- Synthesis and biological activity of pyrido[3′,2′:4,5]thieno[3, 2-d ]pyrimidines as phosphodiesterase type 4 inhibitors
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A series of pyrido[3′,2′:4,5]thieno[3,2-d]pyrimidines (PTP) has been synthesized and tested as phosphodiesterase IV inhibitors (PDE4), a target for the treatment of asthma and chronic obstructive pulmonary disease (COPD). Structure-activity relationships
- Taltavull, Joan,Serrat, Jordi,Gràcia, Jordi,Gavaldà, Amadeu,Andrés, Míriam,Córdoba, Mònica,Miralpeix, Montserrat,Vilella, Dolors,Beleta, Jorge,Ryder, Hamish,Pagès, Lluís
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experimental part
p. 6912 - 6922
(2010/12/25)
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- NEW PYRIDOTHIENOPYRIMIDINE DERIVATIVES
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Use of a pyridothienopyrimidine derivative of formula (I), and the pharmaceutically acceptable salts and N-oxides thereof, wherein G1 represents a group selected from -CR6R7- or -NR6 being R6 and R7 independently selected from hydrogen atoms and C1-4 alkyl groups m and n are integers selected from 0 or 1 R1 and R2 are independently selected from hydrogen atoms and C1-4 alkyl groups R3 represents a group selected from alkyl, amino, monoalkylamino, dialkylamino, aryl, heteroaryl and saturated N-containing heterocyclyl groups bound through the nitrogen atom to the piridine ring, all of them being optionally substituted by one or more substituents selected from the group consisting of halogen atoms and alkyl, alkoxyalkyl, arylalkyl, R8OCO-, alkoxy, R8R9N-CO-, -CN, -CF3, -NR8R9, -SR8 and - SO2NH2 groups wherein R8 and R9 are independently selected from hydrogen atoms and C1-4alkyl groups R4 and R5 are independently selected from the group consisting of hydrogen atoms alkyl groups and groups of formula (II), wherein p and q are integers selected from 1, 2 and 3; A is either a direct bond or a group selected from -CONR14-, -NR14CO-, -O-, -COO-, -OCO-, -NR 14OCO-, - OCONR14-, -NR14CONR15-, -S-, -SO-, -SO2-, -COS- and -SCO-; and G2 is a group selected from aryl, heteroaryl or heterocyclyl; wherein the alkyl groups and the group G2 are optionally substituted by one or more substituents selected from group consisting of halogen atoms and alkyl, alkoxyalkyl, arylalkyl, R16OCO-, hydroxy, alkoxy, oxo, R16R17NCO-, -CN, -CF3, -NR16R17,-SR16 and -SO2NH2 groups; wherein R10 to R17 are independently selected from hydrogen atoms and C1-4 alkyl groups; in the manufacture of a medicament for the treatment or prevention of a pathological condition or disease susceptible to amelioration by inhibition of phosphodiesterase 4.
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Page/Page column 61-62
(2008/06/13)
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