ECSP034683A - Derivados amida de acido tiazolilico, oxazolilico, pirrolilico e imidazolilico utiles como inhibidores de las isozimas pde4 - Google Patents

Derivados amida de acido tiazolilico, oxazolilico, pirrolilico e imidazolilico utiles como inhibidores de las isozimas pde4

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Publication number
ECSP034683A
ECSP034683A EC2003004683A ECSP034683A ECSP034683A EC SP034683 A ECSP034683 A EC SP034683A EC 2003004683 A EC2003004683 A EC 2003004683A EC SP034683 A ECSP034683 A EC SP034683A EC SP034683 A ECSP034683 A EC SP034683A
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EC
Ecuador
Prior art keywords
optionally
carbon atom
members
alkyl
replaced
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Application number
EC2003004683A
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English (en)
Inventor
Anthony Marfat
Michael William Mckechney
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Pfizer Prod Inc
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Publication date
Application filed by Pfizer Prod Inc filed Critical Pfizer Prod Inc
Publication of ECSP034683A publication Critical patent/ECSP034683A/es

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    • C07D417/02—Heterocyclic 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
    • C07D417/12—Heterocyclic 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

Compuestos útiles como inhibidores de las PDE4 en el tratamiento de enfermedades reguladas por la activación y la desgranulación de eosinofilos, especialmente asma, bronquitis crónica y enfermedad pulmonar obstructiva crónica, de fórmula (Gráfico). En la que j es 0 ó 1, con la condición de que cuando j es 0, n debe ser 2; k es 0 ó 1; m es 0, 1,2 ó 3; n es 1 ó 2; W1 es -O-; ó esta ausente; Y es=C(R1a)-ó- [N->(O)k]-siendo K 0 ó 1; RA y RB son -H; -F; -CF3; -alquilo (C1-C4); -cicloalquilo (C3-C7); fenilo; o bencilo sustituido con 0 a 3 sustituyentes R10; ó RA y RB se toman conjuntamente,m pero sólo en el caso en que m sea 1, para formar un resto espiro; RC y RD tienen el mismo significado que RA y RB; excepto que uno de ellos debe ser -H, R1 y R2 son -H, -F, -CI; -CN; -N02; - alquio (C1-C4); -alquinilo (C2-C4); alquilo (C1-C3) fluorado; -OR16; y -C(=0) NR22a R22b; R3 es -H; -, alquilo (C1-C3); fenilo; bencilo; ó -OR16, R4,R5 y R6, además de otros significados pueden tomarse conjuntamente para formar, por ejemplo: G1 es un sistema carbociclico saturado unsaturado monociclito de 3 a 7 miembros, o policiclico condensado de 7 a 12 miembros con la condición de que G1 no es un resto biarilo discontinuo o limitado como se define en G2; puediendo estar opcionalmente reemplazado un átomo de carbono por un heteroatomo seleccionado de N, 0 y S; pudiendo estar reemplazado opcionalemte un segundo átomo de carbona de este, y opcionalemte además un tercer átomo de carbona de este, por N; -G2 es un sistema carbociclico saturado o insaturado monociclico de 3 a 7 miembros, o policiclico condensado de 7 a 12 miembros; o es un resto biarilo discontinuo o limitado de 8 a 18 miembros; pudiendo estar opcionalmentereemplazado, paracada uno de los sistemas carvociclicos enumerados, un átomo de carbono del citado sistema carbociclico por un heteroátomo seleccionado de N, 0 y S; pudiendo estar opcionalmente reemplazado un segundo átomo de carbona del mismo, y opcionalmente un tercer átomo de carbona del mismo por N; y E se selecciona de:
EC2003004683A 2001-01-31 2003-07-04 Derivados amida de acido tiazolilico, oxazolilico, pirrolilico e imidazolilico utiles como inhibidores de las isozimas pde4 ECSP034683A (es)

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US26548601P 2001-01-31 2001-01-31

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ECSP034683A true ECSP034683A (es) 2003-08-29

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US (3) US6559168B2 (es)
EP (1) EP1355907A1 (es)
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CZ (1) CZ20031903A3 (es)
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US6696473B2 (en) * 2001-12-21 2004-02-24 X-Ceptor Therapeutics, Inc. Heterocyclic modulators of nuclear receptors
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