JP7738550B2 - Ｅｒｋ１およびｅｒｋ２の複素環式阻害剤の使用のための改善された方法、キット、組成物、ならびに投与レジメン - Google Patents

Ｅｒｋ１およびｅｒｋ２の複素環式阻害剤の使用のための改善された方法、キット、組成物、ならびに投与レジメン

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JP7738550B2
JP7738550B2 JP2022523718A JP2022523718A JP7738550B2 JP 7738550 B2 JP7738550 B2 JP 7738550B2 JP 2022523718 A JP2022523718 A JP 2022523718A JP 2022523718 A JP2022523718 A JP 2022523718A JP 7738550 B2 JP7738550 B2 JP 7738550B2
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alkyl
amino
methyl
carboxamide
imidazole
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JP2022553351A (ja
JP2022553351A5 (https=
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レディ，サンジーヴァ
デニス，ルイス
ラオ，ニランジャン
ウザンスキー，ヘレン
ケスラー，ダナ
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アサナ バイオサイエンシズ，リミティド ライアビリティ カンパニー
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    • 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
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non 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
    • A61K31/435—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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim 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
    • A61K31/535—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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
JP2022523718A 2019-10-28 2020-10-22 Ｅｒｋ１およびｅｒｋ２の複素環式阻害剤の使用のための改善された方法、キット、組成物、ならびに投与レジメン Active JP7738550B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962926869P 2019-10-28 2019-10-28
US62/926,869 2019-10-28
PCT/US2020/056936 WO2021086726A1 (en) 2019-10-28 2020-10-22 Improved methods, kits, compositions and dosing regimens for the use of heterocyclic inhibitors of erk1 and erk2

Publications (3)

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JP2022553351A JP2022553351A (ja) 2022-12-22
JP2022553351A5 JP2022553351A5 (https=) 2023-10-27
JP7738550B2 true JP7738550B2 (ja) 2025-09-12

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JP2022523718A Active JP7738550B2 (ja) 2019-10-28 2020-10-22 Ｅｒｋ１およびｅｒｋ２の複素環式阻害剤の使用のための改善された方法、キット、組成物、ならびに投与レジメン

Country Status (9)

Country Link
US (1) US20230027072A1 (https=)
EP (1) EP4051264A1 (https=)
JP (1) JP7738550B2 (https=)
KR (1) KR20220106754A (https=)
CN (2) CN120204227A (https=)
AU (1) AU2020375720A1 (https=)
CA (1) CA3158910A1 (https=)
TW (1) TW202128665A (https=)
WO (1) WO2021086726A1 (https=)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112017026159A2 (pt) 2015-06-15 2018-08-14 Asana Biosciences, Llc inibidores heterocíclicos de erk1 e erk2 e seu uso no tratamento de câncer
US11866421B2 (en) * 2021-05-31 2024-01-09 Epigen Biosciences, Inc. Pyrimidine and pyridine amine compounds and usage thereof in disease treatment
JP2024526135A (ja) * 2021-06-24 2024-07-17 エラスカ，インク． Ｅｒｋ１／２阻害剤とｋｒａｓ ｇ１２ｃ阻害剤の併用療法
WO2022271939A1 (en) * 2021-06-24 2022-12-29 Erasca, Inc. Erk1/2 and cdk4/6 inhibitors combination therapy
US20240285624A1 (en) * 2021-06-24 2024-08-29 Erasca, Inc. Erk1/2 or shp2 inhibitors and flt3 inhibitors combination therapy
CN117957001A (zh) * 2021-06-24 2024-04-30 阿沙纳生物科学公司 Erk1/2抑制剂组合疗法
AU2022299193A1 (en) * 2021-06-24 2024-01-04 Erasca, Inc. Erk1/2 and egfr inhibitors combination therapy
IL309401A (en) * 2021-06-24 2024-02-01 Erasca Inc Combined treatment with ERK1/2 and SHP2 inhibitors
WO2023044065A1 (en) * 2021-09-17 2023-03-23 Erasca, Inc. Jak inhibitor with erk1/2 and/or shp2 inhibitors combination therapy
WO2024064690A1 (en) * 2022-09-20 2024-03-28 Erasca, Inc. Erk1/2 inhibitor polymorph forms

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007513172A (ja) 2003-12-02 2007-05-24 バーテックス　ファーマシューティカルズ　インコーポレイテッド 複素環式プロテインキナーゼインヒビターおよびその使用
JP2013510876A (ja) 2009-11-13 2013-03-28 ジェノスコ キナーゼ阻害剤
JP2018517685A (ja) 2015-06-15 2018-07-05 アサナ バイオサイエンシズ，リミティド ライアビリティ カンパニー Ｅｒｋ１及びｅｒｋ２の複素環式阻害剤並びに癌治療におけるその使用

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6743941B2 (en) 2001-06-15 2004-06-01 Aventis Pharma Deutschland Gmbh Process for the production of piperidine derivatives
US8546404B2 (en) 2005-12-13 2013-10-01 Merck Sharp & Dohme Compounds that are ERK inhibitors

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007513172A (ja) 2003-12-02 2007-05-24 バーテックス　ファーマシューティカルズ　インコーポレイテッド 複素環式プロテインキナーゼインヒビターおよびその使用
JP2013510876A (ja) 2009-11-13 2013-03-28 ジェノスコ キナーゼ阻害剤
JP2018517685A (ja) 2015-06-15 2018-07-05 アサナ バイオサイエンシズ，リミティド ライアビリティ カンパニー Ｅｒｋ１及びｅｒｋ２の複素環式阻害剤並びに癌治療におけるその使用

Also Published As

Publication number Publication date
EP4051264A1 (en) 2022-09-07
WO2021086726A8 (en) 2021-06-03
US20230027072A1 (en) 2023-01-26
CN120204227A (zh) 2025-06-27
JP2022553351A (ja) 2022-12-22
CN114901274A (zh) 2022-08-12
WO2021086726A1 (en) 2021-05-06
KR20220106754A (ko) 2022-07-29
TW202128665A (zh) 2021-08-01
CA3158910A1 (en) 2021-05-06
AU2020375720A1 (en) 2022-05-19

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