AR068935A1 - Derivados heterociclicos de piridina, pirimidina y piridazina oxo-sustituidas, inhibidores de quinasas - Google Patents

Derivados heterociclicos de piridina, pirimidina y piridazina oxo-sustituidas, inhibidores de quinasas

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Publication number
AR068935A1
AR068935A1 ARP080104569A ARP080104569A AR068935A1 AR 068935 A1 AR068935 A1 AR 068935A1 AR P080104569 A ARP080104569 A AR P080104569A AR P080104569 A ARP080104569 A AR P080104569A AR 068935 A1 AR068935 A1 AR 068935A1
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Argentina
Prior art keywords
alkyl
hydrogen
alkoxy
halogen
phenyl
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ARP080104569A
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English (en)
Inventor
Yan Lou
Tobias Gabriel
Nolan James Dewdney
Rama K Kondru
Michael Soth
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Hoffmann La Roche
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Publication of AR068935A1 publication Critical patent/AR068935A1/es

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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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    • C07D401/12—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 chain containing hetero atoms as chain links
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Abstract

Los compuestos son utiles además para tratar enfermedades inflamatorias y autoinmunes asociadas con la proliferacion aberrante de células B, como es la artritis reumatoide. Se describen también composiciones farmacéuticas que contienen los compuestos de la formula 1 y por lo menos un vehículo, diluyente o excipiente. Reivindicacion 1: Un compuesto dé la formula 1, en la que: en la que X1 es CH o N; R1 es C(=O)NHR6, fenilo o heteroarilo, dicho heteroarilo se elige entre el grupo formado por piridinilo, piridazinilo, pirimidinilo, pirazinilo; pirrolilo, furanilo, tiofenilo, imidazolilo, pirazolilo, oxazolilo, tiazolilo, isoxazolilo, isotiazolilo, 2-(alquilo C1-6)-piridazin-3-on-6-ilo, 2-bencil-piridazin-3-on-6-ilo, 1,4,5,6-tetra-hidro-pirimidin-2-ilo y 4,5-dihidro-1H-imidazol-ilo, con la condicion de que cuando X1 es CH, R1 sea C(=O)NHR6 o R3 sea CH2OH; dichos fenilo y heteroarilo están opcionalmente sustituidos con independencia de una a tres veces por restos elegidos entre el grupo formado por halogeno, alquilo C1-6, alcoxi C1-6, heteroalquilo C1-6, heteroalcoxi C1-6, alquilsulfanilo C1-6, alquilsulfonilo C1-6, heteroalquilsulfonilo C1-6 y heterociclil-alcoxi C1-6, dicho heterociclilo es azetidinilo, pirrolidinilo o piperidinilo, CONRaRb, CO2Rg, SO2NRaRb, NRaRb, NHSO2R7 o NHCOR7 en el que R6 es hidrogeno, alquilo C1-6, haloalquilo C1-6, heteroalquilo C1-6, cicloalquilo C3-6, piridinil-alquilo C1-3, fenilo o fenil-alquilo C1-3, dicho fenilo está opcionalmente sustituido por alquilo C1-6, alcoxi C1-6, heteroalcoxi C1-6, halogeno, CONRaRb o CO2Rg; Ra y Rb (i) se eligen con independencia entre hidrogeno, alquilo C1-6, heteroalquilo C1-6, (alcoxi C1-3) -alquilo C1-3, carboxi-alquilo C1-3, cicloalquilo C3-6 o heterociclilo; (ii) juntos son (CH2)mX2(CH2)2, en el que m es el numero 2 o 3 y es O, S(O)n o NR8 y n es un numero de cero a dos y R8 es hidrogeno, alquilo C1-6, hidroxialquilo C1-6 o acilo C1-3; o (iii) junto con el átomo de nitrogeno al que están unidos son piperidinilo o pirrolidinilo, dichos piperidinilo o pirrolidinilo están opcionalmente sustituidos por hidroxi, alcoxi C1-3, hidroxialquilo C1-3; Rg es hidrogeno o alquilo C1-6; R7 es alquilo C1-6 o heteroalquilo C1-6; R2 es hidrogeno o alquilo C1-6; R3 y R4 son con independencia hidrogeno, halogeno, amino, hidroxialquilo C1-6, alquilo C1-6 o ciclopropilo; R5 es (i) fenilo, (ii) heteroarilo elegido entre el grupo formado por piridinilo, benzo[b)tiofen-2-ilo, 4,5,6,7-tetrahidro-benzo[b]tiofen-2-ilo, tiofenilo,1',2',3',4',5',6'-hexahidro-[2,4']bipiridin-5-ilo y (alquil C1-3)-indolilo opcionalmente sustituido por uno o dos alquilo C1-6 o halogeno; (iii) azetidin-1-ilo, pirrolidin-2-ilo, piperidin-1-ilo, azepan-1-ilo o 2,3-dihidro-1H-isoindolin-2-ilo, o 6,7- dihidro-5H-pirrolo[3,4-b]piridina; (iv) NRcRd, en el que Rc y Rd juntos son (CH2)oX2(CR2)p, en el que o y p son con independencia el numero 1 o 2, y X2 tiene el significado definido anteriormente, o Rc y Rd con independencia son hidrogeno, alquilo C1-10 o hidroxialquilo C1-10; formulas (2) (3) y (4) en los que R9 es hidrogeno, halogeno o alquilo C1-6; dichos anillos fenilo, heteroarilo, azetidin-1-ilo, pirrolidin-2-ilo, piperidin-1-ilo, azepan-1-ilo o 2,3-dihidro-1H-isoindolin-2-ilo están opcionalmente sustituidos de una a tres veces por restos elegidos con independencia entre el grupo formado por (a) halogeno, (b) alquilo C1-6, (b) alquenilo C2-6, (c) alquinilo C2-6, (d) haloalquilo C1-6, (e) heteroalquilo C1-6, (f) cicloalquilo C3-7 opcionalmente sustituido de una a tres veces por restos elegidos entre alquilo C1-6, haloalquilo C1-6 y halogeno, (g) (alcoxi C1-6)-alquilo, (h) hidroxi, (i) NReRf, en el que Re y Rf son (i) con independencia hidrogeno, alquilo C1-6 o (ii) juntos son (CH2)mX3(CH2)2, en el que m es el numero 2 o 3 y X3 es CH2, O, S(O)n o NR8 y n es un numero de cero a dos y R8 tiene el significado definido anteriormente; (j) alcoxi C1-6, (k) trialquilsililo, (1) cianoalquilo C1-6 y (m) SF5; A es -NHC(=O)-, C(=O)NH-, NHC(=O)NH, CH2C(=O), CH2SO2, o si R5 es (2) o (3), A está ausente; o una sal farmacéuticamente aceptable del mismo.
ARP080104569A 2007-10-23 2008-10-20 Derivados heterociclicos de piridina, pirimidina y piridazina oxo-sustituidas, inhibidores de quinasas AR068935A1 (es)

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AR (1) AR068935A1 (es)
CA (2) CA2909988A1 (es)
CL (1) CL2008003119A1 (es)
ES (2) ES2499017T3 (es)
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