US2012022126A1PendingUtilityA1
Method Of Treating Diabetes Mellitus
Individually held — no corporate assignee on recordPriority: Nov 10, 2004Filed: Jul 29, 2011Published: Jan 26, 2012
Est. expiryNov 10, 2024(expired)· nominal 20-yr term from priority
A61P 43/00A61P 3/08A61P 3/10A61P 7/00A61K 31/40A61K 31/4025A61P 13/12A61K 31/395
49
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Claims
Abstract
The invention provides methods of treating a diabetic subject comprising administering a glucosylceramide synthase inhibitor to the subject.
Claims
exact text as granted — not AI-modified1 . A method of lowering blood glucose in a subject, the method comprising administering to the subject a therapeutically effective amount of a composition comprising a compound of Formula Ib, or a pharmaceutically acceptable salt thereof,
where R 1 is an optionally substituted aromatic ring or an optionally substituted heterocycle; R 2 is an optionally substituted alkyl group; and R 3 is an optionally substituted tertiary cyclic amine,
with the proviso that R 3 is not morpholine.
2 . The method of claim 1 , wherein R 1 is an optionally substituted aromatic ring.
3 . The method of claim 2 , wherein R 1 is an optionally substituted phenyl group.
4 . The method of claim 3 , wherein R 1 is an optionally substituted phenyl group; R 2 is an optionally substituted alkyl group; and R 3 is an optionally substituted tertiary cyclic amine.
5 . The method of claim 3 , wherein R 1 is a substituted phenyl group.
6 . The method of claim 5 , wherein R 1 is (3′,4′-ethylenedioxy)phenyl.
7 . The method of claim 1 , wherein R 3 is pyrrolidine.
8 . The method of claim 1 , wherein R 2 comprises at least 7 carbon atoms.
9 . The method of claim 8 , wherein R 2 is an optionally substituted C 7 -C 18 alkyl group.
10 . The method of claim 9 , wherein R 2 is an optionally substituted C 7 alkyl group.
11 . The method of claim 10 , wherein R 2 is chosen from 1-(1-hydroxyheptyl) and 1-(6-hydroxyheptyl).
12 . The method of claim 9 , wherein R 2 is an optionally substituted C 8 alkyl group.
13 . The method of claim 12 , wherein R 2 is chosen from 1-(1-hydroxyoctyl) and 1-(7-hydroxyoctyl).
14 . The method of claim 1 , wherein the compound of Formula Ib is in the form of a free base.
15 - 16 . (canceled)
17 . The method of claim 1 , wherein the compound of Formula Ib is a D-threo isomer;
wherein the compound of Formula Ib is an L-threo isomer; wherein the compound of Formula Ib is an L-erythro isomer; or wherein the compound of Formula Ib is a D-erythro isomer.
18 - 20 . (canceled)
21 . The method of claim 1 , wherein the compound of Formula Ib is a tartrate salt, and wherein R 1 is D-threo-(3′,4′-ethylenedioxy)phenyl, R 3 is pyrrolidine, and R 2 is a C 7 alkyl group.
22 . The method of claim 1 , wherein the compound of Formula Ib is a tartrate salt, and wherein R 1 is D-threo-(3′,4′-ethylenedioxy)phenyl, R 3 is pyrrolidine, and R 2 is a C 8 alkyl group.
23 - 27 . (canceled)
28 . The method of claim 1 , wherein the compound of Formula Ib is 1-(3′,4′-ethylenedioxy)phenyl-2-nonanoylamino-3-pyrrolidino-1-propanol.
29 . The method of claim 1 , wherein the compound of Formula Ib is 1-(3′,4′-ethylenedioxy)phenyl-2-octanoylamino-3-pyrrolidino-1-propanol.
30 . The method of claim 4 , wherein R 1 is a substituted phenyl group.
31 . The method of claim 30 , wherein the substituted phenyl group is (3′,4′-ethylenedioxy)phenyl.
32 . The method of claim 4 , wherein R 3 is pyrrolidine.
33 . The method of claim 4 , wherein R 2 comprises at least 7 carbon atoms.
34 . The method of claim 33 , wherein R 2 is a C 7 -C 18 alkyl group.
35 . The method of claim 34 , wherein the alkyl group is a C 7 alkyl group.
36 . The method of claim 33 , wherein R 2 is a C 8 alkyl group.
37 - 39 . (canceled)
40 . The method of claim 4 , wherein the compound is a D-threo isomer;
wherein the compound is a L-threo isomer; wherein the compound is a L-erythro isomer; or wherein the compound is a D-erythro isomer.
41 - 43 . (canceled)
44 . The method of claim 4 , wherein the compound is a tartrate salt and wherein R 1 is D-threo-(3′,4′-ethylenedioxy)phenyl, R 3 is pyrrolidine, and R 2 is a C 7 alkyl group.
45 . The method of claim 4 , wherein the compound is a tartrate salt, and wherein R 1 is D-threo-(3′,4′-ethylenedioxy)phenyl, R 3 is pyrrolidine, and R 2 is a C 8 alkyl group.
46 - 51 . (canceled)
52 . A method of improving glucose tolerance in a subject, the method comprising administering to the subject a therapeutically effective amount of a composition comprising a compound of Formula Ib, or a pharmaceutically acceptable salt thereof,
where R 1 is an optionally substituted aromatic ring or an optionally substituted heterocycle; R 2 is an optionally substituted alkyl group; and R 3 is an optionally substituted tertiary cyclic amine,
with the proviso that R 3 is not morpholine.
53 . A method of decreasing plasma TNF-α in a subject, the method comprising administering to the subject a therapeutically effective amount of a composition comprising a compound of Formula 1b, or a pharmaceutically acceptable salt thereof,
where R 1 is an optionally substituted aromatic ring or an optionally substituted heterocycle; R 2 is an optionally substituted alkyl group; and R 3 is an optionally substituted tertiary cyclic amine,
with the proviso that R 3 is not morpholine.
54 . A method of decreasing glycated hemoglobin levels in a subject, the method comprising administering to the subject a therapeutically effective amount of a composition comprising a compound of Formula 1b, or a pharmaceutically acceptable salt thereof,
where R 1 is an optionally substituted aromatic ring or an optionally substituted heterocycle; R 2 is an optionally substituted alkyl group; and R 3 is an optionally substituted tertiary cyclic amine,
with the proviso that R 3 is not morpholine.
55 . A method of treating a subject having renal hypertrophy or hyperplasia associated with diabetic nephropathy, the method comprising administering to the subject a therapeutically effective amount of a composition comprising a compound of Formula 1b, or a pharmaceutically acceptable salt thereof,
where R 1 is an optionally substituted aromatic ring or an optionally substituted heterocycle; R 2 is an optionally substituted alkyl group; and R 3 is an optionally substituted tertiary cyclic amine,
with the proviso that R 3 is not morpholine.
56 . (canceled)Join the waitlist — get patent alerts
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