COMPUESTOS DERIVADOS DE SISTEMAS N-O-S-HETEROCICLICOS FUSIONADOS QUE COMPRENDEN A UN ANILLO SUSTITUYENTE, INHIBIDORES DE FOSFODIESTERASA TIPO 9; COMPOSICION FARMACEUTICA Y USO DEL COMPUESTO EN EL TRATAMIENTO DE DIABTES TIPO 1 Y TIPO 2, HIPERGLUCEMIA
Cyclic guanosine monophosphate derivatives (I) and their stereoisomers and/or prodrugs or salts are new. Cyclic guanosine monophosphate derivatives of formula (I) and their stereoisomers and/or prodrugs or salts are new. [Image] A : 8 heterocyclic derivatives e.g. purine 2-one derivative of formula...
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Zusammenfassung: | Cyclic guanosine monophosphate derivatives (I) and their stereoisomers and/or prodrugs or salts are new. Cyclic guanosine monophosphate derivatives of formula (I) and their stereoisomers and/or prodrugs or salts are new. [Image] A : 8 heterocyclic derivatives e.g. purine 2-one derivative of formula (b) or 2,4,6-tirazole imidazole derivative of formula (c); ring P+C : 3-8C (hetero)cycloalkyl or (hetero)aryl (all optionally substituted with 1-3 substituents of halo, 1-5C alkyl, 1-5C alkoxy or CF 3); J : O, S, N(R 1> 5>), N(R 1> 5>)CO, CON(R 1> 5>), SO 2N(R 1> 5>) or N(R 1> 5>)SO 2; R 1> 0>CO 2H, CONR 3> 0>R 3> 1>, NR 3> 0>R 3> 1> or N(R 1> 5>)SO 2R 4> 0>; R 1>, R 2>H or 1-3C alkyl; R 3>1-8C alkyl, 3-8C (hetero)cycloalkyl, 3-8C (hetero)cycloalkyl-methyl or (hetero)aryl (all optionally substituted with 1-3 substituents of halo, OH, oxo, 1-5C alkyl or 1-5C alkoxy); R 1> 5>H or 1-5C alkyl; either R 3> 0>, R 3> 1>H, 1-5C alkyl, 3-8C (hetero)cycloalkyl or (hetero)aryl (all optionally substituted with 1-3 substituents of halo, oxo, 1-5C alkyl, CO 2R 4> 0>, COR 4> 0>, OR 4> 0>, CONR 5> 0>R 5> 1>, NR 5> 0>R 5> 1> or SO 2R 4> 0>); or NR 3> 0>R 3> 1>5-8 membered heterocycloalkyl ring (the ring optionally having 1 additional heteroatom of N, O or S) (optionally substituted with 1-3 of halo, oxo, 1-5C alkyl, CO 2R 4> 0>, COR 4> 0>, OR 4> 0>, CONR 5> 0>R 5> 1>, NR 5> 0>R 5> 1> or SO 2R 4> 0>); R 4> 0>H, 1-5C alkyl, 3-8C (hetero)cycloalkyl or (hetero)aryl; either R 5> 0>, R 5> 1>H, 1-5C alkyl, 3-8C (hetero)cycloalkyl or (hetero)aryl; or NR 5> 0>R 5> 1>5- to 8-membered heterocycloalkyl ring (the ring optionally having 1 additional heteroatom of N,O or S); and x : 0-6. [Image] ACTIVITY : Antidiabetic; Antilipemic; Cardiovascular-Gen. MECHANISM OF ACTION : Phosphodiesterase 9 (PDE9) inhibitor. (I) were tested for PDE9 inhibitory activity using biological assays. The results showed that (I) exhibited a median inhibitory concentration value of less than 50 nM. |
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