Quinoline-4-carboxamide derivatives as NK-3 and NK-2 receptor antagonists

摘要

A compound, its preparation process, a pharmaceutical composition and the use of this compound and composition in medicines is disclosed, wherein the compound is selected from the group consisting of: 1. 3-[1,4']Bipiperidinyl-1'-ylmethyl-2-phenyl-quinoline-4- carboxylic acid ((S)-1-cyclohexyl-ethyl)-amide 2. 3-{4-[2-(2-Hydroxy-ethoxy)-ethyl]-piperazin-1- ylmethyl}-2-phenyl-quinoline-4-carboxylic acid ((S)-1phenyl- propyl)-amide 3. 3-[4-(2-Hydroxy-ethyl)-piperazin-1-ylmethyl]-2-phenyl- quinoline-4-carboxylic acid ((S)-1-cyclohexyl-ethyl)-amide 4. 3-[4-(1-Methyl-piperidin-4-yl)-piperazin-1-ylmethyl]-2- phenyl-quinoline-4-carboxylic acid ((S)-1-phenyl-propyl)- amide 5. 3-[4-(1-Methyl-piperidin-4-yl)-piperazin-1-ylmethyl]-2- phenyl-quinoline-4-carboxylic acid ((S)-1-cyclohexyl-ethyl)- amide 6. 2-Phenyl-3-piperazin-1-ylmethyl-quinoline-4-carboxylic acid ((S)-1-cyclohexyl-ethyl)-amide 7. 3-[4-(2-Dimethylamino-ethanoyl)-piperazin-1-ylmethyl]- 2-phenyl-quinoline-4-carboxylic acid ((S)-1cyclohexyl- ethyl)-amide 8. 3-[4-(3-Diethylamino-propanoyl)-piperazin-1-ylmethyl]- 2-phenyl-quinoline-4-carboxylic acid ((S)-1-cyclohexyl- ethyl)-amide 9. 3-{4-[2-(4-Methyl-piperazin-1-yl)-ethanoyl]-piperazin- 1-ylmethyl}-2-phenyl-quinoline-4-carboxylic acid((S)-1- cyclohexyl-ethyl)-amide 10. ({4-[4-((S)-1-Cyclohexyl-ethylcarbamoyl)-2-phenyl- quinolin-3-ylmethyl]-piperazin-1-yl}-dimethylamino- methylene)-dimethyl-ammonium 11. 3-(4-Amino-piperidin-1-ylmethyl)-2-phenyl-quinoline-4- carboxylic acid ((S)-1-phenyl-propyl)-amide 12. 3-[4-(4-Methyl-piperidin-1-yl)-piperazin-1-ylmethyl]-2- phenyl-quinoline-4-carboxylic acid ((S)-1-phenyl-propyl)- amide 13. 3-[1,4']Bipiperidinyl-1'-ylmethyl-7-methoxy-2-phenyl- quinoline-4-carboxylic acid ((S)-1-phenyl-propyl)amide 14. 3-[4-(1-Methylimino-1-pyrrolidin-1-yl-methyl)- piperazin-1-ylmethyl]-2-phenyl-quinoline-4-carboxylic acid ((S)-1-cyclohexyl-ethyl)-amide 15. 3-[1,4']Bipiperidinyl-1'-ylmethyl-2-phenyl-quinoline-4- carboxylic acid ((S)-2-methyl-1-phenyl-propyl)amide 16. 3-[4-(3-Diethylamino-propanoyl)-piperazin-1-ylmethyl]- 2-phenyl-quinoline-4-carboxylic acid ((S)-2-methyl1-phenyl- propyl-amide 17. 3-[4-(2-Nitro-1-pyrrolidin-1-yl-vinyl)-piperazin-1- ylmethyl]-2-phenyl-quinoline-4-carboxylic acid ((S)- 1cyclohexyl-ethyl)-amide 18. 3-[1,4']Bipiperidinyl-1'-ylmethyl-7-hydroxy-2-phenyl- quinoline-4-carboxylic acid ((S)-1-phenyl-propyl)amide