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)
- 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 | |
| US62/952,695 | 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 (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 |
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 |
| WO2003063859A1 (en) | 2002-01-14 | 2003-08-07 | Nordic Bioscience A/S | Suppression of cartilage degradation via the estrogen receptor |
| CA2512000C (en) | 2002-12-26 | 2011-08-09 | Eisai Co., Ltd. | Selective estrogen receptor modulator |
| GB0305681D0 (en) | 2003-03-12 | 2003-04-16 | Kudos Pharm Ltd | Phthalazinone derivatives |
| US7449464B2 (en) | 2003-03-12 | 2008-11-11 | Kudos Pharmaceuticals Limited | Phthalazinone derivatives |
| GB0317466D0 (en) | 2003-07-25 | 2003-08-27 | Univ Sheffield | Use |
| SG150548A1 (en) | 2003-12-01 | 2009-03-30 | Kudos Pharm Ltd | Dna damage repair inhibitors for treatment of cancer |
| 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 |
| AU2008343932B2 (en) | 2007-12-19 | 2013-08-15 | Amgen Inc. | Fused pyridine, pyrimidine and triazine compounds as cell cycle inhibitors |
| AU2009284098B2 (en) | 2008-08-22 | 2012-03-29 | Astex Therapeutics Ltd. | Pyrrolopyrimidine compounds as CDK inhibitors |
| EP2346495B2 (en) | 2008-10-07 | 2023-05-24 | Kudos Pharmaceuticals Limited | Pharmaceutical formulation 514 |
| PA8852901A1 (es) | 2008-12-22 | 2010-07-27 | Lilly Co Eli | Inhibidores de proteina cinasa |
| SG183257A1 (en) | 2010-02-11 | 2012-09-27 | Celgene Corp | Arylmethoxy isoindoline derivatives and compositions comprising and methods of using the same |
| US20130035336A1 (en) | 2010-04-13 | 2013-02-07 | Novartis Ag | Combination comprising a cyclin dependent kinase 4 or cyclin dependent kinase (cdk4/6) inhibitor for treating cancer |
| KR20150039705A (ko) | 2011-12-30 | 2015-04-13 | 켄타우루스 바이오파마 컴퍼니 리미티드 | 신규 아릴알켄 유도체 및 이의 선택성 에스트로겐 수용체 조절제에 있어서의 응용 |
| 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 |
| 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 |
| HK1257296A1 (zh) * | 2016-07-12 | 2019-10-18 | Accutar Biotechnology Inc. | 新的化合物及其用途 |
| IL266842B (en) * | 2016-12-01 | 2022-09-01 | Arvinas Operations Inc | History of tetrahydronaphthalene and tetrahydroisoquinoline as estrogen receptor antagonists |
| CA3067023A1 (en) * | 2017-06-12 | 2018-12-20 | Syros Pharmaceuticals, Inc. | Compositions and methods for treating cancers with covalent inhibitors of cyclin-dependent kinase 7 (cdk7) |
| US10519136B2 (en) | 2017-12-29 | 2019-12-31 | Accutar Biotechnology | Dual inhibitors of PARP1 and CDK |
| EP3778590A4 (en) | 2018-04-09 | 2021-12-22 | ShanghaiTech University | ANTI PROTEIN DEGRADATION COMPOUND, ANTITUMOR APPLICATION, INTERMEDIATE THEREOF, AND INTERMEDIATE USE |
| WO2019241231A1 (en) | 2018-06-11 | 2019-12-19 | Abhishek Sharma | Antiestrogen compounds |
| WO2020103878A1 (zh) | 2018-11-21 | 2020-05-28 | 上海科技大学 | Er蛋白调节剂及其应用 |
| SG11202105256QA (en) * | 2018-11-21 | 2021-06-29 | Accutar Biotechnology Inc | Novel compounds having estrogen receptor alpha degradation activity and uses thereof |
| KR20210136973A (ko) * | 2019-01-03 | 2021-11-17 | 더 리젠츠 오브 더 유니버시티 오브 미시간 | 에스트로겐 수용체 단백질 분해제 |
| WO2021041348A1 (en) * | 2019-08-26 | 2021-03-04 | Arvinas Operations, Inc. | Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders |
| CN115003295B (zh) * | 2019-12-12 | 2025-05-06 | 冰洲石生物科技公司 | 具有雌激素受体降解活性的新型色满衍生物及其用途 |
-
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
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 |
| CN116234803B (zh) | 2026-06-30 |
| EP4081518A1 (en) | 2022-11-02 |
| JP7905280B2 (ja) | 2026-08-14 |
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