US2020360366A1PendingUtilityA1
Prolylhydroxylase/atf4 inhibitors and methods of use for treating neural cell injury or death and conditions resulting therefrom
Est. expiryDec 12, 2033(~7.4 yrs left)· nominal 20-yr term from priority
A61K 31/4709A61P 25/00A61K 31/47
57
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Claims
Abstract
Methods for treating a patient suffering from neural cell injury, the method comprising administering to the patient an effective amount of a HIE prolyl-4-hydroxylase inhibiting compound having the following general formula (1) wherein R 1 is a cyclic group containing at least three and up to seven carbon atoms and optionally containing one or more heteroatoms selected from O, N, and S, and optionally attached to the shown carbon atom by a linking group; R 2 is independently selected from said cyclic groups of R 1 and a cyclic hydrocarbon groups R 5 containing up to twenty carbon atoms; R 3 is selected from hydrogen atom and hydrocarbon groups containing up to six carbon atoms; R 6 and R 7 are independently selected from hydrogen atom, hydrocarbon groups containing up to three carbon atoms, halogen atom, and polar groups, as well as methylene-linked versions thereof; and t is 0 or 1.
Claims
exact text as granted — not AI-modified1 . A method for treating a patient suffering from spinal cord injury, the method comprising administering to said patient an effective amount of a HIF prolyl-4-hydroxylase inhibiting compound having the following general formula:
wherein:
R 1 is a cyclic group containing at least three and up to seven ring carbon atoms and optionally containing one or more ring heteroatoms selected from O, N, and S, wherein said cyclic group is optionally substituted with one or more groups selected from —R 4 , —C(O)R 4 , —NR 4 2 , —OR 4 , NO 2 , —C(O)NR 4 2 , —NR 4 C(O)R 4 , —C(O)OR 4 , —OC(O)R 4 , —OC(O)NR 4 2 , —NR 4 C(O)NR 4 2 , —NR 4 C(O)OR 4 , —SO 2 R 4 , nitrile, and halogen atom, wherein R 4 is, independently, hydrogen atom or acyclic hydrocarbon group containing up to six carbon atoms, and wherein said cyclic group is optionally attached to the shown carbon atom by a linking group;
R 2 is independently selected from said cyclic groups of R 1 and acyclic hydrocarbon groups R 5 containing up to twelve carbon atoms, wherein said cyclic group is optionally attached to the shown carbon or nitrogen atom by a linking group;
R 3 is selected from hydrogen atom and hydrocarbon groups containing up to six carbon atoms;
R 2 and R 3 are optionally interconnected;
R 6 and R 7 are independently selected from hydrogen atom, hydrocarbon groups containing up to three carbon atoms, halogen atom, and polar groups selected from —C(O)R 4 , —NR 4 2 , —OR 4 , —NO 2 , —C(O)NR 4 2 , —NR 4 C(O)R 4 , —C(O)OR 4 , —OC(O)R 4 , —OC(O)NR 4 2 , —NR 4 C(O)NR 4 2 , —NR 4 C(O)OR 4 , —SO 2 R 4 , and nitrile, as well as methylene-linked versions thereof; and
t is 0 or 1.
2 . The method of claim 1 , wherein said HIF prolyl-4-hydroxylase inhibiting compound inhibits ATF-4.
3 .- 5 . (canceled)
6 . The method of claim 3 , wherein said HIF prolyl-4-hydroxylase inhibiting compound decreases edema.
7 . (canceled)
8 . The method of claim 1 , wherein said patient suffering from spinal cord injury exhibits somatosensory, sensorimotor, or motor improvement after treatment with said HIF prolyl-4-hydroxylase inhibiting compound.
9 . The method of claim 1 , wherein R 1 is a carbocyclic ring that is unfused or fused with another ring.
10 . The method of claim 9 , wherein said carbocyclic ring is a phenyl ring.
11 . The method of claim 1 , wherein R 1 is a heterocyclic ring that is unfused or fused with another ring.
12 . The method of claim 11 , wherein said heterocyclic ring contains one or two ring nitrogen atoms.
13 . The method of claim 1 , wherein R 2 is selected from cyclic groups of R 1 optionally attached via a linking group.
14 . The method of claim 13 , wherein R 2 is a heterocyclic ring that is unfused or fused with another ring.
15 . The method of claim 13 , wherein R 2 is a carbocyclic ring that is unfused or fused with another ring.
16 . The method of claim 1 , wherein R 2 is selected from acyclic hydrocarbon groups R 5 containing up to twelve carbon atoms.
17 . The method of claim 16 , wherein said acyclic hydrocarbon groups are alkyl groups.
18 . The method of claim 16 , wherein said acyclic hydrocarbon groups contain up to six carbon atoms.
19 . The method of claim 1 , wherein R 6 and R 7 are independently selected from hydrogen atom and hydrocarbon groups containing up to three carbon atoms.
20 . The method of claim 1 , wherein R 3 is hydrogen.
21 . The method of claim 1 , wherein t is 1.
22 . The method of claim 1 , wherein t is 0.
23 . A method for treating a patient suffering from neural cell injury, the method comprising administering to said patient an effective amount of a HIF prolyl-4-hydroxylase inhibiting compound having the following general formula:
wherein:
R 1 is a cyclic group containing at least three and up to seven ring carbon atoms and optionally containing one or more ring heteroatoms selected from O, N, and S, wherein said cyclic group is optionally substituted with one or more groups selected from —R 4 , —C(O)R 4 , —NR 4 2 , —OR 4 , NO 2 , —C(O)NR 4 2 , —NR 4 C(O)R 4 , —C(O)OR 4 , —OC(O)R 4 , —OC(O)NR 4 2 , —NR 4 C(O)NR 4 2 , —NR 4 C(O)OR 4 , —SO 2 R 4 , nitrile, and halogen atom, wherein R 4 is, independently, hydrogen atom or acyclic hydrocarbon group containing up to six carbon atoms, and wherein said cyclic group is optionally attached to the shown carbon atom by a linking group;
R 2 is independently selected from said cyclic groups of R 1 and acyclic hydrocarbon groups R 5 containing up to twelve carbon atoms, wherein said cyclic group is optionally attached to the shown carbon or nitrogen atom by a linking group;
R 3 is selected from hydrogen atom and hydrocarbon groups containing up to six carbon atoms;
R 2 and R 3 are optionally interconnected;
R 6 and R 7 are independently selected from hydrogen atom, hydrocarbon groups containing up to three carbon atoms, halogen atom, and polar groups selected from —C(O)R 4 , —NR 4 2 , —OR 4 , —NO 2 , —C(O)NR 4 2 , —NR 4 C(O)R 4 , —C(O)OR 4 , —OC(O)R 4 , —OC(O)NR 4 2 , —NR 4 C(O)NR 4 2 , —NR 4 C(O)OR 4 , —SO 2 R 4 , and nitrile, as well as methylene-linked versions thereof; and
t is 0 or 1.
24 . The method of claim 23 , wherein said HIF prolyl-4-hydroxylase inhibiting compound inhibits ATF-4.
25 . The method of claim 23 , wherein said method treats a patient suffering from brain injury.
26 . The method of claim 25 , wherein said brain injury is mild traumatic brain injury.
27 . The method of claim 25 , wherein said brain injury is associated with intracerebral hemorrhage.
28 . The method of claim 25 , wherein said HIF prolyl-4-hydroxylase inhibiting compound decreases edema.
29 . The method of claim 23 , wherein said method treats a patient suffering from spinal cord injury.
30 . The method of claim 23 , wherein said patient suffering from neural cell injury exhibits somatosensory, sensorimotor, or motor improvement after treatment with said HIF prolyl-4-hydroxylase inhibiting compound.
31 . The method of claim 23 , wherein R 1 is a heterocyclic ring that is unfused or fused with another ring.
32 . The method of claim 31 , wherein said heterocyclic ring contains one or two ring nitrogen atoms.
33 . The method of claim 23 , wherein R 2 is a carbocyclic ring that is unfused or fused with another ring.
34 . The method of claim 23 , wherein R 2 is selected from acyclic hydrocarbon groups R 5 containing up to twelve carbon atoms.
35 . The method of claim 34 , wherein said acyclic hydrocarbon groups are alkyl groups.
36 . The method of claim 34 , wherein said acyclic hydrocarbon groups contain up to six carbon atoms.
37 . The method of claim 23 , wherein R 6 and R 7 are independently selected from hydrogen atom and hydrocarbon groups containing up to three carbon atoms.
38 . The method of claim 23 , wherein R 3 is hydrogen.
39 . The method of claim 23 , wherein t is 1.Join the waitlist — get patent alerts
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