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AR076228A1 - Piperidinas sustituidas como antagonistas de ccr3 - Google Patents

Piperidinas sustituidas como antagonistas de ccr3

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Publication number
AR076228A1
AR076228A1 ARP100101174A ARP100101174A AR076228A1 AR 076228 A1 AR076228 A1 AR 076228A1 AR P100101174 A ARP100101174 A AR P100101174A AR P100101174 A ARP100101174 A AR P100101174A AR 076228 A1 AR076228 A1 AR 076228A1
Authority
AR
Argentina
Prior art keywords
alkyl
optionally substituted
ring
group
alkylene
Prior art date
Application number
ARP100101174A
Other languages
English (en)
Inventor
Matthias Hoffmann
Christoph Hoenke
Riccardo Giovannini
Georg Rast
Peter Seither
Horst Dollinger
Jan Kriegl
Domnic Martyres
Marc Grundl
Original Assignee
Boehringer Ingelheim Int
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
Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of AR076228A1 publication Critical patent/AR076228A1/es

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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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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
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    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
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    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond
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    • C07D417/14—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 three or more hetero rings

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  • Hydrogenated Pyridines (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Proporcionar antagonistas de CCR3, más particularmente proporcionar composiciones farmacéuticas que comprenden un vehículo farmacéuticamente aceptable y una cantidad terapéuticamente eficaz de al menos uno de los compuestos reivindicados o una sal farmacéuticamente aceptable del mismo. Reivindicacion 1: Un compuesto caracterizado porque tiene la formula 1, en la que A es CH2, O o N-alquilo C1-6; R1 se selecciona entre NHR1.1 o NMeR1.1, NHR1.2 o NMeR1.2, NHCH2-R1.3, NH-cicloalquilo C3-6, mientras que, opcionalmente, un átomo de carbono se reemplaza por un átomo de nitrogeno, mientras que el anillo está opcionalmente sustituido con uno o más restos seleccionados entre el grupo que consiste en alquilo C1-6, O-alquilo C1-6, NHSO2-fenilo, NHCONH-fenilo, halogeno, CN, SO2-alquilo C1-6 y COO-alquilo C1-6; un anillo bicíclico C9 o 10, mientras que uno o dos átomos de carbono se reemplazan por átomos de nitrogeno y el sistema anular se une mediante un átomo de nitrogeno a la estructura básica de formula 1 y mientras que el sistema anular está opcionalmente sustituido con uno o más restos seleccionados entre el grupo que consiste en alquilo C1-6, COO-alquilo C1-6, haloalquilo C1-6, O-alquilo C1-6, NO2, halogeno, CN, NHSO2-alquilo C1-6 y metoxifenilo; un grupo seleccionado entre NHCH(piridinil)CH2COO-alquilo C1-6 y NHCH(CH2O-alquil C1-6)-benzoimidazolilo, opcionalmente sustituido con halogeno o CN; o 1-aminociclopentilo, opcionalmente sustituido con metil-oxadiazol; R1.1 es fenilo, opcionalmente sustituido con uno o más restos seleccionados entre el grupo que consiste en alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, alquileno C1-6-OH, alquenileno C2-6-OH, alquinileno C2-6-OH, CH2CON(alquilo C1-6)2, CH2NHCONH-cicloalquilo C3-6, CN, CO-piridinilo, CONR1.1.1R1.1.2, COO-alquilo C1-6, N(SO2-alquilo C1-6)(CH2CON(alquilo C1-4)2) O-alquilo C1-6, O-piridinilo, SO2-alquilo C1-6, SO2-alquileno C1-6-OH, SO2-cicloalquilo C3-6, SO2-piperidinilo, SO2NH-alquilo C1-6, SO2N(alquilo C1-6)2, halogeno, CN, CO-morfolinilo, CH2-piridinilo o un anillo heterocíclico opcionalmente sustituido con uno o más restos seleccionados entre el grupo que consiste en alquilo C1-6, NHalquilo C1-6 y =O; R1.1.1 H, alquilo C1-6, cicloalquilo C3-6, haloalquilo C1-6, CH2CON(alquilo C1-6)2, CH2CO-azetindinilo, alquileno C1-6-cicloalquilo C3-6, CH2-piranilo, CH2-tetrahidrofuranilo, CH2-furanilo, alquileno C1-6-OH o tiadiazolilo, opcionalmente sustituido con alquilo C1-6; R1.1.2 H, alquilo C1-6 o SO2alquilo C1-6; o R1.1.1 y R1.1.2 forman juntos un anillo carbocíclico de cuatro, cinco o seis miembros, que contiene opcionalmente un N u O, que reemplaza un átomo de carbono del anillo, opcionalmente sustituido con uno o más restos seleccionados entre el grupo que consiste en alquilo C1-6, alquileno C1-4-OH, OH y =O; o R1.1 es fenilo, donde dos restos adyacentes forman juntos un anillo carbocíclico, aromático o no aromático, de cinco o seis miembros, que contiene opcional e independientemente de cualquier otro uno o dos N, S o SO2, que reemplaza un átomo de carbono del anillo, donde el anillo está opcionalmente sustituido con alquilo C1-4 o =O; R1.2 se selecciona entre heteroarilo, opcionalmente sustituido con uno o más restos seleccionados entre el grupo que consiste en alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6, CH2COO-alquilo C1-6, CONR1.2.1R1.2.2, COR1.2.3, COO-alquilo C1-6, CONH2, O-alquilo C1-6, halogeno, CN, SO2N(alquilo C1-6)2 o heteroarilo opcionalmente sustituido con uno o más restos seleccionados entre el grupo que consiste en alquilo C1-6, heteroarilo, opcionalmente sustituido con un anillo carbocíclico no aromático de cinco o seis miembros que contiene independientemente de cualquier otro dos N, O, S o SO2, que reemplaza un átomo de carbono del anillo; un anillo bicíclico C9 o 10 aromático o no aromático, mientras que uno o dos átomos de carbono se reemplazan por N, O o S, cada uno opcionalmente sustituido con uno o más restos seleccionados entre el grupo que consiste en N(alquilo C1-6)2, CONH-alquilo C1-6 y =O; un anillo heterocíclico no aromático, opcionalmente sustituido con piridinilo; 4,5-dihidro-nafto[2,1-d]tiazol, opcionalmente sustituido con NHCO-alquilo C1-6, R1.2.1 H, alquilo C1-6, alquileno C1-6-cicloalquilo C3-6, alquileno C1-4-fenilo, alquileno C1-4-furanilo, cicloalquilo C3-6, alquileno C1-4-O-alquilo C1-4, haloalquilo C1-6 o un anillo carbocíclico no aromático de cinco o seis miembros, que contiene opcional e independientemente de cualquier otro uno o dos N, O, S o SO2, que reemplaza un átomo de carbono del anillo, opcionalmente sustituido con 4-ciclopropilmetil-piperazinilo; R1.2.2 H o alquilo C1-6; R1.2.3 un anillo carbocíclico no aromático de cinco o seis miembros, que contiene opcional e independientemente de cualquier otro uno o dos N, O, S o SO2, que reemplaza un átomo de carbono del anillo; R1.3 se selecciona entre fenilo, heteroarilo o indolilo, cada uno opcionalmente sustituido con uno o más restos seleccionados entre el grupo que consiste en alquilo C1-6, cicloalquilo C3-6, O-alquilo C1-6, O-haloalquilo C1-6, fenilo y heteroarilo; R2 se selecciona entre el grupo que consiste en alquileno C1-6-fenilo, alquileno C1-6-naftilo y alquileno C1-6-heteroarilo; cada uno opcionalmente sustituido con uno, dos o tres restos seleccionados entre el grupo que consiste en alquilo C1-6, haloalquilo C1-6, O-alquilo C1-6, O-haloalquilo C1-6 y halogeno; R3 es H o alquilo C1-6; R4 es H o alquilo C1-6 o R3 y R4 forman juntos un grupo CH2-CH2.
ARP100101174A 2009-04-08 2010-04-07 Piperidinas sustituidas como antagonistas de ccr3 AR076228A1 (es)

Applications Claiming Priority (2)

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EP09157653 2009-04-08
EP09174917 2009-11-03

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AR076228A1 true AR076228A1 (es) 2011-05-26

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UY32547A (es) 2010-11-30
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