AR111479A1 - COMPOUNDS DERIVED FROM PIRIDINA AND PIRAZOL - Google Patents
COMPOUNDS DERIVED FROM PIRIDINA AND PIRAZOLInfo
- Publication number
- AR111479A1 AR111479A1 ARP180100992A ARP180100992A AR111479A1 AR 111479 A1 AR111479 A1 AR 111479A1 AR P180100992 A ARP180100992 A AR P180100992A AR P180100992 A ARP180100992 A AR P180100992A AR 111479 A1 AR111479 A1 AR 111479A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- hydrogen
- heterocyclyl
- heteroaryl
- heteroarylalkyl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 7
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 title 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 7
- 125000000217 alkyl group Chemical group 0.000 abstract 6
- 125000001072 heteroaryl group Chemical group 0.000 abstract 6
- 229910052739 hydrogen Inorganic materials 0.000 abstract 6
- 239000001257 hydrogen Substances 0.000 abstract 6
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 5
- 125000003118 aryl group Chemical group 0.000 abstract 5
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 5
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 5
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 5
- 150000002431 hydrogen Chemical group 0.000 abstract 5
- 125000004415 heterocyclylalkyl group Chemical group 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical group 0.000 abstract 3
- 239000000203 mixture Substances 0.000 abstract 3
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 230000002401 inhibitory effect Effects 0.000 abstract 2
- 230000001404 mediated effect Effects 0.000 abstract 2
- 108091005625 BRD4 Proteins 0.000 abstract 1
- 102100029895 Bromodomain-containing protein 4 Human genes 0.000 abstract 1
- 102000001805 Bromodomains Human genes 0.000 abstract 1
- 108050009021 Bromodomains Proteins 0.000 abstract 1
- 102000006947 Histones Human genes 0.000 abstract 1
- 108010033040 Histones Proteins 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- DTERQYGMUDWYAZ-ZETCQYMHSA-N N(6)-acetyl-L-lysine Chemical compound CC(=O)NCCCC[C@H]([NH3+])C([O-])=O DTERQYGMUDWYAZ-ZETCQYMHSA-N 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 230000001594 aberrant effect Effects 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 230000005754 cellular signaling Effects 0.000 abstract 1
- 230000006718 epigenetic regulation Effects 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 230000001613 neoplastic effect Effects 0.000 abstract 1
- 102000004169 proteins and genes Human genes 0.000 abstract 1
- 108090000623 proteins and genes Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Las formas de realización de la presente se refieren a compuestos terapéuticos derivados heterocíclicos sustituidos, composiciones que comprenden dichos compuestos, y el uso de dichos compuestos y composiciones para la regulación epigenética mediante la inhibición del reconocimiento mediado por bromodominios de regiones de acetil lisina de proteínas, tales como las histonas. Dichas composiciones y métodos son útiles para el tratamiento de enfermedades mediadas por la señalización celular aberrante, tales como trastornos inflamatorios, cáncer y enfermedad neoplásica. Los compuestos particulares descriptos en la presente exhiben actividad inhibidora selectiva contra CBP en comparación con BRD4. Reivindicación 1: Un compuesto que tiene la estructura de fórmula (1), en donde un compuesto de fórmula (1) incluye una sal farmacéuticamente aceptable del mismo, y en donde X⁶ es N o CR⁷, en donde R⁷ es hidrógeno, halógeno, alquilo o alcoxi; R² es hidrógeno, alquilo, arilo, aralquilo, cicloalquilo, cicloalquilalquilo, heterociclilo, heterociclilalquilo, heteroarilo o heteroarilalquilo; R⁵ es hidrógeno, halógeno, -CN, -N(R²²)₂, -NH(R²²), -N(R²²)SO₂R²¹, -N(R²²)SO₂N(R²²)₂, -N(R²²)CO(R²²), -N(R²²)CO₂R²¹, -N(R²²)CON(R²²)₂, -OC(O)N(R²²)₂, -C(O)N(R²²)₂, -OW, -NW, -SW, -SO₂W, o alquilo, arilo, aralquilo, heteroarilo, heteroarilalquilo, cicloalquilo, cicloalquilalquilo, heterociclilo o heterociclilalquilo opcionalmente sustituido, en donde W es por lo menos un hidrógeno, -N(R²²)₂, o alquilo, arilo, aralquilo, cicloalquilo, cicloalquilalquilo, heterociclilo, heterociclilalquilo, heteroarilo o heteroarilalquilo opcionalmente sustituido; R⁶ es hidrógeno, halógeno, -CN, alquilo, cicloalquilo, cicloalquilalquilo, arilo, aralquilo, heteroarilo, heteroarilalquilo, heterociclilo, heterociclilalquilo, -OR²² o -N(R²²)₂; o R⁵ y R⁶ tomados en conjunto forman un anillo de 5 ó 6 miembros opcionalmente sustituido; RA es heteroarilo opcionalmente sustituido que contiene N; en donde cada R²² se selecciona de manera independiente de hidrógeno, alquilo, cicloalquilo, cicloalquilalquilo, arilo, aralquilo, heterociclilo, heterociclilalquilo, heteroarilo o heteroarilalquilo.The embodiments herein refer to substituted heterocyclic derivative therapeutic compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibiting bromodomain-mediated recognition of regions of protein acetyl lysine, such as histones. Such compositions and methods are useful for the treatment of diseases mediated by aberrant cell signaling, such as inflammatory disorders, cancer and neoplastic disease. The particular compounds described herein exhibit selective inhibitory activity against CBP compared to BRD4. Claim 1: A compound having the structure of formula (1), wherein a compound of formula (1) includes a pharmaceutically acceptable salt thereof, and wherein X⁶ is N or CR⁷, wherein R⁷ is hydrogen, halogen, alkyl or alkoxy; R² is hydrogen, alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, heteroaryl or heteroarylalkyl; R⁵ is hydrogen, halogen, -CN, -N (R²²) ₂, -NH (R²²), -N (R²²) SO₂R²¹, -N (R²²) SO₂N (R²²) ₂, -N (R²²) CO (R²²), -N (R²²) CO₂R²¹, -N (R²²) WITH (R²²) ₂, -OC (O) N (R²²) ₂, -C (O) N (R²²) ₂, -OW, -NW, -SW, - SO₂W, or alkyl, aryl, aralkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl or heterocyclyl optionally substituted, where W is at least one hydrogen, -N (R²²) ₂, or alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl , optionally substituted heterocyclyl, heterocyclylalkyl, heteroaryl or heteroarylalkyl; R⁶ is hydrogen, halogen, -CN, alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heteroaryl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl, -OR²² or -N (R²²) ₂; or R⁵ and R⁶ taken together form an optionally substituted 5 or 6 member ring; RA is optionally substituted heteroaryl containing N; wherein each R²² is independently selected from hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heterocyclyl, heterocyclylalkyl, heteroaryl or heteroarylalkyl.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762486894P | 2017-04-18 | 2017-04-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR111479A1 true AR111479A1 (en) | 2019-07-17 |
Family
ID=67439461
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP180100992A AR111479A1 (en) | 2017-04-18 | 2018-04-18 | COMPOUNDS DERIVED FROM PIRIDINA AND PIRAZOL |
Country Status (1)
| Country | Link |
|---|---|
| AR (1) | AR111479A1 (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11890275B2 (en) | 2017-04-18 | 2024-02-06 | Celgene Quanticel Research, Inc. | Therapeutic compounds |
-
2018
- 2018-04-18 AR ARP180100992A patent/AR111479A1/en not_active Application Discontinuation
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11890275B2 (en) | 2017-04-18 | 2024-02-06 | Celgene Quanticel Research, Inc. | Therapeutic compounds |
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