AR064489A1 - Derivados de ciclohexil-metilamina, composiciones farmaceuticas y productos que los comprenden y su uso en la preparacion de medicamentos para el tratamiento de enfermedades mediadas por la dipeptidil-peptidasa (dpp-iv) - Google Patents

Derivados de ciclohexil-metilamina, composiciones farmaceuticas y productos que los comprenden y su uso en la preparacion de medicamentos para el tratamiento de enfermedades mediadas por la dipeptidil-peptidasa (dpp-iv)

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Publication number
AR064489A1
AR064489A1 ARP070105854A ARP070105854A AR064489A1 AR 064489 A1 AR064489 A1 AR 064489A1 AR P070105854 A ARP070105854 A AR P070105854A AR P070105854 A ARP070105854 A AR P070105854A AR 064489 A1 AR064489 A1 AR 064489A1
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AR
Argentina
Prior art keywords
optionally substituted
bond
heterocyclyl
hydrogen
atoms
Prior art date
Application number
ARP070105854A
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English (en)
Original Assignee
Mazzucco Gavieiro Maria Belen
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Application filed by Mazzucco Gavieiro Maria Belen filed Critical Mazzucco Gavieiro Maria Belen
Publication of AR064489A1 publication Critical patent/AR064489A1/es

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    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
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    • 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
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Abstract

Los compuestos pueden ser utiles en el tratamiento o en la prevencion de diversas enfermedades y condiciones en donde esté implicada la dipeptidil-peptidasa-IV (DPP-IV), tales como hiperlipidemia, diabetes mellitas y osteoporosis por calcitonina. Reivindicacion 1: Un compuesto de la formula (1): en donde: uno de V y W se selecciona a partir de un enlace, -(CH2)n-, -O-, -NH- y -N(R8)-; y el otro se selecciona a partir de un enlace, -(CH2)n- y -O-; X es un enlace o un enlazador que tiene de 1 a 5 átomos en cadena, y que comprende uno o más enlaces seleccionados a partir de -O-, -C(O)-, -S(O)l-, -N(R8)- e hidrocarbileno opcionalmente sustituido con 1, 2, 3, 4 o 5 R10; con la condicion de que, cuando al menos uno de V y W es -O-, -NH- o -N(R8)-, X es un enlace; Y es un enlace; o Y y una fraccion R7 tomados junto con los átomos con los que están unidos, forman un carbociclo o un hetero-ciclo, cualquiera de los cuales está opcionalmente sustituido con 1, 2, 3, 4 o 5 R10; Z es un enlace o un enlazador que tiene de 1 a 12 átomos en cadena, y que comprende uno o más enlaces seleccionados a partir de -O-, -C(O)-, -S(O)l-, -N(R8)-, hidrocarbileno opcionalmente sustituido con 1, 2, 3, 4 o 5 R10, y heterociclileno opcionalmente sustituido con 1, 2, 3, 4 o 5 R10; R3 y R4 son cada uno independientemente hidrogeno o R10; o R3 y R4 tomados junto con el átomo de carbono con el que están unidos, forman carbociclilo o heterociclilo, cualquiera de los cuales está opcionalmente sustituido con 1, 2, 3, 4 o 5 R10; R5 se selecciona a partir de hidrogeno, excepto cuando X es un enlace; hidrocarbilo opcionalmente sustituido con 1, 2, 3, 4 o 5 R10; y -(CH2)k-heterociclilo opcionalmente sustituido con 1, 2, 3, 4 o 5 R10; R6 se selecciona a partir de hidrogeno, excepto cuando Y y Z son cada uno un enlace; hidrocarbilo opcionalmente sustituido con 1, 2, 3, 4 o 5 R10; y -(CH2)k-heterociclilo opcionalmente sustituido con 1, 2, 3, 4 o 5 R10; R7 se selecciona independientemente a partir de R10; o dos R7, tomados juntos, pueden formar un puente entre los átomos con los que están unidos, en donde el puente es un puente de hidrocarbileno o de -(CH2)i-O-(CH2)j-, en donde ? y j son cada uno independientemente 0, 1 o 2; R8 se selecciona a partir de R9, -OR9, -C(O)R9, -C(O)OR9 y -S(O)lR9; R9 se selecciona a partir de hidrogeno; hidrocarbilo opcionalmente sustituido con 1, 2, 3, 4 o 5 R10; y -(CH2)k-heterociclilo opcionalmente sustituido con 1, 2. 3, 4 o 5 R10; cada R10 se selecciona independientemente a partir de halogeno, trifluoro-metilo, ciano, nitro, oxo, =NR11, -OR11, -C(O)R11, -C(O)OR11, -OC(O)R11 , -S(O)lR11, -N(R11)R12, -C(O)N(R11)R12, -S(O)lN(R11)R12 y R13; R11 y R12 son cada uno independientemente hidrogeno o R13; R13 se selecciona a partir de hidrocarbilo y -(CH2)k- heterociclilo, cualquiera de los cuales está opcionalmente sustituido con 1, 2, 3, 4 o 5 sustituyentes seleccionados independientemente a partir de halogeno, ciano, amino, hidroxilo, alquilo de 1 a 6 átomos de carbono y alcoxilo de 1 a 6 átomos de carbono; k es 0, 1, 2, 3, 4, 5 o 6; l es 0, 1 o 2; m es 0, 1, 2, 3, 4, 5 o 6; y n es 1 o 2; o una sal farmacéuticamente aceptable o pro-fármaco del mismo; para utilizarse en el tratamiento o prevencion de una enfermedad o condicion seleccionada a partir de diabetes mellitus no dependiente de insulina, artritis, obesidad, trasplante de alo-injerto, osteoporosis por calcitonina, insuficiencia cardíaca, metabolismo deteriorado de la glucosa o tolerancia deteriorada a la glucosa, enfermedades neurodegenerativas, enfermedades renales, trastornos neurodegenerativos o cognoscitivos, hiperglicemia, resistencia a la insulina, trastornos de lípidos, dislipidemia, hipertrigliceridemia, hipercolesterolemia, restenosis vascular, síndrome de intestino irritable, enfermedad inflamatoria del intestino, pancreatitis, retinopatía, nefropatía, neuropatía, síndrome X, hiperandrogenismo de ovarios (síndrome de ovario poliquístico), diabetes tipo 2, deficiencia de hormona de crecimiento, neutropenia, trastornos neuronales, metástasis tumoral, hipertrofia prostática benigna, gingivitis, hipertension, y osteoporosis; o para producir un efecto sedante o ansiolítico, atenuar los cambios catabolicos post-quirurgicos o las respuestas hormonales a la tension, reducir la mortalidad y la patología después de infarto de miocardio. Reivindicacion 48: Un compuesto de la formula (2) o una sal farmacéuticamente aceptable o pro-fármaco del mismo: en donde: V, W, Y, R3, R4, R5, R6, R7, R10 y m son como se definen en la reivindicacion 1; p es 0, 1, 2, 3, 4 o 5; y cuando p es 1, 2, 3, 4 o 5, cuando menos un R10 es halogeno o alquilo de 1 a 6 átomos de carbono; y en donde el compuesto no es uno de los siguientes compuestos (3): o una sal farmacéuticamente aceptable o pro-fármaco de los mismos.
ARP070105854A 2006-12-22 2007-12-21 Derivados de ciclohexil-metilamina, composiciones farmaceuticas y productos que los comprenden y su uso en la preparacion de medicamentos para el tratamiento de enfermedades mediadas por la dipeptidil-peptidasa (dpp-iv) AR064489A1 (es)

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