AR060046A1 - Derivados de 2, 4-dioxo-1, 4-dihidropirido[2, 3 -d]pirimidina, un proceso para prepararlos e intermediario para su sintesis, una composicion farmaceutica que los comprende y su uso en la fabricacion de un medicamento para el tratamiento de enfermedades mediadas por pde4 - Google Patents

Derivados de 2, 4-dioxo-1, 4-dihidropirido[2, 3 -d]pirimidina, un proceso para prepararlos e intermediario para su sintesis, una composicion farmaceutica que los comprende y su uso en la fabricacion de un medicamento para el tratamiento de enfermedades mediadas por pde4

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Publication number
AR060046A1
AR060046A1 ARP070101162A ARP070101162A AR060046A1 AR 060046 A1 AR060046 A1 AR 060046A1 AR P070101162 A ARP070101162 A AR P070101162A AR P070101162 A ARP070101162 A AR P070101162A AR 060046 A1 AR060046 A1 AR 060046A1
Authority
AR
Argentina
Prior art keywords
alkyl
alkoxy
optionally substituted
phenyl
heteroaryl
Prior art date
Application number
ARP070101162A
Other languages
English (en)
Inventor
Grigorios Nikitidis
Peter Sjoe
Rupert Austin
Roger Bonnert
Fraser Hunt
Hitesh Sanganee
Dan Warner
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=38522713&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR060046(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of AR060046A1 publication Critical patent/AR060046A1/es

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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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Abstract

Un proceso para preparar dicho compuesto, composicion farmacéutica que lo comprende y el uso de un compuesto en el tratamiento de un estado de enfermedad mediado por PDE4. Reivindicacion 1: Un compuesto caracterizado porque responde a la formula (1), donde: X es S, S(O) o S(O)2; E es N o CE1; T es C(O) o S(O)2; W es (CH2)n; Y es (CH2)p; n y p son, en forma independiente 0 o 1; m es 0 o 1; L es CH o N; cuando L es CH entonces J es NH; y cuando L es N entonces J está ausente y T está unido directamente a L; R1 es alquilo C1-10 (opcionalmente sustituido con halogeno, hidroxilo, ciano, alcoxi C1-6, alquiltio C1-6, alcoxi C1-6(alcoxi C1-6), arilo, heteroarilo, ariloxi, heteroariloxi, ariltio, heteroariltio, aril(alcoxi C1-4), aril(alquiltio C1-4), cicloalquilo C3-7 (opcionalmente sustituido con alquilo C1-4), CO2H, CO2(alquilo C1-6), NHC(O)R3, tetrahidropiranilo, C(O)NR24R25, S(O)2R26 o NHS(O)2R27), alcoxi C1-6, alquenilo C2-4 (opcionalmente sustituido con fenilo), cicloalquilo C3-6 (opcionalmente sustituido con hidroxilo, halogeno, alquilo C1-6, alcoxi C1-6 o fenilo), heterociclilo (opcionalmente sustituido con oxo, hidroxi, alquilo C1-6, S(O)2(alquilo C1-4), C(O)(alquilo C1-4), arilo, heteroarilo, aril(alquilo C1-4), C(O)heteroarilo o heterociclilo), arilo o heteroarilo; R3 es alquilo C1-6 o fenilo; dichas porciones fenilo, arilo o heteroarilo de R1 y R3 están opcionalmente sustituidas en forma independiente con halogeno, ciano, nitro, hidroxi, S(O)qR4, OC(O)NR5R6, NR7R8, NR9C(O)R10, NR11C(O)NR12R13, S(O)2NR14R15, NR16S(O)2R17, C(O)NR18R19, C(O)R20, CO2R21, NR22CO2R23, alquilo C1-10, hidroxialquilo C1-6, haloalquilo C1-6, alcoxi C1-6-alquilo C1-6, alquil C1-6(S(O)2(alquilo C1-4)), dialquilamino C1-6-alquilo C1-6, alcoxi C1-6, haloalcoxi C1-6, alcoxi C1-6-alcoxi C1-6, alquiltio C1-6, alquenilo C2-6, alquinilo C2-6 (opcionalmente sustituido con fenilo), cicloalquilo C3-10 (a su vez opcionalmente sustituido con alquilo C1-4 u oxo), metilendioxi, OCH2CH2O, difluorometilendioxi, heterociclilo (opcionalmente sustituido con hidroxi, alquilo C1-4, fenilo o heteroarilo), fenilo, fenil-alquilo C1-4, fenoxi, feniltio, fenil-alcoxi C1-4, heteroarilo, heteroaril-alquilo C1-4, heteroariloxi o heteroaril-alcoxi C1-4; donde cualquiera de dichas porciones fenilo y heteroarilo está opcionalmente sustituida con halogeno, hidroxi, nitro, S(O)r(alquilo C1-4), S(O)2NH2, S(O)2NH(alquilo C1-4), S(O)2N(alquil C1-4)2, ciano, alquilo C1-4, alcoxi C1-4, C(O)NH2, C(O)NH(alquilo C1-4), C(O)N(alquil C1-4)2, CO2H, CO2(alquilo C1-4), NHC(O)(alquilo C1-4), NHS(O)2(alquilo C1-4), C(O)(alquilo C1-4), CF3 o OCF3; E1 y G1 son, en forma independiente, hidrogeno, halogeno, ciano, hidroxi, alquilo C1-4, alcoxi C1-4, CF3 o OCF3; q y r son, en forma independiente, 0, 1 o 2; R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21, R22, R23, R24, R25, R26 y R27 son, en forma independiente, alquilo C1-10 {opcionalmente sustituido con halogeno, hidroxi o alcoxi C1-6, o fenilo o heteroarilo ambos opcionalmente sustituidos como se describe más adelante}, CH2(alquenilo C2-6), fenilo {a su vez opcionalmente sustituido con halogeno, hidroxi , nitro, NH2, NH(alquilo C1-4), N(alquil C1-4)2, S(O)2(alquilo C1-4), S(O)2NH2, S(O)2NH(alquilo C1-4), S(O)2N(alquil C1-4)2, ciano, alquilo C1-4, alcoxi C1-4, C(O)NH2, C(O)NH(alquilo C1-4), C(O)N(alquil C1-4)2, CO2H, CO2(alquilo C1-4), NHC(O)(alquilo C1-4), NHS(O)2(alquilo C1-4), C(O)(alquilo C1-4), CF3 o OCF3} o heteroarilo {a su vez opcionalmente sustituido con halogeno, hidroxi, nitro, NH2, NH(alquilo C1-4), N(alquil C1-4)2, S(O)2(alquilo C1-4), S(O)2NH2, S(O)2NH(alquilo C1-4), S(O)2N(alquil C1-4)2, ciano, alquilo C1-4, alcoxi C1-4, C(O)NH2, C(O)NH(alquilo C1-4), C(O)N(alquil C1-4)2, CO2H, CO2(alquilo C1-4), NHC(O)(alquilo C1-4), NHS(O)2(alquilo C1-4), C(O)(alquilo C1-4), CF3 o OCF3}; R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R18, R19, R20, R21, R22, R23, R24 y R25 también pueden ser hidrogeno; o un N-oxido del mismo; o una sal aceptable para uso farmacéutico del mismo. Reivindicacion 16: Un compuesto intermediario caracterizado porque responde a la formula (2) donde m, G1, E, Y, L, W, X y J tienen los valores que se definen en la reivindicacion 1.
ARP070101162A 2006-03-22 2007-03-21 Derivados de 2, 4-dioxo-1, 4-dihidropirido[2, 3 -d]pirimidina, un proceso para prepararlos e intermediario para su sintesis, una composicion farmaceutica que los comprende y su uso en la fabricacion de un medicamento para el tratamiento de enfermedades mediadas por pde4 AR060046A1 (es)

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