ES2824814T3 - Compuestos farmacéuticos - Google Patents
Compuestos farmacéuticos Download PDFInfo
- Publication number
- ES2824814T3 ES2824814T3 ES17790814T ES17790814T ES2824814T3 ES 2824814 T3 ES2824814 T3 ES 2824814T3 ES 17790814 T ES17790814 T ES 17790814T ES 17790814 T ES17790814 T ES 17790814T ES 2824814 T3 ES2824814 T3 ES 2824814T3
- Authority
- ES
- Spain
- Prior art keywords
- benzo
- mmol
- compound
- imidazol
- dazol
- 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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- 150000001875 compounds Chemical class 0.000 title claims abstract description 93
- 150000003839 salts Chemical class 0.000 claims abstract description 17
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract description 14
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims abstract description 11
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract description 7
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims abstract description 4
- 125000003003 spiro group Chemical group 0.000 claims abstract description 3
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims abstract 2
- 238000000034 method Methods 0.000 claims description 64
- -1 2 -cyclopropyl Chemical group 0.000 claims description 58
- XUWHAWMETYGRKB-UHFFFAOYSA-N piperidin-2-one Chemical group O=C1CCCCN1 XUWHAWMETYGRKB-UHFFFAOYSA-N 0.000 claims description 52
- 206010028980 Neoplasm Diseases 0.000 claims description 43
- 201000011510 cancer Diseases 0.000 claims description 28
- 125000003037 imidazol-2-yl group Chemical group [H]N1C([*])=NC([H])=C1[H] 0.000 claims description 24
- 238000011282 treatment Methods 0.000 claims description 22
- 230000000694 effects Effects 0.000 claims description 20
- PUPFATUGTIQBQA-UZQPLGKSSA-N fluorophen Chemical compound C([C@@]1(C)C2=CC(O)=CC=C2C[C@H]2[C@@H]1C)CN2CCC1=CC=C(F)C=C1 PUPFATUGTIQBQA-UZQPLGKSSA-N 0.000 claims description 13
- 239000003814 drug Substances 0.000 claims description 12
- 125000001207 fluorophenyl group Chemical group 0.000 claims description 10
- HYZJCKYKOHLVJF-UHFFFAOYSA-N 1H-benzimidazole Chemical compound C1=CC=C2NC=NC2=C1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 claims description 9
- 230000001225 therapeutic effect Effects 0.000 claims description 8
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- HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical group O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 claims description 6
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims description 5
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims description 5
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- 229910052799 carbon Inorganic materials 0.000 claims description 5
- 238000002560 therapeutic procedure Methods 0.000 claims description 5
- 239000003085 diluting agent Substances 0.000 claims description 4
- JKLZUTQOIVIMDL-DEOSSOPVSA-N (5S)-5-[1-(4,4-difluorocyclohexyl)-5-(2,4-dimethylpyrazol-3-yl)benzimidazol-2-yl]-1-(3,4-difluorophenyl)pyrrolidin-2-one Chemical compound FC1(CCC(CC1)N1C(=NC2=C1C=CC(=C2)C1=C(C=NN1C)C)[C@@H]1CCC(N1C1=CC(=C(C=C1)F)F)=O)F JKLZUTQOIVIMDL-DEOSSOPVSA-N 0.000 claims description 3
- GXZJYHGHHDXIML-DEOSSOPVSA-N (5S)-5-[1-(4,4-difluorocyclohexyl)-5-(3,5-dimethylimidazol-4-yl)benzimidazol-2-yl]-1-(3,4-difluorophenyl)pyrrolidin-2-one Chemical compound Cc1ncn(C)c1-c1ccc2n(C3CCC(F)(F)CC3)c(nc2c1)[C@@H]1CCC(=O)N1c1ccc(F)c(F)c1 GXZJYHGHHDXIML-DEOSSOPVSA-N 0.000 claims description 3
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- PLWILTBCWYTPPW-QHCPKHFHSA-N (5S)-5-[1-(4,4-difluorocyclohexyl)-5-(3,5-dimethyltriazol-4-yl)benzimidazol-2-yl]-1-(3,4-difluorophenyl)pyrrolidin-2-one Chemical compound CN1N=NC(C)=C1C1=CC=C2N(C3CCC(F)(F)CC3)C(=NC2=C1)[C@@H]1CCC(=O)N1C1=CC(F)=C(F)C=C1 PLWILTBCWYTPPW-QHCPKHFHSA-N 0.000 claims description 2
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- SAFFKKSHCVBSOP-DEOSSOPVSA-N (6S)-6-[1-(4,4-difluorocyclohexyl)-5-(3,5-dimethyltriazol-4-yl)benzimidazol-2-yl]-1-(3-fluoro-4-methoxyphenyl)piperidin-2-one Chemical compound FC1(CCC(CC1)N1C(=NC2=C1C=CC(=C2)C1=C(N=NN1C)C)[C@@H]1CCCC(N1C1=CC(=C(C=C1)OC)F)=O)F SAFFKKSHCVBSOP-DEOSSOPVSA-N 0.000 claims 1
- 125000001831 (C6-C10) heteroaryl group Chemical group 0.000 claims 1
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- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract description 16
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- BWHMMNNQKKPAPP-UHFFFAOYSA-L potassium carbonate Chemical compound [K+].[K+].[O-]C([O-])=O BWHMMNNQKKPAPP-UHFFFAOYSA-L 0.000 description 22
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- 239000012071 phase Substances 0.000 description 1
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 229920000136 polysorbate Polymers 0.000 description 1
- 229940068965 polysorbates Drugs 0.000 description 1
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- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 230000004481 post-translational protein modification Effects 0.000 description 1
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- 229940126586 small molecule drug Drugs 0.000 description 1
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- 235000010413 sodium alginate Nutrition 0.000 description 1
- 239000000661 sodium alginate Substances 0.000 description 1
- 229940005550 sodium alginate Drugs 0.000 description 1
- 229910000030 sodium bicarbonate Inorganic materials 0.000 description 1
- 235000017557 sodium bicarbonate Nutrition 0.000 description 1
- 229910001467 sodium calcium phosphate Inorganic materials 0.000 description 1
- 229910000029 sodium carbonate Inorganic materials 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- 239000001488 sodium phosphate Substances 0.000 description 1
- 235000011008 sodium phosphates Nutrition 0.000 description 1
- 229940054269 sodium pyruvate Drugs 0.000 description 1
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- 125000001973 tert-pentyl group Chemical group [H]C([H])([H])C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000005887 tetrahydrobenzofuranyl group Chemical group 0.000 description 1
- 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
- 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
-
- 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
- A61K9/2022—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
- C07D401/02—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
- 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)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| 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 |
|---|---|
| ES2824814T3 true ES2824814T3 (es) | 2021-05-13 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES17790814T Active ES2824814T3 (es) | 2016-10-18 | 2017-10-18 | Compuestos farmacéuticos |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US10647704B2 (OSRAM) |
| EP (1) | EP3529240B1 (OSRAM) |
| JP (1) | JP7082616B2 (OSRAM) |
| CN (1) | CN110036002B (OSRAM) |
| AU (1) | AU2017346454B2 (OSRAM) |
| CA (1) | CA3039643A1 (OSRAM) |
| DK (1) | DK3529240T3 (OSRAM) |
| ES (1) | ES2824814T3 (OSRAM) |
| GB (1) | GB201617627D0 (OSRAM) |
| HU (1) | HUE052107T2 (OSRAM) |
| WO (1) | WO2018073587A1 (OSRAM) |
| ZA (1) | ZA201902335B (OSRAM) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| GB201617630D0 (en) * | 2016-10-18 | 2016-11-30 | Cellcentric Ltd | Pharmaceutical compounds |
| WO2019055877A1 (en) | 2017-09-15 | 2019-03-21 | Forma Therapeutics, Inc. | TETRAHYDROIMIDAZO QUINOLINE COMPOSITIONS AS INHIBITORS OF CBP / P300 |
| AU2019295790B2 (en) | 2018-06-29 | 2023-07-13 | Forma Therapeutics, Inc. | Inhibiting creb binding protein (CBP) |
| WO2020190791A1 (en) | 2019-03-15 | 2020-09-24 | Forma Therapeutics, Inc. | Inhibiting cyclic amp-responsive element-binding protein (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 |
| WO2022143773A1 (zh) * | 2020-12-31 | 2022-07-07 | 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 |
| ES2570994T3 (es) * | 2005-11-08 | 2016-05-23 | Choongwae Pharma Corp | Miméticos de alfa-hélice y método relacionados con el tratamiento de células madre de cáncer |
| 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 |
| ES2661437T3 (es) * | 2013-06-21 | 2018-04-02 | Zenith Epigenetics Corp. | Nuevos compuestos bicíclicos sustituidos como inhibidores de bromodominio |
| WO2016086200A1 (en) * | 2014-11-27 | 2016-06-02 | Genentech, Inc. | 4,5,6,7-tetrahydro-1 h-pyrazolo[4,3-c]pyridin-3-amine compounds as cbp and/or ep300 inhibitors |
| CA2966452A1 (en) | 2014-12-17 | 2016-06-23 | Samuel David Brown | Substituted bicyclic compounds as bromodomain inhibitors |
| GB201506658D0 (en) | 2015-04-20 | 2015-06-03 | Cellcentric Ltd | Pharmaceutical compounds |
| WO2017024412A1 (en) | 2015-08-12 | 2017-02-16 | Neomed Institute | Substituted benzimidazoles, their preparation and their use as pharmaceuticals |
| GB201617630D0 (en) | 2016-10-18 | 2016-11-30 | Cellcentric Ltd | Pharmaceutical compounds |
-
2016
- 2016-10-18 GB GBGB1617627.3A patent/GB201617627D0/en not_active Ceased
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2017
- 2017-10-18 JP JP2019520591A patent/JP7082616B2/ja active Active
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- 2017-10-18 CA CA3039643A patent/CA3039643A1/en active Pending
- 2017-10-18 DK DK17790814.2T patent/DK3529240T3/da active
- 2017-10-18 HU HUE17790814A patent/HUE052107T2/hu unknown
- 2017-10-18 AU AU2017346454A patent/AU2017346454B2/en active Active
- 2017-10-18 ES ES17790814T patent/ES2824814T3/es active Active
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- 2017-10-18 EP EP17790814.2A patent/EP3529240B1/en active Active
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2019
- 2019-04-12 ZA ZA2019/02335A patent/ZA201902335B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP3529240A1 (en) | 2019-08-28 |
| JP7082616B2 (ja) | 2022-06-08 |
| NZ752356A (en) | 2025-02-28 |
| CN110036002B (zh) | 2022-08-30 |
| AU2017346454B2 (en) | 2022-02-17 |
| US10647704B2 (en) | 2020-05-12 |
| ZA201902335B (en) | 2024-11-27 |
| GB201617627D0 (en) | 2016-11-30 |
| US20190263788A1 (en) | 2019-08-29 |
| DK3529240T3 (da) | 2020-09-07 |
| CN110036002A (zh) | 2019-07-19 |
| AU2017346454A1 (en) | 2019-05-02 |
| WO2018073587A1 (en) | 2018-04-26 |
| CA3039643A1 (en) | 2018-04-26 |
| JP2019535658A (ja) | 2019-12-12 |
| EP3529240B1 (en) | 2020-08-05 |
| HUE052107T2 (hu) | 2021-04-28 |
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