2-alkylbenzoxazole carboxamides as 5-HT

1. A compound of formula

wherein

R 1 , R 2 and R 3 are independently selected from hydrogen, halogen, amino, alkylamino, dialkylamino, acylamino, morpholinyl, —O-loweralkyl, hydroxy, loweralkyl, fluoroloweralkyl, —O-lowerfluoroalkyl, methylenedioxy, ethylenedioxy, alkoxy-loweralkyl and hydroxyloweralkyl;

R 4 is a residue chosen from:

(i) a saturated nitrogen heterocycle or methyl-substituted saturated nitrogen heterocycle, in which said nitrogen is tertiary, said heterocycle containing at least one 5 or 6-membered ring; and

(ii) an imidazolylalkyl residue wherein the imidazole of said imidazolylalkyl is optionally substituted with up to three groups chosen from halogen, (C 1 -C 4 )alkyl, substituted (C 1 -C 4 )alkyl and NH 2 ; and

R 10 is chosen from the group consisting of

(i) hydrogen;

(ii) (C 1 -C 10 )alkyl;

(iii) substituted (C 1 -C 10 )alkyl;

(iv) saturated C-attached heterocyclyl; and

(v) substituted, saturated C-attached heterocyclyl.

2. A compound of formula I

according to claim 1 .

3. A compound of formula II

according to claim 1 .

4. A compound according to claim 1 wherein R 4 is chosen from:

wherein

m is 1, 2, 3 or 4;

n is 0, 1, 2, 3 or 4;

Q is N(CH 3 ) or —O—; and

R 5 is hydrogen or methyl.

5. A compound according to claim 4 , wherein R 4 is chosen from quinuclidine, tropane, azabicyclo[3.3.1]nonane, methyl azabicyclo[3.3.1]nonane and dimethyl diazabicyclo[3.3.1]nonane.

6. A compound according to claim 1 , wherein R 1 , R 2 and R 3 are hydrogen.

7. A compound according to claim 1 , wherein one of R 1 , R 2 and R 3 is halogen.

8. A compound according to claim 1 , wherein R 10 is chosen from the group consisting of hydrogen and (C 1 to C 3 )alkyl.

9. A compound according to claim 1 , wherein R 10 is chosen from the group consisting of (C 4 to C 10 )alkyl and substituted (C 1 -C 10 )alkyl.

10. A compound according to claim 9 , wherein R 10 is chosen from

11. A compound according to claim 1 , wherein R 10 is chosen from the group consisting of saturated, C-attached, nitrogenous heterocyclyl; and substituted, saturated, C-attached, nitrogenous heterocyclyl.

12. A compound according to claim 1 , wherein R 10 is chosen from the group consisting of saturated, C-attached, oxygen heterocyclyl; and substituted, saturated, C-attached, oxygen heterocyclyl.

13. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound according to claim 1 .

14. A pharmaceutical composition according to claim 13 additionally comprising a second antiemetic agent.

15. A pharmaceutical composition according to claim 14 , wherein said second antiemetic agent is a neurokinin antagonist.

16. A pharmaceutical composition according to claim 13 additionally comprising a corticosteroid.