AR039842A1 - Compuestos heterociclicos sustituidos y metodos de empleo - Google Patents

Compuestos heterociclicos sustituidos y metodos de empleo

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Publication number
AR039842A1
AR039842A1 ARP030101777A ARP030101777A AR039842A1 AR 039842 A1 AR039842 A1 AR 039842A1 AR P030101777 A ARP030101777 A AR P030101777A AR P030101777 A ARP030101777 A AR P030101777A AR 039842 A1 AR039842 A1 AR 039842A1
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AR
Argentina
Prior art keywords
alkyl
substituted
independently
instance
nrgrg
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ARP030101777A
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English (en)
Inventor
Celia Dominguez
Henry Q Zhang
Guo-Qiang Cao
Martin H Goldberg
Fang-Tsao Hong
Kelvin K C Sham
Seifu Tadesse
Nuria A Tamayo
Kurt E Weiler
Hongyu Liao
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Amgen Inc
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Application filed by Amgen Inc filed Critical Amgen Inc
Publication of AR039842A1 publication Critical patent/AR039842A1/es

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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
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Abstract

Reivindicación 1: Un compuesto de la fórmula (1) o una de sus sales farmacéuticamente aceptable, donde: n es 0, 1 ó 2; R1 es una cadena cerrada de 5, 6 ó 7 miembros, saturada o insaturada, que contiene 0, 1, 2 ó 3 átomos seleccionados de N, O y S, donde la cadena cerrada puede estar fusionada con un grupo benzo, y está sustituida por 0, 1 ó 2 grupos oxo, y donde R1 está adicionalmente sustituido por 0, 1, 2 ó 3 sustituyentes seleccionados de Rd y alquilo C1-4Rd; R2 es alquilo C1-6 sustituido con 1, 2 ó 3 grupos Rd y 0 ó 1 grupos Rc, que están sustituidos por 0, 1 ó 2 grupos Rd, donde R2 no es -C(=O)Obencilo; y donde -R1-R2 no es 3-bencilpiperazin-1-ilo; y donde si tanto R3 como R4 son 4-metilfenilo, -R1-R2 no es 4-(hidroximetil)piperidin-1-ilo; R3 es Rc sustituido por 0, 1, 2 ó 3 sustituyentes seleccionados de Rf y Rd; R4 es Rc sustituido por 0, 1, 2 ó 3 sustituyentes seleccionados de Rf y Rd que no incluyen 1-feniletilamino; siempre que el número total de grupos Rc sustituidos en cada uno de R3 y R4 sea 0 ó 1; R5 es independientemente en cada instancia H, alquilo C1-8 o alquilo C1-6Rc, ambos sustituidos por 0, 1, 2 ó 3 sustituyentes seleccionados de Rd; R6 es independientemente en cada instancia alquilo C1-8 o alquilo C1-6Rc, ambos sustituidos por 0, 1, 2 ó 3 sustituyentes seleccionados de Rd; o R6 es Rd; R7 es independientemente hidrógeno, -alquilo C1-6 o -alquilo C1-4Rc, donde cualquier átomo de carbono de la estructura anterior está sustituido por 0 a 3 sustituyentes seleccionados de Rd; Ra es independientemente en cada instancia h O Rb; Rb es independientemente en cada instancia alquilo C1-8, Rc o alquilo C1-4Rc, cada uno de los cuales está sustituido por 0, 1, 2 ó 3 sustituyentes seleccionados independientemente de Rd; Rc es independientemente en cada instancia arilo o una cadena cerrada heterocíclica de 5, 6 ó 7 miembros saturado o insaturada, que contiene 1, 2 ó 3 átomos seleccionados de N, O y S, donde la cadena cerrada está fusionada con 0 ó 1 grupos benzo y 0 ó 1 cadenas cerradas heterocíclicas de 5, 6 ó 7 miembros, saturadas o insaturadas, que contienen 1, 2 ó 3 átomos seleccionados de N, O y S; donde cualquier cadena cerrada heterocíclica está sustituida por 0, 1 ó 2 grupos oxo; Rd es independientemente en cada instancia alquilo C1-6, halo, haloalquilo C1-4, ciano, -C(=O)Rf, -C(=O)ORe, -C(=O)NRgRg, -C(=NRg)NRgRg, -ORe, --OC(=O)Re, -OC(=O)NRgRg, -OC(=O)N(Rh)S(=O)2Rf, -SRe, -S(=O)Rf, -S(=O)2Rf, -S(=O)2NRgRg, -S(=O)2N(Rh)C(=O)Rf, -S(=O)2N(Rh)C(=O)ORf, -S(=O)2-N(Rh)C(=O)NRgRg, -NRgRg, -N(Rh)C(=O)Re, -N(Rh)C(=O)ORf, -N(Rh)C(=O)NRgRg, -N(Rh)C(=NRg)NRgRg, -N(Rh)S(=O)2Rf ó -N(Rh)S(=O)NRgRg; Re es independientemente en cada instancia hidrógeno o Rf; Rf es independientemente en cada instancia Rc o alquilo C1-8, cualquiera de los cuales está sustituido por 0 a 3 sustituyentes seleccionados de -NRgRg, -C(=O)ORi, -ORi,-N(Ri)C(=O)Rk, -N(Ri)C(=O)ORi, -N(Ri)S(=O)2Rk, -S(=O)nRk, ciano, halo, -O alquilo C1-4 Rc, -S(=O)n alquilo C1-4 Rc y Rc, donde cualquier Rc en Rf puede estar sustituido, también, por alquilo C1-8 o haloalquilo C1-4; Rg es independientemente en cada instancia hidrógeno, Rc, alquilo C1-10 o -alquilo C1-4Rc, donde cada uno está sustituido por 0 a 3 sustituyentes seleccionados de -NRiRi, -N(Ri)C(=O)Rk, -N(Ri)C(=O)ORk, -N(Ri)S(=O)2Rk, -ORi, -S(=O)nRk, ciano, alquilo C1-8 y haloalquilo C1-4; Rh independientemente en cada instancia hidrógeno, alquilo C1-8 o alquilo C1-4Rc cada uno de los cuales está sustituido por 0 a 3 sustituyentes seleccionados de -NRiRi, -N(Ri)C(=O)Rk, -N(Ri)C(=O)ORk, -N(Ri)S(=O)2Rk, -ORi, -S(=O)nRk, ciano, alquilo C1-8 y haloalquilo C1-4; Ri es Rk o hidrógeno; Rk es alquilo C1-6, fenilo o bencilo; V es -N=, -NR5-, -CR6=, C=O, C=S o C=NR7; W es -N=, -NR5-, -CR6=, C=O, C=S o C=NR7; y X es -N=, -NR5-, -CR6=, C=O, C=S o C=NR7; donde el número total de grupos -NR5-, C=O, C=S o C=NR7 representados por V, W y X debe ser 0 ó 2; y al menos uno de V, W y X contiene un átomo de N. También se incluye un método para la profilaxis o el tratamiento de: inflamación, artritis reumatoidea, mal de Paget, osteoporosis, mieloma múltiple, uveitis, leucemia mielógeno aguda o crónica, destrucción de las células beta pancreáticas, osteoartritis, espondilitis reumatoidea, artiritis gotosa, enfermedad inflamatoria intestinal, síndrome de distrés respiratorio del adulto [ARDS, por sus siglas en inglés], soriasis, enfermedad de Crohn, rinitis alérgica, colitis ulcerosa, anafilaxis, dermatitis por contacto, asma, degeneración muscular, caquexia, síndrome de Reiter, diabetes del tipo I y del tipo II, enfermedades relacionadas con la resorción ósea, reacción injerto contra huésped, Mal de Alzheimer, ataque cerebrovascular, infarto del miocardio, lesión por isquemia-reperfusión, ateroesclerosis, trauma cerebral, esclerosis múltiple, malaria cerebral, sepsis, choque séptico, síndrome de choque tóxico, fiebre, mialgias padecidas a raíz de infecciones por VIH-1, VIH-2, VIH-3, citomegalovirus [CMV], gripe, adenovirus, herpes viral o infección por herpes zóster en un mamífero, que comprende la administración de una cantidad eficaz de un compuesto tal como el que se describió previamente.
ARP030101777A 2002-05-21 2003-05-22 Compuestos heterociclicos sustituidos y metodos de empleo AR039842A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US38269902P 2002-05-21 2002-05-21
US10/438,553 US7026326B2 (en) 2002-05-21 2003-05-13 Substituted heterocyclic compounds and methods of use

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AR039842A1 true AR039842A1 (es) 2005-03-02

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US (1) US7026326B2 (es)
EP (1) EP1506186A1 (es)
JP (2) JP4606161B2 (es)
AR (1) AR039842A1 (es)
AU (1) AU2003234628B2 (es)
CA (1) CA2485166A1 (es)
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TW200406399A (en) 2004-05-01
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WO2003099808A1 (en) 2003-12-04
EP1506186A1 (en) 2005-02-16
US20050038010A1 (en) 2005-02-17
AU2003234628A1 (en) 2003-12-12
MXPA04011470A (es) 2005-02-14
US7026326B2 (en) 2006-04-11
AU2003234628B2 (en) 2007-08-23
JP4606161B2 (ja) 2011-01-05
WO2003099808A8 (en) 2009-02-05
JP2010280669A (ja) 2010-12-16

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