Claims
- 1. A compound of formula ##STR22## or a pharmaceutically acceptable salt thereof wherein R.sup.1 is straight or branched, saturated or unsaturated alkyl of from 10 to 22 carbon atoms or adamantyl ethyl;
- R.sup.2 is a straight or branched, saturated or unsaturated alkyl of from 1 to 5 carbon atoms, a cycloalkylmethyl radical having 5 to 7 carbon atoms in the cycloalkyl ring, phenyl, phenylalkyl with 1 to 5 carbon atoms in the straight or branched alkyl chain which phenyl is unsubstituted or substituted by halogen, hydroxyl, alkyl of from 1 to 5 carbon atoms, alkoxy of from 1 to 5 carbon atoms, dialkylamino having of from 1 to 5 carbon atoms, benzyloxy, or R.sup.2 is an aminoalkyl of formula ##STR23## wherein R.sup.4 and R.sup.5, are each independently hydrogen, alkyl of from 1 to 3 carbon atoms and m is an integer of from 2 to 5;
- n is an integer of from 1 to 5; and
- R.sup.3 is ##STR24## wherein R.sup.11 and R.sup.12, are each independently hydrogen, alkyl of from 1 to 3 carbon atoms, phenyl, phenylalkyl with from 1 to 5 carbon atoms in the straight or branched alkyl chain, X is oxygen, or ##STR25## wherein R.sup.13 is hydrogen, phenyl, phenylalkyl, diphenylalkyl with from 1 to 5 carbon atoms in the straight or branched alkyl chain, or X is ##STR26## wherein R.sup.14 is hydrogen, phenyl which is unsubstituted or substituted by halogen, hydroxyl, alkyl from 1 to 5 carbon atoms, alkoxy of from 1 to 5 carbon atoms, dialkylamino having of from 1 to 5 carbon atoms or benzyloxy and R.sup.15 is hydrogen, hyrdoxyl, cyano, hydroxymethyl, aminomethyl, carboxamido, ethoxy or methoxycarbonyl and p and q, are each independently 2.
- 2. A compound of formula ##STR27## or a pharmaceutically acceptable salt thereof wherein R.sup.1 is straight or branched, saturated or unsaturated alkyl of from 1 to 22 carbon atoms or adamantylethyl;
- R.sup.2 is a straight or branched alkyl having from 1 to 4 carbon atoms, cycloalkylmethyl, unsubstituted phenyl, phenylalkyl with from 1 to 5 carbon atoms in the straight or branched alkyl chain which phenyl is monosubstituted by halogen, hydroxyl, methyl, benzyloxy, methoxy or dimethylamino;
- n is an integer of from 1 to 3; and
- R.sup.3 is ##STR28## in which R.sup.11 and R.sup.12, are each independently hydrogen or methyl, X is an amino radical of formula ##STR29## in which R.sup.13 is hydrogen, phenyl, phenylalkyl, or diphenylalkyl with from 1 to 5 carbon atoms in the straight or branched alkyl chain or X is formula ##STR30## in which R.sup.14 is phenyl, R.sup.15 is cyano or aminomethyl, and p and q are each 2.
- 3. A compound of formula ##STR31## or a pharmaceutically acceptable salt thereof wherein n is 1, 2 or 3;
- R.sup.1 is a decyl, tetradecyl, eicosanyl, octadecenyl, octadecyl, 2-octyldecyl or adamantylethyl;
- R.sup.2 is a propyl, methyl, phenyl, benzyl, methylbenzyl, chlorobenzyl, methoxybenzyl, cyclohexylmethyl, dimethylaminobenzyl, dimethylaminopropyl, benzyloxybenzyl, benzyloxyphenyl, phenylethyl, hydroxybenzyl or hydroxyphenyl; and
- R.sup.3 is methoxycarbonylmethyl piperazino, benzylpiperazino, diphenylmethylpiperazino, aminomethylphenylpiperidino, phenylpiperazino, phenylethylpiperazino, pyrimidinylpiperazino or methylpiperazino.
- 4. A compound selected from
- 1-[(1-Benzyl-5-octadecyloxy-4(1H)-pyridon-2-yl)-methyl]-4-cyano-4-cyano-4-phenylpiperidine dihydrochloride,
- 1-[(1-Benzyl-5-octadecyloxy-4(1H)-pyridon-2-yl)-methyl]-4-methoxycarbonyl-2-methyl-piperazine dihydrochloride 3/4hydrate,
- 1-[(1-Benzyl-5-octadecyloxy-4(1H)-pyridon-2-yl)-methyl]-4-piperazine,
- 1-[(1-Benzyl-5-octadecyloxy-4(1H)-pyridon-2-yl)-methyl]-4-diphenylmethylpiperazine sesquixalate monohydrate,
- 1-[(1-Benzyl-5-octadecyloxy-4(1H)-pyridon-2-yl)-methyl]-4-phenylpiperidine.dihydrochloride.H.sub.2 O,
- 1-[(1-Benzyl-5-octadecyloxy-4(1H)-pyridon-2-yl)-methyl]-4-(2-pyrimidinyl)piperazine,
- 1-[(1-Benzyl-5-octadecyloxy-4(1H)-pyridon-2-yl)-methyl]-4-benzylpiperazine.dioxalate.1/2H.sub.2 O,
- 1-[(1-Benzyl-5-octadecyloxy-4(1H)-pyridon-2-yl)-methyl]-4-(2-phenylethyl)piperzine.trihydrochloride.1/2H.sub.2 O,
- 1-[(1-Benzyl-5-octadecyloxy-4(1H)-pyridon-2-yl)-methyl]-4-(2-phenylethyl)piperidine.dihydrochloride,
- (.+-.)-1-[(1-Benzyl-5-ocatdecyloxy-4(1H)-pyridone-2-yl)-methyl]-4-(1-phenylethyl)-piperazine.trihydrochloride 3/4H.sub.2 O,
- (.+-.)-1-[(5-Octadecyloxy-1-(1-phenylethyl)-4(1H)-pyridone-2-yl)-methyl]-4-benzylpiperazine,
- (-)-1-[(5-Octadecyloxy-1-(1-phenylethyl)-4(1H)-pyridone-2-yl)-methyl]-4-benzylpiperazine,
- (+)-1-[(5-Octadecyloxy-1-(1-phenylethyl)-4(1HO-pyridone-2-yl)-methyl]-4-benzylpiperazine,
- 1-[(1-Benzyl-5-octadecyloxy-4(1H)-pyridon-2-yl)-methyl]-4-aminoethyl-4-phenylpiperidine trihydrochloride, and
- (.+-.)-1-[(1-Benzyl-5-octadecyloxy-4(1H)-pyridon-2-yl)methyl]-2-methylpiperazine fumarate.
- 5. A pharmaceutical composition for treating and/or preventing heart and blood vessel diseases comprising an effective amount of a compound according to claim 1 in admixture with a pharmaceutically acceptable carrier.
- 6. A method for treating and/or preventing heart and blood vessel diseases which comprises administering to a mammal in need of such treatment a pharmaceutical composition according to claim 5.
Priority Claims (1)
| Number |
Date |
Country |
Kind |
| 3826846 |
Aug 1988 |
DEX |
|
CROSS REFERENCE TO RELATED APPLICATION
This is a division of U.S. application Ser. No. 07/640,407, filed Jan. 28, 1991, now U.S. Pat. No. 5,185,352.
US Referenced Citations (1)
| Number |
Name |
Date |
Kind |
|
2965641 |
Krimmel |
Dec 1960 |
|
Foreign Referenced Citations (6)
| Number |
Date |
Country |
| 554715 |
Mar 1958 |
CAX |
| 978958 |
Dec 1975 |
CAX |
| 0120670 |
Mar 1984 |
EPX |
| 3826846 |
Feb 1990 |
DEX |
| 110674 |
Jun 1984 |
JPX |
| 110675 |
Jun 1984 |
JPX |
Non-Patent Literature Citations (2)
| Entry |
| Imafuru et al. Bulletin of the Chemical Society of Japan, vol. 52, No. 1, 1979, pp. 107-110. |
| Looker et al., Journal of Heterocyclic Chemistry, vol. 23, No. 5, 1986, pp. 5-8. |
Divisions (1)
|
Number |
Date |
Country |
| Parent |
640407 |
Jan 1991 |
|
Patent Grant
5322844
