TW202334147A - 氮雜吲哚衍生物及其作為erk激酶抑制劑之用途 - Google Patents

氮雜吲哚衍生物及其作為erk激酶抑制劑之用途 Download PDF

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TW202334147A
TW202334147A TW111150950A TW111150950A TW202334147A TW 202334147 A TW202334147 A TW 202334147A TW 111150950 A TW111150950 A TW 111150950A TW 111150950 A TW111150950 A TW 111150950A TW 202334147 A TW202334147 A TW 202334147A
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Taiwan
Prior art keywords
compound
pyridin
atom
ethyl
dimethylamino
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TW111150950A
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English (en)
Chinese (zh)
Inventor
瑟卓克 包理斯
羅伊克 馬修
珍 法司瓦 桂裘
莫瑞爾 吉林
奧瑞琳 碧齊
Original Assignee
法商Agv探索公司
法商英瑟姆公司
法國國家科學研究中心
法國蒙彼利埃大學
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Publication of TW202334147A publication Critical patent/TW202334147A/zh

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • 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
    • A61P35/04Antineoplastic agents specific for metastasis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/62Oxygen or sulfur atoms
    • C07D213/63One oxygen atom
    • C07D213/64One oxygen atom attached in position 2 or 6
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/62Oxygen or sulfur atoms
    • C07D213/63One oxygen atom
    • C07D213/64One oxygen atom attached in position 2 or 6
    • C07D213/6432-Phenoxypyridines; Derivatives thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02Boron compounds
    • C07F5/025Boronic and borinic acid compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02Boron compounds
    • C07F5/027Organoboranes and organoborohydrides

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • AIDS & HIV (AREA)
  • Molecular Biology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
TW111150950A 2022-01-14 2022-12-30 氮雜吲哚衍生物及其作為erk激酶抑制劑之用途 TW202334147A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP22305031.1A EP4212531A1 (en) 2022-01-14 2022-01-14 Azaindole derivatives and their use as erk kinase inhibitors
EP22305031.1 2022-01-14

Publications (1)

Publication Number Publication Date
TW202334147A true TW202334147A (zh) 2023-09-01

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TW111150950A TW202334147A (zh) 2022-01-14 2022-12-30 氮雜吲哚衍生物及其作為erk激酶抑制劑之用途

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Country Link
US (3) US11827637B2 (https=)
EP (2) EP4212531A1 (https=)
JP (1) JP2025502377A (https=)
KR (1) KR20240134887A (https=)
CN (1) CN118541370A (https=)
AR (1) AR128267A1 (https=)
AU (1) AU2023207276A1 (https=)
CA (1) CA3242894A1 (https=)
CL (1) CL2024002070A1 (https=)
CO (1) CO2024008809A2 (https=)
IL (1) IL314199A (https=)
JO (1) JOP20240157A1 (https=)
MX (1) MX2024008629A (https=)
TW (1) TW202334147A (https=)
UA (1) UA130477C2 (https=)
WO (1) WO2023135233A1 (https=)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4212531A1 (en) * 2022-01-14 2023-07-19 AGV Discovery Azaindole derivatives and their use as erk kinase inhibitors
WO2025012386A1 (en) * 2023-07-12 2025-01-16 Agv Discovery Crystalline form of (s)-1-(1-(3-chlorophenyl)-2- (dimethylamino)ethyl)-4-(5-morpholino-1h-pyrrolo[2,3- b]pyridin-3-yl)pyridin-2(1h)-one, its preparation and its use as erk kinase inhibitor
WO2025012357A1 (en) * 2023-07-12 2025-01-16 Ipsen Pharma Fluorinated azaindole derivatives and their use as erk kinase inhibitors
CN121511244A (zh) * 2023-07-12 2026-02-10 Agv探索公司 (s)-1-(1-(3-氯苯基)-2-(二甲氨基)乙基)-4-(5-吗啉代-1h-吡咯并[2,3-b]吡啶-3-基)吡啶-2(1h)-酮的盐,其制备及其作为erk激酶抑制剂的用途
EP4588918A1 (en) 2024-01-18 2025-07-23 AGV Discovery Synthesis of (s)-1-(1-(3-chlorophenyl)-2-(dimethylamino)ethyl)- 4-(5-morpholino-1h-pyrrolo[2,3-b]pyridin-3-yl)pyridin-2(1h)-one
WO2026064271A1 (en) 2024-09-23 2026-03-26 Fmc Corporation Substituted bicyclic amide derivatives as herbicides

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI339206B (en) 2003-09-04 2011-03-21 Vertex Pharma Compositions useful as inhibitors of protein kinases
UA84930C2 (ru) 2004-05-14 2008-12-10 Вертекс Фармасьютикалс Инкорпорейтед Пиррольные соединения как ингибиторы протеинкиназ erk, их синтез и соответствующие промежуточные соединения
US7361764B2 (en) 2004-07-27 2008-04-22 Sgx Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
CN100396678C (zh) 2004-11-16 2008-06-25 财团法人工业技术研究院 1-苯甲基-3-(5’-羟甲基-2’-呋喃基)吲唑的吲哚类似物的合成及用途
EP2038272B8 (en) 2006-06-30 2013-10-23 Sunesis Pharmaceuticals, Inc. Pyridinonyl pdk1 inhibitors
AU2007275221A1 (en) 2006-07-20 2008-01-24 Allen J. Borchardt Benzothiophene inhibitors of RHO kinase
EP2102189B1 (en) 2006-12-15 2015-07-29 Bristol-Myers Squibb Company Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor xia inhibitors
WO2012094313A1 (en) 2011-01-04 2012-07-12 Kinentia Biosciences Llc Pyrazole derivatives as erk inhibitors
EP2739143B1 (en) 2011-08-05 2018-07-11 Gary A. Flynn Preparation and methods of use for ortho-aryl 5- membered heteroaryl-carboxamide containing multi-targeted kinase inhibitors
JO3215B1 (ar) 2012-08-09 2018-03-08 Phenex Pharmaceuticals Ag حلقات غير متجانسة بها 5 ذرات تحتوي على النيتروجين بها استبدال بكربوكساميد أو سلفوناميد كمعدلات لمستقبل نووي غير محمي RORy
MX2015004615A (es) 2012-10-16 2015-07-17 Hoffmann La Roche Inhibidores de serina/treonina cinasa.
GB2515785A (en) 2013-07-03 2015-01-07 Redx Pharma Ltd Compounds
EP3247353A4 (en) 2015-01-23 2018-07-04 Confluence Life Sciences, Inc. Heterocyclic itk inhibitors for treating inflammation and cancer
EP3170822A1 (en) 2015-11-18 2017-05-24 AGV Discovery Azaindole derivatives and their use as erk kinase inhibitors
EP3551651B1 (en) 2016-12-09 2024-03-06 Zealand Pharma A/S Acylated glp-1/glp-2 dual agonists
BR112021009430A2 (pt) * 2018-11-16 2021-08-17 California Institute Of Technology inibidores de erk e usos dos mesmos
EP4212531A1 (en) * 2022-01-14 2023-07-19 AGV Discovery Azaindole derivatives and their use as erk kinase inhibitors

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Publication number Publication date
US12421231B2 (en) 2025-09-23
UA130477C2 (uk) 2026-02-25
WO2023135233A1 (en) 2023-07-20
JP2025502377A (ja) 2025-01-24
CO2024008809A2 (es) 2024-08-08
CN118541370A (zh) 2024-08-23
AU2023207276A1 (en) 2024-08-01
AR128267A1 (es) 2024-04-10
EP4212531A1 (en) 2023-07-19
US11827637B2 (en) 2023-11-28
US20260042758A1 (en) 2026-02-12
US20230227451A1 (en) 2023-07-20
IL314199A (en) 2024-09-01
US20240308997A1 (en) 2024-09-19
EP4463453A1 (en) 2024-11-20
CA3242894A1 (en) 2025-02-28
CL2024002070A1 (es) 2024-11-29
KR20240134887A (ko) 2024-09-10
MX2024008629A (es) 2024-08-19
JOP20240157A1 (ar) 2024-07-14

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