SG11202105256QA - Novel compounds having estrogen receptor alpha degradation activity and uses thereof - Google Patents
Novel compounds having estrogen receptor alpha degradation activity and uses thereofInfo
- Publication number
- SG11202105256QA SG11202105256QA SG11202105256QA SG11202105256QA SG11202105256QA SG 11202105256Q A SG11202105256Q A SG 11202105256QA SG 11202105256Q A SG11202105256Q A SG 11202105256QA SG 11202105256Q A SG11202105256Q A SG 11202105256QA SG 11202105256Q A SG11202105256Q A SG 11202105256QA
- Authority
- SG
- Singapore
- Prior art keywords
- novel compounds
- estrogen receptor
- receptor alpha
- degradation activity
- alpha degradation
- Prior art date
Links
- 108010007005 Estrogen Receptor alpha Proteins 0.000 title 1
- 102100038595 Estrogen receptor Human genes 0.000 title 1
- 230000015556 catabolic process Effects 0.000 title 1
- 150000001875 compounds Chemical class 0.000 title 1
- 238000006731 degradation reaction Methods 0.000 title 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D211/30—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom
- C07D211/32—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom by oxygen atoms
-
- 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
- C07D401/02—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
-
- 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
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C303/00—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
- C07C303/26—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of esters of sulfonic acids
- C07C303/28—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of esters of sulfonic acids by reaction of hydroxy compounds with sulfonic acids or derivatives thereof
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
- C07C309/63—Esters of sulfonic acids
- C07C309/64—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms
- C07C309/65—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms of a saturated carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
- C07D295/084—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
- C07D295/088—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
- C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D309/10—Oxygen atoms
-
- 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
- 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
-
- 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
- C07D471/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
- C07D487/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
- C07D498/02—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 two hetero rings
- C07D498/10—Spiro-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Indole Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862770476P | 2018-11-21 | 2018-11-21 | |
| PCT/US2019/062564 WO2020106933A1 (en) | 2018-11-21 | 2019-11-21 | Novel compounds having estrogen receptor alpha degradation activity and uses thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SG11202105256QA true SG11202105256QA (en) | 2021-06-29 |
Family
ID=68653428
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG11202105256QA SG11202105256QA (en) | 2018-11-21 | 2019-11-21 | Novel compounds having estrogen receptor alpha degradation activity and uses thereof |
Country Status (7)
| Country | Link |
|---|---|
| US (2) | US10696659B2 (en) |
| EP (1) | EP3675839B1 (en) |
| CN (2) | CN113164409B (en) |
| AU (1) | AU2019384807A1 (en) |
| CA (1) | CA3120530A1 (en) |
| SG (1) | SG11202105256QA (en) |
| WO (1) | WO2020106933A1 (en) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2020064002A1 (en) * | 2018-09-30 | 2020-04-02 | 中国科学院上海药物研究所 | Isoindoline compound, preparation method, pharmaceutical composition and use thereof |
| CA3161892A1 (en) | 2019-12-23 | 2021-07-01 | Jie Fan | Combinations of estrogen receptor degraders and cyclin-dependent kinase inhibitors for treating cancer |
| US11351149B2 (en) | 2020-09-03 | 2022-06-07 | Pfizer Inc. | Nitrile-containing antiviral compounds |
| US20240058318A1 (en) * | 2020-12-10 | 2024-02-22 | Mayo Foundation For Medical Education And Research | Degrading pkcb1 to treat cancer |
| WO2022217010A1 (en) * | 2021-04-09 | 2022-10-13 | Endotarget Inc. | Compounds and methods for the targeted degradation of estrogen receptors |
| WO2022245124A1 (en) | 2021-05-18 | 2022-11-24 | 재단법인 대구경북첨단의료산업진흥재단 | Novel ethene compound and pharmaceutical composition including same as active ingredient for prevention or treatment of cancer |
| KR102503296B1 (en) | 2021-05-18 | 2023-02-24 | 재단법인 대구경북첨단의료산업진흥재단 | Novel ethene compounds and pharmaceutical composition for preventing or treating cancer comprising the same as an active ingredient |
| IL309666A (en) | 2021-07-09 | 2024-02-01 | Plexium Inc | Aryl compounds and pharmaceutical compositions that modulate ikzf2 |
| KR20240053589A (en) * | 2021-07-30 | 2024-04-24 | 하이노바 파마슈티컬스 인코포레이티드 | Bifunctional chimeric heterocyclic compounds and their use as androgen receptor degraders |
| CN118043324A (en) * | 2021-07-30 | 2024-05-14 | 百济神州有限公司 | Pyrrolo [2,3-b ] pyrazine-based bifunctional compounds as HPK1 degradants and uses thereof |
| 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 |
| AU2022405474A1 (en) * | 2021-12-08 | 2024-07-18 | Gluetacs Therapeutics (Shanghai) Co., Ltd. | E3 ubiquitin ligase ligand compound, protein degrader developed based thereon and their applications |
| WO2023151559A1 (en) * | 2022-02-08 | 2023-08-17 | 和径医药科技（上海）有限公司 | Heterocyclic compound, pharmaceutical composition containing same, and anti-tumor use thereof |
| WO2023212599A2 (en) * | 2022-04-26 | 2023-11-02 | Endotarget Inc. | Compounds and methods for targeted degradation of estrogen receptors |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW593256B (en) * | 1999-11-16 | 2004-06-21 | Hormos Medical Oy Ltd | Triphenylalkene derivatives and their use as selective estrogen receptor modulators |
| CN102584687A (en) * | 2011-12-30 | 2012-07-18 | 北京赛林泰医药技术有限公司 | Ethylene derivatives used as selective estrogen receptor modulators |
| WO2013097773A1 (en) * | 2011-12-30 | 2013-07-04 | Centaurus Biopharma Co., Ltd. | Novel arylalkene derivatives and use thereof as selective estrogen receptor modulators |
| GB201311891D0 (en) * | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compound |
| EP3368011A4 (en) * | 2016-07-12 | 2019-07-10 | Accutar Biotechnology Inc. | Novel compounds and uses thereof |
| US10647698B2 (en) * | 2016-12-01 | 2020-05-12 | Arvinas Operations, Inc. | Tetrahydronaphthalene and tetrahydroisoquinoline derivatives as estrogen receptor degraders |
| CN110357889B (en) * | 2018-04-09 | 2022-03-15 | 上海科技大学 | Protein degradation targeting compound, anti-tumor application thereof, intermediate thereof and application of intermediate |
| US11667621B2 (en) * | 2018-06-11 | 2023-06-06 | Stevens Institute Of Technology | Antiestrogen compounds |
| US20220016102A1 (en) * | 2018-11-21 | 2022-01-20 | Shanghaitech University | Er protein regulators and use thereof |
-
2019
- 2019-11-21 CA CA3120530A patent/CA3120530A1/en active Pending
- 2019-11-21 EP EP19828177.6A patent/EP3675839B1/en active Active
- 2019-11-21 CN CN201980077029.0A patent/CN113164409B/en active Active
- 2019-11-21 US US16/690,611 patent/US10696659B2/en not_active Expired - Fee Related
- 2019-11-21 SG SG11202105256QA patent/SG11202105256QA/en unknown
- 2019-11-21 WO PCT/US2019/062564 patent/WO2020106933A1/en unknown
- 2019-11-21 CN CN202310843757.6A patent/CN117050002A/en active Pending
- 2019-11-21 AU AU2019384807A patent/AU2019384807A1/en not_active Abandoned
-
2020
- 2020-04-17 US US16/851,994 patent/US11117885B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| CN117050002A (en) | 2023-11-14 |
| EP3675839B1 (en) | 2023-03-01 |
| EP3675839A1 (en) | 2020-07-08 |
| CN113164409A (en) | 2021-07-23 |
| WO2020106933A1 (en) | 2020-05-28 |
| US11117885B2 (en) | 2021-09-14 |
| US10696659B2 (en) | 2020-06-30 |
| CN113164409B (en) | 2023-07-18 |
| US20200157078A1 (en) | 2020-05-21 |
| EP3675839A4 (en) | 2020-12-23 |
| CA3120530A1 (en) | 2020-05-28 |
| AU2019384807A1 (en) | 2021-05-20 |
| US20200299264A1 (en) | 2020-09-24 |
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