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AR032629A1 - Compuestos derivados de imidazol y composicion farmaceutica que los contiene - Google Patents

Compuestos derivados de imidazol y composicion farmaceutica que los contiene

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Publication number
AR032629A1
AR032629A1 ARP010103637A ARP010103637A AR032629A1 AR 032629 A1 AR032629 A1 AR 032629A1 AR P010103637 A ARP010103637 A AR P010103637A AR P010103637 A ARP010103637 A AR P010103637A AR 032629 A1 AR032629 A1 AR 032629A1
Authority
AR
Argentina
Prior art keywords
straight
branched chain
membered
nr7r8
independently selected
Prior art date
Application number
ARP010103637A
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English (en)
Original Assignee
Pfizer Prod Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Pfizer Prod Inc filed Critical Pfizer Prod Inc
Publication of AR032629A1 publication Critical patent/AR032629A1/es

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    • 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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    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
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    • A61P25/06Antimigraine agents
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    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
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    • A61P37/02Immunomodulators
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    • C07ORGANIC CHEMISTRY
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    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/88Nitrogen atoms, e.g. allantoin
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    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D417/14Heterocyclic 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 three or more hetero rings

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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Medicinal Chemistry (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
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  • Pain & Pain Management (AREA)
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Abstract

Un compuesto por ser de formula (1) en la que: R1 es alquilo C1-8 de cadena lineal o ramificada, alquenilo C2-8 de cadena lineal o ramificada, alquinilo C2-8 de cadena lineal o ramificada, cicloalquilo C3-8, cicloalquenilo C4-8, heterocicloalquilo de 3-8 miembros, bicicloalquilo C5-11, bicicloalquenilo C7-11, heterobicicloalquilo de 5-11 miembros, arilo C6-14, o heteroarilo de 5-14 miembros; y estando R1 opcionalmente sustituido con 1-6 sustituyentes R5 seleccionados independientemente entre F, Cl, Br, I, nitro, ciano, -CF3, -NR7R8, -NR7C(=O)R8, -NR7C(=O)OR8, -NR7C(=O)NR8R, -NR7S(=O)2R8, -NR7S(=O)2R8R9, -OR7, -OC(=O)R7, -OC(=O)OR7, -C(=O)OR7, -C(=O)R7, -C(=O)NR7R8, -OC(=O)NR7R8, -OC(=O)SR7, -SR7, -S(=O)R7, -S(=O)2R7, -S(=O)2NR7R8, -O-S(=O)2R7, N3 y R7; R2 es H, F, -CH3, -CN o -C(=O)OR7; R3 es -C(=O)NR9, -C(=O)O-, -C(=O)(CR10R11)n-, o -(CR10R11)n-; R4 es alquilo C1-8 de cadena lineal o ramificada, alquenilo C2-8 de cadena lineal o ramificada, alquinilo C2-8 de cadena lineal o ramificada, cicloalquilo C3-8, cicloalquenilo C4-8, heterocicloalquilo de 3-8 miembros, bicicloalquilo C5-11, bicicloalquenilo C7-11, heterobicicloalquilo de 5-11 miembros, arilo C6-14 o heteroarilo de 5-14 miembros, estando R4 opcionalmente sustituido con 1-3 sustituyentes R6 seleccionados independientemente entre F, Cl, Br, I, nitro, ciano, -CF3, -NR7R8, -NR7C(=O)R8, -NR7C(=O)OR8, -NR7C(=O)NR8R9, -NR7S(=O)2R8, -NR7S(=O)2NR8R9, -OR7, -OC(=O)R7, -OC(=O)OR7, -C(=O)OR7, -C(=O)R7, -C(=O)NR7R8, -OC(=O)NR7R8, -OC(=O)SR7, -SR7, -S(=O)R7, -S(=O)2R7, -S(=O)2NR7R8, o R7; cada uno de R7, R8 y R9 se selecciona independientemente entre H, alquilo C1-8 de cadena lineal o ramificada, alquenilo C2-8 de cadena lineal o ramificada, alquinilo C2-8 de cadena lineal o ramificada, cicloalquilo C3-8, cicloalquenilo C4-8, heterocicloalquilo de 3-8 miembros, bicicloalquilo C5-11, bicicloalquenilo C7-11, heterobicicloalquilo de 5-11 miembros, arilo C6-14 y heteroarilo de 5-14 miembros, estando cada uno de R7, R8 y R9 opcional e independientemente sustituido con 1-6 sustituyentes seleccionados entre F, Cl, Br, I, NO2, -CN, -CF3, -NR10R11, -NR10C(=O)R11, -NR10C(=O)OR11, -NR10C(=O)NR11R12, -NR10S(=O)2R11, -NR10S(=O)2NR11R12, -OR10, -OC(=O)R10, -OC(=O)OR10, -OC(=O)NR10R11, -OC(=O)SR10, -SR10, -S(=O)R10, -S(=O)2R10, -S(=O)2NR10R11, -C(=O)R10, -C(=O)OR10, -C(=O)NR10R11 y R10; o, cuando R7 y R8 son como en NR7R8, pueden estar unidos opcionalmente para formar, junto con el nitrogeno de NR7R8 al que están unidos, un resto heterocicloalquilo de 3-7 miembros de anillo, comprendiendo opcionalmente dicho resto heterocicloalquilo 1-2 heteroátomos adicionales seleccionados independientemente entre N, O y S; cada uno de R10, R11 y R12 se selecciona independientemente entre H, alquilo C1-8 de cadena lineal o ramificada, alquenilo C2-8 de cadena lineal o ramificada, alquinilo C2-8 de cadena lineal o ramificada, cicloalquilo C3-8, cicloalquenilo C4-8, heterocicloalquilo de 3-8 miembros, bicicloalquilo C5-11, bicicloalquenilo C7-11, heterobicicloalquilo de 5-11 miembros, arilo C6-14 y heteroarilo de 5-14 miembros, estando cada uno de R10, R11 y R12 opcional e independientemente sustituido con 1-6 sustituyentes seleccionados entre F, Cl, Br, I, NO2, -CN, -CF3, -NR13R14, -NR13C(=O)R14, -NR13C(=O)OR14, -NR13C(=O)NR14R15, -NR13S(=O)2R14, -NR13S(=O)2NR14R15, -OR13, -OC(=O)R13, -OC(=O)OR13, -OC(=O)NR13R14, -OC(=O)SR13, -SR13, -S(=O)R13, -S(=O)2R13, -S(=O)2NR13R14, -C(=O)R13, -C(=O)OR13, -C(=O)NR13R14 y R13; cada uno de R13, R14 y R15 se selecciona independientemente entre H, alquilo C1-8 de cadena lineal o ramificada, alquenilo C2-8 de cadena lineal o ramificada, alquinilo C2-8 de cadena lineal o ramificada, cicloalquilo C3-8, cicloalquenilo C4-8, heterocicloalquilo de 3-8 miembros, bicicloalquilo C5-11, bicicloalquenilo C7-11, heterobicicloalquilo de 5-11 miembros, arilo C6-14 y heteroarilo de 5-14 miembros, estando cada uno de R13, R14 y R15 opcional e independientemente sustituido con 1-6 sustituyentes seleccionados entre F, Cl, Br, I, NO2, -CN, -CF3, -NR16R17, -NR16C(=O)R17, -NR16C(=O)OR17, -NR16C(=O)NR17R18, -NR16S(=O)2R17, -NR16S(=O)2NR17R18, -OR16, -OC(=O)R16, -OC(=O)OR16, -OC(=O)NR16R17, -OC(=O)SR16, -SR16, -S(=O)R16, -S(=O)2R16, -S(=O)2NR16R17, -C(=O)R16, -C(=O)OR16, -C(=O)NR16R17 y R16; cada uno de R16, R17 y R18 se selecciona independientemente entre H, alquilo C1-8 de cadena lineal o ramificada, alquenilo C2-8 de cadena lineal o ramificada, alquinilo C2-8 de cadena lineal o ramificada, cicloalquilo C3-8, cicloalquenilo C4-8, heterocicloalquilo de 3-8 miembros, bicicloalquilo C5-11, bicicloalquenilo C7-11, heterobicicloalquilo de 5-11 miembros, arilo C6-13 y heteroarilo de 5-12 miembros; n es 0, 1, 2 o 3; siendo R10 y R11 en -C(=O)(CR10R11)n- y -(CR10R11)n-, para cada repeticion de n, independientemente como se ha mencionado anteriormente; o una sal farmacéuticamente aceptable del mismo. Se indica que los compuestos de formula (1) tienen actividad inhibidora de cdk5, cdk2 y GSK-3. También se describen composiciones farmacéuticas y procedimientos que comprenden compuestos de formula (1) para tratar y prevenir enfermedades y afecciones que comprenden un crecimiento celular anormal, tal como el cáncer, enfermedades y afecciones neurodegenerativas, y las afectadas por la neurotransmision de dopamina. También se describen composiciones farmacéuticas y procedimientos que comprenden compuestos de formula (1) para tratar la fertilidad masculina y motilidad de los espermatozoides; diabetes mellitus; disminucion de la tolerancia a la glucosa; síndrome metabolico o síndrome X; síndrome de ovarios poliquísticos; adipogénesis y obesidad; miogénesis y debilidad, por ejemplo, la reduccion del rendimiento físico relacionado con la edad; sarcopenia aguda, por ejemplo, atrofia muscular y/o caquexia asociada con quemaduras, reposo en cama, inmovilizacion de miembros o cirugía torácica, abdominal y/u ortopédica mayor; sepsis; pérdida del cabello, debilitamiento del cabello y calvicie; e inmunodeficiencia.
ARP010103637A 2000-07-31 2001-07-30 Compuestos derivados de imidazol y composicion farmaceutica que los contiene AR032629A1 (es)

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US22172400P 2000-07-31 2000-07-31

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AR032629A1 true AR032629A1 (es) 2003-11-19

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EP (1) EP1305295A1 (es)
JP (2) JP4166084B2 (es)
KR (1) KR20030019644A (es)
CN (1) CN1444567A (es)
AP (1) AP2001002232A0 (es)
AR (1) AR032629A1 (es)
AU (1) AU2001270944A1 (es)
BG (1) BG107469A (es)
BR (1) BR0112862A (es)
CA (1) CA2418115A1 (es)
CR (1) CR6861A (es)
CZ (1) CZ2003225A3 (es)
DO (1) DOP2001000220A (es)
EA (1) EA200300097A1 (es)
EC (1) ECSP034445A (es)
EE (1) EE200300049A (es)
GT (1) GT200100147A (es)
HR (1) HRP20030048A2 (es)
HU (1) HUP0303069A3 (es)
IL (1) IL153787A0 (es)
IS (1) IS6662A (es)
MA (1) MA26932A1 (es)
MX (1) MXPA03000939A (es)
NO (1) NO20030472L (es)
NZ (1) NZ523272A (es)
OA (1) OA12345A (es)
PA (1) PA8523701A1 (es)
PE (1) PE20020337A1 (es)
PL (1) PL365134A1 (es)
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