TWI879854B - 蛋白質酪胺酸磷酸酶降解劑及其使用方法 - Google Patents

蛋白質酪胺酸磷酸酶降解劑及其使用方法 Download PDF

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TWI879854B
TWI879854B TW109145346A TW109145346A TWI879854B TW I879854 B TWI879854 B TW I879854B TW 109145346 A TW109145346 A TW 109145346A TW 109145346 A TW109145346 A TW 109145346A TW I879854 B TWI879854 B TW I879854B
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group
compound
mmol
pharmaceutically acceptable
acceptable salt
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TW109145346A
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TW202136250A (zh
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格辛 克爾斯汀 法伊茲
馬克 E 菲茨杰拉德
亞歷山大 W 赫德
詹姆士 A 亨德森
阿里特 U 沃拉
瑞姆茲 F 史威斯
麥克 E 高特
克里斯多夫 G 納斯梵斯楚克
馬汀 迪普莱西
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美商嘉來克生命科學有限責任公司
美商艾伯維有限公司
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    • 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
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non 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
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • 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
    • 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
    • C07D471/10Spiro-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
TW109145346A 2019-12-20 2020-12-21 蛋白質酪胺酸磷酸酶降解劑及其使用方法 TWI879854B (zh)

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
US201962952097P 2019-12-20 2019-12-20
US201962952161P 2019-12-20 2019-12-20
US62/952,097 2019-12-20
US62/952,161 2019-12-20
US202063121721P 2020-12-04 2020-12-04
US63/121,721 2020-12-04
US202063125937P 2020-12-15 2020-12-15
US63/125,937 2020-12-15

Publications (2)

Publication Number Publication Date
TW202136250A TW202136250A (zh) 2021-10-01
TWI879854B true TWI879854B (zh) 2025-04-11

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TW109145346A TWI879854B (zh) 2019-12-20 2020-12-21 蛋白質酪胺酸磷酸酶降解劑及其使用方法

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US (1) US20240383886A1 (https=)
EP (1) EP4077319A1 (https=)
JP (1) JP7828893B2 (https=)
CN (1) CN116194453A (https=)
AU (1) AU2020407244A1 (https=)
CA (1) CA3162364A1 (https=)
TW (1) TWI879854B (https=)
UY (1) UY38999A (https=)
WO (1) WO2021127586A1 (https=)

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WO2020210630A1 (en) 2019-04-12 2020-10-15 C4 Therapeutics, Inc. Tricyclic degraders of ikaros and aiolos
EP4073242A4 (en) 2019-12-12 2024-01-03 Kumquat Biosciences Inc. Compositions and methods for potentiating immune activity
US20230167081A1 (en) * 2020-04-30 2023-06-01 President And Fellows Of Harvard College 5-amino-2-piperidinon-3-yl-1-oxoisoindoline derivatives for degradation of ikzf2 degraders
CA3194351A1 (en) * 2020-10-14 2022-04-21 Christopher G. Nasveschuk Tricyclic compounds to degrade neosubstrates for medical therapy
CN116723839A (zh) * 2020-10-14 2023-09-08 C4医药公司 用于降解靶蛋白质的三环杂双官能化合物
MX2023004374A (es) * 2020-10-14 2023-07-06 C4 Therapeutics Inc Ligandos tricíclicos para la degradación de la familia ikaros 2 o la familia ikaros 4.
WO2022161414A1 (zh) * 2021-01-26 2022-08-04 成都茵创园医药科技有限公司 芳香化合物、含其的药物组合物及其应用
TW202309039A (zh) 2021-05-05 2023-03-01 美商百健Ma公司 用於靶向布魯頓氏酪胺酸激酶降解之化合物
EP4359409A1 (en) * 2021-06-21 2024-05-01 Calico Life Sciences LLC Degrader compounds and uses thereof
EP4367113A1 (en) 2021-07-07 2024-05-15 Biogen MA Inc. Compounds for targeting degradation of irak4 proteins
US20250302815A1 (en) * 2021-08-10 2025-10-02 Calico Life Sciences Llc Protein tyrosine phosphatase targeting ligands
WO2023061478A1 (zh) * 2021-10-15 2023-04-20 先声再明医药有限公司 三环类化合物
TW202333670A (zh) * 2022-01-04 2023-09-01 大陸商海思科醫藥集團股份有限公司 抑制並降解irak4的化合物及其藥物组合物和藥學上的應用
PE20250756A1 (es) * 2022-06-06 2025-03-13 Treeline Biosciences Inc Degradadores bifuncionales de bcl6 de quinolona triciclica
PE20252789A1 (es) 2023-05-24 2025-12-22 Kumquat Biosciences Inc Compuestos heterociclicos y usos de estos
KR20260040037A (ko) 2023-07-14 2026-03-23 카톨리에케 유니버시테이트 루벤 암 및 대사 질병의 치료를 위한 신규 화합물
TW202535389A (zh) 2023-10-18 2025-09-16 香港商北嶺健康集團(香港)有限公司 Ptpn2/ptp1b降解劑及其治療方法
CN117343052B (zh) * 2023-12-04 2024-02-06 英矽智能科技(上海)有限公司 蛋白酪氨酸磷酸酶抑制剂及其应用
US12565492B2 (en) 2024-08-09 2026-03-03 Triana Biomedicines, Inc. Anaplastic Lymphoma Kinase (ALK) degraders and uses thereof

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WO2007067612A1 (en) * 2005-12-08 2007-06-14 Novartis Ag 1-orthofluorophenyl substituted 1, 2, 5-thiazolidinedione derivatives as ptp-as inhibitors
WO2007067615A2 (en) * 2005-12-08 2007-06-14 Novartis Ag Thiadiazole derivatives as antidiabetic agents
TW200911769A (en) * 2007-06-04 2009-03-16 Novartis Ag Organic compounds
WO2017197046A1 (en) * 2016-05-10 2017-11-16 C4 Therapeutics, Inc. C3-carbon linked glutarimide degronimers for target protein degradation

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US10689366B2 (en) 2016-11-01 2020-06-23 Cornell University Compounds for MALT1 degredation
CN110769822A (zh) 2017-06-20 2020-02-07 C4医药公司 用于蛋白降解的n/o-连接的降解决定子和降解决定子体
WO2019060742A1 (en) 2017-09-22 2019-03-28 Kymera Therapeutics, Inc AGENTS FOR DEGRADING PROTEINS AND USES THEREOF
IL315310A (en) 2017-12-26 2024-10-01 Kymera Therapeutics Inc Irak degraders and uses thereof

Patent Citations (4)

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WO2007067612A1 (en) * 2005-12-08 2007-06-14 Novartis Ag 1-orthofluorophenyl substituted 1, 2, 5-thiazolidinedione derivatives as ptp-as inhibitors
WO2007067615A2 (en) * 2005-12-08 2007-06-14 Novartis Ag Thiadiazole derivatives as antidiabetic agents
TW200911769A (en) * 2007-06-04 2009-03-16 Novartis Ag Organic compounds
WO2017197046A1 (en) * 2016-05-10 2017-11-16 C4 Therapeutics, Inc. C3-carbon linked glutarimide degronimers for target protein degradation

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AU2020407244A1 (en) 2022-07-28
CA3162364A1 (en) 2021-06-24
UY38999A (es) 2021-07-30
US20240383886A1 (en) 2024-11-21
TW202136250A (zh) 2021-10-01
JP2023508914A (ja) 2023-03-06
CN116194453A (zh) 2023-05-30
JP7828893B2 (ja) 2026-03-12
WO2021127586A1 (en) 2021-06-24
EP4077319A1 (en) 2022-10-26

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