US2001031761A1PendingUtilityA1
Derivatives of camptothecin and methods of treating cancer using these derivatives
Priority: Jan 30, 1996Filed: Dec 26, 2000Published: Oct 18, 2001
Est. expiryJan 30, 2016(expired)· nominal 20-yr term from priority
C07D 491/22A61K 31/47A61K 31/4745A61P 35/00
48
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Claims
Abstract
Derivatives of camptothecin are disclosed and are represented by the general formula: wherein when R 2 is H, R 1 is a C 2 -C 4 alkyl group, a C 6 -C 15 alkyl group, a C 3 -C 8 cycloalkyl group, a C 2 -C 15 alkenyl group or a C 2 -C 15 epoxy group; and when R 2 is a nitro group, R 1 is a C 1 -C 15 alkyl group, a C 2 -C 15 alkenyl group, a C 3 -C 8 cycloalkyl group, or an epoxy group. Processes for making these derivatives and for using them in cancer treatment are also disclosed.
Claims
exact text as granted — not AI-modifiedWhat is claimed is:
1 . A compound of formula (I):
wherein R 1 is a C 2 -C 4 alkyl group, a C 6 -C 15 alkyl group, a C 3 -C 8 cycloalkyl group, a C 2 -C 15 alkenyl group or a C 2 -C 15 epoxy group when R 2 is H; and R 1 is a C 1 -C 15 alkyl group, a C 3 -C 8 cycloalkyl group, a C 2 -C 15 alkenyl group or a C 2 -C 15 epoxy group when R 2 is NO 2 .
2 . The compound of claim 1 , wherein R 1 is a linear C 2 -C 4 alkyl group or C 6 -C 15 alkyl group when R 2 is H and R 1 is a linear C 1 -C 15 alkyl group when R 2 is NO 2 .
3 . The compound of claim 1 , wherein R 1 is a linear C 2 -C 15 alkenyl group.
4 . The compound of claim 1 , wherein R 1 is a C 2 -C 15 epoxy group.
5 . A compound of claim 2 , wherein R 2 is H.
6 . The compound of claim 2 , wherein R 2 is NO 2 .
7 . The compound of claim 3 , wherein R 2 is H.
8 . The compound of claim 3 , wherein R 2 is NO 2 .
9 . The compound of claim 4 , wherein R 2 is H.
10 . The compound of claim 4 , wherein R 2 is NO 2 .
11 . The compound of claim 2 , wherein R 1 is a linear ethyl, propyl, butyl, hexyl or octyl group, and R 2 is H.
12 . The compound of claim 11 , wherein R 1 is ethyl.
13 . The compound of claim 2 , wherein R 1 is a linear methyl, ethyl or propyl group and R 2 is NO 2 .
14 . The compound of claim 13 , wherein R 1 is ethyl.
15 . The compound of claim 1 , wherein R 1 is a C 3 -C 8 cycloalkyl group.
16 . The compound of claim 15 , wherein R 2 is H.
17 . The compound of claim 15 , wherein R 2 is NO 2 .
18 . The compound of claim 1 , wherein R 2 is H, and R 1 is
19 . The compound of claim 1 , wherein R 2 is NO 2 , and R 1 is
20 . A method for treating a malignant tumor in a patient comprising administering a composition comprising an effective amount of the compound of claim 1 , wherein said malignant tumor is responsive to said composition.
21 . The method of claim 20 , wherein R 1 is a linear C 2 -C 4 alkyl group or a C 6 -C 15 alkyl group where R 2 is H and R 1 is a linear C 1 -C 15 alkyl group when R 2 is NO 2 .
22 . The method of claim 20 , wherein R 1 is a linear C 2 -C 15 alkenyl group.
23 . The method of claim 20 , wherein R 1 is a C 2 -C 15 epoxy group.
24 . The method of claim 21 , wherein R 2 is H.
25 . The method of claim 21 , wherein R 2 is NO 2 .
26 . The method of claim 22 , wherein R 2 is H.
27 . The method of claim 22 , wherein R 2 is NO 2 .
28 . The method of claim 23 , wherein R 2 is H.
29 . The method of claim 23 , wherien R 2 is NO 2 .
30 . The method of claim 21 , wherein R 1 is a linear ethyl, propyl, butyl, hexyl or octyl group, and R 2 is H.
31 . The method of claim 30 , wherein R 1 is ethyl.
32 . The method of claim 21 , wherein R 1 is a linear methyl, ethyl or propyl group and R 2 is NO 2 .
33 . The method of claim 32 , wherein R 1 is ethyl.
34 . The method of claim 20 , wherein R 1 is a C 3 -C 8 cycloalkyl group.
35 . The method of claim 34 , wherein R 2 is H.
36 . The method of claim 34 , wherein R 2 is NO 2 .
37 . The method of claim 20 , wherein R 2 is H, and R 1 is
38 . The method of claim 20 , wherein R 2 is NO 2 , and R 1 isJoin the waitlist — get patent alerts
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