Claims
- 1. A compound of the formula: ##STR19## wherein A is a saturated hydrocarbon chain interrupted by from 1 to 4 cyclopropanyl groups of the formula ##STR20## said A being of from 7 to 23 carbon atoms plus one additional carbon atom for each cyclopropanyl group; and
- R is:
- (a) an aralkyl radical of the structure ##STR21## wherein g is 0 or 1; wherein
- R.sup.1 is a hydrogen atom, halo having an atomic weight of from about 19 to 80, alkoxy having from 1 to 3 carbon atoms; or alkyl having from 1 to 3 carbon atoms;
- R.sup.2 is a hydrogen atom, alkyl having from 1 to 3 carbon atoms, alkoxy having from 1 to 3 carbon atoms, or halo having an atomic weight of from about 19 to 36; and
- R.sup.3 is (i) a hydrogen atom, a phenyl radical of the structure (ii) ##STR22## wherein y is a hydrogen atom, halo having an atomic weight of from about 19 to 80, alkoxy having from 1 to 3 carbon atoms, or alkyl having from 1 to 3 carbon atoms; and
- y' is a hydrogen atom, alkoxy having from 1 to 3 carbon atoms, alkyl having from 1 to 3 carbon atoms, or halo having an atomic weight of from about 19 to 36; or
- a benzyl radical of the formula (iii) ##STR23## wherein y and y' are as defined above; or (iv) alkyl having from 1 to 8 carbon atoms;
- or R is:
- (b) a phenyl radical of the structure ##STR24## wherein R.sup.2 is as defined above, and R.degree. is a hydrogen atom, halo having an atomic weight of from about 19 to 80, alkyl having from 1 to 3 carbon atoms; alkoxy having from 1 to 3 carbon atoms; or a radical of the structure R.sup.f : ##STR25## in which B is --CH.sub.2 -- or --O--;
- f is 0 or 1; and
- Q is a hydrogen atom, halo having an atomic weight of from about 19 to 80, alkoxy having from 1 to 3 carbon atoms, or alkyl having from 1 to 3 carbon atoms;
- or R is:
- (c) an indolyl radical of the structure: ##STR26## wherein R.sup.1 is as defined above, and
- R.sup.5 is a hydrogen atom, alkyl having from 1 to 8 carbon atoms or benzyl (unsubstituted);
- or R is
- (d) a benzocycloalkyl nucleus of the structure: ##STR27## wherein R.sup.1 and R.sup.2 are as defined above; and
- j is a whole integer of from 1 to 4.
- 2. A compound of claim 1 in which R is a type (a).
- 3. A compound of claim 1 in which R is of type (b).
- 4. A compound of claim 1 in which R is of type (c).
- 5. A compound of claim 1 in which R is of type (d).
- 6. A compound of claim 2 in which g is 0.
- 7. A compound of claim 2 in which g is 1.
- 8. A compound of claim 2 in which R.sup.3 is of type (iii).
- 9. A compound of claim 3 in which R.sup.1 is a radical of the structure ##STR28## in which B, f and Q are as defined.
- 10. A compound of claim 1 wherein A is a cyclopropanyl-bearing hydrocarbon radical of the formula: ##STR29## wherein n is a whole integer of from 1 to 15; m is 1 or 2; and p is a whole integer of from 1 to 13, provided that when m is 1, then n+p is from 3 to 19, and when m is 2 then n+p is from 2 to 16.
- 11. A compound of claim 10 in which m is 1.
- 12. A compound of claim 10 in which m is 2.
- 13. A compound of claim 11 in which n is 7 and p is 6.
- 14. The compound of claim 13 which is cis-2-octylcyclopropanoctanoic acid, 2-(o-methylphenyl)hydrazide.
- 15. The compound of claim 13 which is cis-2-octylcyclopropanoctanoic acid, 2-[.alpha.-(p-methylbenzyl)-p-methylphenylethyl]hydrazide.
- 16. A compound of claim 12 in which n is 4 and p is 6.
- 17. The compound of claim 16 which is cis,cis-2-[(2-pentylcyclopropyl)-methyl]-cyclopropanoctanoic acid, 2-(o-methylphenyl)hydrazide.
- 18. A compound of claim 10 in which the hydrogen atoms of each cyclopropanyl group are in the cis configuration.
- 19. A method of reducing the cholesterol ester content of an arterial wall, in a mammal in need of such treatment, comprising administering a cholesterol ester-reducing amount of a compound of claim 1 to said mammal.
- 20. A pharmaceutical composition suitable for reducing the cholesterol ester content of an arterial wall of a mammal comprising a cholesterol ester-reducing effective amount of a compound of claim 1 and a nontoxic pharmaceutically-acceptable carrier.
- 21. A composition of claim 20 in solid form.
- 22. A composition of claim 20, in which the compound is present in an amount of from about 25 to 2,500 milligrams.
- 23. A composition of claim 22 in which the compound is cis-2-octyl-cyclopropanoctanoic acid, 2-(o-methylphenyl)-hydrazide.
- 24. A method of claim 19 in which the compound is cis-2-octyl-cyclopropanoctanoic acid, 2-(o-methylphenyl)-hydrazide.
- 25. A composition of claim 22 in which the compound is cis-2-octyl-cyclopropanoctanoic acid, 2-[N-.alpha.-(p-methylbenzyl)-p-methyl-phenylethyl]-hydrazide.
- 26. A method of claim 19 in which the compound is cis-2-octyl-cyclopropanoctanoic acid, 2-[N-.alpha.-(p-methylbenzyl)-p-methyl-phenylethyl]-hydrazide.
- 27. The compound of claim 13 which is cis-2-octyl-cyclopropanoic acid, 2-benzyl-hydrazide.
Priority Claims (1)
Number |
Date |
Country |
Kind |
2856856 |
Dec 1978 |
DEX |
|
Parent Case Info
This is a continuation-in-part of copending application Ser. No. 881,781 filed Feb. 27, 1978 now abandoned.
US Referenced Citations (3)
Non-Patent Literature Citations (1)
Entry |
Sumitomo Chemical Co., Derwert Report 027430R. |
Continuation in Parts (1)
|
Number |
Date |
Country |
Parent |
881781 |
Feb 1978 |
|