IL281188A - Polycyclic compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides - Google Patents
Polycyclic compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptidesInfo
- Publication number
- IL281188A IL281188A IL281188A IL28118821A IL281188A IL 281188 A IL281188 A IL 281188A IL 281188 A IL281188 A IL 281188A IL 28118821 A IL28118821 A IL 28118821A IL 281188 A IL281188 A IL 281188A
- Authority
- IL
- Israel
- Prior art keywords
- polypeptides
- methods
- polycyclic compounds
- rapidly accelerated
- targeted degradation
- Prior art date
Links
- 201000008808 Fibrosarcoma Diseases 0.000 title 1
- 230000015556 catabolic process Effects 0.000 title 1
- 238000006731 degradation reaction Methods 0.000 title 1
- 238000000034 method Methods 0.000 title 1
- 125000003367 polycyclic group Chemical group 0.000 title 1
- 229920001184 polypeptide Polymers 0.000 title 1
- 102000004196 processed proteins & peptides Human genes 0.000 title 1
- 108090000765 processed proteins & peptides Proteins 0.000 title 1
Classifications
-
- 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
- C07D471/04—Ortho-condensed systems
-
- 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
- A61K31/4427—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
-
- 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
-
- 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
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/55—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
-
- 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
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06139—Dipeptides with the first amino acid being heterocyclic
- C07K5/06165—Dipeptides with the first amino acid being heterocyclic and Pro-amino acid; Derivatives thereof
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862728581P | 2018-09-07 | 2018-09-07 | |
| PCT/US2019/050114 WO2020051564A1 (en) | 2018-09-07 | 2019-09-07 | Polycyclic compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| IL281188A true IL281188A (en) | 2021-04-29 |
Family
ID=68051923
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL281188A IL281188A (en) | 2018-09-07 | 2021-03-02 | Polycyclic compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides |
Country Status (9)
| Country | Link |
|---|---|
| EP (1) | EP3846907A1 (en) |
| JP (2) | JP2022500368A (en) |
| KR (2) | KR102642203B1 (en) |
| CN (1) | CN113164775A (en) |
| AU (2) | AU2019335516B2 (en) |
| CA (1) | CA3109981A1 (en) |
| IL (1) | IL281188A (en) |
| MX (1) | MX2021002559A (en) |
| WO (1) | WO2020051564A1 (en) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019099868A2 (en) | 2017-11-16 | 2019-05-23 | C4 Therapeutics, Inc. | Degraders and degrons for targeted protein degradation |
| JP2021519337A (en) | 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 | Cereblon binder for the degradation of Ikaras |
| WO2019204354A1 (en) | 2018-04-16 | 2019-10-24 | C4 Therapeutics, Inc. | Spirocyclic compounds |
| CA3162266A1 (en) * | 2019-12-17 | 2021-06-24 | Nikolai Kley | Bifunctional agents for protein recruitment and/or degradation |
| CN115298173A (en) * | 2020-03-31 | 2022-11-04 | 田边三菱制药株式会社 | Hydroxypyrrolidine derivatives and medical use thereof |
| CN115996719A (en) | 2020-06-19 | 2023-04-21 | C4医药公司 | BRAF degradation agent |
| WO2021255213A1 (en) * | 2020-06-19 | 2021-12-23 | F. Hoffmann-La Roche Ag | Heterobifunctional compounds as degraders of braf |
| JP2023539663A (en) * | 2020-08-28 | 2023-09-15 | アルビナス・オペレーションズ・インコーポレイテッド | Rapidly Progressive Fibrosarcoma Proteolytic Compounds and Related Methods of Use |
| JP2024504932A (en) | 2021-01-13 | 2024-02-02 | モンテ ローザ セラピューティクス， インコーポレイテッド | isoindolinone compound |
| WO2022266206A1 (en) * | 2021-06-16 | 2022-12-22 | Erasca, Inc. | Kras inhibitor conjugates |
| WO2022270994A1 (en) | 2021-06-25 | 2022-12-29 | 한국화학연구원 | Novel bifunctional heterocyclic compound having btk degradation function via ubiquitin proteasome pathway, and use thereof |
| WO2023023941A1 (en) * | 2021-08-24 | 2023-03-02 | Biofront Ltd (Cayman) | Hpk1 degraders, compositions comprising the hpki degrader, and methods of using the same |
| CA3235512A1 (en) * | 2021-10-22 | 2023-04-27 | Xiaobao Yang | Crbn e3 ligase ligand compound, protein degrader developed based thereon and their applications |
| TW202330548A (en) * | 2021-11-30 | 2023-08-01 | 英屬開曼群島商百濟神州有限公司 | Compounds for the degradation of egfr kinase |
| CN115894450B (en) * | 2021-11-30 | 2023-09-12 | 山东如至生物医药科技有限公司 | Novel polycyclic compound and composition and application thereof |
| WO2024054591A1 (en) | 2022-09-07 | 2024-03-14 | Arvinas Operations, Inc. | Rapidly accelerated fibrosarcoma (raf) degrading compounds and associated methods of use |
| CN115806503A (en) * | 2022-12-02 | 2023-03-17 | 中国海洋大学 | Selective histone deacetylase inhibitor as well as preparation method and application thereof |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2005206929B2 (en) | 2004-01-16 | 2008-01-24 | The Regents Of The University Of Michigan | Conformationally constrained Smac mimetics and the uses thereof |
| CA2558615C (en) | 2004-03-23 | 2013-10-29 | Genentech, Inc. | Azabicyclo-octane inhibitors of iap |
| DK2253614T3 (en) | 2004-04-07 | 2013-01-07 | Novartis Ag | IAP inhibitors |
| CN101035802A (en) | 2004-07-02 | 2007-09-12 | 健泰科生物技术公司 | Inhibitors of IAP |
| EP1836201B2 (en) | 2004-12-20 | 2013-09-04 | Genentech, Inc. | Pyrrolidine inhibitors of iap |
| WO2007101347A1 (en) | 2006-03-07 | 2007-09-13 | Aegera Therapeutics Inc. | Bir domain binding compounds |
| WO2008014236A1 (en) | 2006-07-24 | 2008-01-31 | Tetralogic Pharmaceuticals Corporation | Dimeric iap inhibitors |
| NZ580468A (en) | 2007-04-13 | 2012-02-24 | Univ Michigan | Diazo bicyclic smac mimetics and the uses thereof |
| US9500653B2 (en) | 2010-12-07 | 2016-11-22 | Yale University | Small-molecule hydrophobic tagging of fusion proteins and induced degradation of same |
| WO2013071039A1 (en) | 2011-11-09 | 2013-05-16 | Ensemble Therapeutics | Macrocyclic compounds for inhibition of inhibitors of apoptosis |
| CN117736134A (en) | 2012-01-12 | 2024-03-22 | 耶鲁大学 | Compounds and methods for enhancing degradation of target proteins and other polypeptides by E3 ubiquitin ligases |
| US9603889B2 (en) | 2012-10-02 | 2017-03-28 | Bristol-Myers Squibb Company | IAP antagonists |
| WO2015006524A1 (en) | 2013-07-12 | 2015-01-15 | Bristol-Myers Squibb Company | Iap antagonists |
| KR20210132233A (en) * | 2014-04-14 | 2021-11-03 | 아비나스 오퍼레이션스, 인코포레이티드 | Imide-based modulators of proteolysis and associated methods of use |
| US20160058872A1 (en) | 2014-04-14 | 2016-03-03 | Arvinas, Inc. | Imide-based modulators of proteolysis and associated methods of use |
| GB201504314D0 (en) * | 2015-03-13 | 2015-04-29 | Univ Dundee | Small molecules |
| BR112017019751A2 (en) * | 2015-03-18 | 2018-05-29 | Arvinas Inc | bifunctional compound, pharmaceutical composition, and methods for treating or preventing a disease or disorder, and for degrading a target protein in a cell |
| EP3544957A4 (en) * | 2016-11-22 | 2020-09-02 | Dana-Farber Cancer Institute, Inc. | Degradation of protein kinases by conjugation of protein kinase inhibitors with e3 ligase ligand and methods of use |
| MX2019007649A (en) * | 2016-12-23 | 2019-09-10 | Arvinas Operations Inc | Compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides. |
-
2019
- 2019-09-07 KR KR1020217009937A patent/KR102642203B1/en active IP Right Grant
- 2019-09-07 CA CA3109981A patent/CA3109981A1/en active Pending
- 2019-09-07 WO PCT/US2019/050114 patent/WO2020051564A1/en unknown
- 2019-09-07 CN CN201980073600.1A patent/CN113164775A/en active Pending
- 2019-09-07 AU AU2019335516A patent/AU2019335516B2/en active Active
- 2019-09-07 EP EP19773614.3A patent/EP3846907A1/en active Pending
- 2019-09-07 MX MX2021002559A patent/MX2021002559A/en unknown
- 2019-09-07 JP JP2021512854A patent/JP2022500368A/en active Pending
- 2019-09-07 KR KR1020247005115A patent/KR20240028539A/en active Application Filing
-
2021
- 2021-03-02 IL IL281188A patent/IL281188A/en unknown
-
2022
- 2022-09-08 AU AU2022228150A patent/AU2022228150A1/en active Pending
-
2023
- 2023-08-03 JP JP2023127233A patent/JP2023159166A/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| EP3846907A1 (en) | 2021-07-14 |
| KR102642203B1 (en) | 2024-03-04 |
| CN113164775A (en) | 2021-07-23 |
| AU2019335516A1 (en) | 2021-03-11 |
| CA3109981A1 (en) | 2020-03-12 |
| KR20240028539A (en) | 2024-03-05 |
| AU2022228150A1 (en) | 2022-09-29 |
| WO2020051564A1 (en) | 2020-03-12 |
| JP2022500368A (en) | 2022-01-04 |
| JP2023159166A (en) | 2023-10-31 |
| MX2021002559A (en) | 2021-07-21 |
| AU2019335516B2 (en) | 2022-06-16 |
| KR20210073519A (en) | 2021-06-18 |
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