申请人:Kelliher Adam
公开号:US20120122982A1
公开(公告)日:2012-05-17
The present invention provides use of compounds which are polyunsaturated fatty acid (PUFA) derivatives of formula (I), in the form of racemates, stereoisomers or mixtures of stereoisomers, or pharmaceutically acceptable salts, or solvates thereof, wherein -AIk- is —(CH
2
)
4
—CH(OR
2
)-[trans]CH═CH-[cis]CH═CH—, —(CH
2
)
4
-[cis]CH═CH-[trans]CH═CH—CH(OR
2
)—, —CH(OR
2
)-[trans]CH═CH-[cis]CH═CH—CH
2
-[cis]CH═CH—(CH
2
)
3
—, —(CH
2
)
3
—CH(OR
2
)-[trans]CH═CH-[cis]CH═CH—CH
2
-[cis]CH═CH—, or —(CH
2
)
3
-[cis]CH═CH—CH
2
-[cis]CH═CH-[trans]CH═CH—CH(OR
2
)—; R
1
is a hydrogen atom; or R
1
is a C
1
-C
6
alkyl, C
2
-C
6
alkenyl, C
2
-C
6
alkynyl, C
6
-C
10
aryl, 5- to 10-membered heteroaryl, C
3
-C
7
carbocyclyl or 5- to 10-membered heterocyclyl group; or R
1
is a group of formula —CH
2
—CH(OR
3
)—CH
2
—(OR
4
), wherein R
3
and R
4
are each independently hydrogen atoms or —(C═O)—R
6
, wherein R
6
is an aliphatic group having from 3 to 29 carbon atoms; or R
1
is a group of formula —(CH
2
OCH
2
)
m
OH, wherein m is an integer of from 1 to 200; or R
1
is a drug moiety; each R
2
is the-same or different- and each independently represents a hydrogen atom; or a group —(C═O)—R
5
, wherein R
5
is a C
1
-C
6
alkyl, C
2
-C6 alkenyl, C
2
-C
6
alkynyl, C
6
-C
10
aryl, 5- to 10-membered heteroaryl, C
3
-C
7
carbocyclyl or 5- to 10-membered heterocyclyl group, or R
5
is an aliphatic group having from 3 to 29 carbon atoms, or R
5
is a drug moiety; or a group of formula —(CH
2
OCH
2
)
n
OH, wherein n is an integer of from 1 to 200; or a drug moiety; and wherein said alkyl, alkenyl, alkynyl and aliphatic groups are the same or different and are each unsubstituted or substituted with 1, 2 or 3 unsubstituted substituents which are the same or different and are selected from halogen atoms and C
1
-C
4
alkoxy, C
2
-C
4
alkenyloxy, C
1
-C
4
haloalkyl, C
2
-C
4
haloalkenyl, C
1
-C
4
haloalkoxy, C
2
-C
4
haloalkenyloxy, hydroxyl, —SR′, and —NR′R″ groups where R′ and R″ are the same or different and represent hydrogen or unsubstituted C
1
-C
2
alkyl; said aryl, heteroaryl, carbocyclyl and heterocyclyl groups are the same or different and are each unsubstituted or substituted by 1, 2, 3 or 4 unsubstituted substituents which are the same or different and are selected from halogen atoms, and cyano, nitro, C
1
-C
4
alkyl, C
1
-C
4
alkoxy, C
2
-C
4
alkenyl, C
2
-C
4
alkenyloxy, C
1
-C
4
haloalkyl, C
2
-C
4
haloalkenyl, C
1
-C
4
haloalkoxy, C
2
-C
4
haloalkenyloxy, hydroxyl, C
1
-C
4
hydroxyalkyl, —SR′ and —NR′R″ groups wherein each R′ and R″ is the same or different and represents hydrogen or unsubstituted C
1
-C
4
alkyl; in the manufacture of a medicament for use in treating or preventing nerve damage in a mammal.