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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EC2003004683A
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English (en)
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Anthony Marfat
Michael William Mckechney
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Pfizer Prod Inc
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Publication of ECSP034683A publication Critical patent/ECSP034683A/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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
    • C07D277/56Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen

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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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EC2003004683A ECSP034683A (es) 2001-01-31 2003-07-04 Derivados amida de acido tiazolilico, oxazolilico, pirrolilico e imidazolilico utiles como inhibidores de las isozimas pde4

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US (3) US6559168B2 (es)
EP (1) EP1355907A1 (es)
JP (1) JP2004518691A (es)
KR (1) KR20030072614A (es)
CN (1) CN1489588A (es)
BG (1) BG108039A (es)
BR (1) BR0116850A (es)
CA (1) CA2436551A1 (es)
CR (1) CR7038A (es)
CZ (1) CZ20031903A3 (es)
EA (1) EA200300622A1 (es)
EC (1) ECSP034683A (es)
EE (1) EE200300362A (es)
HU (1) HUP0401305A2 (es)
IL (1) IL156412A0 (es)
IS (1) IS6844A (es)
MA (1) MA26985A1 (es)
MX (1) MXPA03006886A (es)
NO (1) NO20033398L (es)
OA (1) OA12542A (es)
PL (1) PL365443A1 (es)
TN (1) TNSN03050A1 (es)
WO (1) WO2002060898A1 (es)
ZA (1) ZA200305769B (es)

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