AU2021386149A1 - Tricyclic carboxamide derivatives as prmt5 inhibitors - Google Patents

Tricyclic carboxamide derivatives as prmt5 inhibitors Download PDF

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Publication number
AU2021386149A1
AU2021386149A1 AU2021386149A AU2021386149A AU2021386149A1 AU 2021386149 A1 AU2021386149 A1 AU 2021386149A1 AU 2021386149 A AU2021386149 A AU 2021386149A AU 2021386149 A AU2021386149 A AU 2021386149A AU 2021386149 A1 AU2021386149 A1 AU 2021386149A1
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Prior art keywords
methyl
amino
carboxamide
quinoline
dihydrofuro
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Pending
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AU2021386149A
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AU2021386149A9 (en
Inventor
Albert Amegadzie
Diane Jennifer BEYLKIN
Shon Booker
Matthew Paul Bourbeau
John R. Butler
Sanne Omholt Schroder GLAD
Todd J. Kohn
Brian Alan Lanman
Kexue Li
Qingyian Liu
Patricia Lopez
Francesco Manoni
Primali Vasundera NAVARATNE
Liping H. Pettus
Rene Rahimoff
Nuria A. Tamayo
Mikkel VESTERGAARD
Hui-Ling Wang
Nicholas Anthony WEIRES
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Amgen Inc
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Amgen Inc
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Publication of AU2021386149A1 publication Critical patent/AU2021386149A1/en
Publication of AU2021386149A9 publication Critical patent/AU2021386149A9/en
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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
    • A61K31/435Heterocyclic 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
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K35/00Medicinal preparations containing materials or reaction products thereof with undetermined constitution
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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 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
    • C07D471/12Heterocyclic 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 three hetero rings
    • C07D471/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/12Heterocyclic 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 three hetero rings
    • C07D491/14Ortho-condensed systems
    • C07D491/147Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic 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
    • C07D495/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2021386149A 2020-11-24 2021-11-22 Tricyclic carboxamide derivatives as prmt5 inhibitors Pending AU2021386149A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202063117937P 2020-11-24 2020-11-24
US63/117,937 2020-11-24
PCT/US2021/060332 WO2022115377A1 (en) 2020-11-24 2021-11-22 Tricyclic carboxamide derivatives as prmt5 inhibitors

Publications (2)

Publication Number Publication Date
AU2021386149A1 true AU2021386149A1 (en) 2023-06-22
AU2021386149A9 AU2021386149A9 (en) 2024-08-08

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AU2021386149A Pending AU2021386149A1 (en) 2020-11-24 2021-11-22 Tricyclic carboxamide derivatives as prmt5 inhibitors

Country Status (17)

Country Link
US (1) US20240101570A1 (https=)
EP (1) EP4251624B1 (https=)
JP (1) JP2023550466A (https=)
KR (1) KR20230113339A (https=)
CN (1) CN116783191A (https=)
AU (1) AU2021386149A1 (https=)
CA (1) CA3202141A1 (https=)
CL (1) CL2023001461A1 (https=)
CO (1) CO2023007504A2 (https=)
CR (1) CR20230286A (https=)
ES (1) ES3058979T3 (https=)
IL (1) IL302820B1 (https=)
JO (1) JOP20230113A1 (https=)
MX (1) MX2023006145A (https=)
PE (1) PE20231312A1 (https=)
SA (1) SA523440916B1 (https=)
WO (1) WO2022115377A1 (https=)

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US11077101B1 (en) 2018-07-18 2021-08-03 Tango Therapeutics, Inc. Compounds and methods of use
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
CN116462676A (zh) * 2022-01-20 2023-07-21 上海和誉生物医药科技有限公司 一种多稠环prmt5抑制剂及其制备方法和应用
CN116462677A (zh) * 2022-01-20 2023-07-21 上海和誉生物医药科技有限公司 一种多稠环prmt5抑制剂及其制备方法和应用
US12552760B2 (en) * 2022-04-22 2026-02-17 The Board Of Trustees Of The University Of Illinois Compounds for increasing the nicotinamide adenine dinucleotide in a subject and methods of use thereof
WO2023246873A1 (zh) * 2022-06-23 2023-12-28 南京明德新药研发有限公司 氨基取代的杂芳基衍生物及其应用
EP4549440A4 (en) * 2022-07-01 2026-04-22 Cytosinlab Therapeutics Co Ltd CLASS OF PRMT5 INHIBITORS AND THEIR USES
CN117362304A (zh) * 2022-07-07 2024-01-09 深圳微芯生物科技股份有限公司 一种甲酰胺取代的杂三环类衍生物、其制备方法及其应用
KR20250004026A (ko) * 2022-07-15 2025-01-07 아비스코 테라퓨틱스 컴퍼니 리미티드 Prmt5 억제제, 그 제조 방법과 약학에서의 응용
KR20250002472A (ko) * 2022-08-03 2025-01-07 아비스코 테라퓨틱스 컴퍼니 리미티드 질소 함유 삼중 축합고리 prmt5 억제제 및 이의 제조 방법 및 약학적 용도
WO2024032572A1 (zh) * 2022-08-09 2024-02-15 上海湃隆生物科技有限公司 新型prmt5抑制剂及其应用
AU2023327684A1 (en) 2022-08-15 2025-03-20 Astrazeneca Ab Mta-cooperative prmt5 inhibitors for use in the treatment of cancer
CN118613482B (zh) * 2022-09-26 2025-09-30 上海湃隆生物科技有限公司 新型prmt5抑制剂及其应用
AU2023409398A1 (en) * 2022-12-22 2025-06-05 Gilead Sciences, Inc. Prmt5 inhibitors and uses thereof
CN120418246A (zh) * 2022-12-23 2025-08-01 成都微芯药业有限公司 一类含炔基取代的杂环酰胺衍生物、其制备方法及其应用
CN118103373A (zh) * 2023-01-18 2024-05-28 上海德琪医药科技有限公司 Prmt5抑制化合物和其用途
WO2024170488A1 (en) 2023-02-13 2024-08-22 Astrazeneca Ab Prmt5 inhibitor for use in cancer therapy
TW202438054A (zh) * 2023-03-30 2024-10-01 瑞士商百濟神州瑞士有限責任公司 作為MTA-協同PRMT5抑制劑的5-胺基-6,8-二氫-1H-呋喃并[3,4-d]吡咯并[3,2-b]吡啶-2-甲醯胺衍生物
CR20250446A (es) * 2023-04-21 2025-12-02 Gilead Sciences Inc Inhibidores de prmt5 y usos de los mismos
WO2024234821A1 (zh) * 2023-05-17 2024-11-21 四川科伦博泰生物医药股份有限公司 三并环酰胺化合物、包含其的药物组合物及其制备方法和用途
AU2024275020A1 (en) * 2023-05-24 2025-11-13 Ryvu Therapeutics S.A. Prmt5 inhibitors
TW202513565A (zh) * 2023-06-02 2025-04-01 香港商英矽智能科技知識產權有限公司 Prmt5抑制劑及其用途
WO2025016323A1 (zh) 2023-07-14 2025-01-23 江苏亚虹医药科技股份有限公司 蛋白质精氨酸酶甲基转移酶-5抑制剂及其医药用途
WO2025026381A1 (zh) * 2023-08-02 2025-02-06 成都微芯药业有限公司 杂环炔基取代的酰胺衍生物、其制备方法及其应用
TW202521525A (zh) 2023-08-09 2025-06-01 大陸商江蘇恆瑞醫藥股份有限公司 雜芳基化合物、其製備方法及其在醫藥上的應用
WO2025039979A1 (zh) 2023-08-18 2025-02-27 江苏亚虹医药科技股份有限公司 蛋白质精氨酸酶甲基转移酶-5抑制剂及其医药用途
US11858935B1 (en) 2023-09-06 2024-01-02 King Faisal University Pyrrolo[2,3-c][1,7]naphthyridine-2-carboxylic acid compounds as CK2 inhibitors
US11891394B1 (en) 2023-09-06 2024-02-06 King Faisal University Pyrrolo[2,3-c][1,6]naphthyridine-8-carboxylic acid compounds as CK2 inhibitors
WO2025113705A1 (zh) * 2023-12-01 2025-06-05 上海翰森生物医药科技有限公司 N-取代酰胺类衍生物抑制剂、其制备方法和应用
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WO2025218671A1 (en) * 2024-04-16 2025-10-23 Shanghai Apeiron Therapeutics Company Limited Novel prmt5 proteolysis targeting chimeric molecules and associated methods of use
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KR20230113339A (ko) 2023-07-28
EP4251624B1 (en) 2025-10-29
IL302820B1 (en) 2026-03-01
MX2023006145A (es) 2023-06-06
AU2021386149A9 (en) 2024-08-08
US20240101570A1 (en) 2024-03-28
JP2023550466A (ja) 2023-12-01
IL302820A (en) 2023-07-01
CR20230286A (es) 2023-08-24
PE20231312A1 (es) 2023-08-24
CN116783191A (zh) 2023-09-19
JOP20230113A1 (ar) 2023-05-23
CA3202141A1 (en) 2022-06-02
WO2022115377A1 (en) 2022-06-02
EP4251624A1 (en) 2023-10-04
CO2023007504A2 (es) 2023-09-08
CL2023001461A1 (es) 2023-12-01
ES3058979T3 (en) 2026-03-16
SA523440916B1 (ar) 2025-05-07

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