AR035883A1 - Derivados de ciclohexano-1,4-diamina sustituidos, procedimientos para su preparacion, medicamentos que contienen estos compuestos y su uso para la preparacion de medicamentos - Google Patents

Derivados de ciclohexano-1,4-diamina sustituidos, procedimientos para su preparacion, medicamentos que contienen estos compuestos y su uso para la preparacion de medicamentos

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Publication number
AR035883A1
AR035883A1 ARP020101704A ARP020101704A AR035883A1 AR 035883 A1 AR035883 A1 AR 035883A1 AR P020101704 A ARP020101704 A AR P020101704A AR P020101704 A ARP020101704 A AR P020101704A AR 035883 A1 AR035883 A1 AR 035883A1
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Argentina
Prior art keywords
unsubstituted
polysubstituted
mono
alkyl
unsaturated
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ARP020101704A
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English (en)
Inventor
Sundermann Bernd Dr
Hennies Hagen-Heinrich Dr
Englberger Werner Guenter Dr
Koegel Babette-Yvonne Dr
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Gruenenthal Gmbh
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Publication of AR035883A1 publication Critical patent/AR035883A1/es

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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
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    • C07C211/33—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C211/34—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of a saturated carbon skeleton
    • C07C211/36—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of a saturated carbon skeleton containing at least two amino groups bound to the carbon skeleton
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    • A61K31/16—Amides, e.g. hydroxamic acids
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    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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Abstract

Derivados de ciclohexano-1,4-diamina sustituido, de la fórmula general (1), en la cual R1 y R2 representan independientemente entre sí, H, alquilo C1-8 o cicloalquilo C3-8 saturados o insaturados, ramificados o no ramificados, y no sustituidos o mono- o polisustituidos, arilo o heteroarilo, no sustituidos o mono- o polisustituidos, o los radicales arilo, cicloalquilo C3-8 o heteroarilo no sustituidos o mono- o polisustituidos ligados a través de alquileno C1-3, con la condición que R1 y R2 no puedan representar simultáneamente hidrógeno, o R1 y R2 en conjunto forman un ciclo y significan CH2CH2OCH2CH2, CH2CH2NR6CH2CH2 ó (CH2)3-6, estando elegido R6 entre H, alquilo C1-8 o cicloalquilo C3-8, saturados o insaturados, ramificados o no ramificados, no sustituidos o mono- o polisustituidos, arilo o heteroarilo, no sustituidos o mono- o polisustituidos, o los radicales arilo, cicloalquilo C3-8 o heteroarilo no sustituidos o mono- o polisustituidos, ligados a través de alquileno C1-3; R3 representa alquilo C1-8 o cicloalquilo C3-8, saturados o insaturados, ramificados o no ramificados, no sustituidos o mono- o polisustituidos, arilo, heteroarilo, no sustituidos o mono- o polisustituidos, o los radicales arilo, cicloalquilo C3-8 o heteroarilo no sustituidos o mono- o polisustituidos, ligados a través de un grupo alquilo C1-4, saturado o insaturado, ramificado o no ramificado, no sustituido o sustituido; R4 representa H, alquilo C1-8, saturado o insaturado, ramificado o no ramificado, no sustituido o mono- o polisustituido; o C(X)R7, C(X)NR7R8, C(X)OR9, C(X)SR9, S(O)2R9, siendo X = O ó S, y en donde R7 representa H, alquilo C1-8 o cicloalquilo C3-8, saturados o insaturados, ramificados o no ramificados, no sustituidos o mono- o polisustituidos, arilo o heteroarilo no sustituidos o mono- o polisustituidos, o los radicales arilo, cicloalquilo C3-8 o heteroarilo, no sustituidos o mono- o polisustituidos ligados a través de un grupo alquilo C1-4 saturado o insaturado, ramificado o no ramificado, sustituido o no sustituido; R8 representa H, alquilo C1-4, saturado o insaturado, ramificado o no ramificado, no sustituido o mono- o polisustituido, o R7 y R8 en conjunto forman un ciclo y representan CH2CH2OCH2CH2, CH2CH2NR10CH2CH2 ó (CH2)3-6; R10 representa H, alquilo C1-8 o cicloalquilo C3-8, saturados o insaturados, ramificados o no ramificados, no sustituidos o mono- o polisustituidos, arilo o heteroarilo, no sustituidos o mono- o polisustituidos, o los radicales arilo, cicloalquilo C3-8 o heteroarilo no sustituidos o mono- o polisustituidos y ligados a través de alquileno C1-3; R9 representa alquilo C1-8 o cicloalquilo C3-8, saturados o insaturados, ramificados o no ramificados, no sustituidos o mono- o polisustituidos, arilo, heteroarilo, no sustituidos o mono- o polisustituidos, o los radicales arilo, cicloalquilo C3-8 o heteroarilo no sustituidos o mono o polisustituidos ligados a través de un grupo alquilo C1-4, saturado o insaturado, ramificado o no ramificado, sustituido o no sustituido; R5 representa cicloalquilo C3-8, arilo o heteroarilo, no sustituidos o mono- o polisustituidos, -CHR11R12, -CHR11-CH2R12, -CHR11-CH2-CH2R12, -CHR11-CH2-CH2-CH2R12, -C(Y)R12, -C(Y)-CH2R12, C(Y)-CH2-CH2R12 ó -C(Y)-CH2-CH2-CHR12, siendo Y = O, S ó H2, y en donde R11 representa H, alquilo C1-7, saturado o insaturado, ramificado o no ramificado, no sustituido o mono- o polisustituido, o C(O)O-alquilo C1-6, saturado o insaturado, ramificado o no ramificado, no sustituido o mono- o polisustituido; y R12 representa H, cicloalquilo C3-8, arilo o heteroarilo, no sustituidos o mono- o polisustituidos; o R4 y R5 en conjunto forman un heterociclo de 3 a 8 átomos en el ciclo, saturado o insaturado, no sustituido o mono- o polisustituido, eventualmente condensado con otros ciclos, con la condición que cuando R3 representa fenilo sustituido o no sustituido y al menos uno de R1 o R2 representa H o alquilo C1-8, R4 es distinto de alquilo y R4 y R5 en conjunto no pueden formar un heterociclo, ó cuando R3 representa fenilo no sustituido y R1 y R2 en conjunto forman (CH2)5, R4 representa H o alquilo C1-8, Y es distinto de O ó S y R5 es distinto de alquilo C1-6, eventualmente en forma de sus racematos, sus estereoisómeros puros, particularmente enantiómeros o diastereómeros, o en forma de mezcla de estereoisómeros, particularmente de los enantiómeros o diastereómeros, en cualquier proporción de mezcla, en la forma representada o en forma de sus ácidos o bases o en forma de sus sales, particularmente sales fisiológicamente tolerables, o sales con ácidos o cationes fisiológicamente tolerables o en forma de sus solvatos, particularmente los hidratos, procedimientos para su preparación, medicamentos que contienen estos compuestos y el uso de dichos derivados de ciclohexano-1,4-diamina sustituidos para la preparación de medicamentos. Los medicamentos preparados en base a estos compuestos actúan sobre el sistema nociceptina/receptor ORL1 y, en consecuencia, son empleados en el tratamiento de diversas enfermedades involucradas en este sistema. La nociceptina inhibe la actividad de las neuronas de los ganglios raquídeos posteriores estimulada por cainato o glutamato, siendo eficaz en el tratamiento de los dolores neuropáticos. El receptor de ORL1 también participa en la regulación de otros procesos fisiológicos y patofisiológicos, entre ellos el aprendizaje y formación de la memoria. También interviene o desempena un papel en la analgesia, la absorción de alimentos, tratamiento de fenómenos de privación de drogas, modulación de la actividad motriz, ansiolisis, epilepsia así como cierta acción sobre el sistema cardiovascular, diuresis, antinatriuresis y otros.
ARP020101704A 2001-05-09 2002-05-10 Derivados de ciclohexano-1,4-diamina sustituidos, procedimientos para su preparacion, medicamentos que contienen estos compuestos y su uso para la preparacion de medicamentos AR035883A1 (es)

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DE10123163A DE10123163A1 (de) 2001-05-09 2001-05-09 Substituierte Cyclohexan-1,4-diaminderivate

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AR035883A1 true AR035883A1 (es) 2004-07-21

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DE10252650A1 (de) * 2002-11-11 2004-05-27 Grünenthal GmbH Cyclohexyl-Harnstoff-Derivate
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