AR068058A1 - Metodo para inhibir la inflamacion y la expresion pre-inflamatoria de citoquina/quimioquina usando un analogo de grelina - Google Patents

Metodo para inhibir la inflamacion y la expresion pre-inflamatoria de citoquina/quimioquina usando un analogo de grelina

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AR068058A1
AR068058A1 ARP080103484A AR068058A1 AR 068058 A1 AR068058 A1 AR 068058A1 AR P080103484 A ARP080103484 A AR P080103484A AR 068058 A1 AR068058 A1 AR 068058A1
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Argentina
Prior art keywords
human ghrelin
aib2
human
dap3
octanosulfonyl
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Michael Dewitt Culler
Zheng Xin Dong
Rakesh Datta
John E Taylor
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Sod Conseils Rech Applic
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Publication of AR068058A1 publication Critical patent/AR068058A1/es

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Abstract

Un método para mejorar la inflamacion, inhibir la expresion de las citoquinas y/o quimioquinas proinflamatorias, y tratar diversas enfermedades y/o condiciones que ocurren simultáneamente con el inicio de la inflamacion, en un sujeto que necesita un tratamiento para dichas condiciones, que comprende administrar análogos de grelina humana nativa seleccionados. Reivindicacion 1: Un método para tratar la inflamacion en un sujeto que lo necesita, caracterizado porque comprende administrarle a dicho sujeto una cantidad eficaz de un análogo de peptidilo de grelina, una prodroga de este o una sal aceptable para el uso farmacéutico de este, donde dicho análogo o dicha prodroga de este se selecciona del grupo que consiste en: (Dap3(octanosulfonil))grelina humana (1-28)-NH2; (Aib2, A6c5)grelina humana (1-28)-NH2; (A6c5)grelina humana (1-28)-NH2; (Aib2,6)grelina humana (1-28)-NH2; (Aib2, A5c12)grelina humana (1-28)-NH2; (Aib2, A5c12, Orn15)grelina humana (1-28)-NH2; (Aib2, A5c12, Apc16)grelina humana (1-28)-NH2; (Aib2, Act6)grelina humana (1-28)-NH2; (Aib2, 3-Pal9)grelina humana (1-28)-NH2; (Aib2, Dmt7)grelina humana (1-28)-NH2; (Aib2, Thz7)grelina humana (1-28)-NH2; (A5c2)grelina humana (1-28)-NH2; (Act2)grelina humana (1-28)-NH2; (Aib2, A5c5)grelina humana (1-28)-NH2, (Aib2, A6c5)grelina humana (1-28)-NH2, (Aib2,5)grelina humana (1-28)-NH2, (Aib2, hLeu5)grelina humana (1-28)-NH2, (Aib2, Cha5)grelina humana (1-28)-NH2; (Aib2,6)grelina humana (1-28)-NH2; (Aib2, Act6)grelina humana (1-28)-NH2; (Aib2, Thr6)grelina humana (1-28)-NH2; (Aib2, Abu6)grelina humana (1-28)-NH2; (Aib2, 4-Hyp7)grelina humana (1-28)-NH2; (Aib2, Thz7)grelina humana (1-28)-NH2; (Aib2, Pip7)grelina humana (1-28)-NH2; (Aib2, Dhp7)grelina humana (1-28)-NH2; (Aib2, Ktp7) grelina humana(1-28)-NH2; (Aib2,8)grelina humana (1-28)-NH2; (Aib2, 2-Pal9)grelina humana (1-28)-NH2; (Aib2, 3-PaI9)greIina humana (1-28)-NH2; (Aib2, 4-Pal9)grelina humana (1-28)-NH2; (Aib2, Taz9)grelina humana (1-28)-NH2; (Aib2, 2-Thi9)grelina humana (1-28)-NH2; Aib2, 2-Fua9)grelina humana (1-28)-NH2; (Aib2, Apc9)grelina humana (1-28)-NH2; (Aib2,9)grelina humana (1-28)-NH2; (Aib2,10)grelina humana (1-28)-NH2; (Aib2, Tic7)grelina humana (1-28)-NH2; (Aib6)grelina humana (1-28)-NH2; (A5c5)grelina humana (1-28)-NH2; (A6c5)grelina humana (1-28)-NH2; (Act6)grelina humana (1-28)-NH2; (3-Pal9)grelina humana (1-28)-NH2; (Dmt7)grelina humana (1-28)-NH2; (Thz7)grelina humana (1-28)-NH2; (Aib5)grelina humana (1-28)-NH2; (hLeu5)grelina humana (1-28)-NH2; (Cha5)grelina humana (1-28)-NH2; (Tbr6)grelina humana (1-28)-NH2; (Abu6)grelina humana (1-28)-NH2; (4-Hyp7)grelina humana (1-28)-NH2; (Pip7)grelina. humana (1-28)-NH2; (Dhp7)grelina humana (1-28)-NH2: (Ktp7)grelina humana (1-28)-NH2; (Aib8)grelina humana (1-28)-NH2; (2-Pal9)grelina humana (1-28)-NH2; (4-Pal9)grelina humana (1-28)-NH2; (Taz9)grelina humana (1-28)-NH2; (2-Thi9)grelina humana (1-28)-NH2; (2-Fua9)grelina humana (1-28)-NH2; (Apc9)grelina humana (1-28)-NH2; (Aib9)grelina humana (1-28)-NH2; (Aib10)grelina humana (1-28)-NH2; (Aib2, Dap3(octanosulfonil), A6c5)grelina humana (1-28)-NH2; (Dap3(octanosuIfoniI), A6c5)grelina humana (1-28)-NH2; (Aib2,6, Dap3(octanosulfonil))grelina. humana (1-28)-NH2; (Aib2, Dap3(octanosuIfoniI), A5c12)greIina humana (1-28)-NH2; (Aib2, Dap3(octanosulfonil), A5c12, Orn15)grelina humana (1-28)-NH2; (Aib2, Dap3(octanosulfonil), A5c12, Apc16)grelina humana (1-28)-NH2; (Aib2, Dap3(octanosulfonil), Act6)grelina humana (1-28)-NH2; (Aib2, Dap3(octanosulfonil), 3-Pal9)grelina humana (1-28)-NH2; (Aib2 Dap3(octanosulfonil), Dmt7)grelina humana (1-28)-NH2; (Aib2, Dap3(octanosulfonil), Thz7)grelina humana (1-28)-NH2; (A5c2, Dap3(octanosulfonil))grelina humana (1-28)-NH2; (Act2, Dap3(octanosulfonil))grelina humana (1-28)-NH2; (Aib2, Dap3(octanosulfonil), A5c5)grelina humana (1-28)-NH2; (Aib2,5, Dap3(octanosulfonil))grelina humana (1-28)-NH2; (Aib2, Dap3(octanosulfonil),hLeu5)grelina humana (1-28)-NH2; (Aib2, Dap3(octanosulfonil), Cha5)grelina humana (1-28)-NH2; (Aib2,6, Dap3(octanosulfonil))grelina humana (1-28)-NH2; (Aib2, Dap3(octanosulfoniI), Thr6)grelina humana (1-28)-NH2; (Aib2, Dap3(octanosulfonil), Abu6)greIina humana (1-28)-NH2; (Aib2, Dap3(octanosulfonil),4-Hyp7)grelina humana (1-28)-NH2; (Aib2, Dap3(octanosulfonil) Pip7)grelina humana (1-28)-NH2; (Aib2, Dap3(octanosulfonil), Dhp7)grelina humana (1-28)-NH2; (Aib2, Dap3(octanosulfonil),Ktp7)grelina humana (1-28)-NH2; (Aib2,8, Dap3(octanosulfonil))grelina humana (1-28)-NH2; (Aib2, .Dap3(octanosulfonil) 2-Pal9)grelina humana (1-28)-NH2; (Aib2, Dap3(octanosulfonil), 3-Pal9)grelina humana (1-28)-NH2; (Aib2, Dap3(octanosulfonil), 4-Pal9)grelina humana (1-28)-NH2; (Aib2, Dap3(octanosulfoniI), Taz9)grelina humana (1-28)-NH2; (Aib2, Dap3(octanosulfonil), 2-Thi9)grelina humana (1-28)-NH2; (Aib2, Dap3(octanosulfonil), 2-Fua9)grelina humana (1-28)-NH2; (Aib2, Dap3(octanosulfonil), Apc9)grelina humana (1-28)-NH2; (Aib29, Dap3(octanosulfonil))grelina humana (1-28)-NH2; (Aib210, Dap3(octanosulfonil))grelina humana (1-28)-NH2; (Dap3(octanosulfonil), A6c5)grelina humana (1-28)-NH2; (Dap3(octanosulfonil), Aib6)grelina humana (1-28)-NH2; (Dap3(octanosulfonil), .A5c12)grelina humana (1-28)-NH2; (Dap3(octanosulfonil), A5c12, Orn15)grelina humana (1-28)-NH2; (Dap3(octanosulfonil), A5c12, Apc16)grelina humana (1-28)-NH2; (Dap3(octanosulfonil), Act6)grelina humana (1-28)-NH2; (Dap3(octanosulfonil), 3-PaI9)greIina humana (1-28)-NH2; (Dap3(octanosulfonil), Dmt7)grelina humana (1-28)-NH2; (Dap3(octanosulfonil), Thz7)grelina humana (1-28)-NH2; (Dap3(octanosulfonil) A5c5)greIina humana (1-28)-NH2; (Dap3(octanosulfonil)Aib5)grelina humana (1-28)-NH2; (Dap3(octanosulfonil), hLeu5)grelina humana (1-28)-NH2; (Dap3(octanosulfonil), Cha5)greIina humana (1-28)-NH2; (Dap3(octanosulfonil), Thr6)grelina humana (1-28)-NH2; (Dap3(octanosulfonil), Abu6)grelina humana (1-28)-NH2; (Dap3(octanosulfonil), 4-Hyp7)grelina humana (1-28)-NH2; (Dap3(octanosulfonil), Pip7)grelina humana (1-28)-NH2; (Dap3(octanosulfonil), Dhp7)grelina humana (1-28)-NH2; (Dap3(octanosulfonil), Ktp7)grelina humana (1-28)-NH2; (Dap3(octanosulfonil), Aib8)grelina humana (1-28)-NH2; (Dap3(octanosulfonil), 2-Pal9)grelina humana (1-28)-NH2; (Dap3(octanosulfonil), 3-Pal9)grelina humana (1-28)-NH2; (Dap3(octanosulfonil), 4-Pal9)grelina humana (1-28)-NH2; (Dap3(octanosulfonil), Taz9)grelina humana (1-28)-NH2; (Dap3(octanosulfonil), 2-Thi9)grelina humana (1-28)-NH2; (Dap3(octanosulfonil), 2-Fua9)grelina humana (1-28)-NH2; (Dap3(octanosulfonil), Apc9)grelina humana (1-28)-NH2; (Dap3(octanosulfonil), Aib9)grelina humana (1-28)-NH2; (Dap3(octanosulfonil), Aib10)grelina humana (1-28)-NH2; (Dap3(octanosulfonil), A5c12, .Orn15)grelina humana (1-28)-NH2; (Dab3(octanosulfonil), A5c12, Orn15)grelina humana (1-28)-NH2; (Aib2, A6c5, A5c12, Orn15)grelina humana (1-28)-NH2; (A6c5, A5c12, Orn15)grelina humana (1-28)-NH2; (Aib2,6, A5c12, Orn15)grelina humana (1-28)-NH2; (Aib2, Act6, A5c12, Orn15)grelina humaba (1-28)-NH2; (Aib2, 3-Pal9, A5c12, Orn15)greIina humana (1-28)-NH2; (Aib2, Dmt7, A5c12, Orn15)grelina humana (1-28)-NH2; (Aib2, Thz7, A5c12, Orn15)grelina humana (1-28)-NH2; (Aib2, A5c5, A5c12, Orn15)grelina humana (1-28)-NH2; (Aib2,5, A5c12, Orn15)grelina humana (1-28)-NH2; (Aib2, hLeu5, A5c12, Orn15)grelina. humana (1-28)-NH2; (Aib2, Cha5, A5c12, Orn15)grelina humana (1-28)-NH2; (Aib2,5, A5c12, Orn15)grelina humana (1-28)-NH2; (Aib2, Thr6, A5c12, Orn15)grelina humana (1-28)-NH2; (Aib2, Abu6, A5c12, Orn15)grelina humana (1-28)-NH2; (Aib2, 4-Hyp7, A5c12, Orn15)grelina humana (1-28)-NH2; (Aib2, Pip7, A5c12, Orn15)grelina humana (1-28)-NH2; (Aib2, Dhp7, A5c12, Orn15)grelina humana (1-28)-NH2; (Aib2, Ktp7, A5c12, Orn15)grelina humana (1-28)-NH2; Aib2,8, A5c12, Orn15)grelina humana (1-28)-NH2; (Aib2, 2-Pal9, A5c12, Orn15)grelina humana (1-28)-NH2; (Aib2, 3-Pal9, A5c12, Orn15)grelina humana (1-28)-NH2; (Aib2, 4,Pal9, A5c12, Orn15)greIina humana (1-28)-NH2; (Aib2, Taz9, A5c12, Orn15)grelina humana (1-28)-NH2; (Aib2, 2-Thi9, A5c12, Orn15)grelina humana (1-28)-NH2; (Aib2, 2-Fua9, A5c12, Orn15)grelina humana (1-28)-NH2; (Aib2, Apc9, A5c12, Orn15)grelina humana (1-28)-NH2; (Aib2,9, A5c12, Orn15)grelina humana (1-28)-NH2; (Aib2,10, A5c12, Orn15)greIina humana (1-28)-NH2; (Dap3(octanosulfonil), A5c12, Apc16)grelina humana (1-28)-NH2; (Dab3(octanosulfonil), A5c12, Apc16)grelina humana (1-28)-NH2; (Aib2, A6c5, A5c12, Apc16)grelina humana (1-28)-NH2; (A6c5, A5c12, Apc16)grelina humana (1-28)-NH2; (Aib2,6 A5c12 Apc16)grelina humana (1-28)-NH2; (Aib2, Act6, A5c12, Apc16)grelina humana (1-28)-NH2; (Aib2, 3-Pal9, A5c12, Apc16)grelina humana (1-28)-NH2; (Aib2, Dmt7, A5c12, Apc16)grelina humana (1-28)-NH2; (Aib2, Thz7, A5c12, Apc16)grelina humana (1-28)-NH2; (Aib2, A5c5,12, Apc16)grelina humana (1-28)-NH2; (Aib2,5, A5c12, Apc16)grelina humana (1-28)-NH2; (Aib2, hLeu5, A5c12, Apc16)grelina humana (1-28)-NH2; (Aib2, Cha5, A5c12, Apc16)grelina humana (1-28)-NH2; Aib2,6, A5c12, Apc16)grelina humana (1-28)-NH2; (Aib2, Thr6, A5c12, Apc16)grelina humana (1-28)-NH2; (Aib2, Abu6, A5&2, Apc16)grelina humana (1-28)-NH2; (Aib2, 4Hyp7, A5c12, Apc16)grelina humana (1-28)-NH2; (Aib2, Pip7, A5c12, Apc16)grelina humana .(1-28)-NH2; (Aib2, Dhp7, A5c12, Apc16)grelina humana (1-28)-NH2; (Aib2, Ktp7, A5c12, Apc16)grelina humana (1-28)-NH2; (Aib2,8, A5c12, Apc16)grelina humana (1-28)-NH2; (Aib2, 2-Pal9, A5c12, Apc16)grelina humana (1-28)-NH2; (Aib2, 3-Pal9, A5c12, Apc16)greIina humana (1-28)-NH2; (Aib2, 4-Pal9, A5c12, Apc16)grelina humana (1-28)-NH2; (Aib2, Taz9, A5c12, Apc16)grelina humana (1-28)-NH2; (Aib2, 2-Thi9, A5c12, Apc16)grelina humana (1-28)-NH2; (Aib2, 2-Fua9, A5c12, Apc16)grelina humana (1-28)-NH2; (Aib2, Apc9,16, A5c12)grelina humana (1-28)-NH2; (Aib2-9, A5c12, Apc16)grelina humana (1-28)-NH2; (Aib2,10, A5c12, Apc16)grelina humana (1-28)-NH2; (A6c5, A5c12, Orn15)grelina humana (1-28)-NH2; (Aib6, A5c12, Orn15)grelina humana (1-28)-NH2; (Act6, A5c12, Orn15)grelina humana (1-28)-NH2; (3-Pa
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