ES2624379T3 - Derivados de heterociclilo y su uso como moduladores del receptor de prostaglandina D2 - Google Patents

Derivados de heterociclilo y su uso como moduladores del receptor de prostaglandina D2 Download PDF

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ES2624379T3
ES2624379T3 ES12823031T ES12823031T ES2624379T3 ES 2624379 T3 ES2624379 T3 ES 2624379T3 ES 12823031 T ES12823031 T ES 12823031T ES 12823031 T ES12823031 T ES 12823031T ES 2624379 T3 ES2624379 T3 ES 2624379T3
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substituted
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halogen
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Hamed Aissaoui
Christoph Boss
Sylvia Richard-Bildstein
Romain Siegrist
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Idorsia Pharmaceuticals Ltd
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    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
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    • C07D223/06—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings 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
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  • Plural Heterocyclic Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Un compuesto de fórmula (I):**Fórmula** en la que R1 representa hidrógeno, alquilo (C1-C4), alcoxi (C1-C4), fluoroalquilo (C1-C4), alquilsulfonilo (C1-C4), halógeno o ciano; R2 representa hidrógeno o halógeno; uno de R3, R4 y R5 representa carboxi-alquilo (C1-C3), carboxi-ciclopropilo o carboxi-alcoxi (C1-C3) y los otros dos representan independientemente entre sí hidrógeno, alcoxi (C1-C4) o halógeno; R6 representa hidrógeno, alcoxi (C1-C4) o halógeno; R7 representa hidrógeno, alquilo (C1-C4), alcoxi (C1-C4), cicloalquil (C3-C6)-metoxi, cicloalquiloxi (C3-C6), metoxietoxi, di-[alquilo (C1-C2)]-amino, fluoroalquilo (C1-C4), fluoroalcoxi (C1-C4), halógeno o alquilsulfonilo (C1-C4); o R6 y R7 juntos representan metilendioxi o etilendioxi; R8 representa: - alquilo (C2-C5); - alquilo (C1-C5) que está mono- o di-sustituido donde los sustituyentes se seleccionan independientemente del grupo que consiste en hidroxi, alcoxi (C1-C4), oxo, -NR9R10, cicloalquilo (C3-C6) en el que los grupos cicloalquilo (C3-C6) están no sustituidos o mono-sustituidos con alquilo (C1-C4), alcoxi (C1-C4), hidroxilo o fenilo que está no sustituido o mono-sustituido con halógeno, y en el que un grupo cicloalquilo que contiene cuatro, cinco o seis átomos de carbono puede estar anillado de manera opcional a un anillo benceno o un anillo piridina, en el que el anillo benceno está opcionalmente mono-sustituido con metoxi; arilo en el que el término "arilo" significa un grupo fenilo o un grupo naftilo grupos que están independientemente no sustituidos, mono-, di- o tri-sustituidos, en los que los sustituyentes se seleccionan independientemente del grupo que consiste en halógeno, alquilo (C1-C4), alcoxi (C1-C4) fluoroalquilo (C1-C4) y fluoroalcoxi (C1-C4); heteroarilo en el que el término "heteroarilo" significa un anillo aromático monocíclico o bicíclico de 5 a 10 miembros que contiene 1, 2, 3 o 4 heteroátomos independientemente seleccionados de oxígeno, nitrógeno y azufre y en el que los grupos heteroarilo están independientemente no sustituidos, mono-, di- o tri-sustituidos, en los que los sustituyentes se seleccionan independientemente del grupo que consiste en halógeno, alquilo (C1-C4), alcoxi (C1-C4) y fluoroalquilo (C1-C4); heterociclilo en el que el término "heterociclilo" significa un resto monocíclico saturado de 5 a 7 miembros del anillo que contienen 1 o 2 heteroátomos seleccionados de nitrógeno, oxígeno y azufre, entendiéndose que un grupo heterociclilo no contiene 2 átomos de azufre, en el que el átomo de azufre de un grupo heterociclilo puede estar en una forma oxidada, en el que un grupo heterociclilo puede opcionalmente anillarse a un anillo de benceno o a un anillo de piridina en el que el anillo de benceno está opcionalmente mono-sustituido con fluoro, y en el que los grupos heterociclilo están independientemente no sustituidos, mono-, di- o tri-sustituidos, en los que los sustituyentes se seleccionan independientemente del grupo que consiste en halógeno, oxo y alquilo (C1-C4); ariloxi en el que el término "ariloxi" significa un grupo feniloxi o naftiloxi, grupos que están independientemente no sustituidos, mono-, dio tri-sustituidos, en los que los sustituyentes se seleccionan independientemente del grupo que consiste en halógeno, alquilo (C1-C4), alcoxi (C1-C4) y fluoroalquilo (C1-C4); heteroariloxi en el que el término "heteroarilo" significa un anillo aromático monocíclico o bicíclico de 5 a 10 miembros que contiene 1, 2, 3 o 4 heteroátomos independientemente seleccionados de oxígeno, nitrógeno y azufre y en el que los grupos heteroariloxi están independientemente no sustituidos, mono-, di- o tri-sustituidos, en los que los sustituyentes se seleccionan independientemente del grupo que consiste en halógeno, alquilo (C1-C4), alcoxi (C1-C4) y fluoroalquilo (C1- C4); o arilalcoxi (C1-C2) en el que el término "arilo" significa un grupo fenilo o uno naftilo y en el que los grupos arilo están independientemente no sustituidos, mono-, di- o tri-sustituidos, en los que los sustituyentes se seleccionan independientemente del grupo que consiste en halógeno, alquilo (C1-C4), alcoxi (C1-C4) y fluoroalquilo (C1-C4); - alquenilo (C3-C5); - alquenilo (C2-C3) que está mono-sustituido con arilo en el que el término "arilo" significa un grupo fenilo o uno naftilo grupos que están independientemente no sustituidos, mono-, di- o tri-sustituidos, en los que los sustituyentes se seleccionan independientemente del grupo que consiste en halógeno, alquilo (C1-C4), alcoxi (C1-C4) y fluoroalquilo (C1-C4); o heteroarilo en el que el término "heteroarilo" significa un anillo aromático monocíclico o bicíclico de 5 a 10 miembros que contiene 1, 2, 3 o 4 heteroátomos independientemente seleccionados de oxígeno, nitrógeno y azufre y en el que los grupos heteroarilo están independientemente no sustituidos, mono-, di- o tri-sustituidos, en los que los sustituyentes se seleccionan independientemente del grupo que consiste en halógeno, alquilo (C1-C4), alcoxi (C1-C4) y fluoroalquilo (C1-C4); - alquinilo (C3-C5); - cicloalquilo (C3-C6) que está no sustituido, mono-, di-, tri- o tetra-sustituido con metilo; mono-sustituido con oxo; mono-sustituido con arilo en el que el término "arilo" significa un grupo fenilo o uno naftilo grupos que están independientemente no sustituidos, mono-, di- o tri-sustituidos, en los que los sustituyentes se seleccionan independientemente del grupo que consiste en halógeno, alquilo (C1-C4), alcoxi (C1-C4) y fluoroalquilo (C1-C4); o mono-sustituido con heteroarilo en el que el término "heteroarilo" significa un anillo aromático monocíclico o bicíclico de 5 a 10 miembros que contiene 1, 2, 3 o 4 heteroátomos independientemente seleccionados de oxígeno, nitrógeno y azufre y en el que los grupos heteroarilo están independientemente no sustituidos, mono-, di- o tri-sustituidos, en los que los sustituyentes se seleccionan independientemente del grupo que consiste en halógeno, alquilo (C1-C4), alcoxi (C1-C4) y fluoroalquilo (C1- C4); o - heterociclilo que está opcionalmente mono-sustituido con oxo; R9 representa alquilo (C1-C4); R10 representa difenilmetilo en el que los grupos fenilo están independientemente no sustituidos o mono sustituidos con halógeno; n representa 1 o 2; m representa 1 o 2; y Z representa -NH-, -O- o un enlace; o una sal de dicho compuesto.
ES12823031T 2011-12-21 2012-12-20 Derivados de heterociclilo y su uso como moduladores del receptor de prostaglandina D2 Active ES2624379T3 (es)

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IB2011055866 2011-12-21
PCT/IB2012/057541 WO2013093842A1 (en) 2011-12-21 2012-12-20 Heterocyclyl derivatives and their use as prostaglandin d2 receptor modulators

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US (1) US9255090B2 (es)
EP (1) EP2794563B1 (es)
JP (1) JP6097765B2 (es)
KR (1) KR20140107550A (es)
CN (1) CN104011021B (es)
AR (1) AR089360A1 (es)
AU (1) AU2012356076A1 (es)
BR (1) BR112014015081A2 (es)
CA (1) CA2858328A1 (es)
ES (1) ES2624379T3 (es)
MX (1) MX2014007688A (es)
RU (1) RU2014129613A (es)
TW (1) TW201331179A (es)
WO (1) WO2013093842A1 (es)

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US20150252036A1 (en) 2015-09-10
BR112014015081A8 (pt) 2017-06-13
EP2794563B1 (en) 2017-02-22
CN104011021A (zh) 2014-08-27
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TW201331179A (zh) 2013-08-01
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AR089360A1 (es) 2014-08-20
EP2794563A1 (en) 2014-10-29
BR112014015081A2 (pt) 2017-06-13
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AU2012356076A1 (en) 2014-08-14

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