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AR074336A1 - Compuestos de arilo con sustituyentes heterociclicos y su uso - Google Patents

Compuestos de arilo con sustituyentes heterociclicos y su uso

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Publication number
AR074336A1
AR074336A1 ARP090104356A ARP090104356A AR074336A1 AR 074336 A1 AR074336 A1 AR 074336A1 AR P090104356 A ARP090104356 A AR P090104356A AR P090104356 A ARP090104356 A AR P090104356A AR 074336 A1 AR074336 A1 AR 074336A1
Authority
AR
Argentina
Prior art keywords
ring
alkyl
alkylamino
series
cycloalkyl
Prior art date
Application number
ARP090104356A
Other languages
English (en)
Inventor
Michael Haerter
Peter Ellinghaus
Karl-Heinz Thierauch
Susanne Greschat
Kerstin Berhoerster
Beck Hartmut Dr
Frank Suebmeier
Original Assignee
Bayer Schering Pharma Ag
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
Priority claimed from DE102008057343A external-priority patent/DE102008057343A1/de
Priority claimed from DE102009041242A external-priority patent/DE102009041242A1/de
Application filed by Bayer Schering Pharma Ag filed Critical Bayer Schering Pharma Ag
Publication of AR074336A1 publication Critical patent/AR074336A1/es

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    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
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  • General Health & Medical Sciences (AREA)
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  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
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  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
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  • Pulmonology (AREA)
  • Immunology (AREA)
  • Vascular Medicine (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Se refiere a compuestos de arilo novedosos con sustituyentes heterocíclicos, a procedimientos para su preparación, a su uso para el tratamiento y/o prevención de enfermedades y a su uso para le preparación de medicamentos para tratamiento y/o prevención de enfermedades, en particular para tratamiento y/o prevención de enfermedades hiperproliferativas y angiogénicas y para aquellas enfermedades que surgen de la adaptación metabólica de estados hipóxicos. Tales tratamientos se pueden llevar a cabo como monoterapia o también en combinación con otros medicamentos o medidas terapéuticas adicionales. Reivindicación 1: Compuesto de la fórmula (1) en la que el anillo A representa un anillo fenilo o piridilo; el anillo B con el sustituyente R3 representa un anillo heteroarilo del grupo de fórmulas (2) en las que designa el punto de unión con el grupo CH2 adyacente y designa el punto de unión con el anillo D; el anillo D representa un anillo heteroarilo del grupo de fórmulas (3) en las que * designa el punto de unión con el anillo B y ** designa el punto de unión con el anillo E; el anillo E representa un anillo fenilo o piridilo; el anillo N representa un aza-heterociclo de 4- a 10- miembros saturado, que contiene al menos un átomo de N como un miembro de anillo y además puede contener uno o dos miembros de anillo hetero adicionales de la serie N, O, S y/o S(O)2; X representa un enlace o ¨-(CH2)qN(R6)-¨¨, ¨-N(R6)-(CH2)q-¨¨, -O-, -S-, -C(=O)-, -S(=O)2-, ¨-C(=O)-N(R6)-¨¨ o ¨-N(R6)-C(=O)-¨¨ en los que ¨ designa el punto de unión con el anillo N y ¨¨ designa el punto de unión con el anillo A; q denoto el número 0, 1 ó 2 y R6 denota hidrógeno, alquilo C1-6 o cicloalquilo C3-6, en el que alquilo C1-6 y cicloalquilo C3-6 pueden estar sustituidos cada uno con hidroxilo o alcoxi C1-4; R1 representa un sustituyente unido a un átomo de carbono del anillo N, elegido a partir de la serie flúor, ciano, alquilo C1-6, hidroxilo, alcoxi C1-6, oxo, amino, mono-alquilamino C1-6, di-alquilamino C1-6 y cicloalquilo C3-6, en los que alquilo C1-6 a su vez puede estar sustituido hasta tres veces por flúor y hasta das veces en una manera idéntica o diferente por un radical elegido de la serie hidroxilo, alcoxi C1-4, amino, mono-alquilamino C1-4 y di-alquilamino C1-4 y cicloalquilo C3-6 a su vez puede estar sustituido hasta dos veces en una manera idéntica o diferente por un radical elegido de la serie flúor, alquilo C1-4, hidroxilo, alcoxi C1-4, amino, mono-alquilamino C1-4 y di-alquilamino C1-4; m representa el número 0, 1, 2, 3 ó 4, en el que en el caso donde el sustituyente R1 aparezca varias veces, su significado puede ser idéntico o diferente; R2 representa un sustituyente unido a un átomo de nitrógeno del anillo N, elegido de la serie alquilo C1-6, alquilcarbonilo C1-6, alcoxicarbonilo C1-6, alquilsulfonilo C1-6 y cicloalquilo C3-6, en los que el grupo alquilo en alquilo C1-6, alquilcarbonilo C1-6, alcoxicarbonilo C1-6 y alquilsulfonilo C1-6 a su vez puede estar sustituido hasta tres veces por flúor y hasta dos veces en una manera idéntica o diferente por un radical elegido a partir de la serie hidroxilo, alcoxi C1-4, amino, monoalquilamino C1-4, dialquilamino C1-4, cicloalquilo C3-6 y heterociclilo de 4- a 6- miembros y cicloalquilo C3-6 a su vez puede estar sustituido hasta dos veces en una manera idéntica o diferente por un radical elegido de la serie flúor, alquilo C1-4, hidroxilo, alcoxi C1-4, amino, mono-alquilamino C1-4 y di-alquilamino C1-4; n representa el número 0 ó 1 o además, si el aza-heterociclo contiene átomos de N adicionales como miembros de anillo, el número 2, en el que en el caso donde el sustituyente R2 aparezca dos veces, su significado puede ser idéntico o diferente; R3 representa metilo, etilo o trifluorometilo; R4 representa hidrógeno o un sustituyente elegido de la serie halógeno, ciano, pentafluorotio, alquilo C1-6, tri-alquilsililo C1-4, -OR7, -NR7R8, N(R7)-c(=o)R8, -N(R7)-C(=O)-OR8, -N(R7)-S(=O)2-R8, -C(=O)OR7, -C(=O)-NR7R8, -SR7, -S(=O)R7, -S(=O)2-R7, -S(=O)2-NR7R8, -S(=O)(NH)-R7, -S(=O)(NCH3)-R7, cicloalquilo C3-6, heterociclilo de 4- a 6- miembros y heteroarilo de 5- a 6- miembros y en los que alquilo C1-6 a su vez puede estar sustituido hasta tres veces por flúor o hasta dos veces en una manera idéntica o diferente por un radical elegido de la serie -OR7, -NR7R8, -N(R7)-C(=O)-R8, -N(R7)-C(=O)-OR8, -C(=O)-OR7, -C(=O)-NR7R8, cicloalquilo C3-6, hetorociclilo de 4- a 6- miembros y heteroarilo de 5- o de 6- miembros y en los que los grupos cicloalquilo y heterociclilo mencionados a su vez pueden estar sustituidos hasta dos veces en una manera idéntica o diferente por un radical elegido de la serie flúor, alquilo C1-4, hidroxilo, alcoxi C1-4, trifluorometoxi, oxo, amino, mono-alquilamino C1-4, di-alquilamino C1-4, alquilcarbonilamino C1-4, alcoxicarbonilamino C1-4, alquilcarbonilo C1-4 y alcoxicarbonilo C1-4, y los grupos heteroarilo mencionados a su vez pueden estar sustituidos hasta dos veces en una manera idéntica o diferente por un radical elegido de la serie flúor, cloro, ciano, alquilo C1-4, alcoxi C1-4 y trifluorometoxi en los que los sustituyentes alquilo C1-4 mencionados en el presente documento a su vez pueden estar sustituidos con hidroxilo, alcoxi C1-4, trifluorometoxi, alquilcarbonilo C1-4, aminocarbonilo, mono-alquil-aminocarbonilo C1-4 o di-alquilaminocarbonilo C1-4 o hasta tres veces por flúor; y en los que R7 y R8 independientemente uno del otro por cada aparición individual denotan hidrógeno, alquilo C1-6, cicloalquilo C3-6 o heterociclilo de 4- a 6- miembros, en los que alquilo C1-6 puede estar sustituido hasta tres veces por flúor y hasta dos veces en una manera idéntica o diferente mediante un radical elegido de la serie hidroxilo, alcoxi C1-4, trifluorometoxi, amino, mono-alquilamino C1-4, di-alquilamino C1-4, alcoxicarbonilo C1-4, cicloalquilo C3-6 y heterociclilo de 4- a 6- miembros y los grupos cicloalquilo y heterociclilo mencionados pueden estar sustituidos hasta dos veces en una forma idéntica o diferente por un radical elegido de la serie flúor, alquilo C1-4, trifluorometilo, hidroxilo, alcoxi C1-4, trifluorometoxi, oxo, amino, mono-alquilamino C1-4, di-alquilamino C1-4, alquilcarbonilo C1-4 y alcoxicarbonilo C1-4, o R7 y R8 en el caso donde ambos están unidos a un átomo de nitrógeno forman un heterociclo de 4- a 6- miembros conjuntamente con este átomo de nitrógeno, que puede contener un heteroátomo de anillo adicional de la serie N, O, S o S(O)2 y que puede estar sustituido hasta dos veces en una manera idéntica o diferente por un radical elegido de la serie flúor, alquilo C1-4, trifluorometilo, hidroxilo, alcoxi C1-4, oxo, amino, mono-alquilamino C1-4, di-alquilamino C1-4, alquilcarbonilo C1-4 y alcoxicarbonilo C1-4; R5 representa un sustituyente elegido de la serie flúor, cloro, ciano, metilo, trifluorometilo e hidroxilo y p representa el número 0, 1 ó 2; en el que en el caso donde el sustituyente R5 aparezca dos veces, su significado puede ser idéntico o diferente, y sus sales, solvatos y solvatos de las sales.
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