CN120204227A - 使用erk1和erk2的杂环抑制剂的改善的方法 - Google Patents

使用erk1和erk2的杂环抑制剂的改善的方法 Download PDF

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Publication number
CN120204227A
CN120204227A CN202510314107.1A CN202510314107A CN120204227A CN 120204227 A CN120204227 A CN 120204227A CN 202510314107 A CN202510314107 A CN 202510314107A CN 120204227 A CN120204227 A CN 120204227A
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CN
China
Prior art keywords
alkyl
amino
substituted
carboxamide
unsubstituted
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Pending
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CN202510314107.1A
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English (en)
Chinese (zh)
Inventor
S·雷迪
路易斯·丹尼斯
尼兰詹·拉奥
海伦·乌松斯凯
达纳·凯斯勒
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Asana Biosciences LLC
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Asana Biosciences LLC
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Publication of CN120204227A publication Critical patent/CN120204227A/zh
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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

Landscapes

  • 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)
CN202510314107.1A 2019-10-28 2020-10-22 使用erk1和erk2的杂环抑制剂的改善的方法 Pending CN120204227A (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201962926869P 2019-10-28 2019-10-28
US62/926,869 2019-10-28
CN202080091003.4A CN114901274A (zh) 2019-10-28 2020-10-22 使用erk1和erk2的杂环抑制剂的改善的方法、试剂盒、组合物和给药方案
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

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN202080091003.4A Division CN114901274A (zh) 2019-10-28 2020-10-22 使用erk1和erk2的杂环抑制剂的改善的方法、试剂盒、组合物和给药方案

Publications (1)

Publication Number Publication Date
CN120204227A true CN120204227A (zh) 2025-06-27

Family

ID=73476229

Family Applications (2)

Application Number Title Priority Date Filing Date
CN202510314107.1A Pending CN120204227A (zh) 2019-10-28 2020-10-22 使用erk1和erk2的杂环抑制剂的改善的方法
CN202080091003.4A Pending CN114901274A (zh) 2019-10-28 2020-10-22 使用erk1和erk2的杂环抑制剂的改善的方法、试剂盒、组合物和给药方案

Family Applications After (1)

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CN202080091003.4A Pending CN114901274A (zh) 2019-10-28 2020-10-22 使用erk1和erk2的杂环抑制剂的改善的方法、试剂盒、组合物和给药方案

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

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
EA024729B1 (ru) * 2009-11-13 2016-10-31 Джиноско Киназные ингибиторы
BR112017026159A2 (pt) * 2015-06-15 2018-08-14 Asana Biosciences, Llc inibidores heterocíclicos de erk1 e erk2 e seu uso no tratamento de câncer

Also Published As

Publication number Publication date
EP4051264A1 (en) 2022-09-07
WO2021086726A8 (en) 2021-06-03
US20230027072A1 (en) 2023-01-26
JP2022553351A (ja) 2022-12-22
CN114901274A (zh) 2022-08-12
JP7738550B2 (ja) 2025-09-12
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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