Synthesis and biological activity of pyrido[3′,2′:4,5]thieno[3, 2-d ]pyrimidines as phosphodiesterase type 4 inhibitors

Journal of Medicinal Chemistry

Volumn 53, Issue 19, 2010, Pages 6912-6922

  Taltavull, Joan ^a   Serrat, Jordi ^a   Gràcia, Jordi ^a   Gavaldà, Amadeu ^a   Andrés, Míriam ^a   Córdoba, Mònica ^a   Miralpeix, Montserrat ^a   Vilella, Dolors ^a   Beleta, Jorge ^a   Ryder, Hamish ^a   Pagès, Lluís ^a  

^a Almirall RandD Centre ^*  (Spain)

Author keywords

[No Author keywords available]

Indexed keywords

1 [3 [(2,2 DIMETHYL 5 MORPHOLIN 4 YL 1,4 DIHYDRO 2H PYRANO[4'',3'':4',5']PYRIDO[3',2':4,5]THIENO[3,2 D]PYRIMIDIN 8 YL)AMINO] PROPYL]PYRROLIDIN 2 ONE; 1 [3 [(5 MORPHOLIN 4 YL) 2,2 DIMETHYL 1,2,3,4 TETRAHYDROPYRIMIDO[4',5':4,5]THIENO[2,3 C]ISOQUINOLIN 8 YL)AMINO]PROPYL]PYRROLIDIN 2 ONE; 2 ETHYL 2 METHYL 5 MORPHOLIN 4 YL N (2 MORPHOLIN 4 YLETHYL) 1,4 DIHYDRO 2H PYRANO[4'',3'':4',5']PYRIDO[3',2':4,5]THIENO[3,2 D]PYRIMIDIN 8 AMINE; 2,2 DIMETHYL 4 MORPHOLIN 4 YL N (2 MORPHOLIN 4 YLETHYL) 2,3 DIHYDRO 1H CYCLOPENTA[4',5']PYRIDO[3',2':4,5]THIENO[3,2 D]PYRIMIDIN 7 AMINE; 2,2 DIMETHYL 4 MORPHOLIN 4 YL N 7 (2 MORPHOLIN 4 YLETHYL) 2,3 DIHYDRO 1H CYCLOPENTA[4',5']PYRIDO[3',2':4,5]THIENO[3,2 D]PYRIMIDIN 7 AMINA; 2,2 DIMETHYL 5 (4 METHYLPIPERAZIN 1 YL) N (2 MORPHOLIN 4 YLETHYL) 1,2,3,4 TETRAHYDROPYRIMIDO[4',5':4,5]THIENO[2,3 C]ISOQUINOLIN 8 AMINE; 2,2 DIMETHYL 5 (4 METHYLPIPERAZIN 1 YL) N (2 MORPHOLIN 4 YLETHYL) 1,4 DIHYDRO 2H PYRANO[4'',3'':4',5']PYRIDO [3',2':4,5]THIENO[3,2 D]PYRIMIDIN 8 AMINE; 2,2 DIMETHYL 5 MORPHOLIN 4 YL N (2 MORPHOLIN 4 YLETHYL) 1,2,3,4 TETRAHYDROPYRIMIDO[4',5':4,5]THIENO[2,3 D]ISOQUINOLIN 8 AMINE; 2,2 DIMETHYL 5 MORPHOLIN 4 YL N (2 PIPERIDIN 1 YLETHYL) 1,4 DIHYDRO 2H PYRANO[4'',3'':4',5']PYRIDO[3',2':4,5]THIENO[3,2 D]PYRIMIDIN 8 AMINE; 2,2 DIMETHYL 5 MORPHOLIN 4 YL N (PYRIDIN 3 YLMETHYL) 1,2,3,4 TETRAHYDROPYRIMIDO[4',5':4,5]THIENO[2,3 C]ISOQUINOLIN 8 AMINE; 2,2 DIMETHYL 5 MORPHOLIN 4 YL N (PYRIDIN 3 YLMETHYL) 1,4 DIHYDRO 2H PYRANO[4'',3'':4',5']PYRIDO[3',2':4,5]THIENO[3,2 D]PYRIMIDIN 8 AMINE; 2,2 DIMETHYL 5 MORPHOLIN 4 YL N (PYRIDIN 4 YLMETHYL) 1,2,3,4 TETRAHYDROPYRIMIDO[4',5':4,5]THIENO[2,3 C]ISOQUINOLIN 8 AMINE; 2,2 DIMETHYL 5 MORPHOLIN 4 YL N (PYRIDIN 4 YLMETHYL) 1,4 DIHYDRO 2H PYRANO[4'',3'':4',5']PYRIDO[3',2':4,5]THIENO[3,2 D]PYRIMIDIN 8 AMINE; 2,2 DIMETHYL N (2 MORPHOLIN 4 YLETHYL) 5 PYRROLIDIN 1 YL 1,2,3,4 TETRAHYDROPYRIMIDO[4',5':4,5]THIENO[2,3 C]ISOQUINOLIN 8 AMINE; 2,2,3 TRIMETHYL 5 MORPHOLIN 4 YL N (2 MORPHOLIN 4 YLETHYL) 1,2,3,4 TETRAHYDROPYRIMIDO[4',5':4,5]THIENO[2,3 C]2,7 NAPHTHYRIDIN 8 AMINE; 2,2,5 TRIMETHYL N (2 MORPHOLIN 4 YLETHYL) 1,2,3,4 TETRAHYDROPYRIMIDO[4',5':4,5]THIENO[2,3 C]ISOQUINOLIN 8 AMINE; 5 (2 FURYL) 2,2 DIMETHYL N (2 MORPHOLIN 4 YLETHYL) 1,2,3,4 TETRAHYDROPYRIMIDO[4',5':4,5]THIENO[2,3 C]ISOQUINOLIN 8 AMINE; 5 (3 FURYL) 2,2 DIMETHYL N (2 MORPHOLIN 4 YLETHYL) 1,2,3,4 TETRAHYDROPYRIMIDO[4',5':4,5]THIENO[2,3 C]ISOQUINOLIN 8 AMINE; 5 ISOBUTYL 2,2 DIMETHYL N (2 MORPHOLIN 4 YLETHYL) 1,2,3,4 TETRAHYDROPYRIMIDO[4',5':4,5]THIENO[2,3 C]ISOQUINOLIN 8 AMINE; 5 MORPHOLIN 4 YL N (2 MORPHOLIN 4 YLETHYL) 1,4 DIHYDRO 2H PYRANO[4'',3'':4,5'[PYRIDO[3',2':4,5]THIENO[3,2 D]PYRIMIDIN 8 AMINE; CYCLOHEXYL(PHENYL)(2 PIPERIDINOETHYL)SILANOL; N 5 BENZYL N 5 ,2,2 TRIMETHYL N (2 MORPHOLIN 4 YLETHYL) 1,2,3,4 TETRAHYDROPYRIMIDO[4',5':4,5]THIENO[2,3 C]ISOQUINOLIN 8 AMINE; N 5,2,2 TRIMETHYL N 8 (2 MORPHOLIN 4 YLETHYL) 1,2,3,4 TETRAHYDROPYRIMIDO[4',5':4,5]THIENO[2,3 C]ISOQUINOLIN 5,8 DIAMINE; N 5,2,2 TRIMETHYL N 8 (2 MORPHOLIN 4 YLETHYL) 1,4 DIHYDRO 2H PYRANO[4'',3'':4',5']PYRIDO[3',2':4,5]THIENO[3,2 D]PYRIMIDIN 5,8 DIAMINE; N 5,N 5,2,2 TETRAMETHYL N 8 (2 MORPHOLIN 4 YLETHYL) 1,4 DIHYDRO 2H PYRANO[4'',3'':4',5']PYRIDO[3',2':4,5]THIENO[3,2 D]PYRIMIDIN 5,8 DIAMINE; PHOSPHODIESTERASE IV; PHOSPHODIESTERASE IV INHIBITOR; PYRIDO[3',2':4,5]THIENO[3,2 D]PYRIMIDINE; ROLIPRAM; UNCLASSIFIED DRUG; UNINDEXED DRUG; PYRIDINE DERIVATIVE; PYRIMIDINE DERIVATIVE; RECOMBINANT PROTEIN; THIOPHENE DERIVATIVE;

ARTICLE; DRUG SCREENING; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; HUMAN; STRUCTURE ACTIVITY RELATION; SUBSTITUTION REACTION; ANTAGONISTS AND INHIBITORS; CHEMISTRY; PICHIA; SYNTHESIS;

HUMANS; PHOSPHODIESTERASE 4 INHIBITORS; PICHIA; PYRIDINES; PYRIMIDINES; RECOMBINANT PROTEINS; STRUCTURE-ACTIVITY RELATIONSHIP; THIOPHENES;

EID: 77957921582     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm100524j     Document Type: Article

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