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AR050403A1 - Derivados de bencil(ideno)- lactamas. composiciones farmaceuticas - Google Patents

Derivados de bencil(ideno)- lactamas. composiciones farmaceuticas

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Publication number
AR050403A1
AR050403A1 ARP050101025A ARP050101025A AR050403A1 AR 050403 A1 AR050403 A1 AR 050403A1 AR P050101025 A ARP050101025 A AR P050101025A AR P050101025 A ARP050101025 A AR P050101025A AR 050403 A1 AR050403 A1 AR 050403A1
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AR
Argentina
Prior art keywords
alkyl
ring
zero
naphthyl
phenyl
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ARP050101025A
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English (en)
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Pfizer Prod Inc
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Publication of AR050403A1 publication Critical patent/AR050403A1/es

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    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
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    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D211/72—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
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    • 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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    • C07D401/10—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 carbon chain containing aromatic rings
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    • C07—ORGANIC CHEMISTRY
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    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D405/04—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 directly linked by a ring-member-to-ring-member bond
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    • C07D405/10—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 carbon chain containing aromatic rings
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    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings

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  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
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  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
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  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Public Health (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Psychology (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Obesity (AREA)
  • Child & Adolescent Psychology (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Anesthesiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyrrole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Los compuestos pertenecen a la categoría de antagonistas selectivos, agonistas inversos y agonistas parciales de receptores 5-HT1 de serotonina. Composiciones farmacéuticas que los contienen. Reivindicacion 1: Un compuesto de formula (1), en la que R1 es un grupo de formula (2) o (3) descritas a continuacion: a es cero a ocho; m es uno a tres; R6 se selecciona entre el grupo que consiste en hidrogeno, alquilo C1-6 opcionalmente sustituido con alcoxi C1-6 o uno a tres átomos de fluor, o alquilC1-4-arilo en el que el resto arilo es fenilo, naftilo o heteroaril-(CH2)q-, en que el resto heteroarilo se selecciona entre el grupo que consiste en piridilo, pirimidilo, benzoxazolilo, benzotiazolilo, bencizoxazolilo y bencisotiazolilo y q es cero, uno, dos, tres o cuatro, y en que dichos restos arilo y heteroarilo pueden estar opcionalmente sustituidos con uno o más sustituyentes independientemente seleccionados entre el grupo que consiste en cloro, fluor, bromo, yodo, alquilo C1-6, alcoxi C1-6, trifluorometilo, ciano y -SOt-alquiloC1-6, en que t es cero, uno o dos; cada R13 es, independientemente, alquilo C1-4 o un puente de alquileno C1-4 de uno de los -átomos de carbono anulares del anillo de piperazino o piperidino de formula (2) o (3), respectivamente, al mismo o a otro átomo de carbono del anillo o a un átomo de nitrogeno anular del anillo de piperazino o piperidino de formula (2) o (3), respectivamente, que tiene un sitio de union disponible, o a un átomo de carbono del anillo de R6, cuando R6 tiene una estructura anular que tiene un sitio de union disponible; X es hidrogeno, cloro, fluor, bromo, yodo, ciano, alquilo C1-6, hidroxi, alcoxi C1-6, -SOt-alquiloC1-6 en donde t es cero, uno o dos, -CO2R10 o - CONR11R12; cada uno de R10, R11 y R12 se selecciona independientemente entre hidrogeno, alquilo C1-4, fenilo y naftilo, en donde dicho fenilo o naftilo pueden estar opcionalmente sustituidos con uno o más sustituyentes independientemente seleccionados entre cloro, fluor, bromo, yodo, alquilo C1-6, alcoxi C1-6, trifluorometilo, ciano y -SOt-alquiloC1-6, en donde t es cero, uno o dos; o R11 y R12, junto con el átomo de nitrogeno al que están unidos, forman un anillo de heteroalquilo de 5 a 7 miembros que puede contener de cero a cuatro heteroátomos seleccionados entre nitrogeno, azufre y oxígeno; R3 es vinilo, C(=O)R, en donde R es alquilo C1-8 de cadena lineal o ramificada, cicloalquilo C3-8 o arilo, en donde R es preferiblemente terc-butilo; o R3 es -(CH2)qB, en donde g es cero a tres y B es hidrogeno, fenilo, naftilo o un anillo de heteroarilo de 5 a 6 miembros que contiene de uno a cuatro heteroátomos en el anillo seleccionados entre oxígeno, nitrogeno y azufre, con la condicion de que dicho anillo no puede contener dos átomos de oxígeno adyacentes ni dos átomos de azufre adyacentes y en donde cada uno de los anillos antecedentes de fenilo, naftilo y heteroarilo puede estar opcionalmente sustituidos con uno a tres sustituyentes independientemente seleccionados entre hidroxialquilo C1-8, alcoxi C1-8-alquiloC1-8, hidroxi-cicloalquiloC3-8, cicloalcoxi C3-8, alcoxiC1-8-cicloalquiloC3-8, heterocicloalquilo, hidroxiheterocicloalquilo y alcoxiC1-8- heterocicloalquilo, en donde cada uno de dichos restos cicloalquilo C3-8 o heterocicloalquilo puede estar independientemente sustituido con uno a tres grupos alquilo C1-6 o bencilo; cuando B es un anillo de fenilo, naftilo o heteroarilo, cada uno de dichos anillos puede estar opcionalmente sustituido con uno a tres sustituyentes independientemente seleccionados entre fenilo, naftilo y un anillo de heteroarilo de 5 a 6 miembros que contiene de uno a cuatro heteroátomos seleccionados entre oxígeno, nitrogeno y azufre, con la condicion de que dicho anillo de heteroarilo no puede contener dos átomos de oxígeno adyacentes ni dos átomos de azufre adyacentes, y en donde cada sustituyente fenilo, naftilo o heteroarilo independientemente seleccionado puede estar sustituido en sí mismo con uno a tres sustituyentes alquilo C1-8 o cicloalquilo C3-8; o cuando B es un anillo de fenilo, naftilo o heteroarilo, cada uno de dichos anillos puede estar opcionalmente sustituido con uno a tres sustituyentes independientemente seleccionados entre a) una lactona formada a partir de -(CH2)tOH con un orto-COOH, en donde t es uno, dos o tres; b) -CONR14R15, en donde R14 y R15 se seleccionan independientemente entre alquilo C1-8 y bencilo, o R14 y R15 junto con el átomo de nitrogeno al que están unidos forman un anillo de heteroalquilo de 5 a 7 miembros que puede contener de cero a tres heteroátomos seleccionados entre nitrogeno, azufre y oxígeno del átomo de nitrogeno del grupo - CONR14R15, en donde cuando cualquiera de dichos heteroátomos es nitrogeno, puede estar opcionalmente sustituido con alquilo C1-8 o bencilo, con la condicion de que dicho anillo no puede contener dos átomos de oxígeno adyacentes ni dos átomos de azufre adyacentes; c) -(CH2)vNCOR16R17 en donde v es cero, uno, dos o tres y -COR16 y R17 tomados conjuntamente con el átomo de nitrogeno al que están unidos forman un anillo de lactama de 4 a 6 miembros; y d) -(C1-8)-NR18R19 en donde cada uno de R18 y R19 se selecciona, independientemente, entre hidrogeno y alquilo C1-4, o R18 y R19, junto con el átomo de nitrogeno al que está unidos, forman un anillo de heteroalquilo de 4 a 7 miembros que puede contener de cero a cuatro heteroátomos seleccionados entre nitrogeno, azufre y oxígeno; en donde las líneas intermitentes indican enlaces dobles opcionales; y n es 1, 2, o 3; o una sal o isomero optico farmacéuticamente aceptable del mismo.
ARP050101025A 2004-03-17 2005-03-16 Derivados de bencil(ideno)- lactamas. composiciones farmaceuticas AR050403A1 (es)

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ATE521591T1 (de) * 2005-01-13 2011-09-15 Ge Healthcare Ltd 11c-markierte benzyl-lactam-verbindungen und deren verwendung als bildgebungsmittel
CA2612268A1 (en) * 2005-06-17 2006-12-28 Pfizer Products Inc. Metabolites of 1-[6-(1-ethyl-1-hydroxy-propyl)-pyridin-3-yl]-3-[2-(4-methyl-piperazin-1-yl)-benzyl]-pyrrolidin-2-one as seratonin receptor antagonists
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JP2007529495A (ja) 2007-10-25
UY28811A1 (es) 2005-10-31
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US20050245521A1 (en) 2005-11-03
KR20060124770A (ko) 2006-12-05
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CN1934081A (zh) 2007-03-21
CA2559530C (en) 2012-04-24
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AU2005223481A1 (en) 2005-09-29
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CA2559530A1 (en) 2005-09-29
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