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US 8,946,218 B2Granted
CCR2 receptor antagonists, method for producing the same, and use thereof as medicaments
AssigneeBoehringer Ingelheim International GmbH
InventorsHeiner Ebel, Sara Frattini, Riccardo Giovannini, Christoph Hoenke, Rocco Mazzaferro, Stefan Scheuerer
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Abstract
The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD and pain diseases.
Claims14
A compound according to formula (I),
- wherein R1 is a group selected from among —H, -halogen, —CN, —O—C1-C4-alkyl, —C1-C4-alkyl, —CH═CH2, —C≡H, —CF3, —OCF3, —OCF2H, —C5-C10-heteroaryl, and —OCFH2, and wherein R7 is a group selected from among —H, -halogen, —CN, —O—C1-C4-alkyl, —C1-C4-alkyl, —CH═CH2, —C≡CH, —CF3, —OCF3, —OCF2H, and —OCFH2;
- or wherein R7 and R1 on two neighbouring ring atoms together form a —C3-C6-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, —NH2, —C1-C3-alkyl, —O—C1-C6-alkyl, —CN, —CF3, —OCF3, and halogen;
- wherein R4 is a group selected from among -hydrogen, —C1-C3-alkyl, —CF3, —OCF3, —OCF2H, -halogen, —CN, —O—C1-C4-alkyl, —CH═CH2, —C≡H, and —OCFH2;
- wherein A is C or N;
- wherein R14 is a group selected from among -hydrogen, and —C1-C3-alkyl;
- wherein R2 is selected from among —H, -halogen, —CN, —O—C1-C4-alkyl, —C1-C4-alkyl, -cyclopropyl, —CH═CH2, —C≡H, —CF3, —OCF3, —OCF2H, and —OCFH2;
- wherein R3 is selected from among —H, -methyl, -ethyl, -propyl, -i-propyl, -cyclopropyl, —OCH3, —CF3, and —CN;
- wherein n is 1, 2 or 3;
- wherein G and E are N;
- wherein R5 is a group of the structure -L1-R13,
- wherein L1 is selected from among —NH— and —N(C1-C4-alkyl)-,
- wherein R13 is —C3-C8-heterocyclyl,
- wherein R13 is optionally substituted by one or more groups selected from among halogen, —CF3, —OCF3, —CN, —OH, —O—C1-C4-alkyl, —C1-C6-alkyl;
- wherein R6 is selected from among —H, —C1-C4-alkyl, —OH, —O—C1-C4-alkyl, -halogen, —CN, —CF3, and —OCF3;
- as well as in form of their acid addition salts with pharmacologically acceptable acids.
13 more elements
Dependencies are inferred from the claim text.