inc. Methods of characterizing condensate-associated characteristics of compounds and uses thereof
US12422427B2 (en) 2018-10-15 2025-09-23 MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. Compounds for treatment of diseases and methods of screening therefor
US12422437B2 (en) 2019-09-18 2025-09-23 Dewpoint Therapeutics, Inc. Methods of screening for condensate-associated specificity and uses thereof

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112017022666A8 (pt) 2015-04-20 2022-10-18 Tolero Pharmaceuticals Inc Preparando resposta à alvocidib por perfilamento mitocondrial
CN111349118B (zh) 2015-05-18 2023-08-22 住友制药肿瘤公司 具有增加的生物利用度的阿伏西地前药
RU2759963C2 (ru) 2015-08-03 2021-11-19 Сумитомо Даиниппон Фарма Онколоджи, Инк. Комбинированные терапии для лечения рака
US11279694B2 (en) 2016-11-18 2022-03-22 Sumitomo Dainippon Pharma Oncology, Inc. Alvocidib prodrugs and their use as protein kinase inhibitors
JP6619519B2 (ja) 2016-12-19 2019-12-11 トレロ ファーマシューティカルズ, インコーポレイテッド プロファイリングペプチドおよび感受性プロファイリングのための方法
WO2019055579A1 (en) 2017-09-12 2019-03-21 Tolero Pharmaceuticals, Inc. TREATMENT REGIME FOR CANCERS THAT ARE INSENSITIVE TO BCL-2 INHIBITORS USING THE MCL-1 ALVOCIDIB INHIBITOR
WO2019113260A1 (en) * 2017-12-05 2019-06-13 The Regents Of The University Of Colorado A Body Corporate Genomic targets of histone deacetylase inhibitors (hdaci) and methods of use thereof
JP2021514975A (ja) * 2018-02-27 2021-06-17 ファイザー・インク サイクリン依存性キナーゼ阻害剤およびbet−ブロモドメイン阻害剤の組合せ
MX2021006544A (es) 2018-12-04 2021-07-07 Sumitomo Pharma Oncology Inc Inhibidores de cinasa dependiente de ciclina 9 (cdk9) y polimorfos de los mismos para uso como agentes para el tratamiento de cancer.
JP2022525149A (ja) 2019-03-20 2022-05-11 スミトモ ダイニッポン ファーマ オンコロジー, インコーポレイテッド ベネトクラクスが失敗した急性骨髄性白血病(aml)の処置
EP4453261A1 (en) * 2021-12-22 2024-10-30 Cornell University Prognostic/predictive epigenetic breast cancer signature

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20030026069A (ko) * 2001-09-24 2003-03-31 주식회사 엘지생명과학 티엔에프계 단백질과 플라보피리돌의 조합에 의한 암세포특이적인 세포사멸 유도용 조성물
RU2438664C2 (ru) * 2007-05-15 2012-01-10 Пирамал Лайф Сайнсиз Лимитед Синергическая фармацевтическая комбинация для лечения рака
EP2561867A1 (en) * 2011-08-22 2013-02-27 Lead Discovery Center GmbH CDK9 inhibitors in the treatment of midline carcinoma
KR20160072261A (ko) * 2013-11-08 2016-06-22 다나-파버 캔서 인스티튜트 인크. 브로모도메인 및 엑스트라-말단 (bet) 단백질 저해제를 이용한 암 치료를 위한 조합 요법
EP3206749B1 (en) * 2014-10-14 2021-09-08 The Regents of the University of California The cdk9 and brd4 inhibitors flavopiridol and jq1 to inhibit cartilage inflammation

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US12422427B2 (en) 2018-10-15 2025-09-23 MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. Compounds for treatment of diseases and methods of screening therefor
US12174198B2 (en) 2019-02-08 2024-12-24 Dewpoint Therapeutics, Inc. Methods of characterizing condensate-associated characteristics of compounds and uses thereof
US12422437B2 (en) 2019-09-18 2025-09-23 Dewpoint Therapeutics, Inc. Methods of screening for condensate-associated specificity and uses thereof

Also Published As

Publication number Publication date
RU2017118833A3 (enExample) 2019-06-17
BR112017009552A8 (pt) 2022-10-18
RU2017118833A (ru) 2018-12-10
JP2017533222A (ja) 2017-11-09
AU2015342813A1 (en) 2017-05-18
JP6689841B2 (ja) 2020-04-28
AU2015342813B2 (en) 2021-04-22
EP3215135A4 (en) 2018-05-16
US20180280407A1 (en) 2018-10-04
EP3215135A1 (en) 2017-09-13
CN107205959B (zh) 2021-02-12
EP3215135B1 (en) 2020-05-13
US20200316084A1 (en) 2020-10-08
MX385762B (es) 2025-03-18
CN107205959A (zh) 2017-09-26
IL251816A0 (en) 2017-06-29
CA2965690A1 (en) 2016-05-12
BR112017009552A2 (pt) 2018-01-02
IL251816B (en) 2022-03-01
MX2017005861A (es) 2017-06-26
WO2016073913A1 (en) 2016-05-12
RU2737508C2 (ru) 2020-12-01

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