New ccr2 receptor antagonists and uses thereof
AssigneeCentrexion Therapeutics Corporation
InventorsHeiner Ebel, Sara Frattini, Kai Gerlach, Riccardo Giovannini, Christoph Hoenke, Rocco Mazzaferro, Marco Santagostino, Stefan Scheuerer, Christofer Tautermann, Thomas Trieselmann
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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.
Claims21
1-24. (canceled)
A method for treating a neurologic disease selected from inflammatory and neuropathic pain, comprising administering an effective amount of a compound of Formula I to a patient in need thereof to treat the neurologic disease, wherein Formula I is represented by:
- or an acid addition salt thereof with a pharmacologically acceptable acid;
- wherein:
- R1 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;
- R7 is a ring selected from among —C3-C8-cycloalkyl, —C5-C10-aryl, and —C5-C10-heteroaryl, wherein the ring R7 is optionally substituted with one or more groups selected from among —CF3, —O—CF3, —S—CF3, —CN, —C1-C6-alkyl, —C(CH3)2—CN, and -halogen, or wherein the ring R7 is optionally substituted with one or more groups selected from among —O—C1-C6-alkyl and —C3-C8-cycloalkyl;
- R2 is selected from among —H, -halogen, —CN, —O—C2-C4-alkyl, —C1-C4-alkyl, —CH═CH2, —C≡CH, —CF3, —OCF3, —OCF2H, and —OCFH2;
- R3 is selected from among —H, -methyl, -ethyl, -propyl, -i-propyl, -cyclopropyl, —OCH3, —CF3, and —CN;
- n is 1, 2, or 3;
- G and E are N;
- Z is C;
- R4 denotes —H, and R5 is -L1-R18, wherein L1 is selected from among —NH—, —N(C1-C4-alkyl)-, and a bond, and R18 is —C3-C8-cycloalkyl or —C3-C8-heterocyclyl, wherein R18 is optionally substituted by one or more groups selected from among halogen, —CF3, —OCF3, —CN, —OH, —O—C1-C4-alkyl, —C1-C6-alkyl, —NH—C(O)—C1-C6-alkyl, —N(C1-C4-alkyl)-C(O)—C1-C6-alkyl, and —C(O)—C1-C6-alkyl;
- and
- R6 is selected from among —H, —C1-C4-alkyl, —OH, —O—C1-C4-alkyl, -halogen, —CN, —CF3, and —OCF3.
Dependencies are inferred from the claim text.