Claims
- 1. A method for treating hyperlipidemia comprising administering, to a host afflicted with hyperlipidemia, an effective hyperlipidemia treating amount of a carboxamide compound represented by the following formula: ##STR124## wherein R.sup.1 and R.sup.2 each represents hydrogen, C.sub.1-15 alkyl, C.sub.3-8 cycloalkyl, diphenyl-C.sub.1-6 alkyl, or the following formula: ##STR125## wherein R.sup.5, R.sup.6 and R.sup.7 each represents hydrogen, halogen, nitro, C.sub.1-6 alkoxy, C.sub.1-6 alkoxy-carbonyl, C.sub.1-6 alkyl, halogen-substituted C.sub.1-6 alkyl, cyano, carbonyl or hydroxyl; A represents C.sub.1-4 alkylene; and l represents 0 or 1; wherein
- R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a heterocyclic group or a heterocyclic group containing additional heteroatom(s) selected from the group consisting of a nitrogen atom and an oxygen atom, wherein said heterocyclic group is unsubstituted or substituted with C.sub.1-6 alkyl, phenyl-C.sub.1-6 alkyl, phenyl, or substituted phenyl having substituent(s) selected from the group consisting of the group consisting of C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen and halogen-substituted C.sub.1-6 alkyl;
- R.sup.3 represents hydrogen, C.sub.1-15 alkyl or phenyl-C.sub.1-6 alkyl; R.sup.4 represents C.sub.1-6 alkyl or phenyl; and X represents oxygen or sulfur.
- 2. The method for treating hyperlipidemia according to claim 1, wherein R.sup.1 and R.sup.2 each represents hydrogen, C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl or the following formula: ##STR126## wherein R.sup.5, R.sup.6 and R.sup.7 each represents hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen-substituted C.sub.1-6 alkyl, cyano or nitro; A represents C.sub.1-4 alkylene; l represents 0 or 1; R.sup.3 represents hydrogen; and R.sup.4 represents C.sub.1-6 alkyl.
- 3. The method for treating hyperlipidemia according to claim 2, wherein R.sup.1 and R.sup.2 each represents hydrogen, C.sub.1-6 alkyl or the following formula: ##STR127## wherein R.sup.5, R.sup.6 and R.sup.7 each represents hydrogen, halogen, C.sub.1-6 alkyl, halogen-substituted C.sub.1-6 alkyl, or cyano; A represents C.sub.1-4 alkylene; l represents 0 or 1; R.sup.3 represents hydrogen; and R.sup.4 represents C.sub.1-6 alkyl.
- 4. The method for treating hyperlipidemia according to claim 3, wherein R.sup.1 represents hydrogen.
- 5. The method for treating hyperlipidemia according to claim 3, wherein R.sup.1 represents unsubstituted phenyl-C.sub.1-4 alkylene or substituted phenyl-C.sub.1-4 alkylene having halogen atom(s) as the substituent(s) on the phenyl ring.
- 6. The method for treating hyperlipidemia according to claim 3, wherein R.sup.1 represents C.sub.1-6 alkyl.
- 7. The method for treating hyperlipidemia according to claim 4, wherein said carboxamide compound is selected from the group consisting of:
- 4-diethoxyphosphinoylmethyl-N-phenylbenzamide;
- 4-diethoxyphosphinoylmethyl-N-(4-chlorophenyl)-benzamide;
- 4-diethoxyphosphinoylmethyl-N-(4-bromophenyl)-benzamide;
- 4-diethoxyphosphinoylmethyl-N-(4-iodophenyl)-benzamide;
- 4-diethoxyphosphinoylmethyl-N-(4-fluorophenyl)-benzamide;
- 4-diethoxyphosphinoylmethyl-N-(4-trifluoromethylphenyl)benzamide;
- 4-diethoxyphosphinoylmethyl-N-(cyanophenyl)-benzamide;
- 4-diethoxyphosphinoylmethyl-N-(3,4-diclorophenyl)-benzamide; and
- 4-diethoxyphosphinoylmethyl-N-(4-chloro-3-trifluoromethylphenyl)benzamide.
- 8. The method for treating hyperlipidemia according to claim 5, wherein said carboxamide compound is selected from the group consisting of:
- 4-diethoxyphosphinoylmethyl-N-benzyl-N-(4-chlorophenyl)benzamide;
- 4-diethoxyphosphinoylmethyl-N-(4-chlorobenzyl)-N-(4-chlorophenyl)benzamide;
- 4-diethoxyphosphinoylmethyl-N-benzyl-N-(4-trifluorophenyl)benzamide;
- 4-diethoxyphosphinoylmethyl-N-benzyl-N-(3,4-dichlorophenyl)benzamide;
- 4-diethoxyphosphinoylmethyl-N-benzyl-N-(4-chlorobenzyl-N-(3,4-dichlorophenyl)benzamide; and
- 4-diethoxyphosphinoylmethyl-N-benzyl-N-(4-chloro-3-methylphenyl)benzamide.
- 9. The method for treating hyperlipidemia according to claim 6, wherein said carboxamide compound is selected from the group consisting of:
- 4-diethoxyphosphinoylmethyl-N-methyl-N-phenylbenzamide; and
- 4-diethoxyphosphinoylmethyl-N-(4-chlorophenyl)-N-methylbenzamide.
- 10. The method for treating hyperlipidemia according to claim 2, wherein said carboxamide compound is consisting from the group consisting of:
- 4-diethoxyphosphinoylmethyl-N-(4-methylphenyl)-benzamide;
- 4-diethoxyphosphinoylmethyl-N-(4-methoxyphenyl)-benzamide;
- 4-diethoxyphosphinoylmethyl-N-(4-nitrophenyl)-benzamide;
- 4-diethoxyphosphinoylmethyl-N-(2-phenylethyl)benzamide;
- 4-diethoxyphosphinoylmethyl-N-(4-chlorophenyl-N'-cyclopentylbenzamide; and
- 4-diethoxyphosphinoylmethyl-N-benzyl-N-(4-nitrophenyl)benzamide.
- 11. The method for treating hyperlipidemia according to claim 3, wherein R.sup.1 represents hydrogen, R.sup.2 represents the following formula: ##STR128## wherein R.sup.5, R.sup.6 and R.sup.7 each represents hydrogen, halogen or cyano, provided that when any one of R.sup.5, R.sup.6 and R.sup.7 represents hydrogen, the remaining two substituents are halogen and cyano, respectively, wherein one of the substituents is bonded at the 4-position of the phenyl ring; R.sup.3 represents hydrogen; R.sup.4 represents ethyl, and l represents O.
- 12. The method for treating hyperlipidemia according to claim 11, wherein said carboxamide compound is selected from the group consisting of:
- 4-diethoxyphosphinoylmethyl-N-(4-bromo-2-cyanophenyl)benzamide;
- 4-diethoxyphosphinoylmethyl-N-(4-chloro-2-cyanophenyl)benzamide;
- 4-diethoxyphosphinoylmethyl-N-(4-cyano-2 -chlorophenyl)benzamide;
- 4-diethoxyphosphinoylmethyl-N-(4-iodo-2-cyanophenyl)benzamide;
- 4-diethoxyphosphinoylmethyl-N-(4-cyano-2-bromophenyl)benzamide; and
- 4-diethoxyphosphinoylmethyl-N-(4-bromo-3-cyanophenyl)benzamide;
- 4-diethoxyphosphinoylmethyl-N-(4-cyano-2-iodophenyl)benzamide.
Priority Claims (2)
Number |
Date |
Country |
Kind |
61-313267 |
Dec 1986 |
JPX |
|
62-317246 |
Dec 1987 |
JPX |
|
CROSS REFERENCE TO RELATED APPLICATION
This is a continuation-in-part of application Ser. No. 07/139,234, Dec. 29, 1987 pending.
US Referenced Citations (8)
Foreign Referenced Citations (5)
Number |
Date |
Country |
0015370 |
Sep 1980 |
EPX |
0016310 |
Oct 1980 |
EPX |
0211346 |
Feb 1987 |
EPX |
0273444 |
Jul 1988 |
EPX |
61-151199 |
Jul 1986 |
JPX |
Non-Patent Literature Citations (4)
Entry |
Merck Manual, 14th edition, 1982, pp. 970-977. |
Chem Abstracts 106:67489s, Tsuda et al. (1986). |
Kluger et al., J. Amer. Chem. Soc., 95:2362-2364 (1973). |
Kluger et al., J. Amer. Chem. Soc., 98:4913-4917 (1976). |
Continuation in Parts (1)
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Number |
Date |
Country |
Parent |
139234 |
Dec 1987 |
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