BR112021019508A2 - Composto de amina aromática e uso do mesmo na preparação de reguladores e inibidores duplos de ar e brd4 - Google Patents

Composto de amina aromática e uso do mesmo na preparação de reguladores e inibidores duplos de ar e brd4

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Publication number
BR112021019508A2
BR112021019508A2 BR112021019508A BR112021019508A BR112021019508A2 BR 112021019508 A2 BR112021019508 A2 BR 112021019508A2 BR 112021019508 A BR112021019508 A BR 112021019508A BR 112021019508 A BR112021019508 A BR 112021019508A BR 112021019508 A2 BR112021019508 A2 BR 112021019508A2
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BR
Brazil
Prior art keywords
brd4
compound
preparation
dual
regulators
Prior art date
Application number
BR112021019508A
Other languages
English (en)
Inventor
Dekun Qin
Haibin Lv
Haibo Li
Wu Du
Xinghai Li
Yu Li
Yuanwei Chen
Zhilin Tu
Original Assignee
Hinova Pharmaceuticals Inc
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Publication date
Application filed by Hinova Pharmaceuticals Inc filed Critical Hinova Pharmaceuticals Inc
Publication of BR112021019508A2 publication Critical patent/BR112021019508A2/pt

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4245—Oxadiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/08—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/32—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

são fornecidos um composto de amina aromática e uso do mesmo na preparação de inibidores e reguladores duplos de ar e brd4. especificamente é fornecido o composto mostrado na fórmula i, o dito composto possuindo efeitos inibitórios duplos sobre ar e brd4. o composto não é capaz de inibir apenas a proliferação do receptor ar de androgênio superexpresso na linhagem celular de câncer de próstata lncap/ar, mas também mostra bons efeitos inibitórios sobre as linhagens de câncer de próstata vcap e rrrv1 que são resistentes aos fármacos para câncer de próstata (enzalutamida) do mercado. o próprio composto é um composto capaz de simultaneamente identificar alvos duplos de ar e brd4 e pode ser usado como um inibidor duplo de ar/bdr4 e também é capaz de ser usado na preparação de quimeras direcionadas à proteólise (protacs) para induzir a degradação de alvos duplos de ar/brd4 e tem boas perspectivas para aplicação na preparação de fármacos para o tratamento de doenças relacionadas a ar e brd4. fórmula i
BR112021019508A 2019-04-02 2020-03-31 Composto de amina aromática e uso do mesmo na preparação de reguladores e inibidores duplos de ar e brd4 BR112021019508A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN201910263315 2019-04-02
PCT/CN2020/082513 WO2020200209A1 (zh) 2019-04-02 2020-03-31 芳香胺类化合物及其在制备ar和brd4双重抑制剂和调控剂中的用途

Publications (1)

Publication Number Publication Date
BR112021019508A2 true BR112021019508A2 (pt) 2022-02-01

Family

ID=72664424

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112021019508A BR112021019508A2 (pt) 2019-04-02 2020-03-31 Composto de amina aromática e uso do mesmo na preparação de reguladores e inibidores duplos de ar e brd4

Country Status (9)

Country Link
US (1) US20220177459A1 (pt)
EP (1) EP3950678A4 (pt)
JP (1) JP2022527925A (pt)
KR (1) KR20210125558A (pt)
CN (1) CN111793031B (pt)
AU (1) AU2020251673B2 (pt)
BR (1) BR112021019508A2 (pt)
CA (1) CA3135929A1 (pt)
WO (1) WO2020200209A1 (pt)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110960528A (zh) * 2018-09-30 2020-04-07 四川大学 Ar和bet双重抑制剂及其用途
WO2022175752A1 (en) 2021-02-19 2022-08-25 Sudo Biosciences Limited Tyk2 inhibitors and uses thereof
TW202328096A (zh) * 2021-08-27 2023-07-16 南韓商柳韓洋行 作為egfr抑制劑之含五員雜芳基之胺基吡啶化合物

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2892045C (en) * 2012-11-21 2022-05-31 Ptc Therapeutics, Inc. Substituted reverse pyrimidine bmi-1 inhibitors
EP3227281A4 (en) * 2014-12-01 2018-05-30 Zenith Epigenetics Ltd. Substituted pyridinones as bromodomain inhibitors
CA2966303A1 (en) * 2014-12-01 2016-06-09 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
AU2017209935B2 (en) * 2016-01-22 2021-04-01 Janssen Pharmaceutica Nv New substituted cyanoindoline derivatives as NIK inhibitors
WO2017133681A1 (zh) * 2016-02-05 2017-08-10 正大天晴药业集团股份有限公司 溴区结构域蛋白抑制剂的三环类化合物及其制备、药物组合物和用途
CN107814785B (zh) * 2016-09-14 2021-02-05 四川大学 雄激素受体拮抗剂及其制备方法和用途
CN110960528A (zh) * 2018-09-30 2020-04-07 四川大学 Ar和bet双重抑制剂及其用途
CN109608394A (zh) * 2018-12-03 2019-04-12 湖南大学 氮杂芳胺类化合物的合成方法和氮杂芳胺类化合物

Also Published As

Publication number Publication date
JP2022527925A (ja) 2022-06-07
EP3950678A4 (en) 2023-04-26
CN111793031B (zh) 2021-06-22
WO2020200209A1 (zh) 2020-10-08
CN111793031A (zh) 2020-10-20
KR20210125558A (ko) 2021-10-18
AU2020251673A1 (en) 2021-11-11
AU2020251673B2 (en) 2023-09-28
EP3950678A1 (en) 2022-02-09
CA3135929A1 (en) 2020-10-08
US20220177459A1 (en) 2022-06-09

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