CN110267659A - 用于治疗cdk4/6介导的癌症的组合物和方法 - Google Patents
用于治疗cdk4/6介导的癌症的组合物和方法 Download PDFInfo
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- CN110267659A CN110267659A CN201780085879.6A CN201780085879A CN110267659A CN 110267659 A CN110267659 A CN 110267659A CN 201780085879 A CN201780085879 A CN 201780085879A CN 110267659 A CN110267659 A CN 110267659A
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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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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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
- A61K31/435—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
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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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/43—Enzymes; Proenzymes; Derivatives thereof
- A61K38/45—Transferases (2)
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/55—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- 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
- C07D471/04—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
- C07D487/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Y—ENZYMES
- C12Y203/00—Acyltransferases (2.3)
- C12Y203/02—Aminoacyltransferases (2.3.2)
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Engineering & Computer Science (AREA)
- Zoology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biochemistry (AREA)
- Gastroenterology & Hepatology (AREA)
- Genetics & Genomics (AREA)
- Wood Science & Technology (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicinal Preparation (AREA)
- Investigating Or Analysing Biological Materials (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662431806P | 2016-12-08 | 2016-12-08 | |
| US62/431,806 | 2016-12-08 | ||
| PCT/US2017/065027 WO2018106870A1 (en) | 2016-12-08 | 2017-12-07 | Compositions and methods for treating cdk4/6-mediated cancer |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN110267659A true CN110267659A (zh) | 2019-09-20 |
Family
ID=62491322
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201780085879.6A Pending CN110267659A (zh) | 2016-12-08 | 2017-12-07 | 用于治疗cdk4/6介导的癌症的组合物和方法 |
Country Status (7)
| Country | Link |
|---|---|
| US (2) | US11541051B2 (https=) |
| EP (1) | EP3551185A4 (https=) |
| JP (1) | JP2020514252A (https=) |
| CN (1) | CN110267659A (https=) |
| AU (1) | AU2017370694A1 (https=) |
| CA (1) | CA3045037A1 (https=) |
| WO (1) | WO2018106870A1 (https=) |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114349738A (zh) * | 2020-10-14 | 2022-04-15 | 清华大学 | 一类靶向降解cdk2的小分子缀合物及其应用 |
| CN114957249A (zh) * | 2022-05-20 | 2022-08-30 | 东南大学 | 一种不可逆共价结合cdk抑制剂及其制备方法和应用 |
| CN115650968A (zh) * | 2022-12-27 | 2023-01-31 | 英矽智能科技(上海)有限公司 | 作为cdk选择性抑制剂的新型哒嗪酮化合物 |
| 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 |
| WO2026067249A1 (en) * | 2024-09-29 | 2026-04-02 | K2 Medicines (Nanjing) Co., Ltd. | Cdk4 or cdk4/6 dual degrader and use thereof |
Families Citing this family (66)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK2968290T3 (da) * | 2013-03-15 | 2019-11-25 | G1 Therapeutics Inc | Transient beskyttelse af normale celler under kemoterapi |
| WO2018005863A1 (en) * | 2016-07-01 | 2018-01-04 | G1 Therapeutics, Inc. | Pyrimidine-based compounds for the treatment of cancer |
| EP3858835A1 (en) | 2016-07-01 | 2021-08-04 | G1 Therapeutics, Inc. | Pyrimidine-based antiproliferative agents |
| EP3532464A4 (en) | 2016-10-28 | 2020-07-08 | Icahn School of Medicine at Mount Sinai | COMPOSITIONS AND METHODS FOR THE TREATMENT OF EZH2 MEDIATION CANCER |
| JP2020514252A (ja) | 2016-12-08 | 2020-05-21 | アイカーン スクール オブ メディスン アット マウント シナイ | Cdk4/6媒介性がんを治療するための組成物および方法 |
| US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides |
| TWI791552B (zh) | 2017-07-10 | 2023-02-11 | 美商西建公司 | 抗增生化合物及其使用方法 |
| CN109516989B (zh) * | 2017-09-17 | 2021-12-31 | 上海美志医药科技有限公司 | 一类抑制并降解cdk的化合物 |
| EP3728228A1 (en) | 2017-12-22 | 2020-10-28 | Ravenna Pharmaceuticals, Inc. | Aminopyridine derivatives as phosphatidylinositol phosphate kinase inhibitors |
| CA3092677A1 (en) | 2018-03-06 | 2019-09-12 | Icahn School Of Medicine At Mount Sinai | Serine threonine kinase (akt) degradation / disruption compounds and methods of use |
| US12539292B2 (en) | 2018-04-01 | 2026-02-03 | Arvinas Operations, Inc. | BRM targeting compounds and associated methods of use |
| CN118344338A (zh) | 2018-04-23 | 2024-07-16 | 细胞基因公司 | 取代的4-氨基异吲哚啉-1,3-二酮化合物以及它们用于治疗淋巴瘤的用途 |
| WO2019242625A1 (zh) * | 2018-06-20 | 2019-12-26 | 上海科技大学 | 制备来那度胺衍生物的方法 |
| CA3104298A1 (en) | 2018-06-21 | 2019-12-26 | Icahn School Of Medicine At Mount Sinai | Wd40 repeat domain protein 5 (wdr5) degradation / disruption compounds and methods of use |
| EP3817745A4 (en) * | 2018-07-05 | 2022-04-06 | Icahn School of Medicine at Mount Sinai | PROTEIN TYROSINE KINASE 6 (PTK6) DEGRADATION/DISPUTED COMPOUNDS AND METHODS OF USE |
| WO2020023502A1 (en) * | 2018-07-23 | 2020-01-30 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and uses thereof |
| CN108948136A (zh) * | 2018-08-06 | 2018-12-07 | 浙江华海药业股份有限公司 | 一种赖诺普利杂质及其制备方法 |
| CN110835345A (zh) * | 2018-08-17 | 2020-02-25 | 中国科学院上海药物研究所 | 一类细胞周期依赖性激酶的降解剂、其制备方法、药物组合物及其用途 |
| EP3841100A1 (en) | 2018-08-20 | 2021-06-30 | Arvinas Operations, Inc. | Proteolysis targeting chimeric (protac) compound with e3 ubiquitin ligase binding activity and targeting alpha-synuclein protein for treating neurodegenerative diseases |
| KR20210072043A (ko) * | 2018-10-08 | 2021-06-16 | 더 리젠츠 오브 더 유니버시티 오브 미시간 | 소분자 mdm 2 단백질 분해제 |
| JP7600123B2 (ja) * | 2018-10-15 | 2024-12-16 | ニューリックス セラピューティクス,インコーポレイテッド | ユビキチンプロテオソーム経路を介してbtkを分解するための二官能性化合物 |
| WO2020092662A1 (en) * | 2018-11-02 | 2020-05-07 | The Wistar Institute Of Anatomy And Biology | Proteolysis-targeting chimeras |
| CN111205282B (zh) * | 2018-11-21 | 2023-12-01 | 上海科技大学 | Er蛋白调节剂及其应用 |
| WO2020163823A2 (en) * | 2019-02-08 | 2020-08-13 | University Of Florida Research Foundation, Incorporated | Therapeutic agents and methods of treatment |
| WO2020167518A1 (en) | 2019-02-13 | 2020-08-20 | Nurix Therapeutics, Inc. | Bifunctional compounds for degrading btk via ubiquitin proteosome pathway |
| CN113646002A (zh) * | 2019-02-27 | 2021-11-12 | 上海睿跃生物科技有限公司 | 环amp反应元件结合蛋白(cbp)和/或300kda腺病毒e1a结合蛋白(p300)降解化合物和使用方法 |
| KR20210141554A (ko) | 2019-03-21 | 2021-11-23 | 코디악 바이오사이언시즈, 인크. | 세포외 소포 접합체 및 이의 용도 |
| WO2020191369A1 (en) | 2019-03-21 | 2020-09-24 | Codiak Biosciences, Inc. | Process for preparing extracellular vesicles |
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| TW202112767A (zh) | 2019-06-17 | 2021-04-01 | 美商佩特拉製藥公司 | 作為磷脂酸肌醇磷酸激酶抑制劑之胺基吡啶衍生物 |
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| US11964983B2 (en) * | 2020-06-11 | 2024-04-23 | Lunella Biotech, Inc. | Selective CDK4/6 inhibitor cancer therapeutics |
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| WO2022113003A1 (en) | 2020-11-27 | 2022-06-02 | Rhizen Pharmaceuticals Ag | Cdk inhibitors |
| WO2022149057A1 (en) | 2021-01-05 | 2022-07-14 | Rhizen Pharmaceuticals Ag | Cdk inhibitors |
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| WO2023177451A1 (en) * | 2022-03-18 | 2023-09-21 | EnhancedBio Inc. | Compounds and methods for the targeted degradation of cyclin dependent kinases |
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| CN120359217A (zh) * | 2022-09-15 | 2025-07-22 | 上海睿跃生物科技有限公司 | 经修饰的蛋白质以及蛋白质结合剂和降解剂 |
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| EP4705307A1 (en) * | 2023-05-03 | 2026-03-11 | St. Jude Children's Research Hospital, Inc. | A sequence selective dna binding molecule (syngrader) |
| CN120981456A (zh) | 2023-05-24 | 2025-11-18 | 金橘生物科技公司 | 杂环化合物及其用途 |
| WO2024256569A1 (en) * | 2023-06-13 | 2024-12-19 | Rijksuniversiteit Groningen | Novel cdk degraders |
Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20140031325A1 (en) * | 2010-12-06 | 2014-01-30 | Celgene Corporation | Combination therapy with lenalidomide and a cdk inhibitor for treating multiple myeloma |
| CN104736569A (zh) * | 2012-01-12 | 2015-06-24 | 耶鲁大学 | 通过e3泛素连接酶增强靶蛋白质及其他多肽降解的化合物和方法 |
| US20150274738A1 (en) * | 2012-10-19 | 2015-10-01 | Dana-Farber Cancer, Institute, Inc. | Hydrophobically tagged small molecules as inducers of protein degradation |
| CN105085620A (zh) * | 2015-06-25 | 2015-11-25 | 中山大学附属第一医院 | 一种靶向泛素化降解Smad3的化合物 |
| WO2016105518A1 (en) * | 2014-12-23 | 2016-06-30 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| WO2017185031A1 (en) * | 2016-04-22 | 2017-10-26 | Dana-Farber Cancer Institute, Inc. | Degradation of cyclin-dependent kinase 4/6 (cdk4/6) by conjugation of cdk4/6 inhibitors with e3 ligase ligand and methods of use |
| CN109790143A (zh) * | 2016-05-10 | 2019-05-21 | C4医药公司 | 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体 |
Family Cites Families (45)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5691147A (en) * | 1994-06-02 | 1997-11-25 | Mitotix, Inc. | CDK4 binding assay |
| US6486214B1 (en) | 1997-09-10 | 2002-11-26 | Rutgers, The State University Of New Jersey | Polyanhydride linkers for production of drug polymers and drug polymer compositions produced thereby |
| SI1255752T1 (sl) | 2000-02-15 | 2007-12-31 | Pharmacia & Upjohn Co Llc | S pirolom substituirani zaviralci 2-indolinon protein kinaza |
| PL2076260T3 (pl) | 2006-09-15 | 2011-08-31 | Celgene Corp | Związki N-metyloaminometylo-izoindolu, kompozycje zawierające te związki, oraz metody ich stosowania |
| WO2008109104A1 (en) | 2007-03-07 | 2008-09-12 | The Regents Of The University Of California | Bivalent inhibitors of akt protein kinase |
| CN101918373B (zh) | 2007-07-05 | 2013-06-05 | 阵列生物制药公司 | 作为akt蛋白激酶抑制剂的嘧啶基环戊烷 |
| WO2009134418A2 (en) | 2008-04-30 | 2009-11-05 | Fox Chase Cancer Center | Assay for identifying agents that modulate epigenetic silencing, and agents identified thereby |
| EP2473054B1 (en) | 2009-09-04 | 2017-06-14 | The Regents of the University of Michigan | Compositions and methods for treatment of leukemia |
| EP2536706B1 (en) | 2010-02-11 | 2017-06-14 | Celgene Corporation | Arylmethoxy isoindoline derivatives and compositions comprising and methods of using the same |
| US20150119435A1 (en) | 2012-05-11 | 2015-04-30 | Yale University | Compounds useful for promoting protein degradation and methods using same |
| UA118548C2 (uk) | 2012-12-21 | 2019-02-11 | Епізайм, Інк. | Тетрагідро- та дигідроізохіноліни як інгібітори prmt5 та їх застосування |
| US9796701B2 (en) | 2013-12-31 | 2017-10-24 | Xuanzhu Pharma Co., Ltd. | Kinase inhibitor and use thereof |
| WO2015104677A1 (en) | 2014-01-10 | 2015-07-16 | Piramal Enterprises Limited | Heterocyclic compounds as ezh2 inhibitors |
| AU2015247817C1 (en) | 2014-04-14 | 2022-02-10 | Arvinas Operations, Inc. | Imide-based modulators of proteolysis and associated methods of use |
| JP6744826B2 (ja) | 2014-06-13 | 2020-08-19 | バック バイオサイエンシーズ, エルエルシーBach BioSciences, LLC | Fap活性化治療剤及びそれに関連する使用 |
| EP3885343A1 (en) | 2014-11-06 | 2021-09-29 | Dana-Farber Cancer Institute, Inc. | Indole compounds as ezh2 inhibitors and uses thereof |
| EP3227446A1 (en) | 2014-12-01 | 2017-10-11 | Novartis AG | Compositions and methods for diagnosis and treatment of prostate cancer |
| WO2016106518A1 (zh) | 2014-12-29 | 2016-07-07 | 深圳市日上光电股份有限公司 | 导线集成式照明灯箱 |
| AR103297A1 (es) | 2014-12-30 | 2017-05-03 | Forma Therapeutics Inc | Pirrolo y pirazolopirimidinas como inhibidores de la proteasa 7 específica de ubiquitina |
| WO2016115480A1 (en) | 2015-01-16 | 2016-07-21 | Vedantra Pharmaceuticals, Inc. | Multilamellar lipid vesicle compositions including a conjugated anaplastic lymphoma kinase (alk) variant and uses thereof |
| US10730870B2 (en) | 2015-03-18 | 2020-08-04 | Arvinas Operations, Inc. | Compounds and methods for the enhanced degradation of targeted proteins |
| EP3289074B1 (en) | 2015-04-28 | 2023-10-04 | Université de Strasbourg | Clinical gene signature-based human cell culture model and uses thereof |
| RU2719477C2 (ru) | 2015-06-22 | 2020-04-17 | Оно Фармасьютикал Ко., Лтд. | Соединение, ингибирующее brk |
| WO2017007612A1 (en) | 2015-07-07 | 2017-01-12 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| WO2017011371A1 (en) | 2015-07-10 | 2017-01-19 | Arvinas, Inc | Mdm2-based modulators of proteolysis and associated methods of use |
| CA2988436A1 (en) | 2015-07-13 | 2017-01-19 | Arvinas, Inc. | Alanine-based modulators of proteolysis and associated methods of use |
| US9809603B1 (en) | 2015-08-18 | 2017-11-07 | Deuterx, Llc | Deuterium-enriched isoindolinonyl-piperidinonyl conjugates and oxoquinazolin-3(4H)-yl-piperidinonyl conjugates and methods of treating medical disorders using same |
| WO2017040990A1 (en) | 2015-09-03 | 2017-03-09 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and uses thereof |
| CA3015417A1 (en) | 2016-03-01 | 2017-09-08 | Propellon Therapeutics Inc. | Inhibitors of wdr5 protein-protein binding |
| JP7624690B2 (ja) | 2016-03-01 | 2025-01-31 | プロペロン セラピューティクス インコーポレイテッド | Wdr5タンパク質-タンパク質結合の阻害剤 |
| EP4491236A3 (en) | 2016-05-10 | 2025-04-02 | C4 Therapeutics, Inc. | Heterocyclic degronimers for target protein degradation |
| TW201811799A (zh) | 2016-09-09 | 2018-04-01 | 美商英塞特公司 | 吡唑并嘧啶化合物及其用途 |
| US10160763B2 (en) | 2016-09-13 | 2018-12-25 | Vanderbilt University | WDR5 inhibitors and modulators |
| EP3532464A4 (en) | 2016-10-28 | 2020-07-08 | Icahn School of Medicine at Mount Sinai | COMPOSITIONS AND METHODS FOR THE TREATMENT OF EZH2 MEDIATION CANCER |
| JP2020514252A (ja) | 2016-12-08 | 2020-05-21 | アイカーン スクール オブ メディスン アット マウント シナイ | Cdk4/6媒介性がんを治療するための組成物および方法 |
| US11052091B2 (en) | 2016-12-21 | 2021-07-06 | Ono Pharmaceutical Co., Ltd. | BRK inhibitory compound |
| WO2019113071A1 (en) | 2017-12-05 | 2019-06-13 | Icahn School Of Medicine At Mount Sinai | Compositions and methods for treating alk-mediated cancer |
| WO2019165189A1 (en) | 2018-02-22 | 2019-08-29 | Icahn School Of Medicine At Mount Sinai | Protein arginine methyltransferase 5 (prmt5) degradation / disruption compounds and methods of use |
| CA3092677A1 (en) | 2018-03-06 | 2019-09-12 | Icahn School Of Medicine At Mount Sinai | Serine threonine kinase (akt) degradation / disruption compounds and methods of use |
| JP7421499B2 (ja) | 2018-05-15 | 2024-01-24 | アメリカ合衆国 | 腫瘍転移および腫瘍発生の予防および治療のための製剤および方法 |
| CA3104298A1 (en) | 2018-06-21 | 2019-12-26 | Icahn School Of Medicine At Mount Sinai | Wd40 repeat domain protein 5 (wdr5) degradation / disruption compounds and methods of use |
| CN114269749B (zh) | 2019-06-10 | 2024-10-01 | 苏特罗生物制药公司 | 5H-吡咯并[3,2-d]嘧啶-2,4-二氨基化合物及其抗体偶联物 |
| WO2021021904A1 (en) | 2019-07-30 | 2021-02-04 | The Scripps Research Institute | Pharmacological inhibitors of the enl yeats domain |
| US12103924B2 (en) | 2020-06-01 | 2024-10-01 | Icahn School Of Medicine At Mount Sinai | Mitogen-activated protein kinase kinase (MEK) degradation compounds and methods of use |
| CN112778303A (zh) | 2020-12-31 | 2021-05-11 | 武汉九州钰民医药科技有限公司 | Cdk4/6激酶抑制剂shr6390的制备方法 |
-
2017
- 2017-12-07 JP JP2019530811A patent/JP2020514252A/ja active Pending
- 2017-12-07 US US16/467,888 patent/US11541051B2/en active Active
- 2017-12-07 AU AU2017370694A patent/AU2017370694A1/en not_active Abandoned
- 2017-12-07 CA CA3045037A patent/CA3045037A1/en not_active Abandoned
- 2017-12-07 EP EP17877800.7A patent/EP3551185A4/en active Pending
- 2017-12-07 CN CN201780085879.6A patent/CN110267659A/zh active Pending
- 2017-12-07 WO PCT/US2017/065027 patent/WO2018106870A1/en not_active Ceased
-
2021
- 2021-11-04 US US17/453,619 patent/US20220054488A1/en not_active Abandoned
Patent Citations (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20140031325A1 (en) * | 2010-12-06 | 2014-01-30 | Celgene Corporation | Combination therapy with lenalidomide and a cdk inhibitor for treating multiple myeloma |
| CN104736569A (zh) * | 2012-01-12 | 2015-06-24 | 耶鲁大学 | 通过e3泛素连接酶增强靶蛋白质及其他多肽降解的化合物和方法 |
| US20150274738A1 (en) * | 2012-10-19 | 2015-10-01 | Dana-Farber Cancer, Institute, Inc. | Hydrophobically tagged small molecules as inducers of protein degradation |
| WO2016105518A1 (en) * | 2014-12-23 | 2016-06-30 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| CN105085620A (zh) * | 2015-06-25 | 2015-11-25 | 中山大学附属第一医院 | 一种靶向泛素化降解Smad3的化合物 |
| WO2017185031A1 (en) * | 2016-04-22 | 2017-10-26 | Dana-Farber Cancer Institute, Inc. | Degradation of cyclin-dependent kinase 4/6 (cdk4/6) by conjugation of cdk4/6 inhibitors with e3 ligase ligand and methods of use |
| CN109071552A (zh) * | 2016-04-22 | 2018-12-21 | 达纳-法伯癌症研究所公司 | 细胞周期蛋白依赖性激酶4/6(cdk4/6)通过cdk4/6抑制剂与e3连接酶配体的缀合的降解及使用方法 |
| CN109790143A (zh) * | 2016-05-10 | 2019-05-21 | C4医药公司 | 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体 |
Non-Patent Citations (2)
| Title |
|---|
| TOURE, MOMAR等: "Small-Molecule PROTACS: New Approaches to Protein Degradation", 《ANGEWANDTE CHEMIE-INTERNATIONAL EDITION》 * |
| 费聿东等: "PROTAC及其在肿瘤治疗方面的应用", 《生命的化学》 * |
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114349738A (zh) * | 2020-10-14 | 2022-04-15 | 清华大学 | 一类靶向降解cdk2的小分子缀合物及其应用 |
| CN114349738B (zh) * | 2020-10-14 | 2023-05-05 | 清华大学 | 一类靶向降解cdk2的小分子缀合物及其应用 |
| 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 |
| WO2023104155A1 (zh) * | 2021-12-08 | 2023-06-15 | 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 |
| CN114957249A (zh) * | 2022-05-20 | 2022-08-30 | 东南大学 | 一种不可逆共价结合cdk抑制剂及其制备方法和应用 |
| CN114957249B (zh) * | 2022-05-20 | 2023-04-21 | 东南大学 | 一种不可逆共价结合cdk抑制剂及其制备方法和应用 |
| CN115650968A (zh) * | 2022-12-27 | 2023-01-31 | 英矽智能科技(上海)有限公司 | 作为cdk选择性抑制剂的新型哒嗪酮化合物 |
| WO2026067249A1 (en) * | 2024-09-29 | 2026-04-02 | K2 Medicines (Nanjing) Co., Ltd. | Cdk4 or cdk4/6 dual degrader and use thereof |
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| AU2017370694A1 (en) | 2019-07-25 |
| US20190336503A1 (en) | 2019-11-07 |
| EP3551185A4 (en) | 2021-07-14 |
| EP3551185A1 (en) | 2019-10-16 |
| CA3045037A1 (en) | 2018-06-14 |
| JP2020514252A (ja) | 2020-05-21 |
| WO2018106870A1 (en) | 2018-06-14 |
| US20220054488A1 (en) | 2022-02-24 |
| US11541051B2 (en) | 2023-01-03 |
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