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AR050155A1 - 3-aminoindazoles, un procedimiento de preparcion, uso de los compuestos para preparar medicamentos, dichos medicamentos y un compuesto intermediario - Google Patents

3-aminoindazoles, un procedimiento de preparcion, uso de los compuestos para preparar medicamentos, dichos medicamentos y un compuesto intermediario

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Publication number
AR050155A1
AR050155A1 ARP050102033A ARP050102033A AR050155A1 AR 050155 A1 AR050155 A1 AR 050155A1 AR P050102033 A ARP050102033 A AR P050102033A AR P050102033 A ARP050102033 A AR P050102033A AR 050155 A1 AR050155 A1 AR 050155A1
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Argentina
Prior art keywords
mono
hal
het
trisubstituted
con
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ARP050102033A
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English (en)
Inventor
Lars Thore Burgdorf
Rolf Gericke
Norbert Beier
Werner Mederski
Florian Lang
Dieter Dorsch
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Merck Patent Gmbh
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Publication of AR050155A1 publication Critical patent/AR050155A1/es

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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56Benzopyrazoles; Hydrogenated benzopyrazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
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    • A61P25/20Hypnotics; Sedatives
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    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
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    • A61P35/00Antineoplastic agents
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    • A61P35/00Antineoplastic agents
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    • AHUMAN NECESSITIES
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    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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 chain containing hetero atoms as chain links
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
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    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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Abstract

Los 3-aminoindazoles de la formula (1), son inhibidores de la SGK y pueden ser utilizados para el tratamiento de enfermedades y dolencias causadas por las SGK y tales como diabetes, obesidad, síndrome metabolico (dislipidemia), hipertonía sistémica y pulmonar, enfermedades cardiocirculatorias y renales, en general para todo tipo de fibrosis y procesos inflamatorios. Se reivindica el compuesto, un método de preparacion, su uso para preparar medicamentos y un kid para el compuesto y un compuesto intermediario de síntesis. Reivindicacion 1: Compuestos de la formula (1), en donde: W es -[C(R2)2]n-, -[C(R2)2]nCONR2[C(R2)2]n-, -[C(R2)2]nCONR2NR2[C(R2)2]n-, -[C(R2)2]nNR2CO[C(R2)2]n-, -[C(R2)2]nNR2CO[C(R2)2]nNR2-, -[C(R2)2]nO[C(R2)2]n-, - [C(R2)2]nNR2[C(R2)2]n-, -[C(R2)2]nN[C(R2)2R1][C(R2)2]n-, -[C(R2)2]nO[C(R2)2]nCONR2[C(R2)2]n-, -[C(R2)2]nNR2[C(R2)2]nCONR2[C(R2)2]n-, -[C(R2)2]nNR2COO[C(R2)2]n-, -[C(R2)2]nCO[C(R2)2]n-, -[C(R2)2]nCOO[C(R2)2]n-, -C(R2)=C(R29CONR2[C(R2)2]n o -C(R2)=N- NR2CO[C(R2)2]n; X es H, Hal, A, OR2, N(R2)2, NO2, CN, COOR2, CON(R2)2, NR2COA, NR2SO2A, CO2 o SO2NR2; R1 es un carbociclo o heterociclo saturado o insaturado mono o bicíclico con 0 a 4 átomos de N, O y/o S, que puede estar mono, bi o trisustituido con R2, Hal, A, -[C(R3)2]n-Ar, -[C(R3)2]n-Het, -O-[C(R3)2]n-Het, -[C(R3)2]n-cicloalquilo, OR2, N(R2)2, NO2, CN, -[C(R2)2]nCOOR2, O-[C(R2)2]nCOOR2, -[C(R2)2]nCON(R2)2, -[C(R2)2]nCONR2N(R2)2, O-[C(R2)2]oCON(R2)2, O-[C(R2)2]oCONR2N(R2)2, NR2COA, NR2CON(R2)2, NR2SO2A, COR2, SO2NR2, S(O)mA, =S, =NR3 y/u =O (oxígeno del carbonilo); R2 es H, A, -[C(R3)2]n-Ar', -[C(R3)2]n-Het', -[C(R3)2]n-cicloalquilo, -[C(R3)2]n-OR3, -[C(R3)2]n-COOA o -[C(R3)2]nN(R3)2; R3 es H o A; A es alquilo no ramificado o ramificado con C1-10, en donde uno o dos grupos CH2 pueden estar reemplazados por átomos de O o S y/o por grupos -CH=CH- y/o también 1-7 átomos de H pueden estar reemplazados por F; Ar es fenilo, naftilo o bifenilo insustituido o mono, di o trisustituido con Hal, A, OR2, N(R2)2, NO2, CN, COOR2, CON(R2)2, NR2COA, NR2CON(R2)2, NR2SO2A, COR2, SO2N(R2)2, S(O)mA, -[C(R3)2]n-COOR2 u -O[C(R3)2]o-COOR2; Ar' es fenilo, naftilo o bifenilo insustituido o mono, di o trisustituido con Hal, A, OR3, N(R3)2, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3CON(R3)2, NR3SO2A, COR3, SO2N(R3)2, S(O)mA, -[C(R3)2]n-COOR3 u -O[C(R3)2]o-COOR3; Het es un heterociclo saturado o insaturado mono o bicíclico con 1 a 4 átomos de N, O y/o S, que puede estar mono, bi o trisustituido con R2, Hal, A, -[C(R3)2]n-Ar, -[C(R3)2]n-Het, -[C(R3)2]n-cicloalquilo, OR2, N(R2)2, NO2, CN, -[C(R2)2]nCOOR2, O--[C(R2)2]nCOOR2, -[C(R2)2]nCON(R2)2, -[C(R2)2]nCONR2N(R2)2, O-[C(R2)2]oCON(R2)2, O-[C(R2)2]oCONR2N(R2)2, NR2COA, NR2CON(R2)2, NR2SO2A, COR2, SO2NR2, S(O)MA y/u =O (oxígeno del carbonilo); Het' es un heterociclo saturado o insaturado mono o bicíclico con 1 a 4 átomos de N, O y/o S, que puede estar mono, bi o trisustituido con R3, Hal, A, OR2, N(R3)2, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3SO2A, COR3, SO2NR3, S(O)mA, =S, =NR3 y/u =O (oxígeno del carbonilo), Hal es F, Cl, Br o I; m es 0, 1 o 2; n es 0, 1, 2, 3 o 4; o es 1, 2 o 3; así como sus derivados, sales, solvatos y estereoisomeros de utilidad farmacéutica, incluyendo sus mezclas en todas las proporciones.
ARP050102033A 2004-06-15 2005-05-18 3-aminoindazoles, un procedimiento de preparcion, uso de los compuestos para preparar medicamentos, dichos medicamentos y un compuesto intermediario AR050155A1 (es)

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DE102004028862A DE102004028862A1 (de) 2004-06-15 2004-06-15 3-Aminoindazole

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AR050155A1 true AR050155A1 (es) 2006-10-04

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US (1) US7872039B2 (es)
EP (1) EP1765788B1 (es)
JP (1) JP5128939B2 (es)
AR (1) AR050155A1 (es)
AT (1) ATE432924T1 (es)
AU (1) AU2005254617B2 (es)
CA (1) CA2570264C (es)
DE (2) DE102004028862A1 (es)
ES (1) ES2326897T3 (es)
WO (1) WO2005123688A2 (es)

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CA2570264A1 (en) 2005-12-29
ES2326897T3 (es) 2009-10-21
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ATE432924T1 (de) 2009-06-15
AU2005254617A1 (en) 2005-12-29
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