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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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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    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/428Thiazoles condensed with carbocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62Benzothiazoles
    • C07D277/64Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-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)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (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

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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 (https=)
EP (1) EP3609876B1 (https=)
JP (1) JP7086171B2 (https=)
CN (1) CN110740996B (https=)
AU (1) AU2018251687B2 (https=)
CA (1) CA3059256C (https=)
ES (1) ES2916449T3 (https=)
WO (1) WO2018191199A1 (https=)

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CN109790143A (zh) 2016-05-10 2019-05-21 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
CN109641874A (zh) 2016-05-10 2019-04-16 C4医药公司 用于靶蛋白降解的c3-碳连接的戊二酰亚胺降解决定子体
EP3454862B1 (en) 2016-05-10 2024-09-11 C4 Therapeutics, Inc. Spirocyclic degronimers for target protein degradation
EP4491236A3 (en) 2016-05-10 2025-04-02 C4 Therapeutics, Inc. Heterocyclic degronimers for target protein degradation
EP4717317A2 (en) 2017-06-20 2026-04-01 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
CN118206529A (zh) 2017-09-04 2024-06-18 C4医药公司 二氢苯并咪唑酮
CN111278816B (zh) 2017-09-04 2024-03-15 C4医药公司 二氢喹啉酮
EP3710002A4 (en) 2017-11-16 2021-07-07 C4 Therapeutics, Inc. DEGRADER AND DEGRONE FOR TARGETED PROTEIN DEGRADATION
JP2021519337A (ja) 2018-03-26 2021-08-10 シー4 セラピューティクス, インコーポレイテッド Ikarosの分解のためのセレブロン結合剤
CN119751456A (zh) 2018-04-16 2025-04-04 C4医药公司 螺环化合物
US20220017908A1 (en) * 2018-11-20 2022-01-20 Fulcrum Therapeutics, Inc. Compositions and methods for increasing fetal hemoglobin and treating sickle cell disease
CN120698983A (zh) 2018-12-20 2025-09-26 C4医药公司 靶向蛋白降解
WO2020181232A1 (en) 2019-03-06 2020-09-10 C4 Therapeutics, Inc. Heterocyclic compounds for medical treatment
CA3133751A1 (en) 2019-03-15 2020-09-24 Fulcrum Therapeutics, Inc. Macrocyclic azolopyridine derivatives as eed and prc2 modulators
WO2022125774A1 (en) * 2020-12-10 2022-06-16 Adgero Biopharmaceuticals Holdings, Inc. Methods for treating cutaneous metastatic cancers
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
JP2025523393A (ja) 2022-06-06 2025-07-23 シーフォー セラピューティクス, インコーポレイテッド 二環式置換グルタルイミドセレブロンバインダー
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
WO2025096981A1 (en) 2023-11-03 2025-05-08 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
TW202543650A (zh) 2024-03-08 2025-11-16 美商海爾達醫療運營公司 異雙官能化合物及其在治療疾病中之用途

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)

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

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