BR112020017561A2 - Compostos com atividade indutora de ferroptose e métodos de seu uso - Google Patents

Compostos com atividade indutora de ferroptose e métodos de seu uso Download PDF

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Publication number
BR112020017561A2
BR112020017561A2 BR112020017561-7A BR112020017561A BR112020017561A2 BR 112020017561 A2 BR112020017561 A2 BR 112020017561A2 BR 112020017561 A BR112020017561 A BR 112020017561A BR 112020017561 A2 BR112020017561 A2 BR 112020017561A2
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BR
Brazil
Prior art keywords
c6alkyl
c6alkenyl
heterocyclyl
independently
halo
Prior art date
Application number
BR112020017561-7A
Other languages
English (en)
Portuguese (pt)
Inventor
Chun Jiang
Ruihong Chen
Anjali Pandey
Biswajit KALITA
Athisayamani Jeyaraj Duraiswamy
Original Assignee
Ferro Therapeutics, 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 Ferro Therapeutics, Inc. filed Critical Ferro Therapeutics, Inc.
Publication of BR112020017561A2 publication Critical patent/BR112020017561A2/pt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
    • C07D217/04Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
    • C07D217/06Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines with the ring nitrogen atom acylated by carboxylic or carbonic acids, or with sulfur or nitrogen analogues thereof, e.g. carbamates
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/12Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring
    • C07D217/14Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/12Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring
    • C07D217/14Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals
    • C07D217/16Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals substituted by oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
    • C07D217/26Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/40Cyclodextrins; Derivatives thereof

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
BR112020017561-7A 2018-02-28 2019-02-27 Compostos com atividade indutora de ferroptose e métodos de seu uso BR112020017561A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862636614P 2018-02-28 2018-02-28
US62/636,614 2018-02-28
PCT/US2019/019854 WO2019168999A1 (en) 2018-02-28 2019-02-27 Compounds with ferroptosis inducing activity and methods of their use

Publications (1)

Publication Number Publication Date
BR112020017561A2 true BR112020017561A2 (pt) 2020-12-22

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Family Applications (1)

Application Number Title Priority Date Filing Date
BR112020017561-7A BR112020017561A2 (pt) 2018-02-28 2019-02-27 Compostos com atividade indutora de ferroptose e métodos de seu uso

Country Status (16)

Country Link
US (2) US11098040B2 (https=)
EP (1) EP3759075B1 (https=)
JP (1) JP7348906B2 (https=)
KR (1) KR20200135961A (https=)
CN (1) CN112041301A (https=)
AR (2) AR114417A1 (https=)
AU (1) AU2019229256A1 (https=)
BR (1) BR112020017561A2 (https=)
CA (1) CA3092143A1 (https=)
EA (1) EA202091846A1 (https=)
ES (1) ES3038012T3 (https=)
IL (1) IL276788A (https=)
MX (2) MX2020008906A (https=)
SG (1) SG11202008230PA (https=)
TW (1) TW202000663A (https=)
WO (1) WO2019168999A1 (https=)

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US11040964B2 (en) 2019-02-27 2021-06-22 Ferro Therapeutics, Inc. Compounds and methods of use
MX2021010173A (es) * 2019-02-27 2021-12-10 Ferro Therapeutics Inc Compuestos con actividad inductora de ferroptosis y métodos de uso.
US20220227765A1 (en) * 2019-08-28 2022-07-21 Ferro Therapeutics, Inc. Pyrido-indole analogues as gpx4 inhibitors
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CN110627786B (zh) * 2019-10-29 2020-11-24 株洲千金药业股份有限公司 一种他达拉非中间体的制备方法
JP2023509359A (ja) 2019-12-17 2023-03-08 フラグシップ パイオニアリング イノベーションズ ブイ,インコーポレーテッド 鉄依存性細胞分解の誘導物質との併用抗癌療法
US11998534B2 (en) * 2020-02-12 2024-06-04 Eubulus Biotherapeutics Inc. GPX4 inhibitor in combination with anticancer agent for treating proliferative disease
CN115243719B (zh) * 2020-03-06 2024-09-13 北京先通生物医药技术有限公司 CTB006与Ponatinib联合应用
TW202227399A (zh) * 2020-08-26 2022-07-16 美商費洛醫療公司 化合物及使用方法
AU2021391453A1 (en) * 2020-12-04 2023-07-13 Eubulus Biotherapeutics Inc. Heteroaryl-acetylenes, pharmaceutical compositions thereof, and their therapeutic applications
KR20220139813A (ko) * 2021-04-08 2022-10-17 서울대학교산학협력단 암 환자의 예후 예측용 바이오마커 및 이의 용도
CN113336748B (zh) * 2021-04-12 2022-03-25 北京大学 一种gpx4蛋白降解剂及其制备方法和应用、一种抗肿瘤细胞药物
US11541116B1 (en) 2022-01-07 2023-01-03 Kojin Therapeutics, Inc. Methods and compositions for inducing ferroptosis in vivo
WO2024015637A1 (en) * 2022-07-15 2024-01-18 Ferro Therapeutics, Inc. Glutathione peroxidase 4 (gpx4) inhibitors for the treatment of cancer
WO2024039860A1 (en) * 2022-08-19 2024-02-22 Olema Pharmaceuticals, Inc. 2,3,4,9-tetrahydro-1h-pyrido[3,4-b]indole derivatives as estrogen receptor modulators for the treatment of cancer
WO2024123412A1 (en) * 2022-12-09 2024-06-13 The University Of Toledo Ferroptosis inducers to treat cancer
CN118994147B (zh) * 2024-07-18 2026-01-02 中国海洋大学 一种基于疏水标签的gpx4蛋白降解剂及其制备方法和应用
CN120923499A (zh) * 2025-08-08 2025-11-11 兰州大学 一种铁死亡激动剂、缺氧响应型纳米共递送系统及其应用

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Also Published As

Publication number Publication date
EP3759075B1 (en) 2025-07-23
TW202000663A (zh) 2020-01-01
US20230039846A1 (en) 2023-02-09
AR118205A1 (es) 2021-09-22
AR114417A1 (es) 2020-09-02
MX2023001527A (es) 2023-03-06
WO2019168999A1 (en) 2019-09-06
CA3092143A1 (en) 2019-09-06
AU2019229256A1 (en) 2020-09-17
SG11202008230PA (en) 2020-09-29
ES3038012T3 (en) 2025-10-08
EA202091846A1 (ru) 2021-06-01
KR20200135961A (ko) 2020-12-04
JP7348906B2 (ja) 2023-09-21
US11098040B2 (en) 2021-08-24
CN112041301A (zh) 2020-12-04
JP2021515010A (ja) 2021-06-17
EP3759075A1 (en) 2021-01-06
MX2020008906A (es) 2021-02-26
US20190263802A1 (en) 2019-08-29
IL276788A (en) 2020-10-29

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B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

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