CN116234803B - 用于治疗癌症的雌激素受体降解剂和细胞周期蛋白依赖性激酶抑制剂的组合 - Google Patents
用于治疗癌症的雌激素受体降解剂和细胞周期蛋白依赖性激酶抑制剂的组合Info
- Publication number
- CN116234803B CN116234803B CN202080097414.4A CN202080097414A CN116234803B CN 116234803 B CN116234803 B CN 116234803B CN 202080097414 A CN202080097414 A CN 202080097414A CN 116234803 B CN116234803 B CN 116234803B
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- CN
- China
- Prior art keywords
- phenylbut
- hydroxyphenyl
- dione
- phenoxy
- inhibitor
- 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.)
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Classifications
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- 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 or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- A61K31/4427—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
-
- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
- A61K31/495—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
- A61K31/4995—Pyrazines or piperazines forming part of bridged ring 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
- A61K31/495—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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
-
- 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
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61K31/535—Heterocyclic 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
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962952695P | 2019-12-23 | 2019-12-23 | |
| US62/952695 | 2019-12-23 | ||
| PCT/US2020/066798 WO2021133886A1 (en) | 2019-12-23 | 2020-12-23 | Combinations of estrogen receptor degraders and cyclin-dependent kinase inhibitors for treating cancer |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN116234803A CN116234803A (zh) | 2023-06-06 |
| CN116234803B true CN116234803B (zh) | 2026-06-30 |
Family
ID=76575087
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202080097414.4A Active CN116234803B (zh) | 2019-12-23 | 2020-12-23 | 用于治疗癌症的雌激素受体降解剂和细胞周期蛋白依赖性激酶抑制剂的组合 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US11642342B2 (enExample) |
| EP (1) | EP4081518A4 (enExample) |
| JP (1) | JP7905280B2 (enExample) |
| CN (1) | CN116234803B (enExample) |
| CA (1) | CA3161892A1 (enExample) |
| WO (1) | WO2021133886A1 (enExample) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20220348595A1 (en) * | 2021-04-09 | 2022-11-03 | Endotarget Inc. | Compounds and methods for the targeted degradation of estrogen receptors |
| JP7744061B2 (ja) * | 2021-07-30 | 2025-09-25 | ヒノバ ファーマシューティカルズ インコーポレイテッド | 二官能性キメラ複素環式化合物及びアンドロゲン受容体分解剤としての使用 |
| US20250041303A1 (en) * | 2021-11-30 | 2025-02-06 | Institute For Cancer Research D/B/A The Research Institute Of Fox Chase Cancer Center | Combination therapy for cancer treatment |
| AU2022405474B2 (en) * | 2021-12-08 | 2026-08-13 | Gluetacs Therapeutics (Shanghai) Co., Ltd. | E3 ubiquitin ligase ligand compound, protein degrader developed based thereon and their applications |
| EP4455133A4 (en) * | 2021-12-24 | 2026-04-15 | Suzhou Kintor Pharmaceuticals Inc | MULTI-PROTEIN DEGRADING AGENT WITH AN IMIDE SKELETON |
| US12662467B2 (en) | 2022-04-18 | 2026-06-23 | BioThery X, Inc. | Isoindolinones, pharmaceutical compositions, and therapeutic applications |
| CN117229286A (zh) * | 2022-06-14 | 2023-12-15 | 海创药业股份有限公司 | 一种芳香类化合物及其制备方法及在制备雌激素受体降解剂中的用途 |
| US20260000676A1 (en) * | 2022-07-12 | 2026-01-01 | The Regents Of The University Of Michigan | Chroman derivatives as estrogen receptor degraders |
| CN115724836B (zh) * | 2022-11-24 | 2025-07-04 | 北京大学 | 一种gpx4蛋白降解剂及其制备方法和应用、一种抗肿瘤细胞药物 |
| EP4626890A1 (en) | 2022-12-01 | 2025-10-08 | KRKA, d.d., Novo mesto | Ribociclib salts and formulations thereof |
| CN116751186B (zh) * | 2022-12-23 | 2024-10-18 | 南京知和医药科技有限公司 | 一种雌激素受体调节剂的制备及其用途 |
| CN119258223A (zh) * | 2023-07-06 | 2025-01-07 | 海创药业股份有限公司 | 一种降解雌激素受体的联合用药物及其用途 |
| CN117683020A (zh) * | 2023-11-02 | 2024-03-12 | 华南理工大学 | 一种苯酞嗪酮的氨基吡啶类化合物及其制备方法和在制备抑制剂和抗肿瘤药物中的应用 |
| WO2025245408A1 (en) | 2024-05-22 | 2025-11-27 | Accutar Biotechnology Inc. | Chroman-based compounds for treating cancer |
| CN120623156B (zh) * | 2025-05-29 | 2026-07-07 | 延边大学 | 一种cdk4/parp1双靶点抑制剂和应用 |
Citations (3)
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| CN108495618A (zh) * | 2016-07-12 | 2018-09-04 | 冰洲石生物科技公司 | 新的化合物及其用途 |
| CN110291087A (zh) * | 2016-12-01 | 2019-09-27 | 阿尔维纳斯运营股份有限公司 | 作为雌激素受体降解剂的四氢萘和四氢异喹啉衍生物 |
| WO2020142227A1 (en) * | 2019-01-03 | 2020-07-09 | The Regents Of The University Of Michigan | Estrogen receptor protein degraders |
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| US20010021710A1 (en) | 1996-10-28 | 2001-09-13 | Poul Jacobsen | Novel cis-3,4-chroman derivatives useful in the prevention or treatment of estrogen related diseases or syndromes |
| TW593256B (en) | 1999-11-16 | 2004-06-21 | Hormos Medical Oy Ltd | Triphenylalkene derivatives and their use as selective estrogen receptor modulators |
| JP2001306582A (ja) | 2000-04-20 | 2001-11-02 | Ge Plastics Japan Ltd | 成型品情報の検索システム |
| US7151102B2 (en) | 2000-10-30 | 2006-12-19 | Kudos Pharmaceuticals Limited | Phthalazinone derivatives |
| WO2003063859A1 (en) | 2002-01-14 | 2003-08-07 | Nordic Bioscience A/S | Suppression of cartilage degradation via the estrogen receptor |
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| 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 |
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| GB201311891D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compound |
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| WO2020103878A1 (zh) | 2018-11-21 | 2020-05-28 | 上海科技大学 | Er蛋白调节剂及其应用 |
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-
2020
- 2020-12-23 CN CN202080097414.4A patent/CN116234803B/zh active Active
- 2020-12-23 CA CA3161892A patent/CA3161892A1/en active Pending
- 2020-12-23 WO PCT/US2020/066798 patent/WO2021133886A1/en not_active Ceased
- 2020-12-23 EP EP20905920.3A patent/EP4081518A4/en active Pending
- 2020-12-23 JP JP2022538706A patent/JP7905280B2/ja active Active
-
2021
- 2021-01-04 US US17/140,664 patent/US11642342B2/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108495618A (zh) * | 2016-07-12 | 2018-09-04 | 冰洲石生物科技公司 | 新的化合物及其用途 |
| CN110291087A (zh) * | 2016-12-01 | 2019-09-27 | 阿尔维纳斯运营股份有限公司 | 作为雌激素受体降解剂的四氢萘和四氢异喹啉衍生物 |
| WO2020142227A1 (en) * | 2019-01-03 | 2020-07-09 | The Regents Of The University Of Michigan | Estrogen receptor protein degraders |
Non-Patent Citations (5)
| Title |
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| CDK inhibitors as potential breast cancer therapeutics: new evidence for enhanced efficacy in ER+ disease;Robert L Sutherland等;《Breast Cancer Research》;20091231;112页 * |
| Massimo Cristofanilli等.Fulvestrant plus palbociclib versus fulvestrant plus placebo for treatment of hormone-receptor-positive, HER2-negative metastatic breast cancer that progressed on previous endocrine therapy (PALOMA-3): fi nal analysis of the multicentre, double-blind, phase 3 randomised controlled trial.《HE LANCER ONCOLOGY,ELSEVIER,AMSTERDAM,NL》.2016,426-439. * |
| Massimo Cristofanilli等.Fulvestrant plus palbociclib versus fulvestrant plus placebo for treatment of hormone-receptor-positive, HER2-negative metastatic breast cancer that progressed on previous endocrine therapy (PALOMA-3): fi nal analysis of the multicentre, double-blind, phase 3 randomised controlled trial.《THE LANCER ONCOLOGY,ELSEVIER,AMSTERDAM,NL》.2016,426-439. * |
| Palbociclib Combined with Fulvestrant in Premenopausal Women with Advanced Breast Cancer and Prior Progression on Endocrine Therapy: PALOMA-3 Results;SIBYLLE LOIBL等;《The Oncologist 》;20170626;1028–1 038 * |
| Palbociclib Combined with Fulvestrant in Premenopausal Women with Advanced Breast Cancer and Prior Progression on Endocrine Therapy: PALOMA-3 Results;SIBYLLE LOIBL等;《The Oncologist》;20170626;1028–1 038 * |
Also Published As
| Publication number | Publication date |
|---|---|
| JP2023508357A (ja) | 2023-03-02 |
| CN116234803A (zh) | 2023-06-06 |
| US11642342B2 (en) | 2023-05-09 |
| US20210213012A1 (en) | 2021-07-15 |
| WO2021133886A1 (en) | 2021-07-01 |
| EP4081518A4 (en) | 2023-12-27 |
| CA3161892A1 (en) | 2021-07-01 |
| EP4081518A1 (en) | 2022-11-02 |
| JP7905280B2 (ja) | 2026-08-14 |
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