CN110740996B - 共价小分子dcn1抑制剂和使用其的治疗方法 - Google Patents

共价小分子dcn1抑制剂和使用其的治疗方法 Download PDF

Info

Publication number
CN110740996B
CN110740996B CN201880038225.2A CN201880038225A CN110740996B CN 110740996 B CN110740996 B CN 110740996B CN 201880038225 A CN201880038225 A CN 201880038225A CN 110740996 B CN110740996 B CN 110740996B
Authority
CN
China
Prior art keywords
alkyl
substituted
cycloalkyl
compound
dcn1
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
CN201880038225.2A
Other languages
English (en)
Chinese (zh)
Other versions
CN110740996A (zh
Inventor
王绍梦
珍妮·斯塔基
刘柳
陆剑锋
周海彬
芮良祐
孙毅
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
University of Michigan System
Original Assignee
University of Michigan System
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by University of Michigan System filed Critical University of Michigan System
Publication of CN110740996A publication Critical patent/CN110740996A/zh
Application granted granted Critical
Publication of CN110740996B publication Critical patent/CN110740996B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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

Landscapes

  • 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)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN201880038225.2A 2017-04-10 2018-04-10 共价小分子dcn1抑制剂和使用其的治疗方法 Active CN110740996B (zh)

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
CN110740996A CN110740996A (zh) 2020-01-31
CN110740996B true CN110740996B (zh) 2024-01-09

Family

ID=62067873

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201880038225.2A Active CN110740996B (zh) 2017-04-10 2018-04-10 共价小分子dcn1抑制剂和使用其的治疗方法

Country Status (8)

Country Link
US (1) US10500194B2 (cg-RX-API-DMAC7.html)
EP (1) EP3609876B1 (cg-RX-API-DMAC7.html)
JP (1) JP7086171B2 (cg-RX-API-DMAC7.html)
CN (1) CN110740996B (cg-RX-API-DMAC7.html)
AU (1) AU2018251687B2 (cg-RX-API-DMAC7.html)
CA (1) CA3059256C (cg-RX-API-DMAC7.html)
ES (1) ES2916449T3 (cg-RX-API-DMAC7.html)
WO (1) WO2018191199A1 (cg-RX-API-DMAC7.html)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4491236A3 (en) 2016-05-10 2025-04-02 C4 Therapeutics, Inc. Heterocyclic degronimers for target protein degradation
EP3455219A4 (en) 2016-05-10 2019-12-18 C4 Therapeutics, Inc. AMINE-RELATED C3-GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION
ES2990061T3 (es) 2016-05-10 2024-11-28 C4 Therapeutics Inc Degronímeros espirocíclicos para la degradación de proteínas diana
EP3455218A4 (en) 2016-05-10 2019-12-18 C4 Therapeutics, Inc. C3 CARBON-BASED GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION
EP3641762A4 (en) 2017-06-20 2021-03-10 C4 Therapeutics, Inc. N / O-LINKED DEGRONES AND DEGRONIMERS FOR PROTEIN DEGRADATION
WO2019043214A1 (en) 2017-09-04 2019-03-07 F. Hoffmann-La Roche Ag glutarimide
CN111278816B (zh) 2017-09-04 2024-03-15 C4医药公司 二氢喹啉酮
CN111315735B (zh) 2017-09-04 2024-03-08 C4医药公司 二氢苯并咪唑酮
CN111372585A (zh) 2017-11-16 2020-07-03 C4医药公司 用于靶蛋白降解的降解剂和降解决定子
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
EP3883597A2 (en) * 2018-11-20 2021-09-29 Fulcrum Therapeutics, Inc. Compositions and methods for increasing fetal hemoglobin and treating sickle cell disease
WO2020132561A1 (en) 2018-12-20 2020-06-25 C4 Therapeutics, Inc. Targeted protein degradation
EP3938050A1 (en) 2019-03-15 2022-01-19 Fulcrum Therapeutics, Inc. Macrocyclic azolopyridine derivatives as eed and prc2 modulators
AU2021397774A1 (en) * 2020-12-10 2023-06-29 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
AU2023283735A1 (en) 2022-06-06 2024-10-31 C4 Therapeutics, Inc. Bicyclic-substituted glutarimide cereblon binders
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
WO2025096956A1 (en) 2023-11-03 2025-05-08 Cellarity, Inc. Dcn-1 modulating compounds and methods of use thereof
WO2025096981A1 (en) 2023-11-03 2025-05-08 Cellarity, Inc. Modulators of dcn-1 and methods of use thereof

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1049165A (zh) * 1989-06-29 1991-02-13 沃纳-兰伯特公司 N-取代的环烷基和多环烷基α-取代的色氨酸-苯丙氨酸-和苯乙胺衍生物
WO2017049295A1 (en) * 2015-09-18 2017-03-23 St. Jude Children's Research Hospital Methods and compositions of inhibiting dcn1-ubc12 interaction

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1049165A (zh) * 1989-06-29 1991-02-13 沃纳-兰伯特公司 N-取代的环烷基和多环烷基α-取代的色氨酸-苯丙氨酸-和苯乙胺衍生物
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
A potent small-molecule inhibitor of the DCN1-UBC12 interaction that selectively blocks cullin 3 neddylation;Haibin Zhou et al.;《NATURE COMMUNICATIONS》;20171027;第8卷(第1期);第1-12页 *

Also Published As

Publication number Publication date
ES2916449T3 (es) 2022-07-01
US10500194B2 (en) 2019-12-10
CA3059256A1 (en) 2018-10-18
US20180289677A1 (en) 2018-10-11
JP7086171B2 (ja) 2022-06-17
EP3609876B1 (en) 2022-03-30
JP2020516679A (ja) 2020-06-11
CA3059256C (en) 2024-04-16
CN110740996A (zh) 2020-01-31
AU2018251687A1 (en) 2019-10-24
EP3609876A1 (en) 2020-02-19
WO2018191199A1 (en) 2018-10-18
AU2018251687B2 (en) 2021-07-29

Similar Documents

Publication Publication Date Title
CN110740996B (zh) 共价小分子dcn1抑制剂和使用其的治疗方法
US12012467B2 (en) Small molecule DCN1 inhibitors and therapeutic methods using the same
JP6873980B2 (ja) LRRK2阻害薬としての新規のイミダゾ[4,5−c]キノリンおよびイミダゾ[4,5−c][1,5]ナフチリジン誘導体
EP2888265B1 (en) Bivalent inhibitors of iap proteins and therapeutic methods using the same
JP5642777B2 (ja) Iap阻害剤
CA3033239A1 (en) Spiro bicyclic inhibitors of menin-mll interaction
CN110291084A (zh) 用于治疗癌症的组合物和方法
MXPA06014969A (es) Inhibidores de iap.
KR20190045242A (ko) 메닌-mll 상호작용의 스피로 바이사이클릭 억제제
TW200412966A (en) Novel pyrazolopyrimidines as cyclin dependent kinase inhibitors
CN102458115B (zh) Iap抑制剂
EP1899346B1 (en) Pyrrolotriazine compounds useful as kinase inhibitors
EP2651949B1 (en) Substituted pyrimido[1,2-b]indazoles and their use as modulators of the pi3k/akt pathway
CA3119882A1 (en) Heterocyclic spiro-compounds as am2 receptor inhibitors
EP1899345B1 (en) Pyrrolotriazine compounds useful as kinase inhibitors
WO2025255442A1 (en) Trim21-targeted compounds and uses thereof
JP2025508328A (ja) 抗体にコンジュゲートした化学的分解誘導物質とその方法
HK40005133A (en) Bivalent inhibitors of iap proteins and therapeutic methods using the same
HK40006375A (en) Bivalent inhibitors of iap proteins and therapeutic methods using the same
HK40013658A (en) Compositions and methods for treating cancer

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant