CA2915817C - Substituted (e)-n'-(1-phenylethylidene)benzohydrazide analogs as histone demethylase inhibitors - Google Patents

Substituted (e)-n'-(1-phenylethylidene)benzohydrazide analogs as histone demethylase inhibitors Download PDF

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Publication number
CA2915817C
CA2915817C CA2915817A CA2915817A CA2915817C CA 2915817 C CA2915817 C CA 2915817C CA 2915817 A CA2915817 A CA 2915817A CA 2915817 A CA2915817 A CA 2915817A CA 2915817 C CA2915817 C CA 2915817C
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compound
further aspect
mmol
mao
compounds
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CA2915817A
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English (en)
French (fr)
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CA2915817A1 (en
Inventor
Hariprasad Vankayalapati
Venkataswamy SORNA
Steve L. Warner
David J. Bearss
Sunil Sharma
Bret STEPHENS
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University of Utah Research Foundation Inc
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University of Utah Research Foundation Inc
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Priority claimed from US13/921,895 external-priority patent/US9266838B2/en
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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/22—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with hetero atoms directly attached to ring nitrogen atoms
    • C07D295/26—Sulfur atoms
    • 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
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/92—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with a hetero atom directly attached to the ring nitrogen atom
    • C07D211/96—Sulfur atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/86—Hydrazides; Thio or imino analogues thereof
    • C07D213/87—Hydrazides; Thio or imino analogues thereof in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyridine Compounds (AREA)
CA2915817A 2013-06-19 2014-06-19 Substituted (e)-n'-(1-phenylethylidene)benzohydrazide analogs as histone demethylase inhibitors Active CA2915817C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US13/921,895 2013-06-19
US13/921,895 US9266838B2 (en) 2011-08-15 2013-06-19 Substituted (E)-N′-(1-phenylethylidene)benzohydrazide analogs as histone demethylase inhibitors
PCT/US2014/043179 WO2014205213A1 (en) 2013-06-19 2014-06-19 Substituted (e)-n'-(1-phenylethylidene) benzohydrazide analogs as histone demethylase inhibitors

Publications (2)

Publication Number Publication Date
CA2915817A1 CA2915817A1 (en) 2014-12-24
CA2915817C true CA2915817C (en) 2022-12-13

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
CA2915817A Active CA2915817C (en) 2013-06-19 2014-06-19 Substituted (e)-n'-(1-phenylethylidene)benzohydrazide analogs as histone demethylase inhibitors

Country Status (13)

Country Link
EP (1) EP3010915B1 (enExample)
JP (1) JP6525162B2 (enExample)
KR (1) KR102288648B1 (enExample)
CN (2) CN105555784B (enExample)
AU (1) AU2014281398B2 (enExample)
BR (1) BR112015032113B1 (enExample)
CA (1) CA2915817C (enExample)
ES (1) ES2739814T3 (enExample)
IL (1) IL243200B (enExample)
MX (1) MX366949B (enExample)
NZ (1) NZ715331A (enExample)
SG (2) SG10201710543PA (enExample)
WO (1) WO2014205213A1 (enExample)

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US9527835B2 (en) 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
EP3392244A1 (en) 2014-02-13 2018-10-24 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
WO2015123424A1 (en) 2014-02-13 2015-08-20 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
LT3105218T (lt) 2014-02-13 2019-12-10 Incyte Corp Ciklopropilaminai kaip lsd1 inhibitoriai
WO2016007731A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Imidazopyridines and imidazopyrazines as lsd1 inhibitors
WO2016007722A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
US9758523B2 (en) 2014-07-10 2017-09-12 Incyte Corporation Triazolopyridines and triazolopyrazines as LSD1 inhibitors
WO2016007736A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Imidazopyrazines as lsd1 inhibitors
WO2016119031A1 (pt) * 2015-01-29 2016-08-04 Fundação De Amparo À Pesquisa Do Estado De Minas Gerais - Fapemig Composto, processo de síntese do composto, uso, composição farmacêutica, método de tratamento de inflamações ou de doença neurodegenerativa, forma de dosagem oral e método de inibição de enzima acetilcolinesterase
EA201792205A1 (ru) 2015-04-03 2018-02-28 Инсайт Корпорейшн Гетероциклические соединения как ингибиторы lsd1
KR20180011331A (ko) 2015-06-12 2018-01-31 오리존 지노믹스 에스.에이. Lsd1 억제제와 관련된 바이오마커 및 그의 용도
WO2017013061A1 (en) 2015-07-17 2017-01-26 Oryzon Genomics, S.A. Biomarkers associated with lsd1 inhibitors and uses thereof
DK3334709T3 (da) 2015-08-12 2025-02-03 Incyte Holdings Corp Salte af en lsd1-hæmmer
KR20180099768A (ko) 2015-12-30 2018-09-05 노파르티스 아게 증진된 효능을 갖는 면역 이펙터 세포 요법
CN120661674A (zh) 2016-03-15 2025-09-19 奥莱松基因组股份有限公司 用于治疗实体瘤的lsd1抑制剂的组合
JP2019512546A (ja) 2016-03-16 2019-05-16 オリゾン・ゲノミクス・ソシエダッド・アノニマ Ｋｄｍ１ａ標的会合を決定するための方法、およびそれに有用な化学プローブ
CA3021678A1 (en) 2016-04-22 2017-10-26 Incyte Corporation Formulations of an lsd1 inhibitor
US20190256930A1 (en) 2016-11-03 2019-08-22 Oryzon Genomics, S.A. Biomarkers for determining responsiveness to lsd1 inhibitors
US20190256929A1 (en) 2016-11-03 2019-08-22 Oryzon Genomics, S.A. Pharmacodynamic biomarkers for personalized cancer care using epigenetic modifying agents
CN108727377A (zh) * 2017-04-14 2018-11-02 四川大学 3-氰基吡唑并[1,5-a]嘧啶衍生物及其制备方法和用途
AU2018309372B2 (en) 2017-08-03 2024-08-15 Oryzon Genomics, S.A. Methods of treating behavior alterations
WO2019068326A1 (en) 2017-10-05 2019-04-11 Université D'aix-Marseille INHIBITORS OF LSD1 FOR THE TREATMENT AND PREVENTION OF CARDIOMYOPATHIES
CN108689960B (zh) * 2018-06-07 2022-03-04 济南大学 5-苯亚甲基-2-苯基噻唑酮类化合物及其制备和应用
US10968200B2 (en) 2018-08-31 2021-04-06 Incyte Corporation Salts of an LSD1 inhibitor and processes for preparing the same
HRP20251471T1 (hr) 2019-03-20 2026-01-02 Oryzon Genomics, S.A. Postupci liječenja poremećaja hiperaktivnosti s deficitom pažnje korištenjem inhibitora kdm1a kao što je spoj vafidemstat
SI3941466T1 (sl) 2019-03-20 2026-04-30 Oryzon Genomics, S.A. Vafidemstat za zdravljenje neagresivnih simptomov mejne osebnostne motnje
CN114341366A (zh) 2019-07-05 2022-04-12 奥莱松基因组股份有限公司 用于使用kdm1a抑制剂个体化治疗小细胞肺癌的生物标志物和方法
CN111471095B (zh) * 2020-01-15 2021-12-21 上海众启生物科技有限公司 用于阿尔茨海默症自身抗体检测的含jmjd2d蛋白片段的组合物
EP3964204A1 (en) 2020-09-08 2022-03-09 Université d'Aix-Marseille Lsd1 inhibitors for use in the treatment and prevention of fibrosis of tissues
CA3231846A1 (en) 2021-04-08 2022-10-13 Tamara Maes Combinations of lsd1 inhibitors for treating myeloid cancers
US20250275969A1 (en) 2022-05-09 2025-09-04 Oryzon Genomics, S.A. Methods of treating malignant peripheral nerve sheath tumor (mpnst) using lsd1 inhibitors
US20250295660A1 (en) 2022-05-09 2025-09-25 Oryzon Genomics, S.A. Methods of treating nf1-mutant tumors using lsd1 inhibitors
US20260151399A1 (en) 2022-11-24 2026-06-04 Oryzon Genomics, S.A. Combinations of lsd1 inhibitors and menin inhibitors for treating cancer
CN116444437B (zh) * 2023-03-08 2025-09-16 曲靖师范学院 抗癌医药达洛鲁胺的合成方法
CN116813569B (zh) * 2023-07-10 2024-07-02 衡阳市中心医院 一种抗癌药中间体的制备方法和抗癌药的制备方法
WO2025188857A1 (en) * 2024-03-05 2025-09-12 University Of Florida Research Foundation, Incorporated Hdac8 degraders and uses thereof

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AU2012296639B2 (en) * 2011-08-15 2016-06-09 University Of Utah Research Foundation Substituted (E)-N'-(1-phenylethylidene) benzohydrazide analogs as histone demethylase inhibitors
CN105555784B (zh) * 2013-06-19 2019-03-15 犹他大学研究基金会 作为组蛋白去甲基化酶抑制剂的被取代的(e)-n’-(1-苯亚乙基)苯甲酰肼类似物

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BR112015032113A2 (pt) 2017-03-21
KR102288648B1 (ko) 2021-08-12
EP3010915A1 (en) 2016-04-27
KR20160024929A (ko) 2016-03-07
SG11201510376QA (en) 2016-01-28
JP2016523256A (ja) 2016-08-08
CN105555784B (zh) 2019-03-15
SG10201710543PA (en) 2018-02-27
BR112015032113B1 (pt) 2019-01-29
CA2915817A1 (en) 2014-12-24
IL243200B (en) 2020-10-29
MX366949B (es) 2019-07-30
CN105555784A (zh) 2016-05-04
AU2014281398B2 (en) 2018-10-04
AU2014281398A1 (en) 2016-01-21
NZ715331A (en) 2019-09-27
WO2014205213A1 (en) 2014-12-24
EP3010915B1 (en) 2019-05-08
MX2015018032A (es) 2016-10-03
ES2739814T3 (es) 2020-02-04
IL243200A0 (en) 2016-02-29
CN110015984A (zh) 2019-07-16
EP3010915A4 (en) 2016-12-28
JP6525162B2 (ja) 2019-06-05

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