AU2021209744B2 - Novel heterocyclic compounds useful as Aurora A selective inhibitors - Google Patents

Novel heterocyclic compounds useful as Aurora A selective inhibitors Download PDF

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Publication number
AU2021209744B2
AU2021209744B2 AU2021209744A AU2021209744A AU2021209744B2 AU 2021209744 B2 AU2021209744 B2 AU 2021209744B2 AU 2021209744 A AU2021209744 A AU 2021209744A AU 2021209744 A AU2021209744 A AU 2021209744A AU 2021209744 B2 AU2021209744 B2 AU 2021209744B2
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methyl
chloro
carboxylic acid
amino
pyrazol
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AU2021209744A1 (en
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Mingming Chen
Dai Cheng
Amin LI
Haijun Li
Guiqun YANG
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Jacobio Pharmaceuticals Co Ltd
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Jacobio Pharmaceuticals Co Ltd
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    • 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
    • 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
    • C07D401/14—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 three or more hetero 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
    • A61K31/435—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
    • A61K31/4545—Non 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
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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
    • A61K31/5377—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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P35/04—Antineoplastic agents specific for metastasis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/08—Bridged systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2021209744A 2020-01-22 2021-01-22 Novel heterocyclic compounds useful as Aurora A selective inhibitors Active AU2021209744B2 (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
CN2020073786 2020-01-22
CNPCT/CN2020/073786 2020-01-22
CNPCT/CN2020/076159 2020-02-21
CN2020076159 2020-02-21
CN2020085922 2020-04-21
CNPCT/CN2020/085922 2020-04-21
PCT/CN2021/073169 WO2021147974A1 (en) 2020-01-22 2021-01-22 Novel heterocyclic compounds useful as aurora a selective inhibitors

Publications (2)

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AU2021209744A1 AU2021209744A1 (en) 2022-07-07
AU2021209744B2 true AU2021209744B2 (en) 2023-08-31

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AU2021209744A Active AU2021209744B2 (en) 2020-01-22 2021-01-22 Novel heterocyclic compounds useful as Aurora A selective inhibitors

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US (2) US20230128198A1 (enExample)
EP (1) EP4093736A4 (enExample)
JP (1) JP7688646B2 (enExample)
KR (1) KR102828343B1 (enExample)
CN (2) CN114423751B (enExample)
AU (1) AU2021209744B2 (enExample)
CL (1) CL2022001951A1 (enExample)
CO (1) CO2022010878A2 (enExample)
IL (1) IL294247B2 (enExample)
MX (1) MX2022009059A (enExample)
PH (1) PH12022551858A1 (enExample)
TW (1) TWI785474B (enExample)
WO (1) WO2021147974A1 (enExample)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MA53172A (fr) 2018-07-20 2021-05-26 Hoffmann La Roche Composés de sulfonimidamide en tant qu'inhibiteurs de l'activité de l'interleukine 1
CN112239465A (zh) * 2019-07-16 2021-01-19 微境生物医药科技(上海)有限公司 极光激酶抑制剂及其用途
CN112898292A (zh) 2019-12-03 2021-06-04 微境生物医药科技(上海)有限公司 新型极光激酶抑制剂及其用途
BR112022014480A2 (pt) 2020-01-22 2022-09-13 Hoffmann La Roche Compostos, composições farmacêutica, método para tratar um distúrbio em um paciente, usos de um composto e de uma composição farmacêutica e kit
CN118946560A (zh) * 2022-02-23 2024-11-12 修复治疗公司 Polo样激酶4(plk4)抑制剂、药物组合物、其制备方法和用途
CN115057811B (zh) * 2022-05-26 2024-06-14 安庆朗坤药业有限公司 一种2-溴甲基-3,5-二氟吡啶的制备方法
CN115322143B (zh) * 2022-07-21 2023-07-14 安徽德诺医药股份有限公司 一种4-哌啶甲酸叔丁酯盐酸盐的制备方法
WO2024230647A1 (zh) * 2023-05-05 2024-11-14 苏州信诺维医药科技股份有限公司 杂环类化合物、其药物组合物和其应用
CN116903587B (zh) * 2023-06-01 2024-03-22 三峡大学 一种角鲨烯环氧酶抑制剂及其用途

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008026768A1 (en) * 2006-08-31 2008-03-06 Banyu Pharmaceutical Co., Ltd Novel aminopyridine derivatives having aurora a selective inhibitory action
WO2009104802A1 (en) * 2008-02-22 2009-08-27 Banyu Pharmaceutical Co., Ltd. Novel aminopyridine derivatives having aurora a selective inhibitory action
WO2016077161A1 (en) * 2014-11-14 2016-05-19 Eli Lilly And Company Aurora a kinase inhibitor
WO2020112514A1 (en) * 2018-11-30 2020-06-04 Eli Lilly And Company An aurora a kinase inhibitor for use in the treatment of neuroblastoma
WO2021008338A1 (zh) * 2019-07-16 2021-01-21 微境生物医药科技(上海)有限公司 极光激酶抑制剂及其用途
WO2021110009A1 (zh) * 2019-12-03 2021-06-10 微境生物医药科技(上海)有限公司 新型极光激酶抑制剂及其用途

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI485146B (zh) * 2012-02-29 2015-05-21 Taiho Pharmaceutical Co Ltd Novel piperidine compounds or salts thereof

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008026768A1 (en) * 2006-08-31 2008-03-06 Banyu Pharmaceutical Co., Ltd Novel aminopyridine derivatives having aurora a selective inhibitory action
WO2009104802A1 (en) * 2008-02-22 2009-08-27 Banyu Pharmaceutical Co., Ltd. Novel aminopyridine derivatives having aurora a selective inhibitory action
WO2016077161A1 (en) * 2014-11-14 2016-05-19 Eli Lilly And Company Aurora a kinase inhibitor
WO2020112514A1 (en) * 2018-11-30 2020-06-04 Eli Lilly And Company An aurora a kinase inhibitor for use in the treatment of neuroblastoma
WO2021008338A1 (zh) * 2019-07-16 2021-01-21 微境生物医药科技(上海)有限公司 极光激酶抑制剂及其用途
WO2021110009A1 (zh) * 2019-12-03 2021-06-10 微境生物医药科技(上海)有限公司 新型极光激酶抑制剂及其用途

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IL294247B2 (en) 2025-11-01
KR20220131514A (ko) 2022-09-28
WO2021147974A1 (en) 2021-07-29
US20230128198A1 (en) 2023-04-27
IL294247B1 (en) 2025-07-01
MX2022009059A (es) 2022-08-15
EP4093736A4 (en) 2024-01-10
CO2022010878A2 (es) 2022-08-19
TWI785474B (zh) 2022-12-01
KR102828343B1 (ko) 2025-07-04
CA3161268A1 (en) 2021-07-29
CL2022001951A1 (es) 2023-04-14
TW202140449A (zh) 2021-11-01
CN116354936A (zh) 2023-06-30
CN114423751B (zh) 2023-04-21
PH12022551858A1 (en) 2024-01-03
IL294247A (en) 2022-08-01
AU2021209744A1 (en) 2022-07-07
EP4093736A1 (en) 2022-11-30
JP7688646B2 (ja) 2025-06-04
JP2023513419A (ja) 2023-03-31
US11384066B1 (en) 2022-07-12
CN114423751A (zh) 2022-04-29

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