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AR070569A2 - Compuestos de arilvinilazacicloalcano, composiciones farmaceuticas que los comprenden, un proceso para prepararlos y su uso en la fabricacion de medicamentos para el tratamiento de trastornos neurodegenerativos. - Google Patents

Compuestos de arilvinilazacicloalcano, composiciones farmaceuticas que los comprenden, un proceso para prepararlos y su uso en la fabricacion de medicamentos para el tratamiento de trastornos neurodegenerativos.

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Publication number
AR070569A2
AR070569A2 ARP090100388A ARP090100388A AR070569A2 AR 070569 A2 AR070569 A2 AR 070569A2 AR P090100388 A ARP090100388 A AR P090100388A AR P090100388 A ARP090100388 A AR P090100388A AR 070569 A2 AR070569 A2 AR 070569A2
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AR
Argentina
Prior art keywords
alkyl
heteroaryl
aryl
nr8r9
heterocyclyl
Prior art date
Application number
ARP090100388A
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English (en)
Inventor
Arielle Genevois-Barella
Craig Miller
Gary Maurice Dull
Marc Capet
Michel Cheve
Jeffrey Daniel Schmitt
Original Assignee
Targacept Inc
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Filing date
Publication date
Application filed by Targacept Inc filed Critical Targacept Inc
Publication of AR070569A2 publication Critical patent/AR070569A2/es

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    • A61K31/00—Medicinal preparations containing organic active ingredients
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • C07D401/06—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 linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

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Abstract

Se revelan compuestos vinilazacicloalcano los cuales son ligandos de diversos nAChRs. Los compuestos y sus sales farmacéuticamente aceptables pueden utilizarse para preparar composiciones farmacéuticas y/o medicamentos para prevenir o tratar trastornos asociados con la disfuncion de nAChRs, especialmente dentro del sistema nervioso central o el sistema gastrointestinal. Ejemplos de tipos de trastornos que pueden tratarse incluyen trastornos neurodegenerativos, que incluyen trastornos del sistema nervioso central tales como enfermedad de Alzheimer, trastornos cognitivos, trastornos motores tales como enfermedad de Parkinson, adiccion las drogas, trastornos de conducta y trastornos inflamatorios dentro del sistema gastrointestinal. Los compuestos también pueden servir como analgésicos en el tratamiento del dolor agudo, cronico o recurrente. Reivindicacion 1: Un compuesto vinilazacicloalcano caracterizado por la formula (1) en donde la línea ondulante representa la geometría variable (E o Z) alrededor del enlace doble; X es CR2; R1 es hidrogeno, alquilo C1-6, halogeno, -OR4, -OR4R5, o -SR4; R2 es hidrogeno, alquilo C1-6, arilo, aril-alquilo C1-6, heteroarilo, heteroaril-alquilo C1-6, heterociclilo, heterociclil-alquilo C1-6, cicloalquilo, policicloalquilo, -OR6, -NR6R7, -SR6, -SOR6 o -SO2R6; en donde los grupos alquilo C1-6, cicloalquilo, heterociclilo, heteroarilo o arilo se pueden sustituir con uno o más sustituyentes seleccionados del grupo formado por F, Cl, Br, I, -R8, -OR8, -NR8R9, -CF3, -OCF3, -CN, -NO2, -SR8, -S(O)R8, -SO2R8, -O-SO2R8, -C(=O)NR6R9, -NR8C(=O)R9, -C(=O)OR8, -OC(=O) R8, -NHSO2R8, -SO2NR8R9, -C(S)NR8R9, y -NHC(S)R8; R3 es hidrogeno o metilo; R4 y R5 son, independientemente, hidrogeno o alquilo C1-6; R6 y R7 son, independientemente, hidrogeno, alquilo C1-6, arilo, aril-alquilo C1-6, heteroarilo, heteroaril-alquilo C1-6, heterociclilo, heterociclilalquilo, cicloalquilo o policicloalquilo, en donde los grupos alquilo C1-6, cicloalquilo, heterociclilo, heteroarilo y arilo se pueden sustituir con uno o más sustituyentes seleccionados del grupo formado por F, Cl, Br, I, -R8, -NR8R9, -CF3, -CN, -NO2, -C2R8, -N3, -SO2CH3, -OR8, -SR8, -C(=O)NR8R9, -NR8C(=O)R8, -C(=O)R8, -C(=O)OR8, -(CH2)qOR8, -OC(=O) R8, -OC(=O)NR8R9, y -NR8C(=O)OR8; R8 y R9 son, independientemente, hidrogeno, alquilo C1-6, o una especie que contiene un grupo aromático; en donde la especie que contiene un grupo aromático se puede sustituir con uno o más de alquilo C1-6, halogeno o amino; o R6 y R7 juntos o R8 y R9 juntos con los átomos a los cuales están unidos forman un anillo de 3 a 10 miembros; m es 1, 2, 3 o 4; y n es 1, 2 o 3; o un isomero, mezcla, enantiomero, diastereomero, tautomero o una sal farmacéuticamente aceptable de ellos; siempre que, sin embargo, el compuesto no sea: 3-(2-(1-metilpirrolidin-3-il)vinil)piridina; 3-isopropoxi-5-(2-(1-metilpirrolidin-3-il)vinil)piridina; 3-isopropoxi-5-(2-(pirrolidin-3-il)vinil)piridina; 5-(2-(1-metilpirrolidin-3-il)vinil)-3-fenoxipiridina; o 3-etoxi-5-(2-(1-metilpirrolidin-3-il)vinil)piridina. Reivindicacion 30: Un proceso para preparar compuestos arilvinilazacicloalcano de acuerdo con las reivindicaciones 1 a 12, de la formula (1) en donde: la línea ondulante representa la geometría variable (E o Z) alrededor del enlace doble; X es CR2; R1 es hidrogeno, alquilo C1-6, halogeno, -OR4, -OR4R5, o -SR4; R2 es hidrogeno, alquilo C1-6, arilo, aril-alquilo C1-6, heteroarilo, heteroaril-alquilo C1-6, heterociclilo, heterociclil-alquilo C1-6, cicloalquilo, policicloalquilo, -OR6, -NR6R7, -SR6, -SOR6 o -SO2R6; en donde los grupos alquilo C1-6, cicloalquilo, heterociclilo, heteroarilo o arilo se pueden sustituir con uno o más sustituyentes seleccionados del grupo formado por F, Cl, Br, I, -R8, -OR8, -NR8R9, -CF3, -OCF3, -CN, -NO2, -SR8, -S(O)R8, -SO2R8, -O-SO2R8, -C(=O)NR6R9, -NR8C(=O)R9, -C(=O)OR8, -OC(=O) R8, -NHSO2R8, -SO2NR8R9, -C(S)NR8R9, y -NHC(S)R8; R3 es hidrogeno o metilo; R4 y R5 son, independientemente, hidrogeno o alquilo C1-6; R6 y R7 son, independientemente, hidrogeno, alquilo C1-6, arilo, aril-alquilo C1-6, heteroarilo, heteroaril-alquilo C1-6, heterociclilo, heterociclilalquilo, cicloalquilo o policicloalquilo, en donde los grupos alquilo C1-6, cicloalquilo, heterociclilo, heteroarilo y arilo se pueden sustituir con uno o más sustituyentes seleccionados del grupo formado por F, Cl, Br, I, -R8, -NR8R9, -CF3, -CN, -NO2, -C2R8, -N3, -SO2CH3, -OR8, -SR8, -C(=O)NR8R9, -NR8C(=O)R8, -C(=O)R8, -C(=O)OR8, -(CH2)qOR8, -OC(=O) R8, -OC(=O)NR8R9, y -NR8C(=O)OR8; R8 y R9 son, independientemente, hidrogeno, alquilo C1-6, o una especie que contiene un grupo aromático; en donde la especie que contiene un grupo aromático se puede sustituir con uno o más de alquilo C1-6, halogeno o amino; o R6 y R7 juntos o R8 y R9 juntos con los átomos a los cuales están unidos forman un anillo de 3 a 10 miembros; m es 1, 2, 3 o 4; y n es 1, 2 o 3; o un isomero, mezcla, enantiomero, diastereomero, tautomero o una sal farmacéuticamente aceptable de ellos, caracterizado porque comprende: a) hacer reaccionar un aldehído de la formula (2) en donde m es 1, 2, o 3 y n es 1, 2 o 3, con una fosforano ilida de la formula PPh3=CH2 para dar un vinilazacicloalcano de la formula (3); b) hacer reaccionar el vinilazacicloalcano con un haluro de heteroarilo de la formula (4) en donde X y R1 son lo definido anteriormente e Y es halogeno; y c) remover todos los grupos protectores remanentes.
ARP090100388A 2003-03-05 2009-02-05 Compuestos de arilvinilazacicloalcano, composiciones farmaceuticas que los comprenden, un proceso para prepararlos y su uso en la fabricacion de medicamentos para el tratamiento de trastornos neurodegenerativos. AR070569A2 (es)

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US10/379,868 US7098331B2 (en) 2003-03-05 2003-03-05 Arylvinylazacycloalkane compounds and methods of preparation and use thereof

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ARP040100690A AR043469A1 (es) 2003-03-05 2004-03-04 Compuestos arilvinilazacicloalcano y composiciones farmaceuticas que los contienen
ARP090100388A AR070569A2 (es) 2003-03-05 2009-02-05 Compuestos de arilvinilazacicloalcano, composiciones farmaceuticas que los comprenden, un proceso para prepararlos y su uso en la fabricacion de medicamentos para el tratamiento de trastornos neurodegenerativos.
ARP090100389A AR070570A2 (es) 2003-03-05 2009-02-05 Compuesto de arilvinilazacicloalcano, una composicion farmaceutica que lo comprende y su uso en el tratamiento de enfermedades mediadas por alfa4beta2 nachr.

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US7098331B2 (en) * 2003-03-05 2006-08-29 Targacept, Inc. Arylvinylazacycloalkane compounds and methods of preparation and use thereof
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