JP2020517618A - Ehmt2阻害剤との併用療法 - Google Patents

Ehmt2阻害剤との併用療法 Download PDF

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JP2020517618A
JP2020517618A JP2019556647A JP2019556647A JP2020517618A JP 2020517618 A JP2020517618 A JP 2020517618A JP 2019556647 A JP2019556647 A JP 2019556647A JP 2019556647 A JP2019556647 A JP 2019556647A JP 2020517618 A JP2020517618 A JP 2020517618A
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inhibitor
halo
alkyl
optionally substituted
independently
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JP2020517618A5 (ref
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ジョン エマーソン キャンベル,
ジョン エマーソン キャンベル,
ケネス ウィリアム ダンカン,
ケネス ウィリアム ダンカン,
マリア アレジャンドラ ライモンディ,
マリア アレジャンドラ ライモンディ,
クリスティーン クラウス,
クリスティーン クラウス,
エレイン ペネブレ,
エレイン ペネブレ,
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エピザイム,インコーポレイティド
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/20Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
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    • 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
    • A61K31/403Heterocyclic 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 carbocyclic rings, e.g. carbazole
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    • 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
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    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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    • A61K31/47Quinolines; Isoquinolines
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    • 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
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    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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JP2019556647A 2017-04-21 2018-04-20 Ehmt2阻害剤との併用療法 Withdrawn JP2020517618A (ja)

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JP2022184887A JP2023009301A (ja) 2017-04-21 2022-11-18 Ehmt2阻害剤との併用療法

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201762488679P 2017-04-21 2017-04-21
US62/488,679 2017-04-21
US201762574147P 2017-10-18 2017-10-18
US62/574,147 2017-10-18
PCT/US2018/028609 WO2018195450A1 (en) 2017-04-21 2018-04-20 Combination therapies with ehmt2 inhibitors

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JP2020517618A true JP2020517618A (ja) 2020-06-18
JP2020517618A5 JP2020517618A5 (ref) 2021-05-27

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JP2019556647A Withdrawn JP2020517618A (ja) 2017-04-21 2018-04-20 Ehmt2阻害剤との併用療法
JP2022184887A Pending JP2023009301A (ja) 2017-04-21 2022-11-18 Ehmt2阻害剤との併用療法

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US (2) US11672800B2 (ref)
EP (1) EP3612181A4 (ref)
JP (2) JP2020517618A (ref)
CN (2) CN110621316B (ref)
AU (1) AU2018254577B2 (ref)
CA (1) CA3060416A1 (ref)
WO (1) WO2018195450A1 (ref)

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JP2023532946A (ja) * 2020-07-10 2023-08-01 ブロッサムヒル・セラピューティクス・インコーポレイテッド 大員環分子およびそれらの使用
JP2024525368A (ja) * 2021-07-01 2024-07-12 エアリー ファーマシューティカルズ インコーポレイテッド アゼチジニルピリミジンおよびその使用

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