US2002094990A1PendingUtilityA1
Anti-neoplastic, anti-viral or anti-retroviral spermine derivatives
Priority: Dec 2, 1986Filed: Nov 6, 2001Published: Jul 18, 2002
Est. expiryDec 2, 2006(expired)· nominal 20-yr term from priority
Inventors:Raymond J. Bergeron, Jr.
A61K 31/131C07C 211/14A61K 31/506A61K 31/505C07C 209/08A01N 33/04A61K 31/13C07C 209/62A61K 31/785A01N 43/54C07D 239/04A61K 31/135
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Claims
Abstract
The present invention relates to anti-neoplastic and anti-psoriasis pharmaceutical compositions and methods of treatment and to insecticidal compositions and methods of controlling the growth of insects.
Claims
exact text as granted — not AI-modifiedclaims:
1 . A pharmaceutical composition comprising an anti-neoplastic effective amount of a compound having one of the formulae:
R 1 —H 1 H—(CH 2 ) 3 —N 2 H—(CH 2 ) 3 —N 3 H-—(CH 2 ) 4 —N 4 H—(CH 2 ) 3 —N 5 H—(CH 2 ) 3 —N 6 H—R 6 ( II );
Wherein: R 1 and R 6 may be the same or different and are 1I, alkyl or aralkyl having from 1 to 12 carbon atoms;
R 2 -R 5 may be the same or different and are H, R 1 or R 6 ;
R 7 is H, alkyl, aryl or aralkyl having from 1 to 12 carbon atoms;
m is an integer from 3 to 6, inclusive;
n is an integer from 3 to 6, inclusive; or
(IV), a salt thereof with a pharmaceutically acceptable acid; and a pharmaceutically acceptable carrier therefor.
2 . A composition according to claim 1 wherein m is 3 and n is 4.
3 . A composition according to claim 1 wherein m and n are 3.
4 . A composition according to claim 1 wherein m and n are 4.
5 . A composition according to claim 1 wherein R 1 and R 6 are alkyl.
6 . A composition according to claim 1 wherein R 1 and R 6 are aralkyl.
7 . A composition according to claim 1 wherein R 1 and R 6 are methyl.
8 . A composition according to claim 1 wherein R 1 and R 6 are ethyl.
9 . A composition according to claim 1 wherein R 1 and R 6 are propyl.
10 . A composition according to claim 1 wherein R 1 and R 6 are benzyl.
11 . A method of treating a human or non-human animal in need of anti-neoplastic therapy comprising administering to said animal an anti-neoplastic effective amount of a compound having one of the formulae:
R 1 —N 1 H—(CH 2 ) 3 —N 2 H—(CH 2 ) 3 —N 3 H—(CH 2 ) 4 —N 4 H—(CH 2 ) 3 —N 5 H—(CH 2 ) 3 —N 6 H—R 6 ( III )
Wherein: R 1 and R 6 may be the same or different and are H, alkyl or aralkyl having from 1 to 12 carbon atoms, provided that R 1 and R6 are not H;
R 7 is H, alkyl, aryl or aralkyl having from 1 to 12 carbon atoms;
m is an integer from 3 to 6, inclusive;
n is an integer from 3 to 6, inclusive; or
(IV), a salt thereof with a pharmaceutically acceptable acid.
12 . A method according to claim 11 wherein m is 3 and n is 4.
13 . A method according to claim 11 wherein m and n are 3.
14 . A method according to claim 11 wherein m and n are 4.
15 . A method according to claim 11 wherein R 1 and R 6 are alkyl.
16 . A method according to claim 11 wherein R 1 and R 6 are aralkyl.
17 . A method according to claim 11 wherein R 1 and R 6 are methyl.
18 . A method according to claim 11 wherein R 1 and R 6 are ethyl.
19 . A method according to claim 11 wherein R 1 and R 6 are propyl.
20 . A method according to claim 11 wherein R 1 and R 6 are benzyl.
21 . A compound having the formula:
Wherein: R 1 -R 6 may be the same or different and are methyl, propyl, butyl, pentyl, benzyl or β,β, β,-trifluoroethyl;
m is an integer from 3 to 6, inclusive;
n is an integer from 3 to 6, inclusive, or a salt thereof with an acid.
22 . A compound according to claim 21 wherein R 1 and R 6 are propyl.
23 . A compound according to claim 21 wherein R 1 and R 6 are benzyl.
24 . A compound according to claim 21 wherein m is 3and n Is 4.
25 . A compound according to claim 21 wherein m and n are 3.
26 . A compound according to claim 21 wherein m and n are 4.
27 . A compound having the formula:
R 1 —N 1 H—(CH 2 ) 3 —N 2 H—(CH 2 ) 3 N 3 H—(CH 2 ) 4 —N 4 H—(CH 2 ) 3 —N 5 H—(CH 2 ) 3 N 6 H—R 6 ( II ); Wherein: R 1 and R 6 may be the same or different and are alkyl or aralkyl having from 1 to 12 carbon atoms, or a salt thereof with an acid.
28 . A compound according to claim 27 wherein R 1 and R 6 are alkyl.
29 . A compound according to claim 27 wherein R 1 and R 6 are aralkyl.
30 . A compound according to claim 27 wherein R 1 and R 6 are methyl.
31 . A compound according to claim 27 wherein R 1 and R 6 are ethyl.
32 . A compound according to claim 27 wherein R 1 and R 6 are propyl.
33 . A compound according to claim 27 wherein R 1 and, R 6 are benzyl.
34 . A compound having the formula:
Wherein: R 1 and R 6 may be the same or different and are alkyl or aralkyl having from 1 to 12 carbon atoms;
R 7 is H, alkyl aryl or aralkyl having from 1 to 12 carbon atoms;
n is an integer from 3 to 6, inclusive, or a salt thereof with an acid.
35 . A compound according to claim 34 wherein R 1 and R 6 are alkyl.
36 . A compound according to claim 34 wherein R 1 and R 6 are aralkyl.
37 . A compound according to claim 34 wherein R 1 and R 6 are methyl.
38 . A compound according to claim 34 wherein R 1 and R 6 are ethyl.
39 . A compound according to claim 34 wherein R 1 and R 6 are propyl.
40 . A compound according to claim 34 wherein R 1 and R 6 are benzyl.
41 . A compound according to claim 34 wherein n is 3.
42 . A compound according to claim 34 wherein n is 4.
43 . A pharmaceutical composition comprising an anti-viral, anti-psoriasis or anti-retroviral effective amount of a compound having one of the formula:
R 1 —N 1 H—(CH 2 ) 3 —N 2 H—(CH 2 ) 3 —N 3 H—(CH 2 ) 4 —N 4 —(CH 2 ) 3 —N 5 H—(CH 2 ) 3 —N 6 H—R 6 ( II )
Wherein: R 1 and R 6 may be the same or different and are H. alkyl or aralkyl having from 1 to 12 carbon atoms;
R 2 -R 5 may be the same or different and are H, R 1 or R 6 ;
R 7 is H, alkyl, aryl aralkyl having from 1 to 12 carbon atoms;
m is an integer from 3 to 6, inclusive;
n is an integer from 3 to 6, inclusive; or, (IV), a salt thereof
with a pharmaceutically acceptable acid; and a pharmaceutically acceptable carrier therefor.
44 . A method of treating a human or non-human animal in need of anti-viral, anti-psoriasis or anti-retroviral therapy comprising administering to said animal an anti-viral, anti-psoriasis or anti-retroviral effective amount of a compound having one of the formulae:
R 1 —N 1 H—(CH 2 ) 3 —N 2 H—(CH 2 ) 3 —N 3 H—(CH 2 ) 4 —N 4 H—(CH 2 ) 3 —N 5 H—(CH 2 ) 3 —N 6 H—R 6 ( II );
Wherein: R 1 and R 6 may be the same or different and are H, alkyl or aralkyl having from 1 to 12 carbon atoms, provided that R 1 and R 6 are not H;
R 7 is H, alkyl, aryl or aralkyl having from 1 to 12 carbon atoms; m is an integer from 3 to 6, inclusive; and
n is an integer from 3 to 6, inclusive; or (IV), a salt thereof
with a pharmaceutically acceptable acid.
45 . An insecticidal composition comprising, an insecticidably effective amount of a compound having one of the formula:
R 1 —N 1 H—(CH 2 —N 2 H—(CH 2 ) 3 —N 3 H—(CH 2 ) 4 —N 4 H—(CH 2 ) 3 —N 5 H—(CH 2 ) 3 —N 6 H—R 6 ( II ) Wherein: R 1 and R 6 may be the same or different and are H. alkyl or aralkyl having from 1 to 12 carbon atoms; R 2 -R 5 may be the same or different and are H, R 1 or R 6 ; R 7 is H, alkyl, aryl, aralkyl having from 1 to 12 carbon atoms; m is an integer from 3 to 6, inclusive; n is an integer from 3 to 6 inclusive; or (IV), a salt thereof with an acid and a carrier therefor.
46 . A method of controlling the growth of insects comprising administering to said insects an insecticidal effective amount of a compound having one of the formulae:
R 1 —N 1 H—(CH 2 ) 3 —N 2 H—(CH 2 ) 3 —N 3 H—(CH 2 ) 4 —N 4 H—(CH 2 ) 3 —N 5 H—(CH 2 ) 3 —N 6 H—R 6 ( II );
Wherein: R 1 and R 6 may be the same or different and are H, alkyl or aralkyl having from 1 to 12 carbon atoms, provided that R 1 and R 6 are not H;
R 7 is H, alkyl, aryl or aralkyl having from 1 to 12 carbon atoms;
m is an integer from 3 to 6, inclusive; and
n is an integer from 3 to 6, inclusive; or (IV), a salt thereof
with an acid and a carrier therefor.Join the waitlist — get patent alerts
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