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AR086881A1 - Derivados de picolinamida como agonistas del receptor cb2 - Google Patents

Derivados de picolinamida como agonistas del receptor cb2

Info

Publication number
AR086881A1
AR086881A1 ARP120102046A ARP120102046A AR086881A1 AR 086881 A1 AR086881 A1 AR 086881A1 AR P120102046 A ARP120102046 A AR P120102046A AR P120102046 A ARP120102046 A AR P120102046A AR 086881 A1 AR086881 A1 AR 086881A1
Authority
AR
Argentina
Prior art keywords
alkyl
alkoxy
cycloalkyl
oxadiazolyl
peri
Prior art date
Application number
ARP120102046A
Other languages
English (en)
Inventor
Caterina Bissantz
Uwe Grether
Paul Hebeisen
Atsushi Kimbara
Qingping Liu
Matthias Nettekoven
Marco Prunotto
Stephan Roever
Mark Rogers-Evans
Tanja Schulz-Gasch
Christoph Ullmer
Zhiwei Wang
Wulun Yang
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR086881A1 publication Critical patent/AR086881A1/es

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    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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

El compuesto de la fórmula (1) puede utilizarse como medicamento para el tratamiento de enfermedades tales como la aterosclerosis y la isquemia. Se provee también un método para su obtención.Reivindicación 1: Un compuesto de la fórmula (1) en la que: R1 es cicloalquilo, cicloalquilalcoxi, haloalcoxi, alcoxialcoxi, fenilo, halofenilo, haloalquilfenilo, fenilalquilo, halofenilalquilo, fenilhidroxialquilo, feniloxialquilo, fenilalcoxi, alcoxifenilo, halofeniloxi, piperidinilsulfonilo, tetrahidropiranilo, 3-alcoxi-azetidinilo, tetrahidropiranilalquilo, tetrahidropinanil-alcoxi, 1,1-dióxido de tetrahidrotiopiranilo, 1,1-dioxo-[1,2]-tiazinan-4-ilo, piperidin-2-onilo, tetrahidrofuranil-alcoxi, piridinilalcoxi, alquiloxetanilalcoxi, hidroxil-haloalquiloxi, halofenilhidroxialquilo, alquilsulfonilo, alquilsulfanilo o (halo)(haloalquil)fenilo; R2 es hidrógeno, halógeno, alquilo, haloalquilo, hidroxialquilo, cicloalquilo, hidroxicicloalquilo, alcoxi, haloalcoxi, alquilamino, haloalquilamino, tetrahidropiranilo, 1H-pirazolilo, pirrolidinilo, alquilpirrolidinilo, halo-pirrolidinilo, oxopirrolidinilo, haloazetidinilo, hidroxiazetidinilo, 1,1-dioxido-2-isotioazolidinilo, tetrahidrofuranilo, cicloalquilamino, hidroxioxetanilo, alquilsulfonilo, oxetanilo, 6-oxa-1-aza-espiro[3.3]-heptilo, 3,3-difluoro-2-oxo-azetidinilo, oxo-azetidinilo u oxo-pirrolidinilo; o R1 y R2 junto con el anillo al que están unidos forman un tetrahidroquinolinilo o alquiltetrahidroquinolinilo; uno de R3 y R4 es hidrógeno y el otro es -(CR5R6)m(CR7R8)n-R9; o R3 y R4 junto con el átomo de nitrógeno al que están unidos forman un piperidinilo, 1,1-dioxidotetrahidro-2H-tio-piranilo, tiomorfolinilo, 2-oxa-6-aza-espiro[3.3]heptilo o 1-hidroxialquilpirrolidinilo; R5 y R6 se eligen con independencia entre hidrógeno, alquilo, haloalquilo, cicloalquilo, cicloalquilalquilo, fenilo, piridazinilo, halofenilo, pirimidinilo, alquilsulfanilalquilo y alquilsulfonilalquilo; o R5 y R6 junto con el átomo de carbono al que están unidos forman un cicloalquilo, tetrahidropiranilo u oxetanilo; R7 y R8 se eligen con independencia entre hidrógeno, alquilo y cicloalquilo; R9 es alquilo, hidroxilo, ciano, carboxilo, alcoxicarbonilo, alquil[1,2,4]oxadiazolilo, oxazolilo, tiazolilo, [1,3,4]oxadiazolilo, cicloalquilo, fenilo, piridinilo, tetrahidropiranilo, alquil[1,2,4]tiadiazolilo, [1,2,4]-tiadiazolilo, alquilaminocarbonilo, alquiltetrahidropiranilo, alquilisoxazolilo, aminocarbonilo, morfolinilo, dihidrooxazolilo, [1,2,4]oxadiazolilo, hidroxicicloalquilo, alcoxicarbonilcicloalquilo, alcoxialcoxi, hidroxialquilcicloalquilo, alcoxipiridinilo, piperidinilo, hidroxipiperidinilo, hidroxialquilpiperidinilo, isoxazolilo, azetidina-carbonilo, alcoxialquilaminocarbonilo, cicloalquil-alquilaminocarbonilo, haloazetidinilcarbonilo, alquiloxopirrolidinilo, 1,1-dioxo-tetra-hidro-1l6-tiofenilo, 1,1-dioxo-tetrahidro-1l6-tiofenil-amino, amino[1,2,4]oxadiazolilo, 4-alquil-5-oxo-4,5-dihidro-[1,2,4]oxadiazolilo, nitro-benzo[1,2,5]oxadiazolilo, alquilsulfonilo, alquil[1,2,4]tiazolilo, hidroxialquilaminocarbonilo, oxotetrahidrofuranilo, (cicloalquilalquil)(alcoxicarbonil)amino, 2-oxo-[1,3]-oxazinanilo, haloalquilo o hidroxipirrolidinilaminocarbonilo; m es el número 0 ó 1; y n es el número 0, 1 o 2; o una sal o un éster farmacéuticamente aceptables del mismo.
ARP120102046A 2011-06-10 2012-06-08 Derivados de picolinamida como agonistas del receptor cb2 AR086881A1 (es)

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