JP7338896B2 - Ｍｄｍ２阻害剤、その調製方法、医薬組成物および応用 - Google Patents

Ｍｄｍ２阻害剤、その調製方法、医薬組成物および応用 Download PDF

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JP7338896B2
JP7338896B2 JP2021517766A JP2021517766A JP7338896B2 JP 7338896 B2 JP7338896 B2 JP 7338896B2 JP 2021517766 A JP2021517766 A JP 2021517766A JP 2021517766 A JP2021517766 A JP 2021517766A JP 7338896 B2 JP7338896 B2 JP 7338896B2
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JP2022502448A5 (https=
JP2022502448A (ja
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ワン，ツェー
ゼン，ジホン
ジャン，ロンゼン
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Shanghai Longwood Biopharmaceuticals Co Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D211/72—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D211/74—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D211/72—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D211/74—Oxygen atoms
    • C07D211/76—Oxygen atoms attached in position 2 or 6
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D211/70—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/45—Non condensed piperidines, e.g. piperocaine having oxo groups directly attached to the heterocyclic ring, e.g. cycloheximide
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
JP2021517766A 2018-09-30 2019-09-30 Ｍｄｍ２阻害剤、その調製方法、医薬組成物および応用 Active JP7338896B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201811160163.0A CN110963958B (zh) 2018-09-30 2018-09-30 一种mdm2抑制剂，及其制备方法、药物组合物和应用
CN201811160163.0 2018-09-30
PCT/CN2019/109428 WO2020064004A1 (zh) 2018-09-30 2019-09-30 一种mdm2抑制剂，及其制备方法、药物组合物和应用

Publications (3)

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JP2022502448A JP2022502448A (ja) 2022-01-11
JP2022502448A5 JP2022502448A5 (https=) 2022-12-06
JP7338896B2 true JP7338896B2 (ja) 2023-09-05

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JP2021517766A Active JP7338896B2 (ja) 2018-09-30 2019-09-30 Ｍｄｍ２阻害剤、その調製方法、医薬組成物および応用

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US (1) US11299460B2 (https=)
EP (1) EP3858812B1 (https=)
JP (1) JP7338896B2 (https=)
KR (1) KR102610545B1 (https=)
CN (2) CN110963958B (https=)
AU (1) AU2019351530B2 (https=)
ES (1) ES3013859T3 (https=)
WO (1) WO2020064004A1 (https=)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114853731B (zh) * 2021-02-04 2026-02-06 上海长森药业有限公司 一种双功能mdm2蛋白降解剂，及其制备方法、药物组合物和应用
WO2023089375A1 (en) * 2021-11-22 2023-05-25 Ligature Therapeutics Pte, Ltd. Therapeutic compounds and methods of use thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013530958A (ja) 2010-06-04 2013-08-01 アムジエン・インコーポレーテツド 癌の治療用ｍｄｍ２阻害剤としてのピペリジノン誘導体
JP2016510028A (ja) 2013-02-28 2016-04-04 アムジエン・インコーポレーテツド 癌の治療のための安息香酸誘導体ｍｄｍ２阻害剤
JP2016528179A (ja) 2013-06-10 2016-09-15 アムジエン・インコーポレーテツド 製造方法及びｍｄｍ２阻害剤の結晶形

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9376425B2 (en) * 2011-09-27 2016-06-28 Amgen, Inc. Heterocyclic compounds as MDM2 inhibitors for the treatment of cancer
BR112016010564A2 (pt) * 2013-11-11 2017-10-10 Amgen Inc terapia de combinação incluindo um inibidor de mdm2 e um ou mais agentes farmaceuticamente ativos para tratamento de cânceres
US10759808B2 (en) * 2016-04-06 2020-09-01 The Regents Of The University Of Michigan Monofunctional intermediates for ligand-dependent target protein degradation
SG11201808728QA (en) * 2016-04-06 2018-11-29 Univ Michigan Regents Mdm2 protein degraders
WO2018092020A1 (en) * 2016-11-15 2018-05-24 Novartis Ag Dose and regimen for hdm2-p53 interaction inhibitors

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013530958A (ja) 2010-06-04 2013-08-01 アムジエン・インコーポレーテツド 癌の治療用ｍｄｍ２阻害剤としてのピペリジノン誘導体
JP2016510028A (ja) 2013-02-28 2016-04-04 アムジエン・インコーポレーテツド 癌の治療のための安息香酸誘導体ｍｄｍ２阻害剤
JP2016528179A (ja) 2013-06-10 2016-09-15 アムジエン・インコーポレーテツド 製造方法及びｍｄｍ２阻害剤の結晶形

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
GONZALEZ, A. Z. et al.，Novel Inhibitors of the MDM2-p53 Interaction Featuring Hydrogen Bond Acceptors as Carboxylic Acid Isosteres，Journal of Medicinal Chemistry，2014年，57(7)，2963-2988
WANG, Y. et al.，Optimization beyond AMG 232: Discovery and SAR of sulfonamides on a piperidinone scaffold as potent inhibitors of the MDM2-p53 protein-protein interaction，Bioorganic & Medicinal Chemistry Letters，2014年，24(16)，3782-3785

Also Published As

Publication number Publication date
AU2019351530A1 (en) 2021-05-27
EP3858812A1 (en) 2021-08-04
US11299460B2 (en) 2022-04-12
AU2019351530B2 (en) 2022-11-17
WO2020064004A1 (zh) 2020-04-02
EP3858812A4 (en) 2022-07-06
EP3858812C0 (en) 2024-12-18
CN110963958B (zh) 2025-10-10
US20220002248A1 (en) 2022-01-06
JP2022502448A (ja) 2022-01-11
CN112867708B (zh) 2023-05-12
CN112867708A (zh) 2021-05-28
KR102610545B1 (ko) 2023-12-05
ES3013859T3 (en) 2025-04-15
EP3858812B1 (en) 2024-12-18
KR20210093870A (ko) 2021-07-28
CN110963958A (zh) 2020-04-07

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