AR109487A1 - Derivados de imidazo-2-il-piridin-2-ona como inhibidores de la unión de las proteínas bet - Google Patents
Derivados de imidazo-2-il-piridin-2-ona como inhibidores de la unión de las proteínas betInfo
- Publication number
- AR109487A1 AR109487A1 ARP170102425A ARP170102425A AR109487A1 AR 109487 A1 AR109487 A1 AR 109487A1 AR P170102425 A ARP170102425 A AR P170102425A AR P170102425 A ARP170102425 A AR P170102425A AR 109487 A1 AR109487 A1 AR 109487A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- hydrogen
- alkoxy
- halogen
- heterocycloalkyl
- Prior art date
Links
Classifications
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/443—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4433—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Se ha descubierto que éstos compuestos y sales de los mismos inhiben la unión de la familia BET de proteínas que contienen bromodominios a, por ejemplo, residuos de lisina acetilados y, por 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 representa un compuesto de fórmula (2) ó (3); R² es hidrógeno, alquilo C₁₋₆, alcoxi C₁₋₆, cicloalquilo C₃₋₇, heterocicloalquilo o -CHR⁵(CH₂)ᶜR⁶; cada R³ está independientemente seleccionado del grupo que consiste en halógeno, -CN, alquilo C₁₋₃, alcoxi C₁₋₃, -NO₂, -CONR⁷R⁸, -NR⁷COR⁸, -OCOR⁸, -CO₂R⁸, -SO₂NR⁷R⁸, -NR⁷SO₂R⁸, -SO₂R⁸, -R⁸, -NR⁷R⁸ y -OR⁸, con la condición de que cuando a es 2, un R³ está seleccionado del grupo que consiste en halógeno, -CN, alquilo C₁₋₃ y alcoxi C₁₋₃; R⁴ᵃ es hidrógeno, alquilo C₁₋₃, alcoxi C₁₋₃, halógeno, -CN, -OH, -NR⁹R¹⁰; R⁴ᵇ es hidrógeno o alquilo C₁₋₃; cada R⁴ᶜ está independientemente seleccionado del grupo que consiste en alquilo C₁₋₃, alcoxi C₁₋₃, halógeno, -CN, -OH y -NR⁹R¹⁰; R⁵ es hidrógeno, alquilo C₁₋₃ o -(CH₂)ᵈOR¹¹; R⁶ es hidrógeno, alquilo C₁₋₃, -(CH₂)ᵈOR¹¹, cicloalquilo C₃₋₇ o heterocicloalquilo, en donde los grupos alquilo C₁₋₃, -(CH₂)ᵈOR¹¹, cicloalquilo C₃₋₇, heterocicloalquilo pueden estar opcionalmente sustituidos con uno o dos sustituyentes independientemente seleccionados del grupo que consiste en alquilo C₁₋₃, alcoxi C₁₋₃, halógeno, -CH₂OH, -COOH y -COCH₃; R⁷ es hidrógeno o alquilo C₁₋₃ y R⁸ es -Y-Z, o cuando R³ es -CONR⁷R⁸, R⁷ y R⁸ junto con el nitrógeno al que están unidos pueden formar un heterocicloalquilo, en donde el grupo heterocicloalquilo puede estar opcionalmente sustituido con uno o dos grupos independientemente seleccionados de alquilo C₁₋₃, halógeno, -NH₂, -CH₂NH₂, -CO₂H, -OH, -CN y -CH₂OH; Y es un enlace o alquileno C₁₋₃, en donde el grupo alquileno C₁₋₃ puede estar opcionalmente sustituido con uno o dos grupos independientemente seleccionados de alquilo C₁₋₃; Z es hidrógeno, alquilo C₁₋₃, cicloalquilo C₃₋₇, heterocicloalquilo, arilo, heteroarilo, -SO₂NR¹²R¹³, -NR¹²SO₂R¹³, -SO₂R¹² o -NR¹²R¹³; en donde alquilo C₁₋₃, cicloalquilo C₃₋₇, heterocicloalquilo, arilo o heteroarilo pueden estar opcionalmente sustituidos con uno o dos grupos independientemente seleccionados de alquilo C₁₋₃, alcoxi C₁₋₃, halógeno, -NH₂, -CH₂NH₂, -CO₂H, -OH, -CN y -CH₂OH; R⁹ es hidrógeno o CH₃; R¹⁰ es hidrógeno o alquilo C₁₋₃; R¹¹ es hidrógeno o alquilo C₁₋₃; R¹² es hidrógeno o alquilo C₁₋₃; R¹³ es hidrógeno o alquilo C₁₋₃; a representa 0, 1 ó 2; b representa 0, 1 ó 2; cada c y d independientemente representan 0 ó 1.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1614934.6A GB201614934D0 (en) | 2016-09-02 | 2016-09-02 | Chemical compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR109487A1 true AR109487A1 (es) | 2018-12-12 |
Family
ID=57140084
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP170102425A AR109487A1 (es) | 2016-09-02 | 2017-08-31 | Derivados de imidazo-2-il-piridin-2-ona como inhibidores de la unión de las proteínas bet |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US20190175571A1 (es) |
| EP (1) | EP3507283A1 (es) |
| JP (1) | JP2019526577A (es) |
| KR (1) | KR20190042701A (es) |
| CN (1) | CN109790147A (es) |
| AR (1) | AR109487A1 (es) |
| AU (1) | AU2017317724A1 (es) |
| BR (1) | BR112019004241A2 (es) |
| CA (1) | CA3035312A1 (es) |
| CL (1) | CL2019000538A1 (es) |
| CO (1) | CO2019001871A2 (es) |
| CR (1) | CR20190106A (es) |
| DO (1) | DOP2019000047A (es) |
| EA (1) | EA201990410A1 (es) |
| GB (1) | GB201614934D0 (es) |
| JO (1) | JOP20190029A1 (es) |
| MA (1) | MA46085A (es) |
| MX (1) | MX2019002491A (es) |
| PE (1) | PE20190478A1 (es) |
| PH (1) | PH12019500460A1 (es) |
| SG (1) | SG11201901673SA (es) |
| TW (1) | TW201817724A (es) |
| UY (1) | UY37393A (es) |
| WO (1) | WO2018041947A1 (es) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL292968A (en) | 2016-09-02 | 2022-07-01 | Cyclerion Therapeutics Inc | scg motors in converging cycles |
| CN111588721B (zh) * | 2020-07-16 | 2021-06-08 | 中国农业科学院兰州兽医研究所 | 化合物zl0580用于制备预防或治疗非洲猪瘟药物的新用途 |
| CN111588725B (zh) * | 2020-07-16 | 2021-06-08 | 中国农业科学院兰州兽医研究所 | 化合物arv-825用于制备预防或治疗非洲猪瘟药物的新用途 |
| CN111686107B (zh) * | 2020-07-16 | 2021-06-08 | 中国农业科学院兰州兽医研究所 | 化合物plx51107用于制备预防或治疗非洲猪瘟药物的新用途 |
| CN111686114B (zh) * | 2020-07-16 | 2021-06-08 | 中国农业科学院兰州兽医研究所 | 化合物i-bet-762用于制备预防或治疗非洲猪瘟药物的新用途 |
| WO2024018423A1 (en) * | 2022-07-21 | 2024-01-25 | Tay Therapeutics Limited | Pyrroles and imidazoles as bet protein inhibitors |
| CN117257964B (zh) * | 2023-10-25 | 2024-04-02 | 苏州大学 | 基于碳酸氢铵的微波诱导吲哚美辛原位无定形化增溶技术 |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3406329A1 (de) * | 1984-02-22 | 1985-08-22 | Merck Patent Gmbh, 6100 Darmstadt | Pyridone |
| GB9004781D0 (en) | 1990-03-02 | 1990-04-25 | Glaxo Group Ltd | Device |
| DE4034060A1 (de) * | 1990-10-26 | 1992-04-30 | Basf Ag | Biskationische azofarbstoffe |
| DE19809994B4 (de) * | 1997-03-19 | 2006-02-09 | Basf Ag | Clathrate von Bis-[6-hydroxy-4-methyl-5-(3-methylimidazolium-1-yl)-3-(phen-4-ylazo)-pyridin-2-on]ethylen |
| GB0201677D0 (en) | 2002-01-25 | 2002-03-13 | Glaxo Group Ltd | Medicament dispenser |
| PE20060285A1 (es) * | 2004-03-30 | 2006-05-08 | Aventis Pharma Inc | Piridonas sustituidas como inhibidores de pol(adp-ribosa)-polimerasa (parp) |
| 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 |
| WO2008029825A1 (fr) * | 2006-09-05 | 2008-03-13 | Kyowa Hakko Kirin Co., Ltd. | Dérivé d'imidazole |
| KR101408517B1 (ko) * | 2008-03-21 | 2014-06-17 | 노파르티스 아게 | 신규한 헤테로시클릭 화합물 및 그의 용도 |
| JP5627574B2 (ja) * | 2008-06-03 | 2014-11-19 | インターミューン， インコーポレイテッド | 炎症性および線維性疾患を治療するための化合物および方法 |
| GB0919423D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919434D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| CA2789474A1 (en) * | 2010-03-04 | 2011-09-09 | Merck Sharp & Dohme Corp. | Inhibitors of catechol o-methyl transferase and their use in the treatment of psychotic disorders |
| AR092742A1 (es) * | 2012-10-02 | 2015-04-29 | Intermune Inc | Piridinonas antifibroticas |
| CA2895905A1 (en) * | 2012-12-21 | 2014-06-26 | Zenith Epigenetics Corp. | Novel heterocyclic compounds as bromodomain inhibitors |
| CN104788423B (zh) * | 2015-03-13 | 2016-10-26 | 成都理工大学 | 一种新的囊性纤维化跨膜传导调节因子抑制剂 |
| GB201504689D0 (en) * | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Chemical compounds |
-
2016
- 2016-09-02 GB GBGB1614934.6A patent/GB201614934D0/en not_active Ceased
-
2017
- 2017-06-16 JO JOP/2019/0029A patent/JOP20190029A1/ar unknown
- 2017-08-31 KR KR1020197009266A patent/KR20190042701A/ko not_active Application Discontinuation
- 2017-08-31 US US16/326,991 patent/US20190175571A1/en not_active Abandoned
- 2017-08-31 WO PCT/EP2017/071868 patent/WO2018041947A1/en unknown
- 2017-08-31 TW TW106129714A patent/TW201817724A/zh unknown
- 2017-08-31 CR CR20190106A patent/CR20190106A/es unknown
- 2017-08-31 UY UY0001037393A patent/UY37393A/es not_active Application Discontinuation
- 2017-08-31 AU AU2017317724A patent/AU2017317724A1/en not_active Abandoned
- 2017-08-31 AR ARP170102425A patent/AR109487A1/es unknown
- 2017-08-31 MA MA046085A patent/MA46085A/fr unknown
- 2017-08-31 CN CN201780059730.0A patent/CN109790147A/zh active Pending
- 2017-08-31 JP JP2019511919A patent/JP2019526577A/ja active Pending
- 2017-08-31 MX MX2019002491A patent/MX2019002491A/es unknown
- 2017-08-31 BR BR112019004241A patent/BR112019004241A2/pt not_active Application Discontinuation
- 2017-08-31 EP EP17758878.7A patent/EP3507283A1/en not_active Withdrawn
- 2017-08-31 EA EA201990410A patent/EA201990410A1/ru unknown
- 2017-08-31 CA CA3035312A patent/CA3035312A1/en not_active Abandoned
- 2017-08-31 SG SG11201901673SA patent/SG11201901673SA/en unknown
- 2017-08-31 PE PE2019000455A patent/PE20190478A1/es unknown
-
2019
- 2019-02-27 CO CONC2019/0001871A patent/CO2019001871A2/es unknown
- 2019-02-28 CL CL2019000538A patent/CL2019000538A1/es unknown
- 2019-02-28 DO DO2019000047A patent/DOP2019000047A/es unknown
- 2019-03-01 PH PH12019500460A patent/PH12019500460A1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CO2019001871A2 (es) | 2019-03-08 |
| TW201817724A (zh) | 2018-05-16 |
| US20190175571A1 (en) | 2019-06-13 |
| PE20190478A1 (es) | 2019-04-04 |
| SG11201901673SA (en) | 2019-03-28 |
| CA3035312A1 (en) | 2018-03-08 |
| CN109790147A (zh) | 2019-05-21 |
| EA201990410A1 (ru) | 2019-09-30 |
| DOP2019000047A (es) | 2019-03-15 |
| CR20190106A (es) | 2019-05-02 |
| MA46085A (fr) | 2019-07-10 |
| BR112019004241A2 (pt) | 2019-06-04 |
| AU2017317724A1 (en) | 2019-03-21 |
| GB201614934D0 (en) | 2016-10-19 |
| WO2018041947A1 (en) | 2018-03-08 |
| UY37393A (es) | 2018-03-23 |
| PH12019500460A1 (en) | 2019-12-16 |
| CL2019000538A1 (es) | 2019-05-17 |
| EP3507283A1 (en) | 2019-07-10 |
| JP2019526577A (ja) | 2019-09-19 |
| MX2019002491A (es) | 2019-07-08 |
| KR20190042701A (ko) | 2019-04-24 |
| JOP20190029A1 (ar) | 2019-02-25 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |