US2003236290A1PendingUtilityA1
Inhibitors of animal cell motility and growth
Priority: Jun 12, 2002Filed: Jun 2, 2003Published: Dec 25, 2003
Est. expiryJun 12, 2022(expired)· nominal 20-yr term from priority
C07D 413/06C07D 263/26C07D 413/10A61P 35/00
37
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Claims
Abstract
Cell motility and growth inhibitors, including compounds of the general structural formula and use of the cell motility and cell growth inhibitors, and pharmaceutically acceptable salts, prodrugs, and solvates thereof, as therapeutic agents, are disclosed.
Claims
exact text as granted — not AI-modifiedWhat is claimed is:
1 . A compound having a formula
wherein R 1 is selected from the group consisting of C(═O)C 3-8 cycloalkenyl, C(═O)C≡C—R b ,
C 2-6 alkenyl, and C 2-6 alkynyl;
R 2 is selected from the group consisting of hydro, C 1-3 alkyl, aryl, heteroaryl, C 1-3 alkylenearyl, C 1-3 alkyleneheteroaryl, C 3-8 cycloalkyl, and C 3-8 heterocycloalkyl;
R 3 is selected from the group consisting of hydro, C 1-3 alkyl, aryl, and heteroaryl;
R a is selected from the group consisting of hydro and C 1-3 alkyl;
R b is selected from the group consisting of hydro, C 1-6 alkyl, CF 3 , C 3-8 cycloalkyl, C 3-8 heterocycloalkyl, aryl, heteroaryl, S-aryl, O-aryl, C 1-3 alkylenearyl, and C 1-3 alkyleneheteroaryl;
R c is selected from the group consisting of hydro, C 1-3 alkyl, and fluoroC 1-3 alkyl, or
R b and R c can be taken together with the carbons to which they attached to form a five- or six-membered aliphatic ring, optionally containing one or two heteroatoms selected from oxygen, nitrogen, and sulfur;
R d , independently, is selected from the group consisting of hydro, C 1-3 alkyl, and fluoroC 1-4 alkyl; and
n is a number 0, 1, or 2, and
pharmaceutically acceptable salts, prodrugs, or hydrates thereof.
2 . The compound of claim 1 having a structure
3 . The compound of claim 1 having a structure
4 . The compound of claim 1 having a structure
5 . The compound of claim 1 wherein R 3 is hydro, C 1-3 alkyl, and aryl; R 2 is selected from the group consisting of hydro, C 1-3 alkyl, aryl, C 1-3 alkylenearyl, or heteroaryl; R 1 is selected from the group consisting of C(═O)C 3-8 cycloalkenyl, C(═O)C≡C—R b , and
R a is hydro or C 1-3 alkyl; R b is selected from the group consisting of hydro, C 1-6 alkyl, C 3-8 cycloalkyl, CF 3 , aryl, heteroaryl, and S-aryl; R c is H or C 1-3 alkyl; and n is 0 or 1.
6 . The compound of claim 1 wherein R 3 is selected from the group consisting of hydro and phenyl; R 2 is selected from the group consisting of benzyl, hydro, isopropyl, methyl, and phenyl; R 1 is selected from the group consisting of C(═O)C≡C—CH 3 and
R a is hydro and methyl; R b is selected from the group consisting of hydro, methyl, ethyl, trifluoromethyl, phenyl, pyridyl, naphthyl, thiophenyl, furyl, thienyl, cyclopentyl, and pentyl; R c is hydro and trifluoromethyl; or R a and R c are taken together with the carbons to which they are attached to form a cyclohexenyl ring; R d is selected from the group consisting of hydro, methyl, and CH 2 CF 3 ; and n is 0 or 1.
7 . The compound of claim 1 wherein R 3 is hydro or phenyl; R 2 is selected from the group consisting of benzyl, hydro, isopropyl, phenyl, and methyl; and R 1 is selected from the group consisting of —C(═O)CH═CHCH 3 ,
8 . The compound of claim 1 having a structure
9 . A compound of claim 1 having a biological IC 50 value of about 50 μM or less.
10 . A compound identified as compound 1, compounds 4-7, compounds 9 and 10, and compounds 12-73, as disclosed herein,
and pharmaceutically acceptable salts, prodrugs, or solvates thereof.
11 . A pharmaceutical composition comprising a compound of claim 1 together with a pharmaceutically acceptable diluent or carrier.
12 . A method of treating a male or female animal for a condition where inhibition of animal cell motility and cell growth is of a therapeutic benefit comprising administering to said animal an effective amount of a pharmaceutical composition comprising a compound of claim 1 , and a pharmaceutically acceptable diluent or carrier.
13 . The method of claim 12 wherein the inhibition is reversible.
14 . The method of claim 12 wherein the condition is a cancer.
15 . A method of treating a condition where inhibition of cell motility and cell growth is of therapeutic benefit, in a human or a nonhuman animal body, comprising administering to said body a therapeutically effective amount of a compound of claim 1 .
16 . A method of treating a male or female animal suffering from a condition where inhibition of cell motility and cell growth is of a therapeutic benefit comprising administering a therapeutically effective amount of (a) a compound of claim 1 , and (b) a second therapeutically active ingredient used in a treatment of the condition.
17 . The method of claim 16 wherein (a) and (b) are administered simultaneously or sequentially.
18 . The method of claim 16 wherein the condition is a cancer.
19 . The method of claim 18 wherein the second therapeutically active ingredient is a chemotherapeutic agent or radiation.
20 . A kit for the treatment of cancer comprising a compound of claim 1 or a composition containing the same, packaged with instructions for administration of the compound, or the composition, to a mammal to treat the cancer.
21 . The kit of claim 19 wherein the mammal is a human subject.Join the waitlist — get patent alerts
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