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US 5,344,830 AGranted
N,N-diacylpiperazine tachykinin antagonists
AssigneeMerck & Co., Inc.
InventorsSander G. Mills, Richard J. Budhu, Conrad P. Dorn, William J. Greenlee, Malcolm MacCoss, Mu T. Wu
Life of this patent
Estimating the term…
Abstract
Diacylpiperazines of general structure ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, and asthma, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
Claims4
A compound which is selected from the group consisting of:
- 1) 4-(N,N-di-n-pentylcarbamoyl)-1-(N,N -diphenyl-carbamoyl)-N-[3-(4-morpholinyl)propyl]-2-piperazinecarboxamide;
- 2) 4-(N,N-di-n-pentylcarbamoyl)-1-(N,N-diphenyl-carbamoyl)-N-[2-(4-morpholiny l)ethyl]-2-piperazinecarboxamide;
- 3) 4-(N,N-di-n-pentylcarbamoyl)-1-(N,N-diphenyl-carbamoyl)-N-[2-(1-piperidiny l)ethyl]-2-piperazinecarboxamide;
- 4) 4-(N,N-di-n-pentylcarbamoyl)-1-(N,N-diphenyl-carbamoyl)-N-[2-(acetamido)et hyl]-2-piperazinecarboxamide;
- 5) 4-(N,N-di-n-pentylcarbamoyl)-1-(N,N-diphenyl-carbamoyl)-N-[2-(N'-benzyl-N' -methylamino)-ethyl]-N-methyl-2-piperazinecarboxamide;
- 6) 4-(N,N-di-n-pentylcarbamoyl)-1-(N,N-diphenyl-carbamoyl)-N-[3-(benzyloxycar bonyl)propyl]-N-methyl-2-piperazinecarboxamide;
- 7) 4-(N,N-di-n-pentylcarbamoyl)-1-(N,N-diphenyl-carbamoyl)-N-[2-[(N'-(3,5-dim ethylphenyl)-methyl-(N'-methyl)amino]ethyl]-N-methyl-2-piperazinecarboxamid e;
- 8) 4-(N,N-di-n-pentylcarbamoyl)-1-(N,N-diphenyl-carbamoyl)-N-[2-[(N'-[3,5-di- (trifluoro-methyl)phenyl]methyl)-(N'-methyl)amino]ethyl]-N-methyl-2-piperaz inecarboxamide;
- 9) 4-(N,N-di-n-pentylcarbamoyl)-1-(N,N-diphenyl-carbamoyl)-N-[2-[(N'-(2-metho xyphenyl)-methyl)-(N'-methyl) amino]ethyl]-N-methyl-2-piperazinecarboxamide;
- 10) 4-(N,N-di-n-pentylcarbamoyl)-1-(N,N-diphenyl-carbamoyl)-N-[2-(N'-[(1,1-dim ethyl)ethoxy-carbonyl]-(N'-methyl)aminoethyl]-N-methyl-2-piperazinecarboxam ide;
- 11) (S)-2-(2-(N-(2-methoxybenzyl)amino)ethylaminocarbonyl)-4-(N,N-di-n-pentylc arbamoyl)-1-(N,N-diphenylcarbamoyl)-piperazine;
- 12) 2-(2-(N-methyl-N-(2-methoxybenzyl)amino)-ethylamino-carbonyl)-4-(N,N-di-n- pentylcarbamoyl)-1-(N,N-diphenylcarbamoyl)piperazine;
- 13) (S)-2-(2-(1-piperidinyl)ethylaminocarbonyl)-1-[N-(3-chlorophenyl)-N-phenyl carbamoyl]-4-(N,N-di-n-pentylcarbamoyl)piperazine;
- 14) (S)-2-(2-(1-piperidinyl)ethylaminocarbonyl)-4-(N,N-di-n-pentylcarbamoyl)-1 -(N,N-diphenyl-carbamoyl)piperazine;
- 15) (S)-2-(2-(N,N-bis(2-methoxybenzyl)amino)-ethylamino-carbonyl)-1-(N,N-diphe nylcarbamoyl)-4-(N,N-di-n-pentylcarbamoyl)piperazine;
- 16) (S)-4-(N,N-di-n-pentylcarbamoyl)-1-(N,N-diphenyl-carbamoyl)-2-(2-(4-morpho linyl)ethylaminocarbonyl)-piperazine;
- 17) (S)-2-(2-(N-benzyl-N-methylamino)-N-(methyl)ethylaminocarbonyl)-4-(N,N-di- n-pentylcarbamoyl)-1-(N,N-diphenylcarbamoyl)piperazine;
- 18) (S)-1-(N-(3-chlorophenyl)-N-phenylcarbamoyl)-2-(2-(N-methyl-N(2-methoxyben zyl)amino)-ethylaminocarbonyl)-4-(N,N-di-n-pentylcarbamoyl)piperazine;
- 19(S)-1-(N-(3,5-dimethylphenyl)-N-phenylcarbamoyl)-2-(2-(N-methyl-N-(2-meth oxybenzyl)-amino)ethylaminocarbonyl)-4-(N,N-di-n-pentyl-carbamoyl)piperazin e;
- 20) (S)-1-(N-(3,5-dichlorophenyl)-N-phenylcarbamoyl)-2-(2-(N-methyl-N-(2-metho xybenzyl)-amino)ethylaminocarbonyl)-4-(N,N-di-n-pentyl-carbamoyl)piperazine
- 21) (S)-4-(N,N-di-n-pentylcarbamoyl)-1-(N,N-diphenyl-carbamoyl)-2-(2-N-(benzyl oxycarbonylmethyl)amino)-ethylaminocarbonyl)piperazine;
- 22) (S)-4-(N,N-di-n-pentylcarbamoyl)-1-(N,N-diphenyl-carbamoyl)-2-(2-N-(benzyl oxycarbonylmethyl)-N-methylamino)ethylaminocarbonyl)piperazine;
- or a pharmaceutically acceptable salt thereof.
20 more elements
A compound which is selected from the group consisting of:
- 1) 2-[2-((N-[2-(N'-benzyl -N'-methyl)aminoethyl])-N -methyl)aminoethyl]-4-(N,N-di-n-pentyl-carbamoyl)-1-(N,N-diphenylcarbamoyl )-piperazine;
- 2) 2-[2-(N,N-dibenzylamino)ethyl]-4-(N,N-di-n-pentyl-carbamoyl)-1-(N,N-diphen ylcarbamoyl)-piperazine;
- 3) 2-[2-(N -[2-phenylethyl]amino)ethyl]-4-(N,N -di-n-pentylcarbamoyl)-1-(N,N-diphenyl-carbamoyl)piperazine;
- 4) 2-[2-(N-benzylamino)ethyl]-4-(N,N-di-n-pentylcarbamoyl)-1-(N,N-diphenylcar bamoyl)-piperazine;
- 5) 2-[2-(N -[4-phenylbutyl]amino)ethyl]-4-(N,N-di-n-pentylcarbamoyl)-1-(N,N-diphenyl- carbamoyl)piperazine;
- 6) 4-(N,N-di-n-pentylcarbamoyl)-1-(N,N-diphenyl-carbamoyl)-2-(2-(3-phenylprop ylamino)ethyl)-piperazine;
- 7) 4-(N,N-di-n-pentylcarbamoyl)-1-(N,N-diphenyl-carbamoyl)-2-(2-(2-(2-methoxy phenyl)ethylamino)ethyl)piperazine;
- 8) 2-(2-(2-(3,5-di-methylphenyl)ethylamino)ethyl)-4-(N,N -di-n-pentylcarbamoyl)-1-(N,N-di-phenylcarbamoyl)piperazine;
- or a pharmaceutically acceptable salt thereof.
6 more elements
Dependencies are inferred from the claim text.