CA3161892A1 - Combinations of estrogen receptor degraders and cyclin-dependent kinase inhibitors for treating cancer - Google Patents
Combinations of estrogen receptor degraders and cyclin-dependent kinase inhibitors for treating cancer Download PDFInfo
- Publication number
- CA3161892A1 CA3161892A1 CA3161892A CA3161892A CA3161892A1 CA 3161892 A1 CA3161892 A1 CA 3161892A1 CA 3161892 A CA3161892 A CA 3161892A CA 3161892 A CA3161892 A CA 3161892A CA 3161892 A1 CA3161892 A1 CA 3161892A1
- Authority
- CA
- Canada
- Prior art keywords
- phenylbut
- phenoxy
- substituted
- dione
- alkyl
- 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.)
- Pending
Links
Classifications
-
- 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
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (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 | |
| US62/952,695 | 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 (1)
| Publication Number | Publication Date |
|---|---|
| CA3161892A1 true CA3161892A1 (en) | 2021-07-01 |
Family
ID=76575087
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3161892A Pending CA3161892A1 (en) | 2019-12-23 | 2020-12-23 | Combinations of estrogen receptor degraders and cyclin-dependent kinase inhibitors for treating cancer |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US11642342B2 (https=) |
| EP (1) | EP4081518A4 (https=) |
| JP (1) | JP2023508357A (https=) |
| CN (1) | CN116234803A (https=) |
| CA (1) | CA3161892A1 (https=) |
| WO (1) | WO2021133886A1 (https=) |
Families Citing this family (12)
| 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 |
| KR20240053589A (ko) * | 2021-07-30 | 2024-04-24 | 하이노바 파마슈티컬스 인코포레이티드 | 이중 기능성 키메라 헤테로 고리 화합물 및 이의 안드로겐 수용체 분해제로서의 용도 |
| WO2023102379A1 (en) * | 2021-11-30 | 2023-06-08 | Institute For Cancer Research D/B/A The Research Institute Of Fox Chase Cancer Center | Combination therapy for cancer treatment |
| EP4446324A4 (en) * | 2021-12-08 | 2026-05-06 | Gluetacs Therapeutics Shanghai Co Ltd | Ligand compounds for e3 ubiquitin ligase, protein degraders developed on basis of ligand compounds, and uses thereof |
| WO2023116835A1 (zh) * | 2021-12-24 | 2023-06-29 | 苏州开拓药业股份有限公司 | 一种具有酰亚胺骨架的多蛋白降解剂 |
| 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 |
| US20250381179A1 (en) | 2024-05-22 | 2025-12-18 | Accutar Biotechnology Inc. | Chroman-based compounds for treating cancer |
Family Cites Families (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| JP2005524630A (ja) | 2002-01-14 | 2005-08-18 | ノルディック・ビオサイエンス・エー／エス | エストロゲン受容体を介する軟骨破壊の抑制 |
| CA2512000C (en) | 2002-12-26 | 2011-08-09 | Eisai Co., Ltd. | Selective estrogen receptor modulator |
| US7449464B2 (en) | 2003-03-12 | 2008-11-11 | Kudos Pharmaceuticals Limited | Phthalazinone derivatives |
| GB0305681D0 (en) | 2003-03-12 | 2003-04-16 | Kudos Pharm Ltd | Phthalazinone derivatives |
| GB0317466D0 (en) | 2003-07-25 | 2003-08-27 | Univ Sheffield | Use |
| PL2305221T3 (pl) | 2003-12-01 | 2015-11-30 | Kudos Pharm Ltd | Inhibitory naprawy uszkodzeń DNA w leczeniu raka |
| UY30639A1 (es) | 2006-10-17 | 2008-05-31 | Kudos Pharm Ltd | Derivados sustituidos de 2h-ftalazin-1-ona, sus formas cristalinas, proceso de preparacion y aplicaciones |
| EA201001030A1 (ru) | 2007-12-19 | 2011-02-28 | Амген Инк. | Конденсированные соединения пиридина, пиримидина и триазина в качестве ингибиторов клеточного цикла |
| ES2522346T3 (es) | 2008-08-22 | 2014-11-14 | Novartis Ag | Compuestos de pirrolopirimidina como inhibidores de CDK |
| CA2737400C (en) | 2008-10-07 | 2016-11-22 | Astrazeneca Uk Limited | Pharmaceutical formulation 514 |
| PA8852901A1 (es) | 2008-12-22 | 2010-07-27 | Lilly Co Eli | Inhibidores de proteina cinasa |
| PL3202460T3 (pl) | 2010-02-11 | 2019-12-31 | Celgene Corporation | Pochodne arylometoksyizoindoliny i zawierające je kompozycje oraz sposoby ich zastosowania |
| EP2558092B1 (en) | 2010-04-13 | 2018-06-27 | Novartis AG | Combination comprising a cyclin dependent kinase 4 or cyclin dependent kinase 6 (cdk4/6) inhibitor and an mtor inhibitor for treating cancer |
| 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 |
| WO2013097773A1 (en) | 2011-12-30 | 2013-07-04 | Centaurus Biopharma Co., Ltd. | Novel arylalkene derivatives and use thereof as selective estrogen receptor modulators |
| CA2906157C (en) | 2013-03-15 | 2022-05-17 | G1 Therapeutics, Inc. | Highly active anti-neoplastic and anti-proliferative agents |
| GB201311891D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compound |
| CN108495618B (zh) * | 2016-07-12 | 2019-08-16 | 冰洲石生物科技公司 | 新的化合物及其用途 |
| BR112019011200B1 (pt) * | 2016-12-01 | 2021-12-28 | Arvinas Operations, Inc | Derivados de tetrahidronaftaleno e tetrahidroisoquinolina como degradadores do receptor de estrogênio |
| AU2018282901A1 (en) * | 2017-06-12 | 2020-01-16 | Syros Pharmaceuticals, Inc. | Compositions and methods for treating cancers with covalent inhibitors of cyclin-dependent kinase 7 (CDK7) |
| WO2019133864A1 (en) | 2017-12-29 | 2019-07-04 | Accutar Biotechnology | DUAL INHIBITORS OF PARP1 and CDK |
| 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 |
| 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 |
| SG11202105256QA (en) * | 2018-11-21 | 2021-06-29 | Accutar Biotechnology Inc | Novel compounds having estrogen receptor alpha degradation activity and uses thereof |
| CN113614076A (zh) * | 2019-01-03 | 2021-11-05 | 密执安大学评议会 | 雌激素受体蛋白降解剂 |
| KR20220054347A (ko) * | 2019-08-26 | 2022-05-02 | 아비나스 오퍼레이션스, 인코포레이티드 | 에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 유도체로 유방암을 치료하는 방법 |
| EP3835298B1 (en) * | 2019-12-12 | 2024-06-26 | Accutar Biotechnology Inc. | Novel chroman derivatives having estrogen receptor degradation activity and uses thereof |
-
2020
- 2020-12-23 JP JP2022538706A patent/JP2023508357A/ja active Pending
- 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 CN CN202080097414.4A patent/CN116234803A/zh active Pending
-
2021
- 2021-01-04 US US17/140,664 patent/US11642342B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| WO2021133886A1 (en) | 2021-07-01 |
| JP2023508357A (ja) | 2023-03-02 |
| EP4081518A4 (en) | 2023-12-27 |
| US20210213012A1 (en) | 2021-07-15 |
| US11642342B2 (en) | 2023-05-09 |
| EP4081518A1 (en) | 2022-11-02 |
| CN116234803A (zh) | 2023-06-06 |
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