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 (enExample) | 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 (enExample) |
| EP (1) | EP2978757B1 (enExample) |
| JP (1) | JP6370368B2 (enExample) |
| WO (1) | WO2014154760A1 (enExample) |
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 |
| WO2014080291A2 (en) | 2012-11-21 | 2014-05-30 | Rvx Therapeutics Inc. | Biaryl derivatives as bromodomain inhibitors |
| US9073878B2 (en) | 2012-11-21 | 2015-07-07 | Zenith Epigenetics Corp. | Cyclic amines as bromodomain inhibitors |
| WO2014096965A2 (en) | 2012-12-21 | 2014-06-26 | Rvx Therapeutics Inc. | 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. |
| CA2901083A1 (en) | 2013-04-26 | 2014-10-30 | Beigene, Ltd. | Substituted 5-(3,5-dimethylisoxazol-4-yl)indoline-2-ones |
| WO2015004533A2 (en) | 2013-06-21 | 2015-01-15 | Zenith Epigenetics Corp. | Novel substituted bicyclic compounds as bromodomain inhibitors |
| SG11201510409QA (en) | 2013-06-21 | 2016-01-28 | Zenith Epigenetics Corp | Novel bicyclic bromodomain inhibitors |
| WO2015006193A1 (en) | 2013-07-08 | 2015-01-15 | Incyte Corporation | Tricyclic heterocycles as bet protein inhibitors |
| WO2015015318A2 (en) | 2013-07-31 | 2015-02-05 | Zenith Epigenetics Corp. | Novel quinazolinones as bromodomain inhibitors |
| US9315501B2 (en) | 2013-11-26 | 2016-04-19 | Incyte Corporation | Bicyclic heterocycles as BET protein inhibitors |
| WO2015081203A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| US9309246B2 (en) | 2013-12-19 | 2016-04-12 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| UA119870C2 (uk) | 2014-04-23 | 2019-08-27 | Інсайт Корпорейшн | 1H-ПІРОЛО[2,3-c]ПІРИДИН-7(6H)-ОНИ ТА ПІРАЗОЛО[3,4-c]ПІРИДИН-7(6H)-ОНИ ЯК ІНГІБІТОРИ БІЛКІВ BET |
| US9902702B2 (en) * | 2014-07-15 | 2018-02-27 | Bristol-Myers Squibb Company | Spirocycloheptanes as inhibitors of rock |
| ES2855225T3 (es) | 2014-09-15 | 2021-09-23 | Incyte Corp | Heterociclos tricíclicos para su uso como inhibidores de proteínas BET |
| DK3212789T3 (da) | 2014-10-31 | 2020-07-27 | Massachusetts Inst Technology | Massiv parallel kombinatorisk genetik til crispr |
| US10710992B2 (en) | 2014-12-01 | 2020-07-14 | Zenith Epigenetics Ltd. | Substituted pyridinones as bromodomain inhibitors |
| EP3227280B1 (en) * | 2014-12-01 | 2019-04-24 | Zenith Epigenetics Ltd. | Substituted pyridines as bromodomain inhibitors |
| JP2017537946A (ja) | 2014-12-11 | 2017-12-21 | 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置換複素環 |
| 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 |
| CA2988209A1 (en) * | 2015-06-16 | 2016-12-22 | Orion Corporation | Spiro[cyclobutane-1,3'-indolin]-2'-one derivatives as bromodomain inhibitors |
| 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 |
| AU2017281286B2 (en) | 2016-06-20 | 2021-05-20 | Incyte Corporation | Crystalline solid forms of a bet inhibitor |
| 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 |
| ES3053198T3 (en) * | 2018-08-27 | 2026-01-20 | Arcus Biosciences Inc | Cd73 inhibitors |
| WO2020102216A1 (en) | 2018-11-13 | 2020-05-22 | Incyte Corporation | Substituted heterocyclic derivatives as pi3k inhibitors |
| WO2020102150A1 (en) | 2018-11-13 | 2020-05-22 | Incyte Corporation | Heterocyclic derivatives as pi3k inhibitors |
| WO2020102198A1 (en) | 2018-11-13 | 2020-05-22 | Incyte Corporation | Heterocyclic derivatives as pi3k inhibitors |
| CN113710668B (zh) * | 2019-04-09 | 2025-01-07 | Opna生物公司 | 用于ep300或cbp调节及其适应症的缩合吖嗪 |
| WO2021065980A1 (ja) | 2019-09-30 | 2021-04-08 | 協和キリン株式会社 | Bet分解剤 |
| 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 |
| EP4580618A2 (en) * | 2022-08-30 | 2025-07-09 | Pannex Therapeutics Inc. | Pannexin-1 modulators and methods of treating disorders in which pannexin-1 is implicated |
| 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 EP EP14714655.9A patent/EP2978757B1/en active Active
- 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 WO PCT/EP2014/056079 patent/WO2014154760A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| US9102684B2 (en) | 2015-08-11 |
| EP2978757B1 (en) | 2017-02-08 |
| US20140296229A1 (en) | 2014-10-02 |
| WO2014154760A1 (en) | 2014-10-02 |
| JP2016515560A (ja) | 2016-05-30 |
| EP2978757A1 (en) | 2016-02-03 |
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