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US 2007/0161692 A1Published application
Conformationally restricted polyamine analogs as disease therapies
AssigneeCellgate, Inc.
InventorsBenjamin Frydman, Linda Clifford, Laurence Marton, Venodhar Reddy, Aldonia Valasinas, Andrei Blokhin, Hirak Basu
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Abstract
Novel conformationally restricted polyamine analogs are provided, as well as compositions comprising these novel polyamine analogs. Methods of using the novel polyamine analogs in treatment of diseases such as cancer are also provided. Also provided is a method of delivering these analogs specifically to tumor cells by covalently attaching polyamine analogs to porphyrin compounds, along with novel polyamine-porphyrin covalent conjugates.
Claims24
A conformationally restricted polyamine analog of the formula:
- E-NH—B-A-B—NH—B-A-B—NH—B-A-B—NH—B-A-B—NH-E
- wherein each A is independently selected from the group consisting of:
- a single bond, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C3-C6 cycloaryl, and C3-C6 cycloalkenyl;
- each B is independently selected from the group consisting of:
- a single bond, C1-C6 alkyl, and C2-C6 alkenyl;
- and each E is independently selected from the group consisting of H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C3-C6 cycloaryl, and C3-C6 cycloalkenyl;
- with the proviso that either at least one A moiety is selected from the group consisting of C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C3-C6 cycloaryl, and C3-C6 cycloalkenyl, or at least one B moiety is selected from the group consisting of C2-C6 alkenyl;
- and any salt or stereoisomer thereof.
5 more elements
A conformationally restricted polyamine analog of the formula:
- E-NH—B-A-B—NH—B-A-B—NH—B-A-B—NH(—B-A-B—NH)x-E
- wherein each A is independently selected from the group consisting of:
- a single bond, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C3-C6 cycloaryl, and C3-C6 cycloalkenyl;
- each B is independently selected from the group consisting of:
- a single bond, C1-C6 alkyl, and C2-C6 alkenyl;
- each E is independently selected from the group consisting of H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C3-C6 cycloaryl, and C3-C6 cycloalkenyl;
- and x is an integer from 2 to 16;
- with the proviso that either at least one A moiety is selected from the group consisting of C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C3-C6 cycloaryl, and C3-C6 cycloalkenyl, or at least one B moiety is selected from the group consisting of C2-C6 alkenyl;
- and any salt or stereoisomer thereof.
6 more elements
A polyamine analog of the formula:
- E-NH—B-A-B—NH—B-A-B—NH—B-A-B—NH(—B-A-B—NH)x-E
- wherein each A is independently selected from the group consisting of:
- a single bond, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C3-C6 cycloaryl, and C3-C6 cycloalkenyl;
- each B is independently selected from the group consisting of:
- a single bond, C1-C6 alkyl, and C2-C6 alkenyl;
- each E is independently selected from the group consisting of C1-C6 alkyl, C1-C6 alkanol, C3-C6 cycloalkanol, and C3-C6 hydroxyaryl,
- with the proviso that at least one E moiety be selected from the group consisting of C1-C6 alkanol, C3-C6 cycloalkanol, and C3-C6 hydroxyaryl;
- and x is an integer from 0 to 16;
- and any salt or stereoisomer thereof.
6 more elements
A conformationally restricted polyamine analog of the formula:
- E-N H-D-NH—B-A-B—NH-D-NH-E
- wherein each A is selected from the group consisting of C2-C6 alkynyl;
- each B is independently selected from the group consisting of:
- a single bond, C1-C6 alkyl, and C2-C6 alkenyl;
- each D is independently selected from the group consisting of C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C3-C6 cycloalkenyl, and C3-C6 cycloaryl;
- and
- each E is independently selected from the group consisting of H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C3-C6 cycloaryl, and C3-C6 cycloalkenyl;
- and any salt or stereoisomer thereof.
5 more elements
A conformationally restricted polyamine analog of the formula:
- E-NH—B-A-B—NH—F—NH—B-A-B—N H-E
- wherein F is selected from the group consisting of C1-C6 alkyl;
- each A is independently selected from the group consisting of:
- a single bond, C1-C6 alkyl;
- C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C3-C6 cycloaryl, and C3-C6 cycloalkenyl;
- each B is independently selected from the group consisting of:
- a single bond, C1-C6 alkyl, and C2-C6 alkenyl;
- and
- each E is independently selected from the group consisting of H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C3-C6 cycloaryl, and C3-C6 cycloalkenyl;
- with the proviso that either at least one A moiety is selected from the group consisting of C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C3-C6 cycloaryl, and C3-C6 cycloalkenyl, or at least one B moiety is selected from the group consisting of C2-C6 alkenyl;
- and any salt or stereoisomer thereof.
8 more elements
A conformationally restricted polyamine analog of the formula:
- wherein A is independently selected from the group consisting of:
- a single bond, C1-C6 alkyl;
- C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C3-C6 cycloaryl, and C3-C6 cycloalkenyl;
- each B is independently selected from the group consisting of:
- a single bond, C1-C6 alkyl, and C2-C6 alkenyl;
- with the proviso that A and both B moieties are not all a single bond;
- and any salt or stereoisomer thereof.
4 more elements
A conformationally restricted polyamine analog of the formula:
- E-NH-D-NH—B-A-B—NH-D-NH-E
- wherein A is selected from the group consisting of C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C3-C6 cycloalkenyl, and C3-C6 cycloaryl;
- each B is independently selected from the group consisting of:
- a single bond, C1-C6 alkyl, and C2-C6 alkenyl;
- each D is independently selected from the group consisting of C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C3-C6 cycloalkenyl, and C3-C6 cycloaryl;
- and
- each E is independently selected from the group consisting of H and C1-C6 alkyl;
- with the proviso that either at least one A moiety is selected from the group consisting of C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C3-C6 cycloaryl, and C3-C6 cycloalkenyl, or at least one B moiety is selected from the group consisting of C2-C6 alkenyl;
- and the proviso that at least one E is selected from the group consisting of H or methyl;
- and any salt or stereoisomer thereof.
7 more elements
A conformationally restricted polyamine analog of the formula:
- wherein A is trans-ethene
- each B is independently selected from the group consisting of:
- a single bond, C1-C6 alkyl, and C2-C6 alkenyl;
- each D is independently selected from the group consisting of C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C3-C6 cycloaryl, and C3-C6 cycloalkenyl, with the proviso that D is not C3 alkyl;
- and
- each E is independently selected from the group consisting of H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C3-C6 cycloaryl, and C3-C6 cycloalkenyl;
- and any salt thereof.
4 more elements
24-31. (canceled)
Dependencies are inferred from the claim text.