CCR2 receptor antagonists, method for producing the same, and use thereof as medicaments

1. A compound according to formula (I),

wherein R 1 is a group selected from among —H, -halogen, —CN, —O—C 1 -C 4 -alkyl, —C 1 -C 4 -alkyl, —CH═CH 2 , —C≡H, —CF 3 , —OCF 3 , —OCF 2 H, —C 5 -C 10 -heteroaryl, and —OCFH 2 , and wherein R 7 is a group selected from among —H, -halogen, —CN, —O—C 1 -C 4 -alkyl, —C 1 -C 4 -alkyl, —CH═CH 2 , —C≡CH, —CF 3 , —OCF 3 , —OCF 2 H, and —OCFH 2 ;

or wherein R 7 and R 1 on two neighbouring ring atoms together form a —C 3 -C 6 -alkenylene group, such that an annellated aromatic ring is formed, in which one or two or three carbon centers may optionally be replaced by 1 or 2 or 3 hetero atoms selected from N, O, and S,

wherein the resulting annelated ring being optionally substituted by one or more groups selected from among —OH, —NH 2 , —C 1 -C 3 -alkyl, —O—C 1 -C 6 -alkyl, —CN, —CF 3 , —OCF 3 , and halogen;

wherein R 4 is a group selected from among -hydrogen, —C 1 -C 3 -alkyl, —CF 3 , —OCF 3 , —OCF 2 H, -halogen, —CN, —O—C 1 -C 4 -alkyl, —CH═CH 2 , —C≡H, and —OCFH 2 ;

wherein A is C or N;

wherein R 14 is a group selected from among -hydrogen, and —C 1 -C 3 -alkyl;

wherein R 2 is selected from among —H, -halogen, —CN, —O—C 1 -C 4 -alkyl, —C 1 -C 4 -alkyl, -cyclopropyl, —CH═CH 2 , —C≡H, —CF 3 , —OCF 3 , —OCF 2 H, and —OCFH 2 ;

wherein R 3 is selected from among —H, -methyl, -ethyl, -propyl, -i-propyl, -cyclopropyl, —OCH 3 , —CF 3 , and —CN;

wherein n is 1, 2 or 3;

wherein G and E are N;

wherein R 5 is a group of the structure -L 1 -R 13 ,

wherein L 1 is selected from among —NH— and —N(C 1 -C 4 -alkyl)-,

wherein R 13 is —C 3 -C 8 -heterocyclyl,

wherein R 13 is optionally substituted by one or more groups selected from among halogen, —CF 3 , —OCF 3 , —CN, —OH, —O—C 1 -C 4 -alkyl, —C 1 -C 6 -alkyl;

wherein R 6 is selected from among —H, —C 1 -C 4 -alkyl, —OH, —O—C 1 -C 4 -alkyl, -halogen, —CN, —CF 3 , and —OCF 3 ;

as well as in form of their acid addition salts with pharmacologically acceptable acids.

2. The compound of formula (I) according to claim 1 ,

wherein R 1 is a group selected from among —H, -halogen, —C 1 -C 4 -alkyl, —CF 3 , —OCF 3 , and —C 6 -heteroaryl comprising a N atom;

wherein R 7 is a group selected from among —H, -halogen, —C 1 -C 4 -alkyl, —CF 3 , —OCF 3 , and —C 6 -heteroaryl comprising a N atom; and

wherein R 4 denotes -hydrogen.

3. The compound of formula (I) according to claim 1 ,

wherein R 7 and R 1 on two neighbouring ring atoms together form a —C 4 -alkenylene group, such that an annellated aromatic ring is formed, in which one or two carbon centers may optionally be replaced by 1 or 2 hetero atoms selected from N;

wherein R 4 is a group selected from among -hydrogen, and —C 1 -C 3 -alkyl.

4. The compound of formula (I) according to claim 1 , wherein A denotes N.

5. The compound of formula (I) according to claim 1 , wherein A denotes C.

6. The compound of formula (I) according to claim 1 , wherein R 2 is selected from among —H, —C 1 -C 4 -alkyl, and —O—C 1 -C 4 -alkyl.

7. The compound of formula (I) according to claim 1 , wherein R 2 is selected from among -methyl, and —OCH 3 .

8. The compound of formula (I) according to claim 1 , wherein R 3 denotes hydrogen.

9. The compound of formula (I) according to claim 1 , wherein n is 2.

10. The compound of formula (I) according to claim 1 , wherein

R 5 is a group of the structure -L 1 -R 13 ,

wherein L 1 denotes —NH—,

wherein R 13 is —C 6 -heterocyclyl comprising an O atom,

wherein R 13 is optionally substituted by a group selected from among —O—C 1 -C 4 -alkyl.

11. The compound of formula (I) according to claim 1 , wherein R 6 is —H.

12. The compound of formula (I) according to claim 1 , wherein R 14 is —H.

13. The compound according to claim 1 selected from the group consisting of

as well as in form of their acid addition salts with pharmacologically acceptable acids.

14. A method for the treatment of a disease selected from osteoarthritis, diabetic nephropathy, low back pain, neuropathic pain or a pain disease, comprising administering to a patient in need thereof a therapeutic amount of compound according to claim 1 .