AR089445A1 - Heteroarilos y sus usos - Google Patents
Heteroarilos y sus usosInfo
- Publication number
- AR089445A1 AR089445A1 ARP120104956A ARP120104956A AR089445A1 AR 089445 A1 AR089445 A1 AR 089445A1 AR P120104956 A ARP120104956 A AR P120104956A AR P120104956 A ARP120104956 A AR P120104956A AR 089445 A1 AR089445 A1 AR 089445A1
- Authority
- AR
- Argentina
- Prior art keywords
- optionally substituted
- nitrogen
- membered
- sulfur
- oxygen
- Prior art date
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- 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
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- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- 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
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- 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
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- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/36—Oxygen or sulfur atoms
- C07D207/40—2,5-Pyrrolidine-diones
- C07D207/416—2,5-Pyrrolidine-diones with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
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- 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
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- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/14—Ortho-condensed systems
Abstract
Reivindicación 1: Un compuesto de fórmula (1) o una sal del mismo farmacéuticamente aceptable, caracterizado porque: -G⁵-G⁶-G⁷-G⁸-G⁹ es -CR³=C-N-N=C, -CR³=C-N-CR³=C, =CR³-C=C-NR¹⁵-C, =CR³-N-C=CR³-C, =N-N-C=CR³-C o -NR¹⁵-C=C-CR³=C; cuando G⁵ y G⁶ ambos son nitrógeno, o G⁷ y G⁸ ambos son nitrógeno, entonces R³ es hidrógeno, -CN, halógeno, -Z-R⁵, o un grupo opcionalmente sustituido seleccionado de alifático C₁₋₆ y cicloalifático 3 a 10-miembros, en donde: Z es seleccionado de una cadena alquileno C₁₋₃ opcionalmente sustituida, -O-, -N(R³ᵃ)-, -S-, -S(O)-, -S(O)₂-, -C(O)-, -CO₂-, -C(O)NR³ᵃ-, -N(R³ᵃ)C(O)-, -N(R³ᵃ)CO₂-, -S(O)₂NR³ᵃ-, -N(R³ᵃ)S(O)₂, -OC(O)N(R³ᵃ)-, -N(R³ᵃ)C(O)NR³ᵃ-, -N(R³ᵃ)S(O)₂N(R³ᵃ)-, o -OC(O)-; R³ᵃ es hidrógeno o un alifático C₁₋₄ opcionalmente sustituido, y R⁵ es hidrógeno o un grupo opcionalmente sustituido seleccionado de alifático C₁₋₆, cicloalifático 3 a 10-miembros, heterociclilo 4 a 10-miembros que tiene 1 - 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno, o azufre, arilo 6 a 10-miembros o heteroarilo 5 a 10-miembros que tiene 1 - 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno, o azufre; cuyo G⁵ es CR³ y G⁶ es nitrógeno, o G⁶ es carbono y G⁵ es NR¹⁵, o G⁷ es N y G⁸ es CR³, o G⁷ es C y G⁸ es NR¹⁵ entonces cada aparición de R³ es independientemente hidrógeno, CN, o un alifático C₁₋₃ opcionalmente sustituido; R¹⁵ es hidrógeno, ciclopropilo, o un grupo alifático C₁₋₆ opcionalmente sustituido; R¹ es -CN, -C(O)N(R⁴)₂, -C(O)OR⁴, -C(NR⁴)N(R⁴)₂, -NHCOR⁴, -NHSO₂R⁴, -NHCON(R⁴)₂, -NHCOOR⁴, -NHSO₂N(R⁴)₂, -CH₂OR⁴, -CH₂N(R⁴)₂, -CH₂NHC(O)R⁴, -SO₂N(R⁴)₂, -C(O)NHC(=NH)N(R⁴)₂, -NHSO₂OR⁴, o CY, en donde CY es un grupo opcionalmente sustituido seleccionado de un cicloalifático de 3 a 7 miembros; un heterociclilo de 4 a 10 miembros que tiene 1 - 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno, o azufre; un arilo 6 a 10-miembros, o heteroarilo 5 a 10-miembros que tiene 1 - 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno, o azufre; en donde cada R⁴ es independientemente seleccionado de hidrógeno, -OH, o un grupo opcionalmente sustituido seleccionado de alifático C₁₋₆, cicloalifático 3 a 10-miembros, arilo 6 a 10-miembros, o heteroarilo 5 a 10-miembros que tiene 1 - 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno, o azufre; o R⁴ es -Z²-R⁶ en donde: Z² es seleccionado de una cadena alquileno C₁₋₃ opcionalmente sustituida, -S(O)-, -S(O)₂-, -C(O)-, -CO₂-, -C(O)NR⁴ᵃ-, -C(NH)-, o -S(O)₂NR⁴ᵃ-; R⁴ᵃ es hidrógeno o un alifático C₁₋₄ opcionalmente sustituido, y R⁶ es hidrógeno, -NH₂, o un grupo opcionalmente sustituido seleccionado de alifático C₁₋₆, cicloalifático 3 a 10-miembros, heterociclilo 4 a 10-miembros que tiene 1 - 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno, o azufre, arilo 6 a 10-miembros, o heteroarilo 5 a 10-miembros que tiene 1 - 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno, o azufre; o dos apariciones de R⁴, tomados juntos con un átomo de nitrógeno al cual están unidos, forman un anillo heterociclilo de 4 a 7 miembros opcionalmente sustituido que tiene 0 - 1 heteroátomos adicionales independientemente seleccionados de nitrógeno, oxígeno, o azufre; R² es hidrógeno, halo, o un grupo opcionalmente sustituido seleccionado de alifático C₁₋₆, cicloalifático 3 a 10-miembros, heterociclilo 4 a 10-miembros que tiene 1 - 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno, o azufre, arilo 6 a 10-miembros, o heteroarilo 5 a 10-miembros que tiene 1 - 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno, o azufre, en donde R² es opcionalmente sustituido con 1 - 4 apariciones de R²ᵃ, en donde cada aparición de R²ᵃ es independientemente -R¹²ᵃ, -T²-R¹²ᵈ, -T²-R¹²ᵃ, o -V²-T²-R¹²ᵈ, y: cada aparición de R¹²ᵃ es independientemente halógeno, -CN, -NO₂, -R¹²ᶜ, -N(R¹²ᵇ)₂, -OR¹²ᵇ, -SR¹²ᶜ, -S(O)₂R¹²ᶜ, -C(O)R¹²ᵇ, -C(O)OR¹²ᵇ, -C(O)N(R¹²ᵇ)₂, -S(O)₂N(R¹²ᵇ)₂, -OC(O)N(R¹²ᵇ)₂, -N(R¹²ᵉ)C(O)R¹²ᵇ, -N(R¹²ᵉ)SO₂R¹²ᶜ, -N(R¹²ᵉ)C(O)OR¹²ᵇ, -N(R¹²ᵉ)C(O)N(R¹²ᵇ)₂, o -N(R¹²ᵉ)SO₂N(R¹²ᵇ)₂, o un alifático C₁₋₆ o haloalifático C₁₋₆ opcionalmente sustituido; cada aparición de R¹²ᵇ es independientemente hidrógeno o un grupo opcionalmente sustituido seleccionado de alifático C₁₋₆, cicloalifático 3 a 10-miembros, heterociclilo 4 a 10-miembros que tiene 1 - 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno, o azufre, arilo 6 a 10-miembros o heteroarilo 5 a 10-miembros que tiene 1 - 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno, o azufre, o dos apariciones de R¹²ᵇ, tomados juntos con un átomo de nitrógeno al cual están unidos, forman un anillo heterociclilo de 4 a 7 miembros opcionalmente sustituido que tiene 0 - 1 heteroátomos adicionales seleccionado de nitrógeno, oxígeno, o azufre; cada aparición de R¹²ᶜ es independientemente hidrógeno o un grupo opcionalmente sustituido seleccionado de alifático C₁₋₆, haloalifático C₁₋₆, cicloalifático 3 a 10-miembros, heterociclilo 4 a 10-miembros que tiene 1 - 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno, o azufre, arilo 6 a 10-miembros, o heteroarilo 5 a 10-miembros que tiene 1 - 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno, o azufre; cada aparición de R¹²ᵈ es independientemente hidrógeno o un grupo opcionalmente sustituido seleccionado de cicloalifático 3 a 10-miembros, heterociclilo 4 a 10-miembros que tiene 1 - 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno, o azufre, arilo 6 a 10-miembros o heteroarilo 5 a 10-miembros que tiene 1 - 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno, o azufre; cada aparición de R¹²ᵉ es independientemente hidrógeno o un grupo alifático C₁₋₆ opcionalmente sustituido; cada aparición de V² es independientemente -N(R¹²ᵉ)-, -O-, -S-, -S(O)-, -S(O)₂-, -C(O)-, -C(O)O-, -C(O)N(R¹²ᵉ)-, -S(O)₂N(R¹²ᵉ)-, -OC(O)N(R¹²ᵉ)-, -N(R¹²ᵉ)C(O)-, -N(R¹²ᵉ)SO₂-, -N(R¹²ᵉ)C(O)O-, -N(R¹²ᵉ)C(O)N(R¹²ᵉ)-, -N(R¹²ᵉ)SO₂N(R¹²ᵉ)-, -OC(O)-, o -C(O)N(R¹²ᵉ)-O-; y T² es una cadena alquileno C₁₋₆ opcionalmente sustituido en donde la cadena alquileno es opcionalmente interrumpida por -N(R¹³)-, -O-, -S-, -S(O)-, -S(O)₂-, -C(O)-, -C(O)O-, -C(O)N(R¹³)-, -S(O)₂N(R¹³)-, -OC(O)N(R¹³)-, -N(R¹³)C(O)-, -N(R¹³)SO₂-, -N(R¹³)C(O)O-, -N(R¹³)C(O)N(R¹³)-, -N(R¹³)S(O)₂N(R¹³)-, -OC(O)-, o -C(O)N(R¹³)-O- o en donde T² o una porción del mismo opcionalmente forma parte de un cicloalifático de 3 a 7 miembros opcionalmente sustituido o anillo heterociclilo en donde R¹³ es hidrógeno o un grupo alifático C₁₋₄ opcionalmente sustituido; y HY es un compuesto seleccionado del grupo de fórmulas (2) en donde cada aparición de X⁴, X⁵, X⁶, X⁷, y X⁸ es independientemente -CR¹⁰, -CR¹⁰, o N, siempre que no más de dos apariciones de X⁴, X⁵, X⁶, X⁷, y X⁸ es N; cada aparición de Y¹, Y², Y³, Y⁴, Y⁵, Y⁶, Y⁷, y Y⁸ es -CR¹⁰; cada aparición de Q¹ y Q² es independientemente S, O ó -NR⁹; dos apariciones adyacentes de X⁴ y X⁵, X⁶ y X⁷, X⁷ y X⁸, Y¹ y -NR⁹, Y³ y -NR⁹, o Y⁴ y Y⁵, pueden ser tomados juntos con los átomos al cual están unidos, para formar un grupo heteroarilo o heterociclilo fusionado no sustituido que tiene de 8 a 10 átomos y que tiene 1 - 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno, o azufre; cada aparición de R¹⁰ o R¹⁰ es independientemente -R¹⁰ᵇ, -V¹-R¹⁰ᶜ, -T¹-R¹⁰ᵇ, o -V¹-T¹-R¹⁰ᵇ, en donde V¹ es -NR¹¹-, -NR¹¹-C(O)-, -NR¹¹-C(S)-, -NR¹¹C(NR¹¹)-, -NR¹¹C(O)O-, -NR¹¹C(O)NR¹¹-, -NR¹¹C(O)S-, -NR¹¹C(S)O-, -NR¹¹(S)NR¹¹-, -NR¹¹C(S)S-, -NR¹¹C(NR¹¹)O-, -NR¹¹C(NR¹¹)NR¹¹-, -NR¹¹S(O)₂-, -NR¹¹S(O)₂NR¹¹-, -C(O)-, -CO₂-, -C(O)NR¹¹-, -C(O)NR¹¹O-, -SO₂-, o -SO₂NR¹¹-; cada aparición de R¹⁰ᵃ es independientemente hidrógeno o un grupo opcionalmente sustituido seleccionado de alifático C₁₋₆, cicloalifático 3 a 10-miembros, heterociclilo 4 a 10-miembros que tiene 1 - 5 heteroátomos independientemente seleccionados de nitrógeno oxígeno, o azufre, arilo 6 a 10-miembros o heteroarilo 5 a 10-miembros que tiene 1 - 5 heteroátomos independientemente seleccionados de nitrógeno, oxígeno, o azufre; T¹ es una cadena alquileno C₁₋₆ opcionalmente sustituida en donde la cadena a
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US20130165483A1 (en) | 2013-06-27 |
UY34539A (es) | 2013-06-28 |
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EP2793880A1 (en) | 2014-10-29 |
WO2013096642A1 (en) | 2013-06-27 |
EP2793894A1 (en) | 2014-10-29 |
UY34540A (es) | 2013-06-28 |
WO2013096637A1 (en) | 2013-06-27 |
AR089446A1 (es) | 2014-08-27 |
TW201332989A (zh) | 2013-08-16 |
UY34538A (es) | 2013-06-28 |
JP2015506347A (ja) | 2015-03-02 |
WO2013096630A1 (en) | 2013-06-27 |
US20130165472A1 (en) | 2013-06-27 |
JP2015503505A (ja) | 2015-02-02 |
TW201332988A (zh) | 2013-08-16 |
TW201331194A (zh) | 2013-08-01 |
JP2015503504A (ja) | 2015-02-02 |
EP2793894A4 (en) | 2015-07-08 |
AR089447A1 (es) | 2014-08-27 |
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