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AR031364A1 - Agonistas del receptor adrenergico beta-2, una composicion farmaceutica, uso de dichos agonistas para la manufactura de un medicamento, un metodo para identificar compuestos de ligando multimerico que poseen propiedades de enlace multimerico, y un centro de compuestos de ligando multimerico que pose - Google Patents

Agonistas del receptor adrenergico beta-2, una composicion farmaceutica, uso de dichos agonistas para la manufactura de un medicamento, un metodo para identificar compuestos de ligando multimerico que poseen propiedades de enlace multimerico, y un centro de compuestos de ligando multimerico que pose

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Publication number
AR031364A1
AR031364A1 ARP990102698A ARP990102698A AR031364A1 AR 031364 A1 AR031364 A1 AR 031364A1 AR P990102698 A ARP990102698 A AR P990102698A AR P990102698 A ARP990102698 A AR P990102698A AR 031364 A1 AR031364 A1 AR 031364A1
Authority
AR
Argentina
Prior art keywords
substituted
group
multimeric
ligand
alkyl
Prior art date
Application number
ARP990102698A
Other languages
English (en)
Original Assignee
Advanced Medicine Inc
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 Advanced Medicine Inc filed Critical Advanced Medicine Inc
Publication of AR031364A1 publication Critical patent/AR031364A1/es

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    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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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Abstract

Agonistas del receptor adrenérgico b, que comprenden un compuesto de enlace multiple de la formula (1): (L)p (X)q, en la cual p es un numero entero desde 2 hasta 10; q es un numero entero desde 1 hasta 20; L es un ligando en el cual: Uno de los ligando, L, es un compuesto de la formula (2), en la cual Ar1 es seleccionado del grupo que consiste de arilo, heteroarilo, cicloalquilo, cicloalquilo sustituido, y heterociclilo donde cada uno de los sustituyentes mencionados Ar1 y Ar2 opcionalmente forma el enlace entre el ligando y un agente de union; R1 es seleccionado del grupo que consiste de hidrogeno, alquilo y alquilo sustituido, o R1 es una union covalente que une el ligando con un agente de union; R2 y R3 independientemente son seleccionados del grupo que consiste de hidrogeno, alquilo, acilo y alquilo sustituido, o R2 y R3 son uniones covalentes uniendo el ligando con un agente de union; y los otros ligandos son seleccionados independientemente de un compuesto de la formula -Q-Ar2, donde Ar2 es seleccionado del grupo que consiste de arilo, heteroarilo, cicloalquilo, cicloalquilo sustituido y heterociclilo; Q es una union covalente, o un grupo de alquileno sustituido donde uno o más átomos de carbono en dicho grupo de alquileno sustituido son opcionalmente reemplazados por un sustituyente seleccionado entre ûNRa- (donde Ra es hidrogeno, alquilo, acilo, o una union covalente que une el ligando con un agente de union), -O-, -S(O)n (donde n es un numero entero desde 0 hasta 2), -CO-, -PRb- (donde Rb es alquilo), -P(O)2-, y -O-P(O)O- y une el ligando con un agente de union. Cada agente de union, X, en el compuesto de enlaces multiples de la Formula (1), independientemente tiene la formula: -Xa-Z-(Ya-Z)m-Xa-, donde m es un numero entero desde 0 hasta 20; Xa en cada ocurrencia separada es seleccionado del grupo que consiste de -O-, -S-, -NR-, -C(O)-, -C(O)O-, -C(O)NR-, -NRC(O)-, -C(S)=, -C(S)NR-, -NRC(S)-, o una union covalente donde R es definido como sigue: Z en cada ocurrencia separada es seleccionada del grupo que consiste de alquileno, alquileno sustituido, alquenileno, alquenileno sustituido, alquinileno, alquinileno sustituido, o una union covalente; cada Ya en cada ocurrencia separada es seleccionado del grupo que consiste de -O-, C(O)-, -OC(O)-, -NR-, -S(O)n, -C(O)NR' -NR'C(O)-, -NR'C(O)NR', -NR'C(S)NR'-, -C(=NR')-NR'-, -NR'-C(=NR')-, -OC(O)-NR'-, -NR'-C(O)-O-, -N=C(Xa)-NR'-, -NR'-C(Xa)=N-, -P(O)(OR')-O-, -O-P(O)(OR')-, -S(O)nCR'R''-, -S(O)n-NR'-, -NR'-S(O)n-, y una union covalente; donde n es 0, 1 o 2; y R, R', y R'' en cada ocurrencia separada es seleccionado del grupo que consiste de hidrogeno, alquilo, alquilo sustituido, cicloalquilo, cicloalquilo sustituido, alquenilo, alquenilo sustituido, cicloalquenilo, cicloalquenilo sustituido, alquinilo, alquinilo sustituido, arilo, heteroarilo, y heterocíclico a condicion de que Xa, Xa, y Z no son uniones covalentes al mismo tiempo; y sales farmacéuticamente aceptables de éstos a condicion de que: i) cuando Q es un grupo de 2-hidroxietilamino entonces el agente de union no es alquileno o -C(O)-alquileno-C(O)-; ii) cuando Q, Xa y Ya son uniones covalentes entonces Z no puede ser alquileno y por lo tanto son utiles en el tratamiento y prevencion de enfermedades respiratorias como por ejemplo asma, bronquitis, y otras similares. Estos compuestos también son utiles en el tratamiento de lesiones del sistema nervioso y parto prematuro. Además se describe agonistas del receptor adrenérgico b-2, una composicion farmacéutica, uso de dichos agonistas para la manufactura de un medicamento, un método para identificar compuestos de ligando multimérico que poseen propiedades de enlace multimérico, un centro de compuestos de ligando multimérico que posee propiedades multivalentes y un método iterativo para identificar los compuestos de ligando multimérico.
ARP990102698A 1998-06-08 1999-06-08 Agonistas del receptor adrenergico beta-2, una composicion farmaceutica, uso de dichos agonistas para la manufactura de un medicamento, un metodo para identificar compuestos de ligando multimerico que poseen propiedades de enlace multimerico, y un centro de compuestos de ligando multimerico que pose AR031364A1 (es)

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US9293898P 1998-07-15 1998-07-15

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ARP990102699A AR031973A1 (es) 1998-06-08 1999-06-08 Agonistas de los receptores beta2-adrenergicos, una composicion farmaceutica, y uso de dichos agonistas para la manufactura de un medicamento
ARP990102702A AR019628A1 (es) 1998-06-08 1999-06-08 Metodo para identificar nuevos agentes multimericos que modulan receptores.
ARP990102706A AR019630A1 (es) 1998-06-08 1999-06-08 Agentes multiaglutinantes que modulan receptores ppar gama y rxr
ARP990102698A AR031364A1 (es) 1998-06-08 1999-06-08 Agonistas del receptor adrenergico beta-2, una composicion farmaceutica, uso de dichos agonistas para la manufactura de un medicamento, un metodo para identificar compuestos de ligando multimerico que poseen propiedades de enlace multimerico, y un centro de compuestos de ligando multimerico que pose
ARP990102697A AR030142A1 (es) 1998-06-08 1999-06-08 Agonistas de los receptores beta2-adrenergicos, una composicion farmaceutica, uso de dichos agonistas para la manufactura de un medicamento, un metodo para la identificacion de compuestos con ligandos multimericos que poseen propiedades de multiple ligamiento, una biblioteca de compuestos con ligand

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ARP990102699A AR031973A1 (es) 1998-06-08 1999-06-08 Agonistas de los receptores beta2-adrenergicos, una composicion farmaceutica, y uso de dichos agonistas para la manufactura de un medicamento
ARP990102702A AR019628A1 (es) 1998-06-08 1999-06-08 Metodo para identificar nuevos agentes multimericos que modulan receptores.
ARP990102706A AR019630A1 (es) 1998-06-08 1999-06-08 Agentes multiaglutinantes que modulan receptores ppar gama y rxr

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