Claims
- 1. A method of treating Irritable Bowel Syndrome in mammals comprising administering to a mammal in need of treatment therefor an effective dose of a compound of formula I ##STR11## wherein: R is hydrogen, C.sub.1 -C.sub.3 alkyl, allyl, or ##STR12## R.sup.1 is hydrogen, C.sub.1 -C.sub.3 alkyl, allyl, ##STR13## or (CH.sub.2).sub.n --X; n is 1 to 5;
- X is an optionally substituted phenyl, C.sub.1 -C.sub.3 alkoxy, or C.sub.1 -C.sub.3 alkylthio;
- R.sup.2 and R.sup.3 are independently hydrogen, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.3 alkylthio, halo, CN, phenyl; or together are --(CH.sub.2).sub.p --;
- p is 3 to 6;
- Y is --CH.sub.2 --, --O--, --SO.sub.m --;
- m is 0, 1, or 2;
- or a pharmaceutically acceptable acid addition salt or solvate thereof.
- 2. The method according to claim 1 wherein the mammal is a human.
- 3. The method according to claim 2 wherein the compound is one in which R is C.sub.1 -C.sub.3 alkyl, or ##STR14##
- 4. The method according to claim 3 wherein the compound is one in which R is propyl.
- 5. The method according to claim 4 wherein the compound is one in which R.sup.1 is C.sub.1 -C.sub.3 alkyl, or ##STR15##
- 6. The method according to claim 5 wherein the compound is one in which R.sup.1 is propyl.
- 7. The method according to claim 6 wherein the compound is one in which R.sup.2 and R.sup.3 are independently hydrogen, C.sub.1 -C.sub.3 alkyl, or together are --(CH.sub.2).sub.p.
- 8. The method according to claim 6 wherein the compound is one in which R.sup.2 and R.sup.3 are independently hydrogen or methyl.
- 9. The method according to claim 7 wherein the compound is one in which R.sup.2 and R.sup.3 are together --(CH.sub.2).sub.p.
- 10. The method according to claim 2 wherein the compound is one in which Y is --CH.sub.2 --.
- 11. The method according to claim 10 wherein the compound is one in which R is C.sub.1 -C.sub.3 alkyl or ##STR16##
- 12. The method according to claim 11 wherein the compound is one in which R is propyl.
- 13. The method according to claim 10 wherein the compound is one in which R.sup.1 is C.sub.1 -C.sub.3 alkyl or ##STR17##
- 14. The method according to claim 13 wherein the compound is one in which R.sup.1 is propyl.
- 15. The method according to claim 10 wherein the compound is one in which R and R.sup.1 are both propyl.
- 16. The method according to claim 10 wherein the compound is one in which R.sup.2 and R.sup.3 are independently hydrogen or C.sub.1 -C.sub.3 alkyl.
- 17. The method according to claim 10 wherein the compound is one in which R.sup.2 and R.sup.3 are together --(CH.sub.2).sub.p.
- 18. The method according to claim 16 wherein the compound is one in which R is C.sub.1 -C.sub.3 alkyl or ##STR18##
- 19. The method according to claim 18 wherein the compound is one in which R is propyl.
- 20. The method according to any of claim 16 wherein the compound is one in which R.sup.1 is C.sub.1 -C.sub.3 alkyl or ##STR19##
- 21. The method according to claim 20 wherein the compound is one in which R.sup.1 is propyl.
- 22. The method according to claim 15 wherein the compound is one in which R.sup.2 and R.sup.3 are independently hydrogen or C.sub.1 -C.sub.3 alkyl.
- 23. The method according to claim 15 wherein the compound is one in which R.sup.2 and R.sup.3 are together --(CH.sub.2).sub.p.
- 24. The method according to claim 2 wherein the compound is one in which Y is --O--.
- 25. The method according to claim 24 wherein the compound is one in which R is C.sub.1 -C.sub.3 alkyl or ##STR20##
- 26. The method according to claim 24 wherein the compound is one in which R.sup.1 is C.sub.1 -C.sub.3 alkyl or ##STR21##
- 27. The method according to claim 24 wherein the compound is one in which R.sup.2 and R.sup.3 are independently hydrogen or C1-C3 alkyl.
- 28. The method according to claim 2 wherein the compound is one in which Y is --SOm--.
- 29. The method according to claim 28 wherein the compound is one in which R is C.sub.1 -C.sub.3 alkyl or ##STR22##
- 30. The method according to claim 1 wherein the compound is a d-isomer.
- 31. The method according to claim 30 wherein the compound is one in which R.sup.1 is C.sub.1 -C.sub.3 alkyl or ##STR23##
- 32. The method according to claim 30 wherein the compound is one in which R.sup.2 and R.sup.3 are independently hydrogen or C.sub.1 -C.sub.3 alkyl.
- 33. The method according to claim 22 wherein the compound is selected from the group consisting of
- 8-(isoxazol-5-yl)-2-dipropylamino-1,2,3,4-tetrahydronaphthalene;
- 8-(4-methylisoxazol-5-yl)-2-dipropylamino-1,2,3,4-tetrahydronaphthalene; and
- 8-(3-methylisoxazol-5-yl)-2-dipropylamino-1,2,3,4-tetrahydronaphthalene.
- 34. The method according to claim 1 wherein the compound is an l-isomer.
- 35. The method according to claim 1 wherein the compound is S-(-)-8-(isoxazol-5-yl)-2-dipropylamino-1,2,3,4-tetrahydronaphthalene or a pharmaceutically acceptable acid addition salt or solvate thereof.
- 36. The method according to claim 1 wherein the compound is R-(+)-8-(isoxazol-5yl)-2-dipropylamino-1,2,3,4-tetrahydronaphthalene or a pharmaceutically acceptable acid addition salt or solvate thereof.
- 37. The method according to claim 1 wherein the compound is R-(+)-8-(4-methylisoxazol-5-yl)-2-dipropylamino-1,2,3,4-tetrahydronaphthalene or a pharmaceutically acceptable acid addition salt or solvate thereof.
- 38. A method for treating Irritable Bowel Syndrome in mammals which comprises administering to a mammal in need of treatment thereof an effective dose of a compound which is both a 5-HT.sub.1A agonist and an M.sub.1 -cholinergic receptor selective agent.
- 39. A method of claim 38 wherein the compound employed is of the formula ##STR24## wherein R is hydrogen, C.sub.1 -C.sub.3 alkyl, allyl, or cyclopropylmethyl;
- R.sup.1 is hydrogen, C.sub.1 -C.sub.3 alkyl, allyl, cyclopropylmethyl, or (CH.sub.2).sub.n --X;
- n is 1 to 5;
- X is an optionally substituted phenyl, C.sub.1 -C.sub.3 alkoxy, or C.sub.1 -C.sub.3 alkylthio;
- R.sup.2 and R.sup.3 are independently hydrogen, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.3 alkylthio, halo, CN, phenyl; or together are --(CH.sub.2).sub.p --;
- p is 3 to 6;
- Y is --CH.sub.2 --, --O--, or --SO.sub.m --;
- m is 0, 1 or 2;
- or a pharmaceutically acceptable acid addition salt or solvate thereof.
Parent Case Info
This application is a continuation of application Ser. No. 07/916,281, filed on Jul. 17, 1992, now abandoned.
US Referenced Citations (2)
Number |
Name |
Date |
Kind |
5096908 |
Gidda et al. |
Mar 1992 |
|
5158956 |
Gidda et al. |
Oct 1992 |
|
Foreign Referenced Citations (1)
Number |
Date |
Country |
0339982 |
Nov 1990 |
EPX |
Continuations (1)
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Number |
Date |
Country |
Parent |
916281 |
Jul 1992 |
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