JP2023514280A - setd2阻害剤、および関連する方法と使用(併用療法を含む) - Google Patents

setd2阻害剤、および関連する方法と使用(併用療法を含む) Download PDF

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JP2023514280A
JP2023514280A JP2022549325A JP2022549325A JP2023514280A JP 2023514280 A JP2023514280 A JP 2023514280A JP 2022549325 A JP2022549325 A JP 2022549325A JP 2022549325 A JP2022549325 A JP 2022549325A JP 2023514280 A JP2023514280 A JP 2023514280A
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cycloalkyl
hydroxy
optionally substituted
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JPWO2021168313A5 (https=
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アレハンドラ ライモンディ マリア
アン トットマン ジェニファー
モトワニ ヴィニー
ルイーズ コスモポウロス キャサリン
ランプ ジョン
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エピザイム インコーポレイテッド
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    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • 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
    • 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
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/542Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/545Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
JP2022549325A 2020-02-19 2021-02-19 setd2阻害剤、および関連する方法と使用(併用療法を含む) Pending JP2023514280A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202062978692P 2020-02-19 2020-02-19
US62/978,692 2020-02-19
PCT/US2021/018863 WO2021168313A1 (en) 2020-02-19 2021-02-19 Setd2 inhibitors and related methods and uses, including combination therapies

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JP2023514280A true JP2023514280A (ja) 2023-04-05
JP2023514280A5 JP2023514280A5 (https=) 2024-02-27
JPWO2021168313A5 JPWO2021168313A5 (https=) 2024-02-27

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US (1) US20230133671A1 (https=)
EP (1) EP4107157A4 (https=)
JP (1) JP2023514280A (https=)
KR (1) KR20220143116A (https=)
CN (2) CN121695288A (https=)
AU (1) AU2021224855A1 (https=)
BR (1) BR112022016573A2 (https=)
CA (1) CA3168069A1 (https=)
IL (1) IL295654A (https=)
MX (1) MX2022010171A (https=)
WO (1) WO2021168313A1 (https=)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2020530844A (ja) 2017-08-14 2020-10-29 エピザイム,インコーポレイティド Setd2を阻害することにより癌を処置する方法
CN111093660A (zh) * 2017-09-05 2020-05-01 Epizyme股份有限公司 用于治疗癌症的组合疗法
CN112585119A (zh) 2018-08-14 2021-03-30 Epizyme股份有限公司 经取代的吲哚及其使用方法
US20240299352A1 (en) * 2021-06-09 2024-09-12 Epizyme, Inc. Combination therapies with setd2 inhibitors
JP2024539726A (ja) * 2021-11-01 2024-10-29 エピザイム,インコーポレイティド N-((1r,3s)-3-(4-アセチルピペラジン-1-イル)シクロヘキシル)-4-フルオロ-7-メチル-1h-インドール-2-カルボキサミドの結晶形態

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017509682A (ja) * 2014-04-04 2017-04-06 イオメット ファーマ リミテッド 医療で使用されるインドール誘導体
JP2021536428A (ja) * 2018-08-14 2021-12-27 エピザイム,インコーポレイティド 置換インドール及びその使用方法
JP2022511443A (ja) * 2018-11-30 2022-01-31 エピザイム,インコーポレイティド Setd2を阻害することにより、whsc1を過剰発現する癌を処置する方法

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4595766A (en) * 1984-10-26 1986-06-17 Ciba-Geigy Corporation Process for the preparation of an indoline carboxylic acid
US20100035862A1 (en) * 2008-06-25 2010-02-11 Abbott Laboratories Novel aza-cyclic indole-2-carboxamides and methods of use thereof
WO2016040505A1 (en) * 2014-09-10 2016-03-17 Epizyme, Inc. Smyd inhibitors

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017509682A (ja) * 2014-04-04 2017-04-06 イオメット ファーマ リミテッド 医療で使用されるインドール誘導体
JP2021536428A (ja) * 2018-08-14 2021-12-27 エピザイム,インコーポレイティド 置換インドール及びその使用方法
JP2022511443A (ja) * 2018-11-30 2022-01-31 エピザイム,インコーポレイティド Setd2を阻害することにより、whsc1を過剰発現する癌を処置する方法

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 20, JPN5023005960, 2010, pages 4620 - 4623, ISSN: 0005577391 *
SARCOMA, vol. 2016, JPN5023005962, 29 September 2016 (2016-09-29), pages 7461783 - 1, ISSN: 0005577392 *

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EP4107157A4 (en) 2024-03-13
MX2022010171A (es) 2022-12-06
BR112022016573A2 (pt) 2022-11-08
CA3168069A1 (en) 2021-08-26
WO2021168313A1 (en) 2021-08-26
KR20220143116A (ko) 2022-10-24
EP4107157A1 (en) 2022-12-28
CN115380033B (zh) 2026-01-09
AU2021224855A1 (en) 2022-09-08
CN121695288A (zh) 2026-03-20
CN115380033A (zh) 2022-11-22
US20230133671A1 (en) 2023-05-04
IL295654A (en) 2022-10-01

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