CA3018270A1 - Ezh2 inhibitors and uses thereof - Google Patents
Ezh2 inhibitors and uses thereof Download PDFInfo
- Publication number
- CA3018270A1 CA3018270A1 CA3018270A CA3018270A CA3018270A1 CA 3018270 A1 CA3018270 A1 CA 3018270A1 CA 3018270 A CA3018270 A CA 3018270A CA 3018270 A CA3018270 A CA 3018270A CA 3018270 A1 CA3018270 A1 CA 3018270A1
- Authority
- CA
- Canada
- Prior art keywords
- substituted
- unsubstituted
- compound
- formula
- 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
-
- 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
- C07D405/14—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 three or more hetero rings
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Obesity (AREA)
- Psychiatry (AREA)
- Oncology (AREA)
- Rheumatology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pyridine Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662326036P | 2016-04-22 | 2016-04-22 | |
| US62/326,036 | 2016-04-22 | ||
| PCT/US2017/028885 WO2017184999A1 (en) | 2016-04-22 | 2017-04-21 | Ezh2 inhibitors and uses thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA3018270A1 true CA3018270A1 (en) | 2017-10-26 |
Family
ID=60116436
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3018270A Pending CA3018270A1 (en) | 2016-04-22 | 2017-04-21 | Ezh2 inhibitors and uses thereof |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US10633371B2 (enExample) |
| EP (1) | EP3445365A4 (enExample) |
| JP (1) | JP7493304B2 (enExample) |
| CN (1) | CN109069508A (enExample) |
| AU (1) | AU2017252460B2 (enExample) |
| CA (1) | CA3018270A1 (enExample) |
| WO (1) | WO2017184999A1 (enExample) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016073956A1 (en) | 2014-11-06 | 2016-05-12 | Dana-Farber Cancer Institute, Inc. | Ezh2 inhibitors and uses thereof |
| US11191741B2 (en) | 2016-12-24 | 2021-12-07 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide |
| CN108314677B (zh) * | 2017-01-17 | 2020-06-30 | 安徽中科拓苒药物科学研究有限公司 | 一种ezh2抑制剂及其用途 |
| US10266542B2 (en) | 2017-03-15 | 2019-04-23 | Mirati Therapeutics, Inc. | EZH2 inhibitors |
| CN109942556A (zh) * | 2017-12-21 | 2019-06-28 | 上海青煜医药科技有限公司 | 嘧啶酮化合物及其应用 |
| PT4043466T (pt) | 2018-01-31 | 2024-10-14 | Mirati Therapeutics Inc | Inibidores de prc2 |
| CN110229151B (zh) * | 2018-03-06 | 2021-09-10 | 上海海和药物研究开发股份有限公司 | 吲嗪类化合物、其制备方法及用途 |
| WO2020011607A1 (en) | 2018-07-09 | 2020-01-16 | Fondation Asile Des Aveugles | Inhibition of prc2 subunits to treat eye disorders |
| EP3959214A1 (en) | 2019-04-22 | 2022-03-02 | Mirati Therapeutics, Inc. | Naphthyridine derivatives as prc2 inhibitors |
| TWI747121B (zh) * | 2019-05-21 | 2021-11-21 | 大江生醫股份有限公司 | 茶樹葉的發酵物用於調控CCT基因、Pink1基因、PARP2基因、MITF基因、UNG基因、ERCC6基因、TERC基因、CD40基因、DYNLL2基因、GRK5基因、RELB基因、TNFSF14基因、IL4R基因與RELA基因的表現量及抗老化、美白、提升免疫力與降低脂肪累積之用途 |
| EP3980422A1 (en) | 2019-06-05 | 2022-04-13 | Mirati Therapeutics, Inc. | Imidazo[1,2-c]pyrimidine derivatives as prc2 inhibitors for treating cancer |
| CN112341390B (zh) * | 2019-08-07 | 2022-08-23 | 四川大学 | 用于制备靶向组蛋白甲基转移酶ezh2共价抑制剂的化合物及其制备方法和用途 |
| AR126670A1 (es) * | 2021-08-02 | 2023-11-01 | Eurofarma Laboratorios S A | COMPUESTOS N-ACILIDRAZÓNICOS INHIBIDORES DE Nav 1.7 Y/O Nav 1.8, SUS PROCESOS DE OBTENCIÓN, COMPOSICIONES, USOS, MÉTODOS DE TRATAMIENTO DE ESTOS Y KITS |
| CN115197202B (zh) * | 2022-07-15 | 2024-01-26 | 四川大学 | 一种ezh2共价抑制剂及其制备方法和应用 |
| AR131658A1 (es) * | 2023-01-30 | 2025-04-16 | Eurofarma Laboratorios S A | Hidrazidas bloqueadoras de nav 1.7 y/o nav 1.8, sus procesos de obtención, composiciones, usos, métodos de tratamiento de los mismos y sus kits |
| TW202508595A (zh) | 2023-05-04 | 2025-03-01 | 美商銳新醫藥公司 | 用於ras相關疾病或病症之組合療法 |
| WO2025034702A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Rmc-6291 for use in the treatment of ras protein-related disease or disorder |
| WO2025080946A2 (en) | 2023-10-12 | 2025-04-17 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| US20250313530A1 (en) * | 2024-04-05 | 2025-10-09 | Trustees Of Boston University | Small molecule inhibitors of interleukin-4 and uses thereof |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
Family Cites Families (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008066887A2 (en) | 2006-11-30 | 2008-06-05 | Albert Einstein College Of Medicine Of Yeshiva University | Small molecule inhibitors of bcl6 |
| KR20080107050A (ko) | 2007-06-05 | 2008-12-10 | 울산대학교 산학협력단 | 항-cd137 단일클론 항체를 포함하는 만성이식편대숙주 질환의 예방 또는 치료용 약학적 조성물 |
| US7989465B2 (en) * | 2007-10-19 | 2011-08-02 | Avila Therapeutics, Inc. | 4,6-disubstituted pyrimidines useful as kinase inhibitors |
| WO2010008436A1 (en) | 2008-06-24 | 2010-01-21 | Albert Einstein College Of Medicine Of Yeshiva University | Methods and compositions for inhibition of bcl6 repression |
| PL2459792T3 (pl) | 2009-07-31 | 2015-01-30 | Lg Electronics Inc | Pralka |
| US9423331B2 (en) * | 2010-04-14 | 2016-08-23 | Mobrey Limited | Method of determining the energy content of a methane-rich gas mixture |
| US8637509B2 (en) | 2010-05-07 | 2014-01-28 | Glaxosmithkline Llc | Azaindazoles |
| EP2566327B1 (en) | 2010-05-07 | 2017-03-29 | Glaxosmithkline LLC | Indoles |
| HUE031073T2 (en) | 2010-05-14 | 2017-06-28 | Dana Farber Cancer Inst Inc | Thieno triazolo-diazepine compounds for the treatment of neoplasia |
| US20120014979A1 (en) | 2010-07-16 | 2012-01-19 | Alexander Dent | Use of bcl6 inhibitors for treating autoimmune diseases |
| US9175331B2 (en) | 2010-09-10 | 2015-11-03 | Epizyme, Inc. | Inhibitors of human EZH2, and methods of use thereof |
| PL2614369T3 (pl) * | 2010-09-10 | 2016-08-31 | Epizyme Inc | Sposób określania przydatności inhibitorów ludzkiego ezh2 w leczeniu |
| JP2014511389A (ja) | 2011-02-28 | 2014-05-15 | エピザイム インコーポレイテッド | 置換6,5−縮合二環式ヘテロアリール化合物 |
| JO3438B1 (ar) * | 2011-04-13 | 2019-10-20 | Epizyme Inc | مركبات بنزين مستبدلة بأريل أو أريل غير متجانس |
| EP2755962B1 (en) | 2011-09-13 | 2017-03-01 | Glaxosmithkline LLC | Azaindazoles |
| BR112014007603A2 (pt) | 2011-09-30 | 2017-06-13 | Glaxosmithkline Llc | métodos de tratamento do câncer |
| KR20140095073A (ko) | 2011-11-04 | 2014-07-31 | 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 | 치료 방법 |
| WO2013067300A1 (en) | 2011-11-04 | 2013-05-10 | Glaxosmithkline Intellectual Property (No. 2) Limited | Method of treatment |
| WO2013067302A1 (en) | 2011-11-04 | 2013-05-10 | Glaxosmithkline Intellectual Property (No. 2) Limited | Method of treatment |
| WO2013074986A1 (en) * | 2011-11-17 | 2013-05-23 | Dana-Farber Cancer Institute, Inc. | Inhibitors of c-jun-n-terminal kinase (jnk) |
| US10579982B2 (en) * | 2012-01-03 | 2020-03-03 | International Business Machines Corporation | Identifying money laundering in micro-commerce |
| JP2015508780A (ja) | 2012-02-17 | 2015-03-23 | アンサン バイオファーマ,インコーポレイテッド | 免疫不全患者のインフルエンザ及びパラインフルエンザウイルスを処置するための方法、化合物、及び組成物 |
| EP2825161B1 (en) * | 2012-03-12 | 2019-01-02 | Epizyme, Inc. | Inhibitors of human ezh2, and methods of use thereof |
| CN104768555B (zh) * | 2012-04-13 | 2018-10-30 | Epizyme股份有限公司 | 用于治疗癌症的联合治疗 |
| WO2013173441A2 (en) * | 2012-05-16 | 2013-11-21 | Glaxosmithkline Llc | Enhancer of zeste homolog 2 inhibitors |
| DE102012011464A1 (de) * | 2012-06-12 | 2013-12-12 | Merck Patent Gmbh | Verfahren zur Erzeugung von dreidimensionalen Mustern in flüssigkristallinen Beschichtungen |
| SG10201705989YA (en) * | 2012-10-15 | 2017-08-30 | Epizyme Inc | Substituted benzene compounds |
| BR112015014090A2 (pt) * | 2012-12-13 | 2017-07-11 | Glaxosmithkline Llc | intensificador de inibidores de zeste homólogo 2 |
| WO2014100080A1 (en) | 2012-12-19 | 2014-06-26 | Glaxosmithkline Llc | Combination |
| AU2013361060B2 (en) | 2012-12-21 | 2018-04-19 | Epizyme, Inc. | 1,4-pyridone compounds |
| CA2894222A1 (en) | 2012-12-21 | 2014-06-26 | Epizyme, Inc. | 1,4-pyridone bicyclic heteroaryl compounds |
| US20160031907A1 (en) * | 2013-03-15 | 2016-02-04 | Epizyme, Inc. | Substituted Benzene Compounds |
| WO2014155301A1 (en) | 2013-03-26 | 2014-10-02 | Piramal Enterprises Limited | Substituted bicyclic compounds as inhibitors of ezh2 |
| WO2015010049A1 (en) * | 2013-07-19 | 2015-01-22 | Epizyme, Inc. | Substituted benzene compounds |
| WO2015077193A1 (en) * | 2013-11-19 | 2015-05-28 | Bristol-Myers Squibb Company | Inhibitors of lysine methyl transferase |
| WO2015110999A1 (en) * | 2014-01-24 | 2015-07-30 | Piramal Enterprises Limited | Ezh2 inhibitors and uses thereof |
| WO2016073903A1 (en) | 2014-11-06 | 2016-05-12 | Dana-Farber Cancer Institute, Inc. | Use of compositions modulating chromatin structure for graft versus host disease (gvhd) |
| WO2016073956A1 (en) | 2014-11-06 | 2016-05-12 | Dana-Farber Cancer Institute, Inc. | Ezh2 inhibitors and uses thereof |
-
2017
- 2017-04-21 CN CN201780025008.5A patent/CN109069508A/zh active Pending
- 2017-04-21 JP JP2018555500A patent/JP7493304B2/ja active Active
- 2017-04-21 EP EP17786731.4A patent/EP3445365A4/en not_active Withdrawn
- 2017-04-21 US US16/095,188 patent/US10633371B2/en active Active
- 2017-04-21 WO PCT/US2017/028885 patent/WO2017184999A1/en not_active Ceased
- 2017-04-21 AU AU2017252460A patent/AU2017252460B2/en not_active Ceased
- 2017-04-21 CA CA3018270A patent/CA3018270A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| EP3445365A4 (en) | 2019-10-16 |
| EP3445365A1 (en) | 2019-02-27 |
| US10633371B2 (en) | 2020-04-28 |
| JP2019514884A (ja) | 2019-06-06 |
| AU2017252460B2 (en) | 2021-11-18 |
| US20190135796A1 (en) | 2019-05-09 |
| CN109069508A (zh) | 2018-12-21 |
| AU2017252460A1 (en) | 2018-10-11 |
| WO2017184999A1 (en) | 2017-10-26 |
| JP7493304B2 (ja) | 2024-05-31 |
| US20200039968A9 (en) | 2020-02-06 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request |
Effective date: 20220324 |
|
| EEER | Examination request |
Effective date: 20220324 |
|
| EEER | Examination request |
Effective date: 20220324 |