AU2017252460B2 - EZH2 inhibitors and uses thereof - Google Patents
EZH2 inhibitors and uses thereof Download PDFInfo
- Publication number
- AU2017252460B2 AU2017252460B2 AU2017252460A AU2017252460A AU2017252460B2 AU 2017252460 B2 AU2017252460 B2 AU 2017252460B2 AU 2017252460 A AU2017252460 A AU 2017252460A AU 2017252460 A AU2017252460 A AU 2017252460A AU 2017252460 B2 AU2017252460 B2 AU 2017252460B2
- Authority
- AU
- Australia
- Prior art keywords
- substituted
- unsubstituted
- certain embodiments
- alkyl
- compound
- 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.)
- Ceased
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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)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hematology (AREA)
- Biomedical Technology (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Obesity (AREA)
- Rheumatology (AREA)
- Psychiatry (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pyridine Compounds (AREA)
- Plural Heterocyclic Compounds (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 (2)
| Publication Number | Publication Date |
|---|---|
| AU2017252460A1 AU2017252460A1 (en) | 2018-10-11 |
| AU2017252460B2 true AU2017252460B2 (en) | 2021-11-18 |
Family
ID=60116436
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2017252460A Ceased AU2017252460B2 (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 (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107105651A (zh) | 2014-11-06 | 2017-08-29 | 达纳-法伯癌症研究所股份有限公司 | Ezh2抑制剂及其用途 |
| 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 |
| WO2019152419A1 (en) | 2018-01-31 | 2019-08-08 | Mirati Therapeutics, Inc | Prc2 inhibitors |
| 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 |
| JP2021531340A (ja) | 2018-07-09 | 2021-11-18 | フォンダシヨン、アジール、デ、アブグルスFondation Asile Des Aveugles | 眼障害を治療するためのprc2サブユニットの阻害 |
| JP7624404B2 (ja) | 2019-04-22 | 2025-01-30 | ミラティ セラピューティクス,インク. | Prc2阻害剤としてのナフチリジン誘導体 |
| 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 |
| WO2020247475A1 (en) | 2019-06-05 | 2020-12-10 | 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 |
| UY39882A (es) * | 2021-08-02 | 2023-06-15 | Eurofarma Laboratorios S A | COMPUESTOS NACILHIDRAZÓNICOS 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 |
| WO2024229406A1 (en) | 2023-05-04 | 2024-11-07 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025213129A1 (en) * | 2024-04-05 | 2025-10-09 | Trustees Of Boston University | Novel small molecule inhibitors of interleukin-4 and uses thereof |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012142504A1 (en) * | 2011-04-13 | 2012-10-18 | Epizyme, Inc. | Aryl-or heteroaryl-substituted benzene compounds |
| WO2013173441A2 (en) * | 2012-05-16 | 2013-11-21 | Glaxosmithkline Llc | Enhancer of zeste homolog 2 inhibitors |
| WO2014100646A1 (en) * | 2012-12-21 | 2014-06-26 | Epizyme, Inc. | 1,4-pyridone compounds |
| WO2015110999A1 (en) * | 2014-01-24 | 2015-07-30 | Piramal Enterprises Limited | Ezh2 inhibitors and uses thereof |
| US9175331B2 (en) * | 2010-09-10 | 2015-11-03 | Epizyme, Inc. | Inhibitors of human EZH2, and methods of use thereof |
Family Cites Families (33)
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| 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 |
| US8791075B2 (en) | 2008-06-24 | 2014-07-29 | 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 |
| EP2558853B1 (en) * | 2010-04-14 | 2020-08-19 | Rosemount Measurement Limited | Methods and apparatuses of determining the energy content of a methan-rich gas mixture |
| ES2528269T3 (es) | 2010-05-07 | 2015-02-06 | Glaxosmithkline Llc | Azaindazoles |
| PH12012502194A1 (en) | 2010-05-07 | 2014-09-05 | Glaxosmithkline Llc | Indoles |
| PL2571503T3 (pl) | 2010-05-14 | 2015-06-30 | Dana Farber Cancer Inst Inc | Kompozycje i sposoby leczenia nowotworu, choroby zapalnej i innych zaburzeń |
| US20120014979A1 (en) | 2010-07-16 | 2012-01-19 | Alexander Dent | Use of bcl6 inhibitors for treating autoimmune diseases |
| AU2011298987B2 (en) * | 2010-09-10 | 2017-09-28 | Epizyme, Inc. | Inhibitors of human EZH2, and methods of use thereof |
| EP2681216B1 (en) | 2011-02-28 | 2017-09-27 | Epizyme, Inc. | Substituted 6,5-fused bicyclic heteroaryl compounds |
| ES2624986T3 (es) | 2011-09-13 | 2017-07-18 | Glaxosmithkline Llc | Azaindazoles |
| EP2760452A4 (en) | 2011-09-30 | 2015-04-01 | Glaxosmithkline Llc | METHODS OF TREATING CANCER |
| 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 |
| AU2012332297B2 (en) | 2011-11-04 | 2016-01-07 | Glaxosmithkline Intellectual Property (No.2) Limited | Method of treatment |
| EP3569598A1 (en) | 2011-11-17 | 2019-11-20 | 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 |
| CN104203267A (zh) | 2012-02-17 | 2014-12-10 | 安迅生物制药公司 | 用于治疗流感和副流感患者的方法、化合物和组合物 |
| TR201904660T4 (tr) * | 2012-03-12 | 2019-05-21 | Epizyme Inc | İnsan EZH2 inhibitörleri ve bunun kullanım yöntemleri. |
| IL308807B2 (en) * | 2012-04-13 | 2025-08-01 | Epizyme Inc | Combination therapy for treating cancer |
| DE102012011464A1 (de) * | 2012-06-12 | 2013-12-12 | Merck Patent Gmbh | Verfahren zur Erzeugung von dreidimensionalen Mustern in flüssigkristallinen Beschichtungen |
| PE20150886A1 (es) | 2012-10-15 | 2015-06-04 | Epizyme Inc | Compuestos de benceno sustituidos |
| BR112015014090A2 (pt) | 2012-12-13 | 2017-07-11 | Glaxosmithkline Llc | intensificador de inibidores de zeste homólogo 2 |
| US20150313906A1 (en) | 2012-12-19 | 2015-11-05 | Glaxosmithkline Llc | Combination |
| AU2013361079B2 (en) | 2012-12-21 | 2018-07-26 | Epizyme, Inc. | 1,4-pyridone bicyclic heteroaryl compounds |
| EP2970281A4 (en) | 2013-03-15 | 2016-08-03 | Epizyme Inc | SUBSTITUTED BENZOL 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 |
| CA2966336A1 (en) | 2014-11-06 | 2016-05-12 | Dana-Farber Cancer Institute, Inc. | Use of compositions modulating chromatin structure for graft versus host disease (gvhd) |
| CN107105651A (zh) | 2014-11-06 | 2017-08-29 | 达纳-法伯癌症研究所股份有限公司 | Ezh2抑制剂及其用途 |
-
2017
- 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 CN CN201780025008.5A patent/CN109069508A/zh active Pending
- 2017-04-21 CA CA3018270A patent/CA3018270A1/en 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
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9175331B2 (en) * | 2010-09-10 | 2015-11-03 | Epizyme, Inc. | Inhibitors of human EZH2, and methods of use thereof |
| WO2012142504A1 (en) * | 2011-04-13 | 2012-10-18 | Epizyme, Inc. | Aryl-or heteroaryl-substituted benzene compounds |
| US8410088B2 (en) * | 2011-04-13 | 2013-04-02 | Epizyme, Inc. | Aryl- or heteroaryl-substituted benzene compounds |
| WO2013173441A2 (en) * | 2012-05-16 | 2013-11-21 | Glaxosmithkline Llc | Enhancer of zeste homolog 2 inhibitors |
| WO2014100646A1 (en) * | 2012-12-21 | 2014-06-26 | Epizyme, Inc. | 1,4-pyridone compounds |
| WO2015110999A1 (en) * | 2014-01-24 | 2015-07-30 | Piramal Enterprises Limited | Ezh2 inhibitors and uses thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| US10633371B2 (en) | 2020-04-28 |
| WO2017184999A1 (en) | 2017-10-26 |
| JP2019514884A (ja) | 2019-06-06 |
| EP3445365A1 (en) | 2019-02-27 |
| AU2017252460A1 (en) | 2018-10-11 |
| US20190135796A1 (en) | 2019-05-09 |
| JP7493304B2 (ja) | 2024-05-31 |
| CN109069508A (zh) | 2018-12-21 |
| EP3445365A4 (en) | 2019-10-16 |
| US20200039968A9 (en) | 2020-02-06 |
| CA3018270A1 (en) | 2017-10-26 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FGA | Letters patent sealed or granted (standard patent) | ||
| MK14 | Patent ceased section 143(a) (annual fees not paid) or expired |