CN107148419A - Zeste增强子同源物2抑制剂 - Google Patents
Zeste增强子同源物2抑制剂 Download PDFInfo
- Publication number
- CN107148419A CN107148419A CN201580058856.7A CN201580058856A CN107148419A CN 107148419 A CN107148419 A CN 107148419A CN 201580058856 A CN201580058856 A CN 201580058856A CN 107148419 A CN107148419 A CN 107148419A
- Authority
- CN
- China
- Prior art keywords
- methyl
- propyl
- oxo
- dihydropyridin
- dimethyl
- 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
- 0 CCC(C)*(*)C[N+]C/C(/*)=C(\C(C)=C)/C(*)=* Chemical compound CCC(C)*(*)C[N+]C/C(/*)=C(\C(C)=C)/C(*)=* 0.000 description 7
- CGRQDNAJUKTBKD-UHFFFAOYSA-N CCC(C(CC1)CCN1C(OC(C)(C)C)=O)c1c(C)c(C(NCC2)=O)c2[s]1 Chemical compound CCC(C(CC1)CCN1C(OC(C)(C)C)=O)c1c(C)c(C(NCC2)=O)c2[s]1 CGRQDNAJUKTBKD-UHFFFAOYSA-N 0.000 description 1
- AOVQLRKTPSEQMT-UHFFFAOYSA-N CCC(C1CCN(CC(C)(F)F)CC1)C(SC1(C)CCN2CC3=C(C)C=C(C)NC3=O)=C(C)C1C2=O Chemical compound CCC(C1CCN(CC(C)(F)F)CC1)C(SC1(C)CCN2CC3=C(C)C=C(C)NC3=O)=C(C)C1C2=O AOVQLRKTPSEQMT-UHFFFAOYSA-N 0.000 description 1
- RDRVLXIALYWMTL-UHFFFAOYSA-N CCC(C1CCN(CC(C)(F)F)CC1)c1c(C)c(C(N(CC2=C(C)C=C(C)NC2O)CC2)O)c2[s]1 Chemical compound CCC(C1CCN(CC(C)(F)F)CC1)c1c(C)c(C(N(CC2=C(C)C=C(C)NC2O)CC2)O)c2[s]1 RDRVLXIALYWMTL-UHFFFAOYSA-N 0.000 description 1
- SJBPGCIWHCAKKL-UHFFFAOYSA-N CCC(C1CCNCC1)c1c(C)c(C(N(Cc2c(C)cc(C)nc2OCc2ccccc2)CC2)=O)c2[s]1 Chemical compound CCC(C1CCNCC1)c1c(C)c(C(N(Cc2c(C)cc(C)nc2OCc2ccccc2)CC2)=O)c2[s]1 SJBPGCIWHCAKKL-UHFFFAOYSA-N 0.000 description 1
- CUSUZAPGOTUVQD-UHFFFAOYSA-N CCC(c1c(C)c(C(NCC2)=O)c2[s]1)N(CC1)CCC1N(C)C Chemical compound CCC(c1c(C)c(C(NCC2)=O)c2[s]1)N(CC1)CCC1N(C)C CUSUZAPGOTUVQD-UHFFFAOYSA-N 0.000 description 1
- KRMXYOABAHJBJQ-UHFFFAOYSA-N CCC(c1c(C)c(C(OC)=O)c[s]1)=C(CC1)CCN1C(OC(C)(C)C)=O Chemical compound CCC(c1c(C)c(C(OC)=O)c[s]1)=C(CC1)CCN1C(OC(C)(C)C)=O KRMXYOABAHJBJQ-UHFFFAOYSA-N 0.000 description 1
- LOUJIHQGULYIIH-UHFFFAOYSA-N CCC(c1c(C)c(C(OC)=O)c[s]1)=C(CC1)CCN1N(C)C Chemical compound CCC(c1c(C)c(C(OC)=O)c[s]1)=C(CC1)CCN1N(C)C LOUJIHQGULYIIH-UHFFFAOYSA-N 0.000 description 1
- CSBYRYCZAMCECL-UHFFFAOYSA-N CCC(c1c(C)c(C(OC)=O)c[s]1)=C1CCN(Cc2ncc[o]2)CC1 Chemical compound CCC(c1c(C)c(C(OC)=O)c[s]1)=C1CCN(Cc2ncc[o]2)CC1 CSBYRYCZAMCECL-UHFFFAOYSA-N 0.000 description 1
- VWMXOWPWCTXAGO-UHFFFAOYSA-N CCC(c1c(C)c(C(OC)=O)c[s]1)=C1CCNCC1 Chemical compound CCC(c1c(C)c(C(OC)=O)c[s]1)=C1CCNCC1 VWMXOWPWCTXAGO-UHFFFAOYSA-N 0.000 description 1
- RQWZJZLXHIPBPL-UHFFFAOYSA-N CCC(c1c(C)c(C(OC)=O)c[s]1)=O Chemical compound CCC(c1c(C)c(C(OC)=O)c[s]1)=O RQWZJZLXHIPBPL-UHFFFAOYSA-N 0.000 description 1
- GTNKQQKZLOXKKJ-OAHLLOKOSA-N C[C@H](C1CCN(CC(F)F)CC1)c1c(C)c(C(NCC2=C(C)C=C(C)NC2=O)=O)c[s]1 Chemical compound C[C@H](C1CCN(CC(F)F)CC1)c1c(C)c(C(NCC2=C(C)C=C(C)NC2=O)=O)c[s]1 GTNKQQKZLOXKKJ-OAHLLOKOSA-N 0.000 description 1
- FCKSGPKSSPUXOP-UHFFFAOYSA-N Cc1c[s]cc1C(OC)=O Chemical compound Cc1c[s]cc1C(OC)=O FCKSGPKSSPUXOP-UHFFFAOYSA-N 0.000 description 1
- RAOBXCQKFIXLOW-UHFFFAOYSA-N Cc1cc(C)nc(OCCc2ccccc2)c1CCl Chemical compound Cc1cc(C)nc(OCCc2ccccc2)c1CCl RAOBXCQKFIXLOW-UHFFFAOYSA-N 0.000 description 1
- HRARFISHYLFDSY-UHFFFAOYSA-N Cc1cc(C)nc(OCc2ccccc2)c1CCl Chemical compound Cc1cc(C)nc(OCc2ccccc2)c1CCl HRARFISHYLFDSY-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero 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
- A61K31/435—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
- A61K31/4436—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
-
- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4535—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/06—Peri-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (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)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462069438P | 2014-10-28 | 2014-10-28 | |
| US62/069,438 | 2014-10-28 | ||
| US201462075596P | 2014-11-05 | 2014-11-05 | |
| US62/075,596 | 2014-11-05 | ||
| PCT/EP2015/075009 WO2016066697A1 (en) | 2014-10-28 | 2015-10-28 | Enhancer of zeste homolog 2 inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN107148419A true CN107148419A (zh) | 2017-09-08 |
Family
ID=54360465
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201580058856.7A Pending CN107148419A (zh) | 2014-10-28 | 2015-10-28 | Zeste增强子同源物2抑制剂 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20170334891A1 (https=) |
| EP (1) | EP3212639A1 (https=) |
| JP (1) | JP6571180B2 (https=) |
| KR (1) | KR20170068603A (https=) |
| CN (1) | CN107148419A (https=) |
| AU (1) | AU2015340614B2 (https=) |
| BR (1) | BR112017008840A2 (https=) |
| CA (1) | CA2965729A1 (https=) |
| MA (1) | MA40848A (https=) |
| RU (1) | RU2017118165A (https=) |
| WO (1) | WO2016066697A1 (https=) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110950834A (zh) * | 2019-11-26 | 2020-04-03 | 济南大学 | 新型eed-ezh2相互作用小分子抑制剂的确定和评价 |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UY36758A (es) * | 2015-06-30 | 2016-12-30 | Glaxosmithkline Ip No 2 Ltd | Inhibidores del potenciador del homólogo zeste 2 |
| TW201718598A (zh) | 2015-08-27 | 2017-06-01 | 美國禮來大藥廠 | Ｅｚｈ２抑制劑 |
| CA3023157A1 (en) * | 2016-05-05 | 2017-11-09 | Glaxosmithkline Intellectual Property (No.2) Limited | Enhancer of zeste homolog 2 inhibitors |
| JP7125353B2 (ja) | 2017-01-19 | 2022-08-24 | 第一三共株式会社 | Ｈｔｌｖ－１関連脊髄症を治療することに用いるための医薬組成物 |
| US10266542B2 (en) | 2017-03-15 | 2019-04-23 | Mirati Therapeutics, Inc. | EZH2 inhibitors |
| WO2018177993A1 (de) | 2017-03-31 | 2018-10-04 | Bayer Cropscience Aktiengesellschaft | Pyrazole zur bekämpfung von arthropoden |
| DK3746446T3 (da) | 2018-01-31 | 2022-06-27 | Mirati Therapeutics Inc | PRC2-inhibitorer |
| CN120097995A (zh) | 2018-05-21 | 2025-06-06 | 星座制药公司 | 甲基修饰酶的调节剂、其组合物和用途 |
| CA3104209A1 (en) | 2018-07-09 | 2020-01-16 | Fondation Asile Des Aveugles | Inhibition of prc2 subunits to treat eye disorders |
| US12421228B2 (en) | 2019-04-22 | 2025-09-23 | Mirati Therapeutics, Inc. | Naphthyridine derivatives as PRC2 inhibitors |
| US12252493B2 (en) | 2019-06-05 | 2025-03-18 | Mirati Therapeutics, Inc. | Imidazo[1,2-c]pyrimidine derivatives as PRC2 inhibitors for treating cancer |
| WO2021016409A1 (en) * | 2019-07-24 | 2021-01-28 | Constellation Pharmaceuticals, Inc. | Ezh2 inhibition in combination therapies for the treatment of cancers |
| WO2021016414A1 (en) | 2019-07-24 | 2021-01-28 | Constellation Pharmaceuticals, Inc. | Crystalline forms of 7-chloro-2-(4-(3-methoxyazetidin-1-yl)cyclohexyl)-2,4-dimethyl-n-((6-methyl-4-(methylthio)-2-oxo-1,2-dihydropyridin-3-yl)methyl)benzo[d][1,3]dioxole-5-carboxamide |
| JP2022545467A (ja) | 2019-08-22 | 2022-10-27 | ジュノー セラピューティクス インコーポレイテッド | Ｔ細胞療法とｚｅｓｔｅホモログ２エンハンサー（ＥＺＨ２）阻害剤との併用療法および関連方法 |
| TW202400140A (zh) | 2022-04-27 | 2024-01-01 | 日商第一三共股份有限公司 | 抗體-藥物結合物與ezh1及/或ezh2抑制劑之組合 |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012142513A1 (en) * | 2011-04-13 | 2012-10-18 | Epizyme, Inc. | Substituted benzene compounds |
| CN102970869A (zh) * | 2010-05-07 | 2013-03-13 | 葛兰素史密斯克莱有限责任公司 | 吲哚 |
| CN104080769A (zh) * | 2011-04-13 | 2014-10-01 | Epizyme股份有限公司 | 芳基或杂芳基取代苯化合物 |
| WO2014177982A1 (en) * | 2013-04-30 | 2014-11-06 | Glaxosmithkline Intellectual Property (No.2) Limited | Enhancer of zeste homolog 2 inhibitors |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112014010803A2 (pt) * | 2011-11-04 | 2017-04-25 | Glaxosmithkline Intellectual Property (No 2) Ltd | método de tratamento |
| NZ628762A (en) * | 2012-02-10 | 2016-07-29 | Constellation Pharmaceuticals Inc | Modulators of methyl modifying enzymes, compositions and uses thereof |
| UA111305C2 (uk) * | 2012-12-21 | 2016-04-11 | Пфайзер Інк. | Конденсовані лактами арилу та гетероарилу |
| KR20160030221A (ko) * | 2013-07-10 | 2016-03-16 | 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 | 제스트 인핸서 상동체 2 억제제 |
-
2015
- 2015-10-28 CN CN201580058856.7A patent/CN107148419A/zh active Pending
- 2015-10-28 KR KR1020177014034A patent/KR20170068603A/ko not_active Withdrawn
- 2015-10-28 RU RU2017118165A patent/RU2017118165A/ru not_active Application Discontinuation
- 2015-10-28 AU AU2015340614A patent/AU2015340614B2/en not_active Ceased
- 2015-10-28 JP JP2017522890A patent/JP6571180B2/ja not_active Expired - Fee Related
- 2015-10-28 MA MA040848A patent/MA40848A/fr unknown
- 2015-10-28 BR BR112017008840A patent/BR112017008840A2/pt not_active Application Discontinuation
- 2015-10-28 CA CA2965729A patent/CA2965729A1/en not_active Abandoned
- 2015-10-28 US US15/522,373 patent/US20170334891A1/en not_active Abandoned
- 2015-10-28 EP EP15786958.7A patent/EP3212639A1/en not_active Withdrawn
- 2015-10-28 WO PCT/EP2015/075009 patent/WO2016066697A1/en not_active Ceased
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102970869A (zh) * | 2010-05-07 | 2013-03-13 | 葛兰素史密斯克莱有限责任公司 | 吲哚 |
| WO2012142513A1 (en) * | 2011-04-13 | 2012-10-18 | Epizyme, Inc. | Substituted benzene compounds |
| CN104080769A (zh) * | 2011-04-13 | 2014-10-01 | Epizyme股份有限公司 | 芳基或杂芳基取代苯化合物 |
| WO2014177982A1 (en) * | 2013-04-30 | 2014-11-06 | Glaxosmithkline Intellectual Property (No.2) Limited | Enhancer of zeste homolog 2 inhibitors |
| CN105308038A (zh) * | 2013-04-30 | 2016-02-03 | 葛兰素史密斯克莱知识产权（第2号）有限公司 | Zeste增强子同源物2的抑制剂 |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110950834A (zh) * | 2019-11-26 | 2020-04-03 | 济南大学 | 新型eed-ezh2相互作用小分子抑制剂的确定和评价 |
Also Published As
| Publication number | Publication date |
|---|---|
| EP3212639A1 (en) | 2017-09-06 |
| KR20170068603A (ko) | 2017-06-19 |
| RU2017118165A (ru) | 2018-11-29 |
| US20170334891A1 (en) | 2017-11-23 |
| MA40848A (fr) | 2021-05-05 |
| BR112017008840A2 (pt) | 2017-12-19 |
| WO2016066697A1 (en) | 2016-05-06 |
| AU2015340614A1 (en) | 2017-05-18 |
| JP6571180B2 (ja) | 2019-09-04 |
| RU2017118165A3 (https=) | 2018-12-10 |
| JP2017532360A (ja) | 2017-11-02 |
| AU2015340614B2 (en) | 2018-07-19 |
| CA2965729A1 (en) | 2016-05-06 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| AD01 | Patent right deemed abandoned | ||
| AD01 | Patent right deemed abandoned |
Effective date of abandoning: 20210319 |