AR103934A1 - Derivados de benzimidazoles como inhibidores de bromodominio - Google Patents
Derivados de benzimidazoles como inhibidores de bromodominioInfo
- Publication number
- AR103934A1 AR103934A1 ARP160100683A ARP160100683A AR103934A1 AR 103934 A1 AR103934 A1 AR 103934A1 AR P160100683 A ARP160100683 A AR P160100683A AR P160100683 A ARP160100683 A AR P160100683A AR 103934 A1 AR103934 A1 AR 103934A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- alkoxy
- hydrogen
- heterocycloalkyl
- cycloalkyl
- Prior art date
Links
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
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- 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
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Abstract
Se ha encontrado que los compuestos de la presente solicitud y sales de los mismos inhiben la unión de la familia BET de proteínas de bromodominio a, por ejemplo, residuos de lisina acetilados y por lo tanto pueden tener uso en terapia, por ejemplo, en el tratamiento de enfermedades autoinmunitarias e inflamatorias, tales como artritis reumatoide; y cánceres. Reivindicación 1: Un compuesto de fórmula (1) o una sal del mismo, en la que R¹ y R² son cada uno independientemente hidrógeno o metilo con la condición de que al menos uno de R¹ y R² sea metilo; R³ es alquilo C₁₋₆, alcoxi C₁₋₆, cicloalquilo, heterocicloalquilo, o -CHR⁵(CH₂)ₐR⁶; R⁴ está unido en la posición 5 ó 6 del benzimidazol y representa un compuesto de fórmula (2); R⁵ es hidrógeno, alquilo C₁₋₃, alcoxi C₁₋₃ o -(CH₂)ᵈOR⁹; R⁶ es hidrógeno, alquilo C₁₋₃, alcoxi C₁₋₃, -(CH₂)ₑOR¹⁰, hidroxilo, -NR¹¹R¹², halo, cicloalquilo, heterocicloalquilo, arilo o heteroarilo, en el que dicho alquilo C₁₋₃, alcoxi C₁₋₃, -(CH₂)ₑOR¹⁰, cicloalquilo, heterocicloalquilo, arilo o heteroarilo puede estar opcionalmente sustituido con uno o dos sustituyentes seleccionados independientemente del grupo que consiste en alquilo C₁₋₃, alcoxi C₁₋₃, halo, CH₂OH, -COOH y -COCH₃; R⁷ es hidrógeno, alquilo C₁₋₆, -(CH₂)ᵍ-cicloalquilo, -(CH₂)ₕ-heterocicloalquilo o CR¹³R¹⁴R¹⁵; R⁸ es hidrógeno, alquilo C₁₋₆, cicloalquilo, heterocicloalquilo o -CHR¹⁶R¹⁷ en el que dicho alquilo C₁₋₆ está opcionalmente sustituido con alcoxi C₁₋₃ y en el que R¹⁶ es hidrógeno o alquilo C₁₋₃ y R¹⁷ es cicloalquilo o heterocicloalquilo; R⁹, R¹⁰, R¹¹, R¹², R¹⁴, R¹⁵ y R¹⁸ son cada uno independientemente hidrógeno o alquilo C₁₋₃; R¹³ es hidrógeno, hidroxilo, -CH₂OR¹⁸, halo, -COOH, -CONH₂, 1H-imidazol-4-ilo, -SH, -SeH, alquilo C₁₋₃, alcoxi C₁₋₃, fenilo o 4-hidroxifenilo en el que dicho alquilo C₁₋₃ o alcoxi C₁₋₃ puede estar opcionalmente sustituido con halo, hidroxilo, -NHC(=NH₂)NH₂, -NH₂, -COOH, -CONH₂ o -SCH₃; a es 0, 1, 2 ó 3; b es 0 ó 1; c es 1, 2 ó 3 con la condición de que cuando b sea 1, c sea 2 ó 3; d y e son cada uno independientemente 1 ó 2; y g y h son cada uno independientemente 0, 1 ó 2.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1504689.9A GB201504689D0 (en) | 2015-03-19 | 2015-03-19 | Chemical compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR103934A1 true AR103934A1 (es) | 2017-06-14 |
Family
ID=53052091
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP160100683A AR103934A1 (es) | 2015-03-19 | 2016-03-15 | Derivados de benzimidazoles como inhibidores de bromodominio |
Country Status (35)
| Country | Link |
|---|---|
| US (2) | US10442786B2 (es) |
| EP (2) | EP3271349B1 (es) |
| JP (1) | JP6419990B2 (es) |
| KR (1) | KR102072850B1 (es) |
| CN (1) | CN107635989B (es) |
| AR (1) | AR103934A1 (es) |
| AU (1) | AU2016232217B2 (es) |
| BR (1) | BR112017019779B1 (es) |
| CA (1) | CA2979504C (es) |
| CL (1) | CL2017002332A1 (es) |
| CO (1) | CO2017009992A2 (es) |
| CR (1) | CR20170430A (es) |
| CY (1) | CY1121855T1 (es) |
| DK (1) | DK3271349T3 (es) |
| DO (1) | DOP2017000213A (es) |
| EA (1) | EA033594B1 (es) |
| ES (1) | ES2735417T3 (es) |
| GB (1) | GB201504689D0 (es) |
| HR (1) | HRP20191186T1 (es) |
| HU (1) | HUE044414T2 (es) |
| IL (1) | IL254318B (es) |
| LT (1) | LT3271349T (es) |
| MA (2) | MA41778A (es) |
| ME (1) | ME03485B (es) |
| MX (1) | MX2017012023A (es) |
| PE (1) | PE20180032A1 (es) |
| PH (1) | PH12017501620A1 (es) |
| PL (1) | PL3271349T3 (es) |
| PT (1) | PT3271349T (es) |
| RS (1) | RS59056B1 (es) |
| SG (1) | SG11201707356QA (es) |
| SI (1) | SI3271349T1 (es) |
| TW (1) | TW201706257A (es) |
| UY (1) | UY36589A (es) |
| WO (1) | WO2016146738A1 (es) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201504689D0 (en) * | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Chemical compounds |
| WO2017024406A1 (en) | 2015-08-11 | 2017-02-16 | Neomed Institute | N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals |
| WO2017024408A1 (en) | 2015-08-11 | 2017-02-16 | Neomed Institute | Aryl-substituted dihydroquinolinones, their preparation and their use as pharmaceuticals |
| WO2017024412A1 (en) | 2015-08-12 | 2017-02-16 | Neomed Institute | Substituted benzimidazoles, their preparation and their use as pharmaceuticals |
| WO2017066876A1 (en) | 2015-10-21 | 2017-04-27 | Neomed Institute | Substituted imidazopyridines, their preparation and their use as pharmaceuticals |
| WO2017127930A1 (en) | 2016-01-28 | 2017-08-03 | Neomed Institute | Substituted [1,2,4]triazolo[4,3-a]pyridines, their preparation and their use as pharmaceuticals |
| GB201614940D0 (en) * | 2016-09-02 | 2016-10-19 | Glaxosmithkline Intellectual Property (No 2) Ltd | Chemical compounds |
| GB201614939D0 (en) * | 2016-09-02 | 2016-10-19 | Glaxosmithkline Ip Dev Ltd | Crystalline hydrate |
| GB201614934D0 (en) * | 2016-09-02 | 2016-10-19 | Glaxosmithkline Intellectual Property (No 2) Ltd | Chemical compounds |
| JP2020516672A (ja) * | 2017-04-18 | 2020-06-11 | セルジーン クオンティセル リサーチ，インク． | 治療用化合物 |
| CN109280046B (zh) * | 2017-07-21 | 2021-02-02 | 浙江海正药业股份有限公司 | 苯并咪唑类衍生物及其制备方法及其在医药上的用途 |
| CN111683932A (zh) * | 2018-02-06 | 2020-09-18 | 上海海和药物研究开发有限公司 | 具有bet抑制活性的化合物及其制备方法和用途 |
| CN109369432B (zh) * | 2018-11-02 | 2021-06-25 | 永农生物科学有限公司 | (s)-4-氯-2-氨基丁酸酯的制备方法 |
| JP2022053557A (ja) * | 2019-02-08 | 2022-04-06 | マルホ株式会社 | ピリドン誘導体 |
| BR112021016921A2 (pt) * | 2019-03-15 | 2021-11-03 | Forma Therapeutics Inc | Inibição de proteína de ligação a elemento responsivo a amp cíclico (creb) |
| US20220259200A1 (en) * | 2019-04-24 | 2022-08-18 | Convergene, Llc | Small molecule bromodomain inhibitors and uses therof |
| WO2020223370A1 (en) * | 2019-04-29 | 2020-11-05 | The Board Of Regents Of The University Of Texas System | Compositions and methods for treating schistosoma infections |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9004781D0 (en) | 1990-03-02 | 1990-04-25 | Glaxo Group Ltd | Device |
| GB0201677D0 (en) | 2002-01-25 | 2002-03-13 | Glaxo Group Ltd | Medicament dispenser |
| GB0515584D0 (en) | 2005-07-28 | 2005-09-07 | Glaxo Group Ltd | Medicament dispenser |
| AR058289A1 (es) | 2005-12-12 | 2008-01-30 | Glaxo Group Ltd | Colector para ser usado en dispensador de medicamento |
| CA2648036C (en) | 2006-03-31 | 2012-05-22 | Janssen Pharmaceutica N.V. | Benzoimidazol-2-yl pyrimidines and pyrazines as modulators of the histamine h4 receptor |
| JP2013508461A (ja) * | 2009-10-27 | 2013-03-07 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー | 脂肪酸シンターゼ阻害剤としてのベンズイミダゾール |
| GB0919423D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919434D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| EP2624696B1 (en) | 2010-10-06 | 2016-12-21 | Glaxosmithkline LLC | Benzimidazole derivatives as pi3 kinase inhibitors |
| GB201114103D0 (en) * | 2011-08-17 | 2011-09-28 | Glaxosmithkline Llc | Novel compounds |
| WO2013097052A1 (en) * | 2011-12-30 | 2013-07-04 | Abbott Laboratories | Bromodomain inhibitors |
| AU2013365926B9 (en) * | 2012-12-21 | 2019-01-17 | Zenith Epigenetics Ltd. | Novel heterocyclic compounds as bromodomain inhibitors |
| KR102244719B1 (ko) | 2013-03-15 | 2021-04-26 | 플렉시콘 인코퍼레이티드 | 헤테로시클릭 화합물 및 그의 용도 |
| TWI530499B (zh) | 2013-03-28 | 2016-04-21 | 吉李德科學股份有限公司 | 作為溴結構域（ｂｒｏｍｏｄｏｍａｉｎ）抑制劑之苯並咪唑酮衍生物類 |
| 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 |
| CA2915622C (en) * | 2013-06-21 | 2020-08-18 | Zenith Epigenetics Corp. | Novel substituted bicyclic compounds as bromodomain inhibitors |
| US20150051208A1 (en) * | 2013-08-14 | 2015-02-19 | Boehringer Ingelheim International Gmbh | Pyridinones |
| US9428515B2 (en) * | 2014-05-09 | 2016-08-30 | Boehringer Ingelheim International Gmbh | Benzimidazole derivatives |
| GB201504689D0 (en) * | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Chemical compounds |
| GB201504694D0 (en) * | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Covalent conjugates |
| GB201614939D0 (en) * | 2016-09-02 | 2016-10-19 | Glaxosmithkline Ip Dev Ltd | Crystalline hydrate |
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2015
- 2015-03-19 GB GBGB1504689.9A patent/GB201504689D0/en not_active Ceased
-
2016
- 2016-03-15 AR ARP160100683A patent/AR103934A1/es unknown
- 2016-03-17 BR BR112017019779-0A patent/BR112017019779B1/pt active IP Right Grant
- 2016-03-17 MX MX2017012023A patent/MX2017012023A/es unknown
- 2016-03-17 SI SI201630321T patent/SI3271349T1/sl unknown
- 2016-03-17 CA CA2979504A patent/CA2979504C/en active Active
- 2016-03-17 JP JP2017548404A patent/JP6419990B2/ja active Active
- 2016-03-17 MA MA041778A patent/MA41778A/fr unknown
- 2016-03-17 LT LTEP16710214.4T patent/LT3271349T/lt unknown
- 2016-03-17 PL PL16710214T patent/PL3271349T3/pl unknown
- 2016-03-17 CN CN201680027314.8A patent/CN107635989B/zh active Active
- 2016-03-17 PE PE2017001543A patent/PE20180032A1/es unknown
- 2016-03-17 KR KR1020177030073A patent/KR102072850B1/ko active IP Right Grant
- 2016-03-17 PT PT16710214T patent/PT3271349T/pt unknown
- 2016-03-17 CR CR20170430A patent/CR20170430A/es unknown
- 2016-03-17 MA MA046981A patent/MA46981A/fr unknown
- 2016-03-17 EA EA201791973A patent/EA033594B1/ru not_active IP Right Cessation
- 2016-03-17 EP EP16710214.4A patent/EP3271349B1/en active Active
- 2016-03-17 ME MEP-2019-171A patent/ME03485B/me unknown
- 2016-03-17 UY UY0001036589A patent/UY36589A/es not_active Application Discontinuation
- 2016-03-17 DK DK16710214.4T patent/DK3271349T3/da active
- 2016-03-17 US US15/559,556 patent/US10442786B2/en active Active
- 2016-03-17 AU AU2016232217A patent/AU2016232217B2/en not_active Ceased
- 2016-03-17 RS RS20190986A patent/RS59056B1/sr unknown
- 2016-03-17 SG SG11201707356QA patent/SG11201707356QA/en unknown
- 2016-03-17 ES ES16710214T patent/ES2735417T3/es active Active
- 2016-03-17 WO PCT/EP2016/055792 patent/WO2016146738A1/en active Application Filing
- 2016-03-17 TW TW105108340A patent/TW201706257A/zh unknown
- 2016-03-17 EP EP19174047.1A patent/EP3549939A1/en not_active Withdrawn
- 2016-03-17 HU HUE16710214 patent/HUE044414T2/hu unknown
-
2017
- 2017-09-04 IL IL254318A patent/IL254318B/en active IP Right Grant
- 2017-09-07 PH PH12017501620A patent/PH12017501620A1/en unknown
- 2017-09-14 CL CL2017002332A patent/CL2017002332A1/es unknown
- 2017-09-19 DO DO2017000213A patent/DOP2017000213A/es unknown
- 2017-09-29 CO CONC2017/0009992A patent/CO2017009992A2/es unknown
-
2019
- 2019-07-01 HR HRP20191186TT patent/HRP20191186T1/hr unknown
- 2019-07-26 CY CY20191100796T patent/CY1121855T1/el unknown
- 2019-08-22 US US16/547,909 patent/US11053212B2/en active Active
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| Date | Code | Title | Description |
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| FB | Suspension of granting procedure |