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
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 (zh) |
| EP (1) | EP3675839B1 (zh) |
| CN (2) | CN117050002A (zh) |
| AU (1) | AU2019384807A1 (zh) |
| CA (1) | CA3120530A1 (zh) |
| SG (1) | SG11202105256QA (zh) |
| WO (1) | WO2020106933A1 (zh) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114085212B (zh) * | 2018-09-30 | 2023-05-02 | 中国科学院上海药物研究所 | 异吲哚啉类化合物、其制备方法、药物组合物及用途 |
| 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 (ko) | 2021-05-18 | 2022-11-24 | 재단법인 대구경북첨단의료산업진흥재단 | 신규 에텐 화합물 및 이를 유효성분으로 포함하는 암의 예방 또는 치료용 약학적 조성물 |
| KR102503296B1 (ko) | 2021-05-18 | 2023-02-24 | 재단법인 대구경북첨단의료산업진흥재단 | 신규 에텐 화합물 및 이를 유효성분으로 포함하는 암의 예방 또는 치료용 약학적 조성물 |
| EP4367112A1 (en) | 2021-07-09 | 2024-05-15 | Plexium, Inc. | Aryl compounds and pharmaceutical compositions that modulate ikzf2 |
| WO2023006063A1 (en) * | 2021-07-30 | 2023-02-02 | Beigene, Ltd. | PYRROLO [2, 3-b] PYRAZINE-BASED BIFUNCTIONAL COMPOUNDS AS HPK1 DEGRADERS AND THE USE THEREOF |
| WO2023006097A1 (zh) * | 2021-07-30 | 2023-02-02 | 海创药业股份有限公司 | 一种双功能嵌合体杂环化合物及其作为雄激素受体降解剂的用途 |
| CN115894450B (zh) * | 2021-11-30 | 2023-09-12 | 山东如至生物医药科技有限公司 | 一种新型多环类化合物及其组合物和用途 |
| CN116239566A (zh) * | 2021-12-08 | 2023-06-09 | 标新生物医药科技(上海)有限公司 | E3泛素连接酶配体化合物、基于该配体化合物开发的蛋白降解剂及它们的应用 |
| CN116462685A (zh) * | 2022-02-08 | 2023-07-21 | 和径医药科技（上海）有限公司 | 杂环化合物、包含其的药物组合物及其抗肿瘤应用 |
| 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 (zh) * | 2011-12-30 | 2012-07-18 | 北京赛林泰医药技术有限公司 | 作为选择性雌激素受体调节剂的乙烯衍生物 |
| CA2861939A1 (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 |
| JP2019525955A (ja) * | 2016-07-12 | 2019-09-12 | アキュター バイオテクノロジー インコーポレイテッド | 新規化合物およびその使用 |
| KR102173464B1 (ko) * | 2016-12-01 | 2020-11-04 | 아비나스 오퍼레이션스, 인코포레이티드 | 에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 및 테트라히드로이소퀴놀린 유도체 |
| WO2019196812A1 (zh) * | 2018-04-09 | 2019-10-17 | 上海科技大学 | 蛋白降解靶向化合物、其抗肿瘤应用、其中间体及中间体应用 |
| WO2019241231A1 (en) * | 2018-06-11 | 2019-12-19 | Abhishek Sharma | Antiestrogen compounds |
| US20220016102A1 (en) * | 2018-11-21 | 2022-01-20 | Shanghaitech University | Er protein regulators and use thereof |
-
2019
- 2019-11-21 US US16/690,611 patent/US10696659B2/en active Active
- 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/zh active Pending
- 2019-11-21 CA CA3120530A patent/CA3120530A1/en active Pending
- 2019-11-21 CN CN201980077029.0A patent/CN113164409B/zh active Active
- 2019-11-21 AU AU2019384807A patent/AU2019384807A1/en active Pending
- 2019-11-21 EP EP19828177.6A patent/EP3675839B1/en active Active
-
2020
- 2020-04-17 US US16/851,994 patent/US11117885B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| CN113164409A (zh) | 2021-07-23 |
| US20200299264A1 (en) | 2020-09-24 |
| CA3120530A1 (en) | 2020-05-28 |
| EP3675839A4 (en) | 2020-12-23 |
| US20200157078A1 (en) | 2020-05-21 |
| CN113164409B (zh) | 2023-07-18 |
| CN117050002A (zh) | 2023-11-14 |
| EP3675839B1 (en) | 2023-03-01 |
| US11117885B2 (en) | 2021-09-14 |
| AU2019384807A1 (en) | 2021-05-20 |
| WO2020106933A1 (en) | 2020-05-28 |
| US10696659B2 (en) | 2020-06-30 |
| EP3675839A1 (en) | 2020-07-08 |
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