AR115768A1 - Inhibidores bicíclicos de las histona desacetilasas - Google Patents
Inhibidores bicíclicos de las histona desacetilasasInfo
- Publication number
- AR115768A1 AR115768A1 ARP190101972A ARP190101972A AR115768A1 AR 115768 A1 AR115768 A1 AR 115768A1 AR P190101972 A ARP190101972 A AR P190101972A AR P190101972 A ARP190101972 A AR P190101972A AR 115768 A1 AR115768 A1 AR 115768A1
- Authority
- AR
- Argentina
- Prior art keywords
- 4alkyl
- halo
- 4alkoxy
- hydrogen
- haloc1
- Prior art date
Links
- 108010033040 Histones Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 7
- 125000001475 halogen functional group Chemical group 0.000 abstract 6
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 5
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 4
- -1 haloC1−4alkyl Chemical group 0.000 abstract 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 3
- 102000003964 Histone deacetylase Human genes 0.000 abstract 2
- 108090000353 Histone deacetylase Proteins 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 125000001544 thienyl group Chemical group 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
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
- C07D401/14—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
-
- 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
- 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
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Compuestos de la formula (1); y sales farmacéuticamente aceptables y composiciones con el mismo, que son de utilidad para tratar una variedad de condiciones asociadas con la histona desacetilasas (HDAC). Reivindicación 1: Un compuesto caracterizado porque responde a la fórmula (1); o una sal farmacéuticamente aceptable del mismo, en donde: el anillo A es fenilo o tiofenilo; X es (CRᵃRᵇ)ₜ, O ó NR⁵; q y t son, cada uno de manera independiente, 0, 1, 2 ó 3; R¹ es fenilo o heteroarilo, cada uno de los cuales está sustituido opcionalmente con 1 a 3 grupos seleccionados entre Rᶜ; R² es hidrógeno, halo, C₁₋₄alquilo, C₁₋₄alcoxi u OH; R³ es hidrógeno o halo; R⁴ es halo cuando el anillo A es fenilo y R⁴ es hidrógeno cuando el anillo A es tiofenilo; R⁵ es hidrógeno, C₁₋₄alquilo o C₁₋₄alquil-OC₁₋₄alquilo; Rᵃ y Rᵇ son, cada uno de manera independiente, hidrógeno, C₁₋₄alquilo, haloC₁₋₄alquilo, C₁₋₄alcoxi o halo; y Rᶜ es halo, C₁₋₄alquilo, haloC₁₋₄alquilo, C₁₋₄alcoxi, haloC₁₋₄alcoxi, C₁₋₄alquil-OC₁₋₄alquilo, C₁₋₄alquil-NH C₁₋₄alquilo, C₁₋₄alquil-N(C₁₋₄alquil)₂, -C₁₋₄alquilheteroarilo o -C₁₋₄alquilheterociclilo, en donde dicho heteroarilo y heterociclilo están sustituidos, cada uno de manera opcional e independiente, con 1 a 3 grupos seleccionados entre C₁₋₄alquilo, haloC₁₋₄alquilo, C₁₋₄alcoxi y halo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862697498P | 2018-07-13 | 2018-07-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR115768A1 true AR115768A1 (es) | 2021-02-24 |
Family
ID=67480370
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP190101972A AR115768A1 (es) | 2018-07-13 | 2019-07-12 | Inhibidores bicíclicos de las histona desacetilasas |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US20210276978A1 (es) |
| EP (1) | EP3820859B1 (es) |
| JP (2) | JP7414820B2 (es) |
| KR (1) | KR20210031704A (es) |
| CN (1) | CN112424184A (es) |
| AR (1) | AR115768A1 (es) |
| AU (1) | AU2019300036A1 (es) |
| CA (1) | CA3106355A1 (es) |
| EA (1) | EA202190077A1 (es) |
| IL (2) | IL309951A (es) |
| MA (1) | MA53129A (es) |
| MX (1) | MX2021000468A (es) |
| SG (1) | SG11202012916WA (es) |
| TW (1) | TWI809146B (es) |
| WO (1) | WO2020014605A1 (es) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUE057041T2 (hu) | 2015-07-06 | 2022-04-28 | Alkermes Inc | Hiszton deacetiláz hetero-halogén gátlói |
| PL3570834T3 (pl) | 2017-01-11 | 2022-05-23 | Alkermes, Inc. | Bicykliczne inhibitory deacetylazy histonowej |
| RS63343B1 (sr) | 2017-08-07 | 2022-07-29 | Alkermes Inc | Biciklični inhibitori histonske deacetilaze |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101808518A (zh) * | 2007-06-27 | 2010-08-18 | 默沙东公司 | 作为组蛋白脱乙酰酶抑制剂的吡啶基和嘧啶基衍生物 |
| WO2012149540A1 (en) * | 2011-04-28 | 2012-11-01 | The Broad Institute Inc | Inhibitors of histone deacetylase |
| WO2016018795A1 (en) * | 2014-07-28 | 2016-02-04 | The General Hospital Corporation | Histone deacetylase inhibitors |
| HUE057041T2 (hu) * | 2015-07-06 | 2022-04-28 | Alkermes Inc | Hiszton deacetiláz hetero-halogén gátlói |
| TWI794171B (zh) * | 2016-05-11 | 2023-03-01 | 美商滬亞生物國際有限公司 | Ｈｄａｃ抑制劑與ｐｄ-ｌ１抑制劑之組合治療 |
| US10385031B2 (en) * | 2016-11-23 | 2019-08-20 | Regenacy Pharmaceuticals, Llc | Substituted piperazines as selective HDAC1,2 inhibitors |
-
2019
- 2019-07-12 JP JP2021523578A patent/JP7414820B2/ja active Active
- 2019-07-12 CA CA3106355A patent/CA3106355A1/en active Pending
- 2019-07-12 IL IL309951A patent/IL309951A/en unknown
- 2019-07-12 EP EP19746301.1A patent/EP3820859B1/en active Active
- 2019-07-12 EA EA202190077A patent/EA202190077A1/ru unknown
- 2019-07-12 MX MX2021000468A patent/MX2021000468A/es unknown
- 2019-07-12 SG SG11202012916WA patent/SG11202012916WA/en unknown
- 2019-07-12 TW TW108124686A patent/TWI809146B/zh active
- 2019-07-12 WO PCT/US2019/041592 patent/WO2020014605A1/en unknown
- 2019-07-12 MA MA053129A patent/MA53129A/fr unknown
- 2019-07-12 KR KR1020217002884A patent/KR20210031704A/ko unknown
- 2019-07-12 AU AU2019300036A patent/AU2019300036A1/en active Pending
- 2019-07-12 CN CN201980046820.5A patent/CN112424184A/zh active Pending
- 2019-07-12 US US17/260,193 patent/US20210276978A1/en active Pending
- 2019-07-12 AR ARP190101972A patent/AR115768A1/es unknown
- 2019-07-12 IL IL279940A patent/IL279940B1/en unknown
-
2023
- 2023-12-28 JP JP2023222406A patent/JP2024038202A/ja not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| AU2019300036A1 (en) | 2021-01-14 |
| WO2020014605A1 (en) | 2020-01-16 |
| IL309951A (en) | 2024-03-01 |
| EP3820859C0 (en) | 2024-03-20 |
| US20210276978A1 (en) | 2021-09-09 |
| JP7414820B2 (ja) | 2024-01-16 |
| CN112424184A (zh) | 2021-02-26 |
| IL279940A (en) | 2021-03-01 |
| TW202019903A (zh) | 2020-06-01 |
| MX2021000468A (es) | 2021-06-23 |
| EA202190077A1 (ru) | 2021-08-30 |
| EP3820859B1 (en) | 2024-03-20 |
| JP2024038202A (ja) | 2024-03-19 |
| EP3820859A1 (en) | 2021-05-19 |
| CA3106355A1 (en) | 2020-01-16 |
| JP2021531336A (ja) | 2021-11-18 |
| MA53129A (fr) | 2021-05-19 |
| IL279940B1 (en) | 2024-02-01 |
| SG11202012916WA (en) | 2021-01-28 |
| TWI809146B (zh) | 2023-07-21 |
| KR20210031704A (ko) | 2021-03-22 |
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