AU2015342813B2 - Methods to target transcriptional control at super-enhancer regions - Google Patents

Methods to target transcriptional control at super-enhancer regions Download PDF

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Publication number
AU2015342813B2
AU2015342813B2 AU2015342813A AU2015342813A AU2015342813B2 AU 2015342813 B2 AU2015342813 B2 AU 2015342813B2 AU 2015342813 A AU2015342813 A AU 2015342813A AU 2015342813 A AU2015342813 A AU 2015342813A AU 2015342813 B2 AU2015342813 B2 AU 2015342813B2
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Australia
Prior art keywords
inhibitor
alvocidib
cdk9
pharmaceutically acceptable
cancer
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AU2015342813A
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AU2015342813A1 (en
Inventor
David J. Bearss
Steven L. Warner
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Sumitomo Pharma Oncology Inc
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Sumitomo Pharma Oncology Inc
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Assigned to SUMITOMO DAINIPPON PHARMA ONCOLOGY, INC. reassignment SUMITOMO DAINIPPON PHARMA ONCOLOGY, INC. Request for Assignment Assignors: TOLERO PHARMACEUTICALS, INC.
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Assigned to SUMITOMO PHARMA ONCOLOGY, INC. reassignment SUMITOMO PHARMA ONCOLOGY, INC. Request to Amend Deed and Register Assignors: SUMITOMO DAINIPPON PHARMA ONCOLOGY, INC.
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    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7088—Compounds having three or more nucleosides or nucleotides
    • A61K31/713—Double-stranded nucleic acids or oligonucleotides
    • 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
    • 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
    • A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/451—Non condensed piperidines, e.g. piperocaine having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/453—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic 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
    • A61K31/535—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
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic 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
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic 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
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
    • 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
    • A61P35/00—Antineoplastic agents
    • 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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  • 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)
AU2015342813A 2014-11-07 2015-11-06 Methods to target transcriptional control at super-enhancer regions Ceased AU2015342813B2 (en)

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 (2)

Publication Number Publication Date
AU2015342813A1 AU2015342813A1 (en) 2017-05-18
AU2015342813B2 true AU2015342813B2 (en) 2021-04-22

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AU2015342813A Ceased AU2015342813B2 (en) 2014-11-07 2015-11-06 Methods to target transcriptional control at super-enhancer regions

Country Status (12)

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

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Publication number Priority date Publication date Assignee Title
US9901574B2 (en) 2015-04-20 2018-02-27 Tolero Pharmaceuticals, Inc. Predicting response to alvocidib by mitochondrial profiling
ES2739749T3 (es) 2015-05-18 2020-02-03 Tolero Pharmaceuticals Inc Profármacos de alvocidib que tienen biodisponibilidad aumentada
MX2018001289A (es) 2015-08-03 2018-04-30 Tolero Pharmaceuticals Inc Terapias de combinacion para el tratamiento del cancer.
WO2018094275A1 (en) 2016-11-18 2018-05-24 Tolero Pharmaceuticals, Inc. Alvocidib prodrugs and their use as protein kinase inhibitors
KR20190099260A (ko) 2016-12-19 2019-08-26 톨레로 파마수티컬스, 인크. 프로파일링 펩티드 및 감도 프로파일링을 위한 방법
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
EP3758753A1 (en) * 2018-02-27 2021-01-06 Pfizer Inc Combination of a cyclin dependent kinase inhibitor and a bet-bromodomain inhibitor
CN113196055B (zh) 2018-10-15 2025-06-27 马克斯·普朗克科学促进协会 用于治疗疾病的化合物及其筛选方法
US11034710B2 (en) 2018-12-04 2021-06-15 Sumitomo Dainippon Pharma Oncology, Inc. CDK9 inhibitors and polymorphs thereof for use as agents for treatment of cancer
CA3127237A1 (en) 2019-02-08 2020-08-13 Dewpoint Therapeutics, Inc. Methods of characterizing condensate-associated characteristics of compounds and uses thereof
US11793802B2 (en) 2019-03-20 2023-10-24 Sumitomo Pharma Oncology, Inc. Treatment of acute myeloid leukemia (AML) with venetoclax failure
KR20220084047A (ko) 2019-09-18 2022-06-21 듀포인트 테라퓨틱스, 인크. 응축물 관련 특이성에 대한 스크리닝 방법 및 이의 용도
US20250305055A1 (en) * 2021-12-22 2025-10-02 Cornell University Prognostic/predictive breast cancer signature

Citations (2)

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WO2003028001A2 (en) * 2001-09-24 2003-04-03 Lg Life Sciences Ltd. Method and pharmaceutical composition for inducing cancer cell-specific apoptosis by combination with tnf family proteins and flavopiridol
US20140303167A1 (en) * 2011-08-22 2014-10-09 Lead Discovery Center Gmbh Cdk9 inhibitors in the treatment of midline carcinoma

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RU2438664C2 (ru) * 2007-05-15 2012-01-10 Пирамал Лайф Сайнсиз Лимитед Синергическая фармацевтическая комбинация для лечения рака
CA2929652A1 (en) * 2013-11-08 2015-05-14 Dana-Farber Cancer Institute, Inc. Combination therapy for cancer using bromodomain and extra-terminal (bet) protein inhibitors
JP6930913B2 (ja) * 2014-10-14 2021-09-01 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニアＴｈｅ Ｒｅｇｅｎｔｓ Ｏｆ Ｔｈｅ Ｕｎｉｖｅｒｓｉｔｙ Ｏｆ Ｃａｌｉｆｏｒｎｉａ 炎症を阻害するためのｃｄｋ９及びｂｒｄ４阻害剤の使用法

Patent Citations (2)

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Publication number Priority date Publication date Assignee Title
WO2003028001A2 (en) * 2001-09-24 2003-04-03 Lg Life Sciences Ltd. Method and pharmaceutical composition for inducing cancer cell-specific apoptosis by combination with tnf family proteins and flavopiridol
US20140303167A1 (en) * 2011-08-22 2014-10-09 Lead Discovery Center Gmbh Cdk9 inhibitors in the treatment of midline carcinoma

Non-Patent Citations (2)

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Tomoaki Fukui ET AL, "The Analysis of the Effect of JQ1 and Flavopiridol on Chondrocytes under Inflammatory Stimuli", ORS 2014 Annual Meeting, (2014-03-15), URL: http://www.ors.org/Transactions/60/1251.pdf, (2016-05-26) *

Also Published As

Publication number Publication date
IL251816A0 (en) 2017-06-29
JP2017533222A (ja) 2017-11-09
EP3215135A1 (en) 2017-09-13
CN107205959A (zh) 2017-09-26
RU2737508C2 (ru) 2020-12-01
JP6689841B2 (ja) 2020-04-28
BR112017009552A8 (pt) 2022-10-18
MX2017005861A (es) 2017-06-26
US20180280407A1 (en) 2018-10-04
RU2017118833A (ru) 2018-12-10
BR112017009552A2 (en) 2018-01-02
WO2016073913A1 (en) 2016-05-12
KR20170092543A (ko) 2017-08-11
RU2017118833A3 (https=) 2019-06-17
CN107205959B (zh) 2021-02-12
EP3215135B1 (en) 2020-05-13
EP3215135A4 (en) 2018-05-16
IL251816B (en) 2022-03-01
CA2965690A1 (en) 2016-05-12
MX385762B (es) 2025-03-18
US20200316084A1 (en) 2020-10-08
AU2015342813A1 (en) 2017-05-18

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Owner name: SUMITOMO DAINIPPON PHARMA ONCOLOGY, INC.

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