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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Classifications
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- 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
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- 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
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- 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)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Molecular Biology (AREA)
- Dermatology (AREA)
- Biophysics (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 (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)
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|---|---|
| ES2824814T3 true ES2824814T3 (es) | 2021-05-13 |
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| ES17790814T Active ES2824814T3 (es) | 2016-10-18 | 2017-10-18 | Compuestos farmacéuticos |
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| Country | Link |
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| US (1) | US10647704B2 (enExample) |
| EP (1) | EP3529240B1 (enExample) |
| JP (1) | JP7082616B2 (enExample) |
| CN (1) | CN110036002B (enExample) |
| AU (1) | AU2017346454B2 (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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| 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 |
| IL279734B2 (en) | 2018-06-29 | 2024-11-01 | Forma Therapeutics Inc | Inhibiting creb binding protein (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 |
| CN117645603A (zh) * | 2022-09-05 | 2024-03-05 | 复旦大学 | p300溴结构域抑制剂及其药用组合物及其应用 |
| KR20250113346A (ko) | 2024-01-17 | 2025-07-25 | 주식회사 엘지화학 | CBP/p300 저해제로 사용되는 신규 화합물, 및 이를 유효성분으로 포함하는 암, 염증성 장애 또는 자가면역 질환의 예방 또는 치료용 약학 조성물 |
| TW202542135A (zh) | 2024-01-17 | 2025-11-01 | 南韓商Ｌｇ化學股份有限公司 | 作為ＣＢＰ／ｐ３００抑制劑之新穎化合物和含有彼作為活性成分以預防或治療癌症、發炎病症或自體免疫疾病之醫藥組成物 |
| CN122535608A (zh) | 2024-01-17 | 2026-08-07 | 株式会社Lg化学 | 用作cbp/p300抑制剂的新型化合物以及包含其作为活性成分的用于预防或治疗癌症、炎性障碍或自身免疫性疾病的药物组合物 |
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| TW200501960A (en) * | 2002-10-02 | 2005-01-16 | Bristol Myers Squibb Co | Synergistic kits and compositions for treating cancer |
| US20070129353A1 (en) * | 2005-11-08 | 2007-06-07 | Michael Kahn | Alpha-helix mimetics and method relating to the treatment of cancer stem cells |
| US8501957B2 (en) | 2008-12-10 | 2013-08-06 | China Medical University | Benzimidazole compounds and their use as anticancer agents |
| US9005670B2 (en) * | 2010-01-05 | 2015-04-14 | 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 |
| CN105473581B (zh) * | 2013-06-21 | 2019-04-23 | 齐尼思表观遗传学有限公司 | 作为溴结构域抑制剂的新取代的双环化合物 |
| EP3632915A1 (en) * | 2014-11-27 | 2020-04-08 | 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 |
| 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
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2017
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- 2017-10-18 CN CN201780072397.7A patent/CN110036002B/zh active Active
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| GB201617627D0 (en) | 2016-11-30 |
| EP3529240B1 (en) | 2020-08-05 |
| US10647704B2 (en) | 2020-05-12 |
| ZA201902335B (en) | 2024-11-27 |
| EP3529240A1 (en) | 2019-08-28 |
| US20190263788A1 (en) | 2019-08-29 |
| HUE052107T2 (hu) | 2021-04-28 |
| AU2017346454B2 (en) | 2022-02-17 |
| AU2017346454A1 (en) | 2019-05-02 |
| CA3039643A1 (en) | 2018-04-26 |
| WO2018073587A1 (en) | 2018-04-26 |
| DK3529240T3 (da) | 2020-09-07 |
| NZ752356A (en) | 2025-02-28 |
| CN110036002A (zh) | 2019-07-19 |
| CN110036002B (zh) | 2022-08-30 |
| JP7082616B2 (ja) | 2022-06-08 |
| JP2019535658A (ja) | 2019-12-12 |
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