AU2018251687B2 - Covalent small molecule DCN1 inhibitors and therapeutic methods using the same - Google Patents

Covalent small molecule DCN1 inhibitors and therapeutic methods using the same Download PDF

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Publication number
AU2018251687B2
AU2018251687B2 AU2018251687A AU2018251687A AU2018251687B2 AU 2018251687 B2 AU2018251687 B2 AU 2018251687B2 AU 2018251687 A AU2018251687 A AU 2018251687A AU 2018251687 A AU2018251687 A AU 2018251687A AU 2018251687 B2 AU2018251687 B2 AU 2018251687B2
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alkyl
substituted
cycloalkyl
compound
disease
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AU2018251687A
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AU2018251687A1 (en
Inventor
Liu Liu
Jianfeng Lu
Liangyou Rui
Jeanne STUCKEY
Yi Sun
Shaomeng Wang
Haibin Zhou
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University of Michigan (System)
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University of Michigan (System)
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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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/428—Thiazoles condensed with carbocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/64—Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/495—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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines 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

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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)
  • Gastroenterology & Hepatology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
AU2018251687A 2017-04-10 2018-04-10 Covalent small molecule DCN1 inhibitors and therapeutic methods using the same Active AU2018251687B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762483640P 2017-04-10 2017-04-10
US62/483,640 2017-04-10
PCT/US2018/026789 WO2018191199A1 (en) 2017-04-10 2018-04-10 Covalent small molecule dcn1 inhibitors and therapeutic methods using the same

Publications (2)

Publication Number Publication Date
AU2018251687A1 AU2018251687A1 (en) 2019-10-24
AU2018251687B2 true AU2018251687B2 (en) 2021-07-29

Family

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AU2018251687A Active AU2018251687B2 (en) 2017-04-10 2018-04-10 Covalent small molecule DCN1 inhibitors and therapeutic methods using the same

Country Status (8)

Country Link
US (1) US10500194B2 (cg-RX-API-DMAC10.html)
EP (1) EP3609876B1 (cg-RX-API-DMAC10.html)
JP (1) JP7086171B2 (cg-RX-API-DMAC10.html)
CN (1) CN110740996B (cg-RX-API-DMAC10.html)
AU (1) AU2018251687B2 (cg-RX-API-DMAC10.html)
CA (1) CA3059256C (cg-RX-API-DMAC10.html)
ES (1) ES2916449T3 (cg-RX-API-DMAC10.html)
WO (1) WO2018191199A1 (cg-RX-API-DMAC10.html)

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WO2017197046A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. C3-carbon linked glutarimide degronimers for target protein degradation
CN121974842A (zh) 2016-05-10 2026-05-05 C4医药公司 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体
CN109562107A (zh) 2016-05-10 2019-04-02 C4医药公司 用于靶蛋白降解的杂环降解决定子体
CN109562113A (zh) 2016-05-10 2019-04-02 C4医药公司 用于靶蛋白降解的螺环降解决定子体
EP4717317A3 (en) 2017-06-20 2026-06-03 C4 Therapeutics, Inc. N/o-linked degrons and degronimers for protein degradation
CN118108706A (zh) 2017-09-04 2024-05-31 C4医药公司 戊二酰亚胺
WO2019043208A1 (en) 2017-09-04 2019-03-07 F. Hoffmann-La Roche Ag DIHYDROQUINOLINONES
WO2019043217A1 (en) 2017-09-04 2019-03-07 F. Hoffmann-La Roche Ag DIHYDROBENZIMIDAZOLONES
EP3710002A4 (en) 2017-11-16 2021-07-07 C4 Therapeutics, Inc. DEGRADER AND DEGRONE FOR TARGETED PROTEIN DEGRADATION
CN111902141A (zh) 2018-03-26 2020-11-06 C4医药公司 用于ikaros降解的羟脑苷脂结合剂
WO2019204354A1 (en) 2018-04-16 2019-10-24 C4 Therapeutics, Inc. Spirocyclic compounds
CA3119781A1 (en) * 2018-11-20 2020-05-28 Fulcrum Therapeutics, Inc. Compositions and methods for increasing fetal hemoglobin and treating sickle cell disease
EP3897631A4 (en) 2018-12-20 2022-11-23 C4 Therapeutics, Inc. TARGETED PROTEIN BREAKDOWN
ES2995214T3 (en) 2019-03-06 2025-02-07 C4 Therapeutics Inc Heterocyclic compounds for medical treatment
IL323757A (en) 2019-03-15 2025-12-01 Fulcrum Therapeutics Inc Macrocyclic azolopyridine derivatives as eed and prc2 modulators
EP4259132A4 (en) * 2020-12-10 2025-01-15 Adgero Biopharmaceuticals Holdings, Inc. METHODS OF TREATMENT OF METASTATIC SKIN CANCER
CN112830957B (zh) * 2021-01-07 2022-07-22 江西师范大学 一种制备卡非佐米的方法
WO2023059605A1 (en) * 2021-10-04 2023-04-13 Halda Therapeutics Opco, Inc. Heterobifunctional compounds and their use in treating disease
WO2023059582A1 (en) * 2021-10-04 2023-04-13 Halda Therapeutics Opco, Inc. Heterobifunctional compounds and their use in treating disease
IL316803A (en) 2022-06-06 2025-01-01 C4 Therapeutics Inc Bicyclic glutarimide-modified cervalon-binding agents
CN116987062A (zh) * 2023-08-03 2023-11-03 中国热带农业科学院分析测试中心 一种氨基酸键联槟榔碱衍生物的制备方法
WO2025085738A1 (en) 2023-10-18 2025-04-24 Halda Therapeutics Opco, Inc. Heterobifunctional compounds and methods of treating disease
US12435087B2 (en) 2023-11-03 2025-10-07 Cellarity, Inc. Modulators of DCN-1 and methods of use thereof
US12473285B2 (en) 2023-11-03 2025-11-18 Cellarity, Inc. DCN-1 modulating compounds and methods of use thereof
WO2025189056A1 (en) 2024-03-08 2025-09-12 Halda Therapeutics Opco, Inc. Heterobifunctional compounds and their use in treating disease

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017049295A1 (en) * 2015-09-18 2017-03-23 St. Jude Children's Research Hospital Methods and compositions of inhibiting dcn1-ubc12 interaction

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ234264A (en) * 1989-06-29 1993-05-26 Warner Lambert Co N-substituted cycloalkyl and polycycloalkyl alpha-substituted trp-phe- and phenethylamine derivatives, and pharmaceutical compositions

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017049295A1 (en) * 2015-09-18 2017-03-23 St. Jude Children's Research Hospital Methods and compositions of inhibiting dcn1-ubc12 interaction

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Zhou et al. Structure-based design of highly potent small-molecule inhibitors of DCN1-UBC12 protein-protein interaction, Oral presentation, Apr. 6, 2017, 253rd ACS National Meeting, Medicinal Chemistry Division, Abstract MEDI 377. *

Also Published As

Publication number Publication date
CN110740996A (zh) 2020-01-31
AU2018251687A1 (en) 2019-10-24
CN110740996B (zh) 2024-01-09
US20180289677A1 (en) 2018-10-11
ES2916449T3 (es) 2022-07-01
WO2018191199A1 (en) 2018-10-18
JP7086171B2 (ja) 2022-06-17
JP2020516679A (ja) 2020-06-11
US10500194B2 (en) 2019-12-10
CA3059256A1 (en) 2018-10-18
CA3059256C (en) 2024-04-16
EP3609876A1 (en) 2020-02-19
EP3609876B1 (en) 2022-03-30

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