CA3095912A1 - Cereblon ligands and bifunctional compounds comprising the same - Google Patents

Cereblon ligands and bifunctional compounds comprising the same Download PDF

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Publication number
CA3095912A1
CA3095912A1 CA3095912A CA3095912A CA3095912A1 CA 3095912 A1 CA3095912 A1 CA 3095912A1 CA 3095912 A CA3095912 A CA 3095912A CA 3095912 A CA3095912 A CA 3095912A CA 3095912 A1 CA3095912 A1 CA 3095912A1
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CA3095912A
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English (en)
French (fr)
Inventor
Andrew P. Crew
Craig M. Crews
Hanqing Dong
Keith R. Hornberger
Jing Wang
Yimin Qian
Kurt Zimmermann
Michael Berlin
Lawrence B. Snyder
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Arvinas Operations Inc
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Arvinas Operations Inc
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Priority claimed from US15/953,108 external-priority patent/US20180228907A1/en
Application filed by Arvinas Operations Inc filed Critical Arvinas Operations Inc
Publication of CA3095912A1 publication Critical patent/CA3095912A1/en
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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
    • C07D401/14—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
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    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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    • A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
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    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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    • 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
    • C07D471/04—Ortho-condensed systems
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    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
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    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12—Heterocyclic 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 three hetero rings
    • C07D495/14—Ortho-condensed systems
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic 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 three hetero rings
    • C07D498/14—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
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  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
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  • Diabetes (AREA)
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  • Endocrinology (AREA)
  • Hematology (AREA)
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  • Reproductive Health (AREA)
  • Heart & Thoracic Surgery (AREA)
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  • Obesity (AREA)
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CA3095912A 2018-04-13 2019-04-09 Cereblon ligands and bifunctional compounds comprising the same Pending CA3095912A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US15/953,108 US20180228907A1 (en) 2014-04-14 2018-04-13 Cereblon ligands and bifunctional compounds comprising the same
US15/953,108 2018-04-13
PCT/US2019/026570 WO2019199816A1 (en) 2018-04-13 2019-04-09 Cereblon ligands and bifunctional compounds comprising the same

Publications (1)

Publication Number Publication Date
CA3095912A1 true CA3095912A1 (en) 2019-10-17

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Application Number Title Priority Date Filing Date
CA3095912A Pending CA3095912A1 (en) 2018-04-13 2019-04-09 Cereblon ligands and bifunctional compounds comprising the same

Country Status (9)

Country Link
EP (1) EP3774772A1 (https=)
JP (3) JP2021521192A (https=)
KR (1) KR20210003804A (https=)
CN (2) CN112262134B (https=)
AU (3) AU2019251223A1 (https=)
CA (1) CA3095912A1 (https=)
IL (3) IL302595A (https=)
MX (2) MX2020010571A (https=)
WO (1) WO2019199816A1 (https=)

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US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
MX2019005007A (es) 2016-11-01 2019-07-18 Arvinas Inc Protac dirigidos a la proteína tau y métodos asociados de uso.
CN110769822A (zh) 2017-06-20 2020-02-07 C4医药公司 用于蛋白降解的n/o-连接的降解决定子和降解决定子体
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
EP3773576A4 (en) 2018-03-26 2021-12-29 C4 Therapeutics, Inc. Cereblon binders for the degradation of ikaros
EP3781156A4 (en) 2018-04-16 2022-05-18 C4 Therapeutics, Inc. SPIROCYCLIC COMPOUNDS
CA3099155A1 (en) 2018-05-14 2019-11-21 Nuvation Bio Inc. Anti-cancer nuclear hormone receptor-targeting compounds
EP3807272A1 (en) 2018-06-13 2021-04-21 Amphista Therapeutics Ltd Bifunctional molecules for targeting rpn11
CN120698983A (zh) 2018-12-20 2025-09-26 C4医药公司 靶向蛋白降解
US12186401B2 (en) 2019-03-01 2025-01-07 Ontario Institute for Cancer Research (OICR) and Sinai Health System Amide-based proteolysis modulators of B-rapidly accelerated fibrosarcoma (BRAF) and associated uses
WO2020210630A1 (en) 2019-04-12 2020-10-15 C4 Therapeutics, Inc. Tricyclic degraders of ikaros and aiolos
CA3138197A1 (en) 2019-05-14 2020-11-19 Nuvation Bio Inc. Anti-cancer nuclear hormone receptor-targeting compounds
US11890346B2 (en) * 2019-06-12 2024-02-06 Northwestern University Proteolysis-targeting chimeric molecules (PROTACs) that induce degradation of c-MYC protein
EP3999182A1 (en) 2019-07-17 2022-05-25 Arvinas Operations, Inc. Tau-protein targeting compounds and associated methods of use
KR20220054347A (ko) * 2019-08-26 2022-05-02 아비나스 오퍼레이션스, 인코포레이티드 에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 유도체로 유방암을 치료하는 방법
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