CIS-imidazolines

1. A compound of formula

or the pharmaceutically acceptable salts thereof, wherein

R is selected from saturated and unsaturated 5- and 6-membered rings containing at least one hetero atom wherein the hetero atom is selected from S, N or O and said ring being substituted with a lower alkyl which alkyl is further substituted with at least one group selected from —C═O—R 1 , —SO 2 CH 3 , or —CH 2 C═OCH 3 ,

R 1 is selected from the group consisting of hydrogen, —NH 2 , —N-lower alkyl, lower alkyl substituted with hydroxy, lower alkyl substituted with NH 2 , and a 5- or 6-membered saturated ring containing at least one hetero atom selected from S, N and O,

X 1 and X 2 are independently selected from the group consisting of hydrogen, lower alkoxy, —CH 2 OCH 3 , —CH 2 OCH 2 CH 3 , —OCH 2 CF 3 and —OCH 2 CH 2 F,

Y 1 and Y 2 are each independently selected from the group consisting of —Cl, —Br, —NO 2 , —C≡N, and —C≡CH,

and the absolute stereochemistry at the 4 and 5 position of the imidazoline ring are S and R respectively.

2. The compound of claim 1 wherein Y 1 and Y 2 are each independently selected from —Cl and —Br.

3. A compound of the formula

wherein R is piperazinyl substituted with lower alkyl which alkyl is further substituted with at least one group selected from —C═OR 1 , —SO 2 CH 3 , or —CH 2 C═OCH 3 ,

wherein R 1 is selected from hydrogen, —NH 2 , —N-lower alkyl, lower alkyl substituted with hydroxy, lower alkyl substituted with NH 2 ,

X 1 and X 2 are independently selected from the group consisting of hydrogen, lower alkoxy; —CH 2 OCH 3 , —CH 2 OCH 2 CH 3 , —OCH 2 CF 3 and —OCH 2 CH 2 F,

Y 1 and Y 2 are each independently selected from the group consisting of —Cl, —Br, —NO 2 , —C≡N, and —C≡CH

or the pharmaceutically acceptable salts thereof.

4. The compound of claim 3 wherein the X 1 group at ortho position is selected from lower alkoxy, —OCH 2 CF 3 or —OCH 2 CH 2 F, and the X 2 group at para position is lower alkoxy.

5. The compound of claim 4 wherein the X 1 group at ortho position is selected from ethoxy, isopropoxy, —OCH 2 CF 3 or —OCH 2 CH 2 F, and the X 2 group at para position is selected from methoxy or ethoxy.

6. A pharmaceutical composition comprising: a compound of the formula

or the pharmaceutically acceptable salts thereof, wherein

R is selected from saturated and unsaturated 5- and 6-membered rings containing at least one hetero atom wherein the hetero atom is selected from S, N or O and said ring being

substituted with lower alkyl which alkyl is further substituted with at least one group selected from —C═O—R 1 , —SO 2 CH 3 , or —CH 2 C═OCH 3 ,

R 1 is selected from hydrogen, —NH 2 , —NH-lower alkyl, lower alkyl substituted with hydroxy, lower alkyl substituted with NH 2 , or a 5- or 6-membered saturated ring containing at least one hetero atom selected from S, N and O,

X 1 and X 2 are independently selected from the group consisting of hydrogen, lower alkoxy, —CH 2 OCH 3 , —CH 2 OCH 2 CH 3 , —OCH 2 CF 3 and —OCH 2 CH 2 F,

Y 1 and Y 2 are each independently selected from the group consisting of —Cl, —Br, —NO 2 , —C≡N, and —C≡CH, and

the absolute stereochemistry at the 4 and 5 position of the imidazoline ring are S and R respectively; and a pharmaceutically acceptable carrier or excipient.

7. A compound of the formula

wherein R is

piperidinyl substituted with at least one group selected from the group consisting of —SO 2 CH 3 , —C═OCH 2 NH 2 , —C═OCH(OH)CH 2 OH and —C═ON(CH 3 )CH 3 ,

X 1 and X 2 are independently selected from the group consisting of hydrogen, lower alkoxy, —CH 2 OCH 3 , —CH 2 OCH 2 CH 3 , —OCH 2 CF 3 and —OCH 2 CH 2 F,

Y 1 and Y 2 are each independently selected from the group consisting of —Cl, —Br, —NO 2 , —C≡N, and —C≡CH

or the pharmaceutically acceptable salts thereof.