KR20220106754A - Erk1 및 erk2의 헤테로시클릭 억제제의 사용을 위한 개선된 방법, 키트, 조성물 및 투약 요법 - Google Patents

Erk1 및 erk2의 헤테로시클릭 억제제의 사용을 위한 개선된 방법, 키트, 조성물 및 투약 요법 Download PDF

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KR20220106754A
KR20220106754A KR1020227017170A KR20227017170A KR20220106754A KR 20220106754 A KR20220106754 A KR 20220106754A KR 1020227017170 A KR1020227017170 A KR 1020227017170A KR 20227017170 A KR20227017170 A KR 20227017170A KR 20220106754 A KR20220106754 A KR 20220106754A
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alkyl
amino
carboxamide
chlorophenyl
methyl
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Korean (ko)
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산지바 레디
루이스 데니스
니란잔 라오
헬렌 우산스키
다나 케슬러
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아사나 바이오사이언시스 엘엘씨
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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
    • A61K31/495—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
    • A61K31/41—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
    • A61K31/535—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)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (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)
KR1020227017170A 2019-10-28 2020-10-22 Erk1 및 erk2의 헤테로시클릭 억제제의 사용을 위한 개선된 방법, 키트, 조성물 및 투약 요법 Ceased KR20220106754A (ko)

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 (1)

Publication Number Publication Date
KR20220106754A true KR20220106754A (ko) 2022-07-29

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KR1020227017170A Ceased KR20220106754A (ko) 2019-10-28 2020-10-22 Erk1 및 erk2의 헤테로시클릭 억제제의 사용을 위한 개선된 방법, 키트, 조성물 및 투약 요법

Country Status (9)

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

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107922387B (zh) 2015-06-15 2024-11-22 阿沙纳生物科学公司 Erk1与erk2的杂环抑制剂及其在癌症治疗中的应用
US11866421B2 (en) * 2021-05-31 2024-01-09 Epigen Biosciences, Inc. Pyrimidine and pyridine amine compounds and usage thereof in disease treatment
WO2022271919A1 (en) * 2021-06-24 2022-12-29 Erasca, Inc. Erk1/2 or shp2 inhibitors and flt3 inhibitors combination therapy
KR20240055721A (ko) * 2021-06-24 2024-04-29 아사나 바이오사이언시스 엘엘씨 Erk1/2 억제제 조합 요법
EP4358964A1 (en) * 2021-06-24 2024-05-01 Erasca, Inc. Erk1/2 and kras g12c inhibitors combination therapy
TW202317123A (zh) * 2021-06-24 2023-05-01 美商艾瑞斯卡公司 Erk1/2及cdk4/6抑制劑之組合療法
US20240299388A1 (en) * 2021-06-24 2024-09-12 Erasca, Inc. Erk1/2 and shp2 inhibitors combination therapy
KR20240044419A (ko) * 2021-06-24 2024-04-04 에라스카, 아이엔씨. Erk1/2 및 egfr 억제제 조합 요법
CN117940132A (zh) * 2021-06-24 2024-04-26 医睿世康药业研发公司 Erk1/2和kras g12c抑制剂组合疗法
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

Family Cites Families (5)

* 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
CA2547080A1 (en) 2003-12-02 2005-07-28 Vertex Pharmaceuticals, Inc. Heterocyclic protein kinase inhibitors and uses thereof
US8546404B2 (en) 2005-12-13 2013-10-01 Merck Sharp & Dohme Compounds that are ERK inhibitors
CA2780892C (en) 2009-11-13 2017-02-14 Genosco Kinase inhibitors
CN107922387B (zh) 2015-06-15 2024-11-22 阿沙纳生物科学公司 Erk1与erk2的杂环抑制剂及其在癌症治疗中的应用

Also Published As

Publication number Publication date
EP4051264A1 (en) 2022-09-07
WO2021086726A1 (en) 2021-05-06
CN114901274A (zh) 2022-08-12
JP2022553351A (ja) 2022-12-22
TW202128665A (zh) 2021-08-01
CA3158910A1 (en) 2021-05-06
WO2021086726A8 (en) 2021-06-03
JP7738550B2 (ja) 2025-09-12
US20230027072A1 (en) 2023-01-26
AU2020375720A1 (en) 2022-05-19
CN120204227A (zh) 2025-06-27

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