NOVEL PYRIMIDOTHIENOINDAZOLES
The invention relates to novel pyrimidothienoindazoles of formula (I) processes for their preparation and their use for preparing medicaments for the treatment or prophylaxis of disorders, especially of hyperproliferative disorders.
1 . A compound of formula
wherein
R 1 is selected from the group consisting of hydrogen, methyl, ethyl, and halo;
R 2 is selected from the group consisting of hydrogen, methyl, ethyl, and halo;
R 3 is selected from the group consisting of hydrogen, alkyl, halo, hydroxy, alkoxy, trifluoromethoxy, benzyloxy, halogenated benzyloxy, alkylated benzyloxy, pyridoxy, alkylated pyridoxy, halogenated pyridoxy, pyridylmethoxy, halogenated pyridylmethoxy, and N-morpholinyl, or
R 2 and R 3 , together with the carbon atoms to which they are attached, form an pyrazole ring, wherein said pyrazole ring can optionally be substituted with 0, 1 or 2 substituents independently selected from the group consisting of alkyl, benzyl, halogenated benzyl, pyridylmethoxy, and halogenated pyridylmethoxy;
R 4 is selected from the group consisting of hydrogen, alkyl, cyano, and halo;
R 5 is selected from the group consisting of hydrogen, alkyl, and halo;
R 6 is selected from the group consisting of hydrogen, and alkyl;
R 7 is selected from the group consisting of hydrogen, and alkyl, or
R 7 is a heterocycle selected from the group consisting of pyrrolidinyl, morpholinyl, piperidinyl, and piperazinyl, or
R 7 is alkyl selected from the group consisting of methyl, ethyl, n-propyl, i-propyl, n-butyl, i-butyl and t-butyl, wherein said alkyl is substituted with 1, 2 or 3 independently selected substituents R 7−1 ,
wherein R 7−1 is selected from the group consisting of halo, hydroxy, alkoxy, alkylsulfonyloxy, and amino, or
R 7−1 is alkylamino, wherein said alkylamino can optionally be substituted with 0, 1 or 2 substituents independently selected from the group consisting of hydroxy, alkoxy, amino, alkylamino, alkylsulfonyl, pyrrolidinyl, morpholinyl, piperidinyl, and piperazinyl, or
R 7−1 is alkenylamino, wherein said alkenylamino can optionally be substituted with 0, 1 or 2 substituents independently selected from the group consisting of oxo, hydroxy, alkoxy, amino, alkylamino, alkylsulfonyl, N-pyrrolidinyl, N-morpholinyl, N-piperidinyl, and N-piperazinyl, or
R 7−1 is a heterocycle selected from the group consisting of pyrrolidinyl, imidazolidinyl, imidazolyl, pyrazolyl, morpholinyl, piperidinyl, piperazinyl, and thiomorpholinyl, wherein said heterocycle can optionally be substituted with 0, 1 or 2 substituents independently selected from the group consisting of alkyl, halo, hydroxy, alkoxy, amino, alkylamino, hydroxyalkyl, alkoxyalkyl, carboxyl, alkoxycarbonyl, N-pyrrolidinyl, N-piperidinyl, N-piperazinyl, pyrazinyl, benzyl, and pyridylmethyl, or
R 7 is alkenyl selected from the group consisting of allyl, prop-1-enyl, 2-methyl-prop-1-enyl, but-1-enyl, but-2-enyl, but-3-enyl, pent-1-enyl, pent-2-enyl, pent-3-enyl, pent-4-enyl, wherein said alkenyl is substituted with 1, 2 or 3 independently selected substituents R 7−2
wherein R 7−2 is oxo, or
wherein R 7−2 is alkylamino, wherein said alkylamino can optionally be substituted with 0, 1 or 2 substituents independently selected from the group consisting of oxo, hydroxy, alkoxy, amino, and alkylamino;
or a salt thereof.
2 . A method of treating a disease or condition in a mammal, comprising administering to a mammal in need thereof an effective amount of a compound according to the formula (I) of claim 1 .
3 . The method of claim 2 , wherein the disease or condition is a hyperproliferative disorder.
4 . A compound of formula (II)
wherein R 1 to R 7 have the meaning indicated in claim 1 .