AR054021A1 - Derivados de ciclopentapiridina y tetrahidroquinolina - Google Patents

Derivados de ciclopentapiridina y tetrahidroquinolina

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AR054021A1
AR054021A1 ARP060101218A ARP060101218A AR054021A1 AR 054021 A1 AR054021 A1 AR 054021A1 AR P060101218 A ARP060101218 A AR P060101218A AR P060101218 A ARP060101218 A AR P060101218A AR 054021 A1 AR054021 A1 AR 054021A1
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Argentina
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alkyl
independently selected
membered
group
heteroatoms independently
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Pfizer Prod Inc
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Abstract

En este documento se describen compuestos 6,7-dihidro-5H-ciclopenta[b]piridina y 5,6,7,8-tetrahidroquinolina, incluyendo sales, hidratos y solvatos de los mismos, que actuan como ligandos del receptor 5-Ht2 y sus usos ene el tratamiento de enfermedades relacionadas con la activacion de los receptores 5-HT2c. Reivindicacion 1: Un compuesto de la formula (1) en la que m es 1 o 2; n es 0 o 1; L es -CHR0a-, donde R0a es hidrogeno o alquilo (C1-C4); R2 es hidrogeno o metilo; R3 se selecciona entre el grupo constituido por H, Cl, Br, F, CH3 y CN; R1 es (a) un grupo de la formula (2) donde (i) cada uno de p, r y s es independientemente 0 o 1, y cada uno de R1a, R1b y R1c se selecciona independientemente entre el grupo constituido por F, Cl, Br, I, ciano, -CH2-CN, -NH2, -OH, alquilo (C1-C6), alcoxi (C1-6), alquil (C1-C4) fluoro-sustituido, alcoxi (C1-C4), fluoro sustituido, alquil(C1-C4)-tio fluoro-sustituido, -NH-C(O)-alquilo (C1-C4),-C(O)-alquilo (C1-C4), -C(O)- O-alquilo (C1-C4), -C(O)-NH2, -C(O)-NH-alquilo (C1-C4), un anillo carbocíclico de 3 a 6 miembros y fenilo sustituido con F, CL, Br o I; (ii) cada uno de p y r es 0 o 1, s es 1, cada uno de R1b se selecciona independientemente entre F, Cl, Br, I, ciano, -NH2, -C(O)-alquilo (C1-4), alquilo (C1-6), alcoxi (C1-C6), alquil (C1-C4)-tio, alquilo (C1-C4) fluoro sustituido, alcoxi (C1-4) fluoro sustituido o alquil (C1-4)-tio fluoro-sustituido, y (R1c)s está unido a un átomo de carbono adyacente del anillo distinto del carbono mediante el cual el grupo de formula 1 A se une al resto de la molécula y (R1c)s tomado junto con los dos carbonos a los que está unido forma un anillo seleccionado entre el grupo constituido por: un anillo carbocíclico de 5 a 6 miembros que contiene opcionalmente un grupo ceto, un anillo heterocíclico de 5 a 6 miembros que contiene 1 a 2 heteroátomos seleccionados independientemente entre O, S, o N, y que contiene opcionalmente un grupo ceto, un anillo aromático de 6 miembros, y un anillo heteroaromático de 5 a 6 miembros que contiene de 1 a 2 heteroátomos seleccionados independientemente entre O, S o N, donde dicho anillo carbocíclico, dicho anillo heterocíclico, dicho anillo aromático y dicho anillo heteroaromático están opcionalmente sustituidos con 1 a 2 sustituyentes seleccionados entre el grupo constituido por alquil (C1-C4), ciano, acetilo, F, Cl, Br, I fenilamino, alquilo (C1-C4)-amino, un anillo heterocíclico de 5 a 6 miembros que contiene de 1 a 3 heteroátomos seleccionados independientemente entre N, O y S que está opcionalmente sustituido con 1 a 3 sustituyentes seleccionados entre alquilo (C1-C4) y un anillo heteroarilo de 5 a 6 miembros que contiene de 1 a 3 heteroátomos seleccionados independientemente entre N, O y S y que está opcionalmente sustituido con 1 a 3 sustituyentes seleccionados entre alquilo (C1-C4); o (iii) cada uno de p y r es 0, s es 1, y R1c se selecciona independientemente entre el grupo constituido por fenilo, fenoxi opcionalmente sustituido con F, Cl, Br o I; bencilo, benciloxi, -NH-alquilo (C1-C4), -N[alquilo (C1-C4)]2, -CH2-NH-alquilo(C1-C4), -CH2-N[alquilo (C1-C4)]2, -NH(fenilo), -NH(heteroarilo de 5 a 6 miembros que contiene de 1 a 3 heteroátomos seleccionados independientemente entre O, N y S, que está opcionalmente sustituido con 1 a 3 grupos halo), -N(CH3)-SO2alquilo (C1-4),- NH-SO2alquilo (C1-C4), -NHC(O)NH2, -C(O)-N[alquilo (C1-C4)]2, -C(O)-(heterociclo de 5 a 6 miembros que contiene de 1 a 3 heteroátomos seleccionados independientemente entre O, N y S), -C(O)-NH(heterociclo de 5 a 6 miembros que contiene de 1 a 3 heteroátomos seleccionados independientemente entre O, N y S), -C(O)-(carbociclo de 5 a 6 miembros), - CH2-C(O)-O-alquilo (C1-C4), un anillo heterocíclico de 3 a 6 miembros que contiene de 1 a 3 heteroátomos seleccionados independientemente entre O, N o S, y un heteroarilo de 5 a6 miembros que contiene de 1 a 3 heteroátomos seleccionados independientemente entre O, N o S que está opcionalmente sustituido con de uno a tres sustituyentes seleccionados independientemente entre F, Cl, Br I y -CF3; (b) un heteroarilo de 5 a 6 miembros que contiene de 1 a 3 heteroátomos seleccionados independientemente entre O, S o N, donde dicho heteroarilo está opcionalmente condensado con un anillo carbocíclico de 5 a 6 miembros o un anillo aromático de 6 miembros y dicho heteroarilo está opcionalmente sustituido con 1 a 2 sustituyentes seleccionados independientemente entre el grupo constituido por ciano, F, Cl, Br, I, alquilo (C1-C4), alcoxi (C1-C4) y -C(O)-O alquilo (C1-C4); o una sal farmacéuticamente aceptable del mismo, o un solvato o hidrato de dicho compuesto o de dicha sal.
ARP060101218A 2005-03-31 2006-03-29 Derivados de ciclopentapiridina y tetrahidroquinolina AR054021A1 (es)

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EP (1) EP1869000A1 (es)
JP (1) JP4318744B2 (es)
KR (1) KR100894006B1 (es)
AP (1) AP2007004144A0 (es)
AR (1) AR054021A1 (es)
AU (1) AU2006228378A1 (es)
BR (1) BRPI0609268A2 (es)
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EA (1) EA200701853A1 (es)
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GT200600128A (es) 2007-03-29
CA2602348A1 (en) 2006-10-05
JP2008534568A (ja) 2008-08-28
NL1031473C2 (nl) 2007-03-19
TW200722423A (en) 2007-06-16
MA29354B1 (fr) 2008-03-03
MX2007012082A (es) 2007-11-20
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PE20061333A1 (es) 2007-01-13
NL1031473A1 (nl) 2006-10-03
UY29446A1 (es) 2006-10-31
BRPI0609268A2 (pt) 2010-03-09
DOP2006000076A (es) 2006-11-30
KR100894006B1 (ko) 2009-04-17
CA2602348C (en) 2011-03-01
WO2006103511A1 (en) 2006-10-05
CR9386A (es) 2007-10-02
EA200701853A1 (ru) 2008-08-29
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US7507732B2 (en) 2009-03-24
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