AR090025A1 - Antagonistas del receptor del acido lisofosfatidico - Google Patents

Antagonistas del receptor del acido lisofosfatidico

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Publication number
AR090025A1
AR090025A1 ARP120102985A ARP120102985A AR090025A1 AR 090025 A1 AR090025 A1 AR 090025A1 AR P120102985 A ARP120102985 A AR P120102985A AR P120102985 A ARP120102985 A AR P120102985A AR 090025 A1 AR090025 A1 AR 090025A1
Authority
AR
Argentina
Prior art keywords
connector
formula
optionally substituted
alkyl
heterocycle
Prior art date
Application number
ARP120102985A
Other languages
English (en)
Inventor
b nicholas John
Emayan Kumaraswamy
Buckman Brad
D Seiwert Scott
Original Assignee
Intermune Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Intermune Inc filed Critical Intermune Inc
Publication of AR090025A1 publication Critical patent/AR090025A1/es

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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
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    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
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    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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Abstract

Se proporcionan compuestos, métodos para producir estos compuestos, composiciones farmacéuticas y medicamentos que comprenden estos compuestos, y métodos para usar estos compuestos para tratar, prevenir, diagnosticar enfermedades, trastornos, o afecciones asociadas con uno o más de los receptores del ácido lisofosfatídico. Estas enfermedades están relacionadas con funciones neuronales. Reivindicación 1: Un compuesto de fórmula (1), una sal aceptable para uso farmacéutico del mismo, donde: A es un acetileno o un sistema anular seleccionado de heterociclo de 4 a 7 miembros, hidrocarbilo cíclico de 4 a 7 miembros, heterociclo bicíclico de 8 a 11 miembros, o hidrocarbilo bicíclico de 8 a 11 miembros, donde el sistema anular es no aromático, aromático, o parcialmente aromático, y donde el sistema anular es no sustituido o sustituido con uno o más sustituyentes seleccionados de alquilo, halo, u oxo; B es un acetileno o un sistema anular seleccionado de heterociclo de 4 a 7 miembros, hidrocarbilo cíclico de 4 a 7 miembros, heterociclo bicíclico de 8 a 11 miembros, o hidrocarbilo bicíclico de 8 a 11 miembros, donde el sistema anular es no aromático, aromático, o parcialmente aromático, y donde el sistema anular es no sustituido o sustituido con uno o más sustituyentes seleccionados de alquilo, halo, u oxo; o B está opcionalmente ausente cuando el anillo C de fórmula (2) es el resto de fórmula (3) o una variante opcionalmente sustituida del mismo; el anillo C de fórmula (2) es un sistema anular seleccionado de heterociclo de 5 a 7 miembros, hidrocarbilo cíclico de 5 a 7 miembros, heterociclo bicíclico de 8 a 11 miembros, y hidrocarbilo bicíclico de 8 a 11 miembros, donde el sistema anular es aromático o parcialmente aromático, y donde el sistema anular puede estar opcionalmente sustituido, y L⁴ es un compuesto del grupo de fórmulas (4), o alternativamente, el resto de fórmula (5) es un compuesto de fórmula (6) ó (7); donde el resto de fórmula (8) se selecciona del grupo de fórmulas (9), o variantes opcionalmente sustituidas del mismo; L¹ se selecciona de un enlace, un conector -O-, un conector -NH-, un conector -C(O)-, un conector -CH₂-, un conector -CH₂O-, un conector -OCH₂-, un conector -CºC-, un conector -CH=CH-, un conector =C(R¹⁵)-, o un conector -C(R¹⁵)=; L² se selecciona de un enlace, un conector -O-, un conector -NH-, un conector -C(O)-, un conector -CH₂-, un conector -CH₂O-, un conector -OCH₂-, un conector -CºC-, un conector -CH=CH-; L³ está ausente, es un compuesto del grupo de fórmulas (10), un conector =C(R¹⁵)-, o un conector -C(R¹⁵)=; W es C(R⁶)₂, NR⁶, ó O; X es un resto de fórmula (11) ó S(O)ₚ; cada Y se selecciona independientemente de CR⁶ o N; Y¹ es C(R⁶)₂, NR⁶, ó O; cada Y⁴ está independientemente ausente, CR⁹ o N, siempre que sólo un Y⁴ pueda estar ausente; L⁵ se selecciona de un enlace, un conector -CH₂O-, un conector -OCH₂-, un conector -CH=CH- o un heterociclo de 4 a 7 miembros; D se selecciona del grupo de fórmulas (12), o isósteres del ácido carboxílico; R² y R³ se selecciona cada uno de ellos independientemente de H, alquilo, arilo, o heteroarilo; o R² y R³ se unen junto con el átomo al cual están unidos para formar un cicloalquilo opcionalmente sustituido o un heterociclo opcionalmente sustituido; o R² se selecciona de H, alquilo, o arilo y R³ se une a un átomo a hasta un punto de unión de L⁵ hasta A para formar un cicloalquilo opcionalmente sustituido o un heterociclo opcionalmente sustituido; o R³ se selecciona de H, alquilo, y arilo y R² se une a un átomo a hasta un punto de unión de L⁵ hasta A para formar un cicloalquilo opcionalmente sustituido o un heterociclo opcionalmente sustituido; cada R⁴ y R⁵ se selecciona independientemente de H y alquilo; o R⁴ y R⁵ se unen junto con el átomo al cual están unidos para formar un cicloalquilo opcionalmente sustituido o heterociclo opcionalmente sustituido; cada R⁶ se selecciona independientemente de H, alquilo, halo, arilo, o cicloalquilo C₃₋₆; cada R¹⁰ se selecciona independientemente de H, alquilo, halo, arilo, cicloalquilo C₃₋₆, o ciano; cada R⁹ se selecciona independientemente de H, alquilo o halógeno o dos R⁹ se unen junto con el átomo al cual están unidos para formar un carbociclo opcionalmente sustituido o heterociclo opcionalmente sustituido; cada R⁷ y R⁸ es independientemente H o alquilo C₁₋₆, o R⁷ y R⁸ se unen junto con el átomo o los átomos a los cuales están unidos para formar un heterociclo espirocíclico, un carbociclo espirocíclico, un heterociclo fusionado, o un carbociclo fusionado; cada R¹⁵ se selecciona independientemente de H, alquilo, halo, o ciano; m es independientemente un entero de 0 - 3; n es un entero de 0 - 3; p es un entero de 1 - 2; q es un entero de 1 - 6; y ⁻ ⁻ ⁻ ⁻ ⁻ representa un enlace simple o doble; siempre que al menos se cumpla una de las siguientes condiciones en el compuesto de fórmula (1): I) si A y B se seleccionan independientemente de fenilo, ciclohexilo, indolilo, heteroarilo de 5 miembros, heteroarilo de 6 miembros, y sus variantes sustituidos con halo o metilo; si el anillo C de fórmula (2) es un resto de fórmula (13) ó (14); si L³ está ausente; si L⁵ es un enlace; si D es -COOR⁶ y m es 0 ó 1; y si R² y R³ son ambos H, o R² es H y R³ es alquilo, o R² y R³ se unen junto con el átomo al cual están unidos para formar un cicloalquilo opcionalmente sustituido; entonces el compuesto de fórmula (15) no es un compuesto de fórmula (16); II) si A y B son ambos fenilo; si L¹ es un conector -CH₂O-, un conector -CH₂O-, un conector -OCH₂-, o un conector -CºC-; si el anillo C de fórmula (2) es un resto de fórmula (13); L³ está ausente; si L⁵ es un enlace; y si D es -COOH y m es 1; entonces el compuesto de fórmula (15) no es un compuesto de fórmula (16); III) si A y B son ambos fenilo; si el anillo C de fórmula (2) es el resto de fórmula (13); si L¹, L², y L⁵ son todos un enlace; si L³ está ausente; si D es -COOH y m es 1; si R² y R³ son ambos H, o R² es H y R³ es alquilo, o R² y R³ se unen junto con el átomo al cual están unidos para formar un cicloalquilo opcionalmente sustituido; si R⁴ y R⁵ son H o alquilo; entonces L⁴ es un ligamiento amida, un ligamiento carbamato, un ligamiento urea, un ligamiento metil urea, un ligamiento -CH₂S(=O)CH₂- o un ligamiento -CH₂C(=O)CH₂-; IV) si A y B son ambos fenilo; si el anillo C de fórmula (2) es el resto de fórmula (13); si L¹, L², y L⁵ son todos un enlace; si L³ está ausente; si D es -COOH y m es 1; si n es 1; si un R⁹ es cloro; y si R⁴ y R⁵ son ambos H; entonces L⁴ no es un ligamiento -NH-SO₂-; y V) si A es un resto de fórmula (17); si B es fenilo; si el anillo C de fórmula (2) es un resto de fórmula (13); si n es 1; si un R⁹ es cloro; si R⁴ es metilo; y si R⁵ es hidrógeno; entonces L⁴ no es -NHC(O)O-; y siempre que el compuesto de fórmula (1) no pueda tener la estructura seleccionada del grupo de fórmulas (18); donde Rᵃ es H o etilo.
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US8975235B2 (en) 2015-03-10
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