Claims
- 1. A compound having the formula ##STR7## a pharmaceutically acceptable acid addition salt thereof or a stereoisomeric form thereof, wherein
- R.sup.1 represents hydrogen or halo;
- R.sup.2 represents halo;
- R.sup.3 represents hydrogen or halo;
- R.sup.4 and R.sup.5 each independently represent hydrogen, C.sub.1-4 alkyl or haloC.sub.1-4 alkyl;
- the group NR.sup.4 R.sup.5 may also be azido, and
- Alk represents C.sub.2-4 alkanediyl.
- 2. A compound according to claim 1 wherein the compound is
- 4-amino-N-[1-[3-(4-fluorophenoxy)propyl]-4-methyl-4-piperidinyl]-5-iodo-2-methoxybenzamide;
- 4-amino-5-chloro-N-[1-[3-(4-fluorophenoxy)propyl]-4-methyl-4-piperidinyl]-2-methoxybenzamide;
- 4-amino-5-bromo-N-[1-[3-(4-fluorophenoxy)propyl]-4-methyl-4-piperidinyl]-2-methoxybenzamide;
- 4-amino-N-[1-[3-(2-bromo-4-fluorophenoxy)propyl]-4-methyl-4-piperidinyl]-5-chloro-2-methoxybenzamide;
- 4-amino-N-[1-[3-(4-fluorophenoxy)propyl]-4-methyl-4-piperidinyl]-2-methoxybenzamide;
- 4-azido-5-chloro-N-[1-[3-(4-fluorophenoxy)propyl]-4-methyl-4-piperidinyl]-2-methoxybenzamide;
- 4-azido-N-[1-[3-(4-fluorophenoxy)propyl]-methyl-4-piperidinyl]-5-iodo-2-methoxybenzamide;
- 4-azido-5-bromo-N-[1-[3-(4-4-fluorophenoxy)propyl]-4-methyl-4-piperidinyl]-2-methoxybenzamide, or a pharmaceutically acceptable acid addition salt thereof.
- 3. A compound according to claim 1 having at least one halo which is a radioactive isotope of iodine, bromine or fluorine.
- 4. A compound according to claim 1 wherein the compound is 4-amino-N-[1-[3-(4-fluorophenoxy)propyl]-4-methyl-4-piperidinyl]-5-iodo-2-methoxybenzamide, [5-.sup.125 I] or [5-.sup.123 I].
- 5. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and as active ingredient a compound as claimed in claim 1 in an amount effective for treating serotonin mediated conditions.
- 6. A process of treating smooth muscle contraction disorders in warm blooded mammals that are related to the excessive release of serotonin, which comprises administering to warm blooded mammals a therapeutically effective amount of a compound as defined in claim 1.
- 7. A process of treating smooth muscle contraction disorders in warm blooded mammals that are related to the excessive release of serotonin, which comprises administering to warm blooded mammals a therapeutically effective amount of a compound as defined in claim 2.
CROSS-REFERENCE TO RELATED APPLICATIONS
This application is based upon PCT application Ser. No. PCT/EP 93/01993, filed Jul. 8, 1993, which claims priority from U.S. patent application Ser. No. 07/914,306, filed on Jul. 17, 1992, now abandoned.
PCT Information
Filing Document |
Filing Date |
Country |
Kind |
102e Date |
371c Date |
PCT/EP93/01993 |
1/6/1995 |
|
|
1/6/1995 |
1/6/1995 |
Publishing Document |
Publishing Date |
Country |
Kind |
WO94/02462 |
2/3/1994 |
|
|
US Referenced Citations (1)
Number |
Name |
Date |
Kind |
4962115 |
Van Daele |
Oct 1990 |
|
Foreign Referenced Citations (1)
Number |
Date |
Country |
2207673 |
Feb 1989 |
GBX |
Non-Patent Literature Citations (4)
Entry |
CA 108;49149t (1988) Moriarty et al., "Inhitition of the effect of serotonin on rat ileal transport by cisapride: evidence in favor of the 5-HT.sub.2 receptors". |
Moriarty et al., "Inhibition of the effect of serotonin on rat ileal transport by cisapride: evidence in favor of the 5-HT.sub.2 receptors. " Gut, 1987, 28, 844-848. |
CA 102: 56714c (1985) Arnt et al., "The Citalopram/5-HTP-induced Head Shade Syndrome is Correlated to 5-HT.sub.2 Recptor Affinity and also Influenced by other Transmitters". |
Arnt et al., "The Citalopram/5-HTP-induced Head Shake Syndrome is Correlated to 5-HT.sub.2 Receptor Affinity and also Influenced by other Transmitters", Acta, Pharmacol. et Toxicol. 1984, 55, 363-372. |
Continuation in Parts (1)
|
Number |
Date |
Country |
Parent |
914306 |
Jul 1992 |
|