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AR054021A1 - Derivados de ciclopentapiridina y tetrahidroquinolina - Google Patents

Derivados de ciclopentapiridina y tetrahidroquinolina

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Publication number
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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AR
Argentina
Prior art keywords
alkyl
independently selected
membered
group
heteroatoms independently
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ARP060101218A
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English (en)
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Pfizer Prod Inc
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Publication of AR054021A1 publication Critical patent/AR054021A1/es

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    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
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    • 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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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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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    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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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    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
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    • C07D401/14—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 three or more hetero rings
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    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • 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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  • Chemical & Material Sciences (AREA)
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  • Hospice & Palliative Care (AREA)
  • Gynecology & Obstetrics (AREA)
  • Emergency Medicine (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)

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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MX2007012082A (es) 2007-11-20
CR9386A (es) 2007-10-02
US7507732B2 (en) 2009-03-24
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WO2006103511A1 (en) 2006-10-05
NZ560917A (en) 2011-01-28
NL1031473A1 (nl) 2006-10-03
UY29446A1 (es) 2006-10-31
IL185492A0 (en) 2008-01-06
KR100894006B1 (ko) 2009-04-17
EP1869000A1 (en) 2007-12-26
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TNSN07367A1 (fr) 2008-12-31
AP2007004144A0 (en) 2007-08-31
MA29354B1 (fr) 2008-03-03
CA2602348C (en) 2011-03-01
GT200600128A (es) 2007-03-29
CA2602348A1 (en) 2006-10-05
PE20061333A1 (es) 2007-01-13
JP4318744B2 (ja) 2009-08-26
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EA200701853A1 (ru) 2008-08-29
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