Claims
- 1. A method of treating an indication related to calcium overload in brain cells of mammals, including humans, in a subject in need thereof, which comprises the step of administering to the said subject a calcium overload blocking amount of a piperidine compound having the formula I ##STR23## wherein R.sup.3 is 3,4-methylenedioxyphenyl, aryl having up to twelve carbon atoms, inclusive, which are optionally substituted with one or more halogen, C.sub.1-6 -alkoxy, aryloxy oraryl-C.sub.1-6 -alkoxy, cyano, mono or poly halogenated C.sub.1-6 -alkyl, C.sub.1-6 -alkenyl, C.sub.1-6 -alkyl, or C.sub.3-5 -alkylene groups,
- R.sup.1 is straight or branched C.sub.1-8 -alkyl unsubstituted or substituted with one or more cyano, carboxylic ester, dialkylamino, hydroxy, --CONH.sub.2, halogeno, C.sub.1-8 -alkoxy or C.sub.3-8 cycloalkyl groups,
- X is hydrogen, halogen, trifluoromethyl, hydroxy, cyano or C.sub.1-8 -alkoxy,
- Y is O or S;
- provided that R.sup.1 is not unsubstituted C.sub.1-8 -alkyl, C.sub.1-6 -alkoxy-C.sub.1-8 -alkyl or C.sub.3-8 -cycloalkyl-C.sub.1-8 -alkyl, when R.sup.3 is 3,4-methylenedioxyphenyl or aryl optionally substituted with one or more C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, C.sub.3-5 -alkylene, C.sub.3-8 -cycloalkyl or aralkoxy, and at the same time X is hydrogen or halogen or a salt thereof with a pharmaceutically-acceptable acid.
- 2. A method of claim 1 wherein R.sup.3 is 3,4-methylenedioxyphenyl, optionally substituted with halogen or C.sub.1-6 -alkoxy, or phenyl substituted with C.sub.3-5 -alkylene.
- 3. A method of claim 1 wherein R.sup.1 is straight or branched C.sub.1-8 -alkyl.
- 4. A method of claim 1 wherein X is hydrogen, halogen, trifluoromethyl or C.sub.1-6 -alkoxy.
- 5. A method of claim 1 wherein R.sup.3 is 3,4-methylene dioxyphenyl, optionally substituted with halogen or C.sub.1-6 -alkoxy, or phenyl substituted with C.sub.3-5 -alkylene, and R.sup.1 is straight or branched C.sub.1-8 -alkyl, and x is hydrogen, halogen, trifluoromethyl or C.sub.1-6 -alkoxy.
- 6. A method of claim 1 wherein the compound is (-)-trans-3-(2-bromo-4,5-methylenedioxyphenoxymethyl)-1-butyl-4-(4-fluorophenyl)-piperidine hydrochloride.
- 7. A method of claim 1 wherein the compound is (-)-trans-4-(4-methoxyphenyl)-3-(3,4-methylenedioxyphenoxymethyl)-1-pentylpiperidine oxalate.
- 8. A method of claim 1 wherein the compound is (+)-trans-4-(4-methoxyphenyl)-3-(3,4-methylenedioxyphenoxymethyl)-1-pentyl-piperidine oxalate.
- 9. A method of claim 1 wherein the compound is (+-)-trans-3-(3,4-methylenedioxyphenoxymethyl)-1-pentyl-4-(3-trifluoromethylphenyl)-piperidine hydroxide.
- 10. A method of claim 1 wherein the compound is (+)-trans-3-(2-bromo-4,5-methylenedioxyphenoxymethyl)-4-(4-fluorophenyl)-1-pentylpiperidine hydrochloride.
- 11. A method of claim 1 wherein the compound is (+-)-trans-3-(3,4-methylenedioxyphenoxymethyl)-1-pentyl-4-(4-pentyloxyphenyl)-piperidine hydrochloride.
- 12. A method of claim 1 wherein the compound is (+-)-trans-3-(4-allyl-2-methoxyphenoxymethyl)-1-butyl-4-phenylpiperidine oxalate.
- 13. A method of claim 1 wherein the treatment is directed to the treatment of ischaemia or head injury.
Priority Claims (3)
Number |
Date |
Country |
Kind |
5232/86 |
Nov 1986 |
DKX |
|
3234/87 |
Jun 1987 |
DKX |
|
2310/88 |
Apr 1988 |
DKX |
|
Parent Case Info
The present application is a continuation-in-part of our prior-filed co-pending U.S. application Ser. No. 106,154, filed Oct. 8, 1987, now U.S. Pat. No. 4,877,799 issued Oct. 31, 1989.
US Referenced Citations (2)
Number |
Name |
Date |
Kind |
3912743 |
Christensen et al. |
Oct 1975 |
|
4007196 |
Christensen et al. |
Feb 1977 |
|
Foreign Referenced Citations (1)
Number |
Date |
Country |
61-180769 |
Aug 1986 |
JPX |
Continuation in Parts (1)
|
Number |
Date |
Country |
Parent |
106154 |
Oct 1987 |
|