Derivatives of 1,5-dihydropyrazolo[3,4-d]-pyrimidinone

 

The invention relates to new derivatives of 1,5-dihydropyrazolo[3,4-d] pyrimidinone General formula (I) having the properties of an inhibitor of phosphodiesterase, which can be used, for example, high blood pressure, angina, and heart disease. In the compound of formula (I) and D together denote a residue of the formula-N=CH-R2or-NH -, NA=O, where R2is hydrogen, linear alkoxyl with the number of carbon atoms up to 4, linear alkyl with the number of carbon atoms up to 4, optionally substituted by hydroxyl; R1- linear acyl with the number of carbon atoms up to 6, a linear alkyl with the number of carbon atoms up to 10, possibly substituted by hydroxyl; E. means linear alkylenes chain with the number of carbon atoms up to 6, and possibly substituted by hydroxyl; V is phenyl; L is phenyl, optionally substituted up to three times identically or differently linear alkyl, alkoxyl, alkoxycarbonyl with the number of carbon atoms up to 6, or a group of formula(W)a-NR7R8where a = 0 or 1; W is a residue of the formula-SO2; R7and R8is hydrogen or L - phenyl which may be substituted by phenyl which can be substituted identically or differently up to two times by halogen, linear alkyl or alkoxyl accordingly with the number of atoms in the a, R9and R10is hydrogen or together with the nitrogen form a 6-membered saturated a heterocycle, which optionally may contain an oxygen atom or a residue NR6where R6is hydrogen or a linear or branched alkyl with a number of carbon atoms to 4; W'has the value W, or L is a residue of formula 2, or V - alkyl, T - residue of the formula-CH2-X-Y, where X is a bond, Y represents alkylenes chain with the number of carbon atoms to 9, and their tautomers and salts. 3 C.p. f-crystals, 2 PL.

Description text in facsimile form (see graphic part)

Claims

1. Derivatives of 1,5-dihydropyrazolo[3,4-d]pyrimidinone General formula(I)

in which a and D together denote a residue of the formula

R2is hydrogen, linear alkoxyl with the number of carbon atoms up to 4, linear alkyl with the number of carbon atoms up to 4, optionally substituted by hydroxyl;

R1- linear acyl with the number of carbon atoms up to 6, a linear alkyl with the number of carbon atoms up to 10, possibly substituted by hydroxyl;

E. means linear alkylenes chain with city up to three times identically or differently linear alkyl, alkoxyl, alkoxycarbonyl with the number of carbon atoms up to 6, or a group of formula(W)a-NR7R8where a = 0 or 1, W is a residue of the formula-SO2, R7and R8is hydrogen,

or L - phenyl which may be substituted by phenyl which can be substituted identically or differently up to two times by halogen, linear alkyl or alkoxyl, respectively, with the number of carbon atoms up to 5, or 5-6-membered nitrogen-containing heterocycle, or - (W’)b-R9R10where b has a value a;

R9and R10both hydrogen or together with the nitrogen form a 6-membered saturated a heterocycle, which optionally may contain an oxygen atom or a residue NR6where R6is hydrogen or a linear or branched alkyl with a number of carbon atoms to 4; W’ is W,

or L is a residue of the formula

or V - alkyl;

T - residue of the formula-CH2-X-Y, where X is a bond, Y represents alkylenes chain with the number of carbon atoms to 9,

and their tautomers and salts.

2. Derivatives of 1,5-dihydropyrazolo[3,4-d] pyrimidinone formula (I) under item 1, in which a and D together - the rest of the formula

where R2is hydrogen, linear alkoxyl with the number of atoms operamail with the number of carbon atoms up to 6, linear alkyl with the number of carbon atoms up to 8, possibly substituted by hydroxyl; E. means linear alkylenes chain with the number of carbon atoms up to 5 and possibly substituted by hydroxyl; V is phenyl; L is phenyl, optionally substituted up to three times identically or differently linear alkyl, alkoxyl, alkoxycarbonyl with the number of carbon atoms of 5 or a group of formula(W)a-NR7R8,

where a = 0 or 1, W is a residue of the formula-SO2, R7and R8hydrogen, or L - phenyl which may be substituted by phenyl which can be substituted by fluorine, chlorine, bromine, linear alkyl or alkoxyl accordingly with the number of carbon atoms to 3; or pyridium, perriam or pirimidinom; or(W’)b-NR9R10where b has a value a, W’ is W, R9and R10both signify hydrogen or together with the nitrogen form morpholinyl, piperidinyl or piperazinilnom ring, or an L - residue formulas

or V - methyl, T - residue of the formula-CH2-X-Y, where X is a bond, Y represents alkylenes chain with the number of carbon atoms up to 8, and their tautomers and salts.

3. Derivatives of 1,5-dihydropyrazolo[3,4-d]pyrimidinone formula (I) under item 1, in which a and D

together snakewoman carbon to 4, linear alkyl with the number of carbon atoms up to 4, possibly substituted by hydroxyl;

R1- linear acyl with the number of carbon atoms up to 5, linear alkyl with the number of carbon atoms up to 6, possibly substituted by hydroxyl; E. means linear alkylenes chain with the number of carbon atoms up to 5 and possibly substituted by hydroxyl and V is phenyl; L is phenyl, optionally substituted up to three times identically or differently linear alkyl, alkoxyl, alkoxycarbonyl with the number of carbon atoms up to 4 or a group of formula(W)a-NR7R8where a = 0 or 1, W is a residue of the formula-SO2, R7and R8hydrogen, or L - phenyl, which is substituted by phenyl, which is optionally substituted by fluorine, chlorine, bromine, alkyl or alkoxyl accordingly with the number of carbon atoms to 3; pyridium; or (W’)b-NR9R10where b has a value a, W’ is W, R9and R10both hydrogen, or together with the nitrogen form morpholinyl, piperidine or piperazinilnom ring, or an L - residue formulas

or V - methyl, T - residue of the formula-CH2-X-Y, where X is a bond, Y represents alkylenes chain with the number of carbon atoms up to 6, and their tautomers and salts.

4. Derivatives of 1,5-Digi

 

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