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    ADAMANTYL-ACETAMIDE DERIVATIVES AS INHIBITORS OF THE 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 ENZYME
    23.
    发明专利
    ADAMANTYL-ACETAMIDE DERIVATIVES AS INHIBITORS OF THE 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 ENZYME 未知

    公开(公告)号：NZ587997A

    公开(公告)日：2012-04-27

    申请号：NZ58799705

    申请日：2005-04-29

    Applicant: ABBOTT LAB

    Inventor： LINK JAMES T ,  PLIUSHCHEV MARINA A ,  ROHDE JEFFREY J ,  WODKA DARIUSZ ,  PATEL JYOTI R ,  SHUAI QI

    IPC: C07D213/24 ,  C07C237/04 ,  C07C237/24 ,  C07D207/02 ,  C07D209/08 ,  C07D213/06 ,  C07D213/72 ,  C07D213/74 ,  C07D213/85 ,  C07D223/16 ,  C07D253/06 ,  C07D257/04 ,  C07D277/64 ,  C07D295/15 ,  C07D295/185 ,  C07D471/08 ,  C07D491/04

    Abstract: Disclosed is a substituted adamantine compound selected from the group consisting of: N2- [2-(4-chlorophenyl)ethyl] -N1-[(E)-5-hydroxy-2-adamantyl]alaninamide; N2-[2-(3,4-dichlorophenyl)ethyl] -N1-[(E)-5-hydroxy-2-adamantyl] -N2-methylalaninamide; N2-[2-(4-chlorophenyl)-1-methylethyl] -N1-[(E)-5-hydroxy-2-adamantyl]-N2-methylalaninamide; N-[(E)-5-hydroxy-2-adamantyl]-1-{ [4-(trifluoromethyl)benzyl]amino} cyclopropanecarboxamide; 2-[(cis)-2,6-dimethylmorpholin-4-yl] -N-[(E)-5-hydroxy-2-adamantyl]propanamide; 2-azepan-1-yl-N-[(E)-5-hydroxy-2-adamantyl]propanamide; N-[(E)-5-hydroxy-2-adamantyl]-2-(6,7,9,10-tetrahydro-8H-[1,3]dioxolo[4,5-g] [3]benzazepin-8-yl)propanamide; 2-(1,3-dihydro-2H-isoindol-2-yl)-N- [(E)-5-hydroxy-2-adamantyl]propanamide; 2- [3-(4-chlorophenoxy)azetidin- 1-yl]-N-[(E)-5-hydroxy-2-adamantyl]propanamide; 2-(5-chloro-2,3-dihydro-1H-indol- 1-yl)-N-[(E)-5 -hydroxy-2-adamantyl]propanamide; N-[(E)-5-hydroxy-2-adamantyl] -2-(3-phenylazetidin-1-yl)propanamide; 2-[3-(3-fluorophenoxy)pyrrolidin-1-yl]-N-[(E)-5-hydroxy-2-adamantyl]propanamide; N-[(E)-5-hydroxy-2-adamantyl]-2-methyl-2- [2-(trifluoromethyl)pyrrolidin-1-yl]propanamide; N-[(Z)-5-hydroxy-2-adamantyl]-2-{ 4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl} acetamide; N-[(E)-5-hydroxy-2-adamantyl] -2-{ 4-[5 -(trifluoromethyl)pyridin-2-yl]piperazin-1-yl} acetamide; (2S)-N-[(E)-5-hydroxy-2-adamantyl] -2-{ 4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl} propanamide; (2R)-N- [(E)-5 -hydroxy-2-adamantyl] -2- { 4- [5 -(trifluoromethyl)pyridin-2-yl]piperazin-1-yl} propanamide; N-[(E)-5-fluoro-2-adamantyl] -2-{ 4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl} acetamide; N-[(Z)-5-fluoro-2-adamantyl] -2-{ 4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl} acetamide; N-[(E)-5-hydroxy-2-adamantyl] -2-[4-(5-methylpyridin-2-yl)piperazin-1-yl]propanamide; N-[(E)-5-hydroxy-2-adamantyl] -2-methyl-2-{ 4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl} propanamide; N-[(E)-5-hydroxy-2-adamantyl]-2-(4-pyridin-2-ylpiperazin-1-yl)propanamide; 2- [4-(4-fluorophenyl)piperazin-1-yl]-N-[(E)-5-hydroxy-2-adamantyl]propanamide; N-[(E)-5-hydroxy-2-adamantyl]-2-[4-(4-methoxyphenyl)piperazin-1-yl]propanamide; 2-[4-(5-cyanopyridin-2-yl)piperazin-1-yl]-N-[(E)-5-hydroxy-2-adamantyl]propanamide; 2-[4-(2-furoyl)piperazin-1-yl]-N-[(1R,3S)-5-hydroxy-2-adamantyl]propanamide; N-[(E)-5-hydroxy-2-adamantyl] -2-{ 4-[4-(trifluoromethyl)phenyl]piperazin-1-yl} propanamide; (2S)-N-[(E)-5-hydroxy-2-adamantyl] -2-{ 4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl} propanamide; (2R)-N-[(E)-5-hydroxy-2-adamantyl] -2-{ 4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl} propanamide; 2-[4-(6-chloropyridin-3 yl)piperazin-1-yl]-N-[(E)-5-hydroxy-2-adamantyl]propanamide; 2-(4-benzylpiperidin-1-yl)-N-[(E)-5-hydroxy-2-adamantyl]propanamide; 2-[4-(2-fluorophenoxy)piperidin-1-yl] -N-[(E)-5-hydroxy-2-adamantyl]propanamide; 2-[3-(2-fluorophenoxy)piperidin-1-yl] -N-[(E)-5-hydroxy-2- adamantyl]propanamide; N- [(E)-5 -cyano-2-adamantyl] -2-methyl-2-{ 4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl} propanamide; and N-[(E)-5-(cyanomethyl)-2-adamantyl]-2-methyl-2-{ 4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl} propanamide. Also disclosed is a pharmaceutical composistin comprisining a compound and the use of the compound for the manufacture ofa medicament for treating Cushing's syndrome, non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, hypertension, atherosclerosis, glaucoma, and osteoporosis. The compounds are useful as 11-beta-HSD inhibitors.

    INHIBIDORES DE LA ENZIMA 11-BETA-HIDROXIESTEROIDE DESHIDROGENASA TIPO 1.
    25.
    发明专利
    INHIBIDORES DE LA ENZIMA 11-BETA-HIDROXIESTEROIDE DESHIDROGENASA TIPO 1. 未知

    公开(公告)号：MX2008012970A

    公开(公告)日：2008-10-15

    申请号：MX2008012970

    申请日：2007-04-06

    Applicant: ABBOTT LAB

    Inventor： LINK JAMES T ,  YEH VINCE S ,  MADAR DAVID J ,  KURUKULASSURIYA RAVI

    IPC: C07D401/12 ,  C07D207/26

    Abstract: La presente invención se refiere a un compuesto de la fórmula (i) o una sal, profármaco, sal de profármaco o combinación de los mismos farmacéuticamente aceptable. También se refiere a métodos para inhibir la enzima 11-beta-hidroxiesteroide deshidrogenasa tipo 1; a métodos para el tratamiento de la diabetes tipo 2 no insulinodependiente, resistencia a la insulina, obesidad, trastornos lipídicos, síndrome metabólico y otras enfermedades y trastornos que son mediados por la acción excesiva de glucocorticoides.

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