EA202092253A1 - Замещенные производные имидазолидин-2-она в качестве ингибиторов prmt5 - Google Patents

Замещенные производные имидазолидин-2-она в качестве ингибиторов prmt5

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Publication number
EA202092253A1
EA202092253A1 EA202092253A EA202092253A EA202092253A1 EA 202092253 A1 EA202092253 A1 EA 202092253A1 EA 202092253 A EA202092253 A EA 202092253A EA 202092253 A EA202092253 A EA 202092253A EA 202092253 A1 EA202092253 A1 EA 202092253A1
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EA
Eurasian Patent Office
Prior art keywords
derivatives
prmt5
prmt5 inhibitors
substituted imidazolidin
formula
Prior art date
Application number
EA202092253A
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English (en)
Inventor
Динеш Чикканна
Сунил Кумар Паниграхи
Сриниваса Раджу Саммета
Original Assignee
Ауриген Дискавери Текнолоджиз Лимитед
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Application filed by Ауриген Дискавери Текнолоджиз Лимитед filed Critical Ауриген Дискавери Текнолоджиз Лимитед
Publication of EA202092253A1 publication Critical patent/EA202092253A1/ru

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    • 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
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine 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
    • A61K31/495—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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines 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
    • A61K31/535—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
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
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    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
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    • 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
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    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
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    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
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    • C07D495/02—Heterocyclic 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
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
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    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08—Bridged systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
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  • General Health & Medical Sciences (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Настоящее изобретение относится к замещенным производным имидазолидин-2-она формулы (I) или их фармацевтически приемлемым солям. Настоящее изобретение дополнительно относится к способам получения соединения формулы (I) и применения в качестве ингибиторов PRMT5. Соединения применимы в качестве лекарственных препаратов для лечении состояний и нарушений, опосредованных PRMT5, таких как рак, метаболические нарушения, воспаление, аутоиммунное заболевание и гемоглобинопатия.
EA202092253A 2018-03-22 2019-03-20 Замещенные производные имидазолидин-2-она в качестве ингибиторов prmt5 EA202092253A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN201841010656 2018-03-22
PCT/IB2019/052252 WO2019180631A1 (en) 2018-03-22 2019-03-20 Substituted imidazolidin-2-one derivatives as prmt5 inhibitors

Publications (1)

Publication Number Publication Date
EA202092253A1 true EA202092253A1 (ru) 2021-01-14

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EA202092253A EA202092253A1 (ru) 2018-03-22 2019-03-20 Замещенные производные имидазолидин-2-она в качестве ингибиторов prmt5

Country Status (15)

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US (1) US11542275B2 (ru)
EP (1) EP3768671B1 (ru)
JP (2) JP7254094B2 (ru)
KR (1) KR20200135827A (ru)
CN (1) CN112105609A (ru)
AU (1) AU2019237329B2 (ru)
BR (1) BR112020019111A2 (ru)
CA (1) CA3092770A1 (ru)
CU (1) CU24627B1 (ru)
EA (1) EA202092253A1 (ru)
IL (1) IL277518B2 (ru)
MX (1) MX2020009738A (ru)
PH (1) PH12020551494A1 (ru)
SG (1) SG11202008526VA (ru)
WO (1) WO2019180631A1 (ru)

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WO2019180628A1 (en) * 2018-03-22 2019-09-26 Aurigene Discovery Technologies Limited Imidazolidin-2-one compounds as prmt5 modulators
US11077101B1 (en) 2018-07-18 2021-08-03 Tango Therapeutics, Inc. Compounds and methods of use
EP4188920A1 (en) 2020-07-31 2023-06-07 Tango Therapeutics, Inc. Piperidin-1-yl-n-pyrydine-3-yl-2-oxoacetamide derivatives useful for the treatment of mtap-deficient and/or mta-accumulating cancers
CN115232147B (zh) * 2022-08-09 2023-10-13 南方科技大学 一种作为HIF-2α激动剂的杂环衍生物

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DE69729583T2 (de) * 1996-04-17 2005-06-09 Bristol-Myers Squibb Pharma Co. N-(amidinophenyl)-n'-(subst.)-3h-2,4-benzodiazepin-3-on derivative als faktor xa inhibitoren
KR101360725B1 (ko) 2009-06-26 2014-02-07 노파르티스 아게 Ｃｙｐ17의 억제제로서의 1,3-이치환된 이미다졸리딘-2-온 유도체
MX359399B (es) * 2011-04-28 2018-09-27 Novartis Ag Inhibidores de 17alfa-hidroxilasa/c17-20-liasa.
IN2012CH00067A (ru) * 2012-01-06 2017-08-04
CA2899363A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. Prmt5 inhibitors and uses thereof
CA2894130A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. Prmt5 inhibitors containing a dihydro- or tetrahydroisoquinoline and uses thereof
US10118918B2 (en) 2012-12-21 2018-11-06 Epizyme, Inc. PRMT5 inhibitors and uses thereof
PT2935222T (pt) 2012-12-21 2018-12-10 Epizyme Inc Inibidores de prmt5 e seus usos
JP2016511744A (ja) 2012-12-21 2016-04-21 エピザイム，インコーポレイティド Ｐｒｍｔ５を阻害する方法
WO2014108820A1 (en) * 2013-01-08 2014-07-17 Aurigene Discovery Technologies Limited Substituted 2-pyrazinone derivatives as kinase inhibitors
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JP6510485B2 (ja) 2013-03-15 2019-05-08 オハイオ・ステイト・イノベーション・ファウンデーション Ｐｒｍｔ５インヒビターおよびそれらの使用方法
TWI690521B (zh) * 2014-04-07 2020-04-11 美商同步製藥公司 作為隱花色素調節劑之含有咔唑之醯胺類、胺基甲酸酯類及脲類
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SG11202008526VA (en) 2020-10-29
JP2021518366A (ja) 2021-08-02
CA3092770A1 (en) 2019-09-26
EP3768671A4 (en) 2021-11-24
EP3768671A1 (en) 2021-01-27
AU2019237329B2 (en) 2024-03-28
IL277518B2 (en) 2024-01-01
BR112020019111A2 (pt) 2021-01-12
JP2023082088A (ja) 2023-06-13
MX2020009738A (es) 2020-10-08
US20210002298A1 (en) 2021-01-07
WO2019180631A1 (en) 2019-09-26
US11542275B2 (en) 2023-01-03
CN112105609A (zh) 2020-12-18
KR20200135827A (ko) 2020-12-03
JP7254094B2 (ja) 2023-04-07
AU2019237329A1 (en) 2020-10-01
IL277518B1 (en) 2023-09-01
CU20200067A7 (es) 2021-04-07
CU24627B1 (es) 2022-11-07
IL277518A (en) 2020-11-30
EP3768671B1 (en) 2024-05-22
PH12020551494A1 (en) 2021-09-01

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