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Compounds of 4,5,7,8-tetrahydro-4-oxo-2H-imidazo [1,2-a] pyrrolo [3,4-e] pyrimidine as PDE1 inhibitors
专利权人:
INC.;INTRA-CELLULAR THERAPIES
发明人:
LI, PENG,WENNOGLE, LAWRENCE P.
申请号:
ES09830743
公开号:
ES2551133T3
申请日:
2009.12.07
申请国别(地区):
ES
年份:
2015
代理人:
摘要:
The compound selected from a) the Compound of Formula II-A or II-B: is ** Formula ** in which (i) Q is C (>; = O), C (>; = S) or CH2; (ii) L is a single bond, -N (H) -, -S-, (iii) R1 is H or C1-4 alkyl; (iv) R2 is H and R3 and R4 together form a di, tri or tetramethylene bridge; (v) R5 is a) -D-E-F, in which: D is C1-4 alkylene; E is arylene or heteroarylene; F is aryl, heteroaryl, C3-7 cycloalkyl optionally containing at least one atom selected from a group consisting of N or O; wherein D, E and F are independently and optionally substituted with one or more halo, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, hydroxy, carboxy or an additional aryl or heteroaryl; b) binds to the nitrogen in the pyrrolo portion of Formula II-A or II-B and is a remainder of Formula A ** Formula ** in which X, Y and Z are, independently, N or C, and R8, R9, R11 and R12 are independently H or halogen and R10 is C1-4 alkoxy, with the proviso that when X, Y or Z is nitrogen, R8, R9 or R10, respectively, are not present; (vi) R6 is H, aryl, wherein the aryl is optionally substituted with one or more C1-4 alkyl, halogen, C1-4 haloalkyl, hydroxy, carboxy, or an additional aryl, heteroaryl or C3-8 cycloalkyl; (vii) R7 is H, C1-6 alkyl; (viii) n>; = 0 or 1; (ix) when n>; = 1, A is -C (R13R14) -, in which R13 and R14, are independently H or C1-4 alkyl, in free or salt form.El compuesto seleccionado entre a) el Compuesto de Fórmula II-A o II-B: es**Fórmula** en las que (i) Q es C(>;=O), C(>;=S) o CH2; (ii) L es un enlace sencillo, -N(H)-, -S-, (iii) R1 es H o alquilo C1-4; (iv) R2 es H y R3 y R4 juntos forman un puente di, tri o tetrametileno; (v) R5 es a) -D-E-F, en la que: D es alquileno C1-4; E es arileno o heteroarileno; F es arilo, heteroarilo, cicloalquilo C3-7 que contiene opcionalmente al menos un átomo seleccionado entre un grupo que consiste en N u O; en la que D, E y F están independiente y opcionalmente sustituidos con uno o más halo, alquilo C1-4, haloalquilo C1-4, alcoxi C1-
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