BR112015032113B1 - análogos de (e)-n’-(1-feniletilideno)benzohidrazida substituídos como inibidores de histona demetilase - Google Patents

análogos de (e)-n’-(1-feniletilideno)benzohidrazida substituídos como inibidores de histona demetilase Download PDF

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Publication number
BR112015032113B1
BR112015032113B1 BR112015032113-5A BR112015032113A BR112015032113B1 BR 112015032113 B1 BR112015032113 B1 BR 112015032113B1 BR 112015032113 A BR112015032113 A BR 112015032113A BR 112015032113 B1 BR112015032113 B1 BR 112015032113B1
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Brazil
Prior art keywords
compound
compounds
mmol
disclosed
cancer
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BR112015032113-5A
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English (en)
Portuguese (pt)
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BR112015032113A2 (pt
Inventor
Hariprasad Vankayalapati
Venkataswamy Sorna
Steve L. Warner
David J. Bearss
Sunil Sharma
Bret Stephens
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University Of Utah Research Foundation
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Priority claimed from US13/921,895 external-priority patent/US9266838B2/en
Application filed by University Of Utah Research Foundation filed Critical University Of Utah Research Foundation
Publication of BR112015032113A2 publication Critical patent/BR112015032113A2/pt
Publication of BR112015032113B1 publication Critical patent/BR112015032113B1/pt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic 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
    • C07D295/22Heterocyclic 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
    • C07D295/26Sulfur atoms
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/92Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with a hetero atom directly attached to the ring nitrogen atom
    • C07D211/96Sulfur atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/86Hydrazides; Thio or imino analogues thereof
    • C07D213/87Hydrazides; Thio or imino analogues thereof in position 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic 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
    • C07D231/12Heterocyclic 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)
  • Pyridine Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
BR112015032113-5A 2013-06-19 2014-06-19 análogos de (e)-n’-(1-feniletilideno)benzohidrazida substituídos como inibidores de histona demetilase BR112015032113B1 (pt)

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
BR112015032113A2 BR112015032113A2 (pt) 2017-03-21
BR112015032113B1 true BR112015032113B1 (pt) 2019-01-29

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BR112015032113-5A BR112015032113B1 (pt) 2013-06-19 2014-06-19 análogos de (e)-n’-(1-feniletilideno)benzohidrazida substituídos como inibidores de histona demetilase

Country Status (13)

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

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WO2016007722A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
WO2016007727A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines 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
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CA2987876A1 (en) 2015-06-12 2016-12-15 Oryzon Genomics, S.A. Biomarkers associated with lsd1 inhibitors and uses thereof
WO2017013061A1 (en) 2015-07-17 2017-01-26 Oryzon Genomics, S.A. Biomarkers associated with lsd1 inhibitors and uses thereof
LT3334709T (lt) 2015-08-12 2025-03-10 Incyte Holdings Corporation Lsd1 inhibitoriaus druskos
AU2016382512A1 (en) 2015-12-30 2018-07-12 Novartis Ag Immune effector cell therapies with enhanced efficacy
ES3057783T3 (en) 2016-03-15 2026-03-04 Oryzon Genomics Sa Combinations of lsd1 inhibitors for use in the treatment of neoplastic diseases
WO2017158136A1 (en) 2016-03-16 2017-09-21 Oryzon Genomics, S.A. Methods to determine kdm1a target engagement and chemoprobes useful therefor
JP6999574B2 (ja) 2016-04-22 2022-01-18 インサイト・コーポレイション Lsd1阻害剤の製剤
WO2018083189A1 (en) 2016-11-03 2018-05-11 Oryzon Genomics, S.A. Biomarkers for determining responsiveness to lsd1 inhibitors
WO2018083138A1 (en) 2016-11-03 2018-05-11 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
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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
WO2020047198A1 (en) 2018-08-31 2020-03-05 Incyte Corporation Salts of an lsd1 inhibitor and processes for preparing the same
SG11202109159VA (en) 2019-03-20 2021-10-28 Oryzon Genomics Sa Methods of treating borderline personality disorder
ES3053813T3 (en) 2019-03-20 2026-01-26 Oryzon Genomics Sa Methods of treating attention deficit hyperactivity disorder using kdm1a inhibitors such as the compound vafidemstat
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
CN111471096B (zh) * 2020-01-15 2022-02-18 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有adarb1蛋白片段组合物
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
JP2024513260A (ja) 2021-04-08 2024-03-22 オリゾン ジェノミックス ソシエダッド アノニマ 骨髄癌処置のためのlsd1阻害剤の組み合わせ
CN119546292A (zh) 2022-05-09 2025-02-28 奥莱松基因组股份有限公司 使用lsd1抑制剂治疗恶性周围神经鞘瘤(mpnst)的方法
JP2025516648A (ja) 2022-05-09 2025-05-30 オリゾン・ゲノミクス・ソシエダッド・アノニマ Lsd1阻害薬を用いるnf1変異腫瘍の治療法
CN120529900A (zh) 2022-11-24 2025-08-22 奥莱松基因组股份有限公司 用于治疗癌症的LSD1抑制剂和Menin抑制剂的组合
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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NZ715331A (en) * 2013-06-19 2019-09-27 The Univ Of Utah Research Foundation Substituted (e)-n’-(1-phenylethylidene) benzohydrazide analogs as histone demethylase inhibitors

Also Published As

Publication number Publication date
AU2014281398A1 (en) 2016-01-21
MX2015018032A (es) 2016-10-03
EP3010915B1 (en) 2019-05-08
CA2915817C (en) 2022-12-13
JP6525162B2 (ja) 2019-06-05
IL243200B (en) 2020-10-29
KR20160024929A (ko) 2016-03-07
KR102288648B1 (ko) 2021-08-12
MX366949B (es) 2019-07-30
BR112015032113A2 (pt) 2017-03-21
SG10201710543PA (en) 2018-02-27
CA2915817A1 (en) 2014-12-24
AU2014281398B2 (en) 2018-10-04
ES2739814T3 (es) 2020-02-04
EP3010915A4 (en) 2016-12-28
JP2016523256A (ja) 2016-08-08
CN105555784B (zh) 2019-03-15
CN105555784A (zh) 2016-05-04
SG11201510376QA (en) 2016-01-28
EP3010915A1 (en) 2016-04-27
IL243200A0 (en) 2016-02-29
CN110015984A (zh) 2019-07-16
NZ715331A (en) 2019-09-27
WO2014205213A1 (en) 2014-12-24

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Date Code Title Description
B65X Notification of requirement for priority examination of patent application
B65Y Grant of priority examination of the patent application (request complies with dec. 132/06 of 20061117)
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B07A Application suspended after technical examination (opinion) [chapter 7.1 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B09X Republication of the decision to grant [chapter 9.1.3 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 19/06/2014, OBSERVADAS AS CONDICOES LEGAIS.

B21F Lapse acc. art. 78, item iv - on non-payment of the annual fees in time

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B24J Lapse because of non-payment of annual fees (definitively: art 78 iv lpi, resolution 113/2013 art. 12)

Free format text: EM VIRTUDE DA EXTINCAO PUBLICADA NA RPI 2832 DE 15-04-2025 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDA A EXTINCAO DA PATENTE E SEUS CERTIFICADOS, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013.