AR041271A1 - Quinazolinonas espirocondensadas y su uso como inhibidores de la fosfodiesterasa - Google Patents

Quinazolinonas espirocondensadas y su uso como inhibidores de la fosfodiesterasa

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Publication number
AR041271A1
AR041271A1 ARP030103355A AR041271A1 AR 041271 A1 AR041271 A1 AR 041271A1 AR P030103355 A ARP030103355 A AR P030103355A AR 041271 A1 AR041271 A1 AR 041271A1
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alkyl
nr4r5
groups
nr7r8
substituted
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Warner Lambert Co
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    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/78Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/80Oxygen atoms
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    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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    • C07D401/12Heterocyclic 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

Quinazolinonas espirocondensadas y su uso como inhibidores de la fosfodiesterasa, a su uso como medicamento, a composiciones farmacéuticas que los contienen y a un procedimiento para su preparación. Reivindicación 1: Un compuesto de la fórmula (1)caracterizado porque, m es 1, 2, o 3, y R1 se selecciona entre CH3, Cl, Br, y F, y R2 se selecciona de: Q1-Q2-Q3-Q4 en la que: Q1 es un enlace sencillo o un grupo alquileno C1-6 lineal o ramificado; Q2 es un heterociclo saturado de 4 a 6 miembrosque comprende uno o dos heteroátomos seleccionados entre O o N; Q3 es un grupo alquileno C1-6 lineal o ramificado; Q4 es un heterociclo de 4 a 8 miembros, aromático o no aromático, que comprende de 1 a 4 heteroátomos seleccionados entre O, S, S(=O),SO2 y N, dicho heterociclo está opcionalmente sustituido con uno o varios grupos seleccionados entre OR, NRR´, CN y alquilo C1-6, en los que R y R´ son iguales o diferentes y se seleccionan entre H y alquilo C1-6; el átomo de Q2 unido a Q1 es unátomo de C, y, el átomo de Q4 unido a Q3 es un átomo de C; alquilo C1-6, dicho grupo alquilo está sustituido con 1 a 3 grupos, preferiblemente 1, seleccionado entre OR4, COOR4, NR4R5, NRC(=O)R4, C(=O)NR4R5 y SO2NR4R5, en los que, R es H o alquilo C1-6; R4 es alquilo C1-6 sustituido con uno o varios grupos, preferiblemente de 1 a 3, seleccionados entre F, CN, S(=O)R6, SO3H, SO2R6, SR7, C(=O)-NH-SO2-CH3, -C(=O)R7, NR´C(=O)R7, NR´SO2R6, C(=O)NR7R8, O-C(=O)NR7R8 y SO2NR7R8, en los que R´ es H, oalquilo C1-6, R6 es alquilo C1-6 opcionalmente sustituido con uno o dos grupos OR" en los que R" se selecciona entre H y alquilo C1-6, y R7 y R8 son iguales o diferentes y se seleccionan entre H y R6. R5 se selecciona entre R4, H y alquilo C1-6; odicho grupo alquilo está 1) sustituido con de 1 a 3 grupos, preferiblemente 1, seleccionado entre OC(=O)R4, SR4, S(=O)R3, C(=NR9)R4, C(=NR9)-NR4R5, NR-C(=NR9)-NR4R5, NRCOOR4, NR-C(=O)-NR4R5, NR-SO2-NR4R5, NR-C(=NR9)-R4 y NR-SO2-R3 y, 2)opcionalmente sustituido con 1 o 2 grupos seleccionados entre OR4, COOR4, C(=O)-R4, NR4R5, NRC(=O)R4, C(=O)NR4R5 y SO2NR4R5; en los que, R se selecciona entre H y alquilo C1-6; R9 se selecciona entre H, CN, OH, OCH3, SO2CH3, SO2NH2 y alquilo C1-6, yR3 es alquilo C1-6, sustituido o insustituido con uno o varios grupos, preferiblemente de 1 a 3, seleccionados entre F, CN, S(=O)R6, SO3H, SO2R6, C(=O)-NH-SO2-CH3, OR7, SR7, COOR7, C(=O)R7, O-C(=O)NR7R8, NR7R8, NR´C(=O)R7, NR´SO2R6, C(=O)NR7R8 ySO2NR7R8, en los que R´ es H o alquilo C1-6; R6 es alquilo C1-6 opcionalmente sustituido con uno o dos grupos OR", en los que R" se selecciona entre H y alquilo C1-6 y R7 y R8 son iguales o diferentes y se seleccionan entre H y R6; R4 y R5 soniguales o diferentes y se seleccionan entre H y R3; o sus formas racémicas, sus isómeros y sus derivados farmacéuticamente aceptables
ARP030103355 2002-09-17 2003-09-16 Quinazolinonas espirocondensadas y su uso como inhibidores de la fosfodiesterasa AR041271A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP20020292275 EP1400244A1 (en) 2002-09-17 2002-09-17 New spirocondensed quinazolinones and their use as phosphodiesterase inhibitors

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AR041271A1 true AR041271A1 (es) 2005-05-11

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US (1) US7429598B2 (es)
EP (2) EP1400244A1 (es)
JP (1) JP2006501277A (es)
KR (1) KR20050057371A (es)
CN (1) CN1681507A (es)
AP (1) AP2005003251A0 (es)
AR (1) AR041271A1 (es)
AU (1) AU2003259496A1 (es)
BR (1) BR0314379A (es)
CA (1) CA2499330C (es)
CO (1) CO5540391A2 (es)
CR (1) CR7728A (es)
EA (1) EA200500312A1 (es)
EC (1) ECSP055671A (es)
GT (1) GT200300201A (es)
HN (1) HN2003000285A (es)
HR (1) HRP20050223A2 (es)
IS (1) IS7700A (es)
MA (1) MA27439A1 (es)
MX (1) MXPA05002913A (es)
NO (1) NO20051695L (es)
OA (1) OA12924A (es)
PA (1) PA8582801A1 (es)
PE (1) PE20050073A1 (es)
PL (1) PL375977A1 (es)
TN (1) TNSN05073A1 (es)
TW (1) TWI251590B (es)
UY (1) UY27986A1 (es)
WO (1) WO2004026818A1 (es)
ZA (1) ZA200501381B (es)

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AU2003259496A1 (en) 2004-04-08
TWI251590B (en) 2006-03-21
TW200413333A (en) 2004-08-01
NO20051695L (no) 2005-04-05
EA200500312A1 (ru) 2005-08-25
TNSN05073A1 (fr) 2007-05-14
MXPA05002913A (es) 2005-05-27
CA2499330A1 (en) 2004-04-01
KR20050057371A (ko) 2005-06-16
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CA2499330C (en) 2009-04-28
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