CN114127072B - Prmt5抑制剂及其用途 - Google Patents

Prmt5抑制剂及其用途 Download PDF

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Publication number
CN114127072B
CN114127072B CN202080037608.5A CN202080037608A CN114127072B CN 114127072 B CN114127072 B CN 114127072B CN 202080037608 A CN202080037608 A CN 202080037608A CN 114127072 B CN114127072 B CN 114127072B
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cancer
compound
pharmaceutically acceptable
acceptable salt
alkyl
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Chinese (zh)
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CN114127072A (zh
Inventor
B·M·奥博伊尔
C·M·里夫斯
J·A·希尔夫
B·M·斯托尔茨
M·D·巴特伯格
S·J·维滕贝格
O·C·洛森
M·S·麦克德莫特
N·A·奥布莱恩
D·斯拉蒙
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California Institute of Technology
University of California San Diego UCSD
1200 Pharma LLC
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California Institute of Technology
University of California San Diego UCSD
1200 Pharma LLC
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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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Obesity (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN202080037608.5A 2019-03-25 2020-03-25 Prmt5抑制剂及其用途 Active CN114127072B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201962823374P 2019-03-25 2019-03-25
US62/823,374 2019-03-25
US201962874773P 2019-07-16 2019-07-16
US62/874,773 2019-07-16
PCT/US2020/024654 WO2020198323A1 (en) 2019-03-25 2020-03-25 Prmt5 inhibitors and uses thereof

Publications (2)

Publication Number Publication Date
CN114127072A CN114127072A (zh) 2022-03-01
CN114127072B true CN114127072B (zh) 2024-10-11

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CN202080037608.5A Active CN114127072B (zh) 2019-03-25 2020-03-25 Prmt5抑制剂及其用途

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US (1) US12583859B2 (enExample)
EP (1) EP3947387B1 (enExample)
JP (1) JP7609798B2 (enExample)
KR (1) KR20220023330A (enExample)
CN (1) CN114127072B (enExample)
AU (1) AU2020245480A1 (enExample)
BR (1) BR112021019125A2 (enExample)
CA (1) CA3134779A1 (enExample)
IL (2) IL318073A (enExample)
MX (1) MX2021011524A (enExample)
SG (1) SG11202110272SA (enExample)
WO (1) WO2020198323A1 (enExample)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11077101B1 (en) 2018-07-18 2021-08-03 Tango Therapeutics, Inc. Compounds and methods of use
IL318073A (en) 2019-03-25 2025-02-01 California Inst Of Techn PRMT5 inhibitors and their uses
US12403137B2 (en) 2019-10-28 2025-09-02 Tango Therapeutics, Inc. Compounds and methods of use
WO2022026892A1 (en) 2020-07-31 2022-02-03 Tango Therapeutics, Inc. Piperidin-1- yl-n-pyrydi ne-3-yl-2-oxoacet am ide derivatives useful for the treatment of mtap-deficient and/or mt a-accumulating cancers
CN117157297A (zh) * 2021-07-20 2023-12-01 上海齐鲁制药研究中心有限公司 Prmt5抑制剂
EP4458836A4 (en) * 2021-12-27 2025-05-21 Riken Genesis Co., Ltd. Novel artificial nucleic acid, method for producing same, and use of same

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107278205A (zh) * 2015-02-24 2017-10-20 辉瑞大药厂 用作抗癌药的取代的核苷衍生物
CN107922413A (zh) * 2015-08-26 2018-04-17 詹森药业有限公司 作为prmt5抑制剂的、新颖6‑6二环芳环取代的核苷类似物

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US6143749A (en) 1995-06-07 2000-11-07 Abbott Laboratories Heterocyclic substituted cyclopentane compounds
GB0004297D0 (en) 2000-02-23 2000-04-12 Ucb Sa 2-oxo-1 pyrrolidine derivatives process for preparing them and their uses
US6875751B2 (en) 2000-06-15 2005-04-05 Idenix Pharmaceuticals, Inc. 3′-prodrugs of 2′-deoxy-β-L-nucleosides
US7964580B2 (en) 2007-03-30 2011-06-21 Pharmasset, Inc. Nucleoside phosphoramidate prodrugs
KR102028793B1 (ko) 2013-03-14 2019-10-07 에피자임, 인코포레이티드 아르기닌 메틸기 전이효소 억제제 및 이의 용도
AU2017230658B2 (en) * 2016-03-10 2021-03-04 Janssen Pharmaceutica Nv Substituted nucleoside analogues for use as PRMT5 inhibitors
CA2969295A1 (en) 2016-06-06 2017-12-06 Pfizer Inc. Substituted carbonucleoside derivatives, and use thereof as a prmt5 inhibitor
WO2018065365A1 (en) * 2016-10-03 2018-04-12 Janssen Pharmaceutica Nv Novel monocyclic and bicyclic ring system substituted carbanucleoside analogues for use as prmt5 inhibitors
WO2018160824A1 (en) 2017-03-01 2018-09-07 Prelude Therapeutics, Incorporated Selective inhibitors of protein arginine methyltransferase 5 (prmt5)
EP3939986A1 (en) * 2017-08-09 2022-01-19 Prelude Therapeutics, Incorporated Selective inhibitors of protein arginine methyltransferase 5 (prmt5)
US11059850B2 (en) * 2017-12-08 2021-07-13 Janssen Pharmaceutica Nv Spirobicyclic analogues
IL318073A (en) 2019-03-25 2025-02-01 California Inst Of Techn PRMT5 inhibitors and their uses

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107278205A (zh) * 2015-02-24 2017-10-20 辉瑞大药厂 用作抗癌药的取代的核苷衍生物
CN107922413A (zh) * 2015-08-26 2018-04-17 詹森药业有限公司 作为prmt5抑制剂的、新颖6‑6二环芳环取代的核苷类似物

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EP3947387B1 (en) 2024-10-23
MX2021011524A (es) 2021-12-15
CN114127072A (zh) 2022-03-01
US20220194949A1 (en) 2022-06-23
BR112021019125A2 (pt) 2021-11-30
IL318073A (en) 2025-02-01
JP7609798B2 (ja) 2025-01-07
KR20220023330A (ko) 2022-03-02
EP3947387A4 (en) 2022-11-30
WO2020198323A1 (en) 2020-10-01
SG11202110272SA (en) 2021-10-28
JP2022521818A (ja) 2022-04-12
AU2020245480A1 (en) 2021-11-11
US12583859B2 (en) 2026-03-24
CA3134779A1 (en) 2020-10-01
EP3947387A1 (en) 2022-02-09
IL286622A (en) 2021-12-01

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