JP6370368B2 - Ｂｒｄ４阻害剤としてのインドリノン類似体 - Google Patents
Ｂｒｄ４阻害剤としてのインドリノン類似体 Download PDFInfo
- Publication number
- JP6370368B2 JP6370368B2 JP2016504660A JP2016504660A JP6370368B2 JP 6370368 B2 JP6370368 B2 JP 6370368B2 JP 2016504660 A JP2016504660 A JP 2016504660A JP 2016504660 A JP2016504660 A JP 2016504660A JP 6370368 B2 JP6370368 B2 JP 6370368B2
- Authority
- JP
- Japan
- Prior art keywords
- mmol
- phenyl
- alkyl
- methyl
- hplc
- 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.)
- Active
Links
- VINNLHYHAHJONU-UHFFFAOYSA-N CN(C(c1c2ccc(Br)c1)c1cc(OC)cc(F)c1)C2=O Chemical compound CN(C(c1c2ccc(Br)c1)c1cc(OC)cc(F)c1)C2=O VINNLHYHAHJONU-UHFFFAOYSA-N 0.000 description 1
- VTZIDOPGFQUXPS-VZUCSPMQSA-N COc(c(Br)ccc1)c1NC(/C=N/O)=O Chemical compound COc(c(Br)ccc1)c1NC(/C=N/O)=O VTZIDOPGFQUXPS-VZUCSPMQSA-N 0.000 description 1
- IVMKXIZCOKJNRN-UHFFFAOYSA-N Cc1n[o]c(C)c1-c(cc1)c(C)c(C(c2ccccc2)O2)c1C2=O Chemical compound Cc1n[o]c(C)c1-c(cc1)c(C)c(C(c2ccccc2)O2)c1C2=O IVMKXIZCOKJNRN-UHFFFAOYSA-N 0.000 description 1
- 0 OC(*1)(c2cc(C(F)(F)F)ccc2C1=O)c1ccccc1 Chemical compound OC(*1)(c2cc(C(F)(F)F)ccc2C1=O)c1ccccc1 0.000 description 1
- LGIHPJSPFIMXBZ-UHFFFAOYSA-N OC(c1cc(I)ccc1N1)(C1=O)c1ccccc1 Chemical compound OC(c1cc(I)ccc1N1)(C1=O)c1ccccc1 LGIHPJSPFIMXBZ-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13161486 | 2013-03-27 | ||
| EP13161486.9 | 2013-03-27 | ||
| PCT/EP2014/056079 WO2014154760A1 (en) | 2013-03-27 | 2014-03-26 | Indolinone analogues as brd4 inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016515560A JP2016515560A (ja) | 2016-05-30 |
| JP2016515560A5 JP2016515560A5 (2) | 2017-04-27 |
| JP6370368B2 true JP6370368B2 (ja) | 2018-08-08 |
Family
ID=47997211
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016504660A Active JP6370368B2 (ja) | 2013-03-27 | 2014-03-26 | Ｂｒｄ４阻害剤としてのインドリノン類似体 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US9102684B2 (2) |
| EP (1) | EP2978757B1 (2) |
| JP (1) | JP6370368B2 (2) |
| WO (1) | WO2014154760A1 (2) |
Families Citing this family (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9266891B2 (en) | 2012-11-16 | 2016-02-23 | Boehringer Ingelheim International Gmbh | Substituted [1,2,4]triazolo[4,3-A]pyrazines that are BRD4 inhibitors |
| US9073878B2 (en) | 2012-11-21 | 2015-07-07 | Zenith Epigenetics Corp. | Cyclic amines as bromodomain inhibitors |
| US9765039B2 (en) | 2012-11-21 | 2017-09-19 | Zenith Epigenetics Ltd. | Biaryl derivatives as bromodomain inhibitors |
| AU2013365926B9 (en) | 2012-12-21 | 2019-01-17 | Zenith Epigenetics Ltd. | Novel heterocyclic compounds as bromodomain inhibitors |
| MX366703B (es) | 2013-03-15 | 2019-07-22 | Incyte Holdings Corp | Heterociclos tricíclicos como inhibidores de la proteína bet. |
| EA027139B1 (ru) | 2013-04-26 | 2017-06-30 | Бейджин, Лтд. | Замещенные 5-(3,5-диметилизоксазол-4-ил)индолин-2-оны |
| CA2915838C (en) | 2013-06-21 | 2023-04-18 | Zenith Epigenetics Corp. | Bicyclic bromodomain inhibitors |
| EP3010918B1 (en) | 2013-06-21 | 2018-08-15 | Zenith Epigenetics Ltd. | Novel substituted bicyclic compounds as bromodomain inhibitors |
| AR096837A1 (es) | 2013-07-08 | 2016-02-03 | Incyte Corp | Heterociclos tricíclicos como inhibidores de proteínas bet |
| JP6542212B2 (ja) | 2013-07-31 | 2019-07-10 | ゼニス・エピジェネティクス・リミテッドＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｌｔｄ． | ブロモドメイン阻害剤としての新規キナゾリノン |
| WO2015081189A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| US9399640B2 (en) | 2013-11-26 | 2016-07-26 | Incyte Corporation | Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors |
| WO2015095492A1 (en) | 2013-12-19 | 2015-06-25 | Incyte Corporation | Tricyclic heterocycles as bet protein inhibitors |
| EA034972B1 (ru) | 2014-04-23 | 2020-04-13 | Инсайт Корпорейшн | 1h-пирроло[2,3-c]пиридин-7(6h)-оны в качестве ингибиторов белков bet |
| US9902702B2 (en) * | 2014-07-15 | 2018-02-27 | Bristol-Myers Squibb Company | Spirocycloheptanes as inhibitors of rock |
| US9527864B2 (en) | 2014-09-15 | 2016-12-27 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| CN107429246B (zh) | 2014-10-31 | 2021-06-01 | 麻省理工学院 | 用于crispr的大规模并行组合遗传学 |
| HK1246273B (en) | 2014-12-01 | 2019-12-06 | 恒翼生物医药(上海)股份有限公司 | Substituted pyridines as bromodomain inhibitors |
| EP3227281A4 (en) | 2014-12-01 | 2018-05-30 | Zenith Epigenetics Ltd. | Substituted pyridinones as bromodomain inhibitors |
| EP3230277B1 (en) | 2014-12-11 | 2019-09-18 | Zenith Epigenetics Ltd. | Substituted heterocycles as bromodomain inhibitors |
| HK1245247A1 (zh) | 2014-12-17 | 2018-08-24 | 恒翼生物医药科技(上海)有限公司 | 溴结构域的抑制剂 |
| JP2018527293A (ja) * | 2015-06-16 | 2018-09-20 | オリオン コーポレーション | ブロモドメイン阻害剤としてのスピロ［シクロブタン−１，３’−インドリン］−２’−オン誘導体 |
| WO2016203335A1 (en) | 2015-06-18 | 2016-12-22 | Pfizer Inc. | Novel pyrido[2,3-b]pyrazinones as bet-family bromodomain inhibitors |
| TW201722966A (zh) | 2015-10-29 | 2017-07-01 | 英塞特公司 | Bet蛋白質抑制劑之非晶固體形式 |
| KR102643344B1 (ko) | 2016-06-20 | 2024-03-07 | 인사이트 코포레이션 | Bet 저해제의 결정질 고체 형태 |
| WO2018109271A1 (en) * | 2016-12-13 | 2018-06-21 | Orion Corporation | New bromodomain inhibitors |
| CN107739370B (zh) * | 2017-10-26 | 2021-03-30 | 中国药科大学 | 吡咯酮类brd4蛋白抑制剂的制备方法以及用途 |
| CN109928979B (zh) * | 2017-12-15 | 2021-08-06 | 四川科伦博泰生物医药股份有限公司 | 吲哚酮类衍生物及其制备方法和用途 |
| CN108383771A (zh) * | 2018-01-08 | 2018-08-10 | 华东师范大学 | 手性3,3-二取代异吲哚啉-1-酮衍生物及其合成方法和应用 |
| EP3843714B1 (en) * | 2018-08-27 | 2025-11-12 | Arcus Biosciences, Inc. | Cd73 inhibitors |
| US11161838B2 (en) | 2018-11-13 | 2021-11-02 | Incyte Corporation | Heterocyclic derivatives as PI3K inhibitors |
| US11078204B2 (en) | 2018-11-13 | 2021-08-03 | Incyte Corporation | Heterocyclic derivatives as PI3K inhibitors |
| WO2020102216A1 (en) | 2018-11-13 | 2020-05-22 | Incyte Corporation | Substituted heterocyclic derivatives as pi3k inhibitors |
| KR20220018475A (ko) * | 2019-04-09 | 2022-02-15 | 플렉시콘 인코퍼레이티드 | Ep300 또는 cbp 조절 및 이의 표시를 위한 응축 아진 |
| TW202126638A (zh) | 2019-09-30 | 2021-07-16 | 日商協和麒麟股份有限公司 | Bet分解劑 |
| WO2021175432A1 (en) | 2020-03-04 | 2021-09-10 | Boehringer Ingelheim International Gmbh | Method for administration of an anti cancer agent |
| EP3912625A1 (en) * | 2020-05-20 | 2021-11-24 | Kaerus Bioscience Limited | Novel maxi-k potassium channel openers for the treatment of fragile x associated disorders |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| JP2025529185A (ja) * | 2022-08-30 | 2025-09-04 | パンネックス セラピューティクス インコーポレイテッド | パネキシン－１調節剤及びパネキシン－１が関与する疾患の治療方法 |
| WO2025233532A1 (en) | 2024-05-10 | 2025-11-13 | Les Laboratoires Servier | Maxi-k potassium channel openers and therapeutic applications thereof |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0919423D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
-
2014
- 2014-03-26 US US14/225,484 patent/US9102684B2/en active Active
- 2014-03-26 JP JP2016504660A patent/JP6370368B2/ja active Active
- 2014-03-26 EP EP14714655.9A patent/EP2978757B1/en active Active
- 2014-03-26 WO PCT/EP2014/056079 patent/WO2014154760A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| EP2978757B1 (en) | 2017-02-08 |
| EP2978757A1 (en) | 2016-02-03 |
| US20140296229A1 (en) | 2014-10-02 |
| US9102684B2 (en) | 2015-08-11 |
| JP2016515560A (ja) | 2016-05-30 |
| WO2014154760A1 (en) | 2014-10-02 |
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