AR036027A2 - Un compuesto heterociclico substituido, procedimiento y compuestos intermediarios para su preparacion y composicion farmaceutica que contiene a dicho compuesto - Google Patents

Un compuesto heterociclico substituido, procedimiento y compuestos intermediarios para su preparacion y composicion farmaceutica que contiene a dicho compuesto

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Publication number
AR036027A2
AR036027A2 ARP020101908A ARP020101908A AR036027A2 AR 036027 A2 AR036027 A2 AR 036027A2 AR P020101908 A ARP020101908 A AR P020101908A AR P020101908 A ARP020101908 A AR P020101908A AR 036027 A2 AR036027 A2 AR 036027A2
Authority
AR
Argentina
Prior art keywords
alkyl
unsubstituted
substituted
group
hydrogen
Prior art date
Application number
ARP020101908A
Other languages
English (en)
Inventor
Xavier Emonds-Alt
Isabelle Grossriether
Patrick Gueule
Vincenzo Proietto
Didier Van Broeck
Original Assignee
Sanofi Aventis
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from FR9501016A external-priority patent/FR2729952B1/fr
Application filed by Sanofi Aventis filed Critical Sanofi Aventis
Publication of AR036027A2 publication Critical patent/AR036027A2/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
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    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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    • C07C215/22—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated
    • C07C215/28—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings
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    • C07C215/28—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings
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    • C07C233/18—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
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    • C07C255/43—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being further bound to other hetero atoms the carbon skeleton being further substituted by singly-bound oxygen atoms
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Abstract

Un compuesto heterocíclico sustituido de la fórmula (1) en la cual: -A representa un radical bivalente elegido entre: A1) -O-CO-, A2) -CH2-O-CO-, A3) -O-CH2-CO-, A4) -O-CH2-CH2-, A5) -N(R1)-CO-, A6) -N(R1)-CO-CO-, A7) -N(R1)-CH2-CH2-, A8) -O-CH2-, en los cuales R1 representa un hidrógeno o un alquilo C1-4; -m es 2 ó 3; -Ar1 representa un fenilo no sustituido o sustituido una o varias veces por un sustituyente elegido entre: un átomo de halógeno, un hidroxilo, un alcoxi C1-4, un alquilo C1-4, un trifluorometilo, un metilendioxi, los mencionados sustituyentes siendo idénticos o diferentes; un tienilo no sustituido o sustituido por un átomo de halógeno; un benzotienilo no sustituido o sustituido por un átomo de halógeno; un naftilo no sustituido o sustituido por un átomo de halógeno; un indolilo no sustituido o N-sustituido por un alquilo C1-4 o un bencilo; un imidazolilo no sustituido o sustituido por un átomo de halógeno; un piridilo no sustituido o sustituido por un átomo de halógeno; un bifenilo; -T representa un grupo elegido entre: CH2-Z, -CH(C6H5)2, -C(C6H5)3; T puede además representar el grupo -CO-B-Z cuando A representa un radical bivalente elegido entre: -O-CH2-CH2- ó -N(R1)-CH2-CH2- ó -O-CH2-; -B representa un enlace directo o un metileno; -Z representa: -un fenilo no sustituido o sustituido una o varias veces por un sustituyente elegido entre: un átomo de halógeno; un trifluorometilo; un ciano; un hidroxi; un nitro; un fenilo no sustituido o sustituido una o varias veces por un halógeno, un trifluorometilo, un alquilo C1-4, un hidroxi, un alcoxi C1-4, siendo los mencionados sustituyentes idénticos o diferentes; un amino no sustituido o sustituido una o varias veces por alquilo C1-4; un bencilamino; un carboxi; un alquilo C1-10; un cicloalquilo C3-8 no sustituido o sustituido una o varias veces por un metilo; un alcoxi C1-10; un cicloalquiloxi C3-8 no sustituido o sustituido una o varias veces por un metilo; un mercapto; un alquiltio C1-10; un formiloxi; un alquil C1-6-carboniloxi; un formilamino; un alquil C1-6-carbonilamino; un benzoilamino; un alcoxi C1-4-carbonilo; un cicloalquiloxi C3-7-carbonilo; un cicloalquil C3-7-carbonilo; un carbamoilo no sustituido o sustituido una o dos veces por un alquilo C1-4; un ureido no sustituido o sustituido una o dos veces en posición 3 por un alquilo C1-4 o un cicloalquilo C3-7; un (pirrolidin-1-il)carbonilamino, siendo los mencionados sustituyentes idénticos o diferentes; -un 1- ó 2-naftilo; 1-, 2-, 3-, 4-, 5-, 6-, 7-indenilo, de los cuales una o varias uniones pueden ser hidrogenadas, pudiendo estos grupos ser no sustituidoS o contener eventualmente uno o varios sustituyentes tales como: el grupo alquilo, fenilo, ciano, hidroxialquilo, hidroxi, oxo, alquilcarbonilamino, alcoxicarbonilo, tioalquilo, halógeno, alcoxi y trifluorometilo, en los cuales los alquilos están en C1-4; -un grupo piridilo, tiadiazolilo, indolilo, indazolilo, imidazolilo, bencimidazolilo, benzotriazolilo, benzofuranilo, benzotienilo, benzotiazolilo, bencisotiazolilo, quinolilo, isoquinolilo, benzoxazolilo, bencisoxazolilo, benzoxazinilo, benzodioxinilo, isoxazolilo, benzopiranilo, tiazolilo, tienilo, furilo, piranilo, cromenilo, isobenzofuranilo, pirrolilo, pirazolilo, pirazinilo, pirimidinilo, piridazinilo, indolizinilo, ftalazinilo, quinazolinilo, acridinilo, isotiazolilo, isocromanilo, cromanilo, de los cuales uno o varios dobles enlaces pueden ser hidrogenados, pudiendo dichos grupos ser no sustituido o contener eventualmente uno o varios sustituyentes tales como: el grupo alquilo, fenilo, ciano, hidroxialquilo, hidroxi, alquilcarbonilamino, alcoxicarbonilo, tioalquilo en los cuales los alquilos están en C1-4; -Am representa: i- ya sea un grupo Am1, de fórmula (2) en la cual J1 representa i1- ya sea un grupo Ar2-NR2-CH<; Ar2 representa un piridilo; un fenilo no sustituido o sustituido una o varias veces por un sustituyente elegido entre: un átomo de halógeno, un hidroxi, un alcoxi C1-4, un alquilo C1-4, un trifluorometilo, un nitro, un metilendioxi, los mencionados sustituyentes siendo idénticos o diferentes; un tienilo; un pirimidilo; un imidazolilo no sustituido o sustituido por un alquilo C1-4; R2 representa un hidrógeno; un alquilo C1-7; un bencilo; un formilo; un alquil C1-7-carbonilo; i2- sea un grupo Ar2-(CH2)n-CR3< en el cual: -Ar2 es tal como se ha definido anteriormente; -n es 0 ó 1; -R3 representa un grupo elegido entre: (1) hidrógeno; (2) alquilo C1-7; (3) formilo; (4) alquilcarbonilo C1-7; (5) ciano; (6) -(CH2)q-OH; (7) -(CH2)q-O-alquilo C1-7; (8) -(CH2)q-OCHO; (9) -(CH2)q-OCOR17; (10) -(CH2)q-OCONH-alquilo C1-7; (11) -NR4R5; (12) -(CH2)q-NR6C(=W1)R7; (13) -(CH2)q-NR6COOR8; (14) -(CH2)q-NR6SO2R9; (15) -(CH2)q-NR6C(=W1)NR10R11; (16) -CH2-NR12R13; (17) -CH2-CH2-NR12R13; (18) -COOH; (19) alcoxi C1-7-carbonilo; (20) -C(=W1)NR10R11; (21) -CH2-COOH; (22) alcoxi C1-7-carbonilmetilo; (23) -CH2-C(=W1)NR10R11; (24) -O-CH2CH2-OR18; (25) -NR6COCOR19; (26) -CONR20-NR21R22; (27) un grupo de la fórmula (3); (28) un grupo de la fórmula (4); -o R3 constituye un doble enlace entre el átomo de carbono al cual está unido y el átomo de carbono próximo al ciclo de piperidina; -q es 0, 1 ó 2; -W1 representa un átomo de oxígeno o un átomo de azufre; -R4 y R5 representan cada uno independientemente un hidrógeno o un alquilo C1-7; R5 puede además representar un cicloalquil C3-7-metilo, un bencilo o un fenilo; ó R4 y R5 junto con el átomo de nitrógeno al cual están unidos constituyen un heterociclo elegido entre la azetidina, la pirrolidina, la piperidina, la morfolina, la tiomorfolina, la perhidroazepina o la piperazina no sustituida o sustituida en posición 4 por un alquilo C1-4; -R6 representa un hidrógeno o un alquilo C1-7; -R7 representa un hidrógeno, un alquilo C1-7, un vinilo, un fenilo, un bencilo, un piridilo, un cicloalquilo C3-7 no sustituido o sustituido por uno o varios metilos, un furilo, un tienilo, un pirrolilo, un imidazolilo; ó R6 y R7 juntos representan un grupo -(CH2)p-; -p es 3 ó 4; -R8 representa un alquilo C1-7 o un fenilo; -R9 representa un alquilo C1-7, un amino libre o sustituido por uno o dos alquilos C1-7, un fenilo no sustituido o sustituido una o varias veces por un sustituyente elegido entre: un átomo de halógeno, un alquilo C1-7, un trifluorometilo, un hidroxi, un alcoxi C1-7, un carboxi, un alcoxi C1-7-carbonilo, un alquil C1-7-carboniloxi, un ciano, un nitro, un amino libre o sustituido por uno o dos alquilos C1-7, siendo los mencionados sustituyentes idénticos o diferentes; -R10 y R11 representa cada uno independientemente un hidrógeno o un alquilo C1-7; R11 puede además representar un cicloalquilo C3-7, un cicloalquil C3-7-metilo, un hidroxi, un alcoxi C1-4, un bencilo o un fenilo; ó R10 y R11 juntos con el átomo de nitrógeno al cual están unidos constituyen un heterociclo elegido entre la azetidina, la pirrolidina, la piperidina, la morfolina, la tiomorfolina o la perhidroazepina; -R12 y R13 representan cada uno independientemente un hidrógeno o un alquilo C1-7; R13 puede además representar un cicloalquil C3-7-metilo o un bencilo; -R17 representa un alquilo C1-7; un cicloalquil C3-7-metilo no sustituido o sustituido por uno o varios metilos; un piridilo; un fenilo; un piridilo; -R18 representa un hidrógeno, un alquilo C1-7, un formilo, un alquil C1-7-carbonilo; -R19 representa un alcoxi C1-4; -R20 representa un hidrógeno o un alquilo C1-7; -R21 y R22 representan cada uno independientemente un hidrógeno o un alquilo C1-7; -o bien R21 y R22 juntos con el átomo de nitrógeno al cual están unidos constituyen un heterociclo elegido entre la pirrolidina, la piperidina o la morfolina; -R23 representa un hidrógeno o un alquilo C1-7; -R24 y R25 representan cada uno independientemente un hidrógeno o un alquilo C1-7; R25 puede además representar un formilo o un alquil C1-7-carbonilo; i3 - sea un grupo R14R3C< en el cual -R3 es tal como se ha definido anteriormente; -R14 representa un alquilo C1-7, un cicloalquilo C3-7; R14 puede además representar ya sea un grupo -CONR15R16 cuando R3 representa el hidrógeno, ya sea un grupo -NR15R16 cuando R3 representa el hidrógeno, un ciano, un carboxi, un alcoxi C1-4-carbonilo o un grupo -C(=W1)NR10R11; -R15 y R16 representan cada uno independientemente un alquilo C1-7; o R15 y R16 juntos con el átomo de nitrógeno al cual están unidos constituyen un heterociclo elegido entre la azetidina, la pirrolidina, la piperidina, la morfolina, la tiomorfolina o la perhidroazepina; ii- sea un grupo Am2 de fórmula (5) en la cual J2 representa: ii1 - sea un grupo Ar3R2N-CH< en el cual: -Ar3 representa un fenilo no sustituido o sustituido una o varias veces por un sustituyente elegido entre: un átomo de halógeno, un hidroxi, un alcoxi C1-4, un alquilo C1-4, un trifluorometilo, siendo los mencionados sustituyentes idénticos o diferentes; -R2 es tal como se ha definido anteriormente para J1; ii2 - sea un grupo AR3-(CH2)n-CH- en el cual: -Ar3 es tal como se ha definido anteriormente; -n es 0 ó 1; -Q representa un alquilo C1-6 o un bencilo; estando el mencionado sustituyente en posición axial o en posición ecuatorial; -X- es un anión; iii - sea un grupo Am3 de fórmula (6) en la cual: -Ar2 es tal como se ha definido anteriormente, -n es 0 ó 1; -X- representa un anión; iv - sea un grupo Am4 de fórmula (7) en la cual -Ar2 es tal como se ha definido anteriormente; -n es 0 ó 1; -X- representa un anión; con la condición que cuando A es -O-CH2-CH2-, -N(R1)-CH2-CH2- ó -O-CH2-, m es 2, Ar1 es un fenilo no sustituido o sustituido una o varias veces por un sustituyente elegido entre: un átomo de halógeno, un hidroxi, un alcoxi C1-4, un alquilo C1-4, un trifluorometilo, siendo dichos sustituyentes idénticos o diferentes, T es -CO-Za, siendo Za un fenilo no sustituido o sustituido una o varias veces por un sustituyente elegido entre: un átomo de halógeno, un trifluorometilo, un alquilo C1-10, un alcoxi C1-10, un hidroxi, siendo dichos sustituyentes idénticos o diferent
ARP020101908A 1995-01-30 2002-05-23 Un compuesto heterociclico substituido, procedimiento y compuestos intermediarios para su preparacion y composicion farmaceutica que contiene a dicho compuesto AR036027A2 (es)

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FR9508046A FR2729953B1 (fr) 1995-01-30 1995-07-04 Composes heterocycliques substitues, procede pour leur preparation et compositions pharmaceutiques les contenant
FR9513005A FR2729954B1 (fr) 1995-01-30 1995-11-03 Composes heterocycliques substitues, procede pour leur preparation et compositions pharmaceutiques les contenant

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ATE222251T1 (de) 2002-08-15
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NO308795B1 (no) 2000-10-30
ES2243373T3 (es) 2005-12-01
CN1636983A (zh) 2005-07-13
DK0807111T3 (da) 2002-12-16
CN1179954C (zh) 2004-12-15
FI973148L (fi) 1997-09-29
CN1202093C (zh) 2005-05-18
FR2729954A1 (fr) 1996-08-02
EP1156049B1 (fr) 2005-06-01
PT1156049E (pt) 2005-10-31
HUP9800295A3 (en) 2000-02-28
EP1156049A1 (fr) 2001-11-21
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AU4666996A (en) 1996-08-21
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CA2211668A1 (en) 1996-08-08
AR002955A1 (es) 1998-05-27
CN1172483A (zh) 1998-02-04
FI973148A7 (fi) 1997-09-29
EP1688416A1 (fr) 2006-08-09
NO973479D0 (no) 1997-07-29
SI0807111T1 (en) 2003-02-28
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CZ294267B6 (cs) 2004-11-10
CY2537B1 (fr) 2006-06-28
JP3357660B2 (ja) 2002-12-16
PL321640A1 (en) 1997-12-22
WO1996023787A1 (fr) 1996-08-08
CN1394855A (zh) 2003-02-05
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US6242637B1 (en) 2001-06-05
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RU2157807C2 (ru) 2000-10-20
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CA2211668C (en) 2005-09-20
DE69634806T2 (de) 2006-04-27
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US5977359A (en) 1999-11-02
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US5869663A (en) 1999-02-09
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JPH11507324A (ja) 1999-06-29
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