AR064889A1 - Derivados de piridopirimidinas, un metodo para su preparacion, una composicion y un producto farmaceutico que los comprenden y su uso en la fabricacion de un medicamento para el tratamiento de enfermedades mediadas por pde-4 - Google Patents

Derivados de piridopirimidinas, un metodo para su preparacion, una composicion y un producto farmaceutico que los comprenden y su uso en la fabricacion de un medicamento para el tratamiento de enfermedades mediadas por pde-4

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Publication number
AR064889A1
AR064889A1 ARP080100155A ARP080100155A AR064889A1 AR 064889 A1 AR064889 A1 AR 064889A1 AR P080100155 A ARP080100155 A AR P080100155A AR P080100155 A ARP080100155 A AR P080100155A AR 064889 A1 AR064889 A1 AR 064889A1
Authority
AR
Argentina
Prior art keywords
alkyl
heteroaryl
alkoxy
aryl
optionally substituted
Prior art date
Application number
ARP080100155A
Other languages
English (en)
Inventor
Mark Dickinson
Rhona Cox
Patrick Bonneel
Sousa Simon De
Austen Pimm
Hitesh Jayantilal Sanganee
Premji Meghani
Fraser Hunt
Frank Burkamp
Original Assignee
Astrazeneca Ab
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 Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of AR064889A1 publication Critical patent/AR064889A1/es

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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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Abstract

Un compuesto derivado de 2,4-dioxo-1,4-dihidropirido[2,3-d]pirimidin-3(2H)sustituido, un proceso para preparar ducho compuesto; y el uso de dicho compuesto en el tratamiento de un estado de enfermedad mediado por PDE4. Reivindicacion 1: Un compuesto caracterizado porque responde a la formula (1): en el cual: A es N o CA1; E es N o CE1; W es (CH2)n; Y es (CH2)p; n y p son independientemente 0 o 1; R1 es arilo o heteroarilo cada uno de los cuales se sustituye con uno o más de CO2H, arilo, heteroarilo, (C1-6 alquil)NR39R40, C(O)NHarilo, C(O)N(C1-6 alquil)(aril(C1-6 alquilo)), C(O)NHheteroarilo, C(O)NHheterociclilo, C(O)NH(CH2)vNH2, C(O)NH(CH2)vNHCO2(C1-6 alquilo), C(O)NH((C1-4 alquil)arilo), C(O)N(C1-4 alquil)((C1-4 alquil)arilo), (C1-6 alquil)NHC(O)(C1-6 alcoxi), heterociclil(C1-4 alcoxi), CH=CH(arilo), C.C(arilo), aril(C1-4 alquilo), heteroaril(C1-4 alquilo), ariloxi, heteroariloxi, ariltio, heteroariltio, CH=CH(heteroarilo) o C.C(heteroarilo); y cada uno de los cuales puede estar sustituido opcionalmente con halogeno, ciano, hidroxi, C1-4 alquilo, C1-4 alcoxi, CF3, OCF3, C1-4 alquiltio, S(O)(C1-4 alquilo), S(O)2(C1-4 alquilo) o CO2(C1-4 alquilo); o R1 es aril(C1-4 alquilo) o heteroaril(C1-4 alquilo) cada uno de los cuales está sustituido optativamente con halogeno, ciano, hidroxi, C1-4 alquilo, C1-4 alcoxi, CF3, OCF3, C1-4 alquiltio, S(O)(C1-4 alquilo), S(O)2(C1-4 alquilo), CO2H, CO2(C1-4 alquilo), C(O)NHarilo, C(O)NH(CH2)NH2, C(O)NH(CH2)vNHCO2(C1-6 alquilo), arilo, heteroarilo, CH=CH(arilo), C.C(arilo), CH=CH(heteroarilo) o C.C(heteroarilo); o R1 es C5-7 cicloalquilo sustituido optativamente con hidroxi, C1-4 alquilo, CO2H, CO2(C1-4 alquilo), arilo o heteroarilo; o R1 es C1-10 alquilo; o R1 es C1-6 alquilo sustituido con NR47R48; o R1 es heterociclilo sustituida optativamente con C1-6 alquilo, arilo o heteroarilo; con la condicion de que R1 no es: (2) en el cual: X es S, S(O)o S(O)2 y m es 0 o 1; donde los sustituyentes arilo o heteroarilo de R1 están opcionalmente sustituidos con halogeno, ciano, hidroxi, SH, C1-4 alquilo, C1-4 alcoxi, CF3, OCF3, C(O)H, C1-6 alquiltio, S(O)(C1-6 alquilo), S(O)2(C1-6 alquilo), CO2H, CO2(C1-6 alquilo), NR41R42, C1-6 alquilo (sustituido optativamente con halogeno, OH, CO2H, NR29R30, NHC(O)O(C1-6 alquilo), OS(O)2(C1-6 alquilo) o heterociclilo), C1-6 alcoxi (sustituido optativamente con halogeno, OH, CO2H, NR35R36 o heterociclilo), C3-6 cicloalquilo (halogeno, OH, CO2H, NR37R38 o heterociclilo opcionalmente sustituido) o heterociclilo; v es 1, 2, 3 o 4; R2 es NR50C(O)R3 o NR4R5; R3 es alquilo {sustituido optativamente con hidroxilo, alcoxi, NR7R8, heterociclilo {sustituido optativamente con oxo, hidroxi, C1-6 alquilo, CO2(C1-6 alquilo), arilo, heteroarilo, aril(C1-4 alquilo), heterociclilo o C(O)(C1-4 alquil)fenilo}, arilo, heteroarilo, C3-7 cicloalquilo, C3-7 cicloalquil(C1-4 alquilo), CO2H, CO2(C1-6 alquilo), aril(C1-4 alcoxi), aril(C1-4 alquiltio), S(O)2(C1-6 alquilo), NHC(O)heteroarilo o NHC(O)R6}, C1-6 alcoxi, C3-6 cicloalquilo {sustituido optativamente con hidroxilo, NR43R44 o C1-6 alquilo), heterociclilo {sustituido optativamente con oxo, hidroxi, C1-6 alquilo, amino, arilo, heteroarilo, aril(C1-4 alquilo), heteroaril(C1-4 alquilo), heterociclilo o C(O)(C1-4 alquil)fenilo}, aril(C1-4 alquilo) {sustituido con amino(C1-4 alquilo)}, arilo o heteroarilo; R4 es hidrogeno, C1-6 alquilo (sustituido optativamente con arilo o heteroarilo), arilo o heteroarilo; R5 es hidrogeno, C1-6 alquilo (sustituido optativamente con hidroxilo, C1-6 alcoxi, arilo, ariloxi, fenil(C1-6 alcoxi), heteroarilo, C3-10 cicloalquilo, CO2H, CO2(C1-6 alquilo), NHC(O)O(C1-6 alquilo) o NHC(O)R6), C1-6 alcoxi, C3- 6 cicloalquilo (sustituido optativamente con hidroxi, C1-6 alquilo, fenilo, fenil(C1-6 alquilo), heteroarilo o heteroaril(C1-6 alquilo)), heterociclilo (sustituido optativamente con alquilo, C(O)NH2 o fenil(C1-6 alquilo)), arilo o heteroarilo; R6 es alquilo o fenilo; R7 y R8 son, independientemente, hidrogeno, C1-6 alquilo o fenil(C1-4 alquilo); las siguientes porciones fenilo, arilo y heteroarilo de R3, R4, R5, R6, R7 y R8 se sustituyen opcionalmente, independientemente, con: halogeno, ciano, nitro, hidroxi, S(O)qR9, OC(O)NR10R11, NR12R13, NR14C(O)R15, NR16C(O)NR17R18, S(O)2NR19R20, NR21S(O)2R22, C(O)NR23R24, C(O)R25, CO2R26, NR27CO2R28, OC(O)(C1-6 alquilo), C1-6 alquilo, C1-6 hidroxialquilo, C1-6 haloalquilo, C1-6 alcoxi(C1-6)alquilo, amino(C1-6 alquilo), di(C1-6)alquilamino(C1-6)alquilo, C1-6 alcoxi, C1-6 haloalcoxi, hidroxil(C1-6 alcoxi), heterociclil(C1-6 alcoxi), C1-6 alcoxi(C1-6)alcoxi, amino(C1-4 alcoxi), C1-4 alquilamino(C1-4 alcoxi) (el mismo sustituido opcionalmente con fenilo), di(C1-4 alquil)amino(C1-4 alcoxi), C1-6 alquiltio, C2-6 alquenilo, C2-6 alquinilo, C3-10 cicloalquilo (el mismo sustituido opcionalmente con C1-4 alquilo o oxo), metilendioxi, difluorometilendioxi, heterociclilo, heterocicIil(C1-4 alquilo), fenilo, fenil(C1-4)alquilo, fenoxi, feniltio, fenil(C1-4)alcoxi, heteroarilo, heteroaril(C1-4)alquilo, heteroariloxi o heteroaril(C1-4)alcoxi; donde cualquiera de las porciones fenilo y heteroarilo inmediatamente a continuacion se sustituyen opcionalmente con halogeno, hidroxi, nitro, S(O)r(C1-4 alquilo), S(O)2NH2, S(O)2NH(C1-4 alquilo), S(O)2N(C1-4 alquilo)2, ciano, C1-4 alquilo, C1-4 alcoxi, C(O)NH2, C(O)NH(C1-4 alquilo), C(O)N(C1-4 alquilo)2, CO2H, CO2(C1-4 alquilo), NHC(O)(C1-4 alquilo), NHS(O)2(C1-4 alquilo), C(O)(C1-4 alquilo), CF3 o OCF3; A1, E1 y G1 son, independientemente, hidrogeno, halogeno, ciano, hidroxi, C1-4 alquilo, C1-4 alcoxi, CF3 o OCF3; q y r son, independientemente, 0, 1 o 2; excepto que se especifique lo contrario, el heterociclilo está sustituido optativamente con OH, C1-6 alquilo, C3-7 cicloalquilo, NR31R32, (C1-6 alquil)OH o (C1-6 alquil)NR33R34, NR49CO2(C1-6 alquilo), CO2(C1-6 alquilo), C(O)2(C1-6 alquilo), C(O)heterociclilo, heteroarilo, (C1-6 alquil)C(O)NR53R54, (C1-6 alquil)C(O)NR55R56, (C1-6 alquil)C(O)heterociclilo o heterociclilo; R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, P21, R22, R23, R24, R25, R26, R27 y R28 son, independientemente, C1-6 alquilo {sustituido optativamente con halogeno, hidroxi o C1-6 alcoxi}, CH2(C2-6 alquenilo), fenilo {el mismo sustituido opcionalmente con halogeno, hidroxi, nitro, NH2, NH(C1-4 alquilo), N(C1-4 alquil)2, S(O)2(C1-4 alquilo), S(O)2NH2, S(O)2NH(C1-4 alquilo), S(O)2N(C1- 4 alquil)2, ciano, C1-4 alquilo, C1-4 alcoxi, C(O)NH2, C(O)NH(C1-4 alquilo), C(O)N(C1-4 alquil)2, CO2H, CO2(C1-4 alquilo), NHC(O)(C1-4 alquilo), NHS(O)2(C1-4 alquilo), C(O)(C1-4 alquilo), CF3 o OCF3} o heteroarilo {el mismo sustituido opcionalmente con halogeno, hidroxi, nitro, NH2, NH(C1-4 alquilo), N(C1-4 alquil)2, S(O)2(C1-4 alquilo), S(O)2NH2, S(O)2NH(C1-4 alquilo), S(O)2N(C1-4 alquil)2, ciano, C1-4 alquilo, C1-4 alcoxi, C(O)NH2, C(O)NH(C1-4 alquilo), C(O)N(C1-4 alquil)2, CO2H, CO2(C1-4 alquilo), NHC(O)(C1-4 alquilo), NHS(O)2(C1-4 alquilo), C(O)(C1-4 alquilo), CF3 o OCF3}; R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21, R22, R23, R24, R25, R26, R27 y R28 también pueden ser hidrogeno; R50 es hidrogeno o C1-6 alquilo (sustituido optativamente con NR51R52); R30, R32, R34, R36, R38, R40, R42, R44 o R48 son, independientemente, hidrogeno, C1-6 alquilo (sustituido optativamente con hidroxi, C1-6 alcoxi, C1-6 alquiltio, C3-7 cicloalquilo (sustituido optativamente con hidroxi) o NR45R46), C3-7 cicloalquilo (sustituido optativamente con hidroxi(C1-6 alquil)) o heterociclilo (sustituido optativamente con C1-6 alquilo); R29, R31, R33, R35, R37, R39, R41, R43, R45, R46, R47, R49, R51, R52, R53, R54, R55 y R56 son, independientemente, hidrogeno o C1-6 alquilo; o un N-oxido del mismo; o una sal aceptable para uso farmacéutico del mismo. Reivindicacion 9: Un proceso para preparar un compuesto de la formula (1) de acuerdo con la cláusula 1, caracterizado porque dicho proceso comprende: a) cuando R2 es NHC(O)R3, eliminar el grupo protector Boc de un compuesto de la formula (2): donde R1, G1, E, A, Y y W tienen los valores definidos en la cláusula 1, y hacer reaccionar el producto así formado con un ácido o un derivado ácido de la formula LG-R3 donde R3 tiene los valores definidos en la formula (1) y LG es un grupo saliente. b) cuando R' más abajo es un sustituyente en un grupo fenilo de R1, realizar el siguiente acoplamiento con un ácido R3C(O)OH o un derivado apropiado del mismo (3) o c) realizar la siguiente reaccion de cierre del anillo (4); usando un método conocido en el arte.
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