CA3039643A1 - Benzimidazoles and use thereof as modulators of p300 and/or cbp activity - Google Patents
Benzimidazoles and use thereof as modulators of p300 and/or cbp activity Download PDFInfo
- Publication number
- CA3039643A1 CA3039643A1 CA3039643A CA3039643A CA3039643A1 CA 3039643 A1 CA3039643 A1 CA 3039643A1 CA 3039643 A CA3039643 A CA 3039643A CA 3039643 A CA3039643 A CA 3039643A CA 3039643 A1 CA3039643 A1 CA 3039643A1
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- Canada
- Prior art keywords
- imidazol
- benzo
- compound
- piperidin
- mmol
- 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.)
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- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims abstract description 4
- XUWHAWMETYGRKB-UHFFFAOYSA-N piperidin-2-one Chemical group O=C1CCCCN1 XUWHAWMETYGRKB-UHFFFAOYSA-N 0.000 claims description 124
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- HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical group O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 claims description 15
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- 125000001072 heteroaryl group Chemical group 0.000 claims description 13
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- 238000004611 spectroscopical analysis Methods 0.000 description 1
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- 125000004213 tert-butoxy group Chemical group [H]C([H])([H])C(O*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
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- WHRNULOCNSKMGB-UHFFFAOYSA-N tetrahydrofuran thf Chemical compound C1CCOC1.C1CCOC1 WHRNULOCNSKMGB-UHFFFAOYSA-N 0.000 description 1
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- WROMPOXWARCANT-UHFFFAOYSA-N tfa trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.OC(=O)C(F)(F)F WROMPOXWARCANT-UHFFFAOYSA-N 0.000 description 1
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Classifications
-
- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- C07D401/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Dermatology (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB1617627.3 | 2016-10-18 | ||
| GBGB1617627.3A GB201617627D0 (en) | 2016-10-18 | 2016-10-18 | Pharmaceutical compounds |
| PCT/GB2017/053153 WO2018073587A1 (en) | 2016-10-18 | 2017-10-18 | Pharmaceutical compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA3039643A1 true CA3039643A1 (en) | 2018-04-26 |
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| CA3039643A Pending CA3039643A1 (en) | 2016-10-18 | 2017-10-18 | Benzimidazoles and use thereof as modulators of p300 and/or cbp activity |
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| US (1) | US10647704B2 (enExample) |
| EP (1) | EP3529240B1 (enExample) |
| JP (1) | JP7082616B2 (enExample) |
| CN (1) | CN110036002B (enExample) |
| AU (1) | AU2017346454B2 (enExample) |
| CA (1) | CA3039643A1 (enExample) |
| DK (1) | DK3529240T3 (enExample) |
| ES (1) | ES2824814T3 (enExample) |
| GB (1) | GB201617627D0 (enExample) |
| HU (1) | HUE052107T2 (enExample) |
| WO (1) | WO2018073587A1 (enExample) |
| ZA (1) | ZA201902335B (enExample) |
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| GB201617630D0 (en) * | 2016-10-18 | 2016-11-30 | Cellcentric Ltd | Pharmaceutical compounds |
| TWI846350B (zh) | 2017-09-15 | 2024-06-21 | 美商佛瑪治療公司 | 作為CBP/p300抑制劑之四氫-咪唑並喹啉化合物 |
| MX2023013508A (es) | 2018-06-29 | 2023-12-13 | Forma Therapeutics Inc | Inhibicion de la proteina de union a creb (cbp). |
| TW202102494A (zh) | 2019-03-15 | 2021-01-16 | 美商弗瑪治療公司 | 抑制環amp-反應元件-結合蛋白(creb) |
| CN112574189B (zh) * | 2019-09-27 | 2024-05-31 | 海创药业股份有限公司 | 一种ep300/cbp抑制剂 |
| CN112574191B (zh) * | 2019-09-29 | 2024-01-23 | 南京圣和药业股份有限公司 | 异噁唑杂环类化合物及其应用 |
| US11801243B2 (en) | 2020-09-23 | 2023-10-31 | Forma Therapeutics, Inc. | Bromodomain inhibitors for androgen receptor-driven cancers |
| US11795168B2 (en) | 2020-09-23 | 2023-10-24 | Forma Therapeutics, Inc. | Inhibiting cyclic amp-responsive element-binding protein (CREB) binding protein (CBP) |
| TW202227429A (zh) * | 2020-11-06 | 2022-07-16 | 大陸商貝達藥業股份有限公司 | P300抑制劑、包含其的藥物組合物、其應用及製備其的方法 |
| CN116670129A (zh) * | 2020-12-31 | 2023-08-29 | 南京明德新药研发有限公司 | 苯并咪唑类化合物及其应用 |
| CN114989158A (zh) * | 2021-03-02 | 2022-09-02 | 复旦大学 | 组蛋白乙酰转移酶p300溴结构域抑制剂及其药用组合物及其应用 |
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| TW200501960A (en) * | 2002-10-02 | 2005-01-16 | Bristol Myers Squibb Co | Synergistic kits and compositions for treating cancer |
| JP5536336B2 (ja) * | 2005-11-08 | 2014-07-02 | チョンウェ ファーマ コーポレイション | α−ヘリックス類似体および癌幹細胞の治療に関する方法 |
| US8501957B2 (en) | 2008-12-10 | 2013-08-06 | China Medical University | Benzimidazole compounds and their use as anticancer agents |
| WO2011085039A2 (en) * | 2010-01-05 | 2011-07-14 | The Johns Hopkins University | Use of histone acetyltransferase inhibitors as novel anti-cancer therapies |
| EP2397471A1 (en) | 2010-06-16 | 2011-12-21 | China Medical University | Benzimidazole compounds and their use |
| TWI527811B (zh) | 2013-05-09 | 2016-04-01 | 吉李德科學股份有限公司 | 作爲溴結構域抑制劑的苯並咪唑衍生物 |
| WO2015004534A2 (en) * | 2013-06-21 | 2015-01-15 | Zenith Epigenetics Corp. | Novel substituted bicyclic compounds as bromodomain inhibitors |
| US9763922B2 (en) * | 2014-11-27 | 2017-09-19 | Genentech, Inc. | Therapeutic compounds and uses thereof |
| WO2016097870A1 (en) | 2014-12-17 | 2016-06-23 | Zenith Epigenetics Corp. | Substituted bicyclic compounds as bromodomain inhibitors |
| GB201506658D0 (en) | 2015-04-20 | 2015-06-03 | Cellcentric Ltd | Pharmaceutical compounds |
| CN114605387A (zh) | 2015-08-12 | 2022-06-10 | 埃皮吉纳提克斯股份有限公司 | 取代的苯并咪唑、它们的制备和它们作为药物的用途 |
| GB201617630D0 (en) * | 2016-10-18 | 2016-11-30 | Cellcentric Ltd | Pharmaceutical compounds |
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2016
- 2016-10-18 GB GBGB1617627.3A patent/GB201617627D0/en not_active Ceased
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2017
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- 2017-10-18 EP EP17790814.2A patent/EP3529240B1/en active Active
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- 2017-10-18 ES ES17790814T patent/ES2824814T3/es active Active
- 2017-10-18 CA CA3039643A patent/CA3039643A1/en active Pending
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2019
- 2019-04-12 ZA ZA2019/02335A patent/ZA201902335B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US10647704B2 (en) | 2020-05-12 |
| ES2824814T3 (es) | 2021-05-13 |
| ZA201902335B (en) | 2024-11-27 |
| DK3529240T3 (da) | 2020-09-07 |
| JP2019535658A (ja) | 2019-12-12 |
| WO2018073587A1 (en) | 2018-04-26 |
| EP3529240B1 (en) | 2020-08-05 |
| US20190263788A1 (en) | 2019-08-29 |
| HUE052107T2 (hu) | 2021-04-28 |
| CN110036002B (zh) | 2022-08-30 |
| AU2017346454B2 (en) | 2022-02-17 |
| GB201617627D0 (en) | 2016-11-30 |
| JP7082616B2 (ja) | 2022-06-08 |
| AU2017346454A1 (en) | 2019-05-02 |
| NZ752356A (en) | 2025-02-28 |
| EP3529240A1 (en) | 2019-08-28 |
| CN110036002A (zh) | 2019-07-19 |
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